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21.
公开(公告)号:US20040030132A1
公开(公告)日:2004-02-12
申请号:US10285073
申请日:2002-10-31
发明人: Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Harter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jorg Keldenich , Ulf Brueggemeier , Klemens Lustig
IPC分类号: C07D417/02 , C07D413/02
CPC分类号: C07D213/40 , C07C237/36 , C07C271/22 , C07C275/42 , C07C311/06 , C07C311/09 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/43 , C07C311/47 , C07C317/14 , C07C323/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/34 , C07D213/38 , C07D213/55 , C07D213/74 , C07D213/75 , C07D213/82 , C07D231/18 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/30 , C07D235/32 , C07D261/10 , C07D263/58 , C07D277/42 , C07D277/54 , C07D277/82 , C07D285/10 , C07D285/135 , C07D285/14 , C07D295/096 , C07D295/13 , C07D295/15 , C07D295/215 , C07D307/52 , C07D333/34 , C07D333/48 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) 1 wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
摘要翻译: 本发明涉及联苯和联苯类似物,其作为药物组合物的制备和用途,作为整联蛋白拮抗剂,特别涉及用于治疗和预防癌症,动脉硬化,再狭窄,溶骨性疾病如骨质疏松和 眼科疾病 根据本发明的化合物具有式(1)其中R 1,R 2,U,V,A,B,W,R 3,C和R 4具有如 索赔。
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22.
公开(公告)号:US20030191319A1
公开(公告)日:2003-10-09
申请号:US10157019
申请日:2002-05-30
申请人: G.D. Searle & Co.
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
IPC分类号: C07D213/24 , C07D207/46 , C07C311/47
CPC分类号: C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/42 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D217/26 , C07D233/64 , C07D239/26 , C07D241/18 , C07D241/44 , C07D263/34 , C07D277/24 , C07D277/62 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D307/85 , C07D317/62 , C07D333/32 , C07D333/34 , C07D333/48 , C07D405/12 , C07D417/12 , C07D493/04 , C07K5/06026 , C07K5/06139
摘要: null- and null-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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公开(公告)号:US20030144328A1
公开(公告)日:2003-07-31
申请号:US10218445
申请日:2002-08-15
发明人: Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Susan Ashwell , Dimitrios Sarantakis , Gregory S. Welmaker , Anthony Kreft , Christopher Semko , Robert Warren Sulliva , Christopher Joseph Soares , Kiev Sui Ly , Christine M. Tarby
IPC分类号: A61K031/426 , A61K031/421 , A61K031/4168 , A61K031/235 , A61K031/19
CPC分类号: A61K31/425 , A61K31/41 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/54 , C07D211/58 , C07D213/74 , C07D213/76 , C07D233/88 , C07D239/32 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/52 , C07D241/20 , C07D249/06 , C07D251/18 , C07D251/48 , C07D251/50 , C07D251/52 , C07D251/54 , C07D257/06 , C07D285/06 , C07D285/10 , C07D333/36 , C07D333/48 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , Y02A50/463 , A61K2300/00
摘要: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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24.
公开(公告)号:US20030125324A1
公开(公告)日:2003-07-03
申请号:US10218366
申请日:2002-08-15
发明人: Andrei W. Konradi , Michael A. Pleiss , Eugene D. Thorsett , Susan Ashwell , Gregory S. Welmaker , Anthony Kreft , Dimitrios Sarantakis , Darren B. Dressen , Francine S. Grant , Christopher Semko , Ying-Zi Xu
IPC分类号: A61K031/535 , A61K031/54 , A61K031/445 , A61K031/496 , A61K031/427 , A61K031/425
CPC分类号: A61K31/425 , A61K31/41 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/54 , C07D211/58 , C07D213/74 , C07D213/76 , C07D233/88 , C07D239/32 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/52 , C07D241/20 , C07D249/06 , C07D251/18 , C07D251/48 , C07D251/50 , C07D251/52 , C07D251/54 , C07D257/06 , C07D285/06 , C07D285/10 , C07D333/36 , C07D333/48 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , Y02A50/463 , A61K2300/00
摘要: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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25.
公开(公告)号:US06541475B2
公开(公告)日:2003-04-01
申请号:US09833834
申请日:2001-04-12
IPC分类号: A61K31495
CPC分类号: C07D207/333 , C07C317/10 , C07D213/34 , C07D277/36 , C07D307/10 , C07D333/18 , C07D333/42 , C07D333/48
摘要: &agr;, &bgr;-Unsaturated sulfones of the following formulae are provided, which are useful as antiproliferative agents, including, for example, anticancer agents:
摘要翻译: 提供下式的α,β-不饱和砜,其可用作抗增殖剂,包括例如抗癌剂:
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公开(公告)号:US20020147234A1
公开(公告)日:2002-10-10
申请号:US10108513
申请日:2002-03-29
发明人: Gregory R.J. Thatcher , Brian M. Bennett , James N. Reynolds , Roland J. Boegman , Khem Jhamandas
IPC分类号: A61K031/21
CPC分类号: C07D307/33 , A61K31/21 , A61K31/255 , A61K31/26 , A61K31/275 , A61K31/341 , A61K31/381 , A61K31/39 , A61K31/426 , A61K31/506 , A61K31/575 , A61K31/662 , A61K31/7068 , C07C203/04 , C07C255/14 , C07C317/18 , C07C323/12 , C07C327/28 , C07C331/10 , C07C381/02 , C07D277/24 , C07D327/04 , C07D333/48 , C07D339/08 , C07D411/04 , C07F9/091 , C07F9/4006 , C07J41/0061
摘要: Compounds and methods for mitigating neurodegeneration, effecting neuroprotection and/or effecting cognition enhancement in a subject are described. Neurological or cognitive conditions are treated by administering to a subject an effective amount of a therapeutic compound comprising a nitrate ester, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译: 描述了用于减轻神经变性,影响神经保护和/或影响受试者的认知增强的化合物和方法。 通过向受试者施用有效量的包含硝酸酯或其药学上可接受的盐或酯的治疗化合物来治疗神经或认知状况。
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公开(公告)号:US06365579B2
公开(公告)日:2002-04-02
申请号:US09851591
申请日:2001-05-10
申请人: Gregory R. J. Thatcher , Brian M. Bennett , James N. Reynolds , Roland J. Boegman , Khem Jhamandas
发明人: Gregory R. J. Thatcher , Brian M. Bennett , James N. Reynolds , Roland J. Boegman , Khem Jhamandas
IPC分类号: A61K31255
CPC分类号: C07D307/33 , A61K31/21 , A61K31/255 , A61K31/26 , A61K31/275 , A61K31/341 , A61K31/381 , A61K31/39 , A61K31/426 , A61K31/506 , A61K31/575 , A61K31/662 , A61K31/7068 , C07C203/04 , C07C255/14 , C07C317/18 , C07C323/12 , C07C327/28 , C07C331/10 , C07C381/02 , C07D277/24 , C07D327/04 , C07D333/48 , C07D339/08 , C07D411/04 , C07F9/091 , C07F9/4006 , C07J41/0061
摘要: Compounds and methods for mitigating neurodegeneration, effecting neuroprotection and/or effecting cognition enhancement in a subject are described. Neurological or cognitive conditions are treated by administering to a subject an effective amount of a therapeutic compound comprising a nitrate ester, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译: 描述了用于减轻神经变性,影响神经保护和/或影响受试者的认知增强的化合物和方法。 通过向受试者施用有效量的包含硝酸酯或其药学上可接受的盐或酯的治疗化合物来治疗神经或认知状况。
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公开(公告)号:US06265583B1
公开(公告)日:2001-07-24
申请号:US09177100
申请日:1998-10-22
申请人: Deborah E. Bertenshaw , Daniel Getman , Robert M. Heintz , John J. Talley , Kathryn L. Reed , Robert Alan Chrusciel , Michael Clare
发明人: Deborah E. Bertenshaw , Daniel Getman , Robert M. Heintz , John J. Talley , Kathryn L. Reed , Robert Alan Chrusciel , Michael Clare
IPC分类号: C07D28506
CPC分类号: C07D333/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D279/12 , C07D335/02 , C07D409/12
摘要: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
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29.
公开(公告)号:US06248775B1
公开(公告)日:2001-06-19
申请号:US09288080
申请日:1999-04-08
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
IPC分类号: A61K3138
CPC分类号: C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/42 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D217/26 , C07D233/64 , C07D239/26 , C07D241/18 , C07D241/44 , C07D263/34 , C07D277/24 , C07D277/62 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D307/85 , C07D317/62 , C07D333/32 , C07D333/34 , C07D333/48 , C07D405/12 , C07D417/12 , C07D493/04 , C07K5/06026 , C07K5/06139
摘要: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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公开(公告)号:US6127372A
公开(公告)日:2000-10-03
申请号:US424372
申请日:1996-04-01
申请人: Roger Dennis Tung , Francesco Gerald Salituro , David D. Deininger , Mark Andrew Murcko , Perry Michael Novak , Govinda Rao Bhisetti
发明人: Roger Dennis Tung , Francesco Gerald Salituro , David D. Deininger , Mark Andrew Murcko , Perry Michael Novak , Govinda Rao Bhisetti
IPC分类号: A61K31/18 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/495 , A61P31/12 , A61P43/00 , C07C311/16 , C07C311/29 , C07C311/37 , C07C311/41 , C07C311/51 , C07D211/60 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/70 , C07D213/81 , C07D213/82 , C07D217/24 , C07D217/26 , C07D231/38 , C07D233/54 , C07D233/76 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D235/28 , C07D241/04 , C07D249/18 , C07D261/08 , C07D263/22 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/06 , C07D277/20 , C07D277/26 , C07D277/36 , C07D277/44 , C07D277/46 , C07D307/10 , C07D307/20 , C07D307/33 , C07D309/08 , C07D309/10 , C07D317/18 , C07D317/34 , C07D319/06 , C07D333/36 , C07D333/38 , C07D333/48 , C07D335/02 , C07D401/06 , C07D487/04 , C07D493/04 , C07D521/00 , A61K31/351 , A61K31/381 , A61K31/4192
CPC分类号: C07D213/30 , C07C311/29 , C07C311/41 , C07D211/60 , C07D213/70 , C07D213/81 , C07D213/82 , C07D217/24 , C07D217/26 , C07D231/38 , C07D233/54 , C07D233/64 , C07D233/76 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D235/28 , C07D241/04 , C07D249/18 , C07D261/08 , C07D263/22 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/06 , C07D277/26 , C07D277/36 , C07D277/46 , C07D307/10 , C07D307/20 , C07D309/08 , C07D309/10 , C07D317/18 , C07D317/34 , C07D319/06 , C07D333/36 , C07D333/38 , C07D333/48 , C07D335/02 , C07D401/06 , C07D493/04 , C07C2101/08
摘要: This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: ##STR1## This invention also provides pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
摘要翻译: PCT No.PCT / US95 / 02420 Sec。 371日期:1996年4月1日 102(e)日期1996年4月1日PCT提交1995年2月24日PCT公布。 WO95 / 24385 PCT公开号 日期1995年9月14日本发明提供了一类新颖的式I的磺酰胺化合物,其为天冬氨酰蛋白酶抑制剂:本发明还提供包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性,因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还提供了使用本发明的化合物和组合物来抑制天冬氨酰蛋白酶活性的方法和用于治疗病毒感染的方法。
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