Inventors list

Assignees list

Classification tree browser

Top 100 Inventors

Top 100 Assignees


Three or more ring hetero atoms in the additional hetero ring

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

514228800 - Hetero ring is six-membered and includes at least nitrogen and oxygen as ring hetero atoms (e.g., monocyclic 1,2- and 1,3-oxazines, etc.)

514231200 - Morpholines (i.e., fully hydrogenated 1,4- oxazines)

514231500 - Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding

514235500 - Ring nitrogen in the additional hetero ring

514235800 - Plural ring nitrogens in the additional hetero ring (e.g., imidazole, pyrazine, etc.)

Patent class list (only not empty are listed)

Deeper subclasses:

Entries
DocumentTitleDate
20130029988CERTAIN KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.01-31-2013
20130029989TOPICAL TREATMENTS FOR PAIN - The present invention relates to novel compositions and therapeutic methods for the treatment of pain, in particular neuropathic, ischemic, muscle, arthritic or multiple sclerosis pain. The compositions include a combination of an alpha2-adrenergic agonist or a nitric oxide donor combined with a phosphodiesterase (PDE) or a phosphatidic acid (PA) inhibitor, which have been found to act together synergistically to provide effective treatment for pain, especially when administered topically.01-31-2013
20120184552LATANOPROST-CONTAINING AQUEOUS EYE DROPS AND METHOD FOR INHIBITING ADSORPTION OF LATANOPROST TO RESIN - The invention provides an aqueous eye drop containing latanoprost, a surfactant, and an aliphatic mono- or di-carboxylic acid having a carbon number of 3-10 or a salt thereof. In addition, the invention provides a method of suppressing adsorption of latanoprost to a resin in an aqueous solution, by adding a surfactant and an aliphatic mono- or di-carboxylic acid having a carbon number of 3-10 or a salt thereof.07-19-2012
20120184551COMBINATION OF BRIMONIDINE AND TIMOLOL FOR TOPICAL OPHTHALMIC USE - Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.07-19-2012
20090012087New Aza-Bicyclohexane Compounds Useful As Inhibitors Of Thrombin - This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.01-08-2009
20090181969Hypotensive Lipid And Timolol Compositions And Methods Of Using Same - New compositions for and methods of treating ocular hypertension provide for effective treatment of ocular hypertension often using reduced concentrations of active components. Such compositions include a timolol component and a hypotensive lipid component. The present compositions and methods are relatively straightforward, can be easily produced, for example, using conventional manufacturing techniques, and can be easily and conveniently practiced, for example, using application or administration techniques or methodologies which are substantially similar to those employed with prior compositions used to treat ocular hypertension.07-16-2009
20100113447TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.05-06-2010
20100075970INHIBITORS OF AKT ACTIVITY - The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.03-25-2010
20100075969Angiogenesis - The invention provides medicaments comprising an agent, which selectively modulates β2-adrenergic receptor conformation, or receptor activity, or activation thereof. The medicaments may be used for treating diseases that are characterised by disorganized and/or abnormal vasculature, such as cancer and metastatic disease. The medicaments may also be used for promoting organized/normal branched vasculature.03-25-2010
20130079345PHARMACEUTICALLY ACTIVE DISUBSTITUTED TRIAZINE DERIVATIVES - The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.03-28-2013
20130079344OPHTHALMOLOGIC IRRIGATION SOLUTIONS AND METHOD - Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.03-28-2013
20130035339APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I):02-07-2013
20130035338EYELID TREATMENT - The current application is directed topical treatments that improve facial appearance by causing eyelids to naturally open more widely, or be more fully raised, as well as to treatment of ptosis and other eyelid-related conditions. These topical treatments include one or more of travoprost, dorzolamide hydrochloride, timolol maleate, unoprostone, latanoprost, bimatoprost, and related compounds currently used for treating glaucoma and ocular hypertension.02-07-2013
20130040950MULTISUBSTITUTED AROMATIC COMPOUNDS AS INHIBITORS OF THROMBIN - There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.02-14-2013
20100041655TRIAZOLE DERIVATIVE - An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P02-18-2010
20090156602Organic Compounds - The invention provides a pharmaceutical combination comprising: 06-18-2009
20090203697HETEROCYCLIC TYPE CINNAMIDE DERIVATIVE - Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product.08-13-2009
20090105253Triazole Derivative and Use Thereof - The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I)04-23-2009
20130072489TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof.03-21-2013
20090093481INSECTICIDAL (1,3,5)-TRIAZINYL PHENYL HYDRAZONES - (1,3,5)-Triazinyl phenyl hydrazones are effective at controlling insects.04-09-2009
20090270395EP4 Receptor Agonist, Compositions and Methods Thereof - This invention relates to potent selective agonists of the EP10-29-2009
20120225878COMPOUNDS - The present invention relates to substituted triazole compounds of the formula (I):09-06-2012
20110021526Pharmaceutical Composition for Treatment of Diabetic Complications - A method for treating diabetic complications by administration of a beta-blocker is disclosed. Diabetic complications arise from diabetes and have few or no existing treatment options. The present invention describes the use of a beta-blocker in the treatment of a diabetic. The present invention also describes the inhibition of aldose reductase, one of the chief causative factors of diabetic complications. Also provided are methods of diabetic wound healing. Compositions for treating diabetic complications, such as diabetic wounds, are disclosed. The present invention includes employing a topical formulation of a beta-blocker, having substantially no antibacterial activity, to improve the process of diabetic wound healing. The present invention also involves increasing the rate of collagen accumulation of the healing epithelialized tissue in the wound of a diabetic individual.01-27-2011
20120115868NOVEL TRIAZOLE COMPOUNDS II - The present invention is concerned with novel triazole compounds of formula (I)05-10-2012
20120238577PROSTAGLANDIN TRANSPORTER INHIBITORS AND USES THEREOF - Disclosed are compounds for inhibiting prostaglandin transporter (PGT) activity, pharmaceuticals compositions including the compounds, and methods of treating subjects using the compounds.09-20-2012
20120238576Triazine Derivatives and their Therapeutical Applications - The present invention comprises inter alia compounds as shown in formula (I) or a pharmaceutically acceptable salt thereof.09-20-2012
20090012086Use of Non-Peptidic Nk1 Receptor Antagonists for the Production of Apoptosis in Tumor Cells - The invention relates to the use of substance P antagonists and, in particular, the use of non-peptidic NK1 receptor antagonists for the treatment of cancer and, more specifically, human melanoma, neuroblastoma, glioma, human Hodgkin's lymphoma KM-H2, lymphoblastic leukaemia, human rhabdomyosarcoma, human breast carcinoma, human Burkitt's lymphoma, human lung carcinoma, human Ewing's sarcoma, human glioma and human osteosarcoma.01-08-2009
20080287440Novel Antifungal Triazole Derivatives - Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The triazole derivatives of Chemical Formula 1 or pharmaceutically acceptable salts thereof according to the present invention have excellent inhibitory activity against a broad spectrum of fungi, in addition to being safe to the body, and thus are very useful in the treatment and prevention of fungal infection.11-20-2008
20090239865DIBENZYL AMINE COMPOUNDS AND DERIVATIVES - Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.09-24-2009
20110301164METHOD OF ADMINISTERING OPHTHALMIC FLUIDS - A method is provided of treating an eye with ophthalmologically active compounds, particularly with intra-ocular pressure lowering (IOP) compounds, where a dose of 5-15 microliters is delivered at a standard concentration.12-08-2011
20110028477STABLE OPHTHALMIC FORMULATIONS - Disclosed herein are stable formulations suitable for the treatment of glaucoma and ocular hypertension.02-03-2011
20090209541APREPITANT COMPOSITIONS - Pharmaceutical compositions comprising aprepitant, wherein aprepitant solubility in aqueous media is enhanced.08-20-2009
20100298327APREPITANT POLYMORPH MIXTURES - Intimate mixtures of aprepitant crystalline Form I and crystalline Form II, having specific Hweight ratios of the forms.11-25-2010
20110003816OPHTHALMIC COMPOSITION - An ophthalmic composition comprising therapeutically effective amount of a beta-blocker and a polymeric vehicle consisting essentially of a water soluble cellulose derivative and polyvinylpyrrolidone; wherein the composition is a clear aqueous solution with a viscosity id 20 cps to 60 cps.01-06-2011
20100267725Compounds, Compositions and Methods Comprising 4N-Substituted Triazole Derivatives - The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or 2 or encompassed by formula I) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.10-21-2010
20090149462PROCESS FOR PURIFICATION OF APREPITANT - The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[1(RS)-[3,5-bis(trifluoromethyl)-phenyl)ethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation of aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, a process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having a mean particle size of less than about 11.5 microns, a process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having a content of diastereomeric impurity of 1.1% is dissolved in ethyl acetate at 70° C., the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0-5° C. to give pure aprepitant substantially free of its diastereomeric impurity.06-11-2009
20100249134Use of Beta-Adrenoceptor Antagonists for the Manufacture of a Medicament for the Treatment of Disorders of the Outer Retina - Compositions and methods for treating disorders of the outer retina with β-adrenoceptor antagonists are disclosed.09-30-2010
20090181968Novel 3-Bicyclocarbonylaminopyridine-2-Carboxamides or 3-Bicyclocarbonylaminopyrazine-2-Carboxamides - The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical compositions including the compounds are prepared or thereof: wherein, A07-16-2009
20100125076SUBSTITUTED SULPHONAMIDES, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITION COMPRISING THEREOF AND THEIR USE - Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R05-20-2010
20120270876Treatment of Conditions Through Pharmacological Modulation of the Autonomic Nervous System - Methods are provided for treating a subject for a condition caused by an abnormality in the subject's autonomic nervous system. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is pharmacologically modulated with at least one beta-blocker in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, where such conditions include various disease conditions. Also provided are systems and kits for use in practicing the subject methods.10-25-2012
20100137312NOVEL AROMATIC HETEROCYCLIC CARBOXYLIC ACID AMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel aromatic heterocyclic carboxylic acid amide derivatives of formula (I) that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.06-03-2010
20080306067Modulators of Chemokine Receptor Activity - A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3, in particular inflammatory or obstructive airway diseases.12-11-2008
20080269218Novel Hsp90 Inhibitor - Disclosed is a triazole derivative represented by the general formula (1) below or a pharmacologically acceptable salt thereof. Also disclosed are a prodrug of such a triazole derivative and an HSP90 inhibitor containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or amino group or the like.)10-30-2008
20120196860Triazine derivatives and their therapeutical applications - The invention provides Triazine derivatives and further provides methods of using these compounds to modulate protein kinases and for treating diseases and conditions mediated by protein kinases.08-02-2012
201001447341, 2, 3-Triazole derivatives as new cannabinoid-1 receptor antagonists - The present invention relates to 1,2,3-triazole derivatives which can be used as cannabinoid CB1 receptor antagonists. In addition, the compound of the 1,2,3-triazole derivatives in the present invention can be formulated into a pharmaceutical composition for treating indications relative to signal transduction of CB1 receptors.06-10-2010
20090054437Nitrocatechol Derivatives as Comt Inhibitors - New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.02-26-2009
20090137590N-LINKED HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.05-28-2009
20090163502Tetrazole-substituted arylamides as P2X3 and P2X2/3 antagonists - Compounds of the formula I:06-25-2009
20080318955Novel Thiophene Derivatives as Sphingosine-1-Phosphate-1 Receptor Agonists - The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.12-25-2008
20080261979Phenyl-1,2,4-Oxadiazolone Derivatives, Processes For Their Preparation and Methods For Their Use as Pharmaceuticals - The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula:10-23-2008
20090221585NOVEL COMPOUNDS AND THEIR USE RELATED TO COMPOSITIONS FOR TREATING DISEASE - Novel compounds and their uses are disclosed herein.09-03-2009
20090253699Compounds for Nonsense Suppression, and Methods for Their Use - The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.10-08-2009
20100160324PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES - The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R06-24-2010
20100234378ALKYLSULFONAMIDE-SUBSTITUTED TRIAZOLES AS MATRIX METALLOPROTEASE INHIBITORS - Provided are MMP-2, MMP-3, MMP-9, MMP-12 and/or MMP-13 inhibitors having the Formula (I): wherein R09-16-2010
20100240658Oxadiazole Derivatives - The invention relates to compounds of formula I:09-23-2010
20100240657CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1) wherein the groups R09-23-2010
20130217689HETEROARYLS AND USES THEREOF - This invention provides compounds of formula I:08-22-2013
20090076008DEUTERIUM-ENRICHED FOSAPREPITANT - The present application describes deuterium-enriched fosaprepitant, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090076007DEUTERIUM-ENRICHED APREPITANT - The present application describes deuterium-enriched aprepitant, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20110112094Methods of Treating Pulmonary Hypertension - Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed.05-12-2011
20090247524HSP90 Inhibitor - Compounds represented by formula (1) shown below, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such compounds are provided.10-01-2009
20100152186TRIAZOLYL PYRIDYL BENZENESULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.06-17-2010
20100227865Oligomer-Beta Blocker Conjugates - The invention provides Beta-blocker drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a different biological membrane crossing rate as compared to the biological membrane crossing rate of the Beta-blocker drug not attached to the water soluble oligomer.09-09-2010
20100056526HETEROMONOCYCLIC COMPOUND AND USE THEREOF - A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of circulatory diseases, metabolic diseases and/or central nervous system diseases.03-04-2010
20090215779OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS - Compounds of Formula (I):08-27-2009
20110251195ADRB2 GENE POLYMORPHISM ASSOCIATED WITH INTRAOCULAR PRESSURE RESPONSE TO TOPICAL BETA-BLOCKERS - The invention provides a single nucleotide polymorphism (SNP) rs1042714 in the human ADRB2 gene (Gln27Glu) associated with a clinically meaningful reduction in intraocular pressure (IOP) in a human following treatment with a topical beta-blocker. Nucleic acids comprising the SNP are used to screen glaucoma-afflicted individuals to thereby provide an improved method for genotype-based prescribing of beta-blockers in glaucoma management.10-13-2011
20110152263COMPOSITION AND METHOD FOR INHIBITING NOROVIRUS INFECTION - A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia. The composition contains a therapeutically effective amount of a binding-inhibiting compound selected from Compounds 1 through 15, and at least one diluent, carrier or excipient. The Compounds competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions can be administered to a human prior to or after infection by a Norovirus, to prevent or ameliorate an infection.06-23-2011
20110152264METHOD AND COMPOSITION FOR TREATING OCULAR HYPERTENSION AND GLAUCOMA - The present invention relates to an ophthalmic aqueous composition containing PGF2α analogues for treating ocular hypertension and glaucoma, to a method for treating ocular hypertension and glaucoma by administering said composition to a subject in need of such treatment, and to a method for increasing aqueous solubility and stability of PGF2α analogues in an aqueous composition.06-23-2011
201100772491,2,4-TRIAZOLYLAMINOARYL (HETEROARYL) SULFONAMIDE DERIVATIVES - 1,2,4-Triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I), pharmaceutically acceptable salts thereof, processes for the manufacture of 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives and pharmaceutical compositions containing 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives are disclosed:03-31-2011
20080249094COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS - The present invention relates to compounds of the Formula10-09-2008
20120202812HETEROARYLS AND USES THEREOF - This invention provides compounds of formula I:08-09-2012
20090029995HETERO BIARYL DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS - This invention provides compounds defined by Formula I01-29-2009
20120202815HETEROBICYCLE-SUBSTITUTED AZOLYL BENZENE FUNGICIDES - Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof,08-09-2012
20120202814COMPOUNDS WITH DDX3 INHIBITORY ACTIVITY AND USES THEREOF - The present invention relates to the medical use of the compound of formula 1, 2, 3 or 4:08-09-2012
20120202813TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.08-09-2012
20090118286Heterobicyclic Acrylamides - Use of heterobicyclic acrylamides of the formula (I)05-07-2009
20080280907Triazolophthalazines - The compounds of formula (I)11-13-2008
20100286149NOVEL BENZAMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel benzamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.11-11-2010
20110257177BENZYLTHIOTETRAZOLE INHIBITORS OF STORE OPERATED CALCIUM RELEASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.10-20-2011
20100144733Compounds, compositions and methods comprising heteroaromatic derivatives - The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-14 or encompassed by formulas I-XII) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.06-10-2010
20120309761FAST-RESPONSE PHOTOCHROMIC NANOSTRUCTURED CONTACT LENSES - A bicontinuous microemulsion of water, a monomer, and a surfactant copolymerizable with the monomer is polymerized to form a polymeric material, the polymeric material comprising a polymer matrix defining interconnected pores. The polymeric material may additional comprise at least one photochromic agent. The photochromic agent may be dispersed in one or both of the polymer matrix or the interconnected pores. The polymeric material may be used to form photochromic articles including ophthalmic articles such as contact lenses.12-06-2012
20100022540TRIAZOLE DERIVATIVES II - Novel triazole derivatives of the formula (I) in which R01-28-2010
20090192161Amorphous and Crystalline Forms of Aprepitant and Processes for the Preparation Thereof - An amorphous form of aprepitant and a process for its preparation is provided. Also provided are mixtures of polymorph Forms I and II of aprepitant and a process for the preparation thereof.07-30-2009
20100004242PROCESS FOR THE PREPARATION OF APREPITANT - The present invention relates to a highly pure (2R,3S)-4-benzyl-3-(4-fluorophenyl)morpholin-2-yl 3,5-bis(trifluoromethyl)benzoate of Formula II, and a process for its preparation. The present invention further provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof, using the highly pure compound of Formula II. The present invention also provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof which comprises of cyclising the compound of Formula VII at elevated temperature, in the absence of solvent.01-07-2010
20110003815DIPHENYL SUBSTITUTED CYCLOALKANES - The present invention provides compounds of Formula I which are FLAP inhibitors useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.01-06-2011
20120040985TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY - The present invention comprises TGR5 agonists of structural formula I,02-16-2012
20120040984THIADIAZOLE AND OXADIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.02-16-2012
20100029650BICYCLIC COMPOUNDS AND USE AS ANTIDIABETICS - The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.02-04-2010
20110166138Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors - Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.07-07-2011
20120015944TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I:01-19-2012
20120115869TETRAZOLE DERIVATIVES - 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.05-10-2012
20120022066Insecticidal Triazines and Pyrimidines - The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.01-26-2012
20100280032METHOD FOR TREATING INFLAMMATORY DISORDERS - The present invention relates to a method for suppressing the immune system in a subject in need thereof, and a method for treating an inflammatory or immune disorder in a subject in need thereof.11-04-2010
20110009410APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I):01-13-2011
20110009409DUAL-ACTING PYRAZOLE ANTIHYPERTENSIVE AGENTS - In one aspect, the invention relates to compounds having the formula:01-13-2011
20110092507Process for preparing R-(+)-3-morpholino-4-(3- tert-butylamino-2-hydroxypropoxy)-1,2,5-thiadiazole - The present invention provides a process for preparing optically active timolol. The process comprises the following steps. Firstly, reacting 3-hydroxy-4-morpholino-1,2,5-thiadiazole with an optically active epichlorohydrin in the presence of a solvent system, which has a first volume and a catalyst optionally in the presence of a suitable base to obtain an optically active intermediate product. Secondly, treating the optically active intermediate product with a solution, which has a second volume and comprises tert-butylamine to obtain an optically active timolol. The solvent system used in the first step can be an amide solvent, sulfoxide solvent, cyclic hydrocarbon solvent, ketone solvent, or a heterocyclic solvent. The catalyst used in the first step can be an alkali metal hydroxide, alkali metal carbonate, alkali metal hydrogen carbonate, piperidine, pyridine, triethylamine, potassium hydroxide, sodium hydroxide, potassium carbonate, and other heterocyclic bases.04-21-2011
20100093731MODULATORS FOR AMYLOID BETA - The invention relates to compounds of formula04-15-2010
20120122869TRIZAOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.05-17-2012
20120316171Tryptophan Hydroxylase Inhibitors for the Treatment of Cancer - Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.12-13-2012
20090131438Triazole derivative - A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P05-21-2009
20120129857Substituted sodium 1H-pyrazol-5-olate - The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1 H-pyrazol-5-olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.05-24-2012
20120214812COMPOUNDS AND COMPOSITIONS AS LXR MODULATORS - 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 liver X receptors (LXRs).08-23-2012
20120165333C-MET PROTEIN KINASE INHIBITORS - The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.06-28-2012
20120172361TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS - Compounds of the formula (I) and formula (II) and pharmaceutically acceptable salts thereof.07-05-2012
20120178757Method For The Prevention Of Cancer Metastasis - A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.07-12-2012
20120220591PYRIMIDONE COMPOUNDS - A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof:08-30-2012
20120225879SUBSTITUTED 5-IMINO-1,2,4-THIADIAZOLES THAT CAN BE USED TO TREAT NEURODEGENERATIVE DISEASES - The present invention is based on the use of a broad family of 5-imino-1,2,4-thiadiazoles as potential new drugs for the treatment of diseases in which PDE7 inhibition is important, specially inflammatory diseases, autoimmune and neurodegenerative disorders. On the other hand, compounds of the 5-imino-1,2,4-thiadiazole family are here described, as well as their synthetic procedures, and they may have great application as drug or drug candidates.09-06-2012
20120190682MODULATORS FOR AMYLOID BETA - The invention relates to compounds of formula07-26-2012
20120264753NOVEL 1-(BIPHENYL-4-YL-METHYL)-1H-IMIDAZOLE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME - Disclosed is a novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative represented by general formula (I), which has both angiotensin II receptor antagonist activity and PPAR-γ activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative. In general formula (I), ring A represents a group represented by formula (II) or (III); R10-18-2012
20120322804N-LINKED HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.12-20-2012
20110046136METHODS FOR THE PRODUCTION OF FUNCTIONAL PROTEIN FROM DNA HAVING A NONSENSE MUTATION AND THE TREATMENT OF DISORDERS ASSOCICATED THEREWITH - The present invention relates to functional proteins encoded by nucleic acid sequences comprising a nonsense mutation. The present invention also relates to methods for the production of functional proteins encoded by nucleic acid sequences comprising a nonsense mutation and the use of such proteins for prevention, management and/or treatment of diseases associated with a nonsense mutation(s) in a gene.02-24-2011
20120322803Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors - The present invention encompasses compounds of general formula (I)12-20-2012
201102375871,3,5-Triazine-2,4,6-Triamine Compound or Pharmaceutical Acceptable Salt Thereof, and Pharmaceutical Composition Comprising the Same - Disclosed herein are a 1,3,5-triazine-2,4,6-triamine compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for preventing or treating metabolic syndromes, diabetes, or cancers with deletion of P53 gene, which comprises the same.09-29-2011
20120277233Pyridyl-Triazine Inhibitors of Hedgehog Signaling - The invention provides pyridyl-triazine derivatives to inhibit the hedgehog signaling pathway and the use of such compounds in the treatment of hyperproliferative diseases and angiogenisis mediated diseases.11-01-2012
201202772341,2,4-OXADIAZOLE BENZOIC ACIDS - Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.11-01-2012
20110275634DUAL-ACTING PYRAZOLE ANTIHYPERTENSIVE AGENTS - In one aspect, the invention relates to compounds having the formula:11-10-2011
20110263601METHODS OF TREATING ULCERATIVE COLITIS - Methods are disclosed for treating ulcerative colitis and related diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.10-27-2011
20110319414NOVEL TRIAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides a novel P2X12-29-2011
20120101099HISTONE DEACETYLASE INHIBITORS - The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.04-26-2012
200901118111,2,4-TRIAZOLE CARBOXYLIC ACID 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
20100168108PHENYL DERIVATIVES AND METHODS OF USE - Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.07-01-2010
20100168109PHARMACEUTICAL COMPOSITIONS OF 1,2,4-OXADIAZOLE BENZOIC ACID AND THEIR USE FOR THE TREATMENT OF DISEASE - Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.07-01-2010
20120149704DISUBSTITUTED BENZAMIDE DERIVATIVES AS GLUCOKINASE (GK) ACTIVATORS - The invention relates to disubstituted benzamide derivatives of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating type II diabetes using the compounds of the invention.06-14-2012
20080249093(3,4-Disubstituted)Propanoic Carboxylates as Sip (Edg) Receptor Agonists - The present invention encompasses compounds of Formula I:10-09-2008
201202528126-PYRIMIDINYL-PYRIMID-4-ONE DERIVATIVE - A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof:10-04-2012
20130116255COMBINATION OF BRIMONIDINE AND TIMOLOL FOR TOPICAL OPHTHALMIC USE - Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.05-09-2013
20130116254COMPOSITIONS AND METHODS FOR LOWERING INTRAOCULAR PRESSURE - Disclosed herein are compositions for lowering intraocular pressure (IOP) of an eye comprising a combination of the IOP-lowering agents bimatoprost, brimonidine, and timolol. Further disclosed are methods for reducing IOP in the eye of a subject.05-09-2013
20130116251Novel HSP90 Inhibitor - Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.)05-09-2013
20130116253Novel HSP90 Inhibitor - Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.)05-09-2013
20130116252Novel HSP90 Inhibitor - Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.)05-09-2013
20130143883MODULATORS FOR AMYLOID BETA - The invention relates to compounds of formula06-06-2013
20080200462SUBSTITUTED PYRAZOLE AND TRIAZOLE COMPOUNDS AS KSP INHIBITORS - Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:08-21-2008
20110275635SMALL MOLECULE INHIBITORS OF NADS, NAMNAT, AND NMNAT - Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors.11-10-2011
20110257176NITROGEN HETEROCYCLE DERIVATIVES AS PROTEASOME MODULATORS - A method for treating and/or ameliorating and/or preventing a disease or a disorder, the method comprising administering to an individual in need thereof at least one nitrogen heterocycle derivative of formula (I):10-20-2011
20130150365Insecticidal Triazines and Pyrimidines - The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.06-13-2013
20100286148PYRIDINE COMPOUND, PESTICIDAL COMPOSITION AND METHOD OF CONTROLLING PEST - A pyridine compound represented by the following general formula (1); the pyridine compound in which R11-11-2010
20100317664METHODS OF AFFECTING GASTROINTESTINAL TRANSIT AND GASTRIC EMPTYING, AND COMPOUNDS USEFUL THEREIN - Methods and compounds are disclosed for affecting gastrointestinal motility and gastric emptying, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof12-16-2010
20120028980USE OF NK-1 RECEPTOR ANTAGONISTS IN MANAGEMENT OF VISCERAL PAIN - Methods for managing visceral pain in mammalian subjects are described, in which a NK-1 receptor antagonist is administered to the subject before, during or after administration of general anesthesia. The methods and uses of NK-1 receptor antagonists described herein provide improved visceral pain management and MAC reduction when used with volatile anesthetics for general anesthesia.02-02-2012
20130196994PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.08-01-2013
20130196995COMBINATION OF BRIMONIDINE AND TIMOLOL FOR TOPICAL OPHTHALMIC USE - Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.08-01-2013
20130203758Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.08-08-2013

Patent applications in class Three or more ring hetero atoms in the additional hetero ring