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1. 发明申请

US20140243284A1 BIOLOGICALLY ACTIVE MACROLIDES, COMPOSITIONS, AND USES THEREOF 审中-公开
标题翻译：生物活性成分，组合物及其用途
公开(公告)号：US20140243284A1
公开(公告)日：2014-08-28
申请号：US14275336
申请日：2014-05-12
申请人： The United States of America, as represented by the Secretary, Department of Health and Human Serv
发明人： Michael R. Boyd , Kirk R. Gustafson , Charles L. Cantrell
IPC分类号： C07D498/06 , A61K31/7048 , A61K31/395
CPC分类号： A61K31/395 , A61K31/365 , A61K31/7048 , C07D498/06 , C07D498/08
摘要： The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(═O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(═O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.
摘要翻译：本发明提供式（I）或（II）的化合物，其中R 1为H，烷基，烯基或芳基，R 2为H，烷基或芳基，R 3为H，烷基，烯基或芳基，R 4和R 4 -R 8独立地是R 10，C（O）R 10或SO 2 R 10，其中R 10是H，烷基，烯基或芳基，R 9是R 9a，C（O）R 9a或SO 2 R 9a，其中R 9a是H，烷基，烯基或芳基。 R9a可以是未取代的或被一个或多个氧代（= O），OR 9 b，OC（O）R 9b，OSO 2 R 9 b，NHR 9 b，NHC（O）R 9b和NHSO 2 R 9 b基团取代。 R9b是H，烷基，烯基或芳基。 R9b可以是未取代的或被一个或多个基团取代，例如氧代（= O），OR 9c，CO 2 R 9c，CO 2 R 9c和OC（O）R 9c。 R9c是H或未取代或取代的烷基，烯基或芳基。本发明还提供包含至少一种本发明化合物和药学上可接受的载体的组合物，其单独或与至少一种另外的活性剂组合。本发明还提供了通过抑制液泡型（H +）-ATP酶处理可治疗的病症的方法和治疗癌症的方法。

2. 发明申请

US20150374661A1 BIOLOGICALLY ACTIVE MACROLIDES, COMPOSITIONS, AND USES THEREOF 有权
标题翻译：生物活性成分，组合物及其用途
公开(公告)号：US20150374661A1
公开(公告)日：2015-12-31
申请号：US14849798
申请日：2015-09-10
申请人： The United States of America, as represented by the Secretary, Department of Health and Human Serv
发明人： Michael R. Boyd , Kirk R. Gustafson , Charles L. Cantrell
IPC分类号： A61K31/395 , A61K31/7048 , A61K31/365
CPC分类号： A61K31/395 , A61K31/365 , A61K31/7048 , C07D498/06 , C07D498/08
摘要： The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(═O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(═O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.
摘要翻译：本发明提供式（I）或（II）的化合物，其中R 1为H，烷基，烯基或芳基，R 2为H，烷基或芳基，R 3为H，烷基，烯基或芳基，R 4和R 4 -R 8独立地是R 10，C（O）R 10或SO 2 R 10，其中R 10是H，烷基，烯基或芳基，R 9是R 9a，C（O）R 9a或SO 2 R 9a，其中R 9a是H，烷基，烯基或芳基。 R9a可以是未取代的或被一个或多个氧代（= O），OR 9 b，OC（O）R 9b，OSO 2 R 9 b，NHR 9 b，NHC（O）R 9b和NHSO 2 R 9 b基团取代。 R9b是H，烷基，烯基或芳基。 R9b可以是未取代的或被一个或多个基团取代，例如氧代（= O），OR 9c，CO 2 R 9c，CO 2 R 9c和OC（O）R 9c。 R9c是H或未取代或取代的烷基，烯基或芳基。本发明还提供包含至少一种本发明化合物和药学上可接受的载体的组合物，其单独或与至少一种另外的活性剂组合。本发明还提供了通过抑制液泡型（H +）-ATP酶处理可治疗的病症的方法和治疗癌症的方法。

3. 发明申请

US20180093995A1 HYPOXIA-INDUCIBLE FACTOR 1 (HIF-1) INHIBITORS 审中-公开
公开(公告)号：US20180093995A1
公开(公告)日：2018-04-05
申请号：US15563851
申请日：2016-04-06
申请人： The United States of America, as represented by the Secretary, Department of Health and Human Serv
发明人： Kirk R. Gustafson , Martin J. Schnermann , Susanna T. S. Chan , Paresma R. Patel , William D. Figg , James B. McMahon
IPC分类号： C07D487/16 , A61K31/519 , A61K45/06
CPC分类号： C07D487/16 , A61K31/519 , A61K45/06 , Y02A50/411
摘要： Embodiments of small molecule inhibitors of hypoxia inducible factor 1 (HIF-1) and pharmaceutical compositions thereof are disclosed. The disclosed compounds suppress HIF-1 activity by inhibiting the interaction between the HIF-1 a subunit and transcriptional co-activator protein p300. Embodiments of methods for making and using the small molecule inhibitors are also disclosed.

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