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1.发明申请Rage Antagonists As Agents To Reverse Amyloidosis And Diseases Associated Therewith 审中-公开愤怒的拮抗剂作为反应与之相关的淀粉样变性和疾病的药物公开(公告)号：US20090035302A1
公开(公告)日：2009-02-05
申请号：US12238087
申请日：2008-09-25
IPC分类号： A61K39/395 , A61K31/4164 , A61K31/4184 , A61K31/16 , A61K38/00
CPC分类号： A61K31/4164 , A61K31/4184 , A61K31/425
摘要： Disclosed are RAGE antagonist compounds that have the ability to reverse pre-existing amyloidosis. Treatment with the RAGE antagonist compounds described herein may be used to reduce plaque size and improve cognition for subjects in the later stages of Alzheimer's disease. Additionally, the RAGE antagonists described herein may be used to reduce the onset of plaque formation and thereby prevent loss of cognition and other symptoms associated with Alzheimer's Disease and other diseases of amyloid deposition.
摘要翻译： 公开了具有逆转预先存在的淀粉样变性的能力的RAGE拮抗剂化合物。 本文所述的RAGE拮抗剂化合物的治疗可用于减少斑块大小并改善阿尔茨海默病后期受试者的认知。 此外，本文所述的RAGE拮抗剂可用于减少斑块形成的发作，从而防止与阿尔茨海默病和其他淀粉样蛋白沉积疾病相关的认知和其它症状的丧失。
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公开(公告)号：US07122580B2
公开(公告)日：2006-10-17
申请号：US10637900
申请日：2003-08-08
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Xiao-Chuan Guo , Daniel Peter Christen , Devi Reddy Gohimmukkula , Guoxiang Huang , Robert Rothlein , Sameer Tyagi , Tripura Yaramasu , Christopher Behme
发明人： Adnan M. M. Mjalli , Robert C. Andrews , Xiao-Chuan Guo , Daniel Peter Christen , Devi Reddy Gohimmukkula , Guoxiang Huang , Robert Rothlein , Sameer Tyagi , Tripura Yaramasu , Christopher Behme
IPC分类号： A61K31/245 , C07C233/87
CPC分类号： C07D207/267 , C07C233/29 , C07C233/87 , C07C235/42 , C07C235/52 , C07C235/60 , C07C235/66 , C07C237/36 , C07C237/42 , C07C237/44 , C07C255/60 , C07C257/18 , C07C271/20 , C07C271/44 , C07C311/18 , C07C311/19 , C07C311/44 , C07C317/14 , C07C317/28 , C07C317/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D207/09 , C07D211/26 , C07D213/30 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/81 , C07D217/02 , C07D217/16 , C07D217/22 , C07D231/12 , C07D231/14 , C07D231/18 , C07D233/84 , C07D239/94 , C07D249/08 , C07D261/10 , C07D263/32 , C07D271/10 , C07D277/46 , C07D285/08 , C07D295/088 , C07D295/155 , C07D307/66 , C07D307/79 , C07D307/85 , C07D317/60 , C07D333/24 , C07D333/38 , C07D333/70 , C07D401/04 , C07D409/04 , C07D409/06 , C07D413/04
摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as antagonists, or more preferably, partial antagonist of factor IX and thus, may be used to inhibit the intrinsic pathway of blood coagulation. The compounds are useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway utilizing factor IX. Such diseases or disease states include stroke, myocardial infarction, aneurysm surgery, and deep vein thrombosis associated with surgical procedures, long periods of confinement, and acquired or inherited pro-coagulant states.
摘要翻译： 本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作拮抗剂，或更优选为因子IX的部分拮抗剂，因此可用于抑制血液凝固的内在途径。 该化合物可用于各种应用，包括通过利用因子IX的内在凝血途径部分引起的疾病的管理，治疗和/或控制。 这些疾病或疾病状态包括中风，心肌梗死，动脉瘤手术以及与外科手术相关的深部静脉血栓形成，长时间的约束，以及获得性或遗传的促凝血状态。
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公开(公告)号：US07544699B2
公开(公告)日：2009-06-09
申请号：US10913168
申请日：2004-08-06
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Xiao-Chuan Guo , Daniel Peter Christen , Devi Reddy Gohimmukkula , Guoxiang Huang , Robert Rothlein , Sameer Tyagi , Tripura Yaramasu , Christopher Behme
发明人： Adnan M. M. Mjalli , Robert C. Andrews , Xiao-Chuan Guo , Daniel Peter Christen , Devi Reddy Gohimmukkula , Guoxiang Huang , Robert Rothlein , Sameer Tyagi , Tripura Yaramasu , Christopher Behme
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D295/155 , C07C233/87 , C07C235/42 , C07C235/52 , C07C235/60 , C07C235/66 , C07C237/36 , C07C237/42 , C07C271/20 , C07C311/08 , C07C311/09 , C07C311/21 , C07C311/44 , C07C317/32 , C07C323/36 , C07C2601/08
摘要： This invention provides aryl and heteroaryl compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention may be antagonists, or partial antagonist of factor IX and/or factor XI and thus, may be useful for inhibiting the intrinsic pathway of blood coagulation. The compounds may be useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway.
摘要翻译： 本发明提供芳基和杂芳基化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物病症中的用途。 本发明的化合物可以是拮抗剂或因子IX和/或因子XI的部分拮抗剂，因此可用于抑制凝血的内在途径。 所述化合物可用于各种应用，包括部分由内在凝血途径引起的疾病的管理，治疗和/或控制。
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公开(公告)号：US06933303B2
公开(公告)日：2005-08-23
申请号：US10274546
申请日：2002-10-18
IPC分类号： A61K31/437 , A61K31/573 , A61K31/64 , A61K38/28 , A61K45/00 , A61P3/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/10 , A61P17/06 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.
摘要翻译： 本发明提供可用作蛋白酪氨酸磷酸酶（PTPases）抑制剂的化合物。 作为PTPase的抑制剂，本发明的化合物可用于由PTPase活性介导的疾病的治疗，治疗，控制和辅助治疗。 这些疾病包括I型糖尿病，II型糖尿病，免疫功能障碍，AIDS，自身免疫，葡萄糖不耐受，肥胖症，癌症，牛皮癣，过敏性疾病，感染性疾病，炎症性疾病，涉及调节生长激素合成的疾病或生长调节合成 影响生长激素或阿尔茨海默病生产的因子或细胞因子。
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公开(公告)号：US20110077399A1
公开(公告)日：2011-03-31
申请号：US12958237
申请日：2010-12-01
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Ravindra R. Yarragunta , Rongyuan Xie , Govindan Subramanian , James C. Quada, JR. , Murty N. Arimilli , Dharma R. Polisetti
发明人： Adnan M. M. Mjalli , Robert C. Andrews , Ravindra R. Yarragunta , Rongyuan Xie , Govindan Subramanian , James C. Quada, JR. , Murty N. Arimilli , Dharma R. Polisetti
IPC分类号： C07D413/04 , C07D233/64 , C07D405/10 , C07D401/04
CPC分类号： C07D417/12 , C07D233/54 , C07D263/32 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12 , C07D413/04
摘要： This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.
摘要翻译： 本发明提供可用作蛋白酪氨酸磷酸酶（PTPases）的抑制剂的唑类。 本发明提供式（I）化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作蛋白酪氨酸磷酸酶的抑制剂，因此可用于由PTPase活性介导的疾病的管理，治疗，控制和辅助治疗。 这些疾病包括I型糖尿病，II型糖尿病。
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6.发明授权Substituted imidazole derivatives, compositions, and methods of use as PTPase inhibitors 有权取代的咪唑衍生物，组合物和作为PTPase抑制剂的方法公开(公告)号：US07723369B2
公开(公告)日：2010-05-25
申请号：US11699780
申请日：2007-01-30
申请人： Adnan M. M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
发明人： Adnan M. M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
IPC分类号： A61K31/4178 , C07D233/64
CPC分类号： C07D417/14 , C07D417/10
摘要： The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
摘要翻译： 本发明提供式（I-IV）的咪唑衍生物，其制备方法，包含式（I-IV）化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物抑制蛋白酪氨酸磷酸酶1B，因此可用于对由PTPase活性介导的疾病的治疗，治疗，控制或辅助治疗。 这些疾病包括I型糖尿病和II型糖尿病。
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公开(公告)号：US08877192B2
公开(公告)日：2014-11-04
申请号：US12983604
申请日：2011-01-03
IPC分类号： A61K38/00 , C07K14/705
CPC分类号： C07K14/705 , A61K38/00
摘要： Disclosed are RAGE fusion proteins comprising RAGE polypeptide sequences linked to a second, non-RAGE polypeptide. The RAGE fusion protein may utilize a RAGE polypeptide domain comprising a RAGE ligand binding site and an interdomain linker directly linked to an immunoglobulin CH2 domain. Such fusion proteins may provide specific, high affinity binding to RAGE ligands. Also disclosed is the use of the RAGE fusion proteins as therapeutics for RAGE-mediated pathologies.
摘要翻译： 公开了包含与第二非RAGE多肽连接的RAGE多肽序列的RAGE融合蛋白。 RAGE融合蛋白可以利用包含RAGE配体结合位点和直接连接到免疫球蛋白CH2结构域的域间连接体的RAGE多肽结构域。 这样的融合蛋白可以提供与RAGE配体的特异的高亲和力结合。 还公开了RAGE融合蛋白作为RAGE介导的病理学的治疗剂的用途。
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公开(公告)号：US07901688B2
公开(公告)日：2011-03-08
申请号：US11197038
申请日：2005-08-03
CPC分类号： C07K14/705 , A61K38/00
摘要： Disclosed are RAGE fusion proteins comprising RAGE polypeptide sequences linked to a second, non-RAGE polypeptide. The RAGE fusion protein may utilize a RAGE polypeptide domain comprising a RAGE ligand binding site and an interdomain linker directly linked to an immunoglobulin CH2 domain. Such fusion proteins may provide specific, high affinity binding to RAGE ligands. Also disclosed is the use of the RAGE fusion proteins as therapeutics for RAGE-mediated pathologies.
摘要翻译： 公开了包含与第二非RAGE多肽连接的RAGE多肽序列的RAGE融合蛋白。 RAGE融合蛋白可以利用包含RAGE配体结合位点和直接连接到免疫球蛋白CH2结构域的域间连接体的RAGE多肽结构域。 这样的融合蛋白可以提供与RAGE配体的特异的高亲和力结合。 还公开了RAGE融合蛋白作为RAGE介导的病理学的治疗剂的用途。
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公开(公告)号：US08344120B2
公开(公告)日：2013-01-01
申请号：US13158748
申请日：2011-06-13
IPC分类号： C07H21/04
CPC分类号： C07K14/70503 , A61K38/00 , C07K2319/30 , C12N15/62
摘要： Disclosed are RAGE fusion proteins comprising RAGE polypeptide sequences linked to a second, non-RAGE polypeptide. The RAGE fusion protein may utilize a RAGE polypeptide domain comprising a RAGE ligand binding site and an interdomain linker directly linked to the N-terminus of an immunoglobulin CH2 domain. Also disclosed are RAGE fusion protein formulations and the use of the RAGE fusion proteins and RAGE fusion protein formulations as therapeutics for RAGE-mediated pathologies.
摘要翻译： 公开了包含与第二非RAGE多肽连接的RAGE多肽序列的RAGE融合蛋白。 RAGE融合蛋白可以利用包含RAGE配体结合位点的RAGE多肽结构域和直接连接到免疫球蛋白CH2结构域的N末端的域间连接。 还公开了RAGE融合蛋白制剂以及使用RAGE融合蛋白和RAGE融合蛋白制剂作为RAGE介导的病理学的治疗剂。
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公开(公告)号：US07981424B2
公开(公告)日：2011-07-19
申请号：US11789637
申请日：2007-04-25
CPC分类号： C07K14/70503 , A61K38/00 , C07K2319/30 , C12N15/62
摘要： Disclosed are RAGE fusion proteins comprising RAGE polypeptide sequences linked to a second, non-RAGE polypeptide. The RAGE fusion protein may utilize a RAGE polypeptide domain comprising a RAGE ligand binding site and an interdomain linker directly linked to the N-terminus of an immunoglobulin CH2 domain. Also disclosed are RAGE fusion protein formulations and the use of the RAGE fusion proteins and RAGE fusion protein formulations as therapeutics for RAGE-mediated pathologies.
摘要翻译： 公开了包含与第二非RAGE多肽连接的RAGE多肽序列的RAGE融合蛋白。 RAGE融合蛋白可以利用包含RAGE配体结合位点的RAGE多肽结构域和直接连接到免疫球蛋白CH2结构域的N末端的域间连接。 还公开了RAGE融合蛋白制剂以及使用RAGE融合蛋白和RAGE融合蛋白制剂作为RAGE介导的病理学的治疗剂。
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