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1. 发明申请

WO2005111008A2 COMPOUNDS FOR ENZYME INHIBITION 审中-公开
标题翻译：用于酶抑制的化合物
公开(公告)号：WO2005111008A2
公开(公告)日：2005-11-24
申请号：PCT/US2005/016335
申请日：2005-05-09
申请人： PROTEOLIX, INC. , SMYTH, Mark, S. , LAIDIG, Guy, J. , BORCHARDT, Ronald, T. , BUNIN, Barry, A. , CREWS, Craig, M. , MUSSER, John, H. , SHENK, Kevin, D. , RADEL, Peggy, A.
发明人： SMYTH, Mark, S. , LAIDIG, Guy, J. , BORCHARDT, Ronald, T. , BUNIN, Barry, A. , CREWS, Craig, M. , MUSSER, John, H. , SHENK, Kevin, D. , RADEL, Peggy, A.
IPC分类号： C07D303/00
CPC分类号： C07K5/0812 , C07K5/06034 , C07K5/0827 , Y02A50/412
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。肽类化合物包括环氧化物或氮丙啶，并且在N-末端官能化。除了其它治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

2. 发明申请

WO2005105827A2 COMPOUNDS FOR ENZYME INHIBITION 审中-公开
标题翻译：用于酶抑制的化合物
公开(公告)号：WO2005105827A2
公开(公告)日：2005-11-10
申请号：PCT/US2005/012740
申请日：2005-04-14
申请人： PROTEOLIX, INC. , SMYTH, Mark, S. , LAIDIG, Guy, J. , BORCHARDT, Ronald, T. , BUNIN, Barry, A. , CREWS, Craig, M. , MUSSER, John, H. , SCHNEEKLOTH, John, S., Jr. , CHABALA, John, Clifford
发明人： SMYTH, Mark, S. , LAIDIG, Guy, J. , BORCHARDT, Ronald, T. , BUNIN, Barry, A. , CREWS, Craig, M. , MUSSER, John, H. , SCHNEEKLOTH, John, S., Jr. , CHABALA, John, Clifford
IPC分类号： C07K5/087
CPC分类号： C07K5/1016 , C07K5/0812 , C07K5/0827
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。基于肽的化合物包括至少三个肽单元，环氧化物或氮丙啶，并且在N-末端官能化。除了其它治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

3. 发明申请

WO2003044219A1 METHOD OF FLEXIBLY GENERATING DIVERSE REACTION CHEMISTRIES 审中-公开
标题翻译：灵活生成多元反应化学化学的方法
公开(公告)号：WO2003044219A1
公开(公告)日：2003-05-30
申请号：PCT/US2002/037190
申请日：2002-11-19
申请人： LIBRARIA, INC. , BUNIN, Barry, A. , POWERS, Timothy, S. , MORALES, Guillermo, Antonio , SCHURER, Stephan, C. , MUSKAL, Steve, M. , SAUNDERS, Oliver, L.
发明人： BUNIN, Barry, A. , POWERS, Timothy, S. , MORALES, Guillermo, Antonio , SCHURER, Stephan, C. , MUSKAL, Steve, M. , SAUNDERS, Oliver, L.
IPC分类号： C12Q1/00
CPC分类号： G06F19/702 , C40B50/02 , G06F19/709
摘要： Computational tools automatically suggest/generate diverse reaction sets for particular precursors, classes of precursors, or different reaction chemistries. This is accomplished by automatically generating a group of reaction chemistries for a particular precursor or class of precursors. Some of the reactions and/or products may be produced without reliance on reactions and products reported in available references.
摘要翻译：计算工具自动建议/生成特定前体，前体类别或不同反应化学物质的各种反应组。这是通过自动生成一组用于特定前体或一类前体的反应化学物质来实现的。一些反应和/或产物可以在不依赖可用参考文献中报道的反应和产物的情况下生产。

4. 发明申请

WO2003046799A1 CHEMISTRY RESOURCE DATABASE 审中-公开
标题翻译：化学资源数据库
公开(公告)号：WO2003046799A1
公开(公告)日：2003-06-05
申请号：PCT/US2002/037415
申请日：2002-11-18
申请人： LIBRARIA, INC. , BUNIN, Barry, A. , SCHURER, Stephan, C. , MUSKAL, Steve, M.
发明人： BUNIN, Barry, A. , SCHURER, Stephan, C. , MUSKAL, Steve, M.
IPC分类号： G06F19/00
CPC分类号： G06N5/022 , G06F19/709
摘要： Reaction steps (115, 117, 119, 123, 125) are organized as belonging to particular reaction protocols (113, 121) within a database. Each reaction may represent a discrete step in a multi-step protocol for making a final product from a starting reactant. To populate the database, a system receives information separately from a plurality of references (109, 111), e.g., literature articles, patent publications, etc. Such information typically includes descriptions of reaction steps presented in the references ,e.g., detailed recipes for performing the reaction steps. Alternatively, or in addition, the methodology includes identifying at least one protocol specified in the reference, which protocol comprises two or more reaction steps, and then specifying that the two or more reaction steps belong to the protocol.
摘要翻译：反应步骤（115,117,119,123,125）被组织为属于数据库内的特定反应方案（113,121）。每个反应可以代表从起始反应物制备最终产物的多步骤方案中的离散步骤。为了填充数据库，系统从多个参考文献（109,111）分开接收信息，例如文献文献，专利出版物等。这样的信息通常包括在参考文献中呈现的反应步骤的描述，例如用于执行的详细配方反应步骤。或者或另外，该方法包括识别参考文献中指定的至少一个协议，该协议包括两个或多个反应步骤，然后指定两个或多个反应步骤属于协议。

5. 发明公开

EP1758921A2 COMPOUNDS FOR PROTEASOME ENZYME INHIBITION 审中-公开
标题翻译：蛋白酶抑制剂化合物
公开(公告)号：EP1758921A2
公开(公告)日：2007-03-07
申请号：EP05742187.7
申请日：2005-05-09
申请人： Proteolix, Inc.
发明人： SMYTH, Mark, S. , LAIDIG, Guy, J. , BORCHARDT, Ronald, T. , BUNIN, Barry, A. , CREWS, Craig, M. , MUSSER, John, H. , SHENK, Kevin, D. , RADEL, Peggy, A.
IPC分类号： C07K5/087 , C07K5/08 , A61K38/06 , C07K5/062 , C07K5/078 , C07D303/32 , C07D409/12 , C07K5/027 , C07D413/12 , A61K31/335
CPC分类号： C07K5/0812 , C07K5/06034 , C07K5/0827 , Y02A50/412
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-termmal nucleophile (Nin) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by she compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效且选择性地抑制N-末端亲核体（Ntn）水解酶的特定活性。具有多种活性的那些Ntn的活性可以被所述化合物差异地抑制。例如，用本发明的化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。基于肽的化合物包括环氧化物或氮丙啶，并且在N端官能化。在其他治疗用途中，预计基于肽的化合物显示抗炎特性和抑制细胞增殖。

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