Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.

Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.

Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.

Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.

Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.

Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, wherein the variables G, T, D, L, A, X, R1 and R2 are as described hereinabove, and their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.

Abstract: The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification.

Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.

Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the treatment or prophylaxis of various disorders of humans or animals.

Abstract: The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.

Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.

Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.

Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.

Abstract: 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.

Abstract: The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.

Abstract: An isoxazole derivative is provided. The isoxazole derivative has following formula: wherein R1, R2, R3, R4 and R5, independently, include hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis and cancer including an isoxazole derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.

Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.

Abstract: The invention relates to a compound of the general formula (I), where: R is a hydrogen atom or a group selected from the (C1-C6)alkyl or (C3-C7)-cycloalkyl groups, optionally substituted by one or more groups independently selected from a halogen atom anti the (C3-C7)-cycloalkyl, (C1-C6)alkyl, (C1-C6)alkoxy, and hydroxy groups; R1 is a phenyl group optionally substituted by one or more substituents independently selected from halogen atoms and the (C1-C6)alkyl, (C1-C6)alkoxy, halo-(C1C6)alkyl, hydroxy, halo-(C1-C6)alkoxy, (C1-C6)alkyl-thio, (C1-C6)alkyl-SO, and (C1-C6)alkyl-SO2 groups; R2 is one or more substituents selected from a hydrogen atom, halogen atoms, and the halo-(C1-C6)alkyl, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)-cycloalkyl-(C1C3)alkyl, phenyl, benzyl, (C1-C6)alkoxy, (C1-C6)alkyl-thio, (C1-C6))alkyl-SO, and (C1-C6)alkyl-SO2 groups; and Het is a heteroaryl group; wherein said compound is in the form of a base or an acid addition salt.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.

Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.

Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.

Abstract: Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract: The present invention provides a process for the preparation of the compound 1-[5-(3-chloro-phenyl)-isooxazol-3-yl]-ethanone: Wherein the compound 5-(3-chlorophenyl)-isooxazol-3-carboxylate is reacted with CH3MgX. The present invention also provides a process for the preparation of (R)-1-[5-(3-chloro-phenyl)-isooxazol-3-yl]-ethanol: Wherein 1-[5-(3-chloro-phenyl)-isooxazol-3-yl]-ethanone is reduced to (R)-1-[5-(3-chloro-phenyl)-isooxazol-3-yl]-ethanol.

Abstract: The invention relates to sulfoximinamid compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the sulfoximinamid compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such sulfoximine compounds. The sulfoximinamid compounds of the present invention are defined by the following formula I: wherein Q, Het, R1, R2, R3, R4 and n are defined as in the description.

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.

Abstract: The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R1)(R2)—, —C(R3)?, —N(R4)—, —N?, —N+(R5)?, —O— and —S—; M and Z are independently nondirectionally selected from formula (I) and formula (II).

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.

Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).

Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.

Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.

Abstract: Novel isoxazoline compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for use on non-human animals.