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1. 发明申请

US20070099835A1 Sustained release GLP-1 receptor modulators 有权
标题翻译：缓释GLP-1受体调节剂
公开(公告)号：US20070099835A1
公开(公告)日：2007-05-03
申请号：US11594531
申请日：2006-11-08
申请人： Feng Qian , William Ewing , Claudio Mapelli , Douglas Riexinger , Ving Lee , Richard Sulsky , Yeheng Zhu , Tasir Haque , Rogelio Martinez , Vijay Naringrekar , Nina Ni , Lori Burton
发明人： Feng Qian , William Ewing , Claudio Mapelli , Douglas Riexinger , Ving Lee , Richard Sulsky , Yeheng Zhu , Tasir Haque , Rogelio Martinez , Vijay Naringrekar , Nina Ni , Lori Burton
IPC分类号： A61K38/26
CPC分类号： A61K38/26
摘要： The present invention provides novel pharmaceutical compositions comprising a human glucagon-like peptide-1 (GLP-1)-receptor modulator as an active ingredient in a sustained release formulation.
摘要翻译：本发明提供了包含人胰高血糖素样肽-1（GLP-1） - 受体调节剂作为持续释放制剂中的活性成分的新型药物组合物。

2. 发明申请

US20060287242A1 Human glucagon-like-peptide-1 modulators and their use in treatment of diabetes and related conditions 有权
标题翻译：人胰高血糖素样肽-1调节剂及其在治疗糖尿病和相关病症中的应用
公开(公告)号：US20060287242A1
公开(公告)日：2006-12-21
申请号：US11170968
申请日：2005-06-30
申请人： William Ewing , Claudio Mapelli , Richard Sulsky , Tasir Haque , Ving Lee , Douglas Riexinger , Rogelio Martinez , Yeheng Zhu
发明人： William Ewing , Claudio Mapelli , Richard Sulsky , Tasir Haque , Ving Lee , Douglas Riexinger , Rogelio Martinez , Yeheng Zhu
IPC分类号： A61K38/10 , C07K7/08
CPC分类号： C07K7/06 , A61K38/00 , C07K14/605
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
摘要翻译：本发明提供了具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1） - 受体调节剂，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。本发明的肽在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。

3. 发明申请

US20070238669A1 HUMAN GLUCAGON-LIKE-PEPTIDE-1 MODULATORS AND THEIR USE IN THE TREATMENT OF DIABETES RELATED CONDITIONS 审中-公开
标题翻译：人类GLUCAGON-PEPTIDE-1调节剂及其在治疗糖尿病相关情况中的应用
公开(公告)号：US20070238669A1
公开(公告)日：2007-10-11
申请号：US11622142
申请日：2007-01-11
申请人： Tasir Haque , William Ewing , Claudio Mapelli , Ving Lee , Richard Sulsky , Douglas Riexinger , Rogelio Martinez , Yeheng Zhu , Zheming Ruan
发明人： Tasir Haque , William Ewing , Claudio Mapelli , Ving Lee , Richard Sulsky , Douglas Riexinger , Rogelio Martinez , Yeheng Zhu , Zheming Ruan
IPC分类号： A61K38/00 , C07C233/00 , C07C321/00 , C07K7/00
CPC分类号： C07K14/605 , A61K38/26 , A61K38/28 , C07C271/16 , C07C2603/18 , A61K2300/00
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified compounds that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The compounds of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
摘要翻译：本发明提供了具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1） - 受体调节剂，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的化合物，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。本发明的化合物在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。

4. 发明授权

US07119105B2 Methods for treating neurodegenerative disorders using aspartyl protease inhibitors 失效
标题翻译：使用天冬氨酰蛋白酶抑制剂治疗神经变性疾病的方法
公开(公告)号：US07119105B2
公开(公告)日：2006-10-10
申请号：US10774262
申请日：2004-02-05
申请人： Jonathan A. Ellman , Gary Lynch , Irwin D. Kuntz , Xiaoning Bi , Christina E. Lee , A. Geoffrey Skillman , Tasir Haque
发明人： Jonathan A. Ellman , Gary Lynch , Irwin D. Kuntz , Xiaoning Bi , Christina E. Lee , A. Geoffrey Skillman , Tasir Haque
IPC分类号： A99Z99/00
CPC分类号： C07D209/48 , A61K31/36 , A61K31/4035 , A61K31/423 , A61K31/445 , A61K31/4465 , A61K31/4525 , A61K31/454 , C07D263/58 , C07D317/58 , C07D317/60 , C07D317/62 , C07D405/12 , C07D413/12 , C07D413/14
摘要： The present invention relates to () non-peptide aspartyl protease inhibitors; (ii) methods for modulating the processing of an amyloid precursor protein (APP); (iii) methods for modulating the processing of a tau protein (τ-protein); and (iv) methods for treating neurodegenerative diseases. For instance, in one embodiment, the present invention provides a method for modulating the processing of an amyloid precursor protein (APP), the method comprising contacting a composition containing the APP with an aspartyl protease inhibitor having the formula: wherein: R1, R2 and R3 are members independently selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl, substituted aryloxyalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, heterocycles, substituted heterocycles, heterocyclicalkyl and substituted heterocyclicalkyl; and R5 and R6 are independently selected from the group consisting of hydrogen, halogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl and substituted aryloxyalkyl; or R5 and R6 and the carbons to which they are bound join to form an optionally substituted carbocyclic or heterocyclic fused ring system having a total of 9- or 10-ring atoms within the fused ring system.
摘要翻译：本发明涉及（）非肽天冬氨酰蛋白酶抑制剂; （ii）调节淀粉样蛋白前体蛋白（APP）的加工的方法; （iii）调节tau蛋白（tau蛋白）的加工的方法; 和（iv）治疗神经变性疾病的方法。例如，在一个实施方案中，本发明提供了调节淀粉样蛋白前体蛋白（APP）的加工的方法，所述方法包括将含有APP的组合物与具有下式的天冬氨酰蛋白酶抑制剂接触：其中： 1，R 2和R 3是独立地选自烷基，取代的烷基，芳基，取代的芳基，芳基烷基，取代的芳基烷基，芳氧基烷基取代的芳氧基烷基，杂芳基，取代的杂芳基，杂芳基烷基，取代的杂芳基烷基，杂环，取代的杂环，杂环烷基和取代的杂环烷基; R 5和R 6独立地选自氢，卤素，烷基，取代的烷基，芳基，取代的芳基，芳基烷基，取代的芳基烷基，芳氧基烷基和取代的芳氧基烷基; 或R 5和R 6和它们所连接的碳原子连接形成任选取代的碳环或杂环稠环体系，其具有总共9或10环稠环体系内的原子。

5. 发明申请

US20060089496A1 Pyrazolobenzamides and derivatives as factor Xa inhibitors 有权
标题翻译：吡唑并吡嗪类和衍生物作为因子Xa抑制剂
公开(公告)号：US20060089496A1
公开(公告)日：2006-04-27
申请号：US11256893
申请日：2005-10-24
申请人： Patrick Lam , Charles Clark , Renhua Li , Tasir Haque , Karen Rossi
发明人： Patrick Lam , Charles Clark , Renhua Li , Tasir Haque , Karen Rossi
IPC分类号： C07D471/02 , C07D487/02
CPC分类号： C07D403/12 , C07D231/14 , C07D471/04
摘要： The present application describes pyrazolobenzamides and derivatives thereof of Formula I: P4-P-M-M4 I or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译：本申请描述了式I的吡唑并苯并酰胺及其衍生物：<？in-line-formula description =“In-line Formulas”end =“lead”→> P 或者其药学上可接受的盐形式。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

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