Abstract: The present invention relates to a process for hydrogenating a substrate comprising a carbon-heteroatom double bond, the process comprising the step of reacting the substrate with hydrogen gas in the presence of a hydrogenation catalyst, wherein the hydrogenation catalyst is a complex of formula (I): R1-10, A and Hal are as defined in the specification. The present invention also provides processes for the preparation of the complex of formula (I) and intermediates thereof.

Abstract: A compound having the general formula (I) or a pharmacologically acceptable salt thereof: X—NH—Y—NH—R1??(I) [wherein X represents R2—SO2— in which R2 represents an optionally substituted lower alkyl group or phenyl group; Y represents a group selected from the group consisting of —R3—NH—R4—, —R5—NH—R6—NH—R7—, —R8—NH—R9—NH—R10—NH—R11—and —R12—NH—R13—NH—R14—NH—R15— in which R3 to R15 each independently represent a C3 to C5 alkylene group; and R1 represents hydrogen or an optionally substituted lower alkyl group, with the proviso that the case where X represents a tosyl group, Y represents —(CH2)3—NH—(CH2)4—NH—(CH2)3—and R1 represents hydrogen is excepted].

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Abstract: The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with ?-amyloid peptide.

Abstract: The invention relates to substituted fluoroalkoxyphenylsulfonylureas of the general formula (I) in which n, A, R1, R2, R3 and R4 are as defined in the description, to their use as plant treatment agents, in particular as herbicides and fungicides, and to a process and intermediates for their preparation.

Abstract: A compound having the general formula (I) or a pharmacologically acceptable salt thereof: X—NH—Y—NH—R1??(I) [wherein X represents R2—SO2— in which R2 represents an optionally substituted lower alkyl group or phenyl group; Y represents a group selected from the group consisting of —R3—NH—R4—, —R5—NH—R6—NH—R7—, —R8—NH—R9—NH—R10—NH—R11— and —R12—NH—R13—NH—R14—NH—R15— in which R3 to R15 each independently represent a C3 to C5 alkylene group; and R1 represents hydrogen or an optionally substituted lower alkyl group, with the proviso that the case where X represents a tosyl group, Y represents —(CH2)3—NH—(CH2)4—NH—(CH2)3— and R1 represents hydrogen is excepted].

Abstract: This invention provides a compound of the formula (I): wherein R1 represents a (C1–C6)alkyl group; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1–C6)alkyl group or a (C1–C6)alkoxy group; R3, R4, R5 and R6 each independently represents a hydrogen atom, a (C1–C6)alkyl, or a halogen atom; R7 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1–C6)alkyl group optionally substituted with a piperidino group, a (C1–C6)alkoxy group optionally substituted with a 3–7 membered cycloalkyl ring, a hydroxy(C1–C6)alkoxy group, a (C1–C6)alkoxy-(C1–C6)alkyl group, a (C1–C6)alkoxy-(C1–C6)alkoxy group, a halo (C1–C6)alkyl group, a (C1–C6)alkylthio group, a (C1–C6)alkylsulfinyl group or a (C1–C6)alkylsulfonyl group; R8 represents a (C1–C6)alkyl group, a halo(C1–C6)alkyl group, a (C1–C6)alkoxy group, a hydroxy(C1–C6)alkoxy group, a (C1–C6)alkoxy-(C1–C6)alkyl group or a (C1–C6)alkoxy-(C1–C6)alkoxy group; or R7 and R8, when adjacent to each other, taken together with the carbon atoms to whic

Abstract: A process for the preparation of a sulfonamide of formula (II), comprising reacting at elevated temperature an aniline of formula (I), with a sulfonating agent A of the formula R1—SO2-Z in the presence of a catalytic amount of either: (i) an amide B-1, other than N,N-dimethylformamide, or (ii) a high boiling tertiary amine B-2. Also provided in accordance with the present invention are processes for preparing sulfonamides of formula (II) by reacting an aniline of formula (I) with sulfanating agent A of the formula R1—SO2-Z in the presence of N,N-dimethylformamide, at a temperature in the range of about 120° C. to about 160° C. for about three to about seven hours.

Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2 and R3 each represents a lower alkyl group.

Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g.

Abstract: A water-soluble reference standard is useful for immunoassays of a lipophilic drugs.

Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula

Abstract: A method of synthesizing &agr;-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound &agr;-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.

Abstract: Compounds of peptide mimetic nature having the general formula I 1

Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.

Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.

Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.

Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.

Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.

Abstract: Aromatic sulfonamide derivatives, particularly benzenesulfonamide, 4-fluorobenzenesulfonamide, 5-chloro-1-naphthalenesulfonamide and 5-isoquinolinesulfonamide derivatives are provided that inhibit Ca.sup.2+ -dependent enzymes and proteins such as Phospholipase A.sub.2, protein kinases such as Protein Kinase C, and inhibit membrane fusion, thereby being a valuable drug for the treatment of inflammation, arthritis, infarction, nephritis and many other types of tissue injury.

Abstract: The composition, synthesis, and applications of tumor associated protease activated prodrugs of phosphoramide mustard, isophosphoramide mustard and analogs with detoxification functionalities are described. These drugs release a cytotoxic phosphoramide mustard analog following activation by tumor associated proteases and esterases. The general structure for these drugs is: ##STR1## Wherein R1 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; wherein X is a good leaving group such as a halogen; R2 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; or an amino group (NH.sub.2) which may optionally be substituted. Wherein A is a benzyloxy derivative with one or more acyloxy or acylamino groups in para or ortho portions relative to the phosphoester; and wherein the acyloxy or acylamino groups are not (substituted or unsubstituted) p-guanidino-benzoyloxy groups or p-guanidino-benzoylamino groups.

Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: An electrophotographic toner having polymeric binder and a charge control agent selected from the group consisting of sulfonamides having the general structure: ##STR1## and metal salts thereof. T.sup.1 is independently selected from H, alkyl having from 1 to 20 carbons, cycloalkyl having from 3 to 18 carbons, and aromatic and heteroaromatic ring systems having a solitary ring or 2 to 3 linked or fused rings. R.sup.1 is O, S, N--H, N--R.sup.5, or N--L--R.sup.5 ; where L is a linking group selected from: ##STR2## and R.sup.5 is independently selected from alkyl having from 1 to 20 carbons, cycloalkyl having from 3 to 18 carbons, and aromatic and heteroaromatic ring systems having a solitary ring or 2 to 3 linked or fused rings. L.sup.1 and L.sup.2 are each independently a direct link or divalent alkyl or fluoroalkyl having from 1 to 20 carbons. R.sup.a and R.sup.

Abstract: Process for preparing enantiomerically pure imidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-thiones of formula ##STR1## starting from 2,6-dihalo-3-nitrobenzyl derivatives (II) and suitably N-protected 1,2-diaminopropanes (III) ##STR2## Novel enantiomerically pure intermediates of formula (III) and (IV) prepared in the course of the present process.

Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.

Abstract: A novel hydroxamic acid compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof having cell growth inhibition, vascularization inhibition activities and the like.The compounds of the present invention possess inhibitory activities against the growth of vascular endothelial cells and the expression of lymphocyte adhesive factors and the detransforming activity of cells transformed by ras gene, and inhibit the cell growth and are effective on inflammation and tumor.

Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: A Novel N-substituted peptidyl compound represented by the general formula (1): ##STR1## where R.sub.1 is a straight-chained or branched acyl group having 2-10 carbon atoms, a branched, cyclic or bridged cyclic alkyloxycarbonyl group having 4-15 carbon atoms; a benzyloxycarbonyl group which is unsubstituted or substituted with a halogen atom, nitro group or methoxy group; a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluensulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group;R.sub.2 is a hydrogen atom or when taken together with R.sub.1, may form a phthaloyl group;R.sub.3 is an isobutyl group, a n-butyl group or an isopropyl group;R.sub.4 is a butyl group, andR.sub.5 is a hydrogen atom;provided that R.sub.1 can be an unsubstituted benzyloxycarbonyl group only when R.sub.3 is a n-butyl group.

Abstract: The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I ##STR1## wherein Ar, R, R.sub.1 and R.sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.

Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.

Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.

Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.

Abstract: The composition, methods of synthesis, and applications of a new class of tumor selective antineoplastic drugs is described. These novel antineoplastic agents are of the general structure: A-C-B. The agents are designed with two key functionalities: a trigger which toxifies the drug; (A) and a deactivator which detoxifies the drug (B) The trigger is selected such that it is activated by an enzyme which is present in elevated levels in the tumor. The deactivator is selected such that it is actuated by an enzyme ubiquitous to all tissues. The fate of the drug in a given cell is then determined by the ratio of the enzymatic activity that triggers toxication to the enzymatic activity which detoxifies the drug. The partitioning of the drug between toxic metabolite and nontoxic metabolite defines the resulting specificity of cytotoxic effect.

Abstract: An organic fluorine compound represented by the general formulaR.sub.f -(X).sub.h -R-Mwherein R.sub.f is a group selected from the following (a) and (b); ##STR1## X denotes a linking group selected from --O--, --S--, and --COO--, h denotes 0 or 1, R is a hydrocarbon chain comprising a phenylene group having an alkylene group with a total carbon number of 10 or more, or the derivative thereof, or an aliphatic alkylene group of a carbon number of 10 or more, and M is a group selected from --OH, --COOH, --SH, and --CONH.sub.2.The organic fluorine compound of the present invention greatly improves the dispersibility of magnetic powders in magnetic coating materials, has also an excellent rust prevention effect on metallic magnetic powders, and exhibits a marked dispersing effect even on fluorocarbon resin fine powders, which can be difficultly dispersed with conventional dispersing agents.

Abstract: Arylmethylenesulfonamidoacetamide and thioacetamide derivatives and arylmethylenesulfonamidoester intermediates therefor. The compounds are useful as selective herbicides especially with respect to the prevention and elimination of barnyardgrass in grass crops, especially in rice crops.

Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1 is absent or denotes hydrogen, alkyl or acyl, A denotes an acyl radical or an amino acid residue, B denotes an amino acid residue, and R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification, and to their salts, to a process for their preparation, to pharmaceutical products containing them, and to their use as medicaments, and intermediates for the preparation of these compounds.

Abstract: The process for the reaction of bicyclic amide acetals with reactive protic compounds of the general Formula ##STR1## wherein Y represents a member selected from the group consisting of ##STR2## R.sup.1 represents a member selected from the group consisting of hydrogen, an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 12 carbon atoms, and R.sup.2 represents a member selected from the group consisting of an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 12 carbon atoms, an alkylene ether group having from 1 to 50 carbon atoms, an arylene ether group having from 6 to 50 carbon atoms such as ethyl carbamate to form novel products which are useful as curing agents, blowing agents and monomers is disclosed.

Abstract: New compounds having the formula I ##STR1## where one of A and B is CH or N, the other of A and B is CH, Q is lower alkylene, R is lower alkyl, X.sub.1 is halogen or trifluoromethyl and X.sub.2 and X.sub.3 are independently selected from hydrogen, halogen, trifluoromethyl, lower alkoxy and lower alkyl and the pharmaceutically acceptable acid additions are disclosed as anti-hypertensive agents. New compounds having the formula II ##STR2## where Q, R, X.sub.2 and X.sub.3 are as explained above and n is 0 or 1 and their acid addition salts are useful as intermediates.

Abstract: An optically active alpha-amino acid derivative having the formula: ##STR1## wherein: X is OH, Cl, Br, I, or OCOR.sub.3 ;Y is a radical selected to stabilize the alpha carbon atom of the alpha-amino acid derivative sufficiently to prevent significant change in symmetry thereof during replacement of X with an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl or alkynaryl radical, or such radical having one or more chemical constituents thereon; andR.sub.1 and R.sub.2 are different from one another and are each hydrogen or an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl, or alkynaryl radical, or such radical having one or more non-protic chemical constituents thereon is conventionally synthesized from the corresponding alpha-amino acid. The ##STR2## portion of the above derivative is converted to a ketone functionality without racemization.

Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 momoered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.

Abstract: Cystamine derivatives of the formula: ##STR1## [wherein n represents 2 or 3, R.sup.1 and R.sup.2 each represents a hydrogen atom, or an alkyl group optionally substituted by a hydroxy, amino, alkylamino or dialkylamino group, or represents a cycloalkyl or aryl group, and X.sup.1 represents a group selected from the formulae .dbd.N--CN, .dbd.N--NO.sub.2, .dbd.N--COR.sup.3, .dbd.N--COOR.sup.3, .dbd.N--NH--CONH.sub.2, .dbd.N--SO.sub.2 R.sup.3, .dbd.CH--NO.sub.2, .dbd.CH--SO.sub.2 R.sup.3, .dbd.C(CN).sub.2, .dbd.C(CN)COOR.sup.3 and .dbd.C(CN)CONH.sub.2 (wherein R.sup.3 represents an alkyl or aryl group), or R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl group optionally substituted by a hydroxy, amino, alkylamino or dialkylamino group, or represents a cycloalkyl or aryl group and X.sup.1 represents an oxygen or sulphur atom] have been found to be useful in the promotion of the growth of non-human animals including birds.

Abstract: A method for preparing a 5-mercapto-1,2,3-thiadiazole salt represented by the general formula (I) is disclosed: ##STR1## the method comprises the steps of: providing a sulfonylhydrazone derivative represented by the general formula (II): ##STR2## providing a sulfide represented by the general formula (III):M--S--M' (III)(wherein R is an aryl group, X is a chlorine or bromine atom, M is an alkali metal atom and M' is a hydrogen atom or an alkali metal atom);combining the sulfonylhydrazone derivative represented by the general formula (II) and the sulfide represented by the general formula (III) and allowing a reaction to occur; andobtaining the 5-mercapto-1,2,3-thiadiazole salt represented by the general formula (I).

Abstract: This invention relates to a process for reducing amidine formation during reduction of organonitriles. The process comprises including a boron compound in the reaction medium in sufficient amount to complex the amidine compound as it is formed.

Abstract: N-methyl-N-(benzene sulfonic acid methylamide-N'-sulfenyl)-carbamic acid esters of the formula ##STR1## in which X is halogen, C.sub.1 -C.sub.6 alkyl or hydrogen, andR is a phenyl, naphthyl, benzodioxolanyl or indanyl radical optionally carrying at least one alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, alkynoxy, alkylmercapto, alkenylmercapto, alkynylmercapto, dialkylamino, trihalogenemethyl, halogeno, nitro, nitrile, cycloalkyl, formamidino, dioxanyl or dioxolanyl radical; or an oxime radical of the formula ##STR2## in which R.sup.1 and R.sup.2 each individually is alkyl, alkoxy, alkylthio or alkoxycarbonyl, the alkyl moieties of R.sup.1 and R.sup.2 optionally being linked to one another,which possess insecticidal and acaricidal properties.