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Isoquinolines (including hydrogenated)

Subclass of:

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

514279000 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos

514299000 - Bicyclo ring system having the six-membered hetero ring as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514309000 Chalcogen attached directly to the six-membered hetero ring by nonionic bonding 49
514310000 Nitrogen, other than as nitro or nitroso, attached directly to the isoquinoline ring system by nonionic bonding 25
514308000 Plural isoquinoline ring systems attached directly or indirectly to each other by nonionic bonding 15
Entries
DocumentTitleDate
20090192188TETRAHYDROISOQUINOLINE DERIVATIVES - This invention relates to novel tetrahydroisoquinoline derivatives, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual OX-1/OX-2 orexin antagonist.07-30-2009
20080287489Ophthalmic compositions for treating ocular hypertension - This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.11-20-2008
20130085157ARYLSUBSTITUTED THIAZOLOTRIAZOLES AND THIAZOLOIMIDAZOLES - This disclosure relates to compounds, compositions and methods for the treatment of various disorders. In particular, the disclosure relates to thiazolotriazole and thiazoloimidazole compounds which agonize the activity of the protein TGR5.04-04-2013
20130210859NOVEL CORTISTATIN A ANALOG AND USE THEREOF - A compound represented by the general formula (M):08-15-2013
20100113512METHOD OF TREATMENT USING NOVEL ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS - A method of treatment using pharmaceutical compositions containing novel antagonists or inverse agonists at opioid receptors for the treatment of binge eating disorder, anorexia nervosa, bulimia nervosa, excess drug or alcohol use, or eating disorder not otherwise specified.05-06-2010
20100076015Aminopyridine Derivatives - The present invention provides compounds of formula (I):03-25-2010
20120245200CRYSTAL FORM OF QUINOLINE COMPOUND AND PROCESS FOR ITS PRODUCTION - A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula (09-27-2012
20100144785FUNGICIDE N-6-MEMBERED FUSED (HETERO) ARYL-METHYLENE-N-CYCLOALKYL CARBOXAMIDE DERIVATIVES - The present invention relates N-(aromatic, 6-membered, fused, (hetero)aryl-methylene)-N-cycloalkyl carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—R06-10-2010
20090156635BIARYLOXYMETHYLARENECARBOXYLIC ACIDS AS GLYCOGEN SYNTHASE ACTIVATORS - The present invention relates to compounds of formula (I)06-18-2009
20090124655HETEROCYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS - The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.05-14-2009
20090124654Aryl and Heteroaryl Compounds, Compositions, Methods of Use - This invention provides aryl and heteroaryl compounds of formula (X). The compounds of the invention may be useful as antagonists, or partial antagonist of factor IX and/or factor XI and thus, may be used to inhibit the intrinsic pathway of blood coagulation. Formula (X) wherein R05-14-2009
20110003850DERIVATIVES OF 4-(N-AZACYCLOALKYL) ANILIDES AS POTASSIUM CHANNEL MODULATORS - This invention provides a compound of formula IA01-06-2011
20090306130NOVEL TETRAHYDRO-ISOQUINOLINES - The present invention provides a compound selected from compounds of formula (A) as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (A) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (A) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.12-10-2009
20130059883COMPOUNDS AND METHODS - Disclosed are compounds having the formula:03-07-2013
201300598828-Phenylisoquinolines And Pharmaceutical Composition Used In Treatment For Sepsis - A compound is provided. The compound includes a formula of:03-07-2013
20130065918SOLUBLE GUANYLATE CYCLASE ACTIVATORS - The present invention relates to compounds of formula (I):03-14-2013
20090203734F1F0-ATPASE INHIBITORS AND RELATED METHODS - The present invention relates to inhibitors of mitochondrial F08-13-2009
20090012117Bicyclic derivatives as modulators of ion channels - Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:01-08-2009
20100204269Compounds and methods for treatment of chemotherapy-induced anemia - The invention relates to methods and compounds for treating chemotherapy-induced anemia. In particular, methods for treating chemotherapy-induced anemia in subjects refractory to treatment with recombinant human erythropoietin are encompassed herein.08-12-2010
20090298869Crystalline pharmaceutical and methods of preparation and use thereof - Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.12-03-2009
201003117893-Substituted Propanamine Compounds - Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I):12-09-2010
20090054481Saquinavir Mesylate Oral Dosage Form - A solid unit oral pharmaceutical dosage form of saquinavir mesylate is provided comprising micronized saquinavir mesylate in an amount of from 250 mg to 800 mg calculated as free base, and a pharmaceutically acceptable binder, disintegrant, and water soluble carrier. A solid unit dosage form of saquinavir mesylate is provided comprising from 60% to 80% micronized saquinavir mesylate based on the mesylate salt, 4% to 8% water soluble binder, a disintegrant and a carrier, wherein each percentage is of the kernel weight.02-26-2009
20090326006Benzazole Derivatives, Compositions, and Methods of Use as Beta-Secretase Inhibitors - The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. 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 BACE is involved.12-31-2009
20090048292SYNERGISTIC COMBINATION - Pharmaceutical combinations comprising as compound A at least one compound from the group of angiogenesis inhibitors of general formula I02-19-2009
20100286196NEW INHIBITOR OF DD-PEPTIDASE AND ITS USE AS ANTIBIOTIC OR ANTICANCER DRUG - A new compound is revealed and the strain of 11-11-2010
20090275608Methods of diagnosing and treating parp-mediated diseases - Disclosed are methods of identifying a disease treatable with modulators of differentially expressed genes in a disease, including at least PARP modulators, by identifying the level of expression of differentially expressed genes, including at least PARP, in a plurality of samples from a population, making a decision regarding identifying the disease treatable by modulators to the differentially expressed genes wherein the decision is made based on the level of expression of the differentially expressed genes. The method can further comprise treating the disease in a subject population with modulators of identified differentially expressed genes. The methods relate to identifying up-regulated expression of identified differentially-expressed genes in a disease and making a decision regarding the treatment of the disease. The level of expression of the differentially expressed genes in a disease can also help in determining the efficacy of the treatment with modulators to the differentially expressed genes.11-05-2009
20100035923VR1 VANILLOID RECEPTOR ANTAGONISTS WITH A IONONIC SUBSTRUCTURE - The invention provides compounds of formula (I), wherein Y, R, n and X are as defined in the description, a process for their preparation and pharmaceutical compositions containing them. The compounds of formula (I) inhibit the Transient Receptor Potential Vanilloid 1 (TRPV1), which plays a pivotal role in the development of post-inflammatory analgesia, therefore they can be used as analgesic and anti-inflammatory drugs.02-11-2010
20100173936Compositions comprising renin-angiotensin aldosterone system inhibitors and lipoic acid compounds, and the use thereof for the treatment of renin-angiotensin aldosterone system-related disorders - Compositions are provided which can be useful in treating a renin-angiotensin aldosterone system-related disorder. These compositions include renin-angiotensin aldosterone system inhibitors and lipoic acid compounds, as well as other therapeutic agents, and are useful in treating hypertension, stroke, metabolic syndrome, or other renin-angiotensin aldosterone system-related disorders in a subject. The compositions are also useful in improving vasodilation, reducing proteinuria, and reducing insulin resistance in a subject. Pharmaceutical compositions and methods of treatment using the compositions are further provided.07-08-2010
20090099229Isoquinolines as IGF-1R Inhibitors - Compounds of the formula (I):04-16-2009
20120142727NITROGENOUS-RING ACYLGUANIDINE DERIVATIVE - [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT06-07-2012
20110263641Isoxazolines For Controlling Invertebrate Pests - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof,10-27-2011
20100120845ARYLOXYALKYLCARBAMATE-TYPE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The invention relates to a compound of formula (I):05-13-2010
20120035211NOVEL POLYMORPHS OF SAQUINAVIR - The present invention provides novel polymorphs of saquinavir, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides a process for purification of saquinavir. The present invention further provides a novel process for preparation of known saquinavir crystalline form I.02-09-2012
20100081687BIARYLCARBOXYARYLAMIDES AS VANILLOID-1 RECEPTOR MODULATORS - The present invention provides compounds of formula (I): wherein A and Z are as defined in the description, along with methods for preparing such derivatives and their use for the treatment of inflammatory diseases such as neuropathic pain.04-01-2010
20100099702Therapeutic agent for neuropathic pain - Disclosed is a therapeutic agent for neuropathic pain having an excellent therapeutic effect on neuropathic pain which is a intractable disease. More specifically, disclosed are a therapeutic agent for neuropathic pain which comprises a peripheral benzodiazepine receptor antagonist (particularly PK 11195) as the active ingredient; a pharmaceutical composition for the treatment of neuropathic pain which comprises a peripheral benzodiazepine receptor antagonist as the active ingredient; a method for the treatment of neuropathic pain using a peripheral benzodiazepine receptor antagonist; and others.04-22-2010
20090275607Tetrahydro isoquinoline derivatives, preparation methods and medicinal uses thereof - A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as κ-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The substituents R11-05-2009
20090275609Carboxamide Compounds and Methods for Using The Same - Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure11-05-2009
20100280066ACYLATED AMINO ACID AMIDYL PYRAZOLES AND RELATED COMPOUNDS - This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity, and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.11-04-2010
20100273826METHODS OF USE AND COMPOSITIONS FOR THE DIAGNOSIS AND TREATMENT OF INFECTIOUS DISEASES - Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.10-28-2010
20080287488Use of a Sulfonamide Compound For Improving the Pharmacokinetics of a Drug - A method for improving the pharmacokinetics of drugs, which are metabolized by cytochrome P450 monooxygenase is disclosed. More specifically it relates to a method for improving the pharmacokinetics of retroviral protease inhibitors and in particular for improving the pharmacokinetics of human immunodeficiency virus (HIV) protease inhibitors. A pharmaceutical composition and its use in the manufacture of a medicament for the inhibition or treatment of an HIV infection or AIDS in a human being are also part of the invention.11-20-2008
20090264462KAPPA OPIOID RECEPTOR LIGANDS - Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.10-22-2009
20090082393New addition salts of angiotensin-converting enzyme inhibitors with no donor acids, a process for their preparation and pharmaceutical compositions containing them - Compounds of formula (I):03-26-2009
20090082394Tetrahydroisoquinoline Derivatives to Enhance Memory Function - The invention relates to the use of tetrahydroisoquinoline derivatives for the preparation of a medicament to enhance, maintain and/or restore all stages and/or types of short-, middle- and/or long-term memory.03-26-2009
20110230518OXADIAZOLE FUSED HETEROCYCLIC DERIVATIVES USEFUL FOR THE TREATMENT OF MULTIPLE SCLEROSIS - The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.09-22-2011
20080262032Isoxazoline Derivative and Novel Process for Its Preparation - The present invention relates to an isoxazoline derivative having the cyclic carboxylic acid hemiketal moiety of formula (1) for use as caspase inhibitor, a process for preparing it, and a pharmaceutical composition comprising it.10-23-2008
20090197912Sulfonamide Derivatives for the Treatment of Diseases - The invention relates to compounds of formula (1)08-06-2009
20100160370METHOD OF TREATMENT AND PHARMACEUTICAL COMPOSITIONS - The present invention relates to methods, uses, and compositions comprising the caspase inhibitor (R)-N-((2S,3S)-2-(fluoromethyl)-2-hydroxy-5-oxo-tetrahydrofuran-3-yl)-5-isopropyl-3-(isoquinolin-1-yl)-4,5-dihydroisoxazole-5-carboxamide, or a pharmaceutically acceptable salt thereof.06-24-2010
20120095040CYCLOPENTA[C]PYRROLE-2-CARBOXYLATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds of the general formula (I) where: R04-19-2012
20130123299COMPOUNDS AND METHODS FOR TREATMENT OF SYSTEMIC LUPUS ERYTHEMATOSUS - Small molecule compounds are provided for treating lupus as are methods of treating lupus using these compounds.05-16-2013
20100152235OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (S1P) - The present invention relates to a novel oxadiazole derivative having pharmacological activity, processes for its preparation, pharmaceutical compositions containing it and its use in the treatment of various disorders.06-17-2010
20100113511Mono Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors - Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.05-06-2010
20100120844TETRAHYDROISOQUINOLINE COMPOUND - The present invention relates a specific tetrahydroisoquinoline compound which is useful as a chemokine receptor type 3 (CCR3) antagonist, and a pharmaceutical composition comprising the same as an active ingredient. The tetrahydroisoquinoline compound of the present invention is useful for the treatment or prevention of a disease in which CCR3 participates.05-13-2010
20120142726PHARMACEUTICAL COMPOSITIONS COMPRISING 3,4-DIHYDROISOQUINOLIN-2(1H)-YL-3-PHENYLUREA DERIVATIVES HAVING FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) AGONIST OR ANTAGONIST ACTIVITY - The present invention relates to a method of treating a disorder associated with modulation of the FPRL-1 receptor which comprises administering a therapeutically effective amount of a pharmaceutical composition comprising a 3,4-dihydroisoquinolin-2(1H)-yl-3-phenylurea derivative.06-07-2012
20090247572AGENT FOR TREATING ATRIAL FIBRILLATION - It is intended to provide an agent for treating atrial fibrillation, comprising an I10-01-2009
20130137718PROCESS FOR THE PREPARATION OF 2-(CYCLOHEXYLMETHYL)-N--1,2,3,4-TETRAHYDROISOQUINOLINE-7-SULFONAMIDE - Industrially applicable process for preparing 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, and salts thereof.05-30-2013
20130137719Novel 6,7-disubstituted-sioquinoline derivatives and their use - The present invention relates compounds of general formula (I) and stereoisomers and pharmaceutically acceptable salts and prodrugs thereof; wherein R′ and R05-30-2013
20110009446OLIGOMER-GUANIDINE CLASS CONJUGATES - The invention relates to (among other things) oligomer-guanidine class conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.01-13-2011
20110039885METHODS FOR INCREASING ENDOTHELIAL PROGENITOR CELLS - The present invention relates to methods and compounds useful for increasing endothelial progenitor cell levels in blood and bone marrow. Methods and compounds for increasing endothelial progenitor cell mobilization are also provided.02-17-2011
20090143423SOLID DISPERSION PRODUCT CONTAINING N-ARYL UREA-BASED COMPOUND - A solid dispersion product comprising at least one N-aryl urea-based pharmaceutically active agent or an agent of related structural type is obtained by a) preparing a liquid mixture containing the at least one active agent, at least one pharmaceutically acceptable matrix-forming agent, at least one pharmaceutically acceptable surfactant and at least one solvent, and b) removing the solvent(s) from the liquid mixture to obtain the solid dispersion product.06-04-2009
20100152234Substituted 4-(1,2,3,4-tetrahydroisoquinolin-2-yl)-4-oxobutyric acid amide as KCNQ2/3 modulators - The invention relates to substituted tetrahydroisoquinolinyl-4-oxobutyric acid amides, methods for the preparation thereof, medicinal products containing these compounds and the use of these compounds for the preparation of medicinal products.06-17-2010
20110144153AMIDE COMPOUND - [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided.06-16-2011
20100056567NOVEL ALKYL SUBSTITUTED PIPERIDINE DERIVATIVES AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel alkyl substituted piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.03-04-2010
20110178123NONPEPTIDE HIV-1 PROTEASE INHIBITORS - Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.07-21-2011
20100056566New substituted isoquinoline and isoquinolinone derivatives - The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I)03-04-2010
201200352102,3-DIHYDROBENZO(1,4) DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEME DISEASES - Compounds of formula I02-09-2012
20090030036Nuclear receptor binding agents - The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBAs 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, inflammatory diseases, oxidative stress related disorders such as Parkinson's and stroke, neurological disorders, ophthalamic disorders, cardiovascular disease, and obesity.01-29-2009
20090247573(HETERO)ARYL 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
200902475743-AMINO-PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention provides novel compounds represented by the general formula (I):10-01-2009
200900884505-ht7 receptor antagonists - The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline propyl sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.04-02-2009
20080242698Organic Compounds - The invention relates to novel diamines of the formula10-02-2008
20100298373OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (SIP) - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.11-25-2010
20100120843PHARMACEUTICAL COMPOSITION FOR TREATING ALCOHOL-INDUCED LIVER INJURY COMPRISING (4S,5S)-5-FLUOROMETHYL-5-HYDROXY-4-(AMINO)-DIHYDROFURAN-2-ONE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - The present invention relates to a pharmaceutical composition for treating alcohol-induced liver injury comprising (4S,5S)-5-fluoromethyl-5-hydroxy-4-({[(5R)-5-isopropyl-3-(isoquinolin-1-yl)-4,5-dihydro-5-isoxazolyl]carbonyl}amino)-dihydrofuran-2-one or pharmaceutically acceptable salt thereof, and a use thereof.05-13-2010
20110136859Compounds - A compound of formula (I)06-09-2011
20100190822Pharmaceutical Compositions As Inhibitors of Dipeptidyl Peptidase-IV (DPP-IV) - The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.07-29-2010
20110201643NOVEL N-SUBSTITUTED TETRAHYDROISOQUINOLINE/ISOINDOLINE HYDROXAMIC ACID COMPOUNDS - Compounds of a certain formula (I) wherein R1, R2, R3, X, Y, r, s, t, u and v have the meanings as defined in the specification, and the salts, solvates and hydrates thereof are novel effective HDAC 6 inhibitors.08-18-2011
20100022582Tetrahydroisoquinoline Compound and Medicinal Use Thereof - The present invention provide a tetrahydroisoquinoline compound having a superior ACAT-inhibitory activity and/or anti-oxidation action, particularly, novel compound represented by the formula (I) (wherein each symbol is as described in the specification) and a pharmaceutically acceptable salt thereof.01-28-2010
20100022583PYRIDINYL MODULATORS OF gamma-SECRETASE - The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R01-28-2010
20090221633INHIBITORS OF AKT (PROTEIN KINASE B) - 4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol or a pharmaceutically acceptable salt thereof or a hydrate of the compound or the salt thereof as Akt inhibitors that are antineoplastic and/or antiviral agents as well as compositions comprising these compounds and methods of using these compounds.09-03-2009
20090170895S1P3 RECEPTOR ANTAGONIST - The present invention relates to a medicine, and more particularly to novel arylamidrazone derivatives having an antagonistic action against S1P07-02-2009
20120004259METHOD OF TREATMENT OR PROPHYLAXIS - The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT01-05-2012
20120004260INHIBITION OF FATTY ACID SYNTHESIS BY IODO-NITROBENZAMIDE COMPOUNDS AND METHODS OF TREATMENT THEREOF - The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis.01-05-2012
201200463123-SUBSTITUTED PROPANAMINE COMPOUNDS - Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I):02-23-2012
20110166176COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.07-07-2011
20120022101SALT AND SOLVATES OF A TETRAHYDROISOQUINOLINE DERIVATIVE - (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.01-26-2012
201200590321,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES EFFECTIVE AS ANTIGLIOMA AGENTS, METHODS OF MAKING, AND THEIR USE - Disclosed are tetrahydroisoquinoline-derivative compounds effective for killing cancer cells, shrinking tumor size, and treating cancer.03-08-2012
20110105555SUBSTITUTED N-IMIDAZO[2,1-B]THIAZOLE-5-SULFONAMIDE DERIVATIVES AS 5-HT6 LIGANDS - The invention relates to compounds having pharmacological activity towards the 5-HT05-05-2011
20100093789SULFONAMIDE COMPOUND - A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G04-15-2010
20110184017STABLE AQUEOUS SOLUTION COMPOSITION CONTAINING SULFONAMIDE COMPOUND - An aqueous solution composition containing (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-aminopyrrolidine or (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine as an active ingredient, and not containing citric acid or a salt thereof, which has high stability so as to be storable at room temperature.07-28-2011
20120129886METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.05-24-2012
201002168362,3-DIHYDROBENZO(1,4) DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEME DISEASES - Compounds of formula I08-26-2010
20100273827OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (S1p) - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.10-28-2010
20100292269BIR DOMAIN BINDING COMPOUNDS - The present invention is directed towards an isomer, an enantiomer, a diastereoisomer, or a tautomer of a pyrrolidine compound represented by Formula I:11-18-2010
201101246792-SUBSTITUTED-p-QUINONE DERIVATIVES FOR TREATMENT OF OXIDATIVE STRESS DISEASES - Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein.05-26-2011
20080300269THERAPEUTIC COMPOUNDS - Disclosed herein are compounds of the formula12-04-2008
20090298870PODOPHYLLOTOXIN DERIVATIVES - 4-O esters of podophyllotoxin and 4′-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4′-demethylepipodophyllotoxin. The compounds are useful for treating cancer.12-03-2009
20120270898SULFONAMIDE COMPOUND AND CRYSTAL THEREOF - (S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2θs are about 13.9°, 21.5°, 21.7°, 22.4°, 22.8°, 24.5° and 35.0° in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like.10-25-2012
20100234420TETRAHYDROQUINOLINE DERIVATIVES FOR TREATING POST-TRAUMATIC STRESS DISORDERS - The invention relates to methods of treating, reducing the symptoms of, or preventing a post-traumatic stress syndrome by administration of tetrahydroquinoline derivatives of formula I09-16-2010
20120101125SUBSTITUTED ISOQUINOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS - The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.04-26-2012
20100130545BRIDGED SIX-MEMBERED RING COMPOUNDS - The invention relates to compounds of formula (I), wherein R05-27-2010
20080255188Muscarinic Receptor Antagonists - This present invention generally relates to muscarinic receptor antagonists of Formula (I), which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.10-16-2008
20100087479Compositions Useful as Inhibitors of Voltage-Gated Sodium Channels - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.04-08-2010
20080234317METHODS FOR THE IMPROVEMENT OF MEMORY AND NEUROLOGICAL FUNCTION COMPRISING THE ADMINISTRATION OF COMPOSITIONS THAT ACT AS INHIBITORS OF THE SODIUM PROTON (NA+ /H+ ) EXCHANGER, SUBTYPE 5 (NHE-5) - The present invention comprises the use of pharmaceutical compositions that are effective in the inhibition of the Na09-25-2008
20130172384FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer.07-04-2013
20080221156STABLE FORMULATIONS OF ACE INHIBITORS, AND METHODS FOR PREPARATION THEREOF - The present invention provides stable formulations of ACE inhibitors, especially enalapril maleate, that can be manufactured in a time efficient, cost effective manner. Such formulations can be prepared simply and on a large industrial scale. The present invention also provides methods for the preparation of stable formulations of ACE inhibitors, especially enalapril maleate.09-11-2008
200802146035-Ht7 Receptor Antagonists - The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.09-04-2008
20130143916COMPOUND LIBRARIES MADE THROUGH PHOSPHINE-CATALYZED ANNULATION/TEBBE/DIELS-ALDER REACTIONS - A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library.06-06-2013
20080200501NOVEL CANNABINOID RECEPTOR LIGANDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESSES FOR THEIR PREPARATION - The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).08-21-2008
20080200500Quinoline Derivatives as Nk3 Antagonists - Compounds of Formula I08-21-2008
20080200499Selective Insecticides and/or Acaricides Based on Substituted Cyclic Dicarbonyl Compounds and Safeners - The present invention relates to the use of selective insecticidal and/or acaricidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising 08-21-2008
20100286197Carboxamide Derivatives As Therapeutic Agents - This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.11-11-2010
20100298374NITRILE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I11-25-2010
20130158072KAPPA OPIOID RECEPTOR BINDING LIGANDS - Kappa opioid recep-tor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor, such as heroin or cocaine addictions.06-20-2013
20130184309METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.07-18-2013
20100048617COMPOUNDS - The present invention relates to substituted 3-Aminopyrazole compounds of formula (I)02-25-2010

Patent applications in class Isoquinolines (including hydrogenated)

Patent applications in all subclasses Isoquinolines (including hydrogenated)