公开(公告)号：US20120270893A1

公开(公告)日：2012-10-25

申请号：US13452839

申请日：2012-04-21

申请人： Robert Lee Dow ,  David James Edmonds ,  David Andrew Griffith ,  James Alfred Southers, JR.

发明人： Robert Lee Dow ,  David James Edmonds ,  David Andrew Griffith ,  James Alfred Southers, JR.

IPC分类号： A61K31/438 ,  A61P5/48 ,  A61P1/16 ,  C07D471/10 ,  A61P3/10

CPC分类号： C07D471/10 ,  C07D519/00

摘要： The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐; 其中G为R 1，R 2和R 3如本文所述; 其药物组合物; 以及其用于治疗通过抑制动物体内的乙酰辅酶A羧化酶调节的疾病，病症或病症的用途。

公开(公告)号：US07659115B2

公开(公告)日：2010-02-09

申请号：US11615250

申请日：2006-12-22

申请人： Andrew Griffith ,  Kiyoto Kurima ,  Edward Wilcox ,  Thomas Friedman

发明人： Andrew Griffith ,  Kiyoto Kurima ,  Edward Wilcox ,  Thomas Friedman

IPC分类号： C07H21/04 ,  C12N15/00 ,  C12N5/00

CPC分类号： C12Q1/6883 ,  A61K38/00 ,  C07K14/705 ,  C12Q2600/156 ,  C12Q2600/158

摘要： The invention provides isolated or purified nucleic molecules consisting of a nucleotide sequence encoding human transductin-1 (TDC1), such as SEQ ID NO: 1. The invention also provides vectors comprising the isolated or purified nucleic acid sequences and cells comprising such vectors.

摘要翻译： 本发明提供由编码人转蛋白-1（TDC1）的核苷酸序列（例如SEQ ID NO：1）组成的分离或纯化的核酸分子。本发明还提供了包含分离或纯化的核酸序列的载体和包含该载体的细胞。

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。

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。

公开(公告)号：US06476038B1

公开(公告)日：2002-11-05

申请号：US09676972

申请日：2000-09-29

申请人： James W. Darrow ,  Stéphane De Lombaert ,  Charles Blum ,  Jennifer Tran ,  Mark Giangiordano ,  David Andrew Griffith ,  Philip Albert Carpino

发明人： James W. Darrow ,  Stéphane De Lombaert ,  Charles Blum ,  Jennifer Tran ,  Mark Giangiordano ,  David Andrew Griffith ,  Philip Albert Carpino

IPC分类号： C07D48704

CPC分类号： C07D487/04 ,  G01N2333/5755 ,  G01N2333/70571

摘要： Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.

摘要翻译： 公开了下式的化合物：其中R1，R2，R3，R4，R5，R6和X如本文所定义。 这些化合物是NPY1受体的选择性调节剂。 这些化合物可用于治疗许多CNS疾病，代谢紊乱和外周疾病，特别是进食障碍和高血压。 还提供了治疗这种病症以及包装的药物组合物的方法。本发明的化合物也可用作NPY1受体定位的探针和作为NPY1受体结合测定中的标准物的探针。 给出了在受体定位研究中使用化合物的方法。

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.

公开(公告)号：US08859577B2

公开(公告)日：2014-10-14

申请号：US13876211

申请日：2011-09-20

申请人： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

发明人： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC分类号： A61K31/438 ,  C07D401/14

CPC分类号： C07D471/10 ,  A61K31/435 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

摘要： The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

摘要翻译： 本发明提供式（I）的化合物，其中R1，R2，R3，Z，A1，L和A52如本文所述;化合物或其药学上可接受的盐，其中R 1，R 2，R 3， 其药物组合物; 以及其用于治疗通过抑制动物体内的乙酰辅酶A羧化酶调节的疾病，病症或病症的用途。

公开(公告)号：US20120225900A1

公开(公告)日：2012-09-06

申请号：US13508744

申请日：2010-10-28

申请人： Scott William Bagley ,  David Andrew Griffith ,  Daniel Wei-Shung Kung

发明人： Scott William Bagley ,  David Andrew Griffith ,  Daniel Wei-Shung Kung

IPC分类号： A61K31/438 ,  A61P3/04 ,  A61P3/06 ,  C07D471/10 ,  A61P3/10

CPC分类号： C07D471/10 ,  A61K31/416 ,  A61K45/06 ,  A61K2300/00

摘要： The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

摘要翻译： 本发明提供式（I）化合物或所述化合物的药学上可接受的盐，其中R 1，R 2，R 3和R 4如本文所述; 其药物组合物; 以及其用于治疗通过抑制动物体内的乙酰辅酶A羧化酶调节的疾病，病症或病症的用途。

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。

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。