专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US08907095B2 Bicyclic heterocycle derivatives and their use as modulators of the activity of GPR119 有权
标题翻译：双环杂环衍生物及其作为GPR119活性调节剂的用途
公开(公告)号：US08907095B2
公开(公告)日：2014-12-09
申请号：US12739531
申请日：2008-10-20
申请人： Yan Xia , Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil , Charles Lee Jayne
发明人： Yan Xia , Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil , Charles Lee Jayne
IPC分类号： C07D221/02 , A61K31/439 , C07D451/14 , C07D491/08 , C07D495/08 , C07D471/08 , C07D451/06 , C07D487/08 , C07D401/14 , C07D498/08
CPC分类号： C07D451/06 , A61K31/439 , C07D401/14 , C07D451/14 , C07D471/08 , C07D487/08 , C07D491/08 , C07D495/08 , C07D498/08
摘要： The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
摘要翻译：本发明涉及双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖症，糖尿病，代谢紊乱，心血管疾病或与GPR119活性相关的病症的方法患者。

12. 发明授权

US07304078B2 Thrombin receptor antagonists 有权
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US07304078B2
公开(公告)日：2007-12-04
申请号：US10412982
申请日：2003-04-14
申请人： Samuel Chackalamannil , William J. Greenlee , Yuguang Wang , Wenxue Wu , Enrico P. Veltri , Yan Xia
发明人： Samuel Chackalamannil , William J. Greenlee , Yuguang Wang , Wenxue Wu , Enrico P. Veltri , Yan Xia
IPC分类号： A61K31/443 , C07D405/02
CPC分类号： C07D405/06 , C07D405/14 , C07D417/14
摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond; n is 0–2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1–C6)alkyl, (C3–C8)cycloalkyl, —OH, (C1–C6)alkoxy, R27-aryl(C1–C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3–6 atoms; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：式中的杂环取代三环

13. 发明授权

US06916811B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US06916811B2
公开(公告)日：2005-07-12
申请号：US10304931
申请日：2002-11-26
申请人： Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Unmesh G. Shah , Yan Xia
发明人： Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Unmesh G. Shah , Yan Xia
IPC分类号： A61K31/519 , A61K31/55 , A61K45/00 , A61P9/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P43/00 , C07D487/14 , C07D487/04 , A61P25/18 , C07D519/00
CPC分类号： C07D487/14
摘要： Disclosed herein are compounds having the structural formula A including pharmaceutically acceptable salts or solvates of said compound, wherein X, Y, Q and R are as defined in the specification; pharmaceutical compositions thereof; methods of treating central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment, and processes for preparing the compound of this invention.
摘要翻译：本文公开的是具有结构式A的化合物，包括所述化合物的药学上可接受的盐或溶剂合物，其中X，Y，Q和R如说明书中所定义; 其药物组合物; 通过将本发明化合物给予需要这种治疗的患者来治疗中枢神经系统疾病的方法，以及制备本发明化合物的方法。

14. 发明授权

US06897216B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US06897216B2
公开(公告)日：2005-05-24
申请号：US10448854
申请日：2003-05-30
申请人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
发明人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
IPC分类号： A61K31/505 , A61K31/519 , A61P25/08 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D487/14
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，环烯基或杂芳基; X是亚烷基或-C（O）CH 2 - 。 Y是-N（R 2）CH 2 CH 2，N（R 3） - ， - OCH 2， N 2 - （CH 2） - ， - O - ， - S - ， - CH 2 S- ， - （CH 2）2 -NH-或任选取代的m和n为2-3，Q为氮或任选取代的碳; 和Z是任选取代的苯基，苯基烷基或杂芳基，二苯基甲基，R 6 -C（O） - ，R 6 -SO 2 - ， - R 0 -OC（O） - ，R 7 -N（R 8）-C（O） - ，R 7 -N（R 8）-C（S） - ，苯基-CH（OH） - 或苯基-C（-NOR 2） - ; 或当Q为CH时，苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基或取代的苯基; 和R 2，R 3，R 6，R 7和R 8和/或在说明书中定义的它们在治疗帕金森病中的用途，单独使用或与治疗帕金森病的其它药物组合，以及包含它们的药物组合物; 还公开了制备可用于制备式I化合物的中间体的方法。

15. 再颁专利

USRE44205E1 Adenosine A2a receptor antagonists 有权
公开(公告)号：USRE44205E1
公开(公告)日：2013-05-07
申请号：US13441140
申请日：2012-04-06
申请人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
发明人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
IPC分类号： C07D471/04 , C07D471/22 , C07D487/04
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.

16. 发明申请

US20110212938A1 BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS MODULATORS OF THE ACTIVITY OF GPR119 有权
标题翻译：双相异构体衍生物及其作为GPR119活性调节剂的用途
公开(公告)号：US20110212938A1
公开(公告)日：2011-09-01
申请号：US12739531
申请日：2008-10-20
申请人： Yan Xia , Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil , Charles Lee Jayne
发明人： Yan Xia , Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil , Charles Lee Jayne
IPC分类号： A61K31/506 , C07D471/08 , C07D401/14 , C07D491/08 , C07D471/12 , C07D498/08 , A61K31/537 , C07D487/08 , C07D495/08 , A61P3/04 , A61P3/10
CPC分类号： C07D451/06 , A61K31/439 , C07D401/14 , C07D451/14 , C07D471/08 , C07D487/08 , C07D491/08 , C07D495/08 , C07D498/08
摘要： The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
摘要翻译：本发明涉及双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖症，糖尿病，代谢紊乱，心血管疾病或与GPR119活性相关的病症的方法患者。

17. 发明授权

US06630475B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US06630475B2
公开(公告)日：2003-10-07
申请号：US09865071
申请日：2001-05-24
申请人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
发明人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
IPC分类号： C07D40314
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，环烯基或杂芳基; X是亚烷基或-C（O）CH 2 - ; Y是-N（R 2）CH 2 CH 2 N（R） 3） - ，-OCH 2 CH 2 N（R 2） - ， - O - ， - S - ， - CH 2 S - ， - （CH 2）2 -NH-或任选地被取代的n和n是2-3，并且Q是氮或任选取代的碳; 和Z是任选取代的苯基，苯基烷基或杂芳基，二苯基甲基，R 6 -C（O） - ，R 6 -SO 2 - ，R 6 -OC（O） - ，R 7 -N C（O） - ，R 7 -N（R 8）-C（S） - ，苯基-CH（OH） - 或苯基-C（= NOR 2） ; 或当Q为CH时，为苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基或取代的苯基; 和R 2，R 3，R 6，R 7和R 8如说明书中所定义，其用于治疗帕金森病，单独使用或与其它药剂组合用于治疗帕金森病，以及包含它们的药物组合物; 还公开了制备可用于制备式I化合物的中间体的方法。

18. 发明授权

US08778980B2 Heterocyclic aspartyl protease inhibitors 有权
公开(公告)号：US08778980B2
公开(公告)日：2014-07-15
申请号：US13551315
申请日：2012-07-17
申请人： Zhaoning Zhu , Brian A McKittrick , Zhong-Yue Sun , Yuanzan C Ye , Johannes H Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
发明人： Zhaoning Zhu , Brian A McKittrick , Zhong-Yue Sun , Yuanzan C Ye , Johannes H Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
IPC分类号： A01N43/82 , A61K31/41 , C07D271/06
CPC分类号： C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

19. 发明授权

US08426403B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08426403B2
公开(公告)日：2013-04-23
申请号：US12601322
申请日：2008-05-28
申请人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Brian A. McKittrick , John W. Clader , Mark D. McBriar , Anandan Palani
发明人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Brian A. McKittrick , John W. Clader , Mark D. McBriar , Anandan Palani
IPC分类号： A61K31/5365 , A61K31/5395 , C07D498/04 , A61P25/28
CPC分类号： C07D498/04 , C07D403/10 , C07D471/04 , C07D487/04
摘要： 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.
摘要翻译：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。

20. 发明申请

US20110218194A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 有权
公开(公告)号：US20110218194A1
公开(公告)日：2011-09-08
申请号：US13108454
申请日：2011-05-16
申请人： Zhaoning Zhu , Brian A. Mckittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachel C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
发明人： Zhaoning Zhu , Brian A. Mckittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachel C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
IPC分类号： A61K31/5395 , C07D273/04 , C07D413/10 , A61P9/00 , A61P33/02 , A61P31/10 , A61P25/28 , A61P25/00
CPC分类号： C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式