Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.

Abstract: The invention is directed to 1-methyl-benzo[1,2,4]thiadiazine 1-oxide derivatives and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: The invention is directed to 5,5-disubstituted-indolizinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: The invention is directed to pyridazinone compounds of Formula I and pharmaceutical compositions containing compounds of Formula I wherein R1 and R2 are independently H, alkyl, cycloalkyl, aryl, or heterocyclyl; and Ring A is 5 or 6-membered aryl or heterocyclyl. The invention also encompasses methods of using a compound of Formula I in the treatment of hepatitis C virus infections.

Abstract: Compounds of formula (I): wherein: R1 represents hydrogen, a halogen or alkyl, R1a represents hydrogen or alkyl, R2 represents hydrogen, a halogen or hydroxy, A represents NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, X is as defined in the description, their isomers, and also addition salts thereof. Medicinal products containing the same which are useful in treating disorders of the AMPA system.

Abstract: The invention is directed to saturated fused [1,2-b]pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: The invention is directed to pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: Compounds of formula (I): wherein A represents a 5, 6 or 7-membered (hetero)aromatic or non-aromatic ring, n and n? represent 0, 1 or 2 X represents an alkylene chain as defined in the description, R3 represents an aryl or heteroaryl group, one of the groups R1 and R2 represents a hydrogen atom and the other represents a group of formula (II) as defined in the description. Medicinal products containing the same which are useful in treating conditions involving a defect in apoptosis.

Abstract: Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.

Abstract: The invention relates to compounds of formula (I): wherein: R1 represents alkyl substituted by one or more halogen atoms, R2 represents hydrogen, halogen or hydroxy, R3 represents unsubstituted or substituted aryl, their isomers, and also addition salts thereof. and medicinal products containing the same which are useful in treating or preventing disorders associated with AMPA flux.

Abstract: Compounds of formula (I): wherein: RF represents monofluoro- or polyfluoro-alkyl or monofluoro- or polyfluoro-cycloalkylalkyl, R1 represents hydrogen or a group selected from alkylaminocarbonyl and optionally substituted alkyl, R2 represents hydrogen, halogen or a group selected from cycloalkyl and optionally substituted alkyl, R3 to R6, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, nitro, cyano, alkylsulphonyl, hydroxy, alkoxy, optionally substituted alkyl and optionally substituted amino, its optical isomers when they exist, and also their addition salts with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as AMPA modulators.

Abstract: The invention relates to compounds of formula (I): wherein: X represents oxygen or sulphur, R1 represents linear or branched (C1-C6)alkyl substituted by one or more halogen atoms, R2 represents hydrogen, halogen or hydroxy, R3 represents a group R4 or —Y—R5 wherein R4, Y and R5 are as defined in the description, and medicinal products containing the same which are useful in treating or preventing disorders associated with AMPA flux.

Abstract: The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A represents CR3R4 or NR3 wherein R3 and R4 are as defined in the description, Y represents an alkylene chain as described in the description, X represents NR5R6, S(O)nR7, OR8, C(O)R9, amidino or a heterocycle, their isomers, and addition salts thereof; and medicinal products containing the same which are useful in the prevention or treatment of diseases associated with AMPA flux.

Abstract: Compounds of formula (I): wherein: R1 represents hydroxy or RCO—O—, R2 represents hydrogen, halogen, hydroxy or R?CO—O, R, R?, which may be identical or different, represent linear or branched (C1-C6)alkyl optionally substituted by aryl, linear or branched (C2-C6)alkenyl optionally substituted by aryl, linear or branched (C1-C6)perhaloalkyl, (C3-C7)cycloalkyl, adamantyl, aryl or heteroaryl, R3 represents hydrogen, linear or branched (C1-C6)alkyl or (C3-C7)cycloalkyl, A represents CR4R5 or NR4, R4 represents hydrogen or linear or branched (C1-C6)alkyl, their isomers and also their addition salts with a pharmaceutically acceptable acid or base. Medicaments.

Abstract: The invention provides novel compounds represented by the general formula compound represented by the formula: wherein the bond represented by the broken line may be a single, a double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or C?O or CH2; Y represents —CH(R4)—, —N(R4)— or —N(R4)—CH2—, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application The compounds are useful as positive modulators of the AMPA-receptor.

Abstract: A yellow dye-forming coupler represented by formula (I): wherein Q represents a group of nonmetallic atoms that form a 5- to 7-membered ring in combination with the —N?C—N(R1)—; R1 and R2 each represent a substituent; R4 represents an alkyl group; m represents an integer of 0 to 4; and X represents a hydrogen atom, or a group capable of being split-off upon a coupling reaction with an oxidized product of a developing agent; and when R4 represents a primary alkyl group, R1 represents —(CH2)3O—R101 in which R101 is an alkyl group having 4 to 8 carbon atoms. A silver halide color photographic light-sensitive material having at least one yellow dye-forming coupler represented by formula (I) in at least one layer provided on a support.

Abstract: A yellow dye-forming coupler represented by formula (I): wherein Q represents a group of nonmetallic atoms that form a 5- to 7-membered ring in combination with the —N?C—N(R1)—; R1 and R2 each represent a substituent; R4 represents an alkyl group; m represents an integer of 0 to 4; and X represents a hydrogen atom, or a group capable of being split-off upon a coupling reaction with an oxidized product of a developing agent; and when R4 represents a primary alkyl group, R1 represents —(CH2)3O—R101 in which R101 is an alkyl group having 4 to 8 carbon atoms. A silver halide color photographic light-sensitive material having at least one yellow dye-forming coupler represented by formula (I) in at least one layer provided on a support.

Abstract: This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X-Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: A dye-forming coupler of the formula (I). A silver halide photographic light-sensitive material that contains at least one dye-forming coupler of the formula (I). A method for producing an azomethine dye, which method comprises using a compound of the formula (I): wherein E is an aryl, heterocyclic, or —C(?O)W group, in which W is a nitrogen-containing heterocyclic group, Z is an aryl or heterocyclic group, and X and Y each independently are ?O, ?S or ?N—R, in which R is a substituent, with the proviso that when E is an aryl or heterocyclic group, X and Y each are ?O, and that when E is a —C(?O)W group, Z is a substituted aryl group.

Abstract: The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or C?O of CH2; Y represents —CH(R4)—, —N(R4)—CH2—, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application. The compounds are useful as positive modulators of the AMPA-receptor.

Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.

Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and othe S9 proteases that comprise a compound comprising the formula: 1

Abstract: The present invention relates to modified amino acids of general formula 1

Abstract: A compound represented by the formula I: 1

Abstract: Compounds having the formula 1

Abstract: Compounds useful as HCV anti-infectives having the formula: wherein the formula variables are as defined herein, are disclosed. Also disclosed are methods of making and using the same.

Abstract: Compounds having the formula 1

Abstract: Compounds having the formula 1

Abstract: The present invention relates to a novel processes for preparing pharmaceutically active compounds of formula (I): 1

Abstract: Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.

Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.

Abstract: A compound of Formula I 1

Abstract: This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: 1

Abstract: The present invention relates to modified amino acids of general formula 1

Abstract: The present invention relates to a novel processes for preparing pharmaceutically active fused 1,2,4-thiadiazine derivatives of general formula (I) as defined in the description and intermediates therefore.

Abstract: The present invention involves certain 8-ureido and 8-thioureido, 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the chemokine, Interleukin-8.

Abstract: 1,2,4-Benzothiadiazine derivatives represented by formula wherein D, R1, R2, R3, R4, R5, R12, R13, R14, R15 are defined in the description, composition thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.

Abstract: Substituted cyclohexanol esters, their use for treating diseases, and pharmaceutical preparationsCyclohexanol esters of the formula I ##STR1## are described in which the radicals have the meaning given herein. The compounds are pharmacologically active and my therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.

Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.

Abstract: A benzothiadiazine derivative, hydrate thereof and acid addition salt thereof, the derivative being represented by the general formula (I) ##STR1## wherein X is methylene or a nitrogen atom substituted with a lower alkyl, Y and Z are each methylene or carbonyl, A is phenylene or phenylene substituted with methoxycarbonyl, R.sub.4 is lower alkylene or lower alkenylene, R.sub.1 is a hydrogen atom, acetoxyacetyl, cyclohexylmethyl or benzyl wherein the benzene ring may be substituted with lower alkoxyl, halogen atom, nitro, lower alkyl, methylenedioxy or hydroxyl, R.sub.2 is lower alkyl or phenyl, and R.sub.3 is a hydrogen atom, halogen atom or lower alkoxyl with the exception of the case where X, Y and Z are each methylene, A is unsubstituted phenylene, R.sub.4 is lower alkylene and R.sub.1 is a hydrogen atom; and a peptic ulcer treating agent containing as an effective component the above derivative, hydrate thereof or acid addition salt thereof.

Abstract: Novel compounds having the formula ##STR1## wherein R.sub.1, R.sub.2, X and Y are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.

Abstract: The invention relates to compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and Q are as described, useful in the treatment of ulcers.

Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.

Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.

Abstract: Aryloxy-aminoalkanes useful as antihypertensive agents are described and disclosed.

Abstract: The invention relates to substituted 2-pyrimidinyl-1- piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.

Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

Abstract: Fungicidal trisubstituted 1,3,5-triazine-2,4,6-triones of the formula ##STR1## in which R.sup.1 stands for an optionally substituted aliphatic, aromatic or cycloaliphatic radical,R.sup.2 stands for an optionally substituted aliphatic radical andR.sup.3 stands for optionally substituted, heterocyclically fused phenyl.