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    SUBSTITUTED 5-PHENYL PYRIMIDINES I IN THERAPY
    5.
    发明公开
    SUBSTITUTED 5-PHENYL PYRIMIDINES I IN THERAPY 审中-公开
    取代的5-苯基嘧啶I在治疗中

    公开(公告)号：EP1845991A2

    公开(公告)日：2007-10-24

    申请号：EP06706482.4

    申请日：2006-01-30

    Applicant: BASF AKTIENGESELLSCHAFT

    Inventor： RHEINHEIMER, Joachim ,  GROTE, Thomas ,  MÜLLER, Bernd ,  NAVE, Barbara ,  SCHIEWECK, Frank ,  SCHWÖGLER, Anja ,  JABS, Thorsten ,  BLETTNER, Carsten

    IPC: A61K31/506 ,  A61K31/505 ,  C07D239/48 ,  C07D239/42 ,  C07D403/04 ,  C07D401/04 ,  C07D417/04

    CPC classification number: C07D239/48 ,  C07D239/42 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04

    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 NR1R2, OR1a 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-C8-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 NR1R2, 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-C4-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, C1-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.

    Abstract translation: 本发明涉及取代的5-苯基嘧啶I，其在嘧啶环的4-位带有基团X，在嘧啶环的6-位带有基团Y，基团X表示式NR 1 R 2的基团 ，OR 1a或SR 1a，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， C8卤代环烷基，苯基或5或6元杂芳基或5或6元杂环基，其含有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 其基团可以未被取代或可以带有1,2,3或4个基团Ra 1; 或基团NR 1 R 2还可以形成含有1,2,3或4个氮原子或1,2或3个氮原子和一个硫或氧原子作为环成员的5-或6-元任选取代的杂环， - 与NR 1 R 2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原子可以通过C 1 -C 4亚烷基链连接，并且其中该杂环可以未被取代或可以带有1,2,3 或如权利要求1中所定义的4个基团Ra1，R1a除了氢之外，具有对R1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链烯基，C 2 -C 4炔基，C 3 -C 6环烷基，C 1 -C 4烷氧基，C 3 -C 4链烯氧基， C 1 -C 6烷基硫基，二（C 1 -C 6烷基）氨基或C 1 -C 6烷基氨基，其中Y的烷基，链烯基和炔基可以被卤素，氰基，硝基，C1 -C2-烷氧基或C1-C4-烷氧基羰基; 并且其中嘧啶基团还可以在2-位上带有不同于氢的基团，并且其中嘧啶环的5-位上的苯环可以未被取代或带有1,2,3,4或5个基团L，其是 不同于氢和药学上可接受的盐取代的5-苯基嘧啶用于治疗，特别是用于治疗或治疗癌性疾病。

    TRIAZOLOPYRIMIDIN-VERBINDUNGEN UND IHRE VERWENDUNG ZUR BEKÄMPFUNG VON SCHADPILZEN
    7.
    发明公开
    TRIAZOLOPYRIMIDIN-VERBINDUNGEN UND IHRE VERWENDUNG ZUR BEKÄMPFUNG VON SCHADPILZEN 审中-公开
    TRIAZOLOPYRIMIDIN-VERBINDUNGEN UND IHRE VERWENDUNG ZURBEKÄMPFUNGVON SCHADPILZEN

    公开(公告)号：EP1758457A1

    公开(公告)日：2007-03-07

    申请号：EP05753191.5

    申请日：2005-06-08

    Applicant: BASF Aktiengesellschaft

    Inventor： BLETTNER, Carsten ,  GEWEHR, Markus ,  GRAMMENOS, Wassilios ,  GROTE, Thomas ,  HÜNGER, Udo ,  MÜLLER, Bernd ,  NIEDENBRÜCK, Matthias ,  RHEINHEIMER, Joachim ,  SCHÄFER, Peter ,  SCHIEWECK, Frank ,  SCHWÖGLER, Anja ,  WAGNER, Oliver ,  PARRA RAPADO, Liliana ,  RACK, Michael ,  NAVE, Barbara ,  SCHERER, Maria ,  STRATHMANN, Siegfried ,  SCHÖFL, Ulrich ,  STIERL, Reinhard

    IPC: A01N43/90 ,  C07D487/04

    CPC classification number: A01N43/90

    Abstract: The invention relates to the use of triazolopyrimidines of formula (I), wherein R1, R2 represent hydrogen, alkyl, alkyl halide, cycloalkyl, cycloalkyl halide, alkenyl, alkadienyl, alkenyl halide, cycloalkenyl, cycloalkenyl halide, alkinyl, alkinyl halide, C3-C6 cycloalkinyl, phenyl, naphthyl, or a five-membered or ten-membered saturated, partially unsaturated, or aromatic heterocycle containing one, two, three, or four heteroatoms from the group comprising O, N, or S. R1, R2 can be substituted as described in the description, or R1 and R2 form five-membered to eight-membered heterocyclyl or heteroaryl along with the nitrogen atom to which the same are bound, said heterocyclyl or heteroaryl being bound via N. Furthermore, R1, R2 contain one, two, or three additional heteroatoms from the group comprising O, N, and S as a ring member and/or can be substituted as defined in the description. Additionally, in formula (I), L independently represents halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, alkenyloxy, cyano, C(=O)A1, S(=O)mA2, NRcRd, or NRc-(C=O)-Rd, A1, A2, Rc, Rd, and m being defined as indicated in the description; L1 represents halogen, alkyl, alkyl halide; L2 represents nitro, a -C(S)NR3R4 group, a -C(=N-OR5)(NR6R7) group, or a -C(=N-NR8R9)(NR10R11) group; X represents halogen, cyano, alkyl, alkoxy, alkyl halide, or alkoxy halide; R3, R4, R5, R6, R7, R8, R9, R10, and R11 are independently selected among hydrogen, alkyl, cycloalkyl, alkenyl, or alkinyl, the last four radicals mentioned being optionally substituted as defined in the description; R3 and R4, R6 and R7, R8 and R9, and/or R10 and R11 form a four-membered, five-membered, or six-membered saturated or partially unsaturated ring along with the nitrogen atom, said ring being optionally substituted as defined in the description; and n represents 0, 1, 2, or 3. Also disclosed are the agriculturally acceptable salts thereof, novel triazolopyrimidines, crop protection agents containing at least one compound of general formula (I) and at least one liquid or solid carrier substance, and a method for controlling plant-pathogenic harmful fungi.

    Abstract translation: 本发明涉及式（I）三唑并嘧啶的用途，其中R 1，R 2表示氢，烷基，烷基卤，环烷基，环烷基卤，链烯基，链二烯基，链烯基卤化物，环烯基，环烯基卤化物，炔基， C6环烷基，苯基，萘基或含有1,2,3或4个选自O，N或S的杂原子的五元或十元饱和，部分不饱和或芳族杂环。R1，R2可以是 如说明书中所述被取代，或者R 1和R 2与其所连接的氮原子一起形成五元至八元杂环基或杂芳基，所述杂环基或杂芳基通过N连接。此外，R 1，R 2含有一个 ，两个或三个另外的选自O，N和S的杂原子作为环成员和/或可以如说明书中所定义的那样被取代。 此外，在式（I）中，L独立地表示卤素，烷基，卤代烷基，烷氧基，烷氧基卤化物，烯氧基，氰基，C（= O）A1，S（= O）mA2，NRcRd或NRc-（C = O ）-Rd，A1，A2，Rc，Rd和m如说明书中所示定义; L1代表卤素，烷基，烷基卤; L 2表示硝基，-C（S）NR 3 R 4基，-C（= N-OR 5）（NR 6 R 7）基或-C（= N-NR 8 R 9）（NR 10 R 11） X代表卤素，氰基，烷基，烷氧基，烷基卤或烷氧基卤; R3，R4，R5，R6，R7，R8，R9，R10和R11独立地选自氢，烷基，环烷基，烯基或炔基，所述最后四个基团任选如说明书中所定义的那样被取代; R 3和R 4，R 6和R 7，R 8和R 9和/或R 10和R 11与氮原子一起形成四元，五元或六元饱和或部分不饱和的环，所述环任选如定义 在描述中; 并且n代表0,1,2或3.还公开了其农业上可接受的盐，新的三唑并嘧啶，含有至少一种通式（I）的化合物和至少一种液体或固体载体物质的作物保护剂和 控制植物病原性有害真菌的方法。

    7-AMINO-6-HETARYL-1,2,4-TRIAZOLO[1,5-A]PYRIMIDIN-VERBINDUNGEN UND IHRE VERWENDUNG ZUR BEK[MPFUNG VON SCHADPILZEN
    10.
    发明公开
    7-AMINO-6-HETARYL-1,2,4-TRIAZOLO[1,5-A]PYRIMIDIN-VERBINDUNGEN UND IHRE VERWENDUNG ZUR BEK[MPFUNG VON SCHADPILZEN 审中-公开
    7-氨基-6-杂芳基-1,2,4-三唑并[1,5-a]嘧啶化合物及其使用BEK [缓冲有害真菌

    公开(公告)号：EP1828191A2

    公开(公告)日：2007-09-05

    申请号：EP05816549.9

    申请日：2005-12-16

    Applicant: BASF AKTIENGESELLSCHAFT

    Inventor： WAGNER, Oliver ,  GROTE, Thomas ,  RHEINHEIMER, Joachim ,  NAVE, Barbara ,  STIERL, Reinhard

    IPC: C07D487/04 ,  A01N43/90

    CPC classification number: A01N43/90 ,  C07D213/55 ,  C07D237/14 ,  C07D487/04

    Abstract: The invention relates to novel 7-amino-6-hetaryl-1,2,4-triazolo[1,5-a]pyrimidine compounds and the salts thereof that can be used in agriculture, the use of the same for controlling pathogenic fungi, and plant protection agents containing at least one such compound as an active constituent. Said novel 7-amino-6-hetaryl-1,2,4-triazolo[1,5-a]pyrimidine compounds correspond to general formula (I) wherein the substituents R1, R2, Het, X and Y have the following designations: Het represents a six-membered heteroaromatic radical selected from pyridinyl, pyridazinyl, pyrazinyl, 1,2,4-triazinyl and 1,3,5-triazinyl, the six-membered heteroaromatic radical comprising 1, 2 or 3 substituents L which are the same or different, R1, R2 independently represent hydrogen, C1-C8 alkyl, C1-C8 halogenalkyl, C1-C8 alkoxy, C3-C8 cycloalkyl, C3-C8 cycloalkoxy, C5-C10 bicycloalkyl, C3-C8 halogencycloalkyl, C2-C8 alkenyl, C2-C8 alkenyloxy, C4-C10 alkadienyl, C2-C8 halogenalkenyl, C3-C8 cycloalkenyl, C3-C8 halogencycloalkenyl, C2-C8 alkinyl, C2-C8 alkinyloxy, C2-C8 halogenalkinyl, NH2, C1-C8 alkylamino, Di-C1-C8-alkylamino, phenyl, naphthyl, or a five-membered or six-membered saturated, partially unsaturated or aromatic heterocycle, X represents hydrogen, halogen, OH, cyano, C1-C4 alkyl and the like, and Y represents hydrogen, halogen, cyano, C1-C4 alkyl, and the like.

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