Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is, oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of Formula 1 ##STR1## wherein the symbols are as defined in the specification, have retinoid like biological activity.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.

Abstract: A process for the preparation of a compound of general formula II: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 -C.sub.10 hydrocarbyl or heterocyclyl having 3 to 8 ring atoms, either of which may optionally be substituted; each R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is independently hydrogen or C.sub.1 -C.sub.4 alkyl; A is an optionally substituted aromatic or heteroaromatic ring system; and R.sup.21 is hydrogen, halogen, OH or OCONHR.sup.1, wherein R.sup.1 is as defined above; the process comprising cyclizing a compound of general formula III: ##STR2## wherein A, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.21 are as defined in general formula II and R.sup.25 is a leaving group such as a halogen atom; under basic conditions.

Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid antoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

Abstract: A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.

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: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: This invention relates to perhydroisoindole derivatives of 08/448,402 formula (I), wherein radicals R are phenyl radicals optionally 2-or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R.sub.3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists.

Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: [Object]To provide a new 2,4-oxazolidinedione derivative possessing excellent hypoglycemic and hypolipidemic activities.[Constituent]A 2,4-oxazolidinedione derivative represented by the general formula: ##STR1## wherein X represents --CH.sub.2 --, --C(.dbd.O)--, --CH(OH)--, --C(.dbd.NOH)-- or --CH.dbd.CH--; R represents a hydrocarbon residue or heterocyclic group which may be substituted; n represents an integer from 0 to 5, and m represents an integer from 1 to 3; ....... represents a single or double bond; provided that n is an integer from 1 to 5 when X is --C(.dbd.O)--, or a pharmacologically acceptable salt thereof.

Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.5 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.5 ;(i) --Z.sup.4 --NR.sup.6 R.sup.7 ;--Z.sup.4 --N(R.sup.10)--Z.sup.5 --NR.sup.8 R.sup.9 ; or(k) R.sup.3 and R.sup.4 together may also be alkylene or alkenylene, either of which may be substituted with Z.sup.1, Z.sup.2 and z.sup.3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.

Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: Substituted thiazoles, oxazoles and 2-hydroxy morpholine compounds useful in the treatment of diabetes mellitus and obesity are described.

Abstract: The present invention relates to a group of organic chelators whose affinity for calcium ion in solution is decreased by electromagnetic radiation. Specifically, the chelators are related to fura-2 and utilize the addition of an azide group to the 3-position of the benzofuron ring of a fura-2 type structure. Photolysis of the azide group causes the calcium ion affinity to decrease 100 to 1000 fold. These chelators when incorporated into rat fibroblasts either by microinjection or by incubation as the membrane-permeable, enzymatically-labile esters and flash-photolyzed cause large increases in intracellular free calcium ion. These chelators are used to generate controlled fast elevation of intracellular free calcium ion concentration to mimic or modulate a number of important cellular responses, especially in nerve or muscle.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or (CH.sub.2).sub.m R.sup.3 where R.sup.3 is cycloalkyl and m is 1 or 2;R.sup.1 is alkyl;R.sup.2 is alkyl, aryl or aryl substituted with halogen or alkyl;R.sup.4 is alkyl;n is an integer from 1 to 5;p is an integer from 0 to 6;Y is NH, oxygen or sulfur; andZ is hydrogen, alkyl, alkoxy, NR.sup.6 R.sup.5 wherein R.sup.6 and R.sup.5 are independently hydrogen or alkyl, or SR.sup.7 wherein R.sup.7 is hydrogen, benzyl or alkyl.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in the treatment of leukotriene B.sub.4 mediated conditions.

Abstract: The present invention discloses several new calcium indicator dyes which are retained in the cytosol or which bind to cellular membranes and report calcium levels near the membrane. These indicators are analogs of a previously described tetracarboxylate calcium indicator fura-2 and indo-1 where the 5' methyl of the BAPTA moiety is replaced with a derivative of propionic acid in the form of --CH.sub.2 CH.sub.2 CON--(CH2).sub.n --N(X.sub.1)X.sub.2, where n is 4. The propionic acid derivative provides a flexible means for introducing additional functionality to the calcium indicator without greatly impacting the fluorescence and ion chelating properties of the parental indicator. When X.sub.1 is CH.sub.2 COOH and X.sub.2 is part of a ring system like piperazine, a fluorescent calcium indicator, Fura-PE3, is obtained which resists compartmentalization and leakage out of the cytosol.

Abstract: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.

Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.

Abstract: The present invention relates to a group of organic chelators whose affinity for calcium ion in solution is decreased by electromagnetic radiation. Specifically, the chelators are related to fura-2 and utilize the addition of an azide group to the 3-position of the benzofuran ring of a fura-2 type structure. Photolysis of the azide group causes the calcium ion affinity to decrease 100 to 1000 fold. These chelators when incorporated into rat fibroblasts either by microinjection or by incubation as the membrane-permeable, enzymatically-labile esters and flash-photolyzed cause large increases in intracellular free calcium ion. These chelators are used to generate controlled fast elevation of intracellular free calcium ion concentration to mimic or modulate a number of important cellular responses, especially in nerve or muscle.

Abstract: Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula ##STR1## wherein: C.sub.m H.sub.p is an alkylene chain wherein m is 0, 1, 2, or 3 and p=(2.times.m)-1, except that when m is 0, p is also 0;n is 0, 1, 2 or 3;R is CO.sub.2 R', CH.sub.2 OH, CONHSO.sub.2 R.sup.3, CONHR.sup.4, or --CH.sub.2 --5--tetrazolyl;R' is hydrogen, alkyl, or alkali metal;X is O or NH;Y is --O--, a single bond or vinylene, except that Y cannot be --O-- when n is 0;and the remaining symbols are as defined in the specification.

Abstract: Compounds of the formula ##STR1## wherein X is O or S;Y is O or S;R.sup.1 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy;R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkenyloxy, C.sub.2 -C.sub.4 alkynyl, C.sub.2 -C.sub.4 alkynyloxy, mono-, di- or tri-halomethyl, trifluoromethoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.3 -C.sub.4 branched alkylthio, nitro, or cyano;R.sup.3 is hydrogen, halogen, methyl, mono-, di- or tri-halomethyl;R.sup.4 isa) C.sub.3 -C.sub.8 cycloalkyl substituted by one or more C.sub.1 -C.sub.4 alkyl, preferably one or two methyl;orb) ##STR2## wherein R.sup.6 and R.sup.7 are independently, hydrogen or linear or branched, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, or C.sub.2 -C.sub.4 alkynyl, and R.sup.8 is C.sub.3 -C.sub.8 cycloalkyl substituted by one or more C.sub.1 -C.sub.4 alkyl; andR.sup.5 is an acyclic or cyclic side chain as defined herein.

Abstract: Crop protection agents contain dihydropyrans of the formula ##STR1## wherein the variable substituents are defined in the specification.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 -R.sub.5, X, Y, A, B are as defined in the specification have retinoid-like biological activity.

Abstract: A process for the separation of at least one isomer from a mixture of isomers of a tetrahydropyran-2-one, having at least two chiral centers which comprises selective reaction of at least one isomer with a reagent catalyzed by a hydrolase enzyme whereby at least one isomer is preferentially converted into a distinct chemical species from the other isomers so that it is susceptible of separation by an appropriate chemical or physical separation process in which the tetrahydropyran-2-one is of Formula (1): ##STR1## wherein: Z is --H or a protecting group susceptible of reaction with the reagent under the influence of the enzyme; andY is formyl or protected formyl.

Abstract: A new class of calcium-specific, NMR-active and/or fluorescent indicators having a high dissociation constant is described. Methods of determining intracellular calcium ion concentration using .sup.19 F NMR spectroscopy or optical methods are also provided.

Abstract: A process for the manufacture of 5-cyano-4-lower alkyl-oxazoles is described in which a 5-carbamoyl-4-lower alkyl-oxazole is dehydrated in an organic solvent under mild conditions with cyanuric chloride and an N,N-disubstituted-formamide.

Abstract: Compounds of the formulae ##STR1## where R is cycloalkyl or aryl; R.sub.1 is alkyl, X is O or C.dbd.O; A is O or S; and B is N or CH are useful as hypoglycemic agents.

Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

Abstract: The present invention provides compounds of Formula I, ##STR1## or a pharmaceutically acceptable salt forms thereof, which are inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.

Abstract: Cyanooxime ethers of the formula IR.sup.1 R.sup.2 CH--ON.dbd.C(CN)--R.sup.3 IwhereR.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.2 is an unsubstituted or substituted mononuclear to trinuclear aliphatic or aromatic ring system which, in addition to carbon atoms, may contain from one to four nitrogen atoms or from one to three hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen andR.sup.3 is unsubstituted or substituted alkyl or an unsubstituted or substituted aliphatic ring system which, in addition to carbon atoms, may contain one or two hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen,processes for their preparation, agents containing them and their use.

Abstract: This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; R.sub.3 is optionally 2-substituted phenyl; R.sub.4 is OH or fluorine when R.sub.5 is H, or R.sub.4 and R.sub.5 are OH or R.sub.4 and R.sub.5 together form a bond; isomeric forms and mixtures thereof; optionally salts thereof where applicable; and preparation thereof. The novel derivatives are particularly useful as P substance antagonists.

Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkoxy;R.sup.3 istetrazolyl, orand R.sup.4 and R.sup.5 are each hydrogen, hydroxy, acyloxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halo, optionally substituted phenyl, --SO.sub.3 H or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl;provided that when R.sup.3 is --CR'R".CHR'"CO.sub.2 H or tetrazolyl, R.sup.1 and R.sup.2 are each hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl C.sub.1-4 alkoxy; andor a pharmaceutically acceptable salt or ester thereof.

Abstract: 4-heteroaroylisoxazole derivatives of formula I: ##STR1## wherein: Ar represents an optionally substituted group Het, wherein Het represents a first heterocyclic ring containing from one to four heteroatoms in the ring selected from oxygen, nitrogen and sulphur, which is optionally fused with a benzene, or carbocyclic or second heterocyclic ring (which is optionally saturated or partially saturated) to form a bicyclic system, wherein the first heterocyclic ring of the group Het is attached to the carbonyl group in the 4-position of the isoxazole ring;R represents hydrogen or --CO.sub.2 R.sup.3 ;R.sup.1 represents alkyl or haloalkyl or a cycloalkyl group optionally substituted by one or more groups R.sup.4 ;R.sup.3 and R.sup.4 independently represent alkyl or haloalkyl;agriculturally acceptable salts thereof and their use in weed control is described.

Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.

Abstract: Compounds of the formula ##STR1## as herein defined, have retinoid-like activity and are substantially non-teratogenic and non-irritating to the skin.

Abstract: This invention relates to polyaminopyrrolecarboxyamide derivatives of general formula (I) and their pharmaceutically acceptable salts, in which A represents a chemical bond or an aromatic or heteroaromatic radical, and:if A is a chemical bond, R is hydrogen, alkyl, dialkylaminoalkyl, alkenyl, cycloalkyl, arylalkyl, arylalkenyl, haloalkyl, or an aromatic or heteroaromatic radical;whereas if A is an aromatic or heteroaromatic radical, R is nitro, amino or formylamino;n is 0 or a whole number between 1 and 4;Z is an alkylene or aromatic radical.

Abstract: The preparation of isoxazole-4,5-dicarboxylic diester of the formula I ##STR1## where R.sup.1 is any organic radical which is inert under the reaction conditions, and R.sup.2 and R.sup.3 are each alkyl, cycloalkyl or benzyl, entails reacting an aldoxime of the formula II ##STR2## with a diester of maleic or fumaric acid, of the formula IIIR.sup.2 OOC--C.dbd.C--COOR.sup.3 (III)where R.sup.2 and R.sup.3 are identical or different and have the abovementioned meanings, in the presence of an aqueous solution of a hypohalite which is present in excess relative to II.

Abstract: This invention relates to compounds compounds useful in treating diseases mediated by one or more leukotrienes or oxidative modification of low density lipoprotein such as inflammation, bronchoconstriction or atherosclerosis. The compounds of this invention have the formula: ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, fluorine, chlorine, bromine, iodine, C.sub.1 -C.sub.6 alkyl, trifluoromethyl, C.sub.1 -C.sub.6 alkoxy, or C.sub.1 -C.sub.6 trifluoroalkoxy; R.sup.2 and R.sup.4 are hydrogen or methyl independently;R.sup.5 is hydrogen, methyl or hydroxy;X and Z are independently oxygen or sulfur;andY is --CH.sub.2 --, --CH(CH.sub.3)--, or --CH.dbd.CHCH(CH.sub.3)--.