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1. 发明申请

US20050222143A1 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：US20050222143A1
公开(公告)日：2005-10-06
申请号：US11121337
申请日：2005-05-03
申请人： Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Lee
发明人： Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Lee
IPC分类号： A61P25/06 , A61P25/28 , A61P29/00 , C07D487/08 , C07D498/08 , C07D513/08 , C40B30/04 , C40B40/04 , A61K31/538 , A61K31/519
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: 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。

2. 发明申请

US20060079517A1 Reverse-turn mimetics and methods relating thereto 审中-公开
公开(公告)号：US20060079517A1
公开(公告)日：2006-04-13
申请号：US11292611
申请日：2005-12-02
申请人： Jan Urban , Hiroshi Nakanishi , Min Lee
发明人： Jan Urban , Hiroshi Nakanishi , Min Lee
IPC分类号： A61K31/5415 , A61K31/498
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 having the following structure are disclosed: wherein A, B, X, R1, and R5 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.

3. 发明授权

US07008941B2 Reverse-turn mimetics and methods relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US07008941B2
公开(公告)日：2006-03-07
申请号：US10150481
申请日：2002-05-16
申请人： Jan Urban , Hiroshi Nakanishi , Min S. Lee
发明人： Jan Urban , Hiroshi Nakanishi , Min S. Lee
IPC分类号： G01N33/53 , G08D498/04
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 having the following structure are disclosed: wherein A, B, X, R1, and R5 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：公开了具有以下结构的模拟具有生物活性肽和蛋白质的反向转转区域的二级结构的构象约束化合物：其中A，B，X，R 1和R 5， / SUB>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。

4. 发明授权

US06943167B2 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：US06943167B2
公开(公告)日：2005-09-13
申请号：US10230974
申请日：2002-08-29
申请人： Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Sang Lee
发明人： Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Sang Lee
IPC分类号： A61P25/06 , A61P25/28 , A61P29/00 , C07D487/08 , C07D498/08 , C07D513/08 , C40B30/04 , C40B40/04 , C07D473/00 , A61K31/495
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: 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. Libaries contaning the compounds of this invention are also disclosed, as well as methods for screening such libaries 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本文，以及用于筛选这些文库的方法鉴定生物活性成员。

5. 发明授权

US07407952B2 Reverse-turn mimetics and compositions and methods related thereto 有权
标题翻译：反转模拟物及其组合物和方法
公开(公告)号：US07407952B2
公开(公告)日：2008-08-05
申请号：US11175920
申请日：2005-07-06
申请人： Gangadhar Nagula , Jan Urban , Hwa-Ok Kim , Christopher Lum , Hiroshi Nakanishi
发明人： Gangadhar Nagula , Jan Urban , Hwa-Ok Kim , Christopher Lum , Hiroshi Nakanishi
IPC分类号： A61P29/00 , A61P35/04 , A61P17/00 , A61P25/06
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: 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：公开了具有以下结构的模拟具有生物活性肽和蛋白质的反转转区的二级结构的构象约束的化合物：其中A，R 1，R 2，R 2a和R 3'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. 发明授权

US07405212B2 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：US07405212B2
公开(公告)日：2008-07-29
申请号：US11121337
申请日：2005-05-03
申请人： Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Sang Lee
发明人： Vincent Huber , Jan Urban , Hiroshi Nakanishi , Masakatsu Eguchi , Jessymol Mathew , Min Sang Lee
IPC分类号： C07D498/08 , C07D263/00
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: 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。

7. 发明申请

US20050245528A1 Reverse-turn mimetics and compositions and methods related thereto 有权
标题翻译：反转模拟物及其组合物和方法
公开(公告)号：US20050245528A1
公开(公告)日：2005-11-03
申请号：US11175920
申请日：2005-07-06
申请人： Gangadhar Nagula , Jan Urban , Hwa-Ok Kim , Christopher Lum , Hiroshi Nakanishi
发明人： Gangadhar Nagula , Jan Urban , Hwa-Ok Kim , Christopher Lum , Hiroshi Nakanishi
IPC分类号： C07D487/04 , A61K31/498
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: 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：公开了具有以下结构的模拟具有生物活性肽和蛋白质的反转转区的二级结构的构象约束的化合物：其中A，R 1，R 2，R 2a和R 3'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。

8. 发明授权

US06943157B2 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：US06943157B2
公开(公告)日：2005-09-13
申请号：US10268062
申请日：2002-10-09
申请人： Gangadhar Nagula , Jan Urban , Hwa-Ok Kim , Christopher Lum , Hiroshi Nakanishi
发明人： Gangadhar Nagula , Jan Urban , Hwa-Ok Kim , Christopher Lum , Hiroshi Nakanishi
IPC分类号： C07D487/04 , A61K31/519 , A61K31/55
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: 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：公开了具有以下结构的模拟具有生物活性肽和蛋白质的反转转区的二级结构的构象约束的化合物：其中A，R 1，R 2，R 2a和R 3'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。

9. 发明申请

US20070088163A1 Modulators of calcitonin and amylin activity 审中-公开
标题翻译：降钙素和胰岛淀粉酶活性的调节剂
公开(公告)号：US20070088163A1
公开(公告)日：2007-04-19
申请号：US10571031
申请日：2004-09-10
申请人： Kent Pryor , Eddine Saiah , Jeffrey Kahl , Nancy Delaet , Edward Roberts , Jan Urban , Lubomir Sebo , Christopher Lum , Hiroshi Nakanishi
发明人： Kent Pryor , Eddine Saiah , Jeffrey Kahl , Nancy Delaet , Edward Roberts , Jan Urban , Lubomir Sebo , Christopher Lum , Hiroshi Nakanishi
IPC分类号： C07D471/02 , C07D215/16
CPC分类号： C07D471/04 , C07D405/12
摘要： In various aspects, the present invention relates to novel compounds, which modulate calcitonin and amylin receptor activity; to processes for the preparation of such compounds; and to pharmaceutical compositions including such compounds. Compounds of the invention are useful as calcitonin and/or amylin agonists and in the treatment of bone disease such as osteoporosis, Paget's disease, hypercalcemia, and in the treatment of metabolic diseases, such as insulin-requiring states.
摘要翻译：在各个方面，本发明涉及调节降钙素和胰岛淀粉样多肽受体活性的新化合物; 制备这些化合物的方法; 以及包含这些化合物的药物组合物。本发明的化合物可用作降钙素和/或胰岛淀粉样多肽激动剂和治疗骨疾病如骨质疏松症，佩吉特氏病，高钙血症，以及治疗代谢疾病如胰岛素需求状态。

10. 发明申请

US20100273797A1 ALPHA-KETOAMIDES AND DERIVATIVES THEREOF 审中-公开
标题翻译：阿尔法 - 卡特敏胺及其衍生物
公开(公告)号：US20100273797A1
公开(公告)日：2010-10-28
申请号：US12829701
申请日：2010-07-02
申请人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G. J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhijun Wang
发明人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G. J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhijun Wang
IPC分类号： A61K31/5377 , A61K31/5375 , A61K31/437 , A61P9/00 , A61P19/02 , A61P1/00 , A61P29/00 , A61P37/06 , A61P25/00 , A61P25/28 , A61P3/04 , A61P17/00
CPC分类号： A61K31/416 , C07D207/40 , C07D231/12 , C07D231/40 , C07D239/47 , C07D249/12 , C07D253/075 , C07D295/088 , C07D403/12 , C07D471/04 , C07D487/04 , Y02A50/401 , Y02A50/409 , Y02A50/411
摘要： The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions medicated by cytokines such as arthritis.
摘要翻译：本发明提供可用作细胞因子抑制剂的低分子量化合物及其组合物。特别地，本发明的化合物可用作抗炎剂。还提供了用于制备这些药剂的方法及其在预防或治疗由诸如关节炎的细胞因子药物治疗的病症中的用途。

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