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    Dipeptide derivatives as growth hormone secretagogues
    1.
    再颁专利
    Dipeptide derivatives as growth hormone secretagogues 失效
    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.

    Tartrate salt of a substituted dipeptide as growth hormone secretagogue
    2.
    发明授权
    Tartrate salt of a substituted dipeptide as growth hormone secretagogue 有权
    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。

    Treatment of insulin resistance with growth hormone secretagogues
    7.
    发明授权
    Treatment of insulin resistance with growth hormone secretagogues 失效
    用生长激素促分泌素治疗胰岛素抵抗

    公开(公告)号：US06448263B1

    公开(公告)日：2002-09-10

    申请号：US09380186

    申请日：1999-08-26

    申请人： Philip Albert Carpino ,  Charles Kwok-Fung Chiu ,  Lydia Codetta Pan ,  Bruce Allen Lefker ,  Judith Lee Treadway ,  Michael Paul Zawistoski

    发明人： Philip Albert Carpino ,  Charles Kwok-Fung Chiu ,  Lydia Codetta Pan ,  Bruce Allen Lefker ,  Judith Lee Treadway ,  Michael Paul Zawistoski

    IPC分类号： A61K31424

    CPC分类号： C07D471/04 ,  A61K38/05 ,  A61K38/25 ,  C07D211/78 ,  Y02P20/55

    摘要： This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are 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 compounds and certain processes useful for the synthesis of said intermediates and the compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.

    摘要翻译： 本发明涉及治疗哺乳动物胰岛素抵抗的方法，其包括施用有效量的式I化合物，其中变量在说明书中定义，或立体异构体混合物，非对映异构体富集，非对映体纯，对映体富集或对映体 纯异构体或其药学上可接受的盐和前药给所述哺乳动物。 式I化合物是生长激素促分泌素，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上述化合物的某些中间体和用于合成所述中间体和式I化合物的某些方法。本发明还涉及包括向人或其它动物施用的方法 功能性生长抑素拮抗剂如α-2肾上腺素能激动剂和式I化合物的组合。

    Dipeptide derivatives
    9.
    发明授权
    Dipeptide derivatives 失效
    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。

    Dipeptide derivatives as growth hormone secretagogues
    10.
    发明授权
    Dipeptide derivatives as growth hormone secretagogues 有权
    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。