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    • 3. 发明公开
    • 6-페닐-7-아미노-트리아졸로피리미딘, 이의 제조 방법,병원성 진균을 방제하기 위한 상기 화합물의 용도, 및 상기화합물을 포함하는 제제
    • 6-苯基-7-氨基三唑并嘧啶,其生产方法,其用于控制​​致病真菌的用途,以及含有它们的药剂
    • KR1020070104516A
    • 2007-10-26
    • KR1020077007910
    • 2005-09-02
    • 바스프 에스이
    • 블레트너,카르스텐토르모이블라스코,조르디뮐러,베른트게베어,마르쿠스그래메노스,와실리오스그로테,토마스휜저,유도라인하이머,요아킴샤퍼,페테르쉬베크,프랑크슈뵈글러,안야디츠,요켄스피크맨,존-브라이언얍스,토르스텐스트라트만,지그프리트셰플,울리히셰어러,마리아스티얼,라인하르트
    • C07D487/04A01N43/90
    • A01N43/90A01N47/06A01N47/12A01N47/16C07D487/04
    • The invention relates to 6-phenyl-7-amino-triazolopyrimidines of formula (I), wherein the substituents have the following designations: R1 represents hydrogen, alkyl, halogenalkyl, cycloalkyl, halogencycloalkyl, alkenyl, halogenalkenyl, cycloalkenyl, halogencycloalkenyl, alkinyl, halogenalkinyl or phenyl, naphthyl, or a five-membered or six-membered saturated, partially unsaturated or aromatic heteroycle, containing between one and four heteroatoms from the group containing O, N or S; R2 represents alkyl, halogenalkyl, cycloalkyl, halogencycloalkyl, alkenyl, halogenalkenyl, cycloalkenyl, halogencycloalkenyl, alkinyl, halogenalkinyl or phenyl, naphthyl, or a five-membered or six-membered saturated, partially unsaturated or aromatic heterocycle, containing between one and four heteroatoms from the group containing O, N or S; R3,R4,R5, R6,R7 represent hydrogen or one of the groups cited for R2, R4 also being able to form a five-membered or six-membered saturated or unsaturated ring with R3 or R 6, that can contain, in addition to carbon atoms and as a ring member, between one and three other heteroatoms from the group containing O, N and S; R2 and R3, R4 and R 5, and R6 and R7 can respectively form, in order to form spiro groups, a C2-C5 alkylene, alkenylene, or alkinylene chain, which can be broken by between one and three heteroatoms from the group containing O, N and S; p represents 0 or 1; L represents halogen, alkyl, halogenalkyl, alkoxy, cyano, nitro, amino, alkylamino, dialkylamino, alkylcarbonylamino, C(O)-R, S(O)n-R; where n represents 0, 1 or 2; R represents hydrogen, alkyl, halogenalkyl, alkoxy, alkenyloxy, alkinyloxy, amino, alkylamino, dialkylamino; m represents 1, 2, 3, 4 or 5; X represents halogen, cyano, alkyl, alkoxy, alkenyloxy, alkinyloxy or halogenalkoxy, Y represents oxygen or sulphur; Z represents hydrogen, alkyl, halogenalkyl, cycloalkyl, alkylcarbonyl, cycloalkylcarbonyl, alkenyl, halogenalkenyl, cycloalkenyl, alkinyl, halogenalkinyl, phenyl, naphthyl, a five-membered to ten-membered saturated, partially unsaturated or aromatic heterocycle, containing between one and four heteroatoms from the group containing O, N and S; or Z can also form, with R4 or R6, a five-membered or six-membered ring that can contain, in addition to carbon atoms and Y, one or two other heteroatoms from the group containing O, N and S, as a ring member; the groups R1 to R7, Z and R being able to be substituted according to the description. The invention also relates to methods for producing said compounds, to agents containing the same, and to the use thereof for controlling plant pathogenic fungi.
    • 本发明涉及式(I)的6-苯基-7-氨基 - 三唑并嘧啶,其中取代基具有以下指定:R 1表示氢,烷基,卤代烷基,环烷基,卤代烷基,烯基,卤素链烯基,环烯基,卤代烯基,炔基,卤代羰基 或苯基,萘基或五元或六元饱和,部分不饱和或芳族杂环,含有一个至四个含有O,N或S的基团的杂原子; R 2代表烷基,卤素烷基,环烷基,卤代烷基,链烯基,卤代烯基,环烯基,卤代烯基,炔基,卤代炔基或苯基,萘基或五元或六元饱和的部分不饱和或芳族杂环, 含有O,N或S的基团; R 3,R 4,R 5,R 6,R 7表示氢或R 2所列的基团之一,R4还能够与R 3或R 6形成五元或六元饱和或不饱和的环, 碳原子和作为环成员,来自含有O,N和S的基团的一个和三个其它杂原子; R2和R3,R4和R5以及R6和R7可以分别形成C2-C5亚烷基,亚烯基或亚链烯基链,以形成螺环,其可以由含有 O,N和S; p表示0或1; 烷氧基,氰基,硝基,氨基,烷基氨基,二烷基氨基,烷基羰基氨基,C(O)-R,S(O)n -R; 其中n表示0,1或2; R代表氢,烷基,卤代烷基,烷氧基,烯氧基,烷氧基,氨基,烷基氨基,二烷基氨基; m表示1,2,3,4或5; X表示卤素,氰基,烷基,烷氧基,烯氧基,烷氧基或卤代烷氧基,Y表示氧或硫; Z代表氢,烷基,卤代烷基,环烷基,烷基羰基,环烷基羰基,烯基,卤代烯基,环烯基,炔基,卤代炔基,苯基,萘基,含有一个和四个杂原子的五元至十元饱和,部分不饱和或芳族杂环 来自含有O,N和S的基团; 或Z也可以与R4或R6形成五元或六元环,除了碳原子和Y之外,还可以含有一个或两个其它含有O,N和S的基团的杂原子作为环 会员; 根据说明可以使R1〜R7,Z,R基团取代。 本发明还涉及生产所述化合物,含有该化合物的药剂的方法及其用于防治植物致病真菌的方法。
    • 7. 发明公开
    • 치료요법에 있어서의 치환된 5-페닐 피리미딘 I
    • 取代的5-苯基吡啶在治疗中
    • KR1020070104893A
    • 2007-10-29
    • KR1020077017631
    • 2006-01-30
    • 바스프 에스이
    • 라인하이머,조아킴그로테,토마스뮐러,베른트나베,바르바라쉬벡크,프란크쉬뵈글러,안자잡스,토르스텐블레트너,카르스텐
    • C07D239/42C07D239/48A61K31/506A61K31/505
    • C07D239/48C07D239/42C07D401/04C07D403/04C07D417/04
    • 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 NR1R2, OR 1a or SR1a, in which R1, R2, independently of each other, denote hydrogen, C1-C10-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C10-haloalkyl, C3-C 8-cycloalkyl, C3-C8-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 Ra1; or the radical NR1R2 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 NR1 R2, in which two adjacent C atoms or one N atom and one adjacent C atom can be linked by a C1-C4-alkylene chain and wherein the heterocyclic ring may be unsubstituted or may carry 1, 2, 3 or 4 radicals Ra1 as defined in claim 1, R1a has one of the meanings given for R1 except for hydrogen; the radical Y being selected from the group consisting of halogen, cyano, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C3-C 4-alkenyloxy, C3-C4-alkynyloxy, C1-C6-alkylthio, di-(C1-C6-alkyl)amino or C1-C6-alkylamino, where the alkyl, alkenyl and alkynyl radicals of Y may be substituted by halogen, cyano, nitro, C 1-C2-alkoxy or C1-C4-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.
    • 本发明涉及在嘧啶环的4-位上携带基团X的取代的5-苯基嘧啶I,嘧啶环的6位的基团Y,X表示式NR1R2的基团 ,其中R 1,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 - 卤代烷基,C 3 -C 8 - 环烷基 ,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的C 3 -C 8卤代环烷基,苯基或5-或6-元杂芳基或5-或6-元杂环基 作为环成员,该基团可以是未取代的或可以带有1,2,3或4个基团Ra1; 或者NR1R2基团还可以形成含有1,2,3或4个氮原子或1,2或3个氮原子的5或6元任选取代的杂环,并且一个硫或氧原子作为环成员, 与NR1R2的氮相邻,其中两个相邻的C原子或一个N原子和一个相邻的C原子可以被C1-C4-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4个如权利要求1所定义的基团R 1a,R 1a具有除氢之外对R 1给出的含义之一; 基团Y选自卤素,氰基,C 1 -C 4 - 烷基,C 2 -C 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 - 烯氧基 ,C 3 -C 4 - 炔氧基,C 1 -C 6 - 烷硫基,二 - (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, C 1 -C 2烷氧基或C 1 -C 4 - 烷氧基羰基; 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。