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The additional ring is a six-membered hetero ring consisting of one nitrogen and five carbon atoms

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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

514315000 - Piperidines

514317000 - Additional ring containing

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Entries
DocumentTitleDate
20100063091RENIN INHIBITORS - The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency.03-11-2010
20130072524Compositions And Methods Of Synthesis Of Pyridinolypiperidine 5-HT1F Agonists - The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).03-21-2013
20100137368PYRIDINE DERIVATIVES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS - The present invention relates to (1-benzyl-piperidin-4-yl)-(pyridin-2-yl)-amines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.06-03-2010
20110195993PPAR AGONIST COMPOUNDS, PREPARATION AND USES - The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them.08-11-2011
20130085160NOVEL BENZAMIDE DERIVATIVES - The present invention provides a novel benzamide derivative or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a 5-HT04-04-2013
20130085161PIPERIDINYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES - The invention relates to new derivatives of formula (I),04-04-2013
20100048625PIPERIDINE GPCR AGONISTS - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.02-25-2010
20100076021Organic Compounds - The present invention provides a compound of formula (I):03-25-2010
20130079369METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY - The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.03-28-2013
20120264781METHOD FOR THE TREATMENT, ALLEVIATION OF SYMPTOMS OF, RELIEVING, IMPROVING AND PREVENTING A COGNITIVE DISEASE, DISORDER OR CONDITION - The present invention provides uses of a salt adduct comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, for the preparation of a medicament for the treatment, alleviation of symptoms of relieving, improving and preventing a cognitive disease, disorder or condition in a subject. Additionally, the invention provides use of said salt adducts for the preparation of medicaments for the improvement of cognitive functions in a healthy subject.10-18-2012
20120264780SOLID COMPOSITIONS - The present invention features solid compositions comprising Compound I10-18-2012
20100041702BENZIMIDAZOLE CANNABINOID AGONISTS - The present invention is related to novel benzimidazole compounds of Formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.02-18-2010
20100105732PIPERIDINE GPCR AGONISTS - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.04-29-2010
20100105731NOVEL BENZAMIDINE COMPOUND - Compounds represented by formula (1) and pharmaceutically acceptable salt thereofs: 04-29-2010
20090042938Chemical Compounds - The use of a compound of formula (I), Y is a single bond, C═O, C═S or S(O)02-12-2009
20090069376VLA-4 Antagonists - Substituted N—[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.03-12-2009
20130059887SUBSTITUTED PYRIDOXINE-LACTAM CARBOXYLATE SALTS - The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption.03-07-2013
20130065923SUBSTITUTED N-HETEROARYL BIPYRROLIDINE CARBOXAMIDES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I).03-14-2013
20120115909TAZAROTENE DERIVATIVES - The presently described subject matter relates to new derivatives of tazarotene that also exhibit retinoid activity, pharmaceutical compositions comprising the derivatives, method of treating skin disorders with the pharmaceutical compositions, and process of making the derivatives.05-10-2012
20120115908USE OF A HYDROXIMIC ACID HALIDE DERIVATIVE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - The invention relates to the use of a chemical substance selected from the group consisting of N-′2-hydroxy-3-(1-piperidinyl)-propoxyl 1-pyridine-1-oxide-3-carboximidoyl chloride, the optically active enantiomers and the mixtures of enantiomers thereof and pharmaceutically acceptable salts of the racemic and optically active compounds in the preparation of a pharmaceutical composition for the treatment or prevention of neurodegenerative diseases.05-10-2012
20090012122N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - Disclosed are N-aroyl cyclic amine derivatives having the formula:01-08-2009
200900054151,2-Diarylimidazoles for Use as Cb1 Modulators - Salts of 1,2-diarylimidazole-4-carboxamides and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.01-01-2009
20100022589PYRIDINE-3-CARBOXAMIDE COMPOUNDS AND THEIR USE FOR INHIBITING 11-BETA-HYDROXYSTEROID DEHYDROGENASE - Compounds of formula (I):01-28-2010
20100137367NOVEL CRYSTALLINE BEPOTASTINE METAL SALT HYDRATE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - The present invention discloses a non-hygroscopic crystalline bepotastine metal salt hydrate, a method for preparing same, and a pharmaceutical composition comprising same for treating or preventing a histamine-mediated disease or an allergic disease.06-03-2010
20080293769Polymorphs of a C-Met/Hgfr Inhibitor - This invention relates to polymorphs of (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to compositions including such salts and polymorphs, and to methods of using such compositions in the treatment of abnormal cell growth in mammals, especially humans.11-27-2008
20080269289Vanilloid receptor ligand compounds, pharmaceutical compositions containing them, a method of producing them and the use thereof to treat pain and various other conditions - Compounds corresponding to formula I:10-30-2008
20090281143Dose Reduction of a Cannabinoid CB1 Receptor Antagonist in the Treatment of Overweight or Obesity - O-(3-Piperidino-2-hydroxy-1-propyl)-nicotinic amidoxime or a pharmaceutically acceptable acid addition salt thereof is administered to patients suffering from overweight or obesity and treated with a cannabinoid CB11-12-2009
20090203737Pyrrole Derivatives as Positive Allosteric Modulators of Metabotropic Receptors - The present invention relates to new compounds which are Pyrrole derivatives of formula (I) wherein A, B, P, Q08-13-2009
20100004284Novel Heterocyclic Compounds as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to new compounds which are Heterocyclic derivatives of formula (I) wherein A, B, P, X, Y, Q, W, R01-07-2010
20090149498Pharmaceutical composition having prokinetic effect - The invention refers to the use of O-(3-piperidino-2-hydroxypropyl)nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition that restores and/or enhances the activity of the neuronal nitric oxide synthase enzyme.06-11-2009
20080312281G-Protein Coupled Receptor (Gpr116) Agonists and Use Thereof for Treating Obesity and Diabetes - Compounds of formula (I), or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.12-18-2008
20100120859NOVEL CASE OF RENIN INHIBITORS - The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency.05-13-2010
20120035214RENIN INHIBITORS - The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.02-09-2012
20100249187NOVEL DICARBOXYLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS - The present invention relates to new compounds of formula (I) possessing agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents. The invention is also directed to pharmaceutical compositions containing these compounds and use of these compounds for treatment/prevention of immune mediated diseases and conditions or inflammatory diseases and conditions.09-30-2010
20090018166New Pyridine Analogues X 161 - The present invention relates to certain new pyridin analogues of Formula (I)01-15-2009
20100081690OXAZOLE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention provides new compounds of formula I, wherein P, A, W, B, Q, R1 and R2 are defined as in formula I; invention compounds are positive allosteric modulators of metabotropic receptors—subtype 5 (“mGluR5”) which are useful for the treatment or prevention of central nervous system disorders such as for example: cognitive decline, both positive and negative symptoms in schizophrenia as well as other disorders in which the mGluR5 subtype of glutamate metabotropic receptor is involved.04-01-2010
20090306136Benzenesulfonamide Compounds and the Use Thereof - The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R12-10-2009
20100081691MULTICYCLIC COMPOUNDS AND METHODS OF THEIR USE - This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.04-01-2010
20100099710SRC FAMILY KINASE INHIBITORS - The invention relates to compounds of general formula (I) wherein X, A, R04-22-2010
20100099709PYRIDIN-2-YL-METHYLAMINE DERIVATIVES FOR TREATING OPIATE DEPENDENCE - The invention concerns the use pf compounds of general formula (I)04-22-2010
20090286831VR1 Receptor Ligands and u-Opioid Receptor Ligands for the Treatment of Pain - A pharmaceutical composition comprising i) at least one composition that has affinity to the μ-opioid receptor, and at least one compound that has affinity to the VR1 receptor, or ii) at least one compound, in particular at least one compound corresponding to formula (I), (II), (III), (IV) or (V), that has affinity to the μ-opioid receptor and to the VR1 receptor, and also to the use of the pharmaceutical compositions i) and ii) for the production of a drug for the treatment of pain.11-19-2009
20090270452USE OF SOLUBLE EPOXIDE HYDROLASE INHIBITORS IN THE TREATMENT OF SMOOTH MUSCLE DISORDERS - Disclosed herein are compounds, compositions, and methods for enhancing smooth muscle function in a subject by administration of soluble epoxide hydrolase inhibitors and for treating subjects with smooth muscle disorders including erectile dysfunction, overactive bladder, uterine contractions and irritable bowel syndrome.10-29-2009
20080293768Novel Compounds Derived From 5-Thioxylose And Their Use In Therapeutics - The invention relates to novel 5-thioxylose compounds, preferably derivatives of the 5-thioxylopyranose type, to the process for their preparation and to their use as active principles of drugs intended especially for the treatment or prevention of thrombosis or cardiac insufficiency.11-27-2008
20080306111TRICYCLIC DELTA- OPIOID MODULATORS - The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.12-11-2008
20120142732HETEROARYLS AND USES THEREOF - This invention provides compounds of formula IA or IB:06-07-2012
20080269288CHEMICAL COMPOUNDS - Compounds of formula (I):10-30-2008
20080300273Method of Treating Abnormal Cell Growth - The present invention relates to the use of (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, a novel c-Met/HGFR inhibitor, for treating abnormal cell growth in mammals. In particular, the invention provides methods of treating mammals suffering from cancer.12-04-2008
20090264466Certain Chemical Entities, Compositions and Methods - Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.10-22-2009
20090030040Substituted Heterocyclic Ethers and Their Use in CNS Disorders - The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.01-29-2009
20090143430ERYTHROPOIETIN PRODUCTION ACCELERATOR - The present invention relates to a preventive or therapeutic agent for pathological conditions caused by reduced production of erythropoietin, or for anemia, or for chronic anemia, renal anemia, aplastic anemia, or pure red cell aplasia, the agent comprising, as an active ingredient, a cyclic amine compound represented by the following formula (1):06-04-2009
20090005416BENZIMIDAZOLE DERIVATIVES - The present invention relates to a compound of the Formula I01-01-2009
20080319018ORGANIC COMPOUNDS - The present invention relates to a compound of the formula I12-25-2008
20090082399Carbamate derivatives as positive allosteric modulators of metabotropic glutamate receptors - The present invention relates to new compounds which are Carbamate derivatives of formula I wherein X, B, P, Q5W, R03-26-2009
20090062342AMINES - The invention relates to novel amine derivatives and the 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.03-05-2009
20090054487Pharmaceutical composition for increasing the mitochondrial genesis - The invention refers to the use of O-(3-piperidino-2-hydroxypropyl)nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition increasing the mitochondrial genesis.02-26-2009
201201427334-SUBSTITUTED-CYCLOHEXYLAMINO-4-PIPERIDINYL-ACETAMIDE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I).06-07-2012
20080262039Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process For Making Them, and Use Thereof For Treating Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I:10-23-2008
20080262038Diarylmethylidene Piperidine Derivatives, Preparations Thereof and Uses Thereof - Compounds of Formula: wherein R10-23-2008
20110144158ISOINDOLE-IMIDE COMPOUNDS AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - This invention relates to isoindole-imide compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.06-16-2011
20090221639Heterocyclic GPCR Agonists - Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful as regulators of satiety, e.g. for the treatment of obesity, and for the treatment of diabetes.09-03-2009
20090221640Novel Crystal Modifications - Novel crystal modifications of (5S)-5-[4-(5-chloro-pyridin-2-yloxy)-piperidine-1-sulfonylmethyl]-5-methyl-imidazolidine-2,4-dione are disclosed together with processes for preparing such modifications, pharmaceutical compositions comprising such a modification, and the use of such a modification in therapy.09-03-2009
20090253745MODULATORS OF OCULAR OXIDATIVE STRESS - Described herein are compounds, compositions and methods directed to the treatment of ophthalmic conditions characterized by oxidative stress or damage in a subject by reducing the reactive oxygen species in the subject. Also described herein are methods for reducing ophthalmic photooxidative damage in a subject.10-08-2009
201002738284-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS - The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R10-28-2010
20090258900AMIDE DERIVATIVE - Amide derivatives represented by the formula (I):10-15-2009
20100160377DERIVATIVES OF PYRAZOLE 3,5-CARBOXYLATES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS - The invention relates to derivatives of pyrazole 3,5-carboxylates, of general formula (I):06-24-2010
20100190824Novel Substituted Piperidones as HSP Inducers - The present invention relates to novel compounds of formula (I) or (II), their pharmaceutically acceptable salts and their hydrates, solvates, stereoisomers, conformers, tautomers, polymorphs and prodrugs and also pharmaceutically acceptable compositions containing them Wherein R07-29-2010
20100168167Piperidinones Useful in the Treatment of Inflammation - There is provided compounds of formula (I): wherein R07-01-2010
20080214611Pharmaceutical Compositions - 659 - The invention relates to a process for the preparation of a stable dispersion of amorphous particles of a CB1 modulator of sub-micron size in an aqueous medium.09-04-2008
20100152239Method to Improve Survival in Sepsis - This invention relates to the use of an α7nAChR-agonist such as GTS to control systemic inflammation during resuscitation following severe trauma such blood loss because of severe hemorrhage.06-17-2010
20100216839Pim kinase inhibitors and methods of their use - The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.08-26-2010
20100240701TUBULYSINS AND PROCESSES FOR PREPARING - Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations.09-23-2010
20110112143ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R05-12-2011
20080275085Piperidine derivative and use thereof - The present invention provides a novel piperidine derivative and a tachykinin receptor antagonist containing same, as well as a compound represented by the formula:11-06-2008
20100298377NOVEL SUBSTITUTED INDAZOLES, THE PREPARATION THEREOF AND USE OF SAME IN THERAPEUTICS - This disclosure relates to compounds of formula (I):11-25-2010
20080269287Substituted Pyridone Derivative - Compounds of a formula (I)10-30-2008
200901118541,2,4-TRIAZOLE ARYL N-OXIDES DERIVATIVES AS MODULATORS OF MGLUR5 - The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.04-30-2009
20130137726CONFORMATIONALLY RESTRICTED UREA INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE - Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.05-30-2013
20090069377DEUTERIUM-ENRICHED ENZASTAURIN - The present application describes deuterium-enriched enzastaurin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20110021565PIPERIDINE DERIVATIVES AS NK3 ANTAGONISTS - The invention relates to a compound of formula01-27-2011
20110034511SUBSTITUTED 2-CARBONYLAMINO-6-PIPERIDINAMINOPYRIDINES AND SUBSTITUTED 1-CARBONYLAMINO-3-PIPERIDINAMINOBENZENES AS 5-HT1F AGONISTS - The present invention relates to compounds of formula I:02-10-2011
20100016358GAMMA-GLOBIN INDUCER - The present invention is directed to a γ-globin inducer, to a prophylactic and/or therapeutic agent for sickle cell disease, and to a prophylactic and/or therapeutic agent for β-thalassemia, each containing, as an active ingredient, 4-[N-(4-methoxyphenyl)-N-[[5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]methyl]amino]-1-[[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl]piperidine, a salt thereof, or a solvate of either of these.01-21-2010
20090312368Pyridine Analogues IV - The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12-17-2009
20100048626Aryl Substituted Pyridines and the Use Thereof - This invention relates aryl substituted pyridines of Formula I:02-25-2010
20090215823COMPOSITIONS AND METHODS FOR EFFECTING NAD+ LEVELS USING A NICOTINAMIDE PHOSPHORIBOSYL TRANSFERASE INHIBITOR - The present invention relates to methods for decreasing cellular DNA repair in a patient diagnosed with or suspected to have chronic lymphocytic leukemia (CLL); decreasing cellular NAD08-27-2009
20090215822Substituted Oxadiazole Derivatives as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R08-27-2009
20090215821N-Substituted Azacycles - N-substituted azacycle derivative compounds represented by formula (I):08-27-2009
201000630923-CYANO-4-(4-PHENYL-PIPERIDIN-1-YL)-PYRIDIN-2-ONE DERIVATIVES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 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 such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.03-11-2010
20100069436IMIDAZOLE COMPOUNDS HAVING AN ANTIINFLAMMATORY EFFECT - The invention relates to imidazole derivatives of the Formula (I) in which the radicals R03-18-2010
20110098320Lactam Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.04-28-2011
20110071191INSECTICIDAL COMPOUNDS - A compound of formula (I): wherein R03-24-2011
20120202851PIM KINASE INHIBITORS AND METHODS OF THEIR USE - The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.08-09-2012
20120122926BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I:05-17-2012
20110053979PYRIDINE DERIVATIVES USED TO TREAT OREXIN RELATED DISORDERS - This invention relates to pyridinamine methyl substituted piperidinyl derivatives I and their use as pharmaceuticals.03-03-2011
20110028515NEW PIPERIDINE DERIVATIVES - Compounds of formula (I)02-03-2011
20120302602Vanilloid Receptor Ligand Compounds, Pharmaceutical Compositions Containing Them, a Method of Producing Them and the Use Thereof to Treat Pain and Various Other Conditions - Compounds corresponding to formula I:11-29-2012
20100298378ARYL-SUBSTITUTED POLYCYCLIC AMINES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS A MEDICAMENT - The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof;11-25-2010
20100305157 DERIVATIVES OF DICARBOXYLIC AMINO ACIDS AND THEIR APPLICATION IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - Products of a general formula (I) and their use in the manufacture of medicines useful for the treatment of neurodegenerative diseases such as Alzheimer's disease or, in general, any disease or pathology produced by alterations of biological functions that can be treated or therapeutically modified by these products.12-02-2010
20110190346Diphenyl Substituted Alkanes as Flap Inhibitors - The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors.08-04-2011
20100029718ORGANIC COMPOUNDS - The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.02-04-2010
20100016360ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR INHIBITORS - The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.01-21-2010
20100016361ARYL CARBOXYLIC ACID CYCLOHEXYL AMIDE DERIVATIVES - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: (I) wherein the variants R and X are defined in the specification.01-21-2010
20100016359METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY - The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.01-21-2010
200802937671-Isopropyl-2-Oxo-1,2-Dihydropyridine-3-Carboxamide Derivatives Having 5-Ht4 Receptor Agonistic Activity - This invention provides a compound of formula (I): wherein R11-27-2008
20110118311AZOLE COMPOUND - A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridine-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention. The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain.05-19-2011
201001447891-Isopropyl-2-Oxo-1,2-dihydropyridine-3-carboxamide Derivatives having 5-HT4 Receptor Agonistic Activity - This invention provides a compound of formula (I): wherein R06-10-2010
20110306636OXAZOLE PYRIDINE DERIVATIVES USEFUL AS S1P1 RECEPTOR AGONISTS - The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases.12-15-2011
20100210686THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula:08-19-2010
20100120858Piperidine Derivatives - The invention relates to compounds of Formula (I)05-13-2010
20120157494ISOINDOLYL COMPOUNDS - Compounds of the formula I:06-21-2012
20120316201NOVEL BENZIMIDAZOLE AND IMIDAZOPYRIDINE DERIVATIVES AND USE THEREOF AS A MEDICAMENT - The invention relates to novel benzimidazole and imidazopyridine derivatives having the general Formula (I), which have a good affinity with certain subtypes of melanocortin receptors, particularly MC4 receptors. The derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said the compounds having the general Formula (I).12-13-2012
20110184020Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process For Making Them, and Use Thereof For Treating Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I:07-28-2011
20100048627 SYNERGISTIC PHARMACEUTICAL COMBINATION FOR THE PREVENTION OR TREATMENT OF DIABETES - The invention refers to a synergistic pharmaceutical combination which comprises (a) a first pharmaceutical composition containing an antidiabetic or anti-hyperlipidemic active agent and one or more conventional carrier(s), and (b) a second pharmaceutical composition containing a hydroximic acid derivative of the formula I and one or more conventional carrier(s). The pharmaceutical combination is suitable for the prevention or treatment of, among others, diabetes mellitus.02-25-2010
20100010042ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.01-14-2010
20120225905BEPOTASTINE COMPOSITIONS - Novel compositions including bepotastine besilate are provided such as sorbitol-free compositions, compositions including at least about 0.008% w/v benzalkonium chloride, and compositions including hydroxypropylmethyl cellulose E15 LV.09-06-2012
20110003853Metalloproteinase Inhibitors - Compounds of the formula (I) wherein z is SO01-06-2011
20110003852N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE - Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.01-06-2011
20120270900NOVEL METHOD OF TREATMENT - The present application discloses a method for the treatment or for alleviating the symptoms of a cancer in a subject comprising the steps of a) determining the level of Nicotinic acid phosphoribosyltransferase (NAPRT) in said subject; and b) 1) in the event of a level of NAPRT which is lower than a predetermined threshold value, treating said subject sequentially/simultaneous with i) an effective amount of a nicotinamide phosphoribosyltransferase inhibitor (NAMPRTi), and ii) an effective amount of a nicotinic acid, a nicotinic acid precursor or a prodrug of nicotinic acid; or 2) in the event of a level of NAPRT which is higher than or equal to a predetermined threshold value, treating said subject with i) an effective amount of a NAMPRTi in the absence of sequential/simultaneous treatment with ii) an effective amount of a nicotinic acid, a nicotinic acid precursor or a prodrug of nicotinic acid.10-25-2012
20120322825AQUEOUS LIQUID PREPARATIONS AND LIGHT-STABILIZED AQUEOUS LIQUID PREPARATIONS - An aqueous liquid preparation containing (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, which is stabilized with a water-soluble metal chloride, is provided.12-20-2012
20120088793Bicyclic Compounds and Methods of Making and Using Same - Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same.04-12-2012
20120088792Pyridin-2-YL Methylamine Derivatives for Treating Opiate Dependence - The invention concerns the use of compounds of general formula (I)04-12-2012
20100204275N-PIPERIDIN-4-YLMETHYL-AMIDE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors.08-12-2010
20100204274PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R08-12-2010
20110319448GUANIDINE-CONTAINING COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I:12-29-2011
20130012541Therapeutic Agents Useful for Treating Pain - A compound of formula:01-10-2013
20120149732MULTIFUNCTIONAL LINKERS AND METHODS FOR THE USE THEREOF - In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.06-14-2012
20110136866INSECTICIDAL PHENYL- OR PYRIDYL-PIPERDINE COMPOUNDS - A compound of formula (I): wherein A, p, R06-09-2011
20090298878OXIME COMPOUNDS AND THE USE THEREOF - The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO12-03-2009
20080227813Pharmaceutical compositions and methods for treating diseases associated with neurodegeneration - The present invention relates to methods for treating diseases, conditions or disorders using hydroxyamine compounds, and in particular, N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride (Compound I) alone or in combination with one or more other therapeutic agents for the treatment of conditions, disorders or diseases associated with neurodegeneration in the central nervous system. Additional therapeutic agents are provided. The present invention also relates to pharmaceutical compositions comprising hydroxyamine compounds, an additional therapeutic agent and a pharmaceutically acceptable carrier and methods for treating diseases using them.09-18-2008
20080214610Thiazolylimidazole Derivatives and Their Use as Inhibitors of Microsmal Triglyceride Transfer Protein - The present invention relates to thiazolylimidazole derivatives of the general formula (I) in which: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3; and R09-04-2008
20130131111NMN MODULATORS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS - The invention relates to a nicotinamide mononucleotide (NMN) modulator useful as a neuroprotective medicament in the treatment of neurodegenerative disorders, in particular but not exclusively disorders involving axon degeneration of neuronal tissue such as Wallerian degeneration, to the use of NMN as a biomarker for axon degeneration, to a method of demonstrating axon degeneration using an NMN-based biomarker, to a diagnostic kit for detecting axon degeneration, to a method of screening for an NMN modulator, and to an NMN modulator identified using the aforementioned screening method.05-23-2013
20090062341Nuclear receptor binding agents - The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.03-05-2009
20090048299Biphenyl compounds useful as muscarinic receptor antagonists - This invention provides compounds of formula I:02-19-2009
20090192193DIAGNOSTIC AGENT AND METHOD FOR DETECTION OF CANCER AND A MEANS FOR TREATMENT OF SAME - A method is disclosed for detecting colorectal carcinoma having at least one HERG potassium ion channel, where at least one HERG potassium channel is detected in a tissue biopsy of the human color or rectum. In addition, a method is disclosed for treating colorectal carcinoma having at least one HERG potassium channel in a patient in need of said treatment, which comprises the step of administering to said patient, a therapeutically effective amount of 4-[1-{2-(6-methyl-2-pyridinyl)ethyl-4-piperidinyl}carbonyl]methane-sulfoanilide 2HCl sufficient to treat the colorectal carcinoma having at least one HERG potassium channel by selectively blockading the HERG potassium channel.07-30-2009
20110237622RENIN INHIBITORS - The present invention relates to 3,4-substituted piperidinyl—based renin inhibitor compounds bearing at 4-position oxopyridine or Isoquinolone and having the formula (I): wherein S is Formula (IIa) or Formula (IIb). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.09-29-2011
20130150407PIPERIDINYL NAPHTHYLACETIC ACIDS - The invention is concerned with the compounds of formula (I):06-13-2013
20090253744Acylated piperidine 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.10-08-2009
20130203810Identification, Assessment, and Therapy of Cancers with Innate or Acquired Resistance to ALK Inhibitors - Described herein are compositions, kits, and methods for determining whether subjects having cancer(s) positive for ALK mutations are likely to respond to treatment with an ALK inhibitor and/or whether a patient having such cancer(s) is likely to have a relatively slower disease progression. Further described are methods for prognosing a time course of disease in a subject having such cancer.08-08-2013
20120095047Novel Heteropyrrole Analogs Acting on Cannabinoid Receptors - Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.04-19-2012

Patent applications in class The additional ring is a six-membered hetero ring consisting of one nitrogen and five carbon atoms