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1. 发明申请

US20110312995A1 BRIDGED AND FUSED HETEROCYCLIC ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：桥联和融合的杂环化学抗菌化合物
公开(公告)号：US20110312995A1
公开(公告)日：2011-12-22
申请号：US13145359
申请日：2010-01-21
申请人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Robert Jason Herr , Jason L. Davis , Kai Deng , Ming Min Hsia , Shuangyi Wan
发明人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Robert Jason Herr , Jason L. Davis , Kai Deng , Ming Min Hsia , Shuangyi Wan
IPC分类号： A61K31/4545 , C07D417/14 , C07D417/12 , A61K31/4709 , A61P3/00 , A61K31/4439 , A61P5/48 , A61P3/10 , A61P3/04 , A61P3/06 , C07D401/14 , A61K31/454
CPC分类号： C07D417/12 , C07D215/233 , C07D417/14
摘要： This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译：本发明提供了一些式（I）的桥连和稠合杂环化合物或其药学上可接受的盐，酯溶剂合物或前药，其中：L是：（II），其它变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。

2. 发明申请

US20110313008A1 PENTAFLUOROSULPHOLANE-CONTAINING ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：含芳香脂肪酸的抗菌化合物
公开(公告)号：US20110313008A1
公开(公告)日：2011-12-22
申请号：US13145025
申请日：2010-01-21
申请人： Hubert B. Josien , John W. Clader , Andrew Stamford , William J. Greenlee , Michael John Mayer , Jason L. Davis , Ming Min Hsia , Shuangyi Wan
发明人： Hubert B. Josien , John W. Clader , Andrew Stamford , William J. Greenlee , Michael John Mayer , Jason L. Davis , Ming Min Hsia , Shuangyi Wan
IPC分类号： A61K31/426 , A61P3/10 , A61P3/00 , C07D277/04
CPC分类号： C07D417/04 , C07D277/34
摘要： This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译：本发明提供了具有下式的某些五氟丁烷化合物或其药学上可接受的盐，酯，溶剂合物或前药，其中变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。

3. 发明申请

US20110312967A1 BRIDGED AND FUSED ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：桥接和融合的抗菌化合物
公开(公告)号：US20110312967A1
公开(公告)日：2011-12-22
申请号：US13145152
申请日：2010-01-21
申请人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Jason L. Davis , Shuangyi Wan
发明人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Jason L. Davis , Shuangyi Wan
IPC分类号： A61K31/501 , C07D417/12 , C07D263/44 , C07D417/04 , A61P3/10 , A61K31/426 , A61K31/421 , A61K31/427 , A61K31/4439 , C07D277/34 , C07D417/14
CPC分类号： C07D417/14 , C07D263/44 , C07D277/34 , C07D417/04 , C07D417/12
摘要： This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译：本发明提供了一些具有式G-L-A I的桥连和稠合化合物或其药学上可接受的盐，其溶剂合物的酯，其中：A是：（I），其它变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。

4. 发明申请

US20110257156A1 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：US20110257156A1
公开(公告)日：2011-10-20
申请号：US13126056
申请日：2009-11-05
申请人： Zhaoning Zhu , William J. Greenlee , David James Cole , Dmitri A. Pissarnitski , Gioconda V. Gallo , Hongmei Li , Hubert B. Josien , Jun Qin , Chad E. Knutson , Mihirbaran Mandal , Monica L. Vicarel , Murali Rajagopalan , Pawan Kumar Dhondi , Ruo Xu , Zhong-Yue Sun , Thomas A. Bara , Xianhai Huang , Xiaohong Zhu , Zhiqiang Zhao , John W. Clader , Anandan Palani , Theodros Asberom , Troy McCracken , Chad E. Bennett
发明人： Zhaoning Zhu , William J. Greenlee , David James Cole , Dmitri A. Pissarnitski , Gioconda V. Gallo , Hongmei Li , Hubert B. Josien , Jun Qin , Chad E. Knutson , Mihirbaran Mandal , Monica L. Vicarel , Murali Rajagopalan , Pawan Kumar Dhondi , Ruo Xu , Zhong-Yue Sun , Thomas A. Bara , Xianhai Huang , Xiaohong Zhu , Zhiqiang Zhao , John W. Clader , Anandan Palani , Theodros Asberom , Troy McCracken , Chad E. Bennett
IPC分类号： A61K31/55 , A61K31/5383 , A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/438 , A61K31/437 , C07D413/10 , C07D498/20 , C07D498/04 , A61P25/00 , A61P25/28 , A61K31/4245 , A61K31/5386
CPC分类号： C07D471/04 , C07D413/10 , C07D498/04 , C07D498/20 , C07F7/0812
摘要： In its many embodiments, the present invention provides novel heterocyclic compounds 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.
摘要翻译：在其许多实施方案中，本发明提供了新颖的杂环化合物作为γ-分泌酶的调节剂，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，制备包含一种或多种此类化合物的药物制剂的方法，以及治疗方法，使用这种化合物或药物组合物预防，抑制或改善与中枢神经系统相关的一种或多种疾病。

5. 发明申请

US20120004234A1 PHTHALAZINE-CONTAINING ANTIDIABETIC COMPOUNDS 失效
标题翻译：含PHARALAZ的含有抗菌药物
公开(公告)号：US20120004234A1
公开(公告)日：2012-01-05
申请号：US13146457
申请日：2010-02-04
申请人： Jason L. Davis , Michael John Mayer , Hubert B. Josien
发明人： Jason L. Davis , Michael John Mayer , Hubert B. Josien
IPC分类号： A61K31/502 , C07D417/14 , C07D487/04 , A61P3/00 , A61K31/5025 , A61P3/10 , A61P3/04 , C07D417/12 , A61K31/501
CPC分类号： C07D417/12 , C07D417/14 , C07D487/04
摘要： This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译：本发明提供了式（I）的某些含酞嗪化合物或其药学上可接受的盐，酯或溶剂化物，其中G是任选取代的含N-N杂芳基并且变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。

6. 发明授权

US08575166B2 Phthalazine-containing antidiabetic compounds 失效
标题翻译：含有酞嗪的抗糖尿病化合物
公开(公告)号：US08575166B2
公开(公告)日：2013-11-05
申请号：US13146457
申请日：2010-02-04
申请人： Jason L. Davis , Michael John Mayer , Hubert B. Josien
发明人： Jason L. Davis , Michael John Mayer , Hubert B. Josien
IPC分类号： A61K31/50 , A61K31/501 , C07D237/30
CPC分类号： C07D417/12 , C07D417/14 , C07D487/04
摘要： This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译：本发明提供了式（I）的某些含酞嗪化合物或其药学上可接受的盐，酯或溶剂化物，其中G是任选取代的含N-N杂芳基并且变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。

7. 发明授权

US08569521B2 Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 有权
标题翻译：苯磺酰基 - 苯并二氢吡喃，二氢苯并噻喃，四氢萘和相关的γ分泌酶抑制剂
公开(公告)号：US08569521B2
公开(公告)日：2013-10-29
申请号：US13267324
申请日：2011-10-06
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Anne Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Anne Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： C07D493/00
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译：本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。环烷基环或杂环烷基环可任选被一个或多个取代基取代。一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如，治疗阿尔茨海默病。

8. 发明申请

US20080188485A1 PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS 有权
标题翻译：哌啶衍生物作为CCR5拮抗剂有用
公开(公告)号：US20080188485A1
公开(公告)日：2008-08-07
申请号：US12055900
申请日：2008-03-26
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31/496 , A61P1/00 , A61P19/02
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroarylalkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; 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 is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯甲基或任选取代的苯基或杂芳基烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗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，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

9. 发明授权

US07256186B2 Gamma secretase inhibitors 失效
标题翻译： γ分泌酶抑制剂
公开(公告)号：US07256186B2
公开(公告)日：2007-08-14
申请号：US10941440
申请日：2004-09-15
申请人： Dimitri A. Pissarntiski , Hubert B. Josien , Elizabeth M. Smith , John W. Clader , Theodros Asberom , Tao Guo , Douglas W. Hobbs
发明人： Dimitri A. Pissarntiski , Hubert B. Josien , Elizabeth M. Smith , John W. Clader , Theodros Asberom , Tao Guo , Douglas W. Hobbs
IPC分类号： C07D211/08 , C07D207/46 , C07D205/00 , C07D279/00 , A01N43/00
CPC分类号： C07D401/14 , C07D211/96 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/10 , C07D491/10
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
摘要翻译：本发明公开了下式的新型γ分泌酶抑制剂：其中：R 1是取代的芳基或取代的杂芳基; R 2是R 1基团，烷基，-XC（O）Y，亚烷基-XC（O）Y，亚环烷基-XC（O）-Y，-CH -XC（O）-NR 3 -Y或-CH-XC（O）-Y，其中X和Y如本文所定义; 每个R 3和R 3各自独立地为H或烷基; R 11是芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。还公开了使用一种或多种本发明化合物治疗阿尔茨海默病的方法。

10. 发明授权

US08759337B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08759337B2
公开(公告)日：2014-06-24
申请号：US13140987
申请日：2009-12-18
申请人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John W. Clader , Dmitri A. Pissarnitski , Hubert B. Josien , Hongmei Li
发明人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John W. Clader , Dmitri A. Pissarnitski , Hubert B. Josien , Hongmei Li
IPC分类号： A61K31/553 , C07D498/04
CPC分类号： C07D498/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
摘要翻译：本发明提供了作为γ分泌酶调节剂的新型化合物。这些化合物具有式（化学式应该插在这里，如纸上所示）。还公开了使用式（I）化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

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