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1. 发明申请

WO1996030396A1 'beta'-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS 审中-公开
标题翻译： β-SHEET的MIME类型和作为蛋白酶抑制剂的用途
公开(公告)号：WO1996030396A1
公开(公告)日：1996-10-03
申请号：PCT/US1996004115
申请日：1996-03-25
申请人： MOLECUMETICS LTD. , KAHN, Michael
发明人： MOLECUMETICS LTD.
IPC分类号： C07K05/06
CPC分类号： C07K5/0202 , A61K38/005
摘要： There are disclosed beta -sheet mimetics and methods relating to the same for imparting or stabilizing the beta -sheet structure of a peptide, protein or molecule. In one aspect, the beta -sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The beta -sheet mimetics have utility as protease inhibitors generally, including activity as serine protease inhibitors such as thrombin, elastase and Factor X.
摘要翻译：公开了与用于赋予或稳定肽，蛋白质或分子的β-折叠结构相同的β-折叠模拟物和方法。一方面，β-折叠模拟物在肽或蛋白质的末端或长度内共价连接。 β-折叠模拟物通常用作蛋白酶抑制剂，包括作为丝氨酸蛋白酶抑制剂如凝血酶，弹性蛋白酶和因子X的活性。

2. 发明申请

US20030130168A1 Reverse-turn mimetics and methods relating thereto 审中-公开
公开(公告)号：US20030130168A1
公开(公告)日：2003-07-10
申请号：US10167979
申请日：2002-06-12
申请人： Molecumetics, Ltd.
发明人： Marcin Stasiak , Michael Kahn
IPC分类号： A61K038/16 , A61K031/551 , A61K031/498 , C07K014/00 , C07D487/04
CPC分类号： C07D487/04 , A61K38/00 , C07K5/06139 , C40B40/00 , G01N2333/70546
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: 1 wherein A, R1, R2, R2a, R3, R3a and R4 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

3. 发明申请

US20030236245A1 Helix mimetics and composition and methods related thereto 有权
标题翻译：螺旋模拟物及其组成和方法
公开(公告)号：US20030236245A1
公开(公告)日：2003-12-25
申请号：US10230974
申请日：2002-08-29
申请人： Molecumetics, Ltd.
发明人： Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Sang Lee
IPC分类号： A61K031/554 , A61K031/551 , A61K031/542 , A61K031/5383 , A61K031/498 , G01N033/53 , C07D279/14
CPC分类号： C40B40/04 , C07D487/08 , C07D513/08 , C40B30/04
摘要： Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: 1 including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, R1 and R2 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.
摘要翻译：模拟具有以下结构的生物活性肽和蛋白质的螺旋区域的二级结构的化合物：包括其药学上可接受的盐和立体异构体，其中Y，A，B，R 1和R 2如本文所定义。这些化合物在广泛的应用中具有应用价值，包括用作诊断和治疗剂。特别地，本发明的化合物和含有它们的药物组合物是神经激肽（速激肽）拮抗剂。还公开了含有本发明化合物的文库，以及筛选这些文库以鉴定生物活性成员的方法。

4. 发明申请

US20030027819A1 Beta-sheet mimetics and methods relating to the use thereof 审中-公开
标题翻译： β-折叠模拟物及其使用方法
公开(公告)号：US20030027819A1
公开(公告)日：2003-02-06
申请号：US09960864
申请日：2001-09-21
申请人： Molecumetics Ltd.
发明人： Maher N. Qabar , Michael K. McMillan , Michael S. Kahn , John E. Tulinsky , Cyprian O. Ogbu , Jessymol Mathew
IPC分类号： A61K031/542 , A61K031/5383 , A61K031/4745 , A61K031/429 , A61K031/424
CPC分类号： A61K31/4035 , A61K31/407 , A61K31/4152 , A61K31/4196 , A61K31/424 , A61K31/428 , A61K31/43 , A61K31/437 , A61K31/5025 , C07K1/047 , C07K5/021 , C07K5/06139 , C07K5/06191 , C07K5/0821 , C07K5/1024 , C07K7/06
摘要： null-sheet mimetics and methods relating to the same are disclosed. The null-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a null-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.
摘要翻译：公开了β-折叠模拟物和与其相关的方法。 β-折叠模拟物可用作蛋白酶和激酶抑制剂，以及转录因子和蛋白质 - 蛋白质结合相互作用的抑制剂。本发明的方法包括施用β-折叠模拟物，或其用途用于制备用于治疗与靶向蛋白酶，激酶，转录因子和/或蛋白质 - 蛋白质结合相互作用相关的多种病症的药物。

5. 发明申请

US20030220328A1 Reverse-turn mimetics and composition and methods relating thereto 有权
标题翻译：反转模拟物及其组合和方法
公开(公告)号：US20030220328A1
公开(公告)日：2003-11-27
申请号：US10268062
申请日：2002-10-09
申请人： Molecumetics Ltd.
发明人： Gangadhar Nagula , Jan Urban , Hwa-Ok Kim , Christopher Lum , Hiroshi Nakanishi
IPC分类号： G01N033/53 , A61K031/551 , A61K031/498 , C07D487/04
CPC分类号： C07D487/04
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: 1 wherein A, R1, R2, R2a and R3 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
摘要翻译：公开了模拟具有以下结构的生物活性肽和蛋白质的反转转区的二级结构的构象约束化合物：其中A，R1，R2，R2a和R3如本文所定义。这些化合物可用于广泛的领域，包括用作诊断和治疗剂。特别地，本发明的化合物可用作作为抗炎剂的药物组合物以及中枢神经障碍的抑制剂。还公开了含有本发明化合物的文库，以及筛选该文库以鉴定生物活性成员的方法。

6. 发明申请

WO2003030907A1 REVERSE-TURN MIMETICS AND COMPOSITION AND METHODS RELATING THERETO 审中-公开
标题翻译：反向转换的MIME和组合物以及与之相关的方法
公开(公告)号：WO2003030907A1
公开(公告)日：2003-04-17
申请号：PCT/US2002/032478
申请日：2002-10-09
申请人： MOLECUMETICS LTD. , NAGULA, Gangadhar , URBAN, Jan , KIM, Hwa-Ok , LUM, Christopher , NAKANISHI, Hiroshi
发明人： NAGULA, Gangadhar , URBAN, Jan , KIM, Hwa-Ok , LUM, Christopher , NAKANISHI, Hiroshi
IPC分类号： A61K31/4985
CPC分类号： C07D487/04
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologicallyactive peptides and proteins having structure (I) are disclosed wherein A, R1, R2, R2a and R3 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
摘要翻译：公开了模拟生物活性肽和具有结构（I）的蛋白质的逆转区域的二级结构的构象约束化合物，其中A，R1，R2，R2a和R3如本文所定义。这些化合物可用于广泛的领域，包括用作诊断和治疗剂。特别地，本发明的化合物可用作作为抗炎剂的药物组合物以及中枢神经障碍的抑制剂。还公开了含有本发明化合物的文库，以及筛选该文库以鉴定生物活性成员的方法。

7. 发明申请

WO1996030035A1 'beta'-SHEET MIMETICS AND USE THEREOF AS INHIBITORS OF BIOLOGICALLY ACTIVE PEPTIDES OR PROTEINS 审中-公开
标题翻译： β-HSEET的MIME类型及其作为生物活性肽或蛋白质的抑制剂的用途
公开(公告)号：WO1996030035A1
公开(公告)日：1996-10-03
申请号：PCT/US1996004044
申请日：1996-03-25
申请人： MOLECUMETICS LTD. , KAHN, Michael
发明人： MOLECUMETICS LTD.
IPC分类号： A61K38/00
CPC分类号： C07K5/0202 , A61K38/005
摘要： There are disclosed beta -sheet mimetics and methods relating to the same for imparting or stabilizing the beta -sheet structure of a peptide, protein or molecule. In one aspect, the beta -sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The beta -sheet mimetics have utility as inhibitors of one or more of proteases, kinases, CAAX, peptides binding to SH2 domains and MHC-I and/or MHC-II presentation of peptides to T cell receptors in warm-blooded animals.
摘要翻译：公开了与用于赋予或稳定肽，蛋白质或分子的β-折叠结构相同的β-折叠模拟物和方法。一方面，β-折叠模拟物在肽或蛋白质的末端或长度内共价连接。 β-折叠模拟物可用作一种或多种蛋白酶，激酶，CAAX，与SH2结构域结合的肽和MHC-1和/或MHC-II肽在温血动物中呈递T细胞受体的抑制剂。

8. 发明申请

WO02092010A3 REVERSE-TURN MIMETICS AND METHODS RELATING THERETO 审中-公开
标题翻译：反向转换MIME和与之相关的方法
公开(公告)号：WO02092010A3
公开(公告)日：2003-02-27
申请号：PCT/US0215679
申请日：2002-05-16
申请人： MOLECUMETICS LTD , URBAN JAN , NAKANISHI HIROSHI , LEE MIN S
发明人： URBAN JAN , NAKANISHI HIROSHI , LEE MIN S
IPC分类号： C07D487/04 , C07D487/14 , C07D498/04 , C07D498/14 , A61K31/4985 , A61K31/519 , A61K31/5365 , A61K38/04
CPC分类号： C07D487/04 , C07D487/14
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
摘要翻译：公开了模拟生物活性肽和蛋白质的反转转区的二级结构的构象约束化合物。这些化合物可用于广泛的领域，包括用作诊断和治疗剂。特别地，本发明的化合物可用作作为抗炎剂的药物组合物以及中枢神经障碍的抑制剂。还公开了含有本发明化合物的文库，以及筛选该文库以鉴定生物活性成员的方法。

9. 发明申请

WO1996022304A1 CONFORMATIONALLY CONSTRAINED REVERSE-TURN LIBRARY AND METHODS RELATING THERETO 审中-公开
标题翻译：一致的约束反转图书馆和与之相关的方法
公开(公告)号：WO1996022304A1
公开(公告)日：1996-07-25
申请号：PCT/US1996000786
申请日：1996-01-19
申请人： MOLECUMETICS, LTD.
发明人： MOLECUMETICS, LTD. , KAHN, Michael
IPC分类号： C07K01/04
CPC分类号： C07K1/047 , C07K5/02 , C07K5/021
摘要： Libraries of conformationally constrained-reverse turn mimetics, and methods of constructing the same are disclosed. The reverse-turn mimetics include beta-turn, gamma-turn and beta-bulge mimetics which mimic the biologically active conformation of a linear peptide. In a preferred embodiment, a template library is constructed based on the amino acid sequence of the linear peptide, and which contains a plurality of beta-turn, gamma-turn and beta-bulge mimetics of varying ring sizes. The template library is then screened in a suitable assay to identify a biologically active template library member. An optimized library is then constructed based on structure of the biologically active template member, and which includes substitutions to the amino acid sequence thereof. The optimized library is similarly screened to identify a biologically active reverse-turn mimetic. Methods relating to identifying library members which interact with biological targets of interest, and the use of such members as diagnostic, prophylactic and/or therapeutic agents are also disclosed.
摘要翻译：公开了构象约束反转模拟物的文库及其构建方法。逆转模拟物包括模拟线性肽的生物活性构象的β-转角，γ-转角和β-凸起模拟物。在优选的实施方案中，基于线性肽的氨基酸序列构建模板文库，并且其包含多个具有不同环尺寸的β-匝，γ-匝和β-隆起模拟物。然后在合适的测定中筛选模板文库以鉴定生物活性的模板文库成员。然后基于生物活性模板成员的结构构建优化的文库，其包括对其氨基酸序列的取代。类似地筛选优化的文库以鉴定生物活性的逆转模拟物。还公开了与识别与感兴趣的生物靶标相互作用的文库成员以及诊断，预防和/或治疗剂等成员的用途的方法。

10. 发明申请

WO2003018587A1 HELIX MIMETICS AND COMPOSITION AND METHODS RELATED THERETO 审中-公开
标题翻译： HELIXMIMTICS及其组合物及其相关方法
公开(公告)号：WO2003018587A1
公开(公告)日：2003-03-06
申请号：PCT/US2002/028049
申请日：2002-08-29
申请人： MOLECUMETICS, LTD. , HUBER, Vincent , URBAN, Jan , NAKANISHI, Hiroshi , EGUCHI, Masakatsu , MATHEW, Jessymol , LEE, Min, Sang
发明人： HUBER, Vincent , URBAN, Jan , NAKANISHI, Hiroshi , EGUCHI, Masakatsu , MATHEW, Jessymol , LEE, Min, Sang
IPC分类号： C07D487/18
CPC分类号： C40B40/04 , C07D487/08 , C07D513/08 , C40B30/04
摘要： Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure (Formula) including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, R1 and R2 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.
摘要翻译：模拟具有下列结构（式）的生物活性肽和蛋白质的螺旋区域的二级结构的化合物（式），包括其药学上可接受的盐和立体异构体，其中Y，A，B，R 1和R 2如本文所定义。这些化合物在广泛的应用中具有应用价值，包括用作诊断和治疗剂。特别地，本发明的化合物和含有它们的药物组合物是神经激肽（速激肽）拮抗剂。还公开了含有本发明化合物的文库，以及筛选这些文库以鉴定生物活性成员的方法。

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