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Spiro ring system

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514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514277000 - Hetero ring is six-membered consisting of one nitrogen and five carbon atoms

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Entries
DocumentTitleDate
20110201635SUBSTITUTED SPIROINDOLINONES - There is provided a compound of the formula08-18-2011
20120202837SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS - Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is —(C═O)—, —CH08-09-2012
20100160362SPIRO (FURO [3, 2-C] PYRIDINE-3-3' -INDOL) -2' (1'H)-ONE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF SODIUM-CHANNEL MEDIATED DISEASES, SUCH AS PAIN - This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein j, k, m, Q, X, R06-24-2010
20110195987TREATMENT WITH CHOLINERGIC AGONISTS - Methods of treating disorders with cholinergic agonists for example, muscarinic receptor agonists such as pilocarpine and cevimeline are provided. In particular, methods of treating and/or preventing interstitial cystitis, yeast infections, urinary tract infections, atrophic vaginitis, vaginal dryness, and sexual dysfunction associated with vaginal dryness by administering a cholinergic agonist to the subject suffering from the disorders are provided. In addition, intra-vaginal administration of cholinergic agonists such as muscarinic receptor agonists to patients suffering from interstitial cystitis, vaginal dryness, and sexual dysfunction associated with vaginal dryness is also provided.08-11-2011
20090270435Spiroketone Acetyl-CoA Carboxylase Inhibitors - The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R10-29-2009
20130210851Crystalline forms of a hexahydrofuro[3,4-c]quinoline derivative - The present invention relates to crystalline forms of (3R,9S)-4-isopropyl-7,7-dimethyl-3-(4-(trifluoromethyl)phenyl)-2′,3′,5′,6,6′,7,8,9-octahydro-3H-spiro[furo[3,4-c]quinoline-1,4′-pyran]-9-ol and its hydrochloride or hydrobromide salts, to a process for the manufacture thereof, and to the use thereof in pharmaceutical compositions.08-15-2013
20130210850Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation - The present invention relates to compounds defined by formula I08-15-2013
20100076004BICYCLIC SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE - The present invention is directed to bicyclic spiropiperidine compounds of formula (I)03-25-2010
201000760035-OXAZOLIDIN-2-ONE SUBSTITUTED 1,3,8-TRIAZASPIRO[4.5]DECAN-4-ONE DERIVATIVES USEFUL AS ORL-1 RECEPTOR MODULATORS - The present invention is directed to novel 5-oxazolidin-2-one substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives useful in the treatment of disorders and conditions mediated by the ORL-1 receptor. The present invention is further directed to processes for the preparation of said derivatives, pharmaceutical compositions comprising said derivatives and methods for the treatment of ORL-1 mediated disorders and conditions.03-25-2010
20120245191NEW AZASPIRODECANONE COMPOUNDS - The invention provides novel compounds having the general formula (I)09-27-2012
20090239890SPIRO SUBSTITUTED CYCLOPROPANE COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - A compound of the Formula I:09-24-2009
20090076049Novel Spiro [Imidazolidine-4, 3' -Indole] 2, 2', 5' (1H) Triones for Treatment of Conditions Associated with Vanilloid Receptor 1 - The present invention relates to new compounds of formula (I), wherein R03-19-2009
20130040978SPIRO ISOXAZOLINE COMPOUNDS AS SSTR5 ANTAGONISTS - Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.02-14-2013
20080287478Nociceptin Analogues and Uses Thereof - The present invention relates to nociceptin analogues and uses thereof to modulate biological functions. In one aspect, the invention provides modified triazo-spiro compounds that include at least one specialized chemical group that is bound to the compounds. The invention has a wide range of applications including providing a new class of therapeutically useful aquatics.11-20-2008
20100144775Heterocyclic Cyclopamine Analogs and Methods of Use Thereof - The present invention relates to steroidal alkaloids that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.06-10-2010
20100144774HETEROCYCLIC SPIRO-COMPOUNDS - The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R06-10-2010
20090156626Process for Preparing Spirocyclic Cyclohexane Compounds and Methods of Using Such Compounds - Spirocyclic cyclohexane compounds corresponding to formula I06-18-2009
20090156625 Novel Use of a Nicotinic Receptor Agonist 156 - The invention relates to a novel method of treatment or prophylaxis of osteoarthritis, which comprises administering to a patient in need thereof a therapeutically effective amount of an alpha 7 nicotinic AcetylCholine receptor agonist of Formula (I), or a pharmaceutically acceptable salt thereof:06-18-2009
20100105714Furanone Compounds and Methods of Making and Using The Same - The invention features compounds of the general Formula (I): (formula should be inserted here) Compounds of Formula (I) possess unexpectedly high affinity for Alk5 and/or Alk4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders.04-29-2010
20100105713GLYT1 Transporter Inhibitors and Uses Thereof in Treatment of Neurological and Neuropsychiatric Disorders - Compounds of formula (I) or a salt thereof are provided:04-29-2010
20120214832ISOFORM SELECTIVE PHOSPHOLIPASE D INHIBITORS - Disclosed are isoform selective Phospholipase D inhibitors. In one aspect, the disclosed compounds can have a structure represented by a formula (I): Also disclosed are methods of making and using the compounds. Also disclosed are pharmaceutical compositions and kits comprising the compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.08-23-2012
20090111841Novel 3,9-Diaza-Spiro[5,5]Undecane Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors - This invention relates to novel 3,9-diaza-spiro[5.5]undecane derivatives useful as monoamine neurotransmitter re-uptake inhibitors.04-30-2009
20090124648Synthesis and Crystalline Forms of Npy5 Antagonist - The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide and novel salts, hydrates and polymorphs thereof.05-14-2009
20100069420SPIRO-PIPERIDINE INHIBITORS - Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.03-18-2010
20110003839ANDROGEN RECEPTOR MODULATOR FOR THE TREATMENT OF PROSTATE CANCER AND ANDROGEN RECEPTOR-ASSOCIATED DISEASES - A hydantoin compound useful for the prevention or treatment of hyperproliferative diseases or disorders.01-06-2011
20100081680N-SULFONAMIDO POLYCYCLIC PYRAZOLYL COMPOUNDS - The current invention provides compounds having a structure according to Formulae 1, 2, 3, and 4:04-01-2010
20110009441IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel compounds, in particular novel imidazo[1,2-a]piridine derivatives according to Formula (I). The compounds according to the invention are positive allosteric modulators of metabotropic receptors-sub-type 2 (‘mGluR2’) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.01-13-2011
20090306118Trisubstituted Thiophenes as Progesterone Receptor Modulators - The present invention is directed to novel trisubstituted thiophene derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical usage of these compounds are related to hormonal contraception, the treatment and/or prevention of secondary dysmenorrhea, amenorrhea, dysfunctional uterine bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon or prostate. Additional uses of the invention include stimulation of food intake.12-10-2009
20130072511ANDROGEN RECEPTOR MODULATOR FOR THE TREATMENT OF PROSTATE CANCER AND ANDROGEN RECEPTOR-ASSOCIATED DISEASES - Described herein, inter alia, are compounds useful for the prevention or treatment of hyperproliferative diseases or disorders.03-21-2013
20130059874SUBSTITUTED N-PHENYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I).03-07-2013
20090270436SPIROCHROMANON DERIVATIVES - The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3: R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a machine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.10-29-2009
20110021550Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation - Compounds of formula (I) wherein the groups R1 to R8 have the meanings indicated in the description, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof have valuable pharmacological properties, which make them useful for the treatment of cardiovascular and related disorders.01-27-2011
20090233953ANTAGONISTS OF THE VANILLOID RECEPTOR SUBTYPE 1 (VR1) AND USES THEREOF - The present invention is directed to compounds of formula (I)09-17-2009
20090233952SUBSTITUTED CYCLOALKENE DERIVATIVE - [Object] To provide a substituted cycloalkene derivative having an action to suppress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-α, pharmacologically acceptable salts therefor, a medicament containing them as an active ingredient, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.09-17-2009
20120115895TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS - The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides Spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g., toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light emption (e.g., photoirritant contact dermatitis, photoallergy contact dermatitis, chronic actinic dermatitis), and myositis neurodegenerative disorders such as neuropatic pain and other diseases with an inflammatory component such as rheumatoid arthritis, multiple sclerosis, osteoarthritis, and inflammatory bowel disease (IBD).05-10-2012
20120238594AZASPIRODECANONE COMPOUNDS - The invention provides novel compounds having the general formula (I)09-20-2012
200802937564,4-DISUBSTITUTED PIPERIDINE DERIVATIVES - This invention relates to 4,4-disubstituted piperidine derivatives of the formula11-27-2008
20080293755HETEROCYCLIC CYCLOPAMINE ANALOGS AND METHODS OF USE THEREOF - The present invention relates to steroidal alkaloids that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.11-27-2008
20110294842SPIRO (FURO [3, 2-C] PYRIDINE-3-3' -INDOL) -2' (1'H)-ONE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF SODIUM-CHANNEL MEDIATED DISEASES, SUCH AS PAIN - This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein j, k, m, Q, X, R12-01-2011
20090209568Spiro [Benzopyran] or Spiro [Benzofuran] Derivatives Which Inhibit the Sigma Receptor - The present invention relates to compounds having pharmacological activity towards the sigma (σ) receptor, and more particularly to spiro[benzopyran] or spiro[benzofuran] derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.08-20-2009
20110281903BICYCLIC HETEROCYCLIC SPIRO COMPOUNDS - There are disclosed bicyclic heterocyclic spiro compounds; pharmaceutical compositions comprising these compounds; and methods for the treatment in a mammal of diseases and conditions which are susceptible to modulation of the M1 muscarinic receptor, including Alzheimer's disease, insulin resistance syndrome and type 2 diabetes. Other embodiments are also disclosed.11-17-2011
20130023551DISPIRO TETRAOXANE COMPOUNDS - A compound having the formula (I)01-24-2013
20080318991SPIROCYCLES AS INHIBITORS OF 11-BETA HYDROXYL STEROID DEHYDROGENASE TYPE 1 - The present invention relates to certain spirocyclic compounds that are inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 (11βHSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases.12-25-2008
20120289530COMBINATIONS OF TROSPIUM AND SALIVARY STIMULANTS FOR THE TREATMENT OF OVERACTIVE BLADDER - Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.11-15-2012
20090156624Methionine aminopeptidase-2 inhibitors and methods of use thereof - The present invention provides methods of parasitic infections, thymoma, and lymphoid malignancies in a subject by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.06-18-2009
20100292263CGRP RECEPTOR ANTAGONISTS WITH TERTIARY AMIDE, SULFONAMIDE, CARBAMITE AND UREA GROUPS - Compounds of formula I:11-18-2010
20120289531COMBINATIONS OF TROSPIUM AND SALIVARY STIMULANTS FOR THE TREATMENT OF OVERACTIVE BLADDER - Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.11-15-2012
20110021549SUBSTITUTED BENZOFUSED DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS - The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.01-27-2011
20110124672Thienyl Compounds - Compounds of formula I:05-26-2011
20110288111INHIBITION OF INFLUENZA M2 PROTON CHANNEL - Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.11-24-2011
20100222375Pharmaceutical Composition Comprising Trospium Chloride for Once-A-Day Administration - A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C09-02-2010
20090286822Treatment of psoriasis and of other skin disorders associated with inhibition of differentiation of epidermal cells - This invention concerns the use of cyclopamine, a naturally occurring steroidal alkaloid known for over thirty years, for the treatment of psoriasis and achievement of rapid clearance of the psoriatic skin lesions together with the reversion of the histopathological signs of disease to normalcy with no detectable side effects. The cyclopamine-induced clearance of psoriatic lesions from the skin of patients is associated with the causation of cellular differentiation in lesional epidermis and with the rapid disappearance of CD4(+) lymphocytes and other inflammatory cells from lesional skin. Therapeutic compositions comprising of cyclopamine and a corticosteroid and/or the pre-treatment of lesions with a corticosteroid provide significantly further increased therapeutic effectiveness over the use of cyclopamine alone or a corticosteroid alone.11-19-2009
20100305146Method for the Production of 1,3-Dioxolane-2-Ones and Carboxylic Acid Esters by Means of Transacylation in Basic Reaction Conditions - The invention relates to a method for producing 1,3-dioxolane-2-ones of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1 to R5 have the meanings indicated in the claims and the description. The invention further relates to a method for producing 2-hydroxy carboxylic acid esters of general formula (5) with or without isolation of the intermediate in the form of a derivative of the 1,3-dioxolane-2-one of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1, R2, and R6 have the meanings indicated in the claims and the description. The method according to the invention allows the reaction to take place in very gentle basic conditions, causing fewer secondary reactions and providing a greater yield than reactions in highly polar aprotic solvents. Acid-sensitive and/or temperature-sensitive compounds can be synthesized.12-02-2010
20100056553Cycloalkylamine substituted isoquinoline and isoquinolinone derivatives - The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I)03-04-2010
20090099222Modulators of muscarinic receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.04-16-2009
20090253727NOCICEPTIN ANALOGS - A compound of the having the general formula (I) or general formula (II):10-08-2009
20090318486Tricyclic spiro derivatives as CRTH2 modulators - The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.12-24-2009
20100035909NOVEL SUBSTITUTED DIAZA-SPIRO-PYRIDINONE DERIVATIVES FOR USE IN MCH-1 MEDIATED DISEASES - The present invention concerns aryl and heteroaryl substituted diaza-spiro-pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I)02-11-2010
20080293753Novel Compounds - The invention relates to quaternary α-aminocarboxyamide derivatives of formula (I), wherein R11-27-2008
20090062322Novel Tricyclic Spiropiperidines or Spiropyrrolidines - The invention provides compounds of formula (I)03-05-2009
20080306101Insecticidal Spironindane Derivatives - An insecticidal compound of formula I wherein X is O or NR12-11-2008
20100286181PYRROLE DERIVATIVES WITH ANTIBACTERIAL ACTIVITY - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.11-11-2010
20120065218Heterocyclic Cyclopamine Analogs and Methods of Use Thereof - The present invention relates to steroidal alkaloids that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.03-15-2012
20120035201SPIROHETEROCYCLIC PYRROLIDINE DIONE DERIVATIVES USED AS PESTICIDES - Compounds of the formula (I) wherein the substituents are as defined in claim 02-09-2012
20120035199SPIROHETEROCYCLIC COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiroheterocyclic compounds of formula (I):02-09-2012
20100249167ALKYLSULFONYL-2,3-DIHYDROSPIRO[INDENE-1,4'-PIPERIDINE] ANALOGS AS GLYT1 INHIBITORS, METHODS FOR MAKING SAME, AND USE OF SAME IN TREATING PSYCHIATRIC DISORDERS - In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.09-30-2010
20100120808SPIROCYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF THEIR USE - Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.05-13-2010
20100120809ARYL HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS - Compounds of formula I:05-13-2010
20100184795ASPARTATE OF 1-CYCLOPROPYL-6-FLUORO-7-(8-METHOXYIMINO-2,6-DIAZA-SPIRO[3.4]OCT-6-YL)-4-- OXO-1,4-DIHYDRO-[1,8]NAPHTHYRIDINE-3-CARBOXYLIC ACID, METHOD FOR PREPARING THE SAME, AND ANTIMICROBIAL PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Disclosed are aspartic acid salts of 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid, methods for preparing the same, and antimicrobial pharmaceutical compositions comprising the same.07-22-2010
20120108619N1/N2-LACTAM ACETYL-COA CARBOXYLASE INHIBITORS - The invention provides a compound of Formula (I)05-03-2012
20120108618THIA-TRIAZA-INDACENES - The present invention encompasses compounds of general formula (1) wherein R05-03-2012
20120295931SPIROINDOLINE COMPOUNDS FOR USE AS ANTHELMINTHICS - This invention relates to spiroindoline compounds for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.11-22-2012
20090275602Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I11-05-2009
20080207666Substituted pyrano[2,3-B]pyridine derivatives as cannabinoid-1 receptor modulators - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.08-28-2008
20090281133Heterocyclic antiviral compounds - This invention relates to piperidine derivatives of formula I wherein R11-12-2009
20090042921SPIROINDOLINE DERIVATIVES HAVING INSECTICIDAL PROPERTIES - An insecticidal compound of formula (I), wherein Y is a single bond, C═O, C═S or S(O)02-12-2009
20090203721USE OF SIRAMESINE IN THE TREATMENT OF CANCER - The present invention relates to the treatment of cancer. In particular, the invention provides pharmaceutical compositions comprising siramesine for the treatment of cancer. The invention further provides a method of treatment comprising administering siramesine to a patient suffering from cancer.08-13-2009
20100113493(PYRROLIDIN-2-YL)PHENYL DERIVATIVES - The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I05-06-2010
20110269788SPIRO-OXINDOLE-DERIVATIVES AS SODIUM CHANNEL BLOCKERS - This invention is directed to spiro-oxindole compounds of formulas (I), (II), (III), as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.11-03-2011
20080242689N-ARYL AZASPIROALKENE AND AZASPIROALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle).10-02-2008
20090170887Novel indazole derivative having spiro ring structure in side chain - An object of the present invention is to create a novel indazole derivative having a spiro ring structure in a side chain, which is useful as a pharmaceutical, and to find a new pharmacological activity of the derivative. The present invention compound is represented by the general formula [I] and has an excellent Rho kinase inhibitory activity. In the formula, the ring X represents a benzene ring or a pyridine ring; R07-02-2009
20080287479INHIBITORS OF SERINE PALMITOYLTRANSFERASE - This invention provides compounds of the formula:11-20-2008
20080306102NOVEL SPIROOXYINDOLE COMPOUNDS AND DRUGS CONTAINING SAME - A Spiro oxindole compound represented by formula (1) of the present invention or salt thereof, or their solvate shows a superior inhibitory effect of 11β-hydroxysteroid dehydrogenasel, and is useful as an agent for preventing or treating a disease that involves 11β-hydroxysteroid dehydrogenasel (in particular, diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome).12-11-2008
20080293754CYCLOPAMINE ANALOGS - The invention provides novel derivatives of cyclopamine having the following formula:11-27-2008
20080207664Once daily dosage forms of trospium - A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C08-28-2008
20080207661Once daily dosage forms of trospium - A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C08-28-2008
20080207662Once daily dosage forms of trospium - A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C08-28-2008
20080269272CYCLOPAMINE ANALOGUES AND METHODS OF USE THEREOF - The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.10-30-2008
20080269271Substituted Spiro Compounds and Their Use for Producing Pain-Relief Medicaments - The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.10-30-2008
20110269787Azabicyclic Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.11-03-2011
20090181997THERAPEUTIC CANCER TREATMENTS - The invention is directed to use of hedgehog inhibitors in conjunction with chemotherapy in treating cancers, and preventing relapses thereby.07-16-2009
20090131464SPIROCHROMANONE DERIVATIVES AS ACETYL COENZYME A CARBOXYLASE (ACC) INHIBITORS - The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.05-21-2009
20090163527Spiropiperidines for use as tryptase inhibitors - The present invention is directed to a compound of Formula (I):06-25-2009
20090118319Fused and Spirocycle Compounds and the Use Thereof - The invention relates to fused and spirocycle compounds of Formula (I), or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R05-07-2009
20090012109CYCLOPAMINE ANALOGS - The invention provides novel derivatives of cyclopamine having the following formula:01-08-2009
20090325992COMPOUND HAVING CYCLIC GROUP BOUND THERETO THROUGH SPIRO BINDING AND USE THEREOF - A compound represented by general formula (I):12-31-2009
20090325990ACYLATED SPIROPIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS - Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.12-31-2009
20090325993GLYT1 Transporter Inhibitors and Uses Thereof in Treatment of Neurological and Neuropsychiatric Disorders - Compounds of formula (I) or a salt thereof are provided:12-31-2009
20090325991Spirolactam Bicyclic CGRP Receptor Antagonists - Compounds of formula I:12-31-2009
20090197904Sulphamides for Treatment of Cancer - Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer.08-06-2009
20090099223METHODS OF TREATING HORMONE-RELATED CONDITIONS USING THIO-OXINDOLE DERIVATIVES - The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is:04-16-2009
20120289529COMBINATIONS OF TROSPIUM AND SALIVARY STIMULANTS FOR THE TREATMENT OF OVERACTIVE BLADDER - Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.11-15-2012
20090192182COMPOUND HAVING ACIDIC GROUP WHICH MAY BE PROTECTED, AND USE THEREOF - A compound represented by general formula (I):07-30-2009
20090105291Phenylalanine Enamide Derivatives - Phenylalanine enamide derivatives of formula (1) are described:04-23-2009
2009010528911beta-hydroxysteroid dehydrogenase type 1 active spiro compounds - A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11 β-hydroxy-Steroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.04-23-2009
20090082381Percutaneously Absorbable Ophthalmic Preparation - The present invention provides a percutaneously absorbable ophthalmic preparation that permits the retention of a therapeutically effective concentration of a heterocyclic spiro compound and a salt thereof for promoting lacrimation, and that produces less adverse reactions such as miosis. Specifically, the present invention provides a percutaneously absorbable ophthalmic preparation comprising as an active ingredient a heterocyclic spiro compound represented by the general formula (I):03-26-2009
20080318990SPIROINDOLINES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to a compound of the following formula:12-25-2008
20120077834Methods of Use of Cyclopamine Analogs - The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:03-29-2012
20090105290Substituted 1-oxa-3,8-diazaspiro[4.5]-decan-2-one-Compounds and the Use Thereof for Producing Drugs - The present invention relates to substituted 1-oxa-3,8-diazaspiro[4.5]-decan-2-one compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.04-23-2009
20090239889Spiroindolinone Derivatives - There are provided compounds of the general formulas09-24-2009
20090253726TRI-, TETRA-SUBSTITUTED-3-AMINOPYRROLIDINE DERIVATIVE - A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by formula (I):10-08-2009
20120035200GRISEOFULVIN ANALOGUES FOR THE TREATMENT OF CANCER BY INHIBITION OF CENTROSOMAL CLUSTERING - The invention relates to compounds of the formula (I), where the symbols have the meaning given in the specification, for use in a method for treating cancer, to use of these compounds for the manufacture of a pharmaceutical composition for the treatment of cancer, and to methods of treatment for said diseases employing a compound of formula (I).02-09-2012
201002738193,3'-Spiroindolinone Derivatives - There are provided compounds of the formula10-28-2010
20100273818INHIBITORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED THERETO - The present invention makes availables assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule.10-28-2010
20100197714SPIRO-PYRANO-PYRAZOLE DERIVATIVES - The present invention relates to compounds of formula (I) below having pharmacological activity towards the sigma (σ) receptor, and more particularly to spiro-pyrano-pyrazole compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.08-05-2010
20100184794FUSED HETEROCYCLIC COMPOUND - The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.07-22-2010
20110059998KIT, COMPOSITION, PRODUCT OR MEDICAMENT FOR TREATING COGNITIVE IMPAIRMENT - A kit, composition, product or medicament for treating cognitive impairment is provided, which includes a therapeutic agent for neurodegenerative disease and a heterocyclic compound represented by the following General Formula (I): or a hydrate thereof, a solvate thereof or a pharmaceutically acceptable salt thereof.03-10-2011
201002406881,3-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H,1 H-1,4 BIPYRIDINYL-2-ONES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I)09-23-2010
20100240689N-ARYL AZASPIROALKENE AND AZASPIROALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle).09-23-2010
20100137348PHARMACEUTICAL FORMULATIONS: SALTS OF 8-[-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE AND TREATMENT METHODS USING THE SAME - Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.06-03-2010
20100137349ANTIMICROBIAL OXAZOLIDINONE, HYDANTOIN AND IMIDAZOLIDINONE COMPOSITIONS - The present application relates to N-chlorinated oxazolidinone, hydantoin and imidazolidinone compounds of Formula I06-03-2010
20100222374SPIROCYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF THEIR USE - Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.09-02-2010
20110130417NEW AZACYCLIC DERIVATIVES - Compounds of formula (I)06-02-2011
20100197716N-LINKED HETEROCYCLIC ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS - The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I):08-05-2010
20100197715PIPERIDINE DERIVATIVES - The present invention relates to a compound of formula I08-05-2010
20090181996SUBSTITUTED QUINOLONES III - The invention relates to substituted quinolones and to methods for their preparation as well as to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, particularly against cytomegaloviruses.07-16-2009
20090111842SPIROCYCLIC CYCLOHEXANE COMPOUNDS WITH ANALGESIC ACTIVITY - Spirocyclic cyclohexane compounds corresponding to formula I04-30-2009
20090111840Heterocyclic spiro-compounds as aldosterone synthase inhibitors - The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R04-30-2009
20110046171ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS - This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.02-24-2011
20100280058SPIROCYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF THEIR USE - Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.11-04-2010
20090069362Novel Spiro-benzo[c]chromene derivatives useful as modulators of the estrogen receptors - The present invention is directed to novel spiro-benzo[C]chromene derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.03-12-2009
201003313533,9-DIAZASPIRO[5,5]UNDECANE AMIDES AND UREAS AND METHODS OF USE THEREOF - Compounds of formula (I)12-30-2010
20110009440GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS - Compounds of formula (I) or a salt thereof are provided:01-13-2011
20090186914Phenylalanine Enamide Derivatives - Phenylalanine enamide derivatives of formula (1) are described:07-23-2009
20110009443Pyrazolospiroketone Acetyl-Coa Carboxylase Inhibitors - The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R01-13-2011
20110015220MIXED ORL1/MU-AGONISTS FOR THE TREATMENT OF PAIN - The invention relates to the use of compounds which exhibit an affinity for the μ-opioid receptor of at least 100 nM (K01-20-2011
20110245286TREATMENT OF INFLAMMATION USING ALPHA 7 RECEPTOR-BINDING AGONISTS - Methods of inhibiting release of a proinflammatory cytokine from a macrophage are provided. The methods comprise treating the macrophage with a cholinergic agonist in an amount sufficient to decrease the amount of the proinflammatory cytokine that is released from the macrophage, wherein the cholinergic agonist is selective for an α7 nicotinic receptor. Methods for inhibiting an inflammatory cytokine cascade in a patient are also provided. The methods comprise treating the patient with a cholinergic agonist in an amount sufficient to inhibit the inflammatory cytokine cascade, wherein the cholinergic agonist is selective for an α7 nicotinic receptor. Methods for determining whether a compound is a cholinergic agonist reactive with an α7 nicotinic receptor are also provided. The methods comprise determining whether the compound inhibits release of a proinflammatory cytokine from a mammalian cell. Additionally, methods for determining whether a compound is a cholinergic antagonist reactive with an α7 nicotinic receptor are provided. These methods comprise determining whether the compound reduces the ability of a cholinergic agonist to inhibit the release of a proinflammatory cytokine from a mammalian cell. Oligonucleotides or mimetics capable of inhibiting attenuation of lipopolysaccharide-induced TNF release from a mammalian macrophage upon exposure of the macrophage to a cholinergic agonist are also provided. The oligonucleotides or mimetics consist essentially of a sequence greater than 5 nucleotides long that is complementary to an mRNA of an α7 receptor. Additionally, methods of inhibiting attenuation of TNF release from a mammalian macrophage upon exposure of the macrophage to a cholinergic agonist are provided. These methods comprise treating the macrophage with the above-described oligonucleotide or mimetic.10-06-2011
20110034500SPIROHETEROCYCLIC COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiroheterocyclic compounds of formula (I):02-10-2011
20130150394PESTICIDAL COMPOSITIONS - A pesticidal composition comprising a pesticidal effective amount of at least one compound of formula (I) in which the substituents are as defined as in claim 06-13-2013
20110039874MONOACYLGLYCEROL LIPASE INHIBITORS FOR MODULATION OF CANNABINOID ACTIVITY - Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.02-17-2011
20110124671SPIROINDENES AND SPIROINDANES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to a compound of the following formula:05-26-2011
20090298861Novel tricyclic spiroderivatives as modulators of chemokine receptor activity - The invention provides compounds of formula (I) wherein m, R12-03-2009
20090312356NICOTINIC AGONISTS SELECTIVE FOR THE ALPHA7 RECEPTOR SUBTYPE, THE PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS THEREFROM - The invention discloses compounds of formula I endowed with agonistic activity at the alpha7 nicotinic acetylcholine receptors (α7 nAChRs), a process for the preparation thereof, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric disorders as well as inflammatory diseases.12-17-2009
20100069419SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE - The present invention is directed to spiropiperidine compounds of formula (I)03-18-2010
20120245190AUTOPHAGY INDUCING COMPOUND AND THE USES THEREOF - The present invention relates to a composition comprising compounds of formula (I-V),09-27-2012
20100048599Compounds As Kinase Inhibitors - The present invention relates to compounds of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.02-25-2010
20090215807Novel Diazaspiroalkanes and Their Use for Treatment of CCR8 Mediated Diseases - The invention provides compounds of general formula. [Chemical formula should be inserted here. Please see paper copy] (II) wherein R and R08-27-2009
20110251225SUBSTITUTED TETRAHYDROPYRAN SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I):10-13-2011
20110098316CHROMANE DERIVATIVES AS TRPV3 MODULATORS - The present invention provides chromane derivatives as transient receptor potential vanilloid (TRPV) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.04-28-2011
20110105546SPIROTROPANE COMPOUNDS - Compounds according to formula (I):05-05-2011
20110077262NOVEL SPIROCHROMANONE CARBOXYLIC ACIDS - The invention relates to a compound of a general formula (I): wherein A represents a linking group; Ar03-31-2011
20110071179MACROCYCLIC INHIBITORS OF JAK - The present invention relates to the use of novel macrocyclic compounds of Formula I,03-24-2011
20110071178Methods and Compounds for Modulating Cannabinoid Activity - Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.03-24-2011
20110071180SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES - The present invention relates to compounds of the following formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).03-24-2011
20110251224SPIRO-OXINDOLE COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds of formula (I):10-13-2011
20110034498DOSING REGIMENS FOR THE TREATMENT OF CANCER - The invention relates to a method of treating cancer. The method includes administering systemically a therapeutically effective amount of a small molecule hedgehog pathway inhibitor, such that the concentration of the inhibitor in the blood does not vary by more than about ±30% from the average concentration, and such that the concentration remains at or below the maximum tolerated dose of the inhibitor for a time period of at least about one day.02-10-2011
200802491221,3,8-TRISUBSTITUTED-1,3,8-TRIAZA-SPIRO[4.5]DECAN-4-ONE DERIVATIVES AS LIGANDS OF THE ORL-1 RECEPTOR - The present invention is directed to novel 1,3,8-trisubstituted-1,3,8-triaza-spiro[4.5]decan-4-one derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor.10-09-2008
20100280057NOVEL ANALGESIC THAT BINDS FILAMIN A - A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula I, wherein R11-04-2010
20110251226CYCLOHEXYLAMIN ISOQUINOLONE DERIVATIVES - The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I)10-13-2011
20110160238OCTAHYDROQUINOLIZINES FOR ANTIDIABETIC TREATMENT - This invention relates to octahydroquinolizines for pharmaceutical use with the following formula: (I), X=H, F; R=Methyl, Ethyl, nPropyl, nButyl.06-30-2011
20120122910METHOD OF TREATING CANCER USING A SURVIVIN INHIBITOR - Disclosed herein are methods of treating cancer by administering to a patient a small molecule inhibitor of Survivin. Also disclosed herein are methods of inhibiting Survivin dimerization in a patient by administering a compound of formula (I), (II), (III), or (IV). Methods of inducing cell cycle arrest in cancer cells, comprising G2/M stage arrest, in a patient by administering a compound of formula (I), (II), (III), or (IV) are also disclosed. Further disclosed herein are methods of inducing apoptosis in cancer cells in a patient by administering a compound of formula (I), (II), (III), or (IV).05-17-2012
20110152304SPIROAZAINDOLES - The present invention relates to spiroazaindole compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.06-23-2011
20090247560Diaryl ketimine derivative - Provided is a compound of a formula (I):10-01-2009
20090247561SUBSTITUTED SPIROCYCLIC CYCLOHEXANE DERIVATIVES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.10-01-2009
20120122912NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.05-17-2012
20090124649AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLOPROTEASES - The present invention provides a compound of Formula I or Formula II:05-14-2009
20090118318Novel Diazaspiroalkanes and Their Use for Treatment of CCR8 Mediated Diseases - The invention provides compounds of general formula wherein R and R05-07-2009
20090036477Novel 3-Aza-Spiro[5,5]Undec-8-Ene Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors - This invention relates to novel 3-aza-spiro[5.5]undec-8-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors.02-05-2009
20100029702Method For Identification of Compound Having Anti-Anxiety Effect - There are provided a method for identifying a compound having an anti-anxiety effect, an inhibitor of a function of a protein having a function as a G-protein coupled receptor, characterized by finding the protein and a gene encoding the protein and using at least one of a DNA represented by the nucleotide sequence of this gene or a complementary strand thereof, a homologue of the DNA, a protein encoded by the DNA, and a cell expressing the protein encoded by the DNA, an agent and a method for improving an anxiety condition, a method and an agent for prophylactic and/or therapeutic treatment of an anxiety disorder, and a measurement method for diagnosis and a diagnostic method of an anxiety disorder.02-04-2010
20080214591N-Aryl Diazaspirocyclic Compounds and Methods of Preparation and Use Thereof - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle).09-04-2008
20110053969NOVEL DIAZASIPIROAKANES AND THEIR USE FOR TREATMENT OF CCR8 MEDIATED DISEASES - The invention provides compounds of general formula. (II) wherein R and 03-03-2011
20110053970Spirocyclic Cyclohexane Compounds Useful To Treat Substance Dependency - Spirocyclic cyclohexane compounds useful in pharmaceutical compositions for use in the treatment of substance dependency.03-03-2011
20100286182HYDRAZIDE COMPOUNDS AS THYROID HORMONE RECEPTOR MODULATORS AND USES THEREOF - A method of identification of compounds that modulate thyroid hormone activity, and the use of such compounds and compositions thereof for such purposes are disclosed. The compounds may be selected from the group consisting of:11-11-2010
20100286180METHODS OF USE OF CYCLOPAMINE ANALOGS - The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:11-11-2010
20100286183SPIROHYDANTOIN COMPOUNDS AND METHODS FOR THE MODULATION OF CHEMOKINE RECEPTOR ACTIVITY - Novel compounds represented by formula (I):11-11-2010
20110257213SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I).10-20-2011
20110257212NEW AZACYCLIC DERIVATIVES - The invention provides novel compounds having the general formula (I)10-20-2011
20110136843Novel Combination of Compounds to be Used in the Treatment of Airway Diseases, Especially Chronic Obstructive Pulmonary Disease (COPD) and Asthma - The present invention relates to a combination of (a) a chemokine receptor 1 (CCR1) antagonist and (b) a muscarinic antagonist. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treatment of airway diseases, such as chronic obstructive pulmonary disease (COPD) and asthma in mammals by administrating said combination. The invention further relates to a kit comprising the combination and use of said kit in treatment of airway diseases.06-09-2011
20110015219(+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof - The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as a method for identifying (+)-morphinans that may be therapeutically effective by determining whether the (+)-morphinan inhibits the activation of TLR9. Also provided are methods of using the (+)-morphinans comprising TLR9 antagonist activity to treat conditions such as traumatic pain, neuropathic pain, inflammatory disorders, acetaminophen toxicity, autoimmune disorders, neurodegenerative disorders, and cancer.01-20-2011
20100168145FUSED IMIDAZOLE DERIVATIVES AND USE THEREOF AS ALDOSTERONE SYNTHASE INHIBITORS - The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R07-01-2010
20110034499SPIROINDOLINES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to a compound of the following formula:02-10-2011
20110136845(+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof - The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain.06-09-2011
20110136844METHODS FOR INHIBITING DYRK1A TO TREAT CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS - Compositions and methods for treating, preventing and/or delaying the onset and/or the development of diseases and disorders of the central nervous system are disclosed. The present disclosure relates to indoloquinoline compounds that are capable of inhibiting at least one protein kinase, and to methods for preparing and uses of such compounds. The compounds described herein are administered to patients to achieve a therapeutic effect.06-09-2011
20110178112PPAR Modulators - 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections.07-21-2011
20110190330SPIROCYCLIC GPR40 MODULATORS - The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I′A or I′B:08-04-2011
20090176815Novel Tricyclic Spiropiperidine Compounds, Their Synthesis and Their Uses as Modulators of Chemokine Receptor Activity - Compounds of formula (I) wherein R07-09-2009
20100190814SPIROINDOLINONE DERIVATIVE PRODRUGS - There are provided compounds of the formula07-29-2010
20110190329NON-AMIDIC LINKERS WITH BRANCHED TERMINI AS CGRP RECEPTOR ANTAGONISTS - The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.08-04-2011
201000297001-(2-ARYL-2-OXOETHYL)-3-PHENYL-1, 4-DIAZASPIRO [4.5]DEC-3-EN-2-ONE DERIVATIVES AND THEIR USE AS GLYCINE TRANSPORTER INHIBITORS - Novel acetophenone compounds of formula (I), compositions containing (I), processes for the preparation of (I), and use of (I) as inhibitors of the glycine transporter, are provided.02-04-2010
20100029701MACROCYCLIC SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE - The present invention is directed to compounds of formula (I)02-04-2010
20100022571SUBSTITUTED PYRAZOLO [3,4-B]PYRIDINES AS PHOSPHODIESTERASE INHIBITORS - The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV.01-28-2010
20100210674Spiroindolinone Derivatives - There are provided compounds of the formula08-19-2010
20110009442METHODS FOR STEREOSELECTIVE REDUCTION - The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of β ketone product and α ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.01-13-2011
20110112128METHOD OF TREATING ILEUS BY PHARMACOLOGICAL ACTIVATION OF CHOLINERGIC RECEPTORS - A method of treating ileus in a subject by administering to the subject an effective amount of a pharmacological agent that increases the activity of cholinergic receptor in a subject. Examples of pharmacological agents are brain muscarinic agonist, cholinergic agonist or cholinesterase inhibitor. The methods of the present invention can be used to treat ileus caused by abdominal surgery, or administration of narcotics or chemotherapeutic agents such as during cancer chemotherapy.05-12-2011
20120041013NEW AZACYCLIC COMPOUNDS - The invention provides novel compounds having the general formula (I)02-16-2012
20090253725ACETYL CoA CARBOXYLASE INHIBITORS - The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula10-08-2009
20080280933BENZIMIDAZOLYL COMPOUNDS - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I11-13-2008
20080200492METHODS FOR THE TREATMENT OF ALCOHOL ABUSE, ADDICTION AND DEPENDENCY - The present invention is directed to methods for the treatment of alcohol abuse, addiction and/or dependency, alone and in combination with one or more anti-addiction agents.08-21-2008
20080306103METHODS AND COMPOSITIONS FOR TREATMENT OF CENTRAL AND PERIPHERAL NERVOUS SYSTEM DISORDERS AND NOVEL COMPOUNDS USEFUL THEREFOR - There are provided methods for the treatment of diseases involving dysfunction of the peripheral and central nervous system comprising administering one or more spiro compounds. Also provided are pharmaceutical compositions useful in such methods, compounds for use in the preparation of such pharmaceutical compositions, processes for preparing compounds useful in the practice of such methods, and some novel such compounds per se.12-11-2008
20100298368ANTAGONISTS OF PGD2 RECEPTORS - Described herein are compounds and pharmaceutical compositions containing such compounds that modulate the PGD11-25-2010
20120010229THERAPEUTIC REGIMENS FOR HEDGEHOG-ASSOCIATED CANCERS - Provided herein are methods, therapeutic regimens, and kits that optimize the benefits of hedgehog inhibition for cancer therapy.01-12-2012
20120010230METHODS AND COMPOSITIONS FOR IDENTIFICATION, ASSESSMENT AND TREATMENT OF CANCERS ASSOCIATED WITH HEDGEHOG SIGNALING - Provided herein are methods, assays and kits for evaluating a sample, e.g., a sample obtained from a cancer patient, to detect one or more hedgehog biomarkers and/or one or more cilium markers. Thus, the invention can be used, inter alia, as a means to identify patients likely to benefit from administration of one or more hedgehog inhibitors, alone or in combination with therapeutic agents; to predict a time course of disease or a probability of a significant event in the disease of a cancer patient; to stratify patient populations; and/or to more effectively treat or prevent a cancer or a tumor associated with hedgehog signaling.01-12-2012
20120010228D2 ANTAGONISTS, METHODS OF SYNTHESIS AND METHODS OF USE - Provided are D01-12-2012
20120015970NEW AZACYCLIC COMPOUNDS - The invention provides novel compounds having the general formula (I)01-19-2012
20120065219SPIROCYCLIC AZAADAMANTANE DERIVATIVES AND METHODS OF USE - The invention relates to compounds that are spirocyclic azaadamantane derivatives, particularly spirocyclic azaadamantanyl ether or amine derivatives, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.03-15-2012
20100190813SPIRO [PIPERIDINE-4- 4' -THIENO [3,2-C] PYRAN] DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE SIGMA RECEPTOR FOR THE TREATMENT OF PSYCHOSIS - The present invention relates to compounds having pharmacological activity towards the sigma (σ) receptor, and more particularly to some thieno-pyrano-pyrazole derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis or pain.07-29-2010
20120122911PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.05-17-2012
20120071499Substituted Spiro[3H-Indole-3,6'(5'H)-[1H]Pyrrolo[1,2c]Imidazole-1',2(1H,2'H)-diones - There are provided compounds of the formula03-22-2012
20110092531Novel Spiropiperidine Compounds - A compound of the formula:04-21-2011
20110092530Cyclopamine tartrate salt and uses thereof - The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides highly water-soluble analogs of cyclopamine that are potent, hedgehog signaling inhibitors less toxic than cyclopamine. The compounds of the present invention are particularly useful in treating cancers associated with hedgehog signalling.04-21-2011
201100925291,2,4-Triazole Derivatives and Their Use as Oxytocin Antagonists - The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).04-21-2011
20120309778Fused and Spirocycle Compounds and the Use Thereof - The invention relates to fused and spirocycle compounds of Formula (I), or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R12-06-2012
20110105549BRANCHED 3- AND 6-SUBSTITUTED QUINOLINES AS CGRP RECEPTORS ANTAGONISTS - The present invention is directed to novel branched 3- and 6-substituted quinoline derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.05-05-2011
20110105547FILAMIN A-BINDING ANTI-INFLAMMATORY ANALGESIC - A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within.05-05-2011
20110105548N-ARYL DIAZASPIROCYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle).05-05-2011
20100093777SPIRO-RING COMPOUND - The present invention aims to provide a compound having an acetyl-CoA carboxylase (ACC) inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy.04-15-2010
20120122909SPIRO-OXINDOLE COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds of formula (I):05-17-2012
20100267756PHARMACEUTICAL PREPARATION FOR TREATING DEMYELINATING DISEASES OF THE NERVOUS SYSTEM; PREPARATION PROMOTING RESTORATION OF THE MYELIN SHEATH OF NERVE FIBERS; AND A METHOD FOR TREATING DEMYELINATING DISEASES OF THE NERVOUS SYSTEM - The invention relates to a pharmaceutical remedy used to treat demyelinating diseases of the nervous system, said remedy containing stephaglabrin sulfate that contributes to the restoration of the myelin sheath of nerve fibers, and to a method for treating demyelinating diseases of the nervous system.10-21-2010
20120258979SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I).10-11-2012
20120165356SPIROCYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF THEIR USE - Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.06-28-2012
20100173925OXYINDOLE DERIVATIVES - This invention relates to compounds of the formula (I):07-08-2010
20100048600NOVEL BENZIMIDAZOLE DERIVATIVES - The present invention relates to a compound of the formula (I):02-25-2010
20100048601HYDROCHLORIDE SALTS OF 8-[-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one AND PREPARATION PROCESS THEREFOR - Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-S[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.02-25-2010
20080207663Once daily dosage forms of trospium - A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C08-28-2008
20100022572NOVEL SPIRO COMPOUND AND MEDICINE COMPRISING THE SAME - It is to provide a novel compound useful for preventing and/or treating diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome.01-28-2010
20090036478Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I02-05-2009
20120220616NOVEL SPIROPIPERIDINE COMPOUNDS - A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.08-30-2012
20120225900N2-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS - The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R09-06-2012
20120190701RENIN INHIBITORS - Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R07-26-2012
20100022573INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.01-28-2010
20120270893SUBSTITUTED ACETYL-COA CARBOXYLASE INHIBITORS - The invention provides a compound of Formula (I)10-25-2012
20110230509METHODS OF USE FOR CYCLOPAMINE ANALOGS - The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:09-22-2011
20100234410HYDRATE FOR MEDICAL PURPOSES - The present invention relates to [7-[(7S)-7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hemihydrate. This hemihydrate is stable and easy to prepare, and has excellent properties for a pharmaceutical bulk powder.09-16-2010
20100234409Amino cyclopentyl heterocyclic and carbocyclic modulators of chemokine receptor activity - Compounds of the formulae (I) and (II): (wherein Q, X, E, G09-16-2010
20100234411New Combination for the Treatment of Respiratory Diseases - The present invention relates to novel pharmaceutical compositions based on telmisartan 1 and anticholinergics 2 processes for preparing them and their use for the treatment of respiratory diseases.09-16-2010
20100204257SPIROINDOLINONE PYRIDINE DERIVATIVES - There are provided compounds of the formula08-12-2010
20110306626IMIDAZOLINONE DERIVATIVES AS CGRP RECEPTOR ANTAGONISTS - The present invention is directed to imidazolinone derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.12-15-2011
20100168146Composition Comprising (R)-Spiro[L-Azabicyclo[2.2.2]Octane-3,2'(3'H)-Furo[2,3-B]Pyridine (AZD0328) and its Use in the Treatment of Alzheimer's Disease, ADHD or Cognitive Dysfunction - A pharmaceutical composition comprising (R)-spiro[1-azabicyclo[2.2.2]octane-3,2′(3′H)-furo[2,3-b]pyridine (AZD0328) and its use in the treatment of subjects suffering from schizophrenia, Alzheimer's disease or other conditions with impaired cognitive function.07-01-2010
20130018068SPIROCYCLES AS INHIBITORS OF 11-BETA HYDROXYL STEROID DEHYDROGENASE TYPE 1 - The present invention relates to certain spirocyclic compounds that are inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 (11βHSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases.01-17-2013
20130018067POLYCYCLIC PYRROLIDINE-2,5-DIONE DERIVATIVES AS -FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS - The present invention relates to novel polycyclic pyrrolidine-2,5-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.01-17-2013
20080255174Hydroalcoholic Extract Of Erythrina Mulungu, Pharmaceutical Compositions And Processes For Producing These Substances - The use of molecules for cholinergic and/or serotonergic system models, revealing pharmaceutical compositions comprising 11-OH-erythravine, erythravine, erythrartine, pharmaceutically acceptable isotherals, salts, byproducts and/or solvates thereof, optionally containing other erythrina byproducts, for the treatment of anxiety disorders; processes for obtaining said pharmaceutical compositions are also revealed.10-16-2008
20130172379Combined Acetylcholinesterase Inhibitor and Quaternary Ammonium Antimuscarinic Therapy to Alter Progression of Cognitive Diseases - A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.07-04-2013
20080242688Method 741 - Methods of treatment and pharmaceutical compositions for providing improved cognition in subjects suffering from schizophrenia, Alzheimer's disease or other conditions with impaired cognitive function.10-02-2008
20080234305Novel Tetrahydropyridine Derivatives - The invention relates to novel tetrahydropyridine derivatives and use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin. (I) wherein X and Y represent independently hydrogen, fluorine or a methyl group; X and Y do not represent both hydrogen at the same time or X and Y may together form a cyclopropyl ring; W represents a phenyl or a heteroaryl, the heteroaryl ring being a six-membered and non-fused ring, the phenyl ring and the heteroaryl are substituted with V in position 3 or 4; A and B independently represent —O—; —S—; —SO— or —SO09-25-2008
20080227801Pharmaceutical Compositions Containing Erythrina Mulungu Derivatives, Processes for their Production and Uses Thereof - The present invention provides the use of molecules for cholinergic serotonergic and/or gabaergic system models, revealing pharmaceutical compositions comprising 11-OH-erythravine, erythravine, erythrartine, pharmaceutically acceptable isotherals, salts, byproducts and/or solvates thereof, optionally containing other Erythrine byproducts, for the treatment of anxiety disorders; processes for obtaining said pharmaceutical compositions are also revealed.09-18-2008
20110263629AMIDES OF DIAZABICYCLOOCTANES AND USES THEREOF - The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).10-27-2011
20130116270NOVEL COMPOUNDS - The invention relates to novel spirocyclic derivatives with affinity for Ca.,2.2 calcium channels and which are capable of interfering with Ca05-09-2013
20080207665Alpha-(Aryl-or Heteroaryl-Methyl)-Beta-Piperidinopropanoic Acid Compounds as Orl-1-Receptor Antagonists - This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester or salt thereof, wherein R08-28-2008
200802004911,2-Dihydro-Spiro[3H-Indole-3,4'-Piperidine] Compounds, as Modulators of the Mas Receptor Novel - The present invention relates to certain 1,2-dihydro-spiro[3H-indole-3,4′-piperidine]compounds of Formula (Ia): and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein G, R1, R2, R3, R4, R5, and Ar are as disclosed herein (“Compound(s) of the Invention”), which are useful, for example, as cardio-protective and/or neuro-protective agents. The invention also provides pharmaceutical compositions comprising a Compound of the Invention and methods for treating, preventing and/or managing a vascular, cardiovascular or neurological disease or disorder, comprising administering to a patient in need thereof a Compound of the Invention.08-21-2008
20080200490Alpha-(Aryl-or Heteroaryl-Methyl)-Beta-Piperidino Propanamide Compounds as Orl-1-Receptor Antagonists - This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R08-21-2008
20110212984USE OF (3R)-4--3-(4-CHLOROPHENYL) BUTANOIC ACID FOR TREATING URINARY INCONTINENCE - Use of (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl) butanoic acid for treating urinary incontinence is disclosed.09-01-2011
20090131465Synthesis and crystalline forms of melanocortin-4 receptor agonist - The present invention relates to a process for producing crystalline N-[1-((3R)-1′-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-yl]carbonyl}-6-chloro-5-methyl-2,3-dihydrospiro[indene-1,4′-piperidine]-3-yl)-1-methylethyl]acetamide, and novel salts, solvates, hydrates and polymorphs thereof.05-21-2009
20110251223CGRP Receptor Antagonists - The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).10-13-2011
201102756563H-Imidazo [4, 5-C] Pyridine- 6 -Carboxamides As Anti-Inflammatory Agents - There are provided compounds of formula (I), wherein R11-10-2011
20110275657MELANOCORTIN RECEPTOR MODULATORS, PROCESS FOR PREPARING THEM AND USE THERE IN HUMAN MEDICINE AND COSMETICS - Melanocortin receptor modulators, processes for preparing them and use thereof in human medicine and cosmetics are described. Melanocortin receptor modulators corresponding to formula (I):11-10-2011
20130123291BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS - Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; R05-16-2013
20110312986Composition and Method for Treating Overactive Bladder - The present specification discloses compounds, compositions including such compounds, kits including such compounds and compositions, and methods of treating an individual suffering from overactive bladder and/or diabetes by administering such compounds or compositions to an individual in need thereof.12-22-2011
20110319440Process for Preparing Spirocyclic Cyclohexane Compounds, Compositions Containing Such Compounds and Method of Using Such Compounds - Spirocyclic cyclohexane compounds corresponding to formula I12-29-2011
20120029006Cis-tetrahydro-spiro(cyclohexane-1,1'-pyrido[3,4-b]indole)-4-amine Compounds - Cis-tetrahydro-spiro(cyclohexane-1,1′-pyrido[3,4-b]indole)-4-amine compounds which act on the nociceptin/ORL-1 receptor system as well as on the μ-opioid receptor system and which are distinguished in particular by selective effectiveness in the treatment of chronic pain, such as inflammatory pain, visceral pain, tumour pain, and neuropathic pain, without at the same time developing pronounced effectiveness against acute, nociceptive pain.02-02-2012
20120029005SPIPERONE DERIVATIVES AND METHODS OF TREATING DISORDERS - Described herein are spiperone derivative compounds which have been found to be useful in methods of stimulating CaCC and treating disorders (or symptoms thereof) associated with CaCC including cystic fibrosis, wherein a compound of the invention is administered to a subject.02-02-2012
201301970191',3'-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H,1'H-[1,4']BIPYRIDINYL-2- '-ONES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I)08-01-2013
20130203793Protection and Treatment Against Influenza Infection - Method and composition for protection and treatment against influenza viral infection by modulating the activity of at least one essential host signaling pathways, including the Hedgehog (Hh), the Bone Morphogenetic Protein (BMP), the Notch (N) signaling pathways or combinations thereof, which activity is altered by the viral protein NS1. The method and composition comprise use of a compound that modulates at least one of these essential host signaling pathways for preventing or controlling symptoms associated with influenza viral infection. The method or composition can also be used either alone or in combination with other therapeutic agents for treating or protecting against influenza infection, and associated syndromes.08-08-2013
20130203794COMPOUNDS AND METHODS FOR THE PREVENTION AND TREATMENT OF CANCER - The present invention relates to compounds for modulating sonic hedgehog signaling and preventing or treating cancer.08-08-2013
20120088785NEW USES FOR QUATERNARY AMMONIUM ANTICHOLINERGIC MUSCARINIC RECEPTOR ANTAGONISTS IN PATIENTS BEING TREATED FOR COGNITIVE IMPAIRMENT OR ACUTE DELIRIUM - A method for treating the adverse effects of acetyl-cholinesterase inhibitors used in the treatment of cognitive disorders such as acute delirium and cognitive impairment in elderly human patients. The administration of a clinically effective amount of a quaternary ammonium anti-cholinergic muscarinic receptor antagonist having very low lipid solubility substantially eliminates the adverse effects of urinary and/or fecal incontinence, nausea, bradycardia, bronchorrhea or brochospasm caused by the acetyl-cholinesterase inhibitors, without affecting the beneficial activity of the acetyl-cholinesterase inhibitors. This permits the administration of the optimum effective dosing of acetyl-cholinesterase inhibitors to provide maximum benefit to the patient with the added benefit of reducing or eliminating the unwanted side effects of fecal and urinary incontinence. Further, the combination of rivastigmine and glycopyrrolate has been effective in significantly improving cognitive function in patients suffering from acute dementia or cognitive impairment.04-12-2012

Patent applications in class Spiro ring system