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1. 发明申请

US20120052130A1 GPR 119 MODULATORS 审中-公开
标题翻译： GPR 119调制器
公开(公告)号：US20120052130A1
公开(公告)日：2012-03-01
申请号：US13318152
申请日：2010-04-12
申请人： Etzer Darout , Michael Paul DeNinno , Kentaro Futatsugi , Cristiano Ruch Werneck Guimaraes , Bruce Allen Lefker , Vincent Mascitti , Kim Francis McClure , Michael John Munchhof , Ralph Pelton Robinson, JR.
发明人： Etzer Darout , Michael Paul DeNinno , Kentaro Futatsugi , Cristiano Ruch Werneck Guimaraes , Bruce Allen Lefker , Vincent Mascitti , Kim Francis McClure , Michael John Munchhof , Ralph Pelton Robinson, JR.
IPC分类号： A61K35/56 , A61K31/506 , A61K31/497 , A61K31/55 , A61K31/536 , A61K31/566 , A61K38/22 , A61K31/4985 , A61K31/4965 , A61K38/16 , A61K31/715 , A61K38/26 , A61K31/513 , A61K31/706 , A61K31/517 , A61P3/10 , A61P3/04 , A61P3/08 , A61P3/06 , A61P9/10 , A61P9/00 , A61P19/02 , A61P19/10 , A61P13/12 , A61P7/02 , A61P25/28 , A61P25/18 , A61P25/00 , A61P1/00 , C07D239/47
CPC分类号： C07D471/04 , C07D401/14 , C07D491/08
摘要： Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPFM 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
摘要翻译：本文描述了调节G-蛋白偶联受体GPFM19的活性的式（I）化合物及其在治疗与动物中G蛋白偶联受体GPR119的调节相关的疾病中的用途。

2. 发明申请

US20120095028A1 3-OXA-7-AZABICYCLO[3.3.1]NONANES 审中-公开
标题翻译： 3-OXA-7-AZABICYCLO [3.3.1] NONANES
公开(公告)号：US20120095028A1
公开(公告)日：2012-04-19
申请号：US13257384
申请日：2010-03-04
申请人： Michael Paul DeNinno , Kentaro Futatsugi , Bruce Allen Lefker , Vincent Mascitti , Kim Francis McClure , Michael John Munchhof
发明人： Michael Paul DeNinno , Kentaro Futatsugi , Bruce Allen Lefker , Vincent Mascitti , Kim Francis McClure , Michael John Munchhof
IPC分类号： A61K31/519 , A61P13/00 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P19/02 , A61P19/10 , A61P9/12 , A61P13/12 , A61P15/00 , A61P9/10 , A61P15/10 , A61P17/00 , A61P25/28 , A61P25/18 , A61P1/00 , C07D471/04
CPC分类号： C07D491/08 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
摘要翻译：本文描述了调节G-蛋白偶联受体GPR119的活性的式（I）化合物及其在治疗与动物中G蛋白偶联受体GPR119的调节相关的疾病中的用途。

3. 再颁专利

USRE38524E1 Dipeptide derivatives as growth hormone secretagogues 失效
标题翻译：二肽衍生物作为生长激素促分泌素
公开(公告)号：USRE38524E1
公开(公告)日：2004-06-01
申请号：US10270816
申请日：2002-10-15
申请人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
发明人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
IPC分类号： A61K31517
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

4. 发明授权

US06248717B1 Tartrate salt of a substituted dipeptide as growth hormone secretagogue 有权
标题翻译：取代二肽的酒石酸盐作为生长激素促分泌素
公开(公告)号：US06248717B1
公开(公告)日：2001-06-19
申请号：US09380886
申请日：1999-09-07
申请人： Philip Albert Carpino , Paul Andrew Dasilva-Jardine , Bruce Allen Lefker , Jerry Anthony Murry
发明人： Philip Albert Carpino , Paul Andrew Dasilva-Jardine , Bruce Allen Lefker , Jerry Anthony Murry
IPC分类号： A61K3805
CPC分类号： C07D401/06 , A61K38/06 , C07D471/04 , C07K5/0202 , C07K5/06191 , Y02P20/55 , A61K2300/00
摘要： This invention is directed to the (L)-tartaric acid salt of 2-amino-N-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo{4,3-c}pyridin-5-yl]-ethyl]-2-methyl-propionamide which is a growth hormone secretagogue and as such is useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compound. The (L)-tartaric acid salt of the compound of this invention is useful in the treatment and/or prevention of osteoporosis, insulin resistance and other conditions or diseases associated with growth hormone deficiency. The (L)-tartaric acid salt of the compound of the present invention is also useful in treating osteoporosis when used in combination with: a bisphosphonate compound; estrogen, Premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin. Further, the present invention is directed to pharmaceutical compositions. This invention is further directed to methods comprising administering to a human or other animal a combination of an alpha-2 adrenergic agonist and the (L)-tartaric acid salt of the compound of this invention.
摘要翻译：本发明涉及2-氨基-N- {1-（2,4-二氟 - 苄氧基甲基）-2-氧代-2- [3-氧代-3a-吡啶-2-基] （2,2,2-三氟 - 乙基）-2,3,3a，4,6,7-六氢 - 吡唑并[4,3-c]吡啶-5-基] - 乙基] -2- 作为生长激素促分泌素的甲基丙酰胺，因此可用于增加内源性生长激素的水平。在另一方面，本发明提供了可用于合成前述化合物的某些中间体。本发明化合物的（L） - 酒石酸盐可用于治疗和/或预防与生长激素缺乏相关的骨质疏松症，胰岛素抵抗和其它病症或疾病。本发明化合物的（L） - 酒石酸盐与二膦酸盐化合物组合使用时也可用于治疗骨质疏松症。雌激素，孕激素，以及孕激素; 雌激素激动剂或拮抗剂; 或降钙素。此外，本发明涉及药物组合物。本发明进一步涉及包括向人或其他动物施用α-2肾上腺素能激动剂和本发明化合物的（L） - 酒石酸盐的组合的方法。

5. 发明申请

US20090105349A1 ANDROGEN MODULATORS 审中-公开
标题翻译：安德鲁调制器
公开(公告)号：US20090105349A1
公开(公告)日：2009-04-23
申请号：US11572760
申请日：2005-08-08
申请人： Nicole Chantel Barvian , Daniel Yunlong Du , Lain-Yen Hu , Donna Michele Iula , Bruce Allen Lefker , Huangshu Lei , Raj Kumar Raheja , Yvonne Dorothy Smith
发明人： Nicole Chantel Barvian , Daniel Yunlong Du , Lain-Yen Hu , Donna Michele Iula , Bruce Allen Lefker , Huangshu Lei , Raj Kumar Raheja , Yvonne Dorothy Smith
IPC分类号： A61K31/135 , A61P5/26
CPC分类号： A61K31/275
摘要： The present invention is directed to the discovery of a new class of androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease sebum secretion and to stimulate hair growth.
摘要翻译：本发明涉及新型雄激素受体调节剂的发现。本发明的其它方面涉及这些化合物减少皮脂分泌和刺激毛发生长的用途。

6. 发明授权

US06432945B1 Dipeptide derivatives 失效
标题翻译：二肽衍生物
公开(公告)号：US06432945B1
公开(公告)日：2002-08-13
申请号：US09822095
申请日：2001-03-30
申请人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
发明人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
IPC分类号： A61K31542
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.
摘要翻译：本发明涉及式的化合物及其药学上可接受的盐，其中取代基如本说明书中所定义，其是生长激素分泌元素，并且其增加内源性生长激素的水平。本发明的化合物可用于治疗和预防骨质疏松症和/或虚弱，充血性心力衰竭，与衰老相关的脆弱性，肥胖症; 加速骨折修复，减轻主要手术后的蛋白质分解代谢反应，减少慢性疾病引起的恶病质和蛋白质损失，加速伤口愈合，或加速烧伤患者或经历大手术的患者的恢复; 改善肌肉力量，移动性，维持皮肤厚度，代谢体内平衡或肾脏体内平衡。当与以下物质组合使用时，本发明的化合物还可用于治疗骨质疏松症和/或虚弱：双膦酸盐化合物如阿仑膦酸盐; 雌激素，雌激素和可选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素，以及对此有用的药物组合物。此外，本发明涉及可用于增加人或其他动物中生长激素的内源性产生或释放的药物组合物，其包含有效量的本发明化合物和选自GHRP-6的生长激素促分泌素， Hexarelin，GHRP-1，生长激素释放因子（GRF），IGF-1，IGF-2或B-HT920。本发明还涉及可用于制备式I化合物的中间体。

7. 发明授权

US06251902B1 Dipeptide derivatives as growth hormone secretagogues 有权
标题翻译：二肽衍生物作为生长激素促分泌素
公开(公告)号：US06251902B1
公开(公告)日：2001-06-26
申请号：US09380887
申请日：1999-09-08
申请人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
发明人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
IPC分类号： A61K31517
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.
摘要翻译：本发明涉及式的化合物及其药学上可接受的盐，其中取代基如本说明书中所定义，其是生长激素分泌元素，并且其增加内源性生长激素的水平。本发明的化合物可用于治疗和预防骨质疏松症和/或虚弱，充血性心力衰竭，与衰老相关的脆弱性，肥胖症; 加速骨折修复，减轻主要手术后的蛋白质分解代谢反应，减少慢性疾病引起的恶病质和蛋白质损失，加速伤口愈合，或加速烧伤患者或经历大手术的患者的恢复; 改善肌肉力量，移动性，维持皮肤厚度，代谢体内平衡或肾脏体内平衡。当与以下物质组合使用时，本发明的化合物还可用于治疗骨质疏松症和/或虚弱：双膦酸盐化合物如阿仑膦酸盐; 雌激素，雌激素和可选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素，以及对此有用的药物组合物。此外，本发明涉及可用于增加人或其他动物中生长激素的内源性产生或释放的药物组合物，其包含有效量的本发明化合物和选自GHRP-6的生长激素促分泌素， Hexarelin，GHRP-1，生长激素释放因子（GRF），IGF-1，IGF-2或B-HT920。本发明还涉及可用于制备式I化合物的中间体。

8. 发明授权

US06953791B2 Dipeptide derivatives 失效
标题翻译：二肽衍生物
公开(公告)号：US06953791B2
公开(公告)日：2005-10-11
申请号：US10371315
申请日：2003-02-21
申请人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
发明人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
IPC分类号： A61K31/138 , A61K31/40 , A61K31/4168 , A61K31/4174 , A61K31/437 , A61K31/4439 , A61K31/4453 , A61K31/4535 , A61K31/4725 , A61K31/4985 , A61K31/565 , A61K31/663 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/23 , A61K38/27 , A61K45/00 , A61P3/00 , A61P3/02 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/06 , A61P5/10 , A61P7/00 , A61P9/04 , A61P13/12 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/02 , A61P25/20 , A61P43/00 , C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07K1/02 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/062 , A61K31/551
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的盐，其中取代基如本说明书中所定义，其为生长激素分泌因子并且增加内源性生长激素的水平。本发明的化合物可用于治疗和预防骨质疏松症和/或虚弱，充血性心力衰竭，与衰老相关的脆弱性，肥胖症; 加速骨折修复，减轻主要手术后的蛋白质分解代谢反应，减少慢性疾病引起的恶病质和蛋白质损失，加速伤口愈合，或加速烧伤患者或经历大手术的患者的恢复; 改善肌肉力量，移动性，维持皮肤厚度，代谢体内平衡或肾脏体内平衡。当与以下物质组合使用时，本发明的化合物还可用于治疗骨质疏松症和/或虚弱：双膦酸盐化合物如阿仑膦酸盐; 雌激素，雌激素和可选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素，以及对此有用的药物组合物。此外，本发明涉及可用于增加人或其他动物中生长激素的内源性产生或释放的药物组合物，其包含有效量的本发明化合物和选自GHRP-6的生长激素促分泌素， Hexarelin，GHRP-1，生长激素释放因子（GRF），IGF-1，IGF-2或B-HT920。本发明还涉及可用于制备式I化合物的中间体。

9. 发明授权

US06951850B2 Dipeptide derivatives 失效
标题翻译：二肽衍生物
公开(公告)号：US06951850B2
公开(公告)日：2005-10-04
申请号：US10371953
申请日：2003-02-21
申请人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
发明人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
IPC分类号： A61K31/138 , A61K31/40 , A61K31/4168 , A61K31/4174 , A61K31/437 , A61K31/4439 , A61K31/4453 , A61K31/4535 , A61K31/4725 , A61K31/4985 , A61K31/565 , A61K31/663 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/23 , A61K38/27 , A61K45/00 , A61P3/00 , A61P3/02 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/06 , A61P5/10 , A61P7/00 , A61P9/04 , A61P13/12 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/02 , A61P25/20 , A61P43/00 , C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07K1/02 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/062 , A61K31/519
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, conjugated estrogens, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的盐，其中取代基如本说明书中所定义，其为生长激素分泌因子并且增加内源性生长激素的水平。本发明的化合物可用于治疗和预防骨质疏松症和/或虚弱，充血性心力衰竭，与衰老相关的脆弱性，肥胖症; 加速骨折修复，减轻主要手术后的蛋白质分解代谢反应，减少慢性疾病引起的恶病质和蛋白质损失，加速伤口愈合，或加速烧伤患者或经历大手术的患者的恢复; 改善肌肉力量，移动性，维持皮肤厚度，代谢体内平衡或肾脏体内平衡。当与以下物质组合使用时，本发明的化合物还可用于治疗骨质疏松症和/或虚弱：双膦酸盐化合物如阿仑膦酸盐; 雌激素，结合雌激素和任选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素及其有用的药物组合物。此外，本发明涉及可用于增加人或其他动物中生长激素的内源性产生或释放的药物组合物，其包含有效量的本发明化合物和选自GHRP-6的生长激素促分泌素， Hexarelin，GHRP-1，生长激素释放因子（GRF），IGF-1，IGF-2或B-HT920。本发明还涉及可用于制备式I化合物的中间体。

10. 发明授权

US06429313B2 Dipeptide derivatives 失效
公开(公告)号：US06429313B2
公开(公告)日：2002-08-06
申请号：US09822109
申请日：2001-03-30
申请人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
发明人： Philip Albert Carpino , David Andrew Griffith , Bruce Allen Lefker
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

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