专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1996033187A1 OXYGENATED-HETEROCYCLE CONTAINING SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE 审中-公开
标题翻译：含有ASPARTYL PROTEASE的磺酰胺抑制剂的含氧杂环化合物
公开(公告)号：WO1996033187A1
公开(公告)日：1996-10-24
申请号：PCT/US1996005473
申请日：1996-04-18
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： VERTEX PHARMACEUTICALS INCORPORATED , TUNG, Roger, D. , BHISETTI, Govinda, Rao
IPC分类号： C07D319/06
CPC分类号： C07D493/04 , C07D307/20 , C07D309/12 , C07D317/24 , C07D317/34 , C07D317/36 , C07D319/06
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. 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 the activity of HIV aspartyl protease using the compounds of this invention.
摘要翻译：本发明涉及一类新型的磺酰胺，它们是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化合物抑制HIV天冬氨酰蛋白酶活性的方法。

2. 发明申请

WO1996033184A1 THF-CONTAINING SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE 审中-公开
标题翻译：含有THF的磺酰胺抑制剂的ASPARTYL PROTEASE
公开(公告)号：WO1996033184A1
公开(公告)日：1996-10-24
申请号：PCT/US1996005475
申请日：1996-04-18
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： VERTEX PHARMACEUTICALS INCORPORATED , TUNG, Roger, D.
IPC分类号： C07D307/20
CPC分类号： C07D213/30 , A61K38/00 , C07D207/26 , C07D209/08 , C07D215/48 , C07D231/12 , C07D231/14 , C07D233/56 , C07D239/22 , C07D249/08 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06139
摘要： The present invention relates to a class of THF-containing sulfonamides which are aspartyl protease inhibitors. 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 the activity of HIV aspartyl protease using the compounds of this invention.
摘要翻译：本发明涉及一类含有THF的磺酰胺，它们是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化合物抑制HIV天冬氨酰蛋白酶活性的方法。

3. 发明申请

WO2004078733A1 QUINAZOLINES USEFUL AS MODULATORS OF ION CHANNELS 审中-公开
标题翻译：喹诺酮作为离子通道的调节剂有用
公开(公告)号：WO2004078733A1
公开(公告)日：2004-09-16
申请号：PCT/US2004/006451
申请日：2004-03-03
申请人： VERTEX PHARMACEUTICALS INCORPORATED , GONZALES, Jesus, E., III , WILSON, Dean, Mitchell , TERMIN, Andreas, Peter , GROOTENHUIS, Peter, Diederik, Jan , ZHANG, Yulian , PETZOLDT, Benjamin, John , FANNING, Lev, Tyler, Dewey , NEUBERT, Timothy, Donald , TUNG, Roger, D. , MARTINBOROUGH, Esther , ZIMMERMANN, Nicole
发明人： GONZALES, Jesus, E., III , WILSON, Dean, Mitchell , TERMIN, Andreas, Peter , GROOTENHUIS, Peter, Diederik, Jan , ZHANG, Yulian , PETZOLDT, Benjamin, John , FANNING, Lev, Tyler, Dewey , NEUBERT, Timothy, Donald , TUNG, Roger, D. , MARTINBOROUGH, Esther , ZIMMERMANN, Nicole
IPC分类号： C07D239/94
CPC分类号： C07D239/94 , C07D239/91 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to quinazoline compounds of formula (I) useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. or a pharmaceutically acceptable derivative thereof, wherein R 1 , X, R 3 , x, and ring A are as defined in the present application.
摘要翻译：本发明涉及可用作电压门控钠通道和钙通道抑制剂的式（I）喹唑啉化合物。本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。或其药学上可接受的衍生物，其中R 1，X，R 3，x和环A如本申请中所定义。

4. 发明申请

WO1997012855A1 BUTYRATE PRODRUGS OF LACTIC ACID 审中-公开
标题翻译：苦味酸乳酸菌（BUTYRATE PRODRUGS OF LACTIC ACID）
公开(公告)号：WO1997012855A1
公开(公告)日：1997-04-10
申请号：PCT/US1996015660
申请日：1996-09-30
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： VERTEX PHARMACEUTICALS INCORPORATED , TUNG, Roger, D. , LI, Biqin
IPC分类号： C07C69/68
CPC分类号： C07C69/68 , A61K31/22
摘要： This invention relates to butyrate prodrugs derived from lactic acid and pharmaceutical compositions and methods employing them, either alone or in combination with other agents, for increasing gamma globin and fetal hemoglobin in a patient. These compounds, compositions and methods are particularly effective in treating beta -hemoglobinopathies, including sickle cell syndromes and beta -thalassemia syndromes. In addition, this invention relates to the use of these prodrugs, alone or in combination with other agents, to stimulate cell differentiation which prevents proliferation of malignant cells. These methods are particularly useful in treating cancer, especially malignant hematological disorders.
摘要翻译：本发明涉及衍生自乳酸的丁酸酯前药以及使用它们的药物组合物和方法，单独或与其它试剂组合，用于增加患者中的γ珠蛋白和胎儿血红蛋白。这些化合物，组合物和方法在治疗β-血红蛋白病，包括镰状细胞综合征和β-地贫综合征中特别有效。此外，本发明涉及这些前药单独使用或与其它试剂组合来刺激细胞分化，其可防止恶性细胞的增殖。这些方法特别适用于治疗癌症，特别是恶性血液病。

5. 发明申请

WO2002100405A1 ISOQUINOLINE INHIBITORS OF P38 审中-公开
标题翻译： P38的异喹啉抑制剂
公开(公告)号：WO2002100405A1
公开(公告)日：2002-12-19
申请号：PCT/US2002/021130
申请日：2002-06-11
申请人： VERTEX PHARMACEUTICALS INCORPORATED , COCHRAN, John, E. , TUNG, Roger, D.
发明人： COCHRAN, John, E. , TUNG, Roger, D.
IPC分类号： A61K31/472
CPC分类号： C07D217/12 , C07D217/18 , C07D217/22
摘要： The present invention relates to inhibitors (ia)-(id) 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. All substituents are as in claim 1.
摘要翻译：本发明涉及p38的抑制剂（ia） - （id），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。所有取代基如权利要求1所述。

6. 发明申请

WO1992000278A1 NOVEL IMMUNOSUPPRESSIVE COMPOUNDS 审中-公开
标题翻译：新型免疫抑制剂
公开(公告)号：WO1992000278A1
公开(公告)日：1992-01-09
申请号：PCT/US1991004694
申请日：1991-07-02
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： VERTEX PHARMACEUTICALS INCORPORATED , ARMISTEAD, David, M. , BOGER, Joshua, S. , MEYERS, Harold, V. , SAUNDERS, Jeffrey, O. , TUNG, Roger, D.
IPC分类号： C07D211/60
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

7. 发明申请

WO2004108133A2 MODULATORS OF VR1 RECEPTOR 审中-公开
标题翻译： VR1受体的调节剂
公开(公告)号：WO2004108133A2
公开(公告)日：2004-12-16
申请号：PCT/US2004/017779
申请日：2004-06-04
申请人： VERTEX PHARMACEUTICALS INCORPORATED , MAKINGS, Lewis, R. , GROOTENHUIS, Peter , HURLEY, Dennis, James , TUNG, Roger, D. , TERMIN, Andreas, P.
发明人： MAKINGS, Lewis, R. , GROOTENHUIS, Peter , HURLEY, Dennis, James , TUNG, Roger, D. , TERMIN, Andreas, P.
IPC分类号： A61K31/4184
CPC分类号： A61K31/497 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/501 , A61K31/506 , C07D231/56 , C07D235/06 , C07D235/26 , C07D241/44 , C07D263/58 , C07D277/68 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to compounds useful as modulators of the vanilloid receptor, and also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译：本发明涉及可用作香草素受体调节剂的化合物，并且还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。

8. 发明申请

WO1992016501A1 TETRAHYDROXYALKANE DERIVATIVES AS INHIBITORS OF HIV ASPARTYL PROTEASE 审中-公开
标题翻译：作为HIV ASPARTYL PROTEASE的抑制剂的四氢羟基酮衍生物
公开(公告)号：WO1992016501A1
公开(公告)日：1992-10-01
申请号：PCT/US1992002290
申请日：1992-03-20
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： VERTEX PHARMACEUTICALS INCORPORATED , TUNG, Roger, D. , DEININGER, David, D.
IPC分类号： C07C271/22
CPC分类号： C07D295/215 , C07C233/83 , C07C235/12 , C07C255/57 , C07C271/22 , C07C2601/10 , C07D209/42 , C07D213/55 , C07D213/56 , C07D215/48 , C07D217/26 , C07D239/38 , C07D241/44 , C07D307/68 , C07D307/85 , C07D317/24 , C07D317/68
摘要： This invention relates to a novel class of glycolic compounds which contain a linear backbone having four contiguous oxygen-substituted methine carbons. The compounds of this invention inhibit the ability of aspartyl protease from HIV to catalyze the hydrolysis of peptides. These novel compounds can be used to reduce production of infectious virions from chronically infected cells and can inhibit the further infection of host cells. As such, they are useful as therapeutic agents to treat acquired immunodefiency syndrom (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia, and non-symptomatic HIV infection.
摘要翻译：本发明涉及一类含有具有四个相邻的氧取代的次甲基碳的直链骨架的乙醇酸化合物。本发明的化合物抑制HIV的天冬氨酰蛋白酶催化肽水解的能力。这些新型化合物可用于减少长期感染细胞感染性病毒粒子的产生，并可抑制宿主细胞的进一步感染。因此，它们可用作治疗获得性免疫缺陷综合征（AIDS）以及AIDS相关综合征（ARC），AIDS相关性痴呆和无症状性HIV感染的治疗剂。

9. 发明申请

WO1992004370A1 MODIFIED DI- AND TRIPEPTIDYL IMMUNOSUPPRESSIVE COMPOUNDS 审中-公开
标题翻译：改良的DI-和TRIPEPTIYL免疫抑制化合物
公开(公告)号：WO1992004370A1
公开(公告)日：1992-03-19
申请号：PCT/US1991005691
申请日：1991-08-09
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： VERTEX PHARMACEUTICALS INCORPORATED , TUNG, Roger, D. , MEYERS, Harold, V.
IPC分类号： C07K05/06
CPC分类号： C07K5/081 , A61K38/00 , C07K5/06078 , C07K5/0806 , C07K5/0808
摘要： A series of linear, modified di- and tripeptides are claimed, which have an affinity for FK-506 binding protein (FKBP) and are immunosuppressive agents. These compounds, which are characterized by high lipophilicity and the absence of charged groups, can be depicted by general formula (I). These compounds are useful as T-cell specific immunosuppressive agents for the treatment of graft rejection, graft versus host disease, and a wide variety of autoimmune diseases in an individual.
摘要翻译：要求一系列线性，修饰的二肽和三肽，其对FK-506结合蛋白（FKBP）具有亲和力，并且是免疫抑制剂。这些具有高亲脂性和不带电基团特征的化合物可以由通式（I）描述。这些化合物可用作T细胞特异性免疫抑制剂，用于治疗移植物排斥，移植物抗宿主病和个体中各种各样的自身免疫性疾病。

10. 发明授权

EP0659181B1 SULFONAMIDE INHIBITORS OF HIV-ASPARTYL PROTEASE 失效
标题翻译： SULFONAMID INHIBITOREN VON HIV-ASPARTYL PROTEASE
公开(公告)号：EP0659181B1
公开(公告)日：1999-04-07
申请号：EP93921428.4
申请日：1993-09-07
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： TUNG, Roger, D. , MURCKO, Mark, A. , BHISETTI, Govinda, Rao
IPC分类号： C07D215/48 , A61K31/16 , C07D413/12 , C07D417/12 , C07D409/14 , C07D409/12 , C07D213/30 , C07C311/41 , C07D207/26 , C07D305/12 , C07D239/54
CPC分类号： C07D207/26 , A61K38/00 , C07C307/06 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/39 , C07C311/46 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D213/30 , C07D213/78 , C07D215/38 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06139

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式