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 novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

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: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising

Abstract: Optically active maleimide derivatives of the formula: 1

Abstract: Designed iminocylitols that have potent inhibition activity with respect to hexominidases and glycosides are disclosed.

Abstract: Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO—NH— or HO—, R1 is selected from phenyl, 4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (i.e., —NH—CO-Ph) and benzamido substituted on the terminal phenyl ring by C1-C4 alkyl, fluoro, chloro, cyano or C1-4 alkoxy; R2 is selected from (a) —S—Ar or —S—CH2—Ar wherein Ar is an aromatic moiety; (b) —O—Ar wherein Ar is as defined above; (c) —S-Het or —S—CH2-Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.

Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. In particular, the present invention relates to chemical compounds of Formula (I) wherein: R1 may be the same of different and are independently selected from hydrogen, alkoyl, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl groups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor; R2 may be the same or different and are independently selected from alkyl groups; n is an integer 1, 2, or 3; or a salt thereof.

Abstract: The present invention provides water-soluble drugs, in particular, water-soluble analogues of geldanamycin, and compositions comprising the same. This invention also provides a method of rendering water-soluble drugs soluble in water through derivatization with a bifunctional linking molecule and subsequent conjugation to a polar moiety through a thio ether. The present invention ether provides a method of treating cancer in a mammal.

Abstract: Novel substituted pyrrolidine-2,3,4-trione compounds of formula I and methods for preparing the compounds. Also disclosed are pharmarceutical compositions comprising the compounds and methods of using the compounds for treating pain, anxiety and various other diseases or conditions.

Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.

Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) to processes for their preparation and to their use in medicaments, in particular for the prevention and/or treatment of cardiovascular disorders.

Abstract: Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.

Abstract: A substituted 1,5-dihydropyrrol-2-one compound of formula I: and methods for preparing the compounds. Also disclosed are pharmarceutical compositions comprising the compounds and methods of using the compounds for the treatment or prophylaxis of pain, inflammatory and allergic reactions, depressions, drug abuse and various other diseases or conditions.

Abstract: Compounds of general formula (I): 1

Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Additionally, antiinflammatory drugs, such as steroids and NSAIDs can inhibit angiogenesis dependent diseases either alone or in combination with thalidomide and related compounds. Importantly, these compounds can be administered orally.

Abstract: The object of the present invention is to provide a microbicidal deodorant in a tractable liquid form that has excellent long-term storage stability.

Abstract: Novel non-steroidal estrogen receptor ligands and methods of synthesis are disclosed. The novel molecules are intended for use in therapeutic preparations for the treatment of estrogen receptor related disease states. The compounds specified are tetra-cyclic derivatives and have been shown to be antiproliferative against human estrogen-dependent cancer cells and to have good binding affinity for the estrogen receptor.

Abstract: A method for making a composition containing calcium incorporated into a fatty acid or fatty ester compound and the compositions produced by this method. These compositions can be administered to a patient to increase the calcium content of cells or tissue having a calcium deficiency or to treat at least some of the symptoms of diseases or adverse effects caused by this calcium deficiency.

Abstract: Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. The disclosed method and novel compounds can be used to reduce pain in an individual or animal suffering from pain, reducing nausea in an individual undergoing chemotherapy, for example cancer chemotherapy, suppressing appetite in an individual, reducing intraocular pressure in the eye of an individual or animal suffering from glaucoma and suppressing the immune system in an individual with an organ transplant.

Abstract: The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R1, R2, R3, R4, R5, R10, R11, b, m, n, p and v are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and methods of treating hyperproliferative disorders in mammals by administering the above compounds.

Abstract: Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.

Abstract: The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

Abstract: Carbamate compounds of 2-heteroaryl-1,2-ethanediol are described. The compounds are effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.

Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: A compound of formula (I) wherein: R1, R2, R3, R4, R5, R6 and R7 are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2  I  in which A, R1 and R2 are as defined in the description, and b) compounds of the formula II, their N-oxide or one of their salts  where the substituents R12 to R18 are as defined in the description, and/or c) compounds of the formula III  where the substituents X1 to X5 and R19 to R22 are as defined in the description, in a synergistically effective amount.

Abstract: The present invention related to safe botanical drug for treatment and prevention of Alzheimer's disease. Specifically, this invention proves a safe botanical drug, Huperzine (HUE) and Clausenamide (CLE) and their preparation. HUE has the following pharmaceutical functions: inhibiting acetylcholinesterase (CAT), increasing memory, decreasing Alzheimer amyloid protein, increasing RNA and protein synthesis of brain, increasing calcium in brain, decreasing superoxide anion. CLE has the following pharmaceutical functions: increasing memory, decreasing Alzheimer amyloid protein, increasing RNA and protein synthesis of brain, increasing calcium in brain, decreasing superoxide anion, increasing long-term potentiation and increasing dopanmine (DA). It is important that HUE combined with CLE have stronger function as mentioned above.

Abstract: Novel tetramic acid-type compounds isolated from a CCR-5 active complex produced by fermentation under controlled conditions of a biologically pure culture of the microorganism, Chaetomium globosum Kunze SCH 1705, ATCC 74489., pharmaceutical compositions containing the compounds and the use of the CCR-5 antagonist compounds and compositions to treat HIV-1 infections in humans are disclosed.

Abstract: The invention provides the use of certain succinimide compounds in the treatment of mycobacterial diseases.

Abstract: The present invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) in which A, B, G, X, Y and Z have the meanings given in the description, to processes for their preparation, and to intermediates therefor. The compounds of the formula (I) are used as pesticides.

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. For example, the present invention relates to chemical compounds of the formula: wherein R1 may be the same or different and are independently selected from hydrogen, alkoyl, alkoxy, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl groups and groups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor; R2 may the same or different and are independently selected from alkyl groups; n is an integer 1, 2 or 3; or a salt thereof.

Abstract: A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having the general formula (I): The compounds are potentially useful as glycosidase inhibitors. The synthetic schemes comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds in moderate to good yields with limited side-reactions.

Abstract: The use of menthyl 2-pyrrolidone-5-carboxylate as an insect repellent, usually by application to a substrate or into an air space. The menthyl 2-pyrrolidone-5-arboxylate can be used as a composition, which may be perfumed. A useful composition comprises a mixture of menthyl 2-pyrrolidone-5-arboxylate and a known insect repellent or a compound shown to be an effective insect repellent on a test described herein.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols, their preparation and the use of such ketoenols as pesticides and/or herbicides. The novel arylphenyl-substituted cyclic ketoenols are of the formula (I) in which CKE refers to the cyclic ketoenol and W, X, Y and Z are as defined in the specification.

Abstract: The present invention relates to (2R,3R,4R)-3,4-dihydroxy-2-hydroxymethylpyrrolidine and other substituted 2-methylpyrrolidines and their use for inhibiting liver glycogen phosphorylase.

Abstract: Novel tetramic acid-type compounds isolated from a CCR-5 active complex produced by fermentation under controlled conditions of a biologically pure culture of the microorganism, Chaetomium globosum Kunze SCH 1705, ATCC 74489., pharmaceutical compositions containing the compounds and the use of the CCR-5 antagonist compounds and compositions to treat HIV-1 infections in humans are disclosed.

Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.

Abstract: Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1 is an integer of 1 to 2n+4; and q2 is an integer of 0 to 2n+3, provided that q1+q2 is 2n+4.

Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl o

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lizoxygenase, such as inflammation.

Abstract: The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.

Abstract: Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. The disclosed method can be used to reduce pain in an individual or animal suffering from pain, reducing nausea in an individual undergoing chemotherapy, suppressing appetite in an individual, reducing intraocular pressure in the eye of an individual or animal suffering from glaucoma and suppressing the immune system in an individual with an organ transplant.

Abstract: The present invention relates to a compound named Vancoresmycin which is obtainable by cultivation of the microorganism HIL-006734 (DSM 12216), and to its pharmaceutically acceptable salts. The present invention further relates to a process for the production of Vancoresmycin, to the microorganism HIL-006734 (DSM 12216), to the use of Vancoresmycin and its pharmaceutically acceptable salts as pharmaceuticals, and in particular to their use as antibiotics, and to pharmaceutical compositions comprising Vancoresmycin or a pharmaceutically acceptable salt thereof.

Abstract: Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH-R antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or X-ray therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH-R agonist, either simultaneous with or subsequent to LHRH-R antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH-R antagonist.

Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: The present invention pertains to single morphic forms of a compound selected from 2S-[4-(2,5-dioxopyrrolidin-1-yl)-2S-mercaptobutyrylamino]-4-methylpentanoic acid (2,2-dimethyl-1S-methylcarbamoylpropyl)amide and 2S-[2S-mercapto-4-(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)butyrylamino]-4-methylpentanoic acid (2,2-dimethyl-1S-methylcarbamoylpropyl)amide, isolable as such.