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    Diazeniumdiolate Cyclohexyl Derivatives
    3.
    发明申请
    Diazeniumdiolate Cyclohexyl Derivatives 有权
    二氮烯二硫代环己基衍生物

    公开(公告)号：US20130059823A1

    公开(公告)日：2013-03-07

    申请号：US13698444

    申请日：2011-05-16

    申请人： Amjad Ali ,  Lin Yan ,  Pei Huo ,  Ravi Nargund

    发明人： Amjad Ali ,  Lin Yan ,  Pei Huo ,  Ravi Nargund

    IPC分类号： A61K31/655 ,  A61P9/12 ,  C07C245/02

    CPC分类号： C07C291/02 ,  C07B59/001 ,  C07C2601/14

    摘要： A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen, deuterium, —OH, —OC1-6alkyl, or halogen; R8 is hydrogen, deuterium, or C1-6alkyl; R11 and R12 are independently hydrogen, —C1-6alkyl, —OH, —OC1-6alkyl, or halogen; R13 and R14 are independently —C1-6alkyl, —(CH2)1-2OH, or —OC1-6alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or —C1-6alkyl; R15 is (CR1R2)nC(O)OR16, wherein n is 0, 1 or 2, —C(O)NHCH(R17)OR16, or —C(O)NHCH(R17)C(O)NHCH(R18)C(O)OR16; R16 is hydrogen, C1-6alkyl, or (CH2)1-2N+R19R20R21; R1, R2, R4, R5, R6, R7, R9, R10, R17, R18, R19, R20, and R21 are independently hydrogen or —C1-6alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.

    摘要翻译： 具有结构（I）的化合物或其药学上可接受的盐，其中R 3是氢，氘，-OH，-OC 1-6烷基或卤素; R8是氢，氘或C1-6烷基; R 11和R 12独立地是氢，-C 1-6烷基，-OH，-OC 1-6烷基或卤素; R 13和R 14独立地为C 1-6烷基， - （CH 2）1-2 OH或-OC 1-6烷基，或者与它们所连接的氮原子一起形成含有一个氮的4-至7-元杂环 原子和0或1个氧原子，其中所述环是未取代的或被卤素或-C 1-6烷基单取代，二取代或三取代; R15是（CR1R2）nC（O）OR16，其中n是0,1或2，-C（O）NHCH（R17）OR16或-C（O）NHCH（R17）C（O）NHCH（R18） （O）OR16; R16是氢，C1-6烷基或（CH2）1-2N + R19R20R21; R 1，R 2，R 4，R 5，R 6，R 7，R 9，R 10，R 17，R 18，R 19，R 20和R 21独立地为氢或-C 1-6烷基; 其立体异构体及其药学上可接受的盐及其立体异构体的药学上可接受的盐。

    Diazeniumdiolate cyclohexyl derivatives
    4.
    发明授权
    Diazeniumdiolate cyclohexyl derivatives 有权
    二氮烯二硫代环己基衍生物

    公开(公告)号：US08623846B2

    公开(公告)日：2014-01-07

    申请号：US13698444

    申请日：2011-05-16

    申请人： Amjad Ali ,  Lin Yan ,  Pei Huo ,  Ravi Nargund

    发明人： Amjad Ali ,  Lin Yan ,  Pei Huo ,  Ravi Nargund

    IPC分类号： A61K31/655 ,  C07C245/02 ,  C09B44/02

    CPC分类号： C07C291/02 ,  C07B59/001 ,  C07C2601/14

    摘要： A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen, deuterium, —OH, —OC1-6alkyl, or halogen; R8 is hydrogen, deuterium, or C1-6alkyl; R11 and R12 are independently hydrogen, —C1-6alkyl, —OH, —OC1-6alkyl, or halogen; R13 and R14 are independently —C1-6alkyl, —(CH2)1-2OH, or —OC1-6alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or —C1-6alkyl; R15 is —C(O)OH, —C(O)OCH2CH2N+CH3)3 wherein n is 0, 1 or 2, —C(O)NHCH(R17)OR16, or —C(O)NHCH(R17)C(O)NHCH(R18)C(O)OR16; R16 is hydrogen, C1-6alkyl, or (CH2)1-2N+R19R20R21; R1, R2, R4, R5, R6, R7, R9, R10, R17, R18, R19, R20, and R21 are independently hydrogen or —C1-6alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.

    摘要翻译： 具有结构（I）的化合物或其药学上可接受的盐，其中R 3是氢，氘，-OH，-OC 1-6烷基或卤素; R8是氢，氘或C1-6烷基; R 11和R 12独立地是氢，-C 1-6烷基，-OH，-OC 1-6烷基或卤素; R 13和R 14独立地为C 1-6烷基， - （CH 2）1-2 OH或-OC 1-6烷基，或者与它们所连接的氮原子一起形成含有一个氮的4-至7-元杂环 原子和0或1个氧原子，其中所述环是未取代的或被卤素或-C 1-6烷基单取代，二取代或三取代; R 15是-C（O）OH，-C（O）OCH 2 CH 2 N + CH 3）3，其中n是0,1或2，-C（O）NHCH（R 17）OR 16或-C（O）NHCH（R 17）C （O）NHCH（R 18）C（O）OR 16; R16是氢，C1-6烷基或（CH2）1-2N + R19R20R21; R 1，R 2，R 4，R 5，R 6，R 7，R 9，R 10，R 17，R 18，R 19，R 20和R 21独立地为氢或-C 1-6烷基; 其立体异构体及其药学上可接受的盐及其立体异构体的药学上可接受的盐。

    Piperidines promote release of growth hormone
    7.
    发明授权
    Piperidines promote release of growth hormone 失效
    皮质激素促进生长激素的释放

    公开(公告)号：US5965565A

    公开(公告)日：1999-10-12

    申请号：US988816

    申请日：1997-12-11

    申请人： Meng H. Chen ,  Zhijian Lu ,  Ravi Nargund ,  Arthur A. Patchett ,  James R. Tata ,  Lihu Yang ,  Mu Tsu Wu

    发明人： Meng H. Chen ,  Zhijian Lu ,  Ravi Nargund ,  Arthur A. Patchett ,  James R. Tata ,  Lihu Yang ,  Mu Tsu Wu

    IPC分类号： C07D401/06 ,  C07D413/14 ,  C07D471/10 ,  C07D495/10 ,  C07D209/04 ,  A61K31/445 ,  C07D211/00

    CPC分类号： C07D401/06 ,  C07D413/14 ,  C07D471/10 ,  C07D495/10

    摘要： The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

    摘要翻译： 本发明涉及一般结构式的某些哌啶，吡咯烷和六氢-1H-吖庚因：其中B选自：和R1，R1a，R2a，R3a，R3b，R4，R4a，R4b，R4c，R5， D，X，Y，n，x和y如本文所定义。 这些化合物促进人和动物中生长激素的释放。 这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小 儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。 还公开了含有这些化合物作为其活性成分的生长激素释放组合物。

    3-substituted piperidines promote release of growth hormone
    8.
    发明授权
    3-substituted piperidines promote release of growth hormone 失效
    3-取代的哌啶促进生长激素的释放

    公开(公告)号：US5559128A

    公开(公告)日：1996-09-24

    申请号：US424750

    申请日：1995-04-18

    申请人： Prasun K. Chakravarty ,  Ravi Nargund ,  Robert W. Marquis ,  Arthur A. Patchett ,  Lihu Yang

    发明人： Prasun K. Chakravarty ,  Ravi Nargund ,  Robert W. Marquis ,  Arthur A. Patchett ,  Lihu Yang

    IPC分类号： C07D211/56 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14 ,  A61K31/445 ,  C07D209/04

    CPC分类号： C07D401/06 ,  C07D211/56 ,  C07D401/14 ,  C07D413/14

    摘要： The present invention is directed to certain novel compounds identified as 3-substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing these compounds as the active ingredient thereof are also disclosed.

    摘要翻译： 本发明涉及鉴定为以下结构式的3-取代哌啶的某些新化合物：其中R1，R1a，R2a，R4，R5，A，X和Y如本文所定义。 这些化合物促进人和动物中生长激素的释放。 这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小 儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。 还公开了含有这些化合物作为其活性成分的生长激素释放组合物。

    Bicyclic piperidine derivatives as melanocortin-4 receptor agonists
    10.
    发明申请
    Bicyclic piperidine derivatives as melanocortin-4 receptor agonists 失效
    双环哌啶衍生物作为黑皮质素-4受体激动剂

    公开(公告)号：US20060194780A1

    公开(公告)日：2006-08-31

    申请号：US10548782

    申请日：2004-03-22

    申请人： Ravi Nargund ,  Zhixiong Ye ,  Liangqin Guo

    发明人： Ravi Nargund ,  Zhixiong Ye ,  Liangqin Guo

    IPC分类号： A61K31/4745 ,  A61K31/46

    CPC分类号： C07D451/02

    摘要： Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

    摘要翻译： 某些新型双环N-酰化哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。