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1.发明申请公开(公告)号：US20060148822A1
公开(公告)日：2006-07-06
申请号：US10547691
申请日：2004-03-05
申请人： Graham Bloomfield , Ian Bruce , Catherine Leblanc , Mrinalini Oza , Lewis Whithead , Bernard Cuenoud , Thomas Keller , Louise Kirman , Clive McCarthy , Gaynor Woodward
发明人： Graham Bloomfield , Ian Bruce , Catherine Leblanc , Mrinalini Oza , Lewis Whithead , Bernard Cuenoud , Thomas Keller , Louise Kirman , Clive McCarthy , Gaynor Woodward
IPC分类号： C07D417/02 , A61K31/497 , A61K31/4439
CPC分类号： C07D417/14 , C07D277/42 , C07D417/12
摘要： Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 游离或盐形式的式I化合物，其中R 1，R 2，R 3，R 4， 和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。
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公开(公告)号：US20050119320A1
公开(公告)日：2005-06-02
申请号：US10504259
申请日：2003-02-27
申请人： Ian Bruce , Peter Finan , Catherine Leblanc , Clive McCarthy , Lewis Whitehead , Nicola Press , Graham Bloomfield , Judy Hayler , Louise Kirman , Mrinalini Oza , Lena Shukla
发明人： Ian Bruce , Peter Finan , Catherine Leblanc , Clive McCarthy , Lewis Whitehead , Nicola Press , Graham Bloomfield , Judy Hayler , Louise Kirman , Mrinalini Oza , Lena Shukla
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61P1/04 , A61P3/04 , A61P3/10 , A61P7/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/48 , C07D417/04 , C07D417/12 , C07D417/02 , C07D277/18
CPC分类号： C07D277/40 , C07D277/46 , C07D277/48 , C07D417/04 , C07D417/12
摘要： Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 游离或盐形式的式I化合物，其中R 1，R 2，R 3，R 4， 和R 5具有如说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。
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3.发明授权公开(公告)号：US08017608B2
公开(公告)日：2011-09-13
申请号：US10547691
申请日：2004-03-05
申请人： Graham Charles Bloomfield , Ian Bruce , Catherine Leblanc , Mrinalini Sachin Oza , Lewis Whithead , Bernard Cuenoud , Thomas Hugo Keller , Louise Kirman , Clive McCarthy , Gaynor Elizabeth Woodward
发明人： Graham Charles Bloomfield , Ian Bruce , Catherine Leblanc , Mrinalini Sachin Oza , Lewis Whithead , Bernard Cuenoud , Thomas Hugo Keller , Louise Kirman , Clive McCarthy , Gaynor Elizabeth Woodward
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/506 , A61K31/4523 , A61K31/41 , A61K31/426 , A61K31/427 , C07D413/02 , C07D401/02 , C07D403/02 , C07D285/12
CPC分类号： C07D417/14 , C07D277/42 , C07D417/12
摘要： Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 游离或盐形式的式I化合物，其中R 1，R 2，R 3，R 4和R 5具有说明书中指出的含义，可用于治疗由磷脂酰肌醇3-激酶介导的疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。
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公开(公告)号：US08129541B2
公开(公告)日：2012-03-06
申请号：US12640479
申请日：2009-12-17
申请人： Ian Bruce , Peter Finan , Catherine LeBlanc , Clive McCarthy , Lewis Whitehead , Nicola Press , Graham Charles Bloomfield , Judy Hayler , Louise Kirman , Mrinalini Sachin Oza , Lena Shukla
发明人： Ian Bruce , Peter Finan , Catherine LeBlanc , Clive McCarthy , Lewis Whitehead , Nicola Press , Graham Charles Bloomfield , Judy Hayler , Louise Kirman , Mrinalini Sachin Oza , Lena Shukla
IPC分类号： A61K31/426 , C07D277/46
CPC分类号： C07D277/40 , C07D277/46 , C07D277/48 , C07D417/04 , C07D417/12
摘要： Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 游离或盐形式的式I化合物，其中R 1，R 2，R 3，R 4和R 5具有说明书中指出的含义，可用于治疗由磷脂酰肌醇3-激酶介导的疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。
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公开(公告)号：US20100093690A1
公开(公告)日：2010-04-15
申请号：US12640479
申请日：2009-12-17
申请人： Ian Bruce , Peter Finan , Catherine LeBlanc , Clive McCarthy , Lewis Whitehead , Nicola Press , Graham Charles Bloomfield , Judy Hayler , Louise Kirman , Mrinalini Sachin Oza , Lena Shukla
发明人： Ian Bruce , Peter Finan , Catherine LeBlanc , Clive McCarthy , Lewis Whitehead , Nicola Press , Graham Charles Bloomfield , Judy Hayler , Louise Kirman , Mrinalini Sachin Oza , Lena Shukla
IPC分类号： A61K31/397 , C07D277/20 , A61K31/426 , C07D417/02 , A61K31/496 , A61K31/4436 , C07D413/14 , A61K31/5377 , A61P35/00 , A61P11/00
CPC分类号： C07D277/40 , C07D277/46 , C07D277/48 , C07D417/04 , C07D417/12
摘要： Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 游离或盐形式的式I化合物，其中R 1，R 2，R 3，R 4和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。
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公开(公告)号：US07687637B2
公开(公告)日：2010-03-30
申请号：US10504259
申请日：2003-02-27
申请人： Ian Bruce , Peter Finan , Catherine Leblanc , Clive McCarthy , Lewis Whitehead , Nicola Press , Graham Charles Bloomfield , Judy Hayler , Louise Kirman , Mrinalini Sachin Oza , Lena Shukla
发明人： Ian Bruce , Peter Finan , Catherine Leblanc , Clive McCarthy , Lewis Whitehead , Nicola Press , Graham Charles Bloomfield , Judy Hayler , Louise Kirman , Mrinalini Sachin Oza , Lena Shukla
IPC分类号： A61K31/426 , C07D277/46
CPC分类号： C07D277/40 , C07D277/46 , C07D277/48 , C07D417/04 , C07D417/12
摘要： Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 游离或盐形式的式I化合物，其中R 1，R 2，R 3，R 4和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。
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公开(公告)号：US08084448B2
公开(公告)日：2011-12-27
申请号：US12295545
申请日：2007-03-29
申请人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/55 , A61K31/445 , A61K31/41 , C07D487/00 , C07D401/00 , C07D285/10
CPC分类号： C07D285/10 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译： 式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。 本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。 因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症 ，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。 此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，肌肉骨骼，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。
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公开(公告)号：US20090181928A1
公开(公告)日：2009-07-16
申请号：US12295545
申请日：2007-03-29
申请人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/695 , C07D285/10 , A61K31/433 , A61K31/454 , C07D417/10 , C07D417/12 , A61K31/55 , C07F7/10 , A61P3/10
CPC分类号： C07D285/10 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译： 式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。 本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。 因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症 ，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。 此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，肌肉骨骼，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。
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![Thiazolo[5,4-B]pyridine glucokinase activators](/abs-image/US/2012/08/28/US08252931B2/abs.jpg.150x150.jpg)
公开(公告)号：US08252931B2
公开(公告)日：2012-08-28
申请号：US12088594
申请日：2006-09-28
IPC分类号： C07D513/04 , A61K31/4365
CPC分类号： C07D231/40 , C07D213/75 , C07D239/42 , C07D239/84 , C07D241/20 , C07D277/46 , C07D277/82 , C07D285/135 , C07D285/16 , C07D417/12 , C07D513/04
摘要： The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.
摘要翻译： 本发明提供了作为葡萄糖激酶活性的激活剂的下式的化合物，因此可用作治疗葡糖激酶介导的病症的治疗剂。 因此，式（I）化合物可用于预防和治疗葡萄糖耐量异常，2型糖尿病和肥胖症。
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公开(公告)号：US20080312256A1
公开(公告)日：2008-12-18
申请号：US12088594
申请日：2006-09-28
IPC分类号： A61K31/437 , A61P3/00 , A61K31/433 , A61K31/44 , A61K31/428 , A61K31/4164 , A61K31/519 , C07D513/04
CPC分类号： C07D231/40 , C07D213/75 , C07D239/42 , C07D239/84 , C07D241/20 , C07D277/46 , C07D277/82 , C07D285/135 , C07D285/16 , C07D417/12 , C07D513/04
摘要： The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.
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