公开(公告)号：EP1976828A1

公开(公告)日：2008-10-08

申请号：EP06848156.3

申请日：2006-12-22

申请人： Schering Aktiengesellschaft

发明人： ARNAIZ, Damian ,  DAVEY, David ,  GUILFORD, William ,  CLEVE, Arwed ,  KIRKLAND, Thomas ,  CLARET, Emmanuel ,  KHIM, Seock-Kyu ,  BROWN, Greg ,  YE, Bin ,  VOGEL, David ,  LIGHT, David ,  LIANG, Amy ,  KOCHANNY, Monica ,  WEI, Guo, Ping ,  PARKINSON, John

IPC分类号： C07D207/04 ,  C07D211/58 ,  C07D243/08 ,  C07D295/04 ,  C07D295/16 ,  C07D451/04 ,  C07D487/08 ,  A61K31/13 ,  A61K31/33 ,  C07C211/01 ,  C07C211/43 ,  A61P29/00

CPC分类号： C07D487/08 ,  C07B2200/07 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07C2601/14 ,  C07D207/04 ,  C07D207/09 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/58 ,  C07D243/08 ,  C07D263/14 ,  C07D263/32 ,  C07D277/22 ,  C07D277/68 ,  C07D295/04 ,  C07D295/096 ,  C07D295/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04

摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

摘要翻译： 本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体 或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

公开(公告)号：EP1565446A1

公开(公告)日：2005-08-24

申请号：EP03780086.9

申请日：2003-11-28

申请人： Schering Aktiengesellschaft

发明人： BRYANT, Judi ,  KOCHANNY, Monica ,  YUAN, Shendong ,  KHIM, Seock-Kyu ,  BUCKMAN, Brad ,  ARNAIZ, Damian ,  BÖMER, Ulf ,  BRIEM, Hans ,  ESPERLING, Peter ,  HUWE, Peter ,  KUHNKE, Joachim ,  SCHÄFER, Martina ,  WORTMANN, Lars ,  KOSEMUND, Dirk ,  ECKLE, Emil ,  FELDMAN, Richard ,  PHILLIPS, Gary

IPC分类号： C07D239/30 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12 ,  C07D417/14 ,  A61K31/506 ,  A61P35/02

CPC分类号： C07D239/47 ,  C07D239/30 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseases.

公开(公告)号：EP1680401A2

公开(公告)日：2006-07-19

申请号：EP04796276.6

申请日：2004-10-22

申请人： Schering Aktiengesellschaft

发明人： ARNAIZ, Damian ,  BRYANT, Judi ,  CHOU, Yuo-Ling ,  FELDMAN, Richard, I. ,  HRVATIN, Paul ,  ISLAM, Imadul ,  KOCHANNY, Monica ,  LEE, Wheeseong ,  POLOKOFF, Mark ,  YU, Hongyi ,  YUAN, Shendong

IPC分类号： C07D209/34 ,  C07D413/14 ,  C07D409/06 ,  C07D407/14 ,  C07D405/06 ,  C07D403/14 ,  C07D403/06 ,  C07D401/14 ,  C07D401/06 ,  A61K31/404

CPC分类号： C07D209/34 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

摘要： Indolinone derivatives, such as compounds of the formula (I); wherein A, m, n, R1, R 2 , R 3 , R 5 and R 6 are described herein, are disclosed herein as being useful in treating mammal having disease-states alleviated by the inhibition of PDK-1 activity.

公开(公告)号：EP0929547A1

公开(公告)日：1999-07-21

申请号：EP97942015.0

申请日：1997-09-11

申请人： SCHERING AKTIENGESELLSCHAFT

发明人： KOCHANNY, Monica ,  MORRISSEY, Michael, M. ,  NG, Howard, P.

IPC分类号： A61K31 ,  A61P7 ,  C07D401 ,  C07D417

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D417/14

摘要： This invention is directed to benzamidine derivatives substituted by cyclic amico acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants as represented by formulae (I), (II), (III), (IV), (V), (VI), (VII) wherein: A is -C(R8)= or -N=; Z?1 and Z2¿ are independently -O-, -N(R9)-, -S-, -S(O)-, -S(O)¿2?-, or -OCH2-; R?2¿ is -C(NH)NH¿2?, -C(NH)N(H)OR?9¿, -C(NH)N(H)C(O)OR12, -C(NH)N(H)C(O)R9, -C(NH)N(H)S(O)¿2R?12, or -C(NH)N(H)C(O)N(H)R9; R7 is -N(R?9)-(C(R9)(R10))¿n-R13 (where n is 0 to 4), -O-(C(R?9)(R10))¿n-R13 (where n is 0 to 4), or -N(R?14)R15; R1 and R3 - R6¿ are as defined in the description. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

公开(公告)号：EP0929547B1

公开(公告)日：2002-11-27

申请号：EP97942015.5

申请日：1997-09-11

申请人： SCHERING AKTIENGESELLSCHAFT

发明人： KOCHANNY, Monica ,  MORRISSEY, Michael, M. ,  NG, Howard, P.

IPC分类号： C07D401/12 ,  A61K31/44 ,  A61K31/415 ,  C07D401/14 ,  C07D417/14

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D417/14

摘要： This invention is directed to benzamidine derivatives substituted by cyclic amico acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants as represented by formulae (I), (II), (III), (IV), (V), (VI), (VII) wherein: A is -C(R8)= or -N=; Z?1 and Z2¿ are independently -O-, -N(R9)-, -S-, -S(O)-, -S(O)¿2?-, or -OCH2-; R?2¿ is -C(NH)NH¿2?, -C(NH)N(H)OR?9¿, -C(NH)N(H)C(O)OR12, -C(NH)N(H)C(O)R9, -C(NH)N(H)S(O)¿2R?12, or -C(NH)N(H)C(O)N(H)R9; R7 is -N(R?9)-(C(R9)(R10))¿n-R13 (where n is 0 to 4), -O-(C(R?9)(R10))¿n-R13 (where n is 0 to 4), or -N(R?14)R15; R1 and R3 - R6¿ are as defined in the description. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.