Abstract: There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH?CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other than

Abstract: The present invention relates to a process for the preparation of cis substituted cyclic ?-aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme wherein X, Ar, n, and m are defined hereinand corresponding salts thereof.

Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].

Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Abstract: [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.

Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Abstract: The present invention relates to novel substituted aryl sulfone intermediates and processes for preparing the same. An aspect of this invention relates to a process for making substituted aryl sulfone intermediates utilizing a one-pot deacylation-carbon/sulfur bond formation step. The invention also relates to a process for preparing intermediates that are used to make the compounds of formula I. Some of the advantages of the present invention include manufacturing flexibility and efficiency, high yield synthesis using a one pot deacylation and carbon-sulfur bond formation step of a thioester intermediate and the like. This and other aspects of the invention will be realized upon review of the specification as a whole.

Abstract: The present invention provides a more efficient industrial method for producing a pyrazol-3-yl-benzamide derivative expressed by a formula useful as medicine: wherein R2, R3 and R4 each independently represent a lower alkyl group.

Abstract: The present invention provides polymeric linkers containing pyridyl disulfide moieties. Methods of making the polymeric linkers and methods of making conjugates using the same are also disclosed.

Abstract: Provided is a solid polymer electrolyte having increased heat resistance and high proton conductivity and a proton conductive membrane composed of the electrolyte. Also provided is a copolymer having a sulfonic acid group.

Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein W, X, Y, and R1-R7 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Abstract: A compound of formula XIX wherein R1, R2, Z1, Z2, Q1, Q2 and Q3 as defined in the specification.

Abstract: Compounds of Formula (I) wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

Abstract: The present invention is directed to substituted pyridines, methods for their preparation and methods for their use in the treatment and/or prevention of mast cell related conditions.

Abstract: Bivalent linkers derived from compounds of formulae (V), (VI), and (VII), where X1 and X2 are leaving groups and the other variables are as defined in the claims, to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described.

Abstract: The present invention provides a method for producing an organic oxide, wherein a substrate is oxidized using hypohalous acid, hypohalous acid salt, chlorine, bromine or iodine in the presence of water and a catalytic amount of a compound represented by the following formula (I): R1—X1—NY—R2, wherein: X1 represents —CO— or —SO2—; Y represents a hydrogen atom, a potassium atom, a sodium atom, a chlorine atom, a bromine atom or an iodine atom; R1 represents a substituted or unsubstituted hydrocarbon group, —NYR3 group or —OR3 group (in the formulae, R3 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above); and R2 represents a hydrogen atom or —CO—R4 group (in the formula, R4 represents a substituted or unsubstituted hydrocarbon group, —NYR5 group or —OR5 group (in the formulae, R5 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above)); or R1 and R4 may bind to each other to form a further substi

Abstract: The present invention relates to compounds of following formula: or pharmaceutically acceptable salts thereof; pharmaceutical compositions containing them, and their use in the treatment of disorders mediated by the CCR-2 receptor.

Abstract: Compounds of formula I: are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various 10 CNS disorders.

Abstract: This invention relates to a method of preparation of benzofuran-2-carboxylic acid {(S)-3-methyl-1-[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)-azepan-4-ylcarbamoyl]-butyl}-amide.

Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.

Abstract: A compound having the formula Y-A-Z, wherein: A is a 5, 6, or 7 member ring that is monocyclic or is fused to 1 to 3 additional 4 to 8 member rings; wherein ring A and, independently, the fused additional rings are carbocyclic or heterocyclic, and saturated or unsaturated, wherein unsaturated rings are aromatic or non-aromatic; wherein Y and Z are substituents at adjacent positions on ring A; Y represents: Z represents: X and E represent O, S, or NRa or NRb; each of a, b, c, d, e and f independently represents 0 or 1; a+c equals 0, 1, or 2; b+d equals 0, 1, or 2; a+b+c+d+e+f equals 1, 2, or 3; provided that when f is 1, then d is 1, and when d is 0, then f is 0; and when both e and b are 0, then neither R1 nor R2 is chloro or bromo; v represents 0 or 1, provided that when v is 0, then J is hydrogen, a metal ion, or a quaternary ammonium ion, and X is O and G is H; either G is hydrogen, a metal ion, a quaternary ammonium ion, lower alkyl, or comprised of a pharmaceutically active chemical compound or t

Abstract: The invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein X1, X2 and X3 are each independently where Y is an alkylene, alkenylene or alkynylene group, each of which may be optionally substituted with one or more substituents selected from alkyl, halo, CF3, OH, alkoxy, NH2, CN, NO2 and COOH; W is absent or is O, S or NH; R1, R2, R3 and R4 are each independently selected from H, alkyl, aryl and a protecting group P1; R7, R8 and R9 are each independently selected from H, alkyl, halo, CF3, OH, alkoxy, NH2, CN, NO2 and COOH; q and r are each independently 1, 2, 3 or 4; q? and r? are each independently 0, 1, 2 or 3, where q+q? and r+r? each equal 4; p is 1, 2, 3, 4 or 5, and p? is 0, 1, 2, 3 or 4, where p+p? is 5; n is 0, 1, 2, 3 . . .

Abstract: The present invention describes novel pyridine-3-sulfonyl compounds having the formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein. The present invention is also directed lo pesticidal compositions that include a) compounds of formula (II) wherein R1, R2, R3, R4 and R6 are as defined herein and b) a carrier. Moreover, the present invention relates to methods for protecting crops from insect attack by contacting the crop with a pesticidally effective amount of the compound of formula (II). In addition, the present invention includes methods for controlling insects by treating the target species with a pesticidally effective amount of the compound of formula (II).

Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

Abstract: Novel antagonists of ?4?1 integrin and/or ?4?7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.

Abstract: A compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, L1, L2, M1, M2, n, p, q, A, D, X, Y and Z are as described in the specification; pharmaceutical compositions thereof, methods of making said pharmaceutical compositions; and methods of use thereof.

Abstract: Process for the preparation of 2-aminomethylpyridine derivative of general formula (I), in which: n represents 0, 1, 2 or 3; X is halogen atom; Y may be the same or different and may be a halogen atom, a halogenoalkyl, a alkoxycarbonyl or a alkylsulphonyl

Abstract: Pyridinium-Betain compounds of the general formula (A): wherein R1 is H or a primary amino acids that is attached to the structure, X is OH or its ionized form O?, Y is OH, SH, or their ionized forms O? and S?, Z is H, an alkyl group, or a glycosidic group, or a phosphate or ester derivative thereof, and n is an integer of 0 to 4 to represent the chain length of the compound. A counter-ion is associated with these compounds and is preferably an ion of sodium, potassium, ammonium, calcium, magnesium, chloride, nitrate, carbonate, sulphate, phosphate, or the like. These compounds can be used as taste modifiers in various foodstuffs.

Abstract: The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are also provided.

Abstract: The invention relates to compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.

Abstract: The present invention concerns the use of 1-isopropyl-3-[(4-m-toluidino-3-pyridyl)sulphonyl]-urea in the pharmaceutical field. In particular, it proposes the use of a pure and stable polymorphic form of 1-isopropyl-3-[(4-m-toluidino-3-pyridyl)sulphonyl]-urea for the preparation of solid pharmaceutical forms, and likewise a method of synthesis to obtain such a pure and stable polymorphic form of 1-isopropyl-3-[(4-m-toluidino-3-pyridiyl)sulphonyl]-urea.

Abstract: New oxime sulfonate compounds of the formula (I) and (II), wherein R1 is C1-C12alkyl, C1C4haloalkyl, hydrogon, OR9, NR10R11, SR12 or is phenyl which is unsubstituted or substituted by OH, C1-C18alkyl, halogen and/or C1-C12alkoxy; R2, R3, R4 and R5 are for example hydrogen or C1-C12alkyl; R6 is for example is C1-C18alkylsulfonyl, phenyl-C1-C3alkylsulfonyl or phenylsulfonyl; R?6 is for example phenylenedisulfonyl or diphenylenedisulfonyl; R7, R8 and R9 for example are hydrogen or C1-C6alkyl; R10 and R11, are for example hydrogen or C1-C18alkyl; R12 is for example hydrogen, phenyl or C1-C18alkyl; A is S, O, NR13, or a group of formula A1, A2 or A3, R21 and R22 independently of one other have one of the meanings given for R7; R23, R24, R25 and R26 independently of one another are for example hydrogen, C1-C4alkyl, halogen or phenyl; Z is CR22 or N; and Z1 is CR22 or N; and Z1 is CR22 or N; and Z1 is CH2, S, O or NR13 are particularly suitable as photo-latent acids in resist applications.

Abstract: The present invention relates to a simple and efficient process for the preparation of amorphous form of torsemide. The process includes recovering amorphous torsemide from a solution thereof in a suitable solvent comprising alcohols, ketones, chlorinated hydrocarbons, esters, nitriles, cyclic ethers, and mixtures thereof, by spray drying.

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 relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use as a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.

Abstract: The present invention relates to a simple and efficient process for the preparation of amorphous form of torsemide, demonstrated in the X-ray diffraction pattern of FIG. 1.

Abstract: The present invention relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use as a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.

Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) 1

Abstract: A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.

Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R3, Q, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.

Abstract: The present invention provides a sulfonamide- or sulfonylurea-containing heterocyclic compounds. Specifically, it provides a heterocyclic compound represented by the formula (I), a pharmacologically acceptable salt thereof or a hydrate of them.

Abstract: The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and an optionally substituted heteroaryl group at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.

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: The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them.

Abstract: Compounds of Formula (I) 1

Abstract: A process of preparation of optically pure or optically enriched isomers of omeprazole and structurally related sulfoxides is provided. Also provided are an amorphous form of esomeprazole, as well a pharmaceutical composition containing it and a method of using it for treatment of gastric disorders.

Abstract: A method of synthesizing a compound having the formula: from a compound having the formula: wherein R1 is hydrogen, fluorine, chlorine or SiR5R6R7, wherein R5, R6, and R7 are independently the same or different an alkyl group or an aryl group, R2 is an alkyl group, R3 is a protecting group, R4 is an alkyl group, an allyl group, a propargyl group —CO2H, or a benzyl group, R8 is —CO2R10, wherein R10 is an alkyl group or an aryl group, X1 is OH and X2 is H, includes the step of exposing compound (III) to at least one of an organic acid or an inorganic acid. A compound has the general formula (III).

Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which m represents integers from 3 to 10, n represents 0, 1 or 2 and Het represents the following, in each case optionally substituted, groupings: to processes for their preparation and to their use as pesticides.