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1. 发明申请

WO2007130626A3 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：WO2007130626A3
公开(公告)日：2008-01-17
申请号：PCT/US2007010924
申请日：2007-05-04
申请人： UNIV 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： A61K31/00
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。

2. 发明申请

WO2008128171A2 DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF 审中-公开
标题翻译： DIAZO BICYCLIC SMAC MIMETICS及其用途
公开(公告)号：WO2008128171A2
公开(公告)日：2008-10-23
申请号：PCT/US2008060215
申请日：2008-04-14
申请人： UNIV 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： G01N33/53
CPC分类号： G01N33/5011 , C07D487/04
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.
摘要翻译：本发明涉及Smac的重氮双环模拟物，其作为细胞凋亡蛋白抑制剂的抑制剂起作用。本发明还涉及这些模拟物用于诱导凋亡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

WO2005069894A8 CONFORMATIONALLY CONSTRAINED SMAC MIMETICS AND THE USES THEREOF 审中-公开
标题翻译：一致的约束SMAC的MIME类型及其用途
公开(公告)号：WO2005069894A8
公开(公告)日：2007-01-04
申请号：PCT/US2005001406
申请日：2005-01-18
申请人： UNIV 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 , C07K5/08 , C07K5/083
CPC分类号： C07K5/0806 , C07D487/04 , C07K5/0808 , C07K5/0827
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.
摘要翻译：本发明涉及Smac的构象约束模拟物，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。

4. 发明申请

WO2009126947A2 HETEROARYL-SUBSTITUTED BICYCLIC SMAC MIMETICS AND THE USES THEREOF 审中-公开
标题翻译：杂芳基取代的Bicyclic SMAC模拟物及其用途
公开(公告)号：WO2009126947A2
公开(公告)日：2009-10-15
申请号：PCT/US2009040312
申请日：2009-04-13
申请人： UNIV MICHIGAN , WANG SHAOMENG , SUN HAIYING , NIKOLOVSKA-COLESKA ZANETA
发明人： WANG SHAOMENG , SUN HAIYING , NIKOLOVSKA-COLESKA ZANETA
IPC分类号： C07D403/04 , C07D235/06 , C07D403/02
CPC分类号： C07D487/04
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.
摘要翻译：本发明涉及Smac的杂芳基取代的双环模拟物，其作为细胞凋亡蛋白抑制剂的抑制剂起作用。本发明还涉及这些模拟物用于诱导凋亡细胞死亡和使细胞对细胞凋亡诱导剂敏感的用途。

5. 发明申请

WO2011050068A2 BIVALENT DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF 审中-公开
标题翻译： BIVALENT DIAZO BICYCLIC SMAC MIMETICS及其用途
公开(公告)号：WO2011050068A2
公开(公告)日：2011-04-28
申请号：PCT/US2010053384
申请日：2010-10-20
申请人： UNIV MICHIGAN , WANG SHAOMENG , SUN HAIYING
发明人： WANG SHAOMENG , SUN HAIYING
IPC分类号： C07D487/04 , A61P35/00 , C07D245/04 , C07D403/14
CPC分类号： C07D519/00 , C07D487/04
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.
摘要翻译：本发明涉及重氮双环Smac模拟物，其通过共价连接物连接以产生二价物质。二价重氮双环Smac模拟物作为细胞凋亡蛋白抑制剂（IAP）的抑制剂起作用。本发明还涉及二价重氮双环Smac模拟物用于诱导或敏化细胞诱导凋亡细胞死亡的用途。因此，本发明化合物可用于治疗，改善或预防过度增殖性疾病如癌症。

6. 发明申请

WO2004022569A9 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：WO2004022569A9
公开(公告)日：2004-06-10
申请号：PCT/US0327607
申请日：2003-09-03
申请人： UNIV GEORGETOWN , US GOV HEALTH & HUMAN SERV , 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： A61K31/683 , A61K31/66 , A61P9/00 , A61P11/00 , A61P11/08 , A61P15/00 , A61P17/00 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/14 , A61P33/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07C43/196 , C07F9/02 , C07F9/117 , A61K31/185 , C07C59/13 , C07C59/68
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, CF2, CH2, and CHF; wherein A is independently selected from the group consisting of P(O)OH, CH2000H, and CH(COOH)2; R2 is selected from the group consisting of H, OH, isosteres of OH, C1-C25 alkyloxy, C6-Cl0 aryloxy, C3-C8 cycloalkyloxy, C3-C8 cycloalkyl C1-C6 alkoxy, C2-C22 alkenyloxy, C3-C8 cycloalkenyloxy, C7-C32 aralkyloxy, C7-C32 alkylaryloxy, C9-C32 aralkenyloxy, and C9-C32 alkenylaryloxy; R3-R6 are independently selected from the group consisting of H, OH, isosteres of OH; and Rl and R7 are independently selected from the group consisting of C1-C25 alkyl, C6-C10 aryl, C3-C8 cycloalkyl, C2-C22 alkenyl, C3-C8 cycloalkenyl, C7-C32 aralkyl, C7-C32 alkylaryl, C9-C32 aralkenyl, and C9-C32 alkenylaryl; with the provisos that (i) when X is O, Y is O or CH2, and R3 is H, at least one of R2 and R4-R6 is not OH; (ii) when A is CH2C00H or CH(COOH)2, X and Y cannot be simultaneously O; and (iii) all of R2-R6 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，包含此类抑制剂的药物组合物，以及通过使用这些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独立地选自由P（O）OH，CH2000H和CH（COOH）2组成的组; R2选自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烯氧基，C 3 -C 8环烯氧基， C7-C32芳烷氧基，C7-C32烷基芳氧基，C9-C32芳烯氧基和C9-C32烯基芳氧基; R3-R6独立地选自H，OH，OH的电子等排体; 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是O时，Y是O或CH 2，且R 3是H，R 2和R 4 -R 6中的至少一个不是OH; （ii）当A是CH2C00H或CH（COOH）2时，X和Y不能同时为O; 和（iii）R2-R6全部不同时为H.抑制剂也可以是盐的形式。

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