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1. 发明申请

WO0026199A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO0026199A2
公开(公告)日：2000-05-11
申请号：PCT/GB9903607
申请日：1999-11-01
申请人： LILLY CO ELI , CLARK BARRY PETER , HARRIS JOHN RICHARD , KINGSTON ANN ELIZABETH
发明人： CLARK BARRY PETER , HARRIS JOHN RICHARD , KINGSTON ANN ELIZABETH
IPC分类号： A61K31/535 , A61P25/00 , A61P25/04 , A61P25/06 , A61P43/00 , C07D265/02 , A61R31/535
CPC分类号： C07D265/02
摘要： Use of a compound of formula (I) in which, R , R and R are independently hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C3-C10)cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryl(C1-C6)alkyl, unsubstituted or substituted aryl(c2-C6)alkenyl, halo, carboxy, (C1-C6)alkoxycarbonyl or -(CH2)m-OH wherein m is 1, 2 or 3; --- indicates a single or a double bond; X and Y are each independently hydrogen, or X and Y together represent a bridge of the formula -(CH2)n-, where n is 1 or 2; A1 and A2 are each independently an unsubstituted or substituted aryl; Z is -CO-, -SO2- or -CH2-; provided that, when Z is -CO-, A1 is not 3,4,5-trimethoxyphenyl; or a pharmaceutically-acceptable salt or ester thereof, for the manufacture of a medicament for the treatment of a condition indicating the administration of a selective mGluR1 antagonist.
摘要翻译：其中R 1，R 2和R 3独立地是氢，（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 3 -C 10）环烷基未取代或取代的芳基（C 1 -C 6）烷基，未取代或取代的芳基（C 2 -C 6）烯基，卤素，羧基，（C 1 -C 6）烷氧基羰基或 - （CH 2）m -OH，其中m为1 ，2或3; ---表示单键或双键; X和Y各自独立地为氢，或X和Y一起表示式 - （CH 2）n - 的桥，其中n为1或2; A1和A2各自独立地为未取代或取代的芳基; Z是-CO - ， - SO2-或-CH 2 - ; 条件是当Z是-CO-时，A1不是3,4,5-三甲氧基苯基; 或其药学上可接受的盐或酯，用于制备用于治疗指示施用选择性mGluR1拮抗剂的病症的药物。

2. 发明申请

WO0132632A3 PHARMACEUTICALLY ACTIVE 4-SUBSTITUTED PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：药物活性4-取代的吡嗪衍生物
公开(公告)号：WO0132632A3
公开(公告)日：2001-11-08
申请号：PCT/US0026261
申请日：2000-10-19
申请人： LILLY CO ELI , AMBLER SAMANTHA JAYNE , BAKER STEPHEN RICHARD , CLARK BARRY PETER , COLEMAN DARRELL STEPHEN , FOGLESONG ROBERT JAMES , GOLDSWORTHY JOHN , JAGDMANN GUNNAR ERIK JUNIOR , JOHNSON KIRK WILLIS , KINGSTON ANN ELIZABETH , OWTON WILLIAM MARTIN , SCHOEPP DARRYLE DARWIN , HONG JIAN ERIC , SCHKERYANTZ JEFFREY MICHAEL , VANNIEUWENHZE MICHAEL SCOTT , ZIA EBRAHIMI MOHAMMAD SADEGH
发明人： AMBLER SAMANTHA JAYNE , BAKER STEPHEN RICHARD , CLARK BARRY PETER , COLEMAN DARRELL STEPHEN , FOGLESONG ROBERT JAMES , GOLDSWORTHY JOHN , JAGDMANN GUNNAR ERIK JUNIOR , JOHNSON KIRK WILLIS , KINGSTON ANN ELIZABETH , OWTON WILLIAM MARTIN , SCHOEPP DARRYLE DARWIN , HONG JIAN ERIC , SCHKERYANTZ JEFFREY MICHAEL , VANNIEUWENHZE MICHAEL SCOTT , ZIA-EBRAHIMI MOHAMMAD SADEGH
IPC分类号： C07D239/46 , C07D239/94 , C07D239/95 , C07D403/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , A61K31/517 , A61P25/18
CPC分类号： C07D239/47 , C07D239/94 , C07D239/95 , C07D403/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to the use of certain 4-substituted pyrimidine derivatives as mGluR1 antagonists, to novel 4-substituted pyrimidine derivatives, to pharmaceutical formulations comprising 4-substituted pyrimidine derivatives, to a process for preparing 4-substituted pyrimidine derivatives and to intermediates useful in the preparation of 4-substituted pyrimidine derivatives.
摘要翻译：本发明涉及一种4-取代的嘧啶衍生物作为mGluR1拮抗剂，新颖的4-取代的嘧啶衍生物，包含4-取代的嘧啶衍生物的药物制剂，用于制备4-取代的嘧啶衍生物的方法和中间体有用在制备4-取代的嘧啶衍生物时。

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