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    • 72. 发明申请
    • NOVEL 2-NITROMETHYLIDENE/2-CYANIMINO/2-NITRO-IMINO-PYRROLIDINES AND PIPERIDINES, INTERMEDIATES, AND THEIR USE AS PESTICIDES
    • 新型2-硝基苯胺/ 2-氰基咪唑/ 2-硝基 - 吡咯烷酮和哌啶,中间体及其作为杀虫剂的用途
    • WO1994024124A1
    • 1994-10-27
    • PCT/EP1994000963
    • 1994-03-26
    • CIBA-GEIGY AGMAIENFISCH, PeterGONDA, JozefJACOB, OlivierGSELL, Laurenz
    • CIBA-GEIGY AG
    • C07D401/06
    • C07D401/06A01N43/40A01N47/38A01N51/00C07D417/06
    • Compounds of formula (I), wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group N -O (N-oxide); R1 is hydrogen or C1-C3alkyl; R2 is hydrogen or C1-C3alkyl; R3 is hydrogen, an unsubstituted or substituted C1-C6alkyl, C3-C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl group, or C(=O)-R5, R5 is C1-C4alkyl, C1-C4alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R6)2, each R6, independently of the other, is hydrogen, C1-C4alkyl or unsubstituted or substituted phenyl, X is CH-NO2, N-CN or N-NO2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    • 式(I)化合物,其中A是未取代或取代的芳族或非芳族单环或双环杂环基团,其中环氮原子可能已被基团N + N-氧化物); R1是氢或C1-C3烷基; R2是氢或C1-C3烷基; R3是氢,未取代或取代的C1-C6烷基,C3-C6环烷基,C2-C6链烯基或C2-C6炔基,或C(= O)-R5,R5是C1-C4烷基,C1-C4烷氧基,未取代或取代的苯基, 苯氧基或苄氧基或N(R6)2,每个R6独立地为氢,C1-C4烷基或未取代或取代的苯基,X为CH-NO2,N-CN或N-NO2,n为1 至3,以游离形式或盐形式,并且在适当时,这些化合物及其盐的互变异构体可用作农业化学活性成分,并且可以以本身已知的方式制备。
    • 76. 发明申请
    • SUBSTITUTED BENZAZEPINONES
    • 取代benzazepinones
    • WO1994013642A1
    • 1994-06-23
    • PCT/EP1993003425
    • 1993-12-06
    • CIBA-GEIGY AGBÜHLMAYER, PeterFURET, Pascal
    • CIBA-GEIGY AG
    • C07D223/16
    • C07D223/16
    • The invention concerns substituted 3-amino-1-arylalkyl-benzazepin-2-ones of general formula (I) in which Ar is aryl; X is C1-C2 alkylene or a single bond; R1 is hydrogen, lower alkyl, aryl(lower alkyl) or acyl; R2 is lower alkyl, hydroxy(lower alkyl), (lower alkoxy)(lower alkyl), aryl(lower alkoxy)(lower alkyl), aryl(lower alkyl) or (C3-C7 cycloalkyl)(lower alkyl); R3 is a carboxylic group, 5-tetrazolyl, PO2H2, PO3H2 or SO3H2 (lower alkoxy)carbonyl, (lower alkoxy)(lower alkoxy)carbonyl, aryl(lower alkoxy)carbonyl, aryloxycarbonyl, carbamoyl, carbamoyl which is (i) mono-substituted by hydroxy, (lower alkyl)sulphonyl, halo(lower alkyl)sulphonyl or arylsulphonyl, (ii) mono-substituted or independently disubstituted by lower alkyl, lower alkenyl, lower alkinyl or phenyl(lower alkyl) or (iii) disubstituted by lower alkylene or (lower alkylene)-X1-(lower alkylene), X1 being O, S or NH; the ring A is unsubstituted or singly or multiply substituted by substituents selected from the group comprising lower alkyl, aryl(lower alkyl), (lower alkoxy)(lower alkyl), lower alkoxy, (lower alkoxy)(lower alkoxy), aryl(lower alkoxy, C3-C7 cycloalkyl, (C3-C7 cycloalkyl)(lower alkyl), nitro, halogen, trifluoromethyl, amino or amino which is mono-substituted or independently disubstituted by lower alkyl, aryl(lower alkyl) or aryl or disubstituted by lower alkylene or (lower alkylene)-oxy-(lower alkylene); or a salt thereof. The invention also concerns methods of preparing these compounds, their use, and pharmaceutical preparations containing compounds of formula (I) or pharmaceutically usable salts thereof.
    • 80. 发明申请
    • 2-(PYRID-2'-YL)-2-THIAZOLINE-4(S)-CARBOXYLIC ACID DERIVATIVES
    • 2-(PYRID-2'-YL)-2-噻唑烷-4(S) - 羧酸衍生物
    • WO1994011367A1
    • 1994-05-26
    • PCT/US1993010936
    • 1993-11-12
    • CIBA-GEIGY AGUNIVERSITY OF FLORIDA RESEARCH FOUNDATION INC.PETER, Heinrich, H.MOERKER, ThéophileBERGERON, Raymond, J., Jr.
    • CIBA-GEIGY AGUNIVERSITY OF FLORIDA RESEARCH FOUNDATION INC.
    • C07D417/04
    • C07D417/04
    • 2-(Pyrid-2'-yl)-2-thiazoline-4-carboxylic acid derivatives of formula (I) in which R1 represents hydrogen, halogen, hydroxy, C1-C4 alkoxy or C1-C4 alkyl; R2 represents hydroxy or resterified hydroxy; and R3 represents etherified hydroxy or a group of the partial formula -N(R4, R5) in which R4 and R5 independently from each other represent hydrogen or C1-C4 alkyl or in which R4 represents hydroxy or esterified hydroxy and R5 represents hydrogen, C1-C4 alkyl or a group -X-R6 in which X is C2-C12 alkylen or oxaalkylen having 4-12 chain members and R6 represents C1-C2 alkyl or a hydroxylamino group -N(OH)-R7 in which R7 represents C1-C4 alkanoyl; and salts thereof form chelate-type metal complexes with trivalent metal ions, especially iron (III), and can be used, for example, for the treatment of pathological conditions in warm-blooded animals that are associated with an excess of trivalent metal ions in the body. Valuable starting material embraces alkali and alkaline earth salts of 2-(3'hydroxypyrid-2'-yl)-2-thiazoline-4(S)-carboxylic acid.
    • 式(I)的2-(吡啶-2'-基)-2-噻唑啉-4-羧酸衍生物,其中R 1表示氢,卤素,羟基,C 1 -C 4烷氧基或C 1 -C 4烷基; R2表示羟基或羟基; 并且R 3表示醚化羟基或其中R 4和R 5彼此独立地表示氢或C 1 -C 4烷基或其中R 4表示羟基或酯化羟基的部分式-N(R 4,R 5)的基团,R 5表示氢,C 1 -C4烷基或基团-X-R6,其中X为具有4-12个链成员的C 2 -C 12亚烷基或氧杂亚烷基,R 6表示C 1 -C 2烷基或羟基氨基-N(OH)-R 7,其中R 7表示C1- C4烷酰基; 其盐与三价金属离子特别是铁(III)形成螯合型金属络合物,并且可用于例如治疗与过量三价金属离子相关的温血动物的病理状况 身体。 有价值的起始材料包含2-(3'-羟基吡啶-2'-基)-2-噻唑啉-4(S) - 羧酸的碱金属和碱土金属盐。