公开(公告)号：US20080161592A1

公开(公告)日：2008-07-03

申请号：US12043872

申请日：2008-03-06

申请人： Mark Arnold Thomas Blaskovich ,  Ted Baughman ,  Thomas Little ,  William Patt ,  Maher Qabar ,  Lauri Marie Schultz ,  Feng Hong ,  Gangadhar Nagula ,  Jennifer Lynn Gage ,  James Jeffrey Howbert

发明人： Mark Arnold Thomas Blaskovich ,  Ted Baughman ,  Thomas Little ,  William Patt ,  Maher Qabar ,  Lauri Marie Schultz ,  Feng Hong ,  Gangadhar Nagula ,  Jennifer Lynn Gage ,  James Jeffrey Howbert

IPC分类号： C07F9/22 ,  C07F9/28

CPC分类号： C07F9/6541 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/59 ,  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。

公开(公告)号：US07829737B2

公开(公告)日：2010-11-09

申请号：US12043872

申请日：2008-03-06

申请人： Mark Arnold Thomas Blaskovich ,  Ted Baughman ,  Thomas Little ,  Maher Qabar ,  Lauri Marie Schultz ,  Feng Hong ,  William Patt ,  Gangadhar Nagula ,  Jennifer Lynn Gage ,  James Jeffry Howbert

发明人： Mark Arnold Thomas Blaskovich ,  Ted Baughman ,  Thomas Little ,  Maher Qabar ,  Lauri Marie Schultz ,  Feng Hong ,  William Patt ,  Gangadhar Nagula ,  Jennifer Lynn Gage ,  James Jeffry Howbert

IPC分类号： C07F9/02

CPC分类号： C07F9/6541 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/59 ,  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。

公开(公告)号：US20090131374A1

公开(公告)日：2009-05-21

申请号：US12363422

申请日：2009-01-30

申请人： Mark Arnold Thomas Blaskovich ,  Ted Baughman ,  Thomas Little ,  William Patt ,  Maher Qabar ,  Lauri Marie Schultz ,  Feng Hong ,  Gangadhar Nagula ,  Jennifer Lynn Gage ,  James Jeffry Howbert

发明人： Mark Arnold Thomas Blaskovich ,  Ted Baughman ,  Thomas Little ,  William Patt ,  Maher Qabar ,  Lauri Marie Schultz ,  Feng Hong ,  Gangadhar Nagula ,  Jennifer Lynn Gage ,  James Jeffry Howbert

IPC分类号： A61K31/662 ,  A61P3/10

CPC分类号： C07F9/6541 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/59 ,  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。

公开(公告)号：US07504389B2

公开(公告)日：2009-03-17

申请号：US11280724

申请日：2005-11-15

申请人： Mark Arnold Thomas Blaskovich ,  Ted Baughman ,  Thomas Little ,  William Patt ,  Maher Qabar ,  Lauri Mario Schultz ,  Gangadhar Nagula ,  Jennifer Lynn Gage ,  James Jeffry Howbert

发明人： Mark Arnold Thomas Blaskovich ,  Ted Baughman ,  Thomas Little ,  William Patt ,  Maher Qabar ,  Lauri Mario Schultz ,  Gangadhar Nagula ,  Jennifer Lynn Gage ,  James Jeffry Howbert

IPC分类号： A61K31/66 ,  C07F9/02

CPC分类号： C07F9/6541 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/59 ,  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。

公开(公告)号：US20060142250A1

公开(公告)日：2006-06-29

申请号：US11280724

申请日：2005-11-15

申请人： Mark Blaskovich ,  Ted Baughman ,  Thomas Little ,  William Patt ,  Maher Qabar ,  Lauri Schultz ,  Feng Hong ,  Gangadhar Nagula ,  Jennifer Gage ,  James Howbert

发明人： Mark Blaskovich ,  Ted Baughman ,  Thomas Little ,  William Patt ,  Maher Qabar ,  Lauri Schultz ,  Feng Hong ,  Gangadhar Nagula ,  Jennifer Gage ,  James Howbert

IPC分类号： A61K31/675 ,  A61K31/66

CPC分类号： C07F9/6541 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/59 ,  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.

公开(公告)号：US20050250780A1

公开(公告)日：2005-11-10

申请号：US11108267

申请日：2005-04-18

申请人： Maher Qabar ,  Marcin Stasiak ,  Jessymol Mathew ,  Thomas Little ,  Danwen Huang

发明人： Maher Qabar ,  Marcin Stasiak ,  Jessymol Mathew ,  Thomas Little ,  Danwen Huang

IPC分类号： A61K31/525 ,  A61P29/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： Reverse-turn mimetics and methods relating to the same having the following structure are disclosed: including pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3 and R4 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： 公开了具有下列结构的逆转模拟物及其相关方法：包括其药学上可接受的盐和立体异构体，其中R 1，R 2，R 2， 3＆gt;和R 4＆gt;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。

公开(公告)号：US20060293372A1

公开(公告)日：2006-12-28

申请号：US10774043

申请日：2004-02-05

申请人： Maher Qabar ,  Michael McMillan ,  Michael Kahn ,  John Tulinsky ,  Cyprian Ogbu ,  Jessymol Mathew

发明人： Maher Qabar ,  Michael McMillan ,  Michael Kahn ,  John Tulinsky ,  Cyprian Ogbu ,  Jessymol Mathew

IPC分类号： A61K31/43 ,  A61K31/424 ,  A61K31/4196

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： β-sheet mimetics and methods relating to the same are disclosed. The β-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 β-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.