Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

Abstract: Compounds of formula (1): 1

Abstract: Method of producing compounds of formula 1

Abstract: 1

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates the

Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: 1

Abstract: The present invention is directed to cyclic amines of the formula I: (wherein R1, R2, R3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.

Abstract: The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with matrix metalloproteinase, ADAM or ADAM-TS enzymes, a condition that is mediated by TNF &agr; or a condition involving a membrane-shedding event that is mediated by a metalloproteinase. Compounds of the invention are of formula I (B)2N—X—(CH2)m—W—(CR1R2)n—COY  (I) wherein n=0 or 1; m=0 or 1; X is S(O)1-2; Y is OH or NHOH; W is aryl or heteroaryl; and the other groups are as defined herein.

Abstract: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).

Abstract: Compounds of the formula: wherein the substituents are defined herein which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.

Abstract: Novel 2,5-substituted benzolsulfonyl ureas and thioureas of formula (I) as illustrated in the disclosure. The compounds are useful active ingredients for medicaments. The compounds of formula (I) act as inhibitors on ATP-sensitive potassium canals and are suitable for the treatment of cardiovascular disorders, especially the treatment of arrhythmias, prevention of sudden death from heart disease or affect diminished contractility of the heart. The invention also relates to methods for producing compounds of formula (I), the use thereof and pharmaceutical preparations containing said compounds.

Abstract: &agr;-Unsaturated amines of the formula: wherein X1 and X2 are such that one is an electron-attracting group with the other being a hydrogen atom or an electron-attracting group; R1 is a group attached through a nitrogen atom; R2 is a hydrogen atom or a group attached through a carbon, nitrogen or oxygen atom; n is an integer equal to 0, 1 or 2; A is a heterocyclic group or a cyclic hydrocarbon group, and salts thereof and their agrochemical use as insecticidal and/or miticidal agents are described.

Abstract: New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

Abstract: A series of antagonists of NPY have been synthesized and are comprised of thiourea linked piperazine and piperidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where Z is NR7R8 or and X is CH or N. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: Compounds of the formula I in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, phenyl which is unsubstituted or at most trisubstituted by halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, or benzyl which is unsubstituted or at most trisubstituted in the aromatic ring in the same manner, or is cyclopropylmethyl, C1-C4haloalkyl, C2-C5alkoxyalkyl, cyanomethyl, CO—R6, OH, NH2, C1-C4alkylamine or C1-C4alkoxycarbonyl-C1-C2alkyl; X is oxygen, sulfur or NR5; R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, C(O)R6, OH or C1-C4alkoxy, NH2 or C1-C4alkylamine; R5 is hydrogen, C1-C4alkyl, C2-C4alkenyl or C2-C4alkynyl; R6 is hydrogen, C114 C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C3-C6cycloalkyl, C1-C4alkoxycarbonyl or phenyl which is unsubstituted or at most trisubstituted; and in which R3 and R4 independently of one another are hy

Abstract: A method for eliciting an &agr;v&bgr;5 or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonizing effect in a mammal which comprises administering to the mammal a therapeutically effective amount of a compound of the formula which are useful for inhibiting restenosis, angiogenesis, atherosclerosis, diabetic retinopathy, macular degeneration, inflammation or tumor growth.

Abstract: The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

Abstract: Compounds of the formula I in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4-alkynyl, C3-C6cycloalkyl, phenyl which is unsubstituted or at most trisubstituted by halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, or benzyl which is unsubstituted or at most trisubstituted in the aromatic ring in the same manner; or is cyclopropylmethyl, C1-C4haloalkyl, C2-C5alkoxyalkyl, cyanomethyl, CO—R6, OH, NH2, C1-C4alkylamine or C1-C4alkoxycarbonyl-C1-C2alkyl; X is oxygen, sulfur or NR5; R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, C(O)R6, OH or C1-C4alkoxy, NH2 or C1-C4alkylamine; R5 is hydrogen, C1-C4alkyl, C2-C4alkenyl or C2-C4alkynyl; R6 is hydrogen, C114 C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C3-C6cycloalkyl, C1-C4alkoxycarbonyl or phenyl which is unsubstituted or at most trisubstituted; and in which R3 and R4 independently of one another are h

Abstract: The present invention relates to a novel process for preparing pyridylmethyl isothiocyanates of the formula (I) ##STR1## in which R.sup.1 represents halogen or C.sub.1 -C.sub.4 -alkyl, characterized in that in a first step, amines of the formula (II) ##STR2## in which R.sup.1 is as defined above, are reacted with xanthogenates of the formula (III)R.sup.2 O--CS--S.sup..crclbar. M.sup..sym. (III)in whichR.sup.2 represents C.sub.1 -C.sub.4 -alkyl, preferably methyl or ethyl andM represents an alkali metal, preferably sodium and potassium or represents ammonium,if appropriate in the presence of a diluent, and in a second step, the resulting novel dithiocarbamates of the formula (IV) ##STR3## in which R.sup.1 and M are each as defined above, are oxidized, if appropriate in the presence of a diluent, to give the isothiocyanates of the formula (I).

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists Substance P and NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The present invention relates to new substituted N-methylenethioureas of the general formula (I) ##STR1## in which n, Het, R.sup.1 and R.sup.2 have the meanings given in the description,to a process for their preparation, and to their use in pesticides, in particular as insecticides.

Abstract: Compositions for topical use in herpes virus infections comprising anti-herpes nucleoside analogue phosphate esters, such as acyclovir monophosphate and acyclovir diphosphate, which show increased activity against native strains of herpes virus as well as against resistant strains, particularly thymidine kinase negative strains of virus. Also disclosed are methods for using the topical compositions in treatment of herpes disease.

Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.10 alkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, furanyl, pyridinyl or thienyl, and Ar.sup.1 is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; and Ar is phenyl, napthyl, furanyl, pyridinyl or thienyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH.

Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2## which are useful for inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.

Abstract: Compounds of of the formula ##STR1## wherein R is a C.sub.6 -C.sub.10 aryl group, optionally substituted with one or more halogen atoms, phenoxy, or, linear or branched, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, or C.sub.1 -C.sub.6 haloalkyl; R.sup.1 is C.sub.3 -C.sub.6 cycloalkyl or, linear or branched, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 haloalkenyl, C.sub.2 -C.sub.8 alkoxyalkyl or C.sub.1 -C.sub.6 haloalkyl; n is 1, 2 or 3; and R.sup.2 is CN, C(O)NH.sub.2 or C(S)NH.sub.2, or the physiologically acceptable salts thereof with organic and inorganic acids. These compounds are useful as fungicides.

Abstract: Process for preparing pyridylmethyl isothiocyanates of the formula (I) ##STR1## comprising reacting amines of the formula (II): ##STR2## with xanthogenates of the formula (III):R.sup.2 O--CS--S.sup..crclbar. M.sup..sym. (III)and oxidizing the resulting dithiocarbamates of the formula (IV): ##STR3## wherein R.sup.1 represents halogen or alkyl; R.sup.2 represents alkyl; and M represents an alkali metal or ammonium.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.

Abstract: A process for the preparation of Phosphodiesterase IV inhibitors is described. The process consists of eight chemical steps involving five isolations to prepare the title compound from readily available isovanillin in 35% overall yield (Scheme 1). The process is highlighted by: a) a highly diastereoselective Michael addition of phenyllithium using (1R, 2S) cis-aminoindanol as a chiral auxiliary, b) highly crystalline intermediates providing for efficient purifications, c) crystallization of the final compound as its CSA salt for excellent enantiomeric purity.

Abstract: Compounds represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, wherein: A.sup.1 is --CH.sub.2 R.sup.6, --OR.sup.6, --N(R.sup.6)(R.sup.7), --S(O).sub.e R.sup.13, --(C(R.sup.6)(R.sup.7)).sub.1-6 --OR.sup.6, --(C(R.sup.6)(R.sup.7).sub.1-6 --N(R.sup.6)(R.sup.7) or --(C(R.sup.6) (R.sup.7)).sub.1-6 --S(O).sub.e R.sup.13 and A.sup.2 is H, or A.sup.1 and A.sup.2 together are .dbd.O, .dbd.C(R.sup.6)(R.sup.7), .dbd.NOR.sup.6 or .dbd.S;Q is phenyl, naphthyl, --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6 or heteroaryl;T is H, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl;b is 0, 1 or 2;b.sub.1 is 1 or 2;X is a bond, --C(O)--, --O--, --NR.sup.6 --, --S(O).sub.e --, --N(R.sup.6)C(O)--, --C(O)N(R.sup.6)--, --OC(O)NR.sup.6 --, --OC(.dbd.S)NR.sup.6 --, --N(R.sup.6)C(.dbd.S)O--, --C(.dbd.NOR.sup.6)--, --S(O).sub.2 N(R.sup.6)--, --N(R.sup.6)S(O).sub.2 --, --N(R.sup.6)C(O)O-- or --OC(O)--;R.sup.6, R.sup.7, R.sup.8a, and R.sup.

Abstract: Compositions for topical use in herpes virus infections comprising anti-herpes nucleoside analogue phosphate esters, such as acyclovir monophosphate and acyclovir diphosphate, which show increased activity against native strains of herpes virus as well as against resistant strains, particularly thymidine kinase negative strains of virus. Also disclosed are methods for using the topical compositions in treatment of herpes disease.

Abstract: Compounds of the following general structure X-Y-Z-Aryl-A-B, for example, ##STR1## which inhibit osteoclast mediated bone resorption. Specifically, the compounds are useful for treating mammals suffering from a bone condition caused or mediated by increased bone resorption, who are in need of such therapy. The compounds may be administered in oral dosage forms such as tablets, capsules, e.g. sustained release capsules, powders, granules, and suspensions.

Abstract: A surface of specific reactivity is formed by adsorbing a modified block polymeric surfactant of the Pluronic-type, i.e., containing pendant poly(ethylene oxide) blocks attached at an end to poly(propylene oxide) center blocks and with specifically reactive groups at the unattached ends of the poly(ethylene oxide) blocks, upon a hydrophobic surface.

Abstract: Novel quaternary pyridinium compounds useful in inhibiting acetylcholinesterase in mammals of the general structure: ##STR1## or pharmaceutically acceptable salts thereof, where R.sub.5 is pentafluorophenyl, phenyl monosubstituted with K, phenyl disubstituted with K, phenyl trisubstituted with K, or naphthyl; R.sub.6 is H, C.sub.1-6 alkyl, phenyl, pentafluorophenyl, phenyl mono, di, or trisubstituted with K, C.sub.1-6 alkyl with an attached phenyl group, C.sub.1-6 alkyl with an attached phenyl group mono, di, or trisubstituted with K; K is halogen, COOH, OH, CN, NO.sub.2, NH.sub.2, C.sub.1-6 alkyl, C.sub.1-6 fluorinated alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylamine, C.sub.1-6 alkyl--O--CO--, C.sub.1-6 alkyl--CO--NH--, C.sub.1-6 alkyl--NH--CO--NH--, C.sub.1-6 alkyl--NH--CO--O--, C.sub.1-6 alkyl--NH--CO--, or (C.sub.1-6 alkyl).sub.2 N--CO--; X is OH, C.sub.1-6 alkyl--NH--CO--O--, (C.sub.1-6 alkyl).sub.2 --N--CO--O--, C.sub.1-6 fluoroalkyl--NH--CO--, or (C.sub.1-6 fluoroalkyl).sub.

Abstract: A compound, composition, and method for controlling Take-all disease of plants by applying to the seed prior to planting, a fungicide of the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is pyridine; R and n are defined herein; A is selected from the group consisting of --C(O)--SR.sub.3, --NH--C(X)R.sub.4, --C(.dbd.NR.sub.3)--XR.sub.7, and --C(X)-amine wherein the amine is substituted with with an alkylaminocarbonyl and a hydrogen or wherein the amine has a first and a second amine substituent defined herein; B is --W.sub.m --Q(R.sub.2).sub.3 or selected from 0-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ; Q is C, Si, Ge, or Sn; W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W may also be selected from --N(R.sub.3).sub.m H(.sub.1-m)--, --S(O)p--, and --O--; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R.sub.

Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 - are hydrogen or alkyl,Y is a group ##STR2## --O--CH.sub.2, --CH.sub.2 --O--, --S--CH.sub.2 --, --CH.sub.2 --S--, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 --O--N.dbd.C(R')-- andR is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.

Abstract: Compositions for topical use in herpes virus infections comprising anti-herpes nucleoside analogue phosphate esters, such as acyclovir monophosphate and acyclovir diphosphate, which show increased activity against native strains of herpes virus as well as against resistant strains, particularly thymidine kinase negative strains of virus. Also disclosed are methods for using the topical compositions in treatment of herpes disease.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification,and a medicinal product containing said compound for treating a disorder of the melatoninergic system.

Abstract: The present invention relates to a novel ribonucleotide reductase inhibitor and new combinations comprising an antiviral compound, such as acyclovir, and a thiocarbonohydrazone ribonucleotide reductase inhibitor for the chemo-therapeutic treatment of virus infections, especially viruses of the herpes group.

Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 are hydrogen or alkyl,Y is a group ##STR2## and R is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.

Abstract: The present invention relates to novel ribonucleotide reductase inhibitors and new combinations comprising an antiviral compound, such as acyclovir, and a thiocarbonohydrazone ribonucleotide reductase inhibitor for the chemotherapeutic treatment of virus infections, especially viruses of the herpes group.

Abstract: Thioformamide compounds of formula (I) are disclosed in which R is alkyl, Y is methylene, ethylene or a direct bond, A is optionally substituted phenyl or pyridyl, R.sup.1 is hydrogen and R.sup.2 is N-alkylsulphonyl-, N-phenylsulphonyl-N'-alkylamidino or an arylsulphonyl group; R.sup.1 and R.sup.2 may both independently represent alkyl- or arylsulphonyl groups.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R.sub.10 wherein R.sub.10 represents OH; a group hydrolysable in vivo to OH or hydrogen; C.sub.1-8 alkoxy; C.sub.2-8 alkenyloxy; C.sub.2-8 alkynyloxy; C.sub.3-8 cycloalkyloxy; or COR.sub.13 wherein R.sub.13 represents hydrogen, C.sub.1-8 alkyl, phenyl or phenyl C.sub.1-4 alkyl; in which any phenyl moiety is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halo, C.sub.1-6 alkoxycarbonyl, cyano, C.sub.1-6 alkylthio or C.sub.1-6 alkylsulphonyl; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.

Abstract: This invention relates to insecticidal compositions containing six-membered heterocyclic derivatives of N'-substituted-N,N'-diacylhydrazines, methods of using such compositions and novel six-membered heterocyclic derivatives of N'-substituted-N,N'-diacylhydrazines.

Abstract: The invention relates to a process for making compounds of formula: ##STR1##

Abstract: Thioformamide derivatives of formula (I): ##STR1## wherein R represents alkyl; A represents optionally substituted pyrid-4-yl; Y represents ethylene or methylene or a direct bond and X represents an optionally substituted phenyl, pyridyl, furyl or thienyl group or optionally substituted alkyl, alkenyl or cycloalkyl, and salts thereof possessing useful pharmacological properties.

Abstract: The .beta.-oxo-.beta.-benzenepropanethioamide derivative of the present invention has potassium channel opening action and is useful for treatment of hypertension, asthma, hypersensitive colon syndrome, and enteritis through pharmacological actions including blood vessel dilation, bronchial tract dilation, relaxation of gastrointestinal tract smooth muscle, and the like. The present invention also includes a pharmaceutical composition containing, as the active ingredient, the compound of the present invention and a method for producing the same.

Abstract: Insecticidal novel nitro compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkyl, R.sup.3 is --S--R.sup.4 or ##STR2## in which R.sup.4 is C.sub.1-4 alkyl, R.sup.5 and R.sup.6 are hydrogen or C.sub.1-4 alkyl,Y is CH or N, andZ is a five- or six-membered heterocyclic group having at least one nitrogen atom which may be substituted by halogen or C.sub.1-4 alkyl, provided that where Y is CH,then R.sup.1 is C.sub.1-4 alkyl.