摘要:
The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1-C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably C1 or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.4 represents alpha-pyridyl or a phenyl in which the phenyl ring can be substituted preferably in the 2-position, by methyl, halogen, preferably chlorine or bromine, nitro or trifluoromethyl;n represents one of the numbers 0, 1, 2, 3, 4, 5, 6, 7 or 8; and novel intermediates therefor.The compounds of formula I are useful in the treatment of pathological conditions and diseases in which platelet activating factor is implicated.
摘要:
Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl,A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,X is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.7 -cycloalkenyl,a substituted or unsubstituted 5-membered saturated heterocyclic radical which contains one or two oxygen and/or sulfur atoms as heteroatoms,a substituted or unsubstituted 6- or 7-membered heterocyclic radical which contains one or two oxygen and/or sulfur atoms and one or two double bonds,a substituted or unsubstituted 5-membered heteroaromatic radical containing one or two nitrogen atoms and an oxygen or a sulfur atom,substituted or unsubstituted phenyl or pyridyl,and their agriculturally useful salts and esters of C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids, methods of manufacturing them, and their use as herbicides.
摘要:
Aliphatically substituted fluorobenzenes of the general formula I ##STR1## where R is an aliphatic or cycloaliphatic radical, n is 2, 3 or 4 and X is hydrogen, fluorine, chlorine or bromine, are prepared by diazotization of the corresponding aniline derivative of the general formula II ##STR2## in the presence of tetrafluoboric acid and decomposition of the resulting diazonium tetrafluoborate of the general formula III ##STR3## by a process in which the decomposition reaction is carried out simultaneously with the diazotization reaction, in the presence of elemental copper and/or copper(I) and/or copper(II) salts and at from -15.degree. to 80.degree. C.
摘要:
The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II ##STR1## wherein A is an anellated and optionally substituted benzene or 5- or 6-membered heterocyclic ring; R.sub.5 and Z are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or is .alpha.-pyridyl; Y is CO, CS or CH.sub.2 ; and nontoxic, pharmaceutically acceptable acid addition salts thereof.
摘要翻译:本发明公开了一种通过用式I或II化合物或其药学上可接受的盐或其药物可接受的方法治疗患有对PAF拮抗剂活性的病症的个体的方法。 取代的苯或5-或6-元杂环; R 5和Z各自独立地为氢或任选取代的C 1 -C 8烷基,烯基或炔基; R6是任选取代的苯基,或是噻吩基或是α-吡啶基; Y是CO,CS或CH2; 和无毒的药学上可接受的酸加成盐。
摘要:
Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is oxygen or sulfur;R is hydrogen or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;and their salts, processes and intermediates for their preparation, and their use are described.
摘要:
Phenylacetic acid derivatives of the formula I ##STR1## where the sqtstituents and the index have the following meanings; X it NOCH.sub.3, CHOC.sub.3, CHCH.sub.3 and [sic] CHCH.sub.2 CH.sub.3 ;R.sup.1 is hydrogen and [sic] alkyl;R.sup.2 is cyano, nitro, triflaormethyl, halogen, alkyl and [sic] alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamine;R.sub.4 is hydrogen, cyano, nitro, hydroxyl, amino, halogen,R.sup.5 is hydrogen,substituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl or alkylsulfonyl;unsubstituted or substituted aryl, arylcarbonyl, arylsulfonyl, hetaryl, hetarylcarbonyl or hetarylsulfonyl,and their salts, processes and intermediates for their preparation, and their use.
摘要:
(Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.
摘要:
Preparation of mixtures of O-phenoxyalkylhydroxylamines Ia and Ib ##STR1## and the corresponding salt mixtures by a) converting mixtures of isomers of O-(2-hydroxyethyl)oximes IIa and IIb ##STR2## with a sulfonyl halide III ##STR3## into a mixture of sulfonates IVa and IVb ##STR4## b) reacting this mixture of IVa and IVb with a phenol HO-Ar (V) to give a mixture of O-phenoxyalkoximes VIa and VIb ##STR5## c) hydrolyzing this mixture in the presence of an acid and, if desired d) liberating the O-phenoxyalkylhydroxylamines Ia and Ib from the resulting salts using a mineral acid. Compounds Ia/Ib and VIa/VIb are important intermediates for crop protection agents.
摘要:
The use of nicotinic anilide derivatives of the general formula ##STR1## where the substituents have the following meanings: R.sup.1 halogen, methyl, trifluoromethyl, methoxy, methylthio, methylsulfinyl, methylsulfonylR.sup.2 unsubstituted or halogen-substituted alkyl, unsubstituted or halogen-substituted alkenyl, alkynyl, unsubstituted or halogen-substituted alkoxy, unsubstituted or halogen-substituted alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxyfor combating Botrytis, and nicotinic anilides of the formula I.