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1. 发明申请

WO1997022619A2 INHIBITORS OF INTERLEUKIN-1'beta' CONVERTING ENZYME 审中-公开
标题翻译： INTERLEUKIN-1转化酶的抑制剂
公开(公告)号：WO1997022619A2
公开(公告)日：1997-06-26
申请号：PCT/US1996020843
申请日：1996-12-20
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： VERTEX PHARMACEUTICALS INCORPORATED , BATCHELOR, Mark, J. , BEBBINGTON, David , BEMIS, Guy, W. , FRIDMAN, Wolf, Herman , GILLESPIE, Roger, J. , GOLEC, Julian, M., C. , GU, Yong , LAUFFER, David, J. , LIVINGSTON, David, J. , MATHARU, Saroop, S. , MULLICAN, Michael, D. , MURCKO, Mark, A. , MURDOCH, Robert , NYCE, Philip, L. , ROBIDOUX, Andrea, L., C. , SU, Michael , WANNAMAKER, M., Woods , WILSON, Keith, P. , ZELLE, Robert, E.
IPC分类号： C07K05/02
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1 beta converting enzyme. The ICE inhibitors of this invention are 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 ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN- gamma - mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN- gamma -mediated diseases and decreasing IGIF and IFN- gamma production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶抑制剂的新型化合物。本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。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ICE活性，因此可有利地用作抗IL-1，细胞凋亡，IGIF和IFN-γ介导的疾病，炎性疾病，自身免疫疾病破坏性骨病，增殖性疾病，感染性疾病，退行性疾病和坏死性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性，用于治疗白介素-1-，细胞凋亡，IGIF-和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。本发明还涉及制备N-酰基氨基化合物的方法。

2. 发明公开

EP0869967A2 INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME 失效
标题翻译：白细胞介素1β的CONVERTIERENDEN EXZYMS抑制剂
公开(公告)号：EP0869967A2
公开(公告)日：1998-10-14
申请号：EP96945318.0
申请日：1996-12-20
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BATCHELOR, Mark, J. , BEBBINGTON, David , BEMIS, Guy, W. , FRIDMAN, Wolf, Herman , GILLESPIE, Roger, J. , GOLEC, Julian, M., C. , GU, Yong , LAUFFER, David, J. , LIVINGSTON, David, J. , MATHARU, Saroop, S. , MULLICAN, Michael, D. , MURCKO, Mark, A. , MURDOCH, Robert , NYCE, Philip, L. , ROBIDOUX, Andrea, L., C. , SU, Michael , WANNAMAKER, M., Woods , WILSON, Keith, P. , ZELLE, Robert, E.
IPC分类号： C07D243 , A61K31 , A61K38 , A61P13 , A61P19 , A61P25 , A61P29 , A61P31 , A61P35 , A61P37 , A61P43 , C07D401 , C07D403 , C07D405 , C07D409 , C07D413 , C07D417 , C07D471 , C07D473 , C07D487 , C07D491 , C07D495 , C07D498 , C07D513 , C07D519 , C07F9 , C07K5
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1² converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physiochemical 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 ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-³-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF-, and IFN-³-mediated diseases and decreasing IGIF, and IFN-³ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

3. 发明公开

EP1076692A2 CRYSTALLIZABLE JNK COMPLEXES 审中-公开
标题翻译：可结晶的JNK配合物
公开(公告)号：EP1076692A2
公开(公告)日：2001-02-21
申请号：EP99920350.8
申请日：1999-05-04
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： XIE, Xiaoling , GU, Yong , MARKLAND, William , SU, Michael, S. , CARON, Paul, R. , FOX, Edward , WILSON, Keith, P.
IPC分类号： C12N9/12
CPC分类号： C12N9/1205
摘要： The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site binding pockets of JNK3. A computer comprising such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to JNK3 or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of JNK3 or close structural homologues of the active site binding pockets.
摘要翻译：本发明涉及用分子和分子复合物的相应结构坐标编码的数据存储介质，所述分子和分子复合物包含JNK3的活性位点结合袋。包含这种数据存储材料的计算机能够将这样的分子和分子复合物或其结构同系物显示为计算机屏幕上的图形三维表示。本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。另外，本发明涉及使用结构坐标来筛选和设计结合JNK3或其同系物的化合物（包括抑制性化合物）的方法。本发明还涉及包含JNK3的活性位点结合袋或活性位点结合袋的紧密结构同系物的分子和分子复合物。

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