SUBSTITUTED 5-PHENYL PYRIMIDINES I IN THERAPY
    44.
    发明申请
    SUBSTITUTED 5-PHENYL PYRIMIDINES I IN THERAPY 审中-公开
    取代的5-苯基吡啶在治疗中

    公开(公告)号:WO2006079556A2

    公开(公告)日:2006-08-03

    申请号:PCT/EP2006000774

    申请日:2006-01-30

    Abstract: The present invention relates to substituted 5-phenyl pyrimidines I, which carry a radical X in the 4-position of the pyrimidine ring, a radical Y in the 6-position of the pyrimidine ring, the radical X denoting a group of the formula NR 1 R 2 , OR 1a or SR 1a , in which R 1 , R 2 , independently of each other, denote hydrogen, C 1 -C 10 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 10 -haloalkyl, C 3 -C 8 -cycloalkyl, C 3 -C 8 -halocycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing 1, 2, 3 or 4 nitrogen atoms or 1, 2 or 3 nitrogen atoms and one sulfur or oxygen atom as ring members, which radicals may be unsubstituted or may carry 1, 2, 3 or 4 radicals R a1 ; or the radical NR 1 R 2 may also form a 5- or 6-membered optionally substituted heterocyclic ring, containing 1, 2, 3 or 4 nitrogen atoms or 1, 2 or 3 nitrogen atoms and one sulfur or oxygen atom as ring members, which are non-adjacent to the nitrogen of NR 1 R 2 , in which two adjacent C atoms or one N atom and one adjacent C atom can be linked by a C 1 -C 4 -alkylene chain and wherein the heterocyclic ring may be unsubstituted or may carry 1, 2, 3 or 4 radicals R a1 as defined in claim 1, R 1a has one of the meanings given for R 1 except for hydrogen; the radical Y being selected from the group consisting of halogen, cyano, C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl, C 3 -C 6 -cycloalkyl, C 1 -C 4 -alkoxy, C 3 -C 4 -alkenyloxy, C 3 -C 4 -alkynyloxy, C 1 -C 6 -alkylthio, di-(C 1 -C 6 -alkyl)amino or C 1 -C 6 -alkylamino, where the alkyl, alkenyl and alkynyl radicals of Y may be substituted by halogen, cyano, nitro, C 1 -C 2 -alkoxy or C 1 -C 4 -alkoxycarbonyl; and wherein the pyrimidine radical may also carry a radical different from hydrogen in the 2-position and wherein the phenyl ring in the 5-position of the pyrimidine ring may be unsubstituted or carry 1, 2, 3, 4 or 5 radicals L which are different from hydrogen, and the pharmaceutically acceptable salts substituted 5-phenyl pyrimidines for use in therapy, in particular in therapy or treatment of cancerous diseases.

    Abstract translation: 本发明涉及取代的5-苯基嘧啶I,其在嘧啶环的4-位上携带基团X,嘧啶环的6-位的基团Y,基团X表示式NR的基团 其中R 1,R 2,R 2,R 1,R 2, R 2彼此独立地表示氢,C 1 -C 10 - 烷基,C 2 - C 6 - 烯基,C 2 -C 6 - 炔基,C 1 -C 10 - C 1 -C 3烷基,C 3 -C 8 - 环烷基,C 3 -C 8 - 卤代烷基,C 3 -C 8 - 苯基或含有1,2,3或4个氮原子或1,2或3个氮原子和一个硫或氧原子作为环成员的5-或6-元杂芳基或5-或6-元杂环基,该基团可以 未被取代或可以携带1,2,3或4个基团R a1a; 或自由基NR 1 R 2还可以形成含有1,2,3或4个氮原子或1,2或2个氮原子的5或6元任选取代的杂环 或3个氮原子和一个硫或氧原子作为环成员,其与NR 1 R 2 O 2的氮不相邻,其中两个相邻的C原子或一个 N原子和一个相邻的C原子可以通过C 1 -C 4 - 亚烷基链连接,并且其中杂环可以是未取代的或可以携带1,2,3 或如权利要求1所定义的4个基团R a1,其中R 1a除了氢之外具有R 1给出的含义之一; 基团Y选自卤素,氰基,C 1 -C 4 - 亚烷基,C 2 -C 3 - 烷基, 4 - 烯基,C 2 -C 4 - 炔基,C 3 -C 6 - 环烷基,C 1 -C 4 - 烷氧基,C 3 -C 4 - 炔基氧基,C 1 -C 4 - 3-C 4 - 炔基氧基,C 1 -C 6 - 烷硫基,二 - (C 1 -C 6) C 1 -C 6 - 烷基)氨基或C 1 -C 6 - 烷基氨基,其中Y的烷基,烯基和炔基可以 被卤素,氰基,硝基取代,C 1 -C 2 - 烷氧基或C 1 -C 4 - - 烷氧基; 并且其中嘧啶基团还可以携带2-位上与氢不同的基团,其中嘧啶环的5-位上的苯环可以是未取代的或携带1,2,3,4或5个基团L,其为 不同于氢,以及用于治疗,特别是治疗或治疗癌性疾病的药学上可接受的盐取代的5-苯基嘧啶。

    FUNGICIDE MIXTURES BASED ON OXIME ETHER DERIVATIVES
    49.
    发明申请
    FUNGICIDE MIXTURES BASED ON OXIME ETHER DERIVATIVES 审中-公开
    基于OXIMETHER衍生物的杀菌剂混合物

    公开(公告)号:WO0249434A9

    公开(公告)日:2002-09-19

    申请号:PCT/EP0114785

    申请日:2001-12-14

    CPC classification number: A01N37/50 A01N39/04 A01N39/02 A01N2300/00

    Abstract: The invention relates to fungicide mixtures containing, as active constituents and in a synergistically active quantity, A) oxime ether derivatives of formula (I) wherein the substituents have the following designations: X represents NH or oxygen; R and R independently represent hydrogen, cyano, alkyl, cyclopropyl or halogenalkyl; and R and R independently represent hydrogen, alkyl, alkenyl, alkynyl, halogenalkyl, halogenalkenyl or halogenalkynyl, and B) at least one compound of formula (II) wherein the substituents and the index have the following designations: R and R independently represent alkyl; R , R and R independently represent hydrogen or alkyl; R represents halogen, alkyl or halogenalkyl; n represents 2, 3 or 4; and the radicals R can be different. The invention also relates to a method for controlling pathogenic fungi using mixtures of compounds (I) and (II), and the use of compounds (I) and (II) for producing such mixtures.

    Abstract translation: 包含作为活性组分的杀真菌混合物:A)式(I)的肟醚衍生物,其中取代基具有以下含义:X是NH或氧; R 1和R 3彼此独立地为氢,氰基,烷基,环丙基或卤代烷基; R 2和R 4彼此独立地为氢,烷基,烯基,炔基,卤代烷基,卤代卤代或卤代炔基; 和B)至少一种式(II)化合物,其中取代基和指数具有以下含义:R 1和R 2彼此独立地为烷基; R 3,R 4和R 5彼此独立地表示氢或烷基; R 6是卤素,烷基或卤代烷基; n是2,3或4,其中基团R 6可以不同; 以协同有效的量,用化合物I和II的混合物控制有害真菌的方法以及化合物I和II在制备这种混合物中的用途。

    AGROCHEMICAL COMPOSITIONS CONTAINING PYRAZOLES AND USE THEREOF AS FUNGICIDAL PLANT PROTECTION AGENTS
    50.
    发明申请
    AGROCHEMICAL COMPOSITIONS CONTAINING PYRAZOLES AND USE THEREOF AS FUNGICIDAL PLANT PROTECTION AGENTS 审中-公开
    含吡唑农业化学化合物及其作为杀菌剂FLANZENSCHUTZMITTEL

    公开(公告)号:WO0130154A3

    公开(公告)日:2002-04-11

    申请号:PCT/EP0010468

    申请日:2000-10-24

    CPC classification number: A01N43/56

    Abstract: The invention relates to agrochemical compositions with a fungicidal action, containing compounds of formula (I) as their active agents, the radicals having the following meanings: R is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C4-alkoxy-C1-C6-alkyl, C1-C6-halogenalkyl, C3-C6-alkenyl, C3-C6-halogenalkenyl or phenyl-C1-C6-alkyl, wherein the phenyl group can be substituted by C1-C6-alkyl, halogen or C1-C6-halogenalkyl; R is hydrogen, C1-C6-alkyl, C1-C6-halogenalkyl, C1-C6-alkoxy, C1-C6-halogenalkoxy or halogen; R is phenyl that is optionally substituted by halogen, C1-C6-alkyl, C1-C6-halogenalkyl, C1-C6-alkoxy, C1-C6-halogenalkoxy, C1-C6-alkylthio, C1-C6-alkylsulfonyl, C1-C6-halogenalkylsulfonyl; and R is a heterocyclic radical with one or two nitrogen atoms - said heterocyclic radical can be substituted by halogen, C1-C6-alkyl or C1-C6-halogenalkyl. The invention also relates to methods for combating harmful fungi on plants using this fungicidal agent.

    Abstract translation: 本发明涉及具有含有(I),其中各基团具有以下含义的式作为活性成分的化合物的杀真菌活性农业化学组合物,R <1>是氢,C1-C6烷基,C1-C6烷基羰基,C1-C4烷氧基 -C1-C6-烷基,C1-C6卤代烷基,C3-C6烯基,C3-C6卤代链烯基或苯基-C 1 -C 6 - 烷基,其中,由C1-C6烷基,卤素或C 1 -C 6卤代烷基的苯基 可以被取代; [R <2>是氢,C1-C6烷基,C1-C6卤代烷基,C1-C6-烷氧基,C1-C6卤代烷氧基或卤素; [R <3>是其任选地被卤素取代的,C1-C6-烷基,C1-C6卤代烷基,C1-C6-烷氧基,C1-C6卤代烷氧基,C1-C6-烷硫基,C1-C6-烷基磺酰基,C1苯基 C6卤代烷基磺酰基; [R <4>杂环基团具有一个或两个氮原子,其中杂环部分可以被卤素,C1-C6烷基或C1-C6卤代烷基。 此外,本发明提供用于在植物中防治有害真菌涉及使用这些杀真菌剂的方法。

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