公开(公告)号：WO2008060476A3

公开(公告)日：2008-12-24

申请号：PCT/US2007023669

申请日：2007-11-09

Applicant: SCHERING CORP ,  PALANI ANANDAN ,  SU JING ,  XIAO DONG ,  HUANG XIANHAI ,  RAO ASHWIN U ,  CHEN XIAO ,  TANG HAIQUN ,  QIN JUN ,  HUANG YING R ,  ASLANIAN ROBERT G ,  MCKITTRICK BRIAN A ,  DEGRADO SYLVIA J

Inventor： PALANI ANANDAN ,  SU JING ,  XIAO DONG ,  HUANG XIANHAI ,  RAO ASHWIN U ,  CHEN XIAO ,  TANG HAIQUN ,  QIN JUN ,  HUANG YING R ,  ASLANIAN ROBERT G ,  MCKITTRICK BRIAN A ,  DEGRADO SYLVIA J

IPC: C07D471/04 ,  A61K31/436 ,  A61K31/519 ,  A61P3/00 ,  A61P3/10 ,  A61P9/00 ,  C07D491/04

CPC classification number: C07D491/04 ,  C07D471/04

Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: (a), (b), (c), (d) and (e); and L is selected from the group consisting of: (f), (g), (h), and (i); pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，溶剂合物，酯和互变异构体，其中：Q选自：（a），（b），（c），（d）和 （E）; 并且L选自：（f），（g），（h）和（i）; 包含一种或多种式（I）化合物的药物组合物，以及使用式（I）化合物的方法。

公开(公告)号：WO0181325A3

公开(公告)日：2002-08-01

申请号：PCT/US0112530

申请日：2001-04-17

Applicant: SCHERING CORP

Inventor： VENKATRAMAN SRIKANTH ,  CHEN KEVIN X ,  ARASAPPAN ASHOK ,  NJOROGE F GEORGE ,  GIRIJAVALLABHAN VIYYOOR M ,  CHAN TIN-YAU ,  MCKITTRICK BRIAN A ,  PRONGAY ANDREW J ,  MADISON VINCENT S

IPC: A61K45/00 ,  A61K31/7052 ,  A61K38/00 ,  A61K38/21 ,  A61P31/12 ,  A61P31/14 ,  A61P43/00 ,  C07D273/00 ,  C07K5/02 ,  C07K7/02 ,  C07K7/64 ,  C07K7/06 ,  A61K38/05 ,  A61K38/07 ,  A61K38/08 ,  C07K5/062 ,  C07K5/065 ,  C07K5/087 ,  C07K5/107 ,  C07K14/18

CPC classification number: C07K5/0202 ,  A61K38/00 ,  C07K7/02

Abstract: The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.

Abstract translation: 本发明公开了具有HCV蛋白酶抑制活性的新型大环化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这种大环化合物的药物组合物以及使用它们治疗与HCV蛋白酶相关的病症的方法。

公开(公告)号：WO2008153793A3

公开(公告)日：2009-03-19

申请号：PCT/US2008006734

申请日：2008-05-28

Applicant: SCHERING CORP ,  ZHU ZHAONING ,  GREENLEE WILLIAM J ,  HUANG XIANHAI ,  MCKITTRICK BRIAN A ,  CLADER JOHN W ,  MCBRIAR MARK D ,  PALANI ANANDAN

Inventor： ZHU ZHAONING ,  GREENLEE WILLIAM J ,  HUANG XIANHAI ,  MCKITTRICK BRIAN A ,  CLADER JOHN W ,  MCBRIAR MARK D ,  PALANI ANANDAN

IPC: C07D403/10 ,  A61K31/4166 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5365 ,  A61P25/28 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D498/04 ,  C07D403/10 ,  C07D471/04 ,  C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

公开(公告)号：WO02051808A3

公开(公告)日：2003-01-23

申请号：PCT/US0149063

申请日：2001-12-17

Applicant: SCHERING CORP

Inventor： MCKITTRICK BRIAN A ,  GUO GUIHUA ,  ZHU ZHAONING ,  YE YUANZAN

IPC: A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/4545 ,  A61K31/46 ,  A61K45/00 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D211/34 ,  C07D401/12 ,  C07D405/04 ,  C07D451/04 ,  C07D401/04

CPC classification number: C07D451/04 ,  C07D211/34 ,  C07D405/04

Abstract: Amide derivatives of 1,4 di-substituted piperidine compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R is H, alkyl, or optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl, or bridged heterocycloalkyl; R is alkyl or -CH2OH; and R4 is H or alkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.

Abstract translation: 式（I）的1,4-二取代哌啶化合物或其药学上可接受的盐，酯或溶剂合物的酰胺衍生物，其中R 1是任选取代的环烷基，环烷基烷基，芳基，芳基烷基或杂芳基; R 2是H，烷基或任选取代的环烷基，环烷基烷基，杂环烷基，桥连环烷基或桥连杂环烷基; R 3是烷基或-CH 2 OH; R4为H或烷基; 是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。