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: A series of N-alkanol-N-phenyl benzenesulfonamide and related derivatives of the Formula I are disclosed, 1

Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.

Abstract: Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV, also are disclosed.

Abstract: A method for preparing S-alkyl and S-aryl thiocarbamates comprising reacting a precursor thiol reagent with trichloroacetyl chloride to produce an S-alkyl and S-aryl trichloroacetyl thioester intermediate, which is reacted with an amine to yield the corresponding thiocarbamate product. Also disclosed is the method for preparing S-alkyl and S-aryl thiocarbamates comprising reacting an amine with trichloroacetyl chloride to produce a trichloroacetamide intermediate, which is then reacted with the precursor thiol to yield the corresponding thiocarbamate product.

Abstract: A thermosensitive recording material having high whiteness and resistance to color formation under high temperature, high humidity conditions has a thermosensitive colored image-forming layer formed on a substrate sheet and includes a dye precursor, a binder and a color developing agent including a compound of the formula (I) and optionally a compound of the formula (V). R1, R3=unsubstituted or methyl or chlorine-substituted aryl group, R2=at least C3 divalent organic group, R4=at least C3 alkyl, aralkyl or aryloxyalkyl group.

Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.

Abstract: SNACE derivatives as pharmacological active agents and pharmacological compositions containing these compounds, in particular for transdermal, oral, rectal and inhalational application, are described.

Abstract: The invention relates to novel substituted sulphonylamino(thio)carbonyl compounds of the formula (I) 1

Abstract: The invention relates to a resin-bound synthesis process for the preparation of chemical compounds of the formula (I)

Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to &agr; 4 integrin. They are used as therapeutic agents for various diseases concerning &agr; 4 integrin.

Abstract: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Abstract: The invention relates to compounds of the formula I 1

Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.

Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them.

Abstract: &agr;,&bgr;-Unsaturated amides and esters are converted to &agr;,&bgr;-substituted amino amides, esters, and acids. An &agr;,&bgr;unsaturated amide or ester is first converted to an &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a &agr;,&bgr;-N-sulfonyl- or the &agr;,&bgr;-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(&agr;,&bgr;-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.

Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.

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

Abstract: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflamamatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

Abstract: Provided are an anti-inflammatory agent containing, as an active ingredient, at least one selected from amino acid derivatives represented by formula (I) wherein Ar represents an optionally substituted 2-hydroxyaryl group, n is 0 or 1, R2 represents a hydrogen atom or a side chain of an &agr;-amino acid or &bgr;-amino acid, X represents —O— or —NH—, R1 represents a hydrogen atom or a group that forms, together with R2 and an adjacent atoms, a cyclic structure of pyroglutamic acid, and R3 represents a hydrogen atom, an alkyl group having from 1 to 22 carbon atoms or an alkenyl group having from 2 to 22 carbon atoms, and salts thereof, and toiletries or skin external products containing the same. The anti-inflammatory agent of the invention inhibits expression of an inflammatory protein and activation of a gene transcription control factor that participates therein, and exhibits a good feeling upon use and a safety.

Abstract: A method of selectively controlling undesirable vegetation in crops by using a postemergent application of an herbicidally effective amount of a metal chelate of a 2-(substituted benzoyl)-1,3-cyclohexanedione compound to the locus of such undesirable vegetation.

Abstract: C6 compounds of the formula (I) E—CH2—CH═CH—CH2—E1  (I) are prepared by self metathesis or cross metathesis of compounds of the formulae (II) and/or (III) R—CH═CH—CH2—E  (II) R1—CH═CH—CH2—E1  (III) where E, E1 are independently —CHO, —COOH, —COOR2, —C(O)NR3R4, —CN, R, R1 are independently H, C1-12-alkyl, C6-12-aryl or C7-13-alkylaryl and R2, R3, R4 are independently H, C1-12-alkyl, C7-13-aralkyl, in the presence of a homogeneous catalyst comprising ruthenium compounds or ruthenium complexes.

Abstract: Compounds of the formula B—X—(CH2)m—CR1R2—(CH2)n—CO—Y  (I) have therapeutic utility as inhibitors of metalloproteinases etc.

Abstract: Disclosed is a novel class of compounds of formula (I) wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.

Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: 1

Abstract: A compound of the formula (I): wherein for example, a compound below: wherein R1 is CH3, H or Na; and X1—X2—X3 is or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.

Abstract: The present invention provides a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents, and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating disease

Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.

Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: Compounds of formula I 1

Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.

Abstract: A method of preparing carboxylic acid derivatives comprising mixing a quaternary ammonium salt having a particular triazine ring in the molecules thereof, a carboxylic acid compound and a compound having a nucleophilic functional group, to condense the carboxylic acid with the compound having the nucleophilic functional group. The invention further provides a condensing agent comprising the quaternary ammonium salt. The condensation is conducted under mild conditions to form carboxylic acid derivatives and, particularly, amide compounds or ester compounds maintaining high yields.

Abstract: Compound of formula (I): 1

Abstract: A process for preparing polytetrahydrofuran, polytetrahydrofuran copolymers or diesters or monoesters of these polymers comprises polymerizing tetrahydrofuran in the presence of at least one telogen and/or comonomer over a heterogeneous catalyst comprising hectorite.

Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

Abstract: Compounds of the formula 1

Abstract: This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.

Abstract: The present invention provides an improved process for the preparation of N-(substituted phenyl)-3-alkyl-, aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds of formula I 1

Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.

Abstract: The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia);  wherein R1 is hydrogen, C1-4 alkyl; R2 is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3 is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is — (CH2)m—, in which m is 2, 3 or 4, or in which R6 and R7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP.

Abstract: Compounds of the formula I R1 and R2 independently of one another are C1-C20alkyl, OR11, CF3 or halogen; R3, R4 and R5 independently of one another are hydrogen, C1-C20alkyl, OR1 or halogen; R6, R7, R8, R9 and R10 independently of one another are hydrogen, C1-C20alkyl; C2-C20alkyl which is interrupted once or more than once by nonconsecutive O atoms and which is unsubstituted or substituted by OH and/or SH; or R6, R7, R8, R9 and R10 are OR11, SR11, N(R12)(R13), phenyl or halogen; R11 is C1-C20alkyl, C3-C8cycloalkyl, phenyl, benzyl or C2-C20alkyl which is interrupted once or more than once by O or S and which is unsubstituted or substituted by OH and/or SH; R12 and R13 independently of one another are hydrogen, C1-C20alkyl, C3-C8cycloalkyl, phenyl, benzyl or C2-C20alkyl which is interrupted once or more than once by nonconsecutive O atoms and which is unsubstituted or substituted by OH and/or SH; or R12 and R13 together are C3-C5alkylene which can be interrupted by O, S or NR14; R14 is hydrog

Abstract: A tryptase inhibitor comprising as an active ingredient at least one member selected from among guanidinoaliphatic acid derivatives of the formula (I), guanidinobenzoic acid derivatives of the formula (II), guanidinophenol derivatives of the formula (III), amidinophenol derivatives of the formula (IV), and novel guanidinophenol derivatives of the formula (V) (in the formulae, Gu is guanidino).

Abstract: This invention relates to benzocycloheptene derivatives having novel structure. More particularly, it relates to new benzocycloheptene derivatives and pharmaceutically acceptable salts thereof, their production processes, a pharmaceutical composition containing the same and a use thereof for the manufacture of medicaments.

Abstract: There is provided compounds of formula I, 1

Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.

Abstract: Osmium-catalyzed aminohydroxylation reactions are accelerated and expanded in scope by the use of olefinic substrates having ionic groups, either anionic or cationic. The use of ionic groups on olefinic substrates also extends the aminohydroxylatable positions of unsaturations to include &agr;,&bgr;, &bgr;,&ggr;, and &ggr;,&dgr; positions, with respect to such ionic groups. A mechanism for the disclosed acceleration and extension is provided.

Abstract: Novel aminobutyric acids derivatives and methods for protecting crops against fungal diseases by applying to the crops or their locus a composition containing an effective amount of said derivatives.

Abstract: A process for producing (2R, 3S)-3-amino-4-phenylbutane-1,2-epoxide compounds which comprises treating a (2S, 3S)-3-amino-1-halo-2-hydroxy-4-phenylbutane compound or a (2S, 3S)-3-amino-4-phenylbutane-1,2-epoxide with a carboxylic acid quaternary ammonium salt or a carboxylic acid metal salt a quaternary ammonium salt and a quaternary ammonium salt, to give a (2S, 3S)-1-acyloxy-3-amino-2-hydroxy-4-phenylbutane compound, further treating the same with a sulfonic acid halide in the presence of an organic base to give a (2S, 3S)-1-acyloxy-3-amino-2-sulfonyloxy-4-phenylbutane compound, furthermore treating said compound with an inorganic base. An intermediate for the production of an HIV protease inhibitor can be produced from L-phenylalanine.

Abstract: Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halog

Abstract: Methods for preparing substituted aromatic carboxylic acid esters are described. In particular, the invention relates a method for preparing a nitro-substituted aromatic carboxylic acid ester: Additionally the invention relates to a method for preparing a thioether-substituted aromatic carboxylic acid ester: Such aryl esters are useful in the preparation of various agrochemicals and agrochemical intermediates.