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公开(公告)号：WO2021154669A1
公开(公告)日：2021-08-05
申请号：PCT/US2021/014983
申请日：2021-01-26
发明人： HE, Liqi , GAVAI, Ashvinikumar V. , GANGWAR, Sanjeev , CONG, Qiang , POUDEL, Yam B. , SIVAPRAKASAM, Prasanna , TARBY, Christine M. , GILL, Patrice , DONNELL, Andrew F. , SUBBAIAH, Murugaiah Andappan Murugaiah
IPC分类号： C07D487/04 , A61P35/00 , A61K31/519
摘要： Compounds according to formula I or II are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.
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公开(公告)号：WO2021154665A1
公开(公告)日：2021-08-05
申请号：PCT/US2021/014979
申请日：2021-01-26
发明人： ZHANG, Qian , GANGWAR, Sanjeev , GAVAI, Ashvinikumar V. , CONG, Qiang , POUDEL, Yam B. , HE, Liqi , SIVAPRAKASAM, Prasanna , TARBY, Christine M.
IPC分类号： C07D487/04 , A61P35/00 , A61K31/519
摘要： Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.
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公开(公告)号：WO2019213340A1
公开(公告)日：2019-11-07
申请号：PCT/US2019/030310
申请日：2019-05-02
发明人： TARBY, Christine M. , NORRIS, Derek J. , LO, Julian C. , AHUJA, Vijay T. , SEITZ, Steven P. , GAVAI, Ashvinikumar V. , TOKARSKI, John S. , RAJASAGI, Mohini , WICHROSKI, Michael , BROEKEMA, Matthias
IPC分类号： C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , A61K31/513 , A61P35/00
摘要： The invention relates generally to compounds that are Mer-Axl inhibitors, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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公开(公告)号：WO2014047391A1
公开(公告)日：2014-03-27
申请号：PCT/US2013/060832
申请日：2013-09-20
IPC分类号： C07D243/18 , A61K31/55 , C07D243/26 , C07F9/09 , C07F9/12
CPC分类号： C07F9/645 , A61K31/5513 , A61K31/675 , A61K45/06 , C07D243/18 , C07D243/24 , C07D243/26 , C07D401/12 , C07F9/12 , A61K2300/00
摘要： Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R 1 is H or CH 3 , and R 2 is R y ; or b) R 1 is Rx and R 2 is H; wherein R x and R y are disclosed herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are prodrugs of compounds that are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
摘要翻译： 公开了式（I）的化合物及其盐，其中：a）R1是H或CH3，R2是Ry; 或b）R1是Rx，R2是H; 其中Rx和Ry在本文中公开。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物是可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症进展的化合物的前药。
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公开(公告)号：WO2007005631A1
公开(公告)日：2007-01-11
申请号：PCT/US2006/025632
申请日：2006-06-29
IPC分类号： C07D487/04 , A61K31/53 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to at least one pyrrolotriazine derivative of formula (I), at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.
摘要翻译： 本发明涉及式（I）的至少一种吡咯并三嗪衍生物，至少一种包含至少一种吡咯并三嗪衍生物的药物组合物和至少一种使用至少一种吡咯并三嗪衍生物以治疗至少一种激酶相关病症的方法。
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公开(公告)号：WO2005065266A3
公开(公告)日：2005-07-21
申请号：PCT/US2004/043282
申请日：2004-12-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , GAVAI, Ashvinikumar V. , HAN, Wen-Ching , CHEN, Ping , RUEDIGER, Edward H. , MASTALERZ, Harold , FINK, Brian E. , NORRIS, Derek J.
发明人： GAVAI, Ashvinikumar V. , HAN, Wen-Ching , CHEN, Ping , RUEDIGER, Edward H. , MASTALERZ, Harold , FINK, Brian E. , NORRIS, Derek J.
IPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
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公开(公告)号：WO2014134267A1
公开(公告)日：2014-09-04
申请号：PCT/US2014/018914
申请日：2014-02-27
发明人： POSS, Michael A. , TORTOLANI, David R. , PURANDARE, Ashok Vinayak , TOKARSKI, John S. , MUSSARI, Christopher P. , KAMAU, Muthoni G. , DODD, Dharmpal S. , GAVAI, Ashvinikumar V. , O'MALLEY, Daniel , HUYNH, Tram N. , VACCARO, Wayne , HARIKRISHNAN, Lalgudi S.
IPC分类号： C07D413/04 , A61K31/403 , A61P35/00
CPC分类号： C07D413/04 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61K31/553 , C07D413/10 , C07D413/14 , C07D417/14
摘要： The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
摘要翻译： 本发明涉及咔唑化合物，包含本发明化合物的药学上可接受的组合物以及使用所述组合物治疗各种疾病的方法。
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公开(公告)号：WO2014047392A1
公开(公告)日：2014-03-27
申请号：PCT/US2013/060833
申请日：2013-09-20
发明人： GAVAI, Ashvinikumar V. , SHAN, Weifang , BALOG, James Aaron , QUESNELLE, Claude A. , HAN, Wen-Ching , DELUCCA, George V. , O'MALLEY, Daniel , FINK, Brian E.
IPC分类号： C07D413/14 , C07D401/04 , C07D401/12 , C07D413/12 , C07D243/24 , C07D491/04 , A61K31/5513 , A61P35/00
CPC分类号： C07D243/24 , A61K31/5513 , A61K45/06 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14 , C07D491/04 , C07D491/056
摘要： Disclosed are compounds of Formula (I): wherein: R 2 is phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, or pyridinyl; R 3 is H, CH 3 , CH 2 (cyclopropyl), pyridinyl, chloropyridinyl, or methoxypyridinyl: and R a , R b , y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
摘要翻译： 公开了式（I）的化合物：其中：R 2是苯基，氟苯基，氯苯基，三氟苯基，甲基异恶唑基或吡啶基; R 3是H，CH 3，CH 2（环丙基），吡啶基，氯吡啶基或甲氧基吡啶基：和R a，R b，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。
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9.发明申请BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AS NOTCH INHIBITORS 审中-公开BIS（氟代烷基）-1,4-苯并嗪酮化合物作为止动抑制剂
公开(公告)号：WO2014047372A1
公开(公告)日：2014-03-27
申请号：PCT/US2013/060790
申请日：2013-09-20
发明人： GAVAI, Ashvinikumar V. , DELUCCA, George V. , O'MALLEY, Daniel , GILL, Patrice , QUESNELLE, Claude A. , FINK, Brian E. , ZHAO, Yufen , LEE, Francis Y.
IPC分类号： C07D401/04 , C07D243/18 , C07D243/26 , C07F9/38 , A61K31/55
CPC分类号： C07D243/24 , A61K9/0019 , A61K9/0095 , A61K9/08 , A61K9/4866 , A61K31/138 , A61K31/337 , A61K31/506 , A61K31/5513 , A61K31/555 , A61K31/573 , A61K31/675 , A61K45/06 , A61K47/64 , C07D243/18 , C07D243/26 , C07D401/04 , C07F7/1852 , C07F9/12 , C07F9/38 , C07F9/645 , A61K2300/00
摘要： Disclosed are compounds of Formula (I) and/or salts thereof: (I) wherein R 1 is CH 2 CH 2 CF 3 ; R 2 is CH 2 CH 2 CF 3 or CH 2 CH 2 CH 2 CF 3 ; R 3 is H, CH 3 , or R x ; R 4 is H or R y ; Ring A is phenyl or pyridinyl; and R x , R y , R a , R b , y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
摘要翻译： 公开了式（I）和/或其盐的化合物：（I）其中R 1是CH 2 CH 2 CF 3; R2是CH2CH2CF3或CH2CH2CH2CF3; R3是H，CH3或Rx; R4是H或Ry; 环A是苯基或吡啶基; 并且Rx，Ry，Ra，Rb，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展; 或作为这些化合物的前药。
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公开(公告)号：WO2014047369A1
公开(公告)日：2014-03-27
申请号：PCT/US2013/060781
申请日：2013-09-20
IPC分类号： C07D401/04 , C07D243/24 , A61K31/5513 , A61P35/00
CPC分类号： C07D243/14 , A61K31/5513 , A61K45/06 , C07D243/24 , C07D401/04
摘要： Disclosed are compounds of Formula (I): wherein: R 1 is CH 2 CH 2 CF 3 ; R 2 is CH 2 CH 2 CF 3 , CH 2 (cyclopropyl), or phenyl; R 3 is H or CH 3 ; Ring A is phenyl or pyridinyl; and R x , R y , R a , R b , y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
摘要翻译： 公开了式（I）的化合物：其中：R1是CH2CH2CF3; R 2是CH 2 CH 2 CF 3，CH 2（环丙基）或苯基; R3是H或CH3; 环A是苯基或吡啶基; 并且Rx，Ry，Ra，Rb，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。
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