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11. 发明申请

WO2004056770A3 PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS 审中-公开
标题翻译：哌啶衍生物可用作CCR5拮抗剂
公开(公告)号：WO2004056770A3
公开(公告)日：2004-08-12
申请号：PCT/US0340619
申请日：2003-12-17
申请人： SCHERING CORP
发明人： MILLER MICHAEL W , SCOTT JACK D
IPC分类号： A61P31/18 , A61P37/00 , C07D401/14 , A61K31/506
CPC分类号： C07D401/14
摘要： The present invention provides a compound of the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.
摘要翻译：本发明提供了式（I）化合物或其药学上可接受的盐或溶剂化物，其中各种部分如说明书中所定义。本发明还提供含有本发明化合物的药物组合物和使用本发明化合物的治疗方法。本发明还涉及本发明化合物和一种或多种可用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其他药剂的组合的用途。本发明进一步涉及本发明化合物单独或与其他药物组合用于治疗实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化。

12. 发明专利

JP2008031180A Bipiperidinyl derivative useful as inhibitors of chemokine receptors 审中-公开
标题翻译： BIPIPERIDINYL衍生物作为化合物受体的抑制剂有用
公开(公告)号：JP2008031180A
公开(公告)日：2008-02-14
申请号：JP2007265958
申请日：2007-10-11
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： MILLER MICHAEL W , SCOTT JACK D
IPC分类号： C07D211/58 , A61K31/445 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07D401/14 , C07D413/14
CPC分类号： C07D413/14 , C07D401/14
摘要： PROBLEM TO BE SOLVED: To provide a novel class of bipiperidinyl compounds as inhibitors of CCR5 receptors. SOLUTION: The novel class of the bipiperidinyl compounds represented formula (I) as the inhibitors of the CCR5 receptors in its many embodiments, 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 CCR5 using such compounds or pharmaceutical compositions are provided. The use of a combination of this compound and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV) is also provided. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供一类新的二哌啶基化合物作为CCR5受体的抑制剂。解决方案：在其许多实施方案中，作为CCR5受体的抑制剂的联哌啶基化合物的新类别表示式（I），制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备药物制剂的方法，包括提供一种或多种这样的化合物，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CCR5相关的一种或多种疾病的方法。还提供了使用该化合物与一种或多种用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其它药剂的组合。版权所有（C）2008，JPO＆INPIT

13. 发明专利

JP2012072195A Piperazine derivatives useful as ccr5 antagonists 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：JP2012072195A
公开(公告)日：2012-04-12
申请号：JP2012007201
申请日：2012-01-17
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： RAMANATHAN RAGULAN , GHOSAL ANIMA , MILLER MICHAEL W , CHOWDHURY SWAPAN K , ALTON KEVIN B
IPC分类号： C07D401/14 , A61K31/506 , A61K31/7004 , A61P1/00 , A61P11/06 , A61P17/00 , A61P19/02 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , C07H15/26
CPC分类号： C07D401/14 , C07D401/06 , C07H17/02
摘要： PROBLEM TO BE SOLVED: To provide piperazine derivatives useful as CCR5 antagonists.SOLUTION: The CCR5 antagonists having the following core structure formula (I) (AA) are claimed, for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis. The invention further relates to the use of a CCR-5 antagonist of formula I or II, alone or in combination with another agent, which is useful for the treatment of solid organ transplant rejection, graft v. host disease, inflammatory bowel disease, rheumatoid arthritis or multiple sclerosis.
摘要翻译：待解决的问题：提供可用作CCR5拮抗剂的哌嗪衍生物。解决方案：要求具有以下核心结构式（I）（AA）的CCR5拮抗剂用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化。本发明还涉及式I或II的CCR-5拮抗剂单独使用或与另一种药剂组合的用途，其可用于治疗实体器官移植排斥反应，移植物抗宿主病，炎症性肠病，类风湿病关节炎或多发性硬化。版权所有（C）2012，JPO＆INPIT

14. 发明专利

JP2011219493A Piperazine derivative useful as ccr5 antagonist 审中-公开
标题翻译：哌哌啶衍生物作为CCR5拮抗剂有用
公开(公告)号：JP2011219493A
公开(公告)日：2011-11-04
申请号：JP2011151208
申请日：2011-07-07
申请人： Schering 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 , 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 , A61P17/04 , 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
CPC分类号： C07D413/14 , C07D211/58 , C07D401/14 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide piperazine derivatives useful as selective CCR5 antagonists, pharmaceutical compositions containing compounds thereof, and methods of treatment using the compounds.SOLUTION: There are provided: the method, as for the treatment of HIV, comprising administering to a human in need of such treatment an effective amount of a CCR5 antagonist; the pharmaceutical composition for the treatment of HIV comprising an effective amount of a CCR5 antagonist in combination with a pharmaceutically acceptable carrier; and the pharmaceutical composition for the treatment of solid organ transplant rejection, graft vs host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies, or multiple sclerosis comprising an effective amount of a CCR5 antagonist in combination with a pharmaceutically acceptable carrier.
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，含有其化合物的药物组合物，以及使用该化合物的治疗方法。提供了：用于治疗HIV的方法，包括向需要这种治疗的人施用有效量的CCR5拮抗剂; 用于治疗HIV的药物组合物，其包含与药学上可接受的载体组合的有效量的CCR5拮抗剂; 以及用于治疗实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的药物组合物，其包含有效量的CCR5拮抗剂与药学上可接受的载体。版权所有（C）2012，JPO＆INPIT

15. 发明专利

JP2011251994A Substituted piperazine as cb1 antagonist 审中-公开
标题翻译：取代的哌嗪作为CB1拮抗剂
公开(公告)号：JP2011251994A
公开(公告)日：2011-12-15
申请号：JP2011170530
申请日：2011-08-03
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , STAMFORD ANDREW W , GREENLEE WILLIAM J , WEINSTEIN JAY
IPC分类号： C07D241/04 , A61K31/397 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P25/00 , A61P25/28 , A61P25/30 , A61P43/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06
CPC分类号： C07D241/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/10
摘要： PROBLEM TO BE SOLVED: To provide a novel class of substituted piperazine compounds as CBreceptor antagonists for treating various conditions.SOLUTION: Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CBreceptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions. The selective CBreceptors are piperazine derivatives having the structure of formula (I), or a pharmaceutically acceptable salt, solvate or ester thereof.
摘要翻译：待解决的问题：提供一类新颖的取代的哌嗪化合物作为治疗各种病症的CB 1“/ 1> 1受体拮抗剂。解决方案：式（I）化合物或其药学上可接受的盐，溶剂化物或酯可用于治疗由CB 1 受体介导的疾病或病症，例如代谢综合征和肥胖症，神经炎症性疾病，认知障碍和精神病，成瘾（例如戒烟），胃肠道疾病和心血管疾病。选择性CB 1 受体是具有式（I）结构的哌嗪衍生物或其药学上可接受的盐，溶剂合物或酯。版权所有（C）2012，JPO＆INPIT

16. 发明专利

JP2008222722A Piperidine derivative useful as ccr5 antagonist 审中-公开
标题翻译：哌啶衍生物作为CCR5拮抗剂有用
公开(公告)号：JP2008222722A
公开(公告)日：2008-09-25
申请号：JP2008134844
申请日：2008-05-22
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： PALANI ANANDAN , MILLER MICHAEL W , SCOTT JACK D
IPC分类号： C07D401/04 , C07D401/14 , A61K31/4545 , A61K31/506 , A61K45/00 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P37/06 , A61P37/08 , A61P43/00
CPC分类号： C07D401/14
摘要： PROBLEM TO BE SOLVED: To provide a selective CCR5 antagonist. SOLUTION: The present invention provides a compound of the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , R 9 , R 10 , A and B have specific meanings. The invention also relates to the use of a combination of a compound and one or more antiviral or other agents useful in the treatment of human immunodeficiency virus (HIV). The invention further relates to the use of a compound, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft versus host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供选择性CCR5拮抗剂。解决方案：本发明提供式（I）化合物或其药学上可接受的盐或溶剂化物，其中R 1，R 2，R SP， > 3 ，R 9 ，R 10 ，A和B具有特定含义。本发明还涉及化合物和一种或多种抗病毒剂或其它可用于治疗人类免疫缺陷病毒（HIV）的其他药剂的组合的用途。本发明还涉及化合物单独或与另一种药剂组合用于治疗实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，牛皮癣，哮喘，过敏的用途或多发性硬化症。版权所有（C）2008，JPO＆INPIT

17. 发明专利

JP2008074862A Ccr5 antagonist useful for treatment of aids 审中-公开
标题翻译： CCR5治疗艾滋病的有效方法
公开(公告)号：JP2008074862A
公开(公告)日：2008-04-03
申请号：JP2007279663
申请日：2007-10-26
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： MILLER MICHAEL W
IPC分类号： C07D401/14 , A61K31/18 , A61K31/506 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D403/06 , C07D409/14 , C07D417/14
CPC分类号： C07D401/14 , A61K31/18 , A61K31/506 , A61K45/06 , C07D403/06 , C07D409/14 , C07D417/14 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide CCR5 antagonists. SOLUTION: Disclosed are compounds of formula I (wherein Q, X, and Z are each CH or N; and R and R 1 to R 8 are each a specified substituent) and compositions containing them. These compounds are effective for the treatment of HIV AIDS, solid organ transplantation rejection, graft versus host diseases, inflammatory diseases, atopic dermatitis, asthma, allergies, or multiple sclerosis. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供CCR5拮抗剂。解决方案：公开了式I化合物（其中Q，X和Z各自为CH或N;且R和R 1为R“S” 指定的取代基）和含有它们的组合物。这些化合物对于治疗HIV艾滋病，实体器官移植排斥反应，移植物抗宿主病，炎性疾病，特应性皮炎，哮喘，过敏或多发性硬化有效。版权所有（C）2008，JPO＆INPIT

18. 发明专利

MY144301A SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS 未知
公开(公告)号：MY144301A
公开(公告)日：2011-08-29
申请号：MYPI20055634
申请日：2005-12-01
申请人： SCHERING CORP
发明人： GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , STAMFORD ANDREW W , GREENLEE WILLIAM J , JAY WEINSTEIN
IPC分类号： A61K31/497
摘要： SUBSTITITFED PIFERAZINES AS CB1 ANTAGONISTS COMPOUNDS OF FORMULA (1): X (A) (RL)P -'(B)N N-L 1-R N--AR2 AR' OR PHARMACEUTICALLY ACCEPTABLE SALTS, SOLVALES, OR ESTERS THEREOF, ARE USEFUL IN TREATING DISEASES OR CONDITIONS MEDIATED BY CB, RECEPTORS, SUCH AS METABOLIC SYNDROME AND OBESITY, NEURCINFLAMMATORY DISORDERS, COGNITIVE DISORDERS AND PSYCHOSIS, ADDICTION (E.G., SMOKING CESSATION), GASTROINTESTINAL DISORDERS, AND CARDIOVASCULAR CONDITIONS. 10 .DO') LA

20. 发明专利

SK287418B6 Pharmaceutical compositions comprising CCR5 antagonists and kit comprising this preparation 未知
公开(公告)号：SK287418B6
公开(公告)日：2010-09-07
申请号：SK51242007
申请日：2000-05-01
申请人： SCHERING 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 , SMITH ELIZABETH M , STEENSMA RUO , TAGAT JAYARAM R , VICE SUSAN F , LAUGHLIN MARK A , GILBERT ERIC , LABROLI MARC A
IPC分类号： C07D211/00 , C07D401/04 , A61K31/00 , A61K31/496 , A61K31/497 , A61K31/506 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P31/18 , A61P37/00 , A61P37/08 , A61P43/00 , C07D211/58 , C07D401/00 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/00 , C07D405/12 , C07D409/00 , C07D409/06 , C07D409/14 , C07D413/00 , C07D413/06 , C07D413/14 , G01F1/46
摘要： It is described a pharmaceutical composition comprising an effective amount of compound of the general formula (II) in combination with one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus and a pharmaceutically acceptable carrier. Also it is described a kit comprising mentioned pharmaceutical composition.

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