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1.发明申请USE OF BETA-SHEET MIMETICS AS PROTEASE AND KINASE INHIBITORS AND AS INHIBITORS OF TRANSCRIPTION FACTORS 审中-公开作为蛋白酶和激酶抑制剂和作为转录因子的抑制剂的BETA-SHEET MIME的使用
公开(公告)号：WO1998005333A1
公开(公告)日：1998-02-12
申请号：PCT/US1997013622
申请日：1997-08-05
申请人： MOLECUMETICS LTD. , KAHN, Michael , QABAR, Maher, Nicola , McMILLAN, Michael, Kim , OGBU, Cyprian, Okwara , EGUCHI, Masakatsu , KIM, Hwa-Ok , BOATMAN, Patrick, Douglas, Jr. , URBAN, Jan , MEARA, Joseph, Patrick , BABU, Suresh , FERGUSON, Mark, D. , LUM, Christopher, Todd
发明人： MOLECUMETICS LTD.
IPC分类号： A61K31/50
CPC分类号： C07K7/06 , A61K31/4035 , A61K31/407 , A61K31/4152 , A61K31/428 , A61K31/437 , A61K31/5025 , A61K38/005 , A61K38/04 , A61K38/55 , C07K1/047 , C07K5/021 , C07K5/06139 , C07K5/06191 , C07K5/0821 , C07K5/1024
摘要： beta -sheet mimetics and methods relating to the same are disclosed. The beta -sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors. Methods of the invention include administration of a beta -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 and/or transcription factor.
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，激酶和/或转录因子相关的多种病症的药物。
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2.发明申请
公开(公告)号：WO2004035587A1
公开(公告)日：2004-04-29
申请号：PCT/US2003/032411
申请日：2003-10-14
申请人： MYRIAD GENETICS, INC. , QABAR, Maher, N. , STASIAK, Marcin , MATHEW, Jessymol , LITTLE, Thomas , HUANG, Danwen
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Reverse-turn mimetics and methods relating to the same having Structure (I) are disclosed, including pharmaceutically acceptable salts and stereoisomers thereof, wherein R 1 , R 2 , R 3 and R 4 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 such compounds, are neurokinin (tachykinin) antagonists. Libraries containing the reverse-turn mimetics of this invention are also disclosed.
摘要翻译： 公开了涉及具有结构（I）的反转模拟物和与其相同的方法，包括其药学上可接受的盐和立体异构体，其中R 1，R 2，R 3和R 4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这些化合物的药物组合物是神经激肽（速激肽）拮抗剂。 还公开了包含本发明的反转模拟物的文库。
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公开(公告)号：WO2006055525A2
公开(公告)日：2006-05-26
申请号：PCT/US2005041269
申请日：2005-11-15
申请人： CEPTYR INC , BLASKOVICH MARK A , BAUGHMAN TED , LITTLE THOMAS , PATT WILLIAM , QABAR MAHER , SCHULTZ LAURI , HONG FENG , NAGULA GANGADHAR , GAGE JENNIFER LYNN , HOWBERT JAMES JEFFRY
发明人： BLASKOVICH MARK A , BAUGHMAN TED , LITTLE THOMAS , PATT WILLIAM , QABAR MAHER , SCHULTZ LAURI , HONG FENG , NAGULA GANGADHAR , GAGE JENNIFER LYNN , HOWBERT JAMES JEFFRY
IPC分类号： A61K31/675 , A61K31/66
CPC分类号： C07F9/6541 , C07F9/3808 , C07F9/4006 , C07F9/5721 , C07F9/5728 , C07F9/591 , C07F9/65517
摘要： The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.
摘要翻译： 本发明提供了可用于调节蛋白酪氨酸磷酸酶-1b（PTP1B）酶的生物学活性的式（I）和式（II）的化合物。 本发明的化合物可用于治疗其中PTP1B酶是因子的疾病和/或病症。 这些疾病和/或病症包括但不限于1型糖尿病，2型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖症，高脂血症，高甘油三酯血症，高胆固醇血症，低HDL水平，动脉粥样硬化，血管再狭窄，炎性肠病， 胰腺炎，脂肪细胞瘤，脂肪细胞癌，脂肪肉瘤，血脂异常，癌症和神经变性疾病。
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公开(公告)号：WO2006055525A3
公开(公告)日：2006-05-26
申请号：PCT/US2005/041269
申请日：2005-11-15
申请人： CEPTYR, INC. , BLASKOVICH, Mark A. , BAUGHMAN, Ted , LITTLE, Thomas , PATT, William , QABAR, Maher , SCHULTZ, Lauri , HONG, Feng , NAGULA, Gangadhar , GAGE, Jennifer Lynn , HOWBERT, James Jeffry
发明人： BLASKOVICH, Mark A. , BAUGHMAN, Ted , LITTLE, Thomas , PATT, William , QABAR, Maher , SCHULTZ, Lauri , HONG, Feng , NAGULA, Gangadhar , GAGE, Jennifer Lynn , HOWBERT, James Jeffry
摘要： The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.
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