Abstract: The invention relates to compounds of the formula (I) process for their preparation starting from the plant Beilschmiedia fulva, PLA 101037, and the use thereof for producing a medicament, in particular for the treatment of allergic disorders, of asthmatic disorders, of inflammatory concomitant symptoms of asthma and/or of diseases which can be treated by inhibiting c-maf and NFAT.

Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.

Abstract: The invention relates to compositions in the form of a powder or granules containing L-ascorbic acid and/or a pharmaceutically acceptable salt thereof, and pectin in a quantity within the range of about 0.1 to about 10% by weight.

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

Abstract: FK506 and geldanamycin promote nerve regeneration by a common mechanism that involves the binding of these compounds to polypeptide components of steroid receptor-complexes other than the steroid hormone binding portion of the complex (FKBP52 and hsp90, respectively). These and other agents cause hsp90 dissociation from steroid receptor complexes or block association of hsp90 with steroid receptor complexes.

Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.

Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

Abstract: Described herein are compounds related to lactacystin and lactacystin ?-lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: The present invention provides a device, preferably a collar or ear tag, capable of the controlled, sustained release of an effective amount of an active ingredient that can protect an animal against arthropod pests, comprising a reservoir containing a novel gel formulation comprising a fatty acid, an organic solvent which is a linear aliphatic ester, a silicone-based fluid, or a combination thereof, and an active ingredient that can protect the animal against one or more arthropod pests.

Abstract: The present invention is directed to a method for inhibiting expression of either iNOS or COX-2, or both in mammals using flavone compounds, and pharmaceutically acceptable salts thereof. The present invention is also directed to a method of activating K+ channels in mammals; as well as methods for treating septic shock, for inhibiting expression of angiotensin converting enzyme, for treating or preventing aneurysms and for reducing inflammation and related pathological changes using these compounds. Presently preferred compounds are oroxylin A (5,7-dihydroxy-6-methoxy flavone) and wogonin (5,7-dihydroxy-8-methoxy flavone).

Abstract: The present invention is related to a compound of formula (I), salts and pro-drugs of the compound (I) and methods for treating and/or preventing partial or total ischemia, methods for treating and/or preventing pathologies associated with ischemia or with mitochondrial deficiencies.

Abstract: Low concentrations of gossypol and related phyllophage toxins from cotton improve the effectiveness of insecticidal agents against social insects, including cockroaches, and particularly termites and ants. Levels of gossypol and other cotton phyllophage toxins which are sufficiently low as to be non-biocidal to social insects alone, will significantly increase the control efficacy of other insecticidal agents. Consequently, use of these low levels of these cotton phyllophage toxins allows the levels of insecticidal agents necessary for effectively controlling the insects to be significantly reduced relative to applications without cotton phyllophage toxins. Furthermore, insecticidal agents which are normally ineffective for control of social insects when used alone, may be effective when used in conjunction with the cotton phyllophage toxins.

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

Abstract: An agent comprising the benzoic acid of formula (I) 1

Abstract: Pleuromutilin compounds of the formula: 1

Abstract: The present invention provides compounds of formula (I): 1

Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.

Abstract: The present invention relates to the use of compounds which act as agonists at atypical beta-adrenoceptors, for the treatment of gastrointestinal disorders, especially peptic ulceration, oesophagitis, gastritis and duodenitis, intestinal ulcerations, including inflammatory bowel disease, and gastrointestinal ulcerations, especially when induced by non-steroidal anti-inflammatory drugs or corticosteroids.

Abstract: The invention relates to compounds of formula (I): wherein R1 represents alkyl or ureido, R2 represents alkyl or hydrogen, or R1 and R2 together form a 5- or 6-membered ring, R3 represents CN, NO2, NRaR′a, NRaSO2R′a, NRaCZR5 or CZNRaR′a, R4 represents hydrogen or R3, and medicinal products containing the same which are useful in treating or preventing epilepsy and neurodegenerative diseases.

Abstract: This invention provides compounds of Formula I having the structure wherein R1 and R2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy; R3 and R4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, alkanoyloxy of 2-7 carbon atoms, perfluoroalkanoyloxy of 2-7 carbon atoms, arylalkoxy of 7-15 carbon atoms, aryloxy of 6-12 carbon atoms, aroyloxy of 6-12 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamnino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, nitrile, nitro, amino, —NHSO2CF3, carbamoyl, carb

Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: FK506 and geldanamycin promote nerve regeneration by a common mechanism that involves the binding of these compounds to polypeptide components of steroid receptor complexes other than the steroid hormone binding portion of the complex (FKBPS52 and hsp90, respectively). These and other agents cause hsp90 dissociation from steroid receptor complexes or block association of hsp90 with steroid receptor complexes.

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: A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.

Abstract: The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. The sulfonamides of formula I have the structure: wherein A, B, D, D′, E, G and R7 are as defined above.

Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug 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 provides a phthalamide derivative of the formula (I): wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, —A2—R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, —A2—R4, etc., A2 is —C(═O)—, —C(═S)— or —C(═NR5)—, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., l is 0-4, m is 0-5, n is 0-2; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.

Abstract: The invention relates a pharmaceutical composition comprising a combination of:

Abstract: An adjuvant composition comprising noscapine and its derivatives, for use in the treatment of tumors, cancer, as an adjuvant for vaccines.

Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.

Abstract: A pro-liposomal encapsulated product is made by the process comprising the steps of: (1) forming a first solution comprised of a biogenic active ingredient and a solvent; (2) contacting a lecithin and/or a phospholipid with the first solution to form a second solution; and (3) contacting the second solution with water to form a pro-liposomal encapsulated product. The pro-liposomes are used for the preparation of cosmetic or pharmaceutical preparations.

Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents C

Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: The application relates to the use of topiramate and related sulfamates for the treatment and/or prophylaxis of post traumatic stress disorder (PTSD).

Abstract: A class of substituted biphenyl compounds is described for use in treating inflammation and inflammation-related disorders.

Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.

Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.

Abstract: A phytomicrobicidal composition comprising such an amount of at least two active ingredient components that a synergistic effect is achieved, together with a suitable carrier material, wherein component I is a compound of the formula I in which: X is CH or N; R is CH3 or cyclopropyl; Y is H, F, Cl, Br, CF3, CF3O, propargyloxy; Z is H, F, Cl, CF3, CF3O; or Y and Z together are a methylenedioxy, a (difluoromethylene)dioxy, an ethylenedioxy, a (trifluoroethylene)dioxy or a benzo group; and wherein component II is a compound selected from the group consisting of II A) metalaxyl, II B) R-metalaxyl, II C) furalaxyl, II D) benalaxyl, II E) ofurace, II F) oxadixyl, II G) cymoxanil and II H) mancozeb.

Abstract: The invention concerns LTA4 hydrolase inhibiting compositions of formula (1) as set forth below. It also concerns their therapeutic, in particular anti-inflammatory, applications.

Abstract: The present invention relates to pesticide compositions. In particular, the present invention relates to pesticide compositions comprising a pesticide and a redispersible polymer and to a method for controlling agricultural pests by applying to the pest or the locus of the pest a pesticide composition comprising a pesticide and a redispersible polymer.

Abstract: A lubricating composition for use in mucosal areas is provided to enhance sexual performance. The composition contains combination of a compound which enhances blood circulation to body parts and/or increase nitrous oxide levels at the site of administration together with a compound which can generate heat without any substantial irritation or create the feel of heat in a lubrication base. Preferably, the composition is homeopatic.

Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioarylalkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selec

Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract: The present invention relates to a new pesticide which is based on a photosensitizer or combination of photosensitizers of the tetrapyrrole and/or tetraazapyrrole series which may comprise a biological and/or chemical attractant for pests and to a method of controlling pests using the new pesticide.

Abstract: 3-amino-3-arylpropan-1-ol compounds of formula I: R1 and R2 independently denoting C1-6 alkyl, or together denoting a (CH2)2-6 ring optionally substituted by phenyl, R3 denoting C3-6 alkyl, C3-6 cycloalkyl, aryl optionally containing heteroatoms and optionally substituted by R6 to R8, or a substituted C1-3 alkylphenyl of formula XII:  R4 and R5 independently denoting C1-6 alkyl, C3-6 cycloalkyl, phenyl, benzyl, or phenethyl, or together forming a (CH2)3-6 or CH2CH2OCH2CH2 ring, R6 to R8 independently denoting H, F, Cl, Br, CHF2, CF3, OH, OCF3, OR14, NR15R16, SR14, phenyl, SO2CH3, SO2CF3, C1-6 alkyl, CN, COOR14, or CONR15R16, or together forming a OCH2O, OCH2CH2O, CH═CHO, CH═C(CH3)O or (CH2)4 ring, R14 denoting C1-6 alkyl, phenyl, benzyl, or phenethyl, R15 and R16 independently denoting H, C1-6 alkyl, phenyl, benzyl or phenethyl, and A denoting optionally substituted aryl optionally containing heteroatoms, or a diastereomer or enantiomer or pharmaceutica

Abstract: The present invention relates to a novel drug composition for relieving pain and promoting the removal of calculi in urolithiasis which contains an active ingredient having stimulating effects on both &bgr;2- and &bgr;3-adrenoceptors and exerting a potent relaxing effect on human ureteral smooth muscle.