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1. 发明专利

JP2007297410A Muscarinic antagonist 审中-公开
标题翻译：心理拮抗剂
公开(公告)号：JP2007297410A
公开(公告)日：2007-11-15
申请号：JP2007203608
申请日：2007-08-03
申请人： Schering Plough Corp , シェーリングコーポレイションSchering Corporation
发明人： MCKITTRICK BRIAN A , GUO GUIHUA , ZHU ZHAONING , YE YUANZAN
IPC分类号： C07D211/34 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/4525 , A61K31/453 , A61K31/4545 , A61K31/46 , A61K45/00 , A61P25/00 , A61P25/28 , A61P43/00 , C07D211/58 , C07D401/12 , C07D405/04 , C07D451/04
CPC分类号： C07D451/04 , C07D211/34 , C07D405/04
摘要： PROBLEM TO BE SOLVED: To provide a muscarinic antagonist which is a piperidine derivative useful for treating cognitive disorders such as Alzheimer's disease.
SOLUTION: The compound is an amide derivative of a 1,4 di-substituted piperidine compound of formula (I) (wherein R
1 is an optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R
2 is H, an alkyl or an optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl or bridged heterocycloalkyl; R
3 is an alkyl or -CH
2 OH; R
4 is H or an alkyl; R
5 is 1-4 substituents each independently chosen from the group consisting of H, an alkyl, a halogen, -OH, an alkoxy, CF
3 , -CN, -CO
2 R
4 , -CONHR
4 , -SO
2 NHR
4 , -NHSO
2 R
4 and -NHC(O)R
4 ; and R
6 is 1-4 substituents each independently chosen from the group consisting of H, an alkyl, a halogen, -OH, an alkoxy, CF
3 , -NH
2 , an alkylamino, phenyl, an alkylenedioxy and an alkoxycarbonyl) or a pharmaceutically acceptable salt, ester or solvate thereof.
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供毒蕈碱拮抗剂，其是用于治疗认知障碍如阿尔茨海默氏病的哌啶衍生物。解决方案：该化合物是式（I）的1,4-二取代的哌啶化合物的酰胺衍生物（其中R 1 SP 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 S 2 OH; R SP 4是H或烷基; R 6是独立地选自H，烷基，卤素的1-4个取代基，-OH，烷氧基，CF 3 SB，-CN，-CO 2 SBR，SPON 4，SPON 4，，-SO 2 SBR，NHSO 2，R 4，和-NHC（O）R SP 3， 4 ; R 6是独立地选自H，烷基，卤素，-OH，烷氧基，CF 3，苯基，烷基氨基，苯基，亚烷基二氧基和烷氧基羰基）或其药学上可接受的盐，酯或溶剂合物。版权所有（C）2008，JPO＆INPIT

2. 发明专利

JP2007284451A Piperidine mch antagonist and application of the same to treatment of obesity 审中-公开
标题翻译：哌啶类药物拮抗剂及其应用于治疗肥胖症
公开(公告)号：JP2007284451A
公开(公告)日：2007-11-01
申请号：JP2007195250
申请日：2007-07-26
申请人： Schering Plough Corp , シェーリングコーポレイションSchering Corporation
发明人： MCKITTRICK BRIAN A , SU JING , CLADER JOHN W , LI SHENGJIAN , GUO GUIHUA
IPC分类号： C07D211/30 , C07D211/34 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4965 , A61K31/498 , A61K31/517 , A61P3/04 , A61P3/10 , A61P43/00 , C07D401/06 , C07D405/06 , C07D413/06 , C07D417/06
CPC分类号： C07D401/06 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4709 , A61K31/4965 , A61K31/517 , C07D211/34 , C07D405/06 , C07D413/06 , C07D417/06
摘要： PROBLEM TO BE SOLVED: To provide an antagonist to melanine-concentrating hormone (MCH). SOLUTION: A compound expressed by structural formula (I), pharmaceutically permissible salts, esters or solvates of the same, a pharmaceutical composition containing the compound and application of the compound to treatments for eating disorders and diabetes are provided. The method for treating eating disorders and diabetes includes a process for administering an effective amount of the compound expressed by the structural formula (I) to mammals requiring the treatments for eating disorders (e.g., obesity and hyperphagia) and diabetes. Another aspect of affairs of the invention is the pharmaceutical composition for treatments for eating disorders and obesity containing the compound expressed by the structural formula (I) combined with a pharmaceutically acceptable carrier. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供对黑素浓缩激素（MCH）的拮抗剂。解决方案：提供由结构式（I）表示的化合物，其药学上可允许的盐，酯或溶剂合物，含有该化合物的药物组合物和将该化合物应用于进食障碍和糖尿病的治疗。用于治疗进食障碍和糖尿病的方法包括将有效量的由结构式（I）表达的化合物施用于需要进食障碍（例如肥胖症和肥胖症）和糖尿病的治疗的哺乳动物的方法。本发明的另一方面是用于饮食障碍和肥胖症治疗的药物组合物，其含有结构式（I）表示的化合物与药学上可接受的载体组合。版权所有（C）2008，JPO＆INPIT

3. 发明专利

JP2006225407A PIPERAZINE DERIVATIVE USEFUL AS CCR5 ANTAGONIST 审中-公开
公开(公告)号：JP2006225407A
公开(公告)日：2006-08-31
申请号：JP2006152916
申请日：2006-05-31
申请人： SCHERING PLOUGH CORP
发明人： BAROUDY BAHIGE M , CLADER JOHN W , JOSIEN HUBERT B , MCCOMBIE STUART W , MCKITTRICK BRIAN A , MILLER MICHAEL W , NEUSTADT BERNARD R , PALANI ANANDAN , STEENSMA RUO , TAGAT JAYARAM R , VICE SUSAN F , LAUGHLIN MARK A
IPC分类号： C07D211/58 , A61K31/4468 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/506 , A61P1/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/12 , A61P31/18 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide piperazine derivatives useful as selective CCR5 antagonists, pharmaceutical compositions comprising the compounds and a treatment method using the compounds. SOLUTION: In relation to treatment of HIV, the method includes a step to administer effective dose of CCR5 antagonists to a human in need of such treatment; the pharmaceutical compositions comprise the effective dose of CCR5 antagonists combined with pharmaceutically acceptable carriers and are for treatment of HIV; and the pharmaceutical compositions is for treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis and comprise the effective dose of CCR5 antagonists of Formula II combined with the pharmaceutically acceptable carriers. COPYRIGHT: (C)2006,JPO&NCIPI

4. 发明专利

JP2006052225A Piperazine derivative useful as ccr5 antagonist 审中-公开
标题翻译：哌嗪衍生物作为CCR5拮抗剂有用
公开(公告)号：JP2006052225A
公开(公告)日：2006-02-23
申请号：JP2005236161
申请日：2005-08-16
申请人： Schering Plough Corp , シェーリングコーポレイションSchering Corporation
发明人： BAROUDY BAHIGE M , CLADER JOHN W , JOSIEN HUBERT B , MCCOMBIE STUART W , MCKITTRICK BRIAN A , MILLER MICHAEL W , NEUSTADT BERNARD R , PALANI ANANDAN , SMITH ELIZABETH M , STEENSMA RUO , TAGAT JAYARAM R , VICE SUSAN F , LAUGHLIN MARK A , GILBERT ERIC , LABROLI MARC A
IPC分类号： C07D401/04 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/695 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P37/00 , A61P37/08 , A61P43/00 , C07D211/58 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07F5/02 , C07F7/10 , G01F1/46
CPC分类号： C07D409/06 , A61K31/496 , C07D211/58 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/12 , C07D413/06
摘要： PROBLEM TO BE SOLVED: To provide a piperazine derivative useful as a selective CCR5 antagonist. SOLUTION: The invention relates to the use of a CCR5 antagonist expressed by formula (II) or its pharmacologically permissible salt for the treatment of HIV, etc. In the formula, R is phenyl or the like; R 1 is H or an alkyl; R 2 is a phenyl-substituted group, a heteroaryl, naphthyl, fluorenyl, a diphenylmethyl-substituted group or as necessary a phenylalkyl-substituted group; R 3 is H, an alkyl, an alkoxyalkyl, a cycloalkyl, a cycloalkylalkyl or as necessary phenyl or the like; R 4 , R 5 and R 7 are each H or an alkyl; and R 6 is H, an alkyl or an alkenyl. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供可用作选择性CCR5拮抗剂的哌嗪衍生物。解决方案：本发明涉及由式（II）表示的CCR5拮抗剂或其药理学上允许的盐用于治疗HIV等的用途。在该式中，R是苯基等; R 1是H或烷基; R 2是苯基取代的基团，杂芳基，萘基，芴基，二苯基甲基取代的基团或根据需要的苯基烷基取代的基团; R 3是H，烷基，烷氧基烷基，环烷基，环烷基烷基或必要的苯基等; R 4 ，R 5 和R 7 各自为H或烷基; 且R 6为H，烷基或烯基。版权所有（C）2006，JPO＆NCIPI

5. 发明专利

HUT77088A SULFUR-SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 未知
公开(公告)号：HUT77088A
公开(公告)日：1998-03-02
申请号：HU9701924
申请日：1995-11-15
申请人： SCHERING PLOUGH CORP
发明人： BURNETT DUANE A , DUGAR SUNDEEP , MCKITTRICK BRIAN A
IPC分类号： A61K31/395 , A61K31/397 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P3/06 , A61P9/10 , C07D205/08 , C07D401/12 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula I or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl, R10-substituted aryl or heteroaryl; Ar2 is aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X and Y are -CH2-, -CH(lower alkyl)- or -C(dilower alkyl)-; R is -OR6, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7; R1 is hydrogen, lower alkyl or aryl; or R and R1 together are =O; q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5; R4 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -(lower alkylene)-COOR6 and -CH=CH-COOR6; R5 is selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -CF3, -CN, -NO2, halogen, -(lower alkylene)COOR6 and -CH=CH-COOR6; R6, R7 and R8 are H, lower alkyl, aryl or aryl-substituted lower alkyl; R9 is lower alkyl, aryl or aryl-substituted lower alkyl; and R10 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -CF3, -CN, -NO2 and halogen; are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

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