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 is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: Oligopeptide analogs containing sulfonamide, urea or carbamate linkages in the backbone are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##

Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.

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: Certain dihydroxyindanone compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).

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: Substituted phenylsulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

Abstract: Tertiary amides have been developed which have low volatility and good thermal stability and which are effective in stabilizing organic materials that are normally susceptible to oxidative deterioration. The novel antioxidants are tertiary amides corresponding to the formula: ##STR1## wherein R is a mono-, di-, or trivalent aromatic or saturated aliphatic hydrocarbon group containing 1-20 carbons; n is an integer of 1-3 which is equal to the valence of R; R' is phenyl, benzyl, or C.sub.1 -C.sub.6 alkyl; m is an integer of 1-3; R" is a C.sub.1 -C.sub.4 alkylene group; Z and Z' are independently selected from hydrogen and alkyl; and Q is carbonyl or sulfonyl.

Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.

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 present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: Intermediate compounds (formula [III]and [IV]) useful as starting materials for the synthesis of amino acid derivatives which have renin inhibitory activity and which are useful as remedies for hypertension are prepared stereoselectively in high yield, without requiring complicated process steps. In this method, by reaction of .alpha.-amino aldehyde derivative [I] and compound [II] in the presence of BF.sub.3.OEt.sub.2, as shown in the following reaction formula, .alpha.-amino-.beta.-hydroxy-.delta.-ketone derivative [III] is prepared, and furthermore, by reducing it as required, compound [IV] is obtained: ##STR1## (where R.sup.1 is a protective group on the amino group, R.sup.2 is a lower alkyl group which may be branched, and R.sup.4 is a cyclohexyl group or phenyl group).

Abstract: A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.

Abstract: Adducts containing mesogenic or rodlike moieties are prepared by reacting (1) at least one compound containing an average of more than one vicinal epoxide group per molecule with (2) at least one compound containing an average of more than one reactive hydrogen atom per molecule; with the proviso that at least one member of components (1) and (2) contains a mesogenic or rodlike moiety. These compounds are useful as curing agents for epoxy resins.

Abstract: The invention describes N-fluorosulfonimides which are useful as fluorinating agents. The N-fluorosulfonimides are stable, easily synthesized, and allow the introduction of fluorine into organic compounds under mild conditions.

Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.

Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime either derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COR6, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.

Abstract: A tetrahydronaphthalene derivative of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and R.sup.2 is hydroxymethyl group, carboxyl group, a lower alkoxycarbonyl group or a group of the formula: ##STR2## wherein R.sup.3 is hydrogen atom or a lower alkyl group, R.sup.

Abstract: A sulfonamide derivative represented by the Formula: ##STR1## wherein A, B, X, Y, R, m and n are as defined in the specification, and a salt thereof have thromboxane A.sub.2 antagonism, therefore they are useful, for example, as blood platelet aggregation inhibiting agents.

Abstract: The present invention provides novel sulfonanilide and benzene-alkylaminium compounds which are the products of processes utilizing novel intermediates. Both the novel compounds and the novel intermediates are useful for the therapeutic or prophylactic treatment of arrhythmic activity.

Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.

Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.

Abstract: Compounds of the formula I ##STR1## where R.sup.1 to R.sup.5 have the meaning indicated, a process for their preparation and their use as medicaments are described. They are effective lipid-lowering agents with antioxidative properties from the benzenesulfonamide series. They do not have hypotensive and diuretic properties.

Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.

Abstract: Tertiary sulfonamides having utility as antioxidants are compounds corresponding to the formula: ##STR1## wherein R and R' are independently selected from alkyl, aryl, and benzyl groups, R" is an alkylene group containing 1-5 carbons, and n is an integer of 1-3.

Abstract: Organic materials which are normallly susceptible to oxidative deterioration are stabilized with tertiary sulfonamide antioxidants corresponding to the formula: ##STR1## wherein R and R' are independently selected from alkyl, aryl, and benzyl groups, R" is an alkylene group containing 1-5 carbons, and n is an integer of 1-3.

Abstract: Cyclic 1-one-2-ene-3-ol compounds substituted in 2-position by an aroyl or heteroaroyl group bearing a hydrocarbylsulfonyloxy or hydrocarbylsulfonylamino substituent exhibiting herbicidal activity.

Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH-- or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.

Abstract: Leuco dyes of the formula (I) are disclosed, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent an alkyl group having 1 to 10 carbon atoms; X represents hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms or a halogen; and Y represents R.sub.5 --Z--SO.sub.2 NH--, R.sub.6 --Z--CONH--, or ##STR2## in which Z represents ##STR3## R.sub.5 and R.sub.6 each represent hydrogen, an alkyl group having 1 to 10 carbon atoms, or a halogen; and R.sub.7 and R.sub.8 each represent hydrogen, a cyano group, or --COR.sub.9, in which R.sub.9 represents a lower alkyl group, a lower alkoxyl group, a phenyl group which may be substituted by an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms, or a halogen; a naphthyl group which may be substituted by an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms or a halogen with the proviso that R.sub.7 and R.sub.8 are not both hydrogen.

Abstract: A process for the preparation of alkane- and arenesulfonamides in high purity and yield is provided. Ammonia or alkylamine is reacted under boiling conditions with an alkane- or arenesulfonyl halide in the absence of an added solvent. The heat of reaction is dissipated by the heat of vaporization of the ammonia or alkylamine.

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: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.

Abstract: Process for the introduction of functional or functionalizable substituents para to the amino group in 2-aminophenols and 3-aminophenols. The process proceeds in one step, with substitution occurring selectively at the position para to the amino group. Consequently, the reaction is surprisingly straightforward, with very little or no contamination by isomeric by-products. The process comprises reaction of (a) an aminophenol having an open para position to the amino function, with (b) an unhindered non-enolizable aldehyde, and (c) a thiol or sulfinic acid which acts as a nucleophile. In preferred embodiments, the process is conducted at a temperature of from about 50.degree. C. to about 100.degree. C., and in the presence of a polar solvent. The reaction is promoted by an acid having sufficient acidity to protonate the amino group of the aminophenol. Preferably, the acid promoter is a mineral acid, and it is present in an amount at least substantially equivalent to the amount of aminophenol reactant.

Abstract: A process for preparing a squarylium compound useful as a photoconductive material for an electrophotographic photoreceptor, in which process comprises reacting an arylhydroxycyclobutenedione salt or a hydroxycyclobutenedione derivative with an aniline derivative is disclosed. The process comprises dropwise adding a solution of the arylhydroxycyclobutenedione salt or hydroxycyclobutenedione derivative in a solvent, to an alcohol solution of the aniline derivative in an alcohol solvent. An electrophotographic photoreceptor produced by using the thus obtained squarylium compound exhibits and sensitivity, satisfactory chargeability, low dark decay, low residual potential, and excellent stability after repeated use.

Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.

Abstract: Polymers, such as polysiobutylene or ethylene-propylene copolymers, are functionalized by reaction with an activated imine to yield novel polymers.

Abstract: Polymers, such as polyisobutylene or ethylene-propylene copolymers, are functionalized by reaction with an activated imine to yield novel polymers.

Abstract: Disclosed herein is a sulfonamide compound represented by the formula (I): ##STR1## wherein A represents a phenyl group which may be substituted, B represents a phenyl group which may be substituted, R represents a lower alkyl group, a lower alkoxy group or a lower haloalkyl group, W represents a hydroxyl group or a halogen atom, and z represents a halogen atom, a lower alkysulfonyloxy group which may be substituted, or a phenylsulfonyloxy group which may be substituted, and a herbicidal composition containing the sulfonamide compound as an effective ingredient.

Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.

Abstract: Phenylsulfone alkenoic acids and derivatives thereof are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR wherein R is hydrogen, alkali metal or lower alkyl or X is 5-tetrazolyl or ##STR2## wherein R' is lower alkyl or aryl; n is 2, 3 or 4 and m is 2, 3 or 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic disease.

Abstract: The present invention provides sulphonylphenylalkylamines of the general formula: ##STR1## wherein R.sub.1 is an alkyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3-7 carbon atoms or an aralkyl, aralkenyl or aryl radical, the aryl moiety, in each case, being optionally substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.16 acyl or azide, R.sub.2 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical or an aralkyl or aralkenyl radical, the aryl moiety, in each case, optionally being substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.

Abstract: Novel phenoxyacetic acid derivative of the formula: ##STR1## wherein R is a substituted or unsubstituted phenyl group, naphthyl group or a sulfur-containing 5-membered hetero-monocyclic group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or phenyl group, R.sup.5 is hydrogen atom or a lower alkyl group, R.sup.6 is carboxyl group, a protected carboxyl group, hydroxy group or a di(lower alkyl)-amino group, Ring A is a substituted or unsubstituted phenylene group, m is 0 or 1 and n is an integer 0 to 5, provided that, when m is 0,(1) at least either one of R.sup.1 to R.sup.4 is or/are a phenyl-lower alkyl group or phenyl group,(2) at least either one of R.sup.1 to R.sup.4 is or/are a lower alkyl group, and R.sup.6 is hydroxy group, or(3) all of R.sup.1 to R.sup.4 are hydrogen atom, and Ring A is a substituted phenylene group,or a pharmaceutically acceptable salt thereof are disclosed.

Abstract: Disclosed herein are N-(2-chloro-4-nitrophenyl)-3-trifluoromethyl-benzenesulfonamide derivatives represented by the following general formula (I): ##STR1## wherein X and Y individually mean a hydrogen or chlorine atom and agricultural fungicides containing said derivatives.

Abstract: Amino acid amides of formula (I): ##STR1## wherein R.sup.1 -R.sup.5 and Y represent a variety of organic groups and atoms (including where R.sup.2, Y and the adjacent nitrogen atom together represent a thiazolidine or pyrrolidine group) and X represents carbonyl or sulfonyl are mostly new compounds and have valuable anti-tumor and immuno-regulatory activities. They may be formulated in compositions for pharmaceutical use.

Abstract: A dielectric medium composition comprising a fluorine-containing amide or a fluorine-containing sulfonamide and capacitors or other electric devices incorporating said composition, are disclosed herein.

Abstract: Novel quaternary ammonium salts of general formula (I) ##STR1## wherein: R is a saturated or unsaturated, linear or branched alkyl radical of C.sub.1 to C.sub.8.R' is a saturated or unsaturated, linear or branched alkyl radical of C.sub.1 to C.sub.12, or a benzyl radical.n is a number equal to 2 or 3.X.sup..theta. is a halogenide anion, such as Cl.sup..theta., Br.sup..theta., I.sup..theta., are used as phase transfer catalysts, in heterogeneous ionic reactions wherein the reagents are in different phase and have different polarity.

Abstract: Compounds corresponding to Formula I ##STR1## wherein R.sup.1 denotes an acyl group andX denotes hydrogen, halogen, alkoxy, aroxy, SO.sub.3 H or a heterocyclic group attached through --O-- or --N<are prepared form a compound corresponding to Formula II ##STR2## wherein X has the meaning already indicated and Q denotes the group required for completing a dicarbonimide ringby reduction of the said compound to the amino compound and acylation into a compound corresponding to Formula III ##STR3## wherein X, Q and R.sup.1 have the meanings indicatedfollowed by conversion of the compound corresponding to Formula III into a compound corresponding to Formula I by hydrazinolytic or hydrolytic decomposition of the dicarbonimide ring.

Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4, E.sub.4 and the slow reacting substance of anaphylaxis.As such, these compounds will be useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.