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1. 发明申请

WO2008128171A3 DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF 审中-公开
公开(公告)号：WO2008128171A3
公开(公告)日：2008-10-23
申请号：PCT/US2008/060215
申请日：2008-04-14
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , WANG, Shaomeng , PENG, Yuefeng , SUN, Haiying , CAI, Qian , NIKOLOVSKA-COLESKA, Zaneta , LU, Jianfeng , QIU, Su
发明人： WANG, Shaomeng , PENG, Yuefeng , SUN, Haiying , CAI, Qian , NIKOLOVSKA-COLESKA, Zaneta , LU, Jianfeng , QIU, Su
IPC分类号： A61K31/55 , A61P35/00 , C07D487/00
摘要： The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

2. 发明申请

WO2007130626A2 BIVALENT SMAC MIMETICS AND THE USES THEREOF 审中-公开
标题翻译：双重SMAC的MIME类型及其用途
公开(公告)号：WO2007130626A2
公开(公告)日：2007-11-15
申请号：PCT/US2007/010924
申请日：2007-05-04
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , WANG, Shaomeng , SUN, Haiying , QIN, Dongguang , NIKOLOVSKA-COLESKA, Zaneta , LU, Jianfeng , QIU, Su , PENG, Yuefeng , CAI, Qian
发明人： WANG, Shaomeng , SUN, Haiying , QIN, Dongguang , NIKOLOVSKA-COLESKA, Zaneta , LU, Jianfeng , QIU, Su , PENG, Yuefeng , CAI, Qian
IPC分类号： A61K31/43
CPC分类号： C07D519/00 , A61K38/191 , C07D487/04
摘要： The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
摘要翻译：本发明涉及Smac的二价模拟物，其作为细胞凋亡蛋白抑制剂的抑制剂。本发明还涉及这些模拟物用于诱导凋亡性细胞死亡和使细胞对细胞凋亡诱导剂敏感的用途。

3. 发明申请

WO2009126947A3 HETEROARYL-SUBSTITUTED BICYCLIC SMAC MIMETICS AND THE USES THEREOF 审中-公开
公开(公告)号：WO2009126947A3
公开(公告)日：2009-10-15
申请号：PCT/US2009/040312
申请日：2009-04-13
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , WANG, Shaomeng , SUN, Haiying , NIKOLOVSKA-COLESKA, Zaneta
发明人： WANG, Shaomeng , SUN, Haiying , NIKOLOVSKA-COLESKA, Zaneta
IPC分类号： C07D403/04 , C07D403/02 , C07D235/06
摘要： The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

4. 发明申请

WO2005069894A3 CONFORMATIONALLY CONSTRAINED SMAC MIMETICS AND THE USES THEREOF 审中-公开
公开(公告)号：WO2005069894A3
公开(公告)日：2005-08-04
申请号：PCT/US2005/001406
申请日：2005-01-18
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , WANG, Shaomeng , SUN, Haiying , NIKOLOVSKA-COLESKA, Zaneta , YANG, Chao-Yie , XU, Liang
发明人： WANG, Shaomeng , SUN, Haiying , NIKOLOVSKA-COLESKA, Zaneta , YANG, Chao-Yie , XU, Liang
IPC分类号： A61K31/395 , A61K31/407 , A61K31/4353 , A61K31/437 , A61K31/4375 , A61K31/55 , A61P35/00 , C07D455/02 , C07D471/04 , C07D487/04
摘要： The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

5. 发明申请

WO2011050068A3 BIVALENT DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF 审中-公开
公开(公告)号：WO2011050068A3
公开(公告)日：2011-04-28
申请号：PCT/US2010/053384
申请日：2010-10-20
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , WANG, Shaomeng , SUN, Haiying
发明人： WANG, Shaomeng , SUN, Haiying
IPC分类号： C07D487/04 , C07D403/14 , C07D245/04 , A61P35/00
摘要： The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.

6. 发明申请

WO2014031487A8 BIVALENT INHIBITORS OF IAP PROTEINS AND THERAPEUTIC METHODS USING THE SAME 审中-公开
公开(公告)号：WO2014031487A8
公开(公告)日：2014-02-27
申请号：PCT/US2013/055384
申请日：2013-08-16
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： WANG, Shaomeng , SHENG, Rong , SUN, Haiying , LIU, Liu , LU, Jianfeng , MCEACHERN, Donna
IPC分类号： C07D487/04 , A61K31/395 , A61P35/00
摘要： Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.

7. 发明申请

WO2004022569A1 AKT INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF 审中-公开
标题翻译： AKT抑制剂，药物组合物及其用途
公开(公告)号：WO2004022569A1
公开(公告)日：2004-03-18
申请号：PCT/US2003/027607
申请日：2003-09-03
申请人： GEORGETOWN UNIVERSITY , THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as representedby THE SECRETARY, DEPARTMENT OF HEALT H ANDHUMANSERVICES , KOZIKOWSKI, Alan, P. , DENNIS, Phillip , SUN, Haiying , BROGNARD, John
发明人： KOZIKOWSKI, Alan, P. , DENNIS, Phillip , SUN, Haiying , BROGNARD, John
IPC分类号： C07F9/117
CPC分类号： C07C43/196 , C07C2601/14 , C07F9/117
摘要： Disclosed are inhibitors of the serine/threonine kinase Akt, pharmaceutical compositions comprising such inhibitors, and a method of preventing or treating a disease or condition in an animal by the use of such inhibitors. The Akt inhibitors have the formula (I) wherein X and Y are independently selected from the group consisting of O, CF 2 , CH 2 , and CHF; wherein A is independently selected from the group consisting of P(O)OH, CH 2 000H, and CH(COOH) 2 ; R 2 is selected from the group consisting of H, OH, isosteres of OH, C 1 -C 25 alkyloxy, C 6 -C l0 aryloxy, C 3 -C 8 cycloalkyloxy, C 3 -C 8 cycloalkyl C 1 -C 6 alkoxy, C 2 -C 22 alkenyloxy, C 3 -C 8 cycloalkenyloxy, C 7 -C 32 aralkyloxy, C 7 -C 32 alkylaryloxy, C 9 -C 32 aralkenyloxy, and C 9 -C 32 alkenylaryloxy; R 3 -R 6 are independently selected from the group consisting of H, OH, isosteres of OH; and R l and R 7 are independently selected from the group consisting of C 1 -C 25 alkyl, C 6 -C 10 aryl, C 3 -C 8 cycloalkyl, C 2 -C 22 alkenyl, C 3 -C 8 cycloalkenyl, C 7 -C 32 aralkyl, C 7 -C 32 alkylaryl, C 9 -C 32 aralkenyl, and C 9 -C 32 alkenylaryl; with the provisos that (i) when X is O, Y is O or CH 2 , and R 3 is H, at least one of R 2 and R 4 -R 6 is not OH; (ii) when A is CH 2 C00H or CH(COOH) 2 , X and Y cannot be simultaneously O; and (iii) all of R 2 -R 6 are not simultaneously H. The inhibitors can be in the form of a salt also.
摘要翻译：公开了丝氨酸/苏氨酸激酶Akt的抑制剂，包含这种抑制剂的药物组合物，以及通过使用这种抑制剂预防或治疗动物的疾病或病症的方法。 Akt抑制剂具有式（I），其中X和Y独立地选自O，CF 2，CH 2和CHF; 其中A独立地选自P（O）OH，CH 2，000H和CH（COOH）2; R 2选自H，OH，OH，C 1 -C 25烷氧基，C 6 -C 10芳氧基，C 3 -C 8环烷氧基，C 3 -C 8环烷基C 1 -C 6烷氧基，C 2 -C 22链烯氧基，C 3 -C 8环烯基氧基， C7-C32芳烷氧基，C7-C32烷芳基氧基，C9-C32芳烯基氧基和C9-C32链烯基氧基; R 3 -R 6独立地选自H，OH，OH的异构体; 并且R 1和R 7独立地选自C 1 -C 25烷基，C 6 -C 10芳基，C 3 -C 8环烷基，C 2 -C 22烯基，C 3 -C 8环烯基，C 7 -C 32芳烷基，C 7 -C 32烷基芳基，C 9 -C 32 芳烯基和C 9 -C 32烯基芳基; 条件是（ⅰ）当X为O时，Y为O或CH2，R3为H，R2和R4-R6中的至少一个不为OH; （ii）当A为CH 2 COOH或CH（COOH）2时，X和Y不能同时为O; 和（iii）所有的R2-R6都不是同时的H.抑制剂也可以是盐的形式。

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