Abstract: A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4?-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: Compounds of formula (I) are novel CNS active agents that are useful for treating pain and for treating other disorders associated with the cholinergic system.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: The present invention describes novel compounds of Formula I which inhibit HIV integrase.

Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.

Abstract: An adamantanetricarboxylic acid derivative is represented by following Formula (1): wherein X is a hydrogen atom or a hydrocarbon group; and R1, R2 and R3 may be the same as or different from one another and are each a carboxyl group which may be protected by a protecting group, or a carbonyl halide group, wherein at least one of R1, R2 and R3 is a carboxyl group which is protected by a protecting group, or a carbonyl halide group.

Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract: This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound. The Benzopyranone Compounds have the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is halogen, trifluoromethyl or C1-6 alkyl.

Abstract: A method for preparing 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide (I), a key intermediate in the synthesis of atorvastatin calcium, is described

Abstract: The invention relates to novel ligands of the phosphanylbenzothiophenyl-dihydroisoxazoline, phosphanyl-dihydrooxazolyl-indole and phosphanyl-dihydrooxazolyl-benzofuran type, especially compounds of formula I and mixtures of such compounds, wherein X is oxygen, sulfur, selenium or NQ, wherein Q is unsubstituted or substituted aryl, or alkyl or substituted alkyl; n is 0, 1, 2, 3 or 4; A1 and A2 are each an organic radical capable of bonding to phosphorus, especially unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted cycloalkyl, or —N(D)2 wherein D2 is alkyl or substituted alkyl; or A1 and A2 together with the bonding phosphorus atom form a ring, which may be unsubstituted or substituted; Y, Y?, Y? and Y?? are each independently of the other hydrogen or alkyl, substituted alkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heterocyclyl, at least one of the radicals Y, Y?, Y? or Y?? being one of

Abstract: The invention relates to particular hydroxyl and protected hydroxyl derivatives of compounds known to be useful as HMG CoA-reductase inhibitors. In particular, herein are provided hydroxyl and protected hydroxyl compounds of Formula I and their corresponding lactones.

Abstract: Novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, A, R4 and m have the meanings given in the description, a number of processes for preparing these substances, and their use for controlling pests, and also novel intermediates and their preparation.

Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to 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: Novel azetidinyl and pyrrolidinyl compounds are ligands of melanocortin-4 receptors and are useful for treating conditions responsive to the modulation of melanocortin-4 receptors such as obesity, diabetes, and sexual dysfunction.

Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.

Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The invention relates to substituted pyrrole Mannich bases of general formula (I), wherein R1=H, a C1-10-alkyl-, aryl, a heteroaryl- or an aryl, heteroaryl-, CN, Br—, Cl or OH radical bound by a C1-6 alkylene group, R2=CH(R4)N(R5)(R6), R3, R3?, R3? identically or individually represent H, F, Cl, Br, CF3, CN, NO2, SO2NH2, NHR7, SR8, OR9, CO(OR10), CH2CO(OR11), COR15, a C1-10-alkyl-, aryl-, heteroaryl-aryl radical or a heteroalkyl radical bound by a C1-6 alkylene group, R4=an unsubstituted phenyl radical or a phenyl radical substituted at least with C1-4 alkyl, C1-3-alkoxy-, halogen-, a method for the production of the above-mentioned compounds, medicaments containing said compounds, and the use of said compounds in the production of medicaments.

Abstract: Atorvastatin calcium, the substance known by the chemical name (R—(R*,R*))-2-(4-fluorophenyl)-?, ?-dihydroxy-5-(1-methylethyl)-3-phenyl-((phenylamino)carbonyl)-1H-pyrrole-1-heptanoic acid hemi calcium salt is known as HMG-CoA reductase inhibitor and is used as an antihypercholesterolemic agent. Atorvastatin in the pharmaceutical compositions available in the market, is usually prepared as its calcium salt since it enables atorvastatin to be conveniently formulated in the pharmaceutical formulations, for example, in tablets, capsules, powders and the like for oral administration. Atorvastatin calcium can exist in an amorphous form or in one of the at least four known crystalline forms (Form I, Form II, Form III and Form IV). Atorvastatin calcium is the substance which is sparingly soluble in water, with pKa 4,5, and it has been found that the crystalline forms are less soluble than the amorphous form, which may cause problems in bioavailability of atorvastatin in the body.

Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer.

Abstract: This invention relates to a process for producing 5-methyl-N-(methyl aryl)-2-pyrrolidone, 5-methyl-N-(methyl cycloalkyl)-2-pyrrolidone and 5-methyl-N-alkyl-2-pyrrolidone by reductive amination of levulinic acid esters with aryl or alkyl cyano compounds utilizing a metal catalyst, which is optionally supported.

Abstract: Disclosed are the novel compounds as growth hormone secretagogues represented by structural Formula (I), wherein R1 is, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, or substituted or unsubstituted amino, X is —CO— or —SO2—, Y is Formula (II), wherein n is an integer from 0–4, R4 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, R5 and R6 are independently selected from hydrogen, substituted or unsubstituted alkyl, or R5 and R6 or R4 and R5 are taken together to form substituted or unsubstituted alkylene, R2 is hydrogen, or substituted or unsubstituted alkyl, R3 is substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, D is substituted or unsubstituted amino, substituted or unsubstituted alkoxy, or substituted or unsubstituted alkylthio, * represents an asymmetric center, and ph

Abstract: A (preferably nonaqueous) method of making a dipyrromethane is described.

Abstract: The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) process, comprising: contacting a compound of formula (II): with hydrogen under a suitable pressure in the presence of an iridium complex of the formula (R2)IrL+X? wherein L is a chelating diene, X is a non coordinating anion, and R2 is selected from

Abstract: The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: These compounds contain an oxetane functionality and a maleimide functionality. The oxetane functionality is homopolymerizable in reactions that undergo cationic or anionic ring opening, and the maleimide functionality is homopolymerizable, or polymerizable with compounds such as electron donor compounds. The dual functionality allows for dual cure processing. The compounds have the structure in which R1 is a methyl or ethyl group, R2 is a divalent hydrocarbon, X and Y independently are a direct bond, or an ether, ester, amide, or carbamate functionality, and Q is a divalent organic group, and provided that X and Y will not both be direct bonds.

Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.

Abstract: The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy

Abstract: An E-isomeric fulleropyrrolidine compound of formula (I): is disclosed. Also disclosed is a method for preparing and polymers prepared from such a compound.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: The present invention provides pharmaceutical compositions and novel compounds useful in the treatment of conditions mediated by CCR2, MCP-1 or the interaction thereof. The compounds of the present invention are pyrrolidinones and pyrrolidine-thiones.

Abstract: An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.

Abstract: Benzotriazole adducts contain a benzotriazole segment and a segment with a curable and polymerizable functionality, or an adhesion promoting functionality, particularly suitable for use on metal substrates or in adhesive, sealant or coating compositions for use in proximity to metal substrates.

Abstract: A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease, over active bladder (including symptoms of incontinence, urge and frequency), urinary incontinence, neurogenic urinary urgency or pollakiuria, treatment of bladder functional disorder, urinary leakage, painful or difficult urination caused by neurogenic bladder, spastic or hypertonic bladder, dysfunctional bladder syndrome, gastrointestinal disorders including gastrointestinal hyperactivity, and relaxing effect on intestinal smooth muscle cells.

Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.

Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.

Abstract: Disclosed are compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

Abstract: Infrared absorbing compounds in which the anion is selected from the group consisting of 5-isatinsulfonate, 10-camphorsulfonate, and 4,5-dihydroxy-1,3-benzenedisulfonate are disclosed. Negative-working imageable elements containing these compounds have improved dot stability.

Abstract: The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.

Abstract: Novel selenophene compounds useful as anti-tumor agents are described. Preferred compounds include compounds of formula I: wherein R1 and R2 are independently selected from the group consisting of; ?H, CHO, CH2OH and CH2NH2; and X and Y are independently selected from the group consisting of Se, S, O, NCH3 and NH. Pharmaceutical compositions and a method for treating patients having tumors utilizing the disclosed selenophene compounds are also described.

Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.

Abstract: This invention features a compound having the formula: X is O or NR1; and each of Y and Z, independently, is in which each of R1, R2, R3, and R4, independently, is alkyl, cyclyl, heterocyclyl, aralkyl, aryl, or heteroaryl; Ar1 is aralkyl, aryl, or heteroaryl; and Ar2 is cyclyl, heterocyclyl, aralkyl, aryl, or heteroaryl; or Ar1 and Ar2 taken together is heterocyclyl, aralkyl, or heteroaryl. This compound can be used as a red light emitting material in an electro-luminescence device.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.