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    Substituted 5-Phenyl Pyrimidines I In Therapy
    3.
    发明申请
    Substituted 5-Phenyl Pyrimidines I In Therapy 审中-公开

    公开(公告)号：US20080146593A1

    公开(公告)日：2008-06-19

    申请号：US11815042

    申请日：2006-01-30

    Applicant: Joachim Rheinheimer ,  Thomas Grote ,  Bernd Muller ,  Barbara Nave ,  Frank Schieweck ,  Anja Schwogler ,  Thorsten Jabs ,  Carsten Blettner

    Inventor： Joachim Rheinheimer ,  Thomas Grote ,  Bernd Muller ,  Barbara Nave ,  Frank Schieweck ,  Anja Schwogler ,  Thorsten Jabs ,  Carsten Blettner

    IPC: A61K31/505 ,  A61K31/513 ,  A61P35/00

    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.

    7-Aminomethyl-1,2,4-Triazolo[1,5-A]Pyrimidine Compounds And Their Use For Controlling Pathogenic Fungi
    10.
    发明申请
    7-Aminomethyl-1,2,4-Triazolo[1,5-A]Pyrimidine Compounds And Their Use For Controlling Pathogenic Fungi 审中-公开
    7-氨基甲基-1,2,4-三唑并[1,5-A]嘧啶化合物及其用于控制​​致病真菌

    公开(公告)号：US20080076785A1

    公开(公告)日：2008-03-27

    申请号：US11663982

    申请日：2005-09-27

    Applicant: Carsten Blettner ,  Jordi Tormo i Blasco ,  Bernd Muller ,  Markus Gewehr ,  Wassilios Grammenos ,  Thomas Grote ,  Udo Hunger ,  Joachim Rheinheimer ,  Peter Schafer ,  Frank Schieweck ,  Anja Schwogler ,  Oliver Wagner ,  John-Bryan Speakman ,  Thorsten Jabs ,  Siegfried Strathmann ,  Ulrich Schofl ,  Maria Scherer ,  Reinhard Stierl

    Inventor： Carsten Blettner ,  Jordi Tormo i Blasco ,  Bernd Muller ,  Markus Gewehr ,  Wassilios Grammenos ,  Thomas Grote ,  Udo Hunger ,  Joachim Rheinheimer ,  Peter Schafer ,  Frank Schieweck ,  Anja Schwogler ,  Oliver Wagner ,  John-Bryan Speakman ,  Thorsten Jabs ,  Siegfried Strathmann ,  Ulrich Schofl ,  Maria Scherer ,  Reinhard Stierl

    IPC: A01N43/54 ,  A01P3/00 ,  C07D239/70

    CPC classification number: A01N43/90 ,  C07D487/04

    Abstract: The invention relates to 7-aminomethyl-1,2,4-triazolo[1,5-a]pyrimidine compounds of general formula (I) and the agriculturally compatible salts of said compounds. In said formula: R1 and R2 represent hydrogen, alkyl, haloalkyl, alkoxy, cycloalkyl, bicycloalkyl, halocycloalkyl, alkenyl, alkadienyl, haloalkenyl, cycloalkenyl, halocycloalkenyl, alkynyl, haloalkynyl or phenyl, naphthyl, or a 5- or 6-membered saturated, partially unsaturated or aromatic heterocycle, containing 1 to 4 heteroatoms from the group containing O, N or S, or R1 and R2, together with the nitrogen atom to which they are bonded, can also form a five- or six-membered heterocyclyl or heteroaryl, which is bonded by means of N and can contain 1 to 3 additional heteroatoms from the group containing O, N and S as the ring member and can be substituted according to the description; R3 and R4 represent hydrogen, alkyl, haloalkyl, haloalkoxy, alkoxy, or alkoxyalkyl; X represents halogen, cyano, a 5- or 6-membered saturated, partially unsaturated or aromatic heterocycle, containing 1, 2 or 3 heteroatoms from the group containing O, N or S as the ring member, alkyl, alkoxy, alkenyl or alkynyl, whereby the latter 4 groups can be substituted according to the description; L is defined as cited in the claims and the description; and m represents 0, 1, 2, 3, 4 or 5. The invention also relates to the use of the triazolopyrimidine compounds of general formula (I) and their agriculturally compatible salts for controlling plant-pathogenic fungi, to a method for controlling plant-pathogenic fungi, containing at least one compound of general formula (I) and/or an agriculturally compatible salt of said compound and at least one liquid or solid carrier.

    Abstract translation: 本发明涉及通式（I）的7-氨基甲基-1,2,4-三唑并[1,5-a]嘧啶化合物和所述化合物的农业上相容的盐。 在所述式中：R 1和R 2表示氢，烷基，卤代烷基，烷氧基，环烷基，二环烷基，卤代环烷基，烯基，链烯基，卤代烯基，环烯基，卤代环烯基，炔基，卤代炔基或苯基，萘基或5-或6-元饱和， 部分不饱和或芳族杂环，含有1至4个含有O，N或S的杂原子，或R 1和R 2与它们所键合的氮原子一起也可以形成五元或六元杂环基或杂芳基 ，其通过N键合并且可以含有来自含有O，N和S的基团的1至3个另外的杂原子作为环成员，并且可以根据描述进行取代; R3和R4代表氢，烷基，卤代烷基，卤代烷氧基，烷氧基或烷氧基烷基; X代表卤素，氰基，含有1,2或3个杂原子的5-或6-元饱和的部分不饱和或芳族杂环，所述杂环含有作为环成员的O，N或S，烷基，烷氧基，烯基或炔基， 由此后4个组可以根据描述被替代; L定义为权利要求书和说明书中引用的; 和m表示0,1,2,3,4或5.本发明还涉及通式（I）的三唑并嘧啶化合物及其农业上相容的盐用于控制植物致病真菌的用途，用于控制植物的方法 致病真菌，含有至少一种通式（I）的化合物和/或所述化合物的农业上相容的盐和至少一种液体或固体载体。

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