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1.发明申请
公开(公告)号：WO2010002428A3
公开(公告)日：2010-03-11
申请号：PCT/US2009003411
申请日：2009-06-05
Applicant: SCYNEXIS INC , LI KEQIANG , MAMAI AHMED , PEEL MICHAEL ROBERT
Inventor： LI KEQIANG , MAMAI AHMED , PEEL MICHAEL ROBERT
CPC classification number: C07K7/645
Abstract: Disclosed are cyclosporine derivatives in which the 3-Sarcosine carbon and 5-Valine nitrogen are each substituted by a non-hydrogen substituent, and their use as pharmaceuticals, in particular for the treatment of hepatitis C virus.
Abstract translation: 公开了其中3-肌氨酸碳和5-缬氨酸氮各自被非氢取代基取代的环孢菌素衍生物，以及它们作为药物的用途，特别是用于治疗丙型肝炎病毒。
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公开(公告)号：WO0248148A3
公开(公告)日：2003-05-01
申请号：PCT/US0144231
申请日：2001-11-26
Applicant: GLAXO GROUP LTD , BOYD F LESLIE , CHAMBERLAIN STANLEY D , CHEUNG MUI , GUDMUNDSSON KRISTJAN , HARRIS PHILIP ANTHONY , JOHNS BRIAN A , JUNG DAVID KENDALL , PEEL MICHAEL ROBERT , STANFORD JENNIFER BADIANG , SEXTON CONNIE JO
Inventor： BOYD F LESLIE , CHAMBERLAIN STANLEY D , CHEUNG MUI , GUDMUNDSSON KRISTJAN , HARRIS PHILIP ANTHONY , JOHNS BRIAN A , JUNG DAVID KENDALL , PEEL MICHAEL ROBERT , STANFORD JENNIFER BADIANG , SEXTON CONNIE JO
IPC: A61K31/437 , A61K31/522 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/14 , A61P1/16 , A61P3/02 , A61P9/10 , A61P11/00 , A61P13/12 , A61P25/00 , A61P25/02 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P29/02 , A61P31/12 , A61P31/22 , A61P35/00 , C07D471/04
CPC classification number: C07D471/04
Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
Abstract translation: 本发明提供式（I）化合物：含有该化合物的药物组合物，其制备方法及其作为药剂的用途。
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公开(公告)号：WO2010104933A1
公开(公告)日：2010-09-16
申请号：PCT/US2010/026796
申请日：2010-03-10
Applicant: MERCK SHARP & DOHME CORP. , BANYU PHARMACEUTICAL CO., LTD. , FAN, Weiming , HAXELL, Thomas, F. N. , JENKS, Matthew, G. , KAWANISHI, Nobuhiko , LEE, Shuliang , LIU, Hao , MALASKA, Michael, J. , MOORE, Joseph, A., III , OGINO, Yoshio , ONOZAKI, Yu , PANDI, Bharathi , PEEL, Michael, R. , SAKAMOTO, Toshihiro , SIU, Tony
Inventor： FAN, Weiming , HAXELL, Thomas, F. N. , JENKS, Matthew, G. , KAWANISHI, Nobuhiko , LEE, Shuliang , LIU, Hao , MALASKA, Michael, J. , MOORE, Joseph, A., III , OGINO, Yoshio , ONOZAKI, Yu , PANDI, Bharathi , PEEL, Michael, R. , SAKAMOTO, Toshihiro , SIU, Tony
IPC: C07D403/00 , C07D413/00
CPC classification number: C07D471/14 , C07D487/14 , C07D519/00
Abstract: The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Abstract translation: 本发明提供抑制Akt活性的取代的稠合萘啶衍生物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：WO2007008942A2
公开(公告)日：2007-01-18
申请号：PCT/US2006/026976
申请日：2006-07-11
Applicant: AERIE PHARMACEUTICALS, INC. , DELONG, Mitchell, A. , SZNAIDMAN, Marcos, L. , OAKLEY, Robert, H. , ECKHARDT, Allen, E. , HUDSON, Christine , YINGLING, Jeffrey, D. , PEEL, Michael , RICHARDSON, Thomas, E. , MURRAY, Claire, Louise , RAO, Byappanahally, N. Narasinga , HEASLEY, Brian, H. , PATEL, Paresma, R.
Inventor： DELONG, Mitchell, A. , SZNAIDMAN, Marcos, L. , OAKLEY, Robert, H. , ECKHARDT, Allen, E. , HUDSON, Christine , YINGLING, Jeffrey, D. , PEEL, Michael , RICHARDSON, Thomas, E. , MURRAY, Claire, Louise , RAO, Byappanahally, N. Narasinga , HEASLEY, Brian, H. , PATEL, Paresma, R.
CPC classification number: C07D401/12 , C07D213/53 , C07D213/61 , C07D213/75 , C07D215/12 , C07D215/42 , C07D233/64 , C07D239/52 , C07D239/54 , C07D307/14 , C07D307/52 , C07D333/22 , C07D401/14
Abstract: Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
Abstract translation: 提供具有GPCR脱敏抑制活性的酰肼化合物，其可用于影响，抑制或降低G蛋白受体激酶的作用。 还提供包含治疗有效量的酰肼化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响受GPCR控制或影响的疾病状态或病症的各种方法。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。
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公开(公告)号：WO2004032882A3
公开(公告)日：2004-07-08
申请号：PCT/US0333317
申请日：2003-10-10
Applicant: SMITHKLINE BEECHAM CORP , BROWN MATTHEW LEE , CHEUNG MUI , DICKERSON SCOTT HOWARD , GAUTHIER CASSANDRA , HARRIS PHILIP ANTHONY , HUNTER ROBERT NEIL III , PACOFSKY GREGORY , PEEL MICHAEL ROBERT , STAFFORD JEFFREY ALAN
Inventor： BROWN MATTHEW LEE , CHEUNG MUI , DICKERSON SCOTT HOWARD , GAUTHIER CASSANDRA , HARRIS PHILIP ANTHONY , HUNTER ROBERT NEIL III , PACOFSKY GREGORY , PEEL MICHAEL ROBERT , STAFFORD JEFFREY ALAN
IPC: A61K20060101 , A61K31/421 , A61K31/422 , C07D263/30 , C07D263/48 , C07D413/02 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12
CPC classification number: C07D263/48 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12
Abstract: Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
Abstract translation: 本文描述了用作VEGFR2，CDK2和CDK4抑制剂的恶唑衍生物。 所描述的本发明还包括制备这种恶唑衍生物的方法以及使用它们治疗过度增殖性疾病的方法。
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Patent Agency Ranking
公开(公告)号：WO2010076329A1
公开(公告)日：2010-07-08
申请号：PCT/EP2009/068017
申请日：2009-12-30
Applicant: SCYNEXIS, INC. , LI, Kequiang , HOUCK, David Renwick , OGBU, Cyprian Okwara , PEEL, Michael Robert , SCRIBNER, Andrew William
Inventor： LI, Kequiang , HOUCK, David Renwick , OGBU, Cyprian Okwara , PEEL, Michael Robert , SCRIBNER, Andrew William
Abstract: Disclosed herein are compounds of general formula (I) wherein A, B, R 1 and R 2 are as defined in the specification, and their use as pharmaceuticals.
Abstract translation: 本文公开了通式（I）的化合物，其中A，B，R 1和R 2如说明书中所定义，及其作为药物的用途。
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公开(公告)号：WO2010002428A2
公开(公告)日：2010-01-07
申请号：PCT/US2009/003411
申请日：2009-06-05
Applicant: SCYNEXIS, INC. , LI, Keqiang , MAMAI, Ahmed , PEEL, Michael, Robert
Inventor： LI, Keqiang , MAMAI, Ahmed , PEEL, Michael, Robert
CPC classification number: C07K7/645
Abstract: Disclosed are cyclosporine derivatives in which the 3-Sarcosine carbon and 5-Valine nitrogen are each substituted by a non-hydrogen substituent, and their use as pharmaceuticals, in particular for the treatment of hepatitis C virus.
Abstract translation: 公开了其中3-肌氨酸碳和5-缬氨酸氮各自被非氢取代基取代的环孢菌素衍生物，以及它们作为药物的用途，特别是用于治疗丙型肝炎病毒。
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公开(公告)号：WO2007127012B1
公开(公告)日：2008-02-21
申请号：PCT/US2007007856
申请日：2007-03-29
Applicant: MERCK & CO INC , SCYNEXIS INC , BALKOVEC JAMES M , BOUFFARD FRANCES AILEEN , TSE BRUNO , DROPINSKI JAMES , MENG DONGFANG , GREENLEE MARK L , PEEL MICHAEL , FAN WEIMING , MAMAI AHMED , LIU HAO , LI KEQAING
Inventor： BALKOVEC JAMES M , BOUFFARD FRANCES AILEEN , TSE BRUNO , DROPINSKI JAMES , MENG DONGFANG , GREENLEE MARK L , PEEL MICHAEL , FAN WEIMING , MAMAI AHMED , LIU HAO , LI KEQAING
CPC classification number: C07J71/0005
Abstract: The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (l,3)-ß-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.
Abstract translation: 本发明涉及式I的新型烯虫腈衍生物及其药学上可接受的盐，其合成及其作为（1,3）-β-D-葡聚糖合酶抑制剂的用途。 本发明化合物及其药学上可接受的盐，以及包含本发明化合物及其药学上可接受的盐的药物组合物可用于治疗或预防抗真菌感染和相关疾病和病症。
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公开(公告)号：WO2007127012A1
公开(公告)日：2007-11-08
申请号：PCT/US2007/007856
申请日：2007-03-29
Applicant: MERCK & CO., INC. , SCYNEXIS, INC. , BALKOVEC, James, M. , BOUFFARD, Frances, Aileen , TSE, Bruno , DROPINSKI, James , MENG, Dongfang , GREENLEE, Mark, L. , PEEL, Michael , FAN, Weiming , MAMAI, Ahmed , LIU, Hao , LI, Keqaing
Inventor： BALKOVEC, James, M. , BOUFFARD, Frances, Aileen , TSE, Bruno , DROPINSKI, James , MENG, Dongfang , GREENLEE, Mark, L. , PEEL, Michael , FAN, Weiming , MAMAI, Ahmed , LIU, Hao , LI, Keqaing
CPC classification number: C07J71/0005
Abstract: The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (l,3)-β-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.
Abstract translation: 本发明涉及式I的新型烯虫腈衍生物及其药学上可接受的盐，其合成及其作为（1,3）-β-D-葡聚糖合酶抑制剂的用途。 本发明化合物及其药学上可接受的盐以及包含本发明化合物及其药学上可接受的盐的药物组合物可用于治疗或预防抗真菌感染和相关疾病和病症。
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公开(公告)号：WO2007008926A1
公开(公告)日：2007-01-18
申请号：PCT/US2006/026947
申请日：2006-07-11
Applicant: AERIE PHARMACEUTICALS, INC. , DELONG, Mitchell, A. , SZNAIDMAN, Marcos, L. , OAKLEY, Robert, H. , ECKHARDT, Allen, E. , HUDSON, Christine , YINGLING, Jeffrey, D. , PEEL, Michael , RICHARDSON, Thomas, E. , MURRAY, Claire, Louise , RAO, Byappanahally N., Narasinga , HEASLEY, Brian, H. , PATEL, Paresma, R.
Inventor： DELONG, Mitchell, A. , SZNAIDMAN, Marcos, L. , OAKLEY, Robert, H. , ECKHARDT, Allen, E. , HUDSON, Christine , YINGLING, Jeffrey, D. , PEEL, Michael , RICHARDSON, Thomas, E. , MURRAY, Claire, Louise , RAO, Byappanahally N., Narasinga , HEASLEY, Brian, H. , PATEL, Paresma, R.
IPC: C07D217/02 , A61K31/472 , A61P27/06
CPC classification number: C07D217/02
Abstract: Isoquinoline compounds are provided that influence, inhibit or reduce the action of a G-protein receptor kinase . Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
Abstract translation: 提供了影响，抑制或降低G蛋白受体激酶作用的异喹啉化合物。 还提供包含治疗有效量的异喹啉化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。
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