Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.

Abstract: The invention provides compounds of formula (I) wherein R1,R3,L1,L2,G1,G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.

Abstract: Sulfonylamino(thio)carbonyl compounds are used to control unwanted plants or to regulate growth in plants. Sulfonylamino(thio)carbonyl compounds are applied to plants, the seed or the area on which the plants are growing to control the growth of such plants.

Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.

Abstract: Treating and/or preventing prostate problems and/or metastases, by selectively occluding various groin vessels and tools for selective occluding of various groin veins, including, for example, the deferential vein. Optionally providing anti-androgen treatment after such occluding.

Abstract: A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described. Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.

Abstract: Disclosed herein are novel antagonists of the androgen receptor and androgen receptor mutations associated with clinical failure of currently prescribed anti-androgens and use of said antagonists in the treatment of conditions associated with inappropriate activation of the androgen receptor.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: This case discloses compounds of formula (I) wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano or amino; each R4, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; p is 0, 1 or 2; each R5, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; q is 0, 1 or 2; R6 is —NR6aSO2R6b, —NR6aC(?O)R6b, —NR6a(C?O)N(R6c)2, —(C?O)R6d, —CH2NR6aSO2R6b, —CH2NR6aC(?O)R6b, CH2NR6a(C?O)N(R6c)2 or —CH2(C?O)R6d; where R6a and each R6c, which may be the same or different, is hydrogen or C1-6alkyl; R6b and R6d are C1-6alkyl or haloC1-6alkyl; or R6a and R6b, or R6a and R6c, together with the interconnecting atoms, may form a 5- or 6-membered ring; n is 1 or 2; and R7 and R8, which may be the same or different, are

Abstract: Disclosed is a compound having high optical anisotropy and high compatibility with a polymer resin, which is represented by Formula 1 and necessarily has at least one meta substituent. Also, a resin composition including the compound and a polymer resin, and an optical member including the resin composition are disclosed. Since the compound represented by Formula 1 is an anisotropic compound having high compatibility with a polymer resin and high optical anisotropy, in the case of an optical member obtained by using a polymer resin composition including the compound represented by Formula 1, there is no phase separation, and it is possible to achieve a required optical characteristic with only a small amount thereof.

Abstract: A modest (2-5 fold) increase in androgen receptor (AR) mRNA is the only expression change consistently associated with developing resistance to antiandrogen therapy. Increased levels of AR confer resistance to anti-androgens by amplifying signal output from low levels of residual ligand and altering the normal response to antagonists. This invention provides cell based assays for use in the examination of new therapeutic modalities and provides for the design of novel antiandrogen compounds.

Abstract: The present invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.

Abstract: The present invention provides a method of crystallization of bicalutamide comprising adding an acetone solution containing bicalutamide to water; crystals of bicalutamide wherein particle size distribution of the crystals is 1 to 10 ?m of Dp10, 10 to 25 ?m of Dp50 and 25 to 100 ?m of Dp90, and the crystals are obtainable by the method described above; and crystals of bicalutamide, wherein particle size distribution of the crystals is 1 to 3 ?m of Dp10, 2 to 5 ?m of Dp50 and 5 to 15 ?m of Dp90.

Abstract: Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. The most widely used halogen sulfonamide organic compound for these applications is Chloramine-T. This invention deals with the new use of discovered compositions of matter, halo active aromatic sulfonamide organic compounds and use of solutions of these compounds as, odor control agents. The odor control solutions may be buffered to a predetermined pH. The odor control compositions may further incorporate small percentages of low molecular weight alcohols and wetting agents.

Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.

Abstract: Compositions are provided that include an electron donor and a sensitizing compound. More specifically, the electron donor is an arylsulfinate salt. Methods of polymerization are also provided that can be used to prepare polymeric material from a photopolymerizable composition that includes ethylenically unsaturated monomers and a photoinitiator system. The photoinitiator system includes an electron donor and a sensitizing compound.

Abstract: A biocidal solution comprising aromatic N-halosulfonamide organic compounds and methods of using the biocidal solution are disclosed. The solution may further comprise a wetting agent, a low molecular weight alcohol, and buffering agents. The biocidal solution is used to arrest or kill unwanted organisms.

Abstract: Disclosed herein are novel antagonists of the androgen receptor and androgen receptor mutations associated with clinical failure of currently prescribed anti-androgens and use of said antagonists in the treatment of conditions associated with inappropriate activation of the androgen receptor.

Abstract: The invention relates to 2-cyano-3-(halo)alkoxy-benzenesulfonamide compounds I where the variables Alk and R1 to R5 are as defined in claim 1, and/or to their agriculturally useful salts.

Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.

Abstract: Halo active aromatic sulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to releaser active halogen ions has been utilized in a range of biocidal and fungicidal applications. The most widely used sulfonamide organic compound for these applications has been Chloramine T. This invention deals with nearly discovered halo active aromatic sulfonamide organic compounds and uses of these compounds as biocides, odor control agents, bovine teat cleaners, drugs for cultured fish, soap biocides, stain removal agents, and paint fungicides.

Abstract: The present invention relates to a method of combating animal pests which comprises contacting the animal pests, their habit, breeding ground, food supply, plant, seed, soil, area, material or environment in which the animal pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from animal attack or infestation with a pesticidally effective amount of at least one cyanobenzene compound of the formula (I) and/or at least one agriculturally acceptable salt thereof: where m is 0, 1 or 2; is a radical of the formulae N?CR5R6, N?SR7R8, NR10—C(?X)—R9, where X is O, S A or NR11, or A is a N-bound 5-, 6- or 7-membered heterocycle, which is ethylenically unsaturated or aromatic, and which additionally may contain 1, 2, or 3 further heteroatoms or heteroatom groups, selected from O, S, SO, SO2, N, and NR12, and/or 1, 2 or 3 carbonyl groups as ring members and which may carry 1, 2, 3 or 4 radicals R13, where the radicals R1 to R13 are as defined in the claims or the des

Abstract: Novel sulfon amide derivatives are chemical uncouplers useful e.g. for the treatment of obesity.

Abstract: A process of producing a compound of the following formula (3): wherein R1 is a C1-5 alkyl group, R2 is a halogen atom, a C1-5 alkyl group, a C2-5 alkenyl group, a C2-5 alkynyl group, a C1-5 alkyl group, a C1-5 alkoxy group, a nitro group, or a hydroxy group, wherein multiple R2 may be the same or may be different, and a is an integer of from 0 to 4, comprising reacting a compound of the following formula (2): wherein R2 and a are as defined above with a C1-5-alkanesulfonyl chloride or C1-5-alkanesulfonic acid anhydride followed by hydrolyzing an N,N-disulfonated derivative of compound (3) to the compound of formula (3).

Abstract: Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:

Abstract: The present invention pertains to certain aryl alkyl sulfonamides and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formula: wherein: Ar1 is independently C5-20aryl (e.g., biphenyl, phenanthryl, fluorenyl, or carbazolyl, most preferably biphenyl), and is optionally substituted; RN is independently —H, acyl, C5-20aryl-C1-7alkyl, C3-20heterocyclyl, or C1-7alkyl, and is optionally substituted; Ralk is a C2-10alkylene group, and is optionally substituted; and Q is independently —H or an organic group having from 1 to 30 atoms selected from carbon, nitrogen, oxygen, sulfur, phosphorus, fluorine, chlorine, bromine, and iodine (e.g., an oxy-type group, an amine-type group, etc.); and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.

Abstract: The invention relates to a process for preparing N-(4?-cyano-3?-trifluoromethylphenyl)-3-(4?-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide (bicalutamide).

Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 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: A process for making a compound of formula (I) in which process the compound HC?C—(CH2)n—NH2 is reacted with the compound R1—SO2Cl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formula to produce the compound of formula (I), and compounds produced by the process of this invention. The terms R1, R2, R3, R4 and n have the definitions set forth in the specification.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.

Abstract: Bicalutamide and/or its intermediates are made by the use of p-fluorobenzenesulfinic acid salt as a reagent.

Abstract: The present invention relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.

Abstract: The present invention relates to a crystal of bicalutamide having a defined form, as well as economical and industrially practical production methods of bicalutamide and a crystal thereof, which are superior in environmental benignity and safety. Accordingly, the present invention provides a production method of bicalutamide represented by the formula (I): which includes at least a step of reacting a compound represented by the formula (3): with an oxidizing agent, a production method of a crystal of bicalutamide, as well as a crystal form of bicalutamide as defined by X-ray diffraction (XRD) or solid 13C NMR measurement.

Abstract: The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio) propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof. The present invention further discloses a new process for the isolation and purification of racemic and optically active bicalutamide.

Abstract: A series of N-cycloalkylcarboxamide derivatives of N-benzyl benzenesulfonamides of Formula I are described. The compounds inhibit ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extracellular deposition of ?-amyloid. Pharmaceutical compositions and methods of treatment using these compounds are also disclosed.

Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.

Abstract: The present invention provides certain monofluoroalkyl derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: The present invention is directed to beazophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.

Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.

Abstract: The present invention provides compounds of formula (I): useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: A process for making a compound of formula (I) in which process the compound HC?C—(CH2)n—NH2 is reacted with the compound R1—SO2Cl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formula to produce the compound of formula (I), and compounds produced by the process of this invention. The terms R1, R2, R3, R4 and n have the definitions set forth in the specification.

Abstract: The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.

Abstract: Provided is a bis(diphenylvinyl)arene compound having a reactive functional group on phenyl group, represented by below formula (1), wherein, Ar is an arylene group and has one or more substituents; R1-R22 each independently represent a hydrogen atom, a halogen atom, cyano group, nitro group, etc., and at least one of R1-R20 is a halogen atom, etc. The arene compound has sufficient solubility in an organic solvent and excellent reactivity.

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

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-lipoxygenase, such as inflammation.

Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.