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公开(公告)号：US5945413A
公开(公告)日：1999-08-31
申请号：US724563
申请日：1996-09-30
申请人： Roger Dennis Tung , Francesco Gerald Salituro , David D. Deininger , Govinda Rao Bhisetti , Christopher Todd Baker , Andrew Spaltenstein
发明人： Roger Dennis Tung , Francesco Gerald Salituro , David D. Deininger , Govinda Rao Bhisetti , Christopher Todd Baker , Andrew Spaltenstein
IPC分类号： C07D207/26 , C07D207/27 , C07D233/36 , C07D265/32 , C07D265/34 , C07D285/10 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D491/10 , A61K41/315 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/425 , A61K31/43 , A61K31/44 , A61K31/47
CPC分类号： C07D207/27 , C07D233/36 , C07D265/32 , C07D265/34 , C07D285/10 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D491/10
摘要： This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to 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 relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
摘要翻译： 本发明涉及一类新颖的天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特异性结构和物理化学特征为特征的新型天冬氨酰蛋白酶抑制剂。 本发明还涉及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。 本发明还涉及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治疗病毒感染的方法。
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公开(公告)号：US5883252A
公开(公告)日：1999-03-16
申请号：US592777
申请日：1996-01-26
申请人： Roger Dennis Tung , Francesco Gerald Salituro , David D. Deininger , Govinda Rao Bhisetti , Christopher Todd Baker
发明人： Roger Dennis Tung , Francesco Gerald Salituro , David D. Deininger , Govinda Rao Bhisetti , Christopher Todd Baker
IPC分类号： C07D207/26 , C07D207/27 , C07D233/36 , C07D265/32 , C07D265/34 , C07D285/10 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D491/10 , C07D307/20 , C07D211/60 , C07D241/04 , C07D277/06 , C07D319/06 , C07D493/04
CPC分类号： C07D207/27 , C07D233/36 , C07D265/32 , C07D265/34 , C07D285/10 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D491/10
摘要： This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to 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 relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
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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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公开(公告)号：US20090203702A1
公开(公告)日：2009-08-13
申请号：US12062495
申请日：2008-04-03
申请人： Guy W. Bemis , Francesco Gerald Salituro , John Patrick Duffy , John E. Cochran , Edmund Martin Harrington , Mark A. Murcko , Keith P. Wilson , Michael Su , Vincent P. Galullo
发明人： Guy W. Bemis , Francesco Gerald Salituro , John Patrick Duffy , John E. Cochran , Edmund Martin Harrington , Mark A. Murcko , Keith P. Wilson , Michael Su , Vincent P. Galullo
IPC分类号： A61K31/5025 , C07D487/04 , C07D471/04 , A61K31/519 , A61P29/00 , A61P37/00 , A61P25/00
CPC分类号： C07D213/70 , C07D213/56 , C07D213/75 , C07D237/18 , C07D241/12 , C07D241/20 , C07D401/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07F9/6561
摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
摘要翻译： 本发明涉及p38的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。
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公开(公告)号：US5945418A
公开(公告)日：1999-08-31
申请号：US822373
申请日：1997-03-20
IPC分类号： C07D213/56 , C07D213/70 , C07D213/75 , C07D237/18 , C07D241/12 , C07D241/20 , C07D401/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07F9/6561 , A01N43/58 , C07D237/26 , C07D487/00
CPC分类号： C07D213/56 , C07D213/70 , C07D213/75 , C07D237/18 , C07D241/12 , C07D241/20 , C07D401/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07F9/6561
摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
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公开(公告)号：US20140187435A1
公开(公告)日：2014-07-03
申请号：US13939519
申请日：2013-07-11
申请人： Leonard Luan C. Dang , Valeria Fantin , Stefan Gross , Hyun Gyung Jang , Shengfang Jin , Francesco Gerald Salituro , Jeffrey Owen Saunders , Shin-San Michael Su , Katharine Yen
发明人： Leonard Luan C. Dang , Valeria Fantin , Stefan Gross , Hyun Gyung Jang , Shengfang Jin , Francesco Gerald Salituro , Jeffrey Owen Saunders , Shin-San Michael Su , Katharine Yen
CPC分类号： A61B5/055 , A61K31/41 , A61K31/426 , A61K45/06 , C12N15/1137 , C12N2310/14 , C12Q1/32 , C12Q1/6886 , C12Y101/01042 , G01N33/574 , G06F19/328 , Y02A90/24 , Y02A90/26 , A61K2300/00
摘要： Methods of treating and evaluating subjects having neoactive mutants are described herein.
摘要翻译： 本文描述了治疗和评估具有新生突变体的受试者的方法。
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公开(公告)号：US6147080A
公开(公告)日：2000-11-14
申请号：US862925
申请日：1997-06-10
IPC分类号： A61K31/4375 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/519 , A61K31/5377 , A61P7/02 , A61P9/10 , A61P19/08 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07D213/56 , C07D213/61 , C07D213/70 , C07D213/75 , C07D237/18 , C07D241/12 , C07D241/20 , C07D401/04 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07F9/6561
CPC分类号： C07D213/70 , C07D213/56 , C07D213/75 , C07D237/18 , C07D241/12 , C07D241/20 , C07D401/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07F9/6561
摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The compounds are of the class of pyrido [1,2-c] pyrimidin-3-one or 1,2-dihydro-pyrido [1,2-c] pyrimidin-3-one derivatives, useful as inhibitors of p38. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
摘要翻译： 本发明涉及p38的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应。 该化合物是可用作p38抑制剂的吡啶并[1,2-c]嘧啶-3-酮或1,2-二氢 - 吡啶并[1,2-c]嘧啶-3-酮衍生物。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。
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公开(公告)号：US20110281878A1
公开(公告)日：2011-11-17
申请号：US13107802
申请日：2011-05-13
申请人： Guy W. Bemis , Francesco Gerald Salituro , John Patrick Duffy , John E. Cochran , Edmund Martin Harrington , Mark A. Murko , Keith P. Wilson , Michael Su , Vincent P. Galullo
发明人： Guy W. Bemis , Francesco Gerald Salituro , John Patrick Duffy , John E. Cochran , Edmund Martin Harrington , Mark A. Murko , Keith P. Wilson , Michael Su , Vincent P. Galullo
IPC分类号： A61K31/5025 , C07D471/04 , A61K31/519 , A61P29/00 , A61P37/00 , A61P31/12 , A61P19/08 , A61P35/00 , A61P31/00 , A61P25/28 , A61P37/08 , A61P9/10 , A61P13/12 , A61P7/00 , A61P43/00 , A61P9/00 , A61P7/02 , A61P1/18 , A61P11/06 , A61P11/00 , A61P19/04 , A61P17/00 , A61P5/14 , A61P3/10 , A61P7/06 , A61P31/14 , A61P21/04 , A61P1/00 , A61P1/04 , A61P17/06 , A61P37/06 , A61P19/02 , A61P19/10 , A61P35/02 , A61P35/04 , C07D487/04
CPC分类号： C07D213/70 , C07D213/56 , C07D213/75 , C07D237/18 , C07D241/12 , C07D241/20 , C07D401/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07F9/6561
摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
摘要翻译： 本发明涉及p38的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。
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公开(公告)号：US6093742A
公开(公告)日：2000-07-25
申请号：US884160
申请日：1997-06-27
IPC分类号： C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C311/47 , C07D209/08 , C07D213/75 , C07D215/40 , C07D231/56 , C07D277/64 , C07D277/82 , C07D295/135 , C07D307/91 , C07D317/66 , C07D319/18 , A61K31/17
CPC分类号： C07D319/18 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C311/47 , C07D209/08 , C07D213/75 , C07D215/40 , C07D231/56 , C07D277/64 , C07D277/82 , C07D295/135 , C07D307/91 , C07D317/66 , C07C2102/08
摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
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公开(公告)号：US06608060B1
公开(公告)日：2003-08-19
申请号：US09336266
申请日：1999-06-14
申请人： Guy W. Bemis , Francesco Gerald Salituro , John Patrick Duffy , John E. Cochran , Edmund Martin Harrington , Mark A. Murko , Keith P. Wilson , Michael Su , Vincent P. Galullo
发明人： Guy W. Bemis , Francesco Gerald Salituro , John Patrick Duffy , John E. Cochran , Edmund Martin Harrington , Mark A. Murko , Keith P. Wilson , Michael Su , Vincent P. Galullo
IPC分类号： C07D48704
CPC分类号： C07D213/70 , C07D213/56 , C07D213/75 , C07D237/18 , C07D241/12 , C07D241/20 , C07D401/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07F9/6561
摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
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