Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.

Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases and conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.

Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where X, W, Z, A, G, R1, R2, R3, R4, R5, R5′ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. In general formula (I), for example, Ar represents an aryl radical, R represents an alkoxyacetyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof.These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

Abstract: This invention relates to a process for preparing perylene pigment compositions by reaction of(a) a perylene tetracarboxylic compound;(b) about 0.01 to about 20% by weight, relative to the perylene tetracarboxylic compound, of a non-pigmentary cyclic anhydride or imide of formula (I) ##STR1## wherein W is O or NR' (where R.sup.1 is hydrogen, a metal, or optionally substituted alkyl, cycloalkyl, aralkyl, or aryl), R.sup.2, R.sup.3, and R.sup.4 are various combinations of substituents and/or fused-on rings, and the dotted line is an optional double bond representing R.sup.2 --C.dbd.C--R.sup.3 ;(c) ammonia or a primary alkyl, aralkyl, or aryl amine; optionally in the presence of(d) a solvent and/or(e) one or more dispersants.

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

Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.

Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: A description is given of compounds of the formula I ##STR1## where r is 0 or 1 and y is a number from the range 1-3; X is a direct bond or --NR.sub.8 --, --CO--, --CONH-- or --COO-- or a divalent aliphatic or mixed aromatic-aliphatic C.sub.1 -C.sub.18 hydrocarbon radical;Z is an aromatic, aliphatic or mixed aromatic-aliphatic C.sub.3 -C.sub.18 hydrocarbon radical which is interrupted in the aliphatic moiety by one or more divalent functional groups, in each case in a carbon-carbon single bond, and/or in the aromatic or aliphatic moiety by one or more divalent functional groups, in each case in a carbon-hydrogen bond, possible functional groups being --O--, --NR.sub.8 --, --S--, --SO--, --SO.sub.

Abstract: There are provided ammonium oxazole intermediates of formula I and amino oxazolium intermediates of formula II, useful in the manufacture of insecticidal arylpyrrole compounds.

Abstract: This invention provides a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.3 independently are hydrogen, --CHO, --COCH.sub.3, --COR.sup.7, --A--Ar--(Q).sub.z, etc.; wherein D is a C.sub.1-6 linear, C.sub.3-8 branched or cyclic group having from 4 to about 15 atoms, consisting of C, etc.; wherein D is unsubstituted or substituted with one or more groups independently selected from the group consisting of --OH, NH.sub.2, --NHR.sub.7, etc.; wherein each Q is independently --CNH(NHY), --NHCNH(NHY), --SO.sub.2 W, --SOW, etc.; wherein Y is hydrogen, alkyl, alkenyl, --B--NH.sub.2, --B--NHR.sup.8, etc.; wherein W is alkyl, alkenyl, --B--NH.sub.2, etc.; wherein A nd B independently are a bond, or a C.sub.1-6 linear, C.sub.3-8 branched or cyclic linking group having from 1 to about 15 atoms, consisting of C, optionally interrupted by N, S, P and O; wherein A and B independently are unsubstituted or substituted with --OH, NH.sub.2, etc.; wherein R.sup.7 is an alkyl, a branched alkyl, etc.; wherein R.sup.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

Abstract: There are provided ammonium oxazole intermediates of formula I and amino oxazolium intermediates of formula II, useful in the manufacture of insecticidal arylpyrrole compounds.

Abstract: The invention relates to novel heterocyclic imino derivatives, several processes for their preparation and their use for controlling pests.

Abstract: Poly(amino acid) derivatives, which are chelating agents of paramagnetic metal ions, in which at least 3 of the donor nitrogen atoms carry identical or different substituents, of formulaCH(R.sub.1)--X,in which X represents CO.sub.2 R.sub.a, CONR.sub.b R.sub.c or P(R.sub.d)O.sub.2 H and R.sub.a, R.sub.b and R.sub.c, which are identical or different, represent H or optionally hydroxylated (C.sub.1 -C.sub.8)alkyl, R.sub.d represents OH, (C.sub.1 -C.sub.8)alkyl or (C.sub.1 -C.sub.8)alkoxy and R.sub.1 represents a hydrophilic group with a molecular weight greater than 200 containing at least 3 oxygen atoms, with the proviso that at least 3 of the X groups are optionally salified acid functional groups.

Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: A compound of the formula: ##STR1## is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: The present invention relates particularly to novel preorganized hexadentate ligands that are suitable for completing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.

Abstract: 1,4-Diketopyrrolopyrroles of the formula ##STR1## in which A and B independently of one another are a group of the formula ##STR2## R.sub.1 is a long-chain radical containing a reactive group capable of polymerization, and R.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR3## or R.sub.1. The novel diketopyrrolopyrroles are suitable for preparing coloured polymers with unexpectedly advantageous colour effects.

Abstract: The present invention relates to novel DNA alkylating agents and the prodrugs of these agents which are useful as antitumor agents and DNA labelling agents. The compounds are hydroxy dihydrobenzindole oligopeptides and prodrugs thereof wherein the monomeric constituents are derived from monocyclic or bicyclic heterocyclic aromatic residues.

Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.

Abstract: Novel heterocyclic compounds having a structure according to general formula (1), pharmaceutically acceptable acid addition salts and solvates thereof are described as having a pharmacological profile showing potential for treatment of acute and chronic neuropsychiatric disorders which are known as progressively deteriorating conditions leading to neuronal cell death and dysfunction. Pharmaceutical formulations are described as containing said therapeutic compounds.

Abstract: The present invention provides compounds, more particularly dipeptide analogs, which bind to retroviral proteases. These compounds are inhibitors of retroviral proteases and are useful for treating diseases related to infection by retroviruses.

Abstract: A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof.These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Compounds of the Formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, hydroxy, halo, optionally substituted phenyl, amino, nitro or trifluoromethyl; andX is --NH--, --O-- or --S--;and the pharmaceutically acceptable salts thereof exhibit high affinity and selectivity for imidazoline receptors, and are are particularly useful for modification of the female reproductive cycle.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Compounds of general Formula I ##STR1## wherein R.sup.3 is a saturated, unsaturated, straight- or branched-chain or cyclic aliphatic hydrocarbon residue of up to 16 carbon atoms or, if R.sup.4 is a hydrogen atom, a cycloalkyl group or an aryl or aralkyl group optionally substituted by one or several C.sub.1 -C.sub.6 -dialkylamino groups or by one or several C.sub.1 -C.sub.6 -alkoxy groups,R.sup.4 is a hydrogen atom, a saturated, unsaturated, straight- or branched-chain or cyclic hydrocarbon residue of up to 16 carbon atoms, orR.sup.3 and R.sup.4 jointly mean a saturated or unsaturated 5- or 6-membered ring optionally substituted or containing an O, S, N atom or oxo substituent, and Y is COOX or CONR.sub.3 R.sub.4,are valuable complexing agents, complexes or complex salts, e.g., for use as NMR or X-ray diagnostic image-enhancement agents or radioactive diagnostic agents.

Abstract: Compounds of the formula ##STR1## where R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently are H or lower alkyl of 1 to 10 carbons; R.sub.5 is lower alkyl of 1 to 10 carbons, fluoro, chloro, bromo, iodo, nitro, or fluoroalkyl having 1 to 10 carbons; m is an integer having the value of 1-4; n is an integer having the value of 0-4; Y is phenyl or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl, said Y group being optionally substituted with one or more R.sub.5 group; A is (CH.sub.2).sub.p where p is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.

Abstract: A process for the synthesis of a compound of general formula II: ##STR1## wherein: R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl;A is an aromatic or heteroaromatic ring system optionally substituted with one or more substituents as defined herein; and in which any ring nitrogen atom may be quaternised or oxidised;alternatively, any two substituents of the group A may combine to form a fused 5- or 6-membered saturated or partially saturated carbocyclic or heterocyclic ring in which any carbon or quaternised nitrogen atom may be substituted with any of the groups defined herein for A or in which a ring carbon atom may be oxidised;the process comprising cyclising a compound of general formula VII: ##STR2## wherein A, R.sup.2 and R.sup.3 are as defined for general formula II, R.sup.20 is hydrogen, benzyl or benzyl substituted with up to five substituents selected from halo, C.sub.1 -C.sub.6 alkyl, O(C.sub.1 -C.sub.6 alkyl) or nitro and R.sub.21 is C.sub.1 -C.sub.

Abstract: The invention relates to compounds of formula (I): ##STR1## wherein: R.sub.1 and R.sub.2 are selected, each independently of the other, from hydrogen and an alkyl radical,A is selected from the radicals: ##STR2## wherein: R.sub.3 represents a radical selected from halogen, alkyl, alkoxy, amino, 2-acetyl, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, trifluoromethyl and cyano,R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are selected, each independently of the others, from hydrogen, a halogen, an alkyl, alkoxy, amino, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, cyano and a trifluoromethyl radical,R.sub.

Abstract: The present invention provides aminocyclopentane derivatives which are saccharide analogs having extremely high .alpha.-glucosidase inhibitory effects and novel structures and expected to be usable or applicable to drugs or agricultural chemicals. An aminocyclopentane derivative represented by the formula (1), wherein R.sub.1 represents H while R.sub.2 represents CH.sub.2 OH, or R.sub.1 represents CH.sub.2 OH while R.sub.2 represents H and R.sub.3 represents a substituted or unsubstituted aryl group or an alkyl, alkenyl, alkynyl or hydroxyalkyl group having 1 to 10 carbon atoms, intermediates for the synthesis of the same, a process for producing the intermediates and a process for producing the aminocyclopentane derivative.

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

Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.

Abstract: A process for preparing a compound of formula I ##STR1## wherein R and R" are as described herein. Compounds of formula I are useful as intermediates in the preparation of florfenicol.

Abstract: The present invention provides 5-amino-4-aryl-2-perfluoroalkyl-1,3-oxazole derivatives, a method for the preparation of said derivatives and their use as a key intermediate in the manufacture of insecticidal, acaricidal and nematocidal arylpyrrole compounds.

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: New catechol derivatives and pharmaceutically acceptable salts and esters thereof useful as pharmaceutical antioxidants are disclosed. Cellular damage by oxygen derived radicals is a significant factor in heart disease, rheumatoid arthritis, cancer, inflammatory disease, transplant rejection reactions and ischemia.

Abstract: Herbicidal novel tetrazolinone derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, andR.sup.2 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, orR.sup.1 and R.sup.2 form, together with the nitrogen atom to which R.sup.1 and R.sup.2 are bonded, a 5- or 6-membered heterocyclic ring, optionally fused to a carbocyclic ring optionally and independently substituted by C.sub.1-4 alkyl, andR.sup.3 is a 5-membered heterocyclic radical containing at least one hereto atom selected from the group consisting of nitrogen, oxygen, and sulfur, optionally substituted by at least one substitutent selected from the group consisting of halogen, benzyl, phenyl, halogen-substituted phenyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkyl-sulfonyl and C.sub.

Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.

Abstract: There is disclosed a dithiocarbonimide derivative of the formula: ##STR1## wherein B is a C.sub.1 -C.sub.6 alkyl group; X is an NH group or an oxygen atom and Y is a nitrogen atom or a CH group, A is a phenyl group, a heterocyclic group, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a bicycloalkyl group or a tricycloalkyl group, all of which may be substituted. Also disclosed are a fungicidal/insecticidal/acaricidal agent containing the dithiocarbonimide derivative as an active ingredient, an intermediate for use in the production of the dithiocarbonimide derivative, and a process for producing the dithiocarbonimide derivative from the intermediate.

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.