Abstract: Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.

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: The present invention relates to a novel sulfonamide derivatives and novel intermediates thereof, preparation thereof, and a pharmaceutical composition comprising the same, and more particularly, to novel sulfonamide derivatives and intermediates thereof that are used as angiogenesis controlling material and that can inhibit overexpression of matrix metalloproteinase that decomposes protein constituents in extracellular and basement membranes of connective tissues, and preparation methods thereof, and a pharmaceutical composition comprising the same.

Abstract: Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are pharmaceutical compositions, methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion, which involve compounds of Formula I.

Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

Abstract: 4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine hydrochloride and its hydrates, processes for preparing this benzoylguanidine salt and its hydrates, pharmaceutical compositions containing this benzoylguanidine salt and its hydrates, and its use in treating diseases, particularly those in which inhibition of the cellular Na+/H+ exchange is of therapeutic benefit.

Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula IIIB have the structure: wherein R1, R2, R, Ar and n are as described in the specification.

Abstract: This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa..

Abstract: PDF inhibitors and novel methods for their use are provided.

Abstract: 4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine hydrochloride and its hydrates, processes for preparing this benzoylguanidine salt and its hydrates, pharmaceutical compositions containing this benzoylguanidine salt and its hydrates, and its use in treating diseases, particularly those in which inhibition of the cellular Na+/H+ exchange is of therapeutic benefit.

Abstract: PDF inhibitors and novel methods for their use are provided.

Abstract: Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

Abstract: A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and the like); M represents an alkylene linking group (a carbon atom constituting the carbon chain may be replaced with a nitrogen atom, an oxygen atom and the like); X represents —S—, —O—, —NR4—, —NR5—CO— and the like (R4 and R5 represent a hydrogen atom, a lower alkyl group and the like) or a single bond; Y represents an alkyl group, an aryl group, an amino group, an aromatic heterocyclic group and the like; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower acyl group; and R21, R22 and R23 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like] or a salt thereof.

Abstract: Disclosed are multibinding compounds which are &bgr;2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Methods of and compositions for pulmonary delivery of therapeutic agents which are capable of forming covalent bonds with a site of interest or which have formed a covalent bond with a pulmonary solution protein are disclosed. Therapeutic agents useful in the invention include wound healing agents, antibiotics, anti-inflammatories, anti-oxidants, anti-proliferatives, immunosupressants, anti-infective and anti-cancer agents.

Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.

Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1&bgr; secretion.

Abstract: The present invention relates to a compound of formula (I); wherein R1 represents isopropyl or trifluoromethyl; R2 represents hydrogen, C1-4alkyl, chloro, fluoro or trifluoromethyl; R3 represents(i) phenyl, optionally substituted by cyano, halogen, trifluoromethyl or an optionally substituted 5-membered heteroaromatic group, where optional substitution is effected by C1-4alkyl, (ii) a 5-membered heteroaromatic group, optionally substituted by halogen, cyano or C1-4alkyl, (ii) aminocabonyl, or(iv) ethyl or eth-1-enyl; R4 represents cyano, methyl, acetyl, a 5-membered heteoaromatic group, optionally substituted by C1-4alkyl or phenyl or a group X—Y-Z; X represents a carboxy, oxo, C1-6alkylene, carboxamido or thiocarboxamido linking group; Y represents a direct link or C1-4alkylene, Z represents (i) hydrogen, (ii) trifluoromethyl, (iii) cyano, (iv) phenyl (v) a 5- or 6-membered heteroaromatic group, optionally substituted by C1-4alkyl, with the proviso that when X represents C1-4alkylene, Y and Z do not re

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Compounds of the formula (I) as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.

Abstract: The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) 1

Abstract: The invention relates to compounds represented by the formula I 1

Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.

Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.

Abstract: A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described.

Abstract: Compounds having the formula 1

Abstract: Novel &bgr;-aryl-&agr;-substituted propanoic acids having hypolipidemic and hypocholesteremic activities.

Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.

Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: where R1 is an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine, said R1 further comprising a cyclic or bicyclic structure; R2 is methyl, CH2CH3, (CH2)2CH3, C(CH3)3, phenyl, 3,4-dichiorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH2-(N-Boc-4-piperidine), 4-tetrahydropyran, CH2-4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl; R3 is R2 or C3-8alkyl, R4 is C1-3alkyl; and R5 is NH2, OH, NHOH, NHOCH3, N(CH3)OH, N(CH3)OCH3, NHCH2CH3, NH(CH2CH3), NHCH2(2,4-(OCH3)2Ph, NHCH2(4-NO2)Ph, NHN(CH3)2, proline, or 2-hydroxymethyl pyrrolidine.

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.

Abstract: The invention discloses a novel series of compound represented by general formula (I), 1

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: Selected substituted piperazine 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: This invention relates to a series of arylsubstituted piperazines, of Formula I 1

Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof; wherein a, b, c, d, e, j, R1, R2, R3, and R4 are as defined herein and are useful to treat inflammation and other immune disorders.

Abstract: The present invention is a series of compounds that are derivatives of 1-sulfonyl-pyrrolidine and that demonstrate affinity towards metabotropic glutamate receptors. The invention further relates to medicaments containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.

Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.

Abstract: The invention provides compounds of Formula (I): 1

Abstract: A compound represented by the following formula (12) useful as an intermediate for production of drug or agricultural chemical: 1

Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Abstract: The present invention relates to new derivatives of amino acids and their use as medicaments.

Abstract: The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives showing superior antioxidant activity compared to the known antioxidant compounds, their pharmaceutically acceptable salt, and pharmaceutical compositions containing them. It can be usefully used in treating neurodegerative diseases such as aging, cancer, diabetes, ischemic stroke, Parkin's disease, dementia and Huntinton's disease.

Abstract: A NK1 antagonist having the formula (I), 1

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