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1. 发明申请

US20060063798A1 Heterocyclic aromatic compounds useful as growth hormone secretagogues 有权
标题翻译：用作生长激素促分泌素的杂环芳族化合物
公开(公告)号：US20060063798A1
公开(公告)日：2006-03-23
申请号：US11272898
申请日：2005-11-14
申请人： Guixue Yu , Jun Li , William Ewing , Richard Sulsky , James Li , Joseph Tino
发明人： Guixue Yu , Jun Li , William Ewing , Richard Sulsky , James Li , Joseph Tino
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D487/04 , C07D231/56 , C07D261/20 , C07D471/04 , C07D513/04
摘要： Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1′, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
摘要翻译：提供了可用于刺激生长激素的内源性产生或释放的新型杂环芳族化合物，所述化合物具有式I的通式结构

2. 发明申请

US20050065156A1 Compounds useful as motilin agonists and method 有权
标题翻译：可用作胃动素激动剂和方法的化合物
公开(公告)号：US20050065156A1
公开(公告)日：2005-03-24
申请号：US10940241
申请日：2004-09-14
申请人： James Li , Hannguang Chao , Joseph Tino , William Ewing
发明人： James Li , Hannguang Chao , Joseph Tino , William Ewing
IPC分类号： A61K31/503 , C07D471/20 , C07D487/14
CPC分类号： C07D471/20 , A61K31/503
摘要： A method is provided for treating disorders of gastrointestinal motility which include the steps of administering to a patient in need of treatment of a compound having the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 is selected from alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from —CON(R4)R4a, —SO2N(R4)R4a, —CN, and R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle; R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. New compounds for use in treating disorders of gastrointestinal motility are also provided.
摘要翻译：提供了一种治疗胃肠蠕动障碍的方法，其包括对需要治疗具有其结构或其药学上可接受的盐的化合物，其前药酯及其所有立体异构体的患者给药的步骤，其中选择R1 烷基，芳基，环烷基，烯基，炔基，芳基烷基，杂芳基，杂芳基烷基或杂环烷基; Z选自-CON（R4）R4a，-SO2N（R4）R4a，-CN，R4和R4a相同或不同，独立地选自氢，烷基，环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基或 R4和R4a可以连接在一起形成杂环; R4b选自氢，卤素，羟基，CN，OCF3，CF3，CONH2，SONH2，SO2CH3，NHCOCH3或NHCO2CH3; Q是取代的双环杂环。还提供了用于治疗胃肠蠕动障碍的新化合物。

3. 发明申请

US20080009533A1 SUBSTITUTED ACID DERIVATIVES USEFUL AS ANTI-ATHEROSCLEROTIC, ANTI-DYSLIPIDEMIC, ANTI-DIABETIC AND ANTI-OBESITY AGENTS AND METHOD 有权
标题翻译：取代的酸衍生物有助于抗甲状腺激素，抗血糖，抗糖尿病和抗胆碱药物和方法
公开(公告)号：US20080009533A1
公开(公告)日：2008-01-10
申请号：US11773545
申请日：2007-07-05
申请人： Joseph Tino , Peter Cheng , Yan Shi , Jun Li , Ranjan Mukherjee
发明人： Joseph Tino , Peter Cheng , Yan Shi , Jun Li , Ranjan Mukherjee
IPC分类号： A61K31/421 , A61P3/08 , C07D263/30
CPC分类号： C07D263/32
摘要： Compounds are provided which have the structure of Formula (I): wherein R1 is halogen; and X is hydrogen or halogen, and salts thereof, which compounds are useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic, and anti-obesity agents.
摘要翻译：提供具有式（I）结构的化合物：其中R 1是卤素; 并且X是氢或卤素，及其盐，该化合物可用作抗动脉粥样硬化，抗血脂异常，抗糖尿病和抗肥胖剂。

4. 发明申请

US20050154043A1 Heterocyclic compounds useful as growth hormone secretagogues 有权
标题翻译：用作生长激素促分泌素的杂环化合物
公开(公告)号：US20050154043A1
公开(公告)日：2005-07-14
申请号：US11033649
申请日：2005-01-12
申请人： Weixu Zhai , Samuel Gerritz , Charles Andres , Joseph Tino
发明人： Weixu Zhai , Samuel Gerritz , Charles Andres , Joseph Tino
IPC分类号： A61K31/40 , C07D207/09 , C07D207/30
CPC分类号： C07D207/09
摘要： The present invention relates to novel heterocyclic compounds, according to Formula I, that stimulate endogenous production and/or release of growth hormone, wherein R1, R2, R3, R4 and X are defined herein. Further, the present invention relates to methods for using such compounds and to pharmaceutical compositions containing such compounds.
摘要翻译：本发明涉及根据式I的刺激生长激素的内源性产生和/或释放的新型杂环化合物，其中R 1，R 2，R 2 > 3，R 4和X如本文所定义。此外，本发明涉及使用这些化合物的方法和含有这些化合物的药物组合物。

5. 发明申请

US20060079549A1 Heterocyclic aromatic compounds useful as growth hormone secretagogues 有权
标题翻译：用作生长激素促分泌素的杂环芳族化合物
公开(公告)号：US20060079549A1
公开(公告)日：2006-04-13
申请号：US11273169
申请日：2005-11-14
申请人： Guixue Yu , Jun Li , William Ewing , Richard Sulsky , James Li , Joseph Tino
发明人： Guixue Yu , Jun Li , William Ewing , Richard Sulsky , James Li , Joseph Tino
IPC分类号： A61K31/4745
CPC分类号： C07D487/04 , C07D231/56 , C07D261/20 , C07D471/04 , C07D513/04
摘要： Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1′, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
摘要翻译：提供了可用于刺激生长激素的内源性产生或释放的新型杂环芳族化合物，所述化合物具有通式I的通式结构，其中R 1，R 1， R 2，R 3，R 4，Xa，Y，Z和n如本文所述。本文提供的化合物可用于治疗肥胖症，骨质疏松症（改善骨密度）和改善肌肉质量和肌肉力量。

6. 发明申请

US20050080116A1 Compounds useful as motilin agonists and method 有权
标题翻译：可用作胃动素激动剂和方法的化合物
公开(公告)号：US20050080116A1
公开(公告)日：2005-04-14
申请号：US10940240
申请日：2004-09-14
申请人： James Li , Hannguang Chao , Joseph Tino , William Ewing
发明人： James Li , Hannguang Chao , Joseph Tino , William Ewing
IPC分类号： A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/495 , A61K31/50 , C07D413/02 , C07D471/20 , C07D43/02
CPC分类号： C07D471/20 , A61K31/495 , A61K31/50
摘要： Compounds are provided which are useful in treating disorders of gastrointestinal motility and which have the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from —CON(R4)R4a, —CO2R4, —SO2N(R4)R4a, —SO2R4, CN, and R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle. R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. A method for using such compounds for treating disorders of gastrointestinal motility is also provided.
摘要翻译：提供了可用于治疗胃肠蠕动障碍并具有其结构或其药学上可接受的盐，其前药酯及其所有立体异构体的化合物，其中R 1和R 2相同或不同并且独立地选自氢，烷基，芳基，环烷基，烯基，炔基，芳基烷基，杂芳基，杂芳基烷基或杂环烷基; Z选自-CON（R4）R4a，-CO2R4，-SO2N（R4）R4a，-SO2R4，CN和R4和R4a相同或不同，独立地选自氢，烷基，环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基或R4和R4a可以连接在一起形成杂环。 R4b选自氢，卤素，羟基，CN，OCF3，CF3，CONH2，SONH2，SO2CH3，NHCOCH3或NHCO2CH3; Q是取代的双环杂环。还提供了使用这些化合物治疗胃肠蠕动障碍的方法。

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