Abstract: Arylpiperazines of Formula I useful as metalloproteinase inhibitors, especially as MMP13 inhibitors.

Abstract: There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17?-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.

Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4-R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9-R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, gra

Abstract: Certain 1,4-dihydropyridine compounds, useful as adrenergic blocking agents and as calcium channel blocking agents, the compounds having the formula wherein R1 is hydrogen, halogen, C1-6-alkyl, or C1-6-alkoxy, R3 is hydrogen, halogen, C1-6-alkyl, C1-6-alkoxy, or CF3(CH2)nO— wherein n is 1, 2, or 3, and R5 is —NHCH2CH2O— or —N(CH2CH2)2N—.

Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.

Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: There are disclosed compounds of the formula (I): 1

Abstract: The invention relates to the compounds of formula: 1

Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4—R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ═O, ═NOR10, ═N—NR11R12 or ═CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, al

Abstract: The use of CCR5 antagonists of the formula 1

Abstract: One aspect of the present invention relates to piperidine-piperazine compounds generically represented by A. A second aspect of the present invention relates to the use of the piperidine-piperazine compounds as ligands for various mammalian cellular receptors or transporters or both, including dopamine, serotonin or norepinephrine receptors or transporters, any combination of them, or all of them.

Abstract: Substituted heterocyclic compounds for treating multidrug resistance are disclosed. Compositions and methods of use for the substituted heterocyclic compounds are disclosed.

Abstract: Compounds having the formula 1

Abstract: Formula (1) wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen, or a C1-4 alkyl group; R4 represents a trifluorometyl group; R5 represents hydrogen, a C1-4 alkyl group or C(0)R6; R6? represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3 and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation and their use in the treatment of conditions mediated bytachykinins.

Abstract: What is described are amides of the formula (I) and salts thereof, 1

Abstract: Selected substituted piperidine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Compounds having the formula 1

Abstract: There are disclosed compounds of the formula (I): 1

Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: The present invention relates to compounds of the formula wherein each A is independently halo; Y is —(CH2)m—, —C(O)— or —S(O)—; R1 and R2 are independently C1-4 alkyl; R3 is substituted azacycloalkyl etc.; R4 is phenyl substituted at the 2-position with a substituent selected from substituted C1-7 alkyl, substituted C1-7 alkoxy, amine, etc; R5 is hydrogen or C1-4 alkyl; m is 0, 1 or 2; and n is 0, 1, 2, 3, 4 or 5. The present invention also relates to pharmaceutical compositions containing such compounds and to the use of such compounds in the treatment and prevention of inflammation, asthma, allergic rhinitis, pain and other disorders.

Abstract: The present invention relates to substituted piperidines of general formula 1

Abstract: The invention relates to novel pyridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors

Abstract: Compounds of formula IIA and IIB are novel guanidine compounds 1

Abstract: The present invention provides an anti-inflammatory medicament and an inhibitor of intraocular pressure rise due to laser irradiation, which contains 1,4-dihydropyridine derivative of the formula (I) wherein X1 and X2 are the same or different and each is hydrogen atom, fluoromethyl, fluoromethoxy, halogen, cyano or nitro, R1 is lower alkyl, R2 is acyl, alkoxycarbonyl, acylalkyl, N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, hetero ring-alkyl, haloalkyl, alkenyl or alkynyl, A is alkylene having a carbon atom bonded with two alkyls and 5 or more carbon atoms in total, and m is an integer of 1 to 3, or an acid addition salt thereof, as an active ingredient.

Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1

Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

Abstract: This invention relates to compounds which are generally muscarinic receptor antagonists and which are represented by Formula I: 1

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: This invention relates to a series of N-heterocyclyl hydrazides of Formula I, 1

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of oxadiazole, thiadiazole and thiadiazole oxide derivatives of dihydropyridines of Formula I. wherein B is with X being O, S or and X1 is O or S. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: This invention relates to novel lactams having the Formula (I): 1

Abstract: The present invention relates to novel 6-methylnicotinamide derivatives and their pharmaceutically acceptable salts, the process for preparing them, and the pharmaceutical compositions containing said compounds as active ingredients. The 6-methylnicotinamide derivatives of the present invention exhibit their inhibitory activity against the proliferation of human immunodeficiency virus (HIV) as well as hepatitis B virus (HBV) and Hepatitis C virus (HCV), such that they can be used for hepatitis B, hepatitis C and acquired immune deficiency syndrome (AIDS).

Abstract: This invention provides compounds of formula I: 1

Abstract: In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor.

Abstract: The use of CCR5 antagonists of the formula 1

Abstract: Ortho, ortho-substituted nitrogen-containing bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.

Abstract: The invention disclosed some 1,4-dihydropiridine derivative chemically have pharmacologically with adrenoceptor blocking and calcium channel blocker is now emerging.

Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent; R2 is Ar2, Ar2C1-6alkyl, Het1 or Het1C1-6alkyl; R3 is hydrogen or C1-6alkyl; L is hydrogen; Ar3; C1-6alkyl; C1-6alkyl substituted with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar3, Ar3C1-6alkyloxy and Het2; C3-6alkenyl; Ar3C3-6alkenyl; di(Ar3)C3-6alkenyl or a radical of formula (a-1), (a-2), (a-3), (a-4) or (a-5); Ar1, Ar2 and Ar3 are each phenyl or substituted phenyl; Het1 and Het2 are each monocyclic or a bicyclic heterocycles; as substanc

Abstract: Compounds of the formula 1

Abstract: The present invention is directed to novel 1-(N-phenylaminoalkyl)piperazine derivatives substituted at the position 2 of the phenyl ring. Pharmaceutical compositions comprising the compounds of the invention also are contemplated. The compounds of the present invention also are contemplated for use in treating neuromuscular dysfunction of the lower urinary tract in a mammal.

Abstract: Novel compounds of the formula I in which X, Y, R1, R2 and R3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.

Abstract: Compounds of the present invention are 4-phenyl-pyridine derivatives with activity as NK-1 receptor antagonists.

Abstract: The preparation of 1-(3-carboxypyridyl-2)-4-methyl-2-phenylpiperazine dihydrate and other mirtazapine intermediates are described. These compounds are particularly useful in the preparation of mirtazapine.

Abstract: The present invention relates to compounds of the formula 1

Abstract: The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D represents the group —V—(CH2)p—COOR, wherein R represents a hydrogen atom. The compound inhibits the aggregation of platelets via the inhibition of the linkage of the platelet membrane protein GPIIb/IIIa to fibrinogen. wherein A represents CH2 or CO, B represents the group —(CH2)k— or —(CH2)m—CO—, X and Y are different from each other and represent N or CH, W represents an ester moiety which can be removed under the physiological condition, and Z represents the groups (II) or (III): wherein D represents the group —V—(CH2)p—COOR.

Abstract: The invention relates to compounds of the formula 1

Abstract: Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment and control of obesity, diabetes, and sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.