Abstract: There is provided compounds of formula I, wherein X1, T, Y, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.

Abstract: The present invention relates to a process for the preparation of an enantiomerically enriched optionally substituted indoline-2-carboxylic acid or a salt thereof, wherein an enantiomerically enriched chiral ortho-X-substituted phenylalanine compound, wherein X is a leaving group, is subjected to cyclisation, preferably at a temperature of below about 140° C., upon formation of the enantiomerically enriched indoline-2-carboxylic acid compound.

Abstract: Indole indane amides which are CB2 agonists are provided which have the structure wherein R1, R2, R3, R4 and R5 are as defined herein, which compounds are useful in treating autoimmune diseases, inflammation, pain, cardiovascular disorders and other diseases mediated by CB2 receptors. A method for preventing or treating such diseases employing the compounds of the invention is also provided.

Abstract: Provided herein are Compounds having the following structure: wherein A, L, X and ring B are as defined herein, compositions comprising an effective amount of a Compound and methods for treating or preventing cancer, hypoxia, diabetes, stroke, autoimmune disease or a condition treatable or preventable by inhibition of Chk2, the ATM-Chk2 pathway or RSK2 comprising administering an effective amount of a Compound to a patient in need thereof.

Abstract: The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them.

Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.

Abstract: The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof.

Abstract: Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.

Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I). The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention.

Abstract: A process for preparation of crystalline perindopril erbumine of formula (II) which exhibits the X-ray (powder) diffraction pattern like that shown in FIG. 2 The process comprises reacting a solution of perindopril of formula (I), in a solvent selected from N,N-dimethylformamide, dimethyl acetals of lower aliphatic aldehydes, dimethyl ketals of lower aliphatic ketones and 1,2-dialkoxyethane with tertiary butylamine and crystallization of the erbumine salt thus obtained by heating the reaction mixture to reflux, filtering hot, cooling gradually to 20° C. to 30° C., and further cooling to 0° C. to 15° C. for 30 minutes to 1 hour and finally filtering off and drying the crystals.

Abstract: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur.

Abstract: N-(benzenesulphonyl)-2,3-dihydro-1H-indols, wherein the indol is substituted by cyano, carboxy or alkylcarbonyloxy and their use as therapeutical agents.

Abstract: Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them.

Abstract: To provide an enzymatic resolution process for efficiently producing an optically active N-protected-octahydro-1H-indole-2-carboxylic acid denoted by the formula (2): by using an enzyme capable of asymmetrically hydrolyzing the —CO2R1 group in the formula (1) wherein R1 indicates an alkyl group having a carbon number of 1 to 4, R2 indicates a protecting group of the imino group, and the carbon atoms marked with asterisks (*) indicate asymmetrical carbon atoms.

Abstract: A compound of the following formula: in which R1, R2, R3, U, V, T, W, X, Y, Z, m, n, p, x, y, and z are as defined herein. Also disclosed are (1) a pharmaceutical composition containing such a compound, and (2) a method for treating Hepatitis C virus infection using such a compound.

Abstract: The present invention relates to 5-hydroxy-indole-3-carboxylate derivatives of formula I, or racemic mixture or optical isomers or pharmaceutically acceptable salts and/or hydrates thereof, wherein: substituents R1, R2, Z, X and Y are as defined in the description. The compounds of formula I can be useful for preparation of medicament for treatment and/or prophylaxis of virus infections, especially for preparation of medicament for anti-HBV (Hepatitis B virus) and anti-HIV (Human immunodeficiency virus).

Abstract: The present invention provides indole inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.

Abstract: Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound and pharmaceutically acceptable salts thereof, and methods of using said compounds. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

Abstract: The invention relates to novel diazoketone derivatives. The invention also relates to processes for homologation of these diazoketone derivatives. The processes are useful for preparing compounds that are caspase inhibitors.

Abstract: The present invention provides indole compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables ring A, X1, X2, X3, X4, R6, and R15 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

Abstract: The invention relates to compounds of Formula (1) for use in modulating potassium channel activity in cells.

Abstract: 3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HIV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other anti-viral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds.

Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using N-linked sulfonamides of heterocyclic thioesters.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia, e.g. myocardial ischemia, or as cardioprotectants or inhibitors of abnormal cell growth.

Abstract: The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R1, R2 and R3 are as described herein. The invention further discloses processes for preparing them, and novel intermediates therefor.

Abstract: A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4)alkyl or (C1-C4)alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.

Abstract: Compounds according to formula I: wherein R1, W, R2, R3, X, R4 and R5 are as described in the specification, enantiomers thereof, pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission.

Abstract: A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.

Abstract: Combinatorial libraries that contains various different 4, 5 fused 3-substituted-2-pyrrolocarboxylic acids for screening pharmacological activity and methods of synthesizing said libraries.

Abstract: There is provided a compound of formula (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.

Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.

Abstract: A dicyclohexyamine salt of compound of formula I, namely perindopril, having an X-ray powder diffraction pattern with characteristic peaks (2?): 8.462, 10.624, 18.693, 9.424, 17.272, 14.177, 19.499, 20.765, 21.409, and 14.540. A process for preparation of the said salt of perindopril and its use in the purification of an impure perindopril and a process for purification of perindropril comprising formation of its salt with dicyclohexylamine. The present invention also relates to preparation of Perindopril tert-butyl amine salt directly from Perindopril dicyclohexylamine salt without isolating the free base.

Abstract: Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound and pharmaceutically acceptable salts thereof, and methods of using said compounds. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.

Abstract: Compounds of the formula (1): in which A, R1, R2 and R3 are as defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.

Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.

Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.

Abstract: The present invention provides a compound of the Formula: a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, wherein m, n, Ar1, R1, R2, R3, R4, and R5 are those defined herein. The present invention also provides methods for using and preparing compounds of Formula I.

Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.

Abstract: 1. An aromatic amino acid derivative represented by the formula (I) or its pharmacologically acceptable salt: wherein, R1 is a hydrogen atom or an amino-protecting group, R2 is a halogen atom or an alkyl, aralkyl or aryl group, R3 is {circle around (1)} a hydrogen atom, {circle around (2)} an aroylamino group, {circle around (3)} a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. {circle around (4)} a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, {circle around (5)} an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, {circle around (6)} an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; l is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5.

Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic esters and amides.

Abstract: The invention relates to 1-{2(S)-[1(S)-(ethoxycarbonyl)butylamino]propionyl}-(3aS,7aS)octahydroindol-2(S)-carboxylic acid of the Formula I and the t-butylamine salt of the Formula I? thereof free of contaminations derivable from dicyclohexyl carbodiimide, and a process for the preparation thereof. The invention also relates to new intermediates of the general Formula III (wherein R stands for lower alkyl or aryl lower alkyl). The compound of the Formula I—perindopril—is a known ACE inhibitor.

Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.

Abstract: Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN—COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an ?,?-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.

Abstract: A process for preparing perindopril is provided comprising condensing an N-[(S)-1-carbethoxybutyl]-(S)-alanyl halide of formula II: wherein X is a halide with an (2S,3aS,7aS)-2-carboxyperhydroindole of formula III: wherein R is hydrogen or a protecting group.

Abstract: The present invention provides novel polymorphic and pseudopolymorphic forms of Trandolaprilat, including crystalline Trandolaprilat Form A, crystalline Trandolaprilat Form B, crystalline Trandolaprilat Form C, crystalline Trandolaprilat Form D, crystalline Trandolaprilat Form E, and mixtures thereof. The invention also provides novel methods for producing Trandolaprilat, pharmaceutically acceptable salts of Trandolaprilat, and polymorphic and pseudopolymorphic forms of Trandolaprilat, pharmaceutical compositions including one or more novel Trandolaprilat compounds and methods for treating high blood pressure and/or cardiac insufficiency using one or more novel Trandolaprilat compounds.

Abstract: This invention relates to novel compositions and uses of N-heterocyclic carboxylic acids and carboxylic acid isosteres for treating a vision disorder, improving vision, treating memory impairment or enhancing memory performance in an animal.

Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.