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    SUBSTITUTED 5-PHENYL PYRIMIDINES I IN THERAPY
    1.
    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

    Applicant: BASF AG ,  RHEINHEIMER JOACHIM ,  GROTE THOMAS ,  MUELLER BERND ,  NAVE BARBARA ,  SCHIEWECK FRANK ,  SCHWOEGLER ANJA ,  JABS THORSTEN ,  BLETTNER CARSTEN

    Inventor： RHEINHEIMER JOACHIM ,  GROTE THOMAS ,  MUELLER BERND ,  NAVE BARBARA ,  SCHIEWECK FRANK ,  SCHWOEGLER ANJA ,  JABS THORSTEN ,  BLETTNER CARSTEN

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

    6-phenyl-7-amino-triazolopyrimidines, methods for the production thereof, the use thereof for controlling pathogenic fungi, and agents containing the same
    4.
    发明专利
    6-phenyl-7-amino-triazolopyrimidines, methods for the production thereof, the use thereof for controlling pathogenic fungi, and agents containing the same 未知

    公开(公告)号：ZA200702822B

    公开(公告)日：2009-12-30

    申请号：ZA200702822

    申请日：2007-04-04

    Applicant: BASF AG

    Inventor： BLETTNER CARSTEN ,  TORMO I BLASCO ,  JORDI MUELLER BERND ,  GEWEHR MARKUS ,  GRAMMENOS WASSILIOS ,  GROTE THOMAS ,  HUENGER UDO ,  RHEINHEIMER JOACHIM ,  SCHAEFER PETER ,  SCHIEWECK FRANK ,  SCHWOEGLER ANJA ,  SPEAKMAN JOHN-BRYAN ,  JABS THORSTEN ,  STRATHMANN SIEGFRIED ,  SCHOEFL ULRICH ,  SCHERER MARIA ,  STIERL REINHARD ,  DIETZ JOCHEN

    IPC: A01N20100101 ,  C07D20100101

    Abstract: 6-Phenyl-7-aminotriazolopyrimidines of the formula I in which the substituents are as defined below: R 1 is hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, cycloalkenyl, halocycloalkenyl, alkynyl, haloalkynyl or phenyl, naphthyl, or a five- or six-membered saturated, partially unsaturated or aromatic heterocycle, which comprises one to four heteroatoms from the group consisting of O, N and S, R 2 is alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, cycloalkenyl, halocycloalkenyl, alkynyl, haloalkynyl or phenyl, naphthyl, or a five- or six-membered saturated, partially unsaturated or aromatic heterocycle which comprises one to four heteroatoms from the group consisting of O, N and S, R 3 ,R 4 ,R 5 ,R 6 ,R 7 are hydrogen or one of the groups mentioned under R 2 , R 4 , together with R 3 or R 6 , may also form a five- or six-membered saturated or unsaturated ring which, in addition to carbon atoms, may comprise one to three further heteroatoms from the group consisting of O, N and S as ring members; R 2 with R 3 , R 4 with R 5 , R 6 with R 7 may in each case together, with formation of spiro groups, also form a C 2 -C 5 -alkylene, or alkenylene or alkynylene chain which may be interrupted by one to three heteroatoms from the group consisting of O, N and S; p is zero or 1; L is halogen, alkyl, haloalkyl, alkoxy, cyano, nitro, amino, alkylamino, dialkylamino, alkylcarbonylamino, C(O)-R, S(O) n -R; where n is zero, 1 or 2; R is hydrogen, alkyl, haloalkyl, alkoxy, alkenyloxy, alkynyloxy, amino, alkylamino, dialkylamino; m is 1, 2, 3, 4 or 5; X is halogen, cyano, alkyl, alkoxy, alkenyloxy, alkynyloxy or haloalkoxy; Y is oxygen or sulfur; Z is hydrogen, alkyl, haloalkyl, cycloalkyl, alkylcarbonyl, cycloalkylcarbonyl, alkenyl, haloalkenyl, cycloalkenyl, alkynyl, haloalkynyl, phenyl, naphthyl, a five- to ten-membered saturated, partially unsaturated or aromatic heterocycle which comprises one to four heteroatoms from the group consisting of O, N and S; or Z together with R 4 or R 6 may also form a five- or six-membered saturated or unsaturated ring which, in addition to carbon atoms and Y, may comprise one or two further heteroatoms from the group consisting of O, N and S as ring members the groups R 1 to R 7 , Z and R may be substituted according to the description; processes for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.

    5-FENILPIRIMIDINAS I EN TERAPEUTICA.
    7.
    发明专利
    5-FENILPIRIMIDINAS I EN TERAPEUTICA. 未知

    公开(公告)号：MX2007008397A

    公开(公告)日：2007-09-07

    申请号：MX2007008397

    申请日：2006-01-30

    Applicant: BASF AG

    Inventor： MULLER BERND ,  GROTE THOMAS ,  JABS THORSTEN ,  RHEINHEIMER JOACHIM ,  SCHIEWECK FRANK ,  BLETTNER CARSTEN ,  NAVE BARBARA ,  SCHWOEGLER ANJA

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

    Abstract: La presente invencion se refiere a 5-fenilpirimidinas I sustituidas que llevan un radical X en la posicion 4 del anillo pirimidina, un radical Y en la posicion 6 del anillo pirimidina, el radical X que designa un grupo de la formula NR1R2, OR1a o SR1a, en donde R1, R2, de modo independiente entre si, designan hidrogeno, alquilo C1-C10, alquenilo C2-C6, alquinilo C2-C6, haloalquilo C1-C10, cicloalquilo C3-C8, halocicloalquilo C3-C8, fenilo, o heteroarilo de 5 o 6 miembros o heterociclilo de 5 o 6 miembros, que contiene 1, 2, 3 o 4 atomos de nitrogeno o 1, 2 o 3 atomos de nitrogeno y un atomo de azufre u oxigeno como miembros del anillo, cuyos radicales pueden no estar sustituidos o pueden llevar 1, 2, 3 o 4 radicales Ra1; o el radical NR1R2 tambien puede formar un anillo heterociclico opcionalmente sustituido de 5 o 6 miembros, que contiene 1, 2, 3 o 4 atomos de nitrogeno o 1, 2 o 3 atomos de nitrogeno y un atomo de azufre u oxigeno como miembros del anillo, que son no adyacentes al nitrogeno de NR1R2, en donde dos atomos de C adyacentes o un atomo de N y un atomo de C adyacente pueden unirse por una cadena alquileno C1-C4 y en donde el anillo heterociclico puede no estar sustituido o puede llevar 1, 2, 3 o 4 radicales Ra1 tal como se definio en la reivindicacion 1 R1a tiene uno de los significados dados para R1 salvo para hidrogeno; el radical Y esta seleccionado del grupo que consiste en halogeno, ciano, alquilo C1-C4, alquenilo C2-C4, alquinilo C2-C4, cicloalquilo C3-C6, alcoxi C1-C4, alqueniloxi C3-C4, alquiniloxi C3-C4, alquiltio C1-C6, di-(alquil C1-C6)amino o alquil C1-C6-amino, en donde los radicales alquilo, alquenilo y alquinilo de Y pueden estar sustituidos con halogeno, ciano, nitro, alcoxi C1-C2 o alcoxi C1-C4-carbonilo; y en donde el radical pirimidina tambien puede llevar un radical diferente de hidrogeno en la posicion 2 y en donde el anillo fenilo en la posicion 5 del anillo pirimidina puede no estar sustituido o puede llevar 1, 2, 3, 4 o 5 radicales L que son diferentes de hidrogeno, y las sales farmaceuticamente aceptables de 5-fenilpirimidinas sustituidas para usar en terapeutica, en particular en terapeutica o tratamiento de enfermedades cancerosas.

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