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公开(公告)号：US6147078A
公开(公告)日：2000-11-14
申请号：US315195
申请日：1999-05-19
IPC分类号： C07D241/20 , C07D401/12 , A61K31/497
CPC分类号： C07D401/12 , C07D241/20
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein ##STR2##
摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓闭塞：其中
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公开(公告)号：US5527819A
公开(公告)日：1996-06-18
申请号：US488957
申请日：1995-06-07
申请人： Theresa M. Williams , Terrence M. Ciccarone , Walfred S. Saari , John S. Wai , William J. Greenlee , Suresh K. Balani , Mark E. Goldman , Anthony D. Theoharides, deceased , Jacob M. Hoffman, Jr. , William C. Lumma, Jr. , Joel R. Huff , Clarence S. Rooney , Philip E. Sanderson
发明人： Theresa M. Williams , Terrence M. Ciccarone , Walfred S. Saari , John S. Wai , William J. Greenlee , Suresh K. Balani , Mark E. Goldman , Anthony D. Theoharides, deceased , Jacob M. Hoffman, Jr. , William C. Lumma, Jr. , Joel R. Huff , Clarence S. Rooney , Philip E. Sanderson
IPC分类号： C07D209/12 , C07D209/30 , C07D209/42 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/12 , C07D521/00 , A61K31/40
CPC分类号： C07D231/12 , C07D209/12 , C07D209/30 , C07D209/42 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/12
摘要： Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 新型吲哚化合物抑制HIV逆转录酶，可用于预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物结合使用，抗感染药物 ，免疫调节剂，抗生素或疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号：US06376499B1
公开(公告)日：2002-04-23
申请号：US09428314
申请日：1999-10-28
IPC分类号： A61K31497
CPC分类号： C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D471/04
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is N Y1 or O; c is CY2 or N; d is CY2; e is CY1 or N; f is CY1 or N; g is CY1 or N; Y1 is hydrogen, C1-4 alkyl, or halogen; Y2 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy; A is and W, X, Z, R3, R4 and R5 are defined in the specification.
摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓形成闭塞：或其药学上可接受的盐，其中b为N Y1或O; c为CY2或N; d为CY2; e是CY1或N; f是CY1或N; g为CY1或N; Y1是氢，C1-4烷基或卤素; Y 2是氢，C 1-4烷基，C 3-7环烷基，卤素，NH 2，OH或C 1-4烷氧基; A是且W，X，Z，R 3，R 4和R 5在本说明书中定义。
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公开(公告)号：US06610692B1
公开(公告)日：2003-08-26
申请号：US09429741
申请日：1999-10-28
申请人： Philip E. Sanderson , Bruce D. Dorsey , Terry A. Lyle , Matthew G. Stanton , Donnette Staas , Adel M. Naylor-Olsen , Craig Coburn , Matthew M. Morrissette
发明人： Philip E. Sanderson , Bruce D. Dorsey , Terry A. Lyle , Matthew G. Stanton , Donnette Staas , Adel M. Naylor-Olsen , Craig Coburn , Matthew M. Morrissette
IPC分类号： A61K31497
CPC分类号： C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/14 , C07D471/04
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2 or N; d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y4, Y5, and Y6 are independently hydrogen, C1-4 alkyl, or halogen; Y1 and Y2 are independently hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y3 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, —CN, NH2, OH or C1-4 alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.
摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓形成闭塞：或其药学上可接受的盐，其中b为NY或O; c为CY2或N; d为CY3或N; e为CY4或N; f是CY5或N; g为CY6或N; Y4，Y5和Y6独立地是氢，C1-4烷基或卤素; Y1和Y2独立地是氢，C1-4烷基，C3-7环烷基，卤素，NH2，OH或C1-4烷氧基，Y3是氢，C1-4烷基，C3-7环烷基，卤素，-CN，NH2， OH或C 1-4烷氧基; A和W，W 1，R 1，R 3，R 4，R 5，X和Z在说明书中定义。
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公开(公告)号：US20110288090A1
公开(公告)日：2011-11-24
申请号：US13147392
申请日：2010-01-25
申请人： Donna J. Armstrong , Yasuhiro Goto , Takashi Hashihayata , Tetsuya Kato , Michael J. Kelly, III , Mark E. Layton , Craig W. Lindsley , Yoshio Ogino , Yu Onozaki , Kenvin J. Rodzinak , Michael A. Rossi , Philip E. Sanderson , Jiabing Wang , Melissa M. Yaroschak
发明人： Donna J. Armstrong , Yasuhiro Goto , Takashi Hashihayata , Tetsuya Kato , Michael J. Kelly, III , Mark E. Layton , Craig W. Lindsley , Yoshio Ogino , Yu Onozaki , Kenvin J. Rodzinak , Michael A. Rossi , Philip E. Sanderson , Jiabing Wang , Melissa M. Yaroschak
IPC分类号： A61K31/5377 , A61K31/4985 , A61K31/496 , A61K31/506 , A61K31/498 , A61K31/438 , A61K31/4375 , C07D475/04 , C07D471/04 , C07D401/12 , A61P35/00 , A61K31/519
CPC分类号： C07D471/04 , C07D217/24 , C07D241/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D475/02 , C07D475/04 , C07D487/04 , C07D519/00
摘要： The instant invention provides for compounds 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.
摘要翻译： 本发明提供抑制Akt活性的化合物。 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：US08008317B2
公开(公告)日：2011-08-30
申请号：US11921352
申请日：2006-06-07
申请人： Donna J. Armstrong , Essa H. Hu , Michael J. Kelly, III , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Michael J. Rossi , Philip E. Sanderson , Jiabing Wang
发明人： Donna J. Armstrong , Essa H. Hu , Michael J. Kelly, III , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Michael J. Rossi , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/437 , A61K31/4375 , C07D471/14 , C07D471/16
CPC分类号： C07D471/14 , C07D487/14
摘要： The instant invention provides for substituted naphthyridine compounds 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.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 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：US06455532B1
公开(公告)日：2002-09-24
申请号：US09585112
申请日：2000-06-01
申请人： Christopher S. Burgey , Kyle A. Robinson , Peter D. Williams , Craig Coburn , Terry A. Lyle , Philip E. Sanderson
发明人： Christopher S. Burgey , Kyle A. Robinson , Peter D. Williams , Craig Coburn , Terry A. Lyle , Philip E. Sanderson
IPC分类号： A61K31497
CPC分类号： C07D401/12 , A61K31/495 , C07D401/14 , A61K31/00 , A61K2300/00
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: A is wherein Y1 and Y2 are independently hydrogen, C1-4 alkyl, C1-4 alkoxy, FuHvC(CH2)0-1 O—, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C3-7 cycloalkyl, thio C1-4 alkyl, C1-4 sulfinylalkyl, C1-4 sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.
摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓闭塞：A是其中Y1和Y2独立地是氢，C1-4烷基，C1-4烷氧基，FuHvC（CH2）0-1 O-，其中u和 v为1或2，条件是当u为1时，v为2，当u为2时，v为1，C 3-7环烷基，硫代C 1-4烷基，C 1-4亚磺酰基烷基，C 1-4磺酰基烷基，卤素基 ，三氟甲基，其中b为0或1。
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公开(公告)号：US6011038A
公开(公告)日：2000-01-04
申请号：US146650
申请日：1998-09-03
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , A61K31/495 , C07D403/12 , C07D413/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## for example: ##STR2##
摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓闭塞：例如：
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公开(公告)号：US20170197968A1
公开(公告)日：2017-07-13
申请号：US15326262
申请日：2015-07-14
申请人： Arthur LEE , John C. MCKEW , Paresma R. PATEL , Paul B. YU , Agustin H. MOHEADS , Philip E. SANDERSON , Wei ZHENG , Xiuli HUANG , THE BRIGHAM AND WOMEN'S HOSPITLAL, INC. , THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN , UNIVERSITY OF HOUSTON SYSTEM
发明人： Arthur Lee , John C. McKew , Paresma R. Patel , Paul B. Yu , Agustin H. Mohedas , Philip E. Sanderson , Gregory D. Cuny , Wei Zheng , Xiuli Huang
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides small-molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.
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公开(公告)号：US08168652B2
公开(公告)日：2012-05-01
申请号：US13255757
申请日：2010-03-03
IPC分类号： A61K31/44 , C07D471/02
CPC分类号： A61K31/4375 , C07D471/04
摘要： The instant invention provides for substituted naphthyridine compounds 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.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 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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