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1. 发明申请

WO2007084319A3 DIARYL PIPERIDINES AS CB1 MODULATORS 审中-公开
标题翻译： DIARYL PIPERIDINES作为CB1调节器
公开(公告)号：WO2007084319A3
公开(公告)日：2007-09-20
申请号：PCT/US2007000705
申请日：2007-01-11
申请人： SCHERING CORP , SCOTT JACK D , WEINSTEIN JAY , MILLER MICHAEL W , STAMFORD ANDREW W , GILBERT ERIC J , XIA YAN , GREENLEE WILLIAM J , LI WEI
发明人： SCOTT JACK D , WEINSTEIN JAY , MILLER MICHAEL W , STAMFORD ANDREW W , GILBERT ERIC J , XIA YAN , GREENLEE WILLIAM J , LI WEI
IPC分类号： C07D211/18 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06
CPC分类号： C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/58 , C07D211/60 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D471/10
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome (e.g., obesity, waist circumference, lipid profile, and insulin sensitivity), neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂化物或酯可用于治疗疾病，病症或病症如代谢综合征（例如，肥胖，腰围，脂质分布和胰岛素敏感性），神经炎症性疾病，认知障碍，精神病，成瘾行为，胃肠道疾病和心血管疾病。

2. 发明申请

WO2009005646A3 SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS 审中-公开
标题翻译：取代的PIPERAZINES作为CB1拮抗剂
公开(公告)号：WO2009005646A3
公开(公告)日：2009-03-19
申请号：PCT/US2008007868
申请日：2008-06-25
申请人： SCHERING CORP , GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , DEMONG DUANE EUGENE , STAMFORD ANDREW , GREENLEE WILLIAM J , CELLY CHANDER SHEKHER
发明人： GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , DEMONG DUANE EUGENE , STAMFORD ANDREW , GREENLEE WILLIAM J , CELLY CHANDER SHEKHER
IPC分类号： C07D241/04 , A61K31/496 , A61K31/506 , A61P3/00 , A61P9/10 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D241/04 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14
摘要： Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或酯可用于治疗由CB1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。

3. 发明申请

WO2009005671A2 SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS 审中-公开
标题翻译：取代的哌嗪作为CB1拮抗剂
公开(公告)号：WO2009005671A2
公开(公告)日：2009-01-08
申请号：PCT/US2008007917
申请日：2008-06-25
申请人： SCHERING CORP , GILBERT ERIC J , GREENLEE WILLIAM J , LI SARAH WEI , MILLER MICHAEL W , SCOTT JACK D , STAMFORD ANDREW , CELLY CHANDER SHEKHER
发明人： GILBERT ERIC J , GREENLEE WILLIAM J , LI SARAH WEI , MILLER MICHAEL W , SCOTT JACK D , STAMFORD ANDREW , CELLY CHANDER SHEKHER
IPC分类号： C07D241/04 , A61K31/495 , A61P3/00 , C07D401/06
CPC分类号： C07D401/06 , C07D241/04
摘要： Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或酯可用于治疗由CB 1受体介导的疾病或病症，所述疾病或病症例如代谢综合征和肥胖症，神经炎性病症，认知障碍和精神病，成瘾（例如吸烟戒烟），胃肠疾病和心血管疾病。

4. 发明申请

WO2007084450A3 CANNIBINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNIBINOID接收器调制器
公开(公告)号：WO2007084450A3
公开(公告)日：2007-11-08
申请号：PCT/US2007001024
申请日：2007-01-16
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , EAGEN KEITH A , SCOTT JACK D , WANG YUGUANG , XIA YAN , GREENLEE WILLIAM J
发明人： CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , EAGEN KEITH A , SCOTT JACK D , WANG YUGUANG , XIA YAN , GREENLEE WILLIAM J
IPC分类号： C07D209/44 , C07C233/05 , C07C233/59 , C07D209/46 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
CPC分类号： C07D209/46 , C07C233/31 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/90 , C07D209/44 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
摘要： A compound having the general structure of Formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.
摘要翻译：具有式（I）通式结构的化合物：化学式应插入此处，如出现在摘要中的纸张形式。或其药学上可接受的盐，溶剂化物或酯可用于治疗诸如肥胖症，代谢紊乱，成瘾，中枢神经系统疾病，心血管疾病，呼吸系统疾病和胃肠疾病的疾病，病症或病症。

5. 发明申请

WO2005042517A3 BIPIPERIDINYL DERIVATIVES USEFUL AS INHIBITORS OF CHEMOKINE RECEPTORS 审中-公开
标题翻译：用作趋化因子受体抑制剂的双脒基衍生物
公开(公告)号：WO2005042517A3
公开(公告)日：2005-07-28
申请号：PCT/US2004036273
申请日：2004-11-01
申请人： SCHERING CORP , MILLER MICHAEL W , SCOTT JACK D
发明人： MILLER MICHAEL W , SCOTT JACK D
IPC分类号： A61K31/445 , C07D401/14 , C07D413/14 , A61P9/02 , A61P11/06 , A61P17/06 , A61P31/18
CPC分类号： C07D413/14 , C07D401/14
摘要： In its many embodiments, the present invention provides a novel class of bipiperidinyl compounds as inhibitors of the CCR5 receptors, 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. 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：在其许多实施方案中，本发明提供了一类新的双哌啶基化合物作为CCR5受体的抑制剂，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此类化合物的药物制剂的方法，以及使用此类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。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。

6. 发明申请

WO2014099788A1 C5-SPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS 审中-公开
标题翻译： C5-SPIRO三嗪基二氧化物作为BACE抑制剂
公开(公告)号：WO2014099788A1
公开(公告)日：2014-06-26
申请号：PCT/US2013075400
申请日：2013-12-16
申请人： MERCK SHARP & DOHME , CUMMING JARED N , SCOTT JACK D , STAMFORD ANDREW W , ISERLOH ULRICH , NEELAMKAVIL SANTHOSH FRANCIS , SHAO PENGCHENG PATRICK , WILSON JONATHAN E
发明人： CUMMING JARED N , SCOTT JACK D , STAMFORD ANDREW W , ISERLOH ULRICH , NEELAMKAVIL SANTHOSH FRANCIS , SHAO PENGCHENG PATRICK , WILSON JONATHAN E
IPC分类号： A61K31/519 , A61K31/497
CPC分类号： C07D285/24 , C07D285/20 , C07D417/12 , C07D471/04 , C07D513/10 , C07D519/00
摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed:
摘要翻译：在其许多实施方案中，本发明提供某些C5-螺亚氨基二嗪二氧化物化合物，包括式（I）化合物：（结构表示）或其互变异构体及所述化合物的药学上可接受的盐，其中R1，R2，R3，X，Y ，s，环A，RA，m，-L1-和RL如本文所定义。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物，

7. 发明申请

WO2008130616A3 DIARYL MORPHOLINES AS CB1 MODULATORS 审中-公开
标题翻译：二芳基吗啉作为CB1调节剂
公开(公告)号：WO2008130616A3
公开(公告)日：2008-12-18
申请号：PCT/US2008005000
申请日：2008-04-17
申请人： SCHERING CORP , SCOTT JACK D , STAMFORD ANDREW
发明人： SCOTT JACK D , STAMFORD ANDREW
IPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , C07D265/32 , C07D413/12
CPC分类号： C07D265/30 , C07D265/32 , C07D413/12
摘要： The present invention provides compounds having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, which are useful as CB1 receptor antagonists. The compounds of the invention may be useful in treating diseases, disorders, or conditions responsive to CB1 receptor antagonists, including, but not limited to, metabolic syndrome, obesity, waist circumference, dyslipidemia, insulin sensitivity, neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：本发明提供了具有通式（I）的通式结构的化合物或其药学上可接受的盐，溶剂合物，酯或前药，其可用作CB 1受体拮抗剂。本发明化合物可用于治疗对CB1受体拮抗剂有响应的疾病，病症或病症，包括但不限于代谢综合征，肥胖症，腰围，血脂异常，胰岛素敏感性，神经炎性病症，认知障碍，精神病，成瘾行为，胃肠疾病和心血管疾病。

8. 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。

9. 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

10. 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

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