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    Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof
    3.
    发明授权
    Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof 有权
    抑制生长素释放肽/生长激素分泌受体途径及其用途的方法

    公开(公告)号：US08883721B2

    公开(公告)日：2014-11-11

    申请号：US13320408

    申请日：2010-05-12

    申请人： Cyril Y. Bowers ,  David H. Coy ,  Simon J. Hocart ,  Gloria S. Tannenbaum

    发明人： Cyril Y. Bowers ,  David H. Coy ,  Simon J. Hocart ,  Gloria S. Tannenbaum

    IPC分类号： A61K38/08 ,  A61K38/10 ,  C07K7/06 ,  C07K7/08 ,  A61K31/00 ,  A61K45/06 ,  A61K31/404 ,  A61K38/16 ,  A61K38/25

    CPC分类号： A61K38/08 ,  A61K31/00 ,  A61K31/404 ,  A61K38/10 ,  A61K38/16 ,  A61K38/25 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18 (SEQ ID NO: 93), wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

    摘要翻译： 本发明通过向受试者施用生长素释放肽O-酰基转移酶（GOAT）抑制剂和/或生长素释放肽受体拮抗剂来提供治疗，预防或控制受试者中肥胖症，肥胖相关病症，糖尿病和代谢综合征的方法。 本发明还提供式（VII）的生长素释放肽受体拮抗剂：A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18（SEQ ID NO：93），其中A11，A12 ，并且A13独立地不存在，氨基酸或氨基保护基; A15，A16，A17和A18各自独立地不存在或氨基酸; 并且A14是与-C（O）C1-C20烷基共轭的 - （O）C1-C20烷基或二氨基丙酸缀合的丝氨酸，条件是存在A11，A12或A13中的至少一种。

    Ghrelin/growth hormone releasing peptide/growth hormone secretatogue receptor antagonists and uses thereof
    4.
    发明授权
    Ghrelin/growth hormone releasing peptide/growth hormone secretatogue receptor antagonists and uses thereof 有权
    生长激素释放肽/生长激素释放肽/生长激素分泌受体拮抗剂及其用途

    公开(公告)号：US08536120B2

    公开(公告)日：2013-09-17

    申请号：US12298826

    申请日：2007-04-30

    申请人： Cyril Y. Bowers ,  Gloria S. Tannenbaum ,  David H. Coy ,  Simon J. Hocart

    发明人： Cyril Y. Bowers ,  Gloria S. Tannenbaum ,  David H. Coy ,  Simon J. Hocart

    IPC分类号： A61K31/15 ,  A61K31/216 ,  A61K38/08 ,  C07K7/06

    CPC分类号： C07C233/75 ,  A61K38/00 ,  C07K7/02 ,  C07K7/06 ,  C07K14/60

    摘要： The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.

    摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，其形式和变体）的调节剂的新化合物。 这些化合物可用作生长素释放肽受体的拮抗剂以及反向激动剂，部分激动剂或这些活性的组合，作为治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病， 胃肠道疾病，心血管疾病，肥胖和肥胖相关疾病，糖尿病，中枢神经系统疾病，遗传疾病和过度增殖性疾病。

    METHODS OF INHIBITING THE GHRELIN/GROWTH HORMONE SECRETATOGUE RECEPTOR PATHWAY AND USES THEREOF
    5.
    发明申请
    METHODS OF INHIBITING THE GHRELIN/GROWTH HORMONE SECRETATOGUE RECEPTOR PATHWAY AND USES THEREOF 有权
    抑制GHRELIN /生长激素分泌受体途径的方法及其用途

    公开(公告)号：US20120135918A1

    公开(公告)日：2012-05-31

    申请号：US13320408

    申请日：2010-05-12

    申请人： Cyril Y. Bowers ,  David H. Coy ,  Simon J. Hocart ,  Gloria S. Tannenbaum

    发明人： Cyril Y. Bowers ,  David H. Coy ,  Simon J. Hocart ,  Gloria S. Tannenbaum

    IPC分类号： A61K38/08 ,  A61K31/454 ,  A61P3/10 ,  C07K7/06 ,  C07K7/08 ,  A61P3/04 ,  A61K31/4965

    CPC分类号： A61K38/08 ,  A61K31/00 ,  A61K31/404 ,  A61K38/10 ,  A61K38/16 ,  A61K38/25 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15-A16-A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a di-aminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

    摘要翻译： 本发明通过向受试者施用生长素释放肽O-酰基转移酶（GOAT）抑制剂和/或生长素释放肽受体拮抗剂来提供治疗，预防或控制受试者中肥胖症，肥胖相关病症，糖尿病和代谢综合征的方法。 本发明还提供式（VII）的生长素释放肽受体拮抗剂：A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18，其中A11，A12和A13各自独立地不存在， 氨基酸或氨基保护基; A15-A16-A17和A18各自独立地不存在或氨基酸; 并且A14是与-C（O）C1-C20烷基或与-C（O）C1-C20烷基共轭的二氨基丙酸缀合的丝氨酸，条件是存在A11，A12或A13中的至少一种。

    GHRELIN/GROWTH HORMONE RELEASING PEPTIDE/GROWTH HORMONE SECRETATOGUE RECEPTOR ANTAGONISTS AND USES THEREOF
    6.
    发明申请
    GHRELIN/GROWTH HORMONE RELEASING PEPTIDE/GROWTH HORMONE SECRETATOGUE RECEPTOR ANTAGONISTS AND USES THEREOF 有权
    GHRELIN / GROWTH HORMONE释放肽/生长激素分泌受体拮抗剂及其用途

    公开(公告)号：US20090069245A1

    公开(公告)日：2009-03-12

    申请号：US12298826

    申请日：2007-04-30

    申请人： Cyril Y. Bowers ,  Gloria S. Tannenbaum ,  David H. Coy ,  Simon J. Hocart

    发明人： Cyril Y. Bowers ,  Gloria S. Tannenbaum ,  David H. Coy ,  Simon J. Hocart

    IPC分类号： A61K38/08 ,  C07K7/06 ,  C07D401/06 ,  A61K31/454 ,  C07D403/08

    CPC分类号： C07C233/75 ,  A61K38/00 ,  C07K7/02 ,  C07K7/06 ,  C07K14/60

    摘要： The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.

    摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，其形式和变体）的调节剂的新化合物。 这些化合物可用作生长素释放肽受体的拮抗剂以及反向激动剂，部分激动剂或这些活性的组合，作为治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病， 胃肠道疾病，心血管疾病，肥胖和肥胖相关疾病，糖尿病，中枢神经系统疾病，遗传疾病和过度增殖性疾病。

    Compounds having growth hormone releasing activity
    8.
    发明授权
    Compounds having growth hormone releasing activity 有权
    具有生长激素释放活性的化合物

    公开(公告)号：US07250399B2

    公开(公告)日：2007-07-31

    申请号：US10112316

    申请日：2002-03-29

    申请人： Cyril Y. Bowers ,  Frank Momany ,  Yongwu Liang

    发明人： Cyril Y. Bowers ,  Frank Momany ,  Yongwu Liang

    IPC分类号： A61K38/08

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/0205 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/1008 ,  C07K5/101 ,  C07K7/02

    摘要： Compounds that promote growth hormone releasing activity are disclosed. These compounds have the formula: A1-A2-X; A1′-X′; or A1′-Y These compounds can be present in a pharmaceutical composition. The compounds can be used with a second compound that acts as an agonist at the growth hormone releasing hormone receptor or which inhibits the effects of somatostatin. These compounds can be used for a variety of uses such as treating hypothalamic pituitary dwarfism, osteoporosis, burns, or promoting wound healing.

    摘要翻译： 公开了促进生长激素释放活性的化合物。 这些化合物具有下式：<？in-line-formula description =“In-line Formulas”end =“lead”？> A 2 A 1'-X'; 或A 1''-Y <？in-line-formula description =“In-line Formulas”end =“tail”？>这些化合物可以存在于药物组合物中。 该化合物可以与在生长激素释放激素受体上作为激动剂的第二化合物一起使用或抑制生长抑素的作用。 这些化合物可用于各种用途，例如治疗下丘脑垂体侏儒症，骨质疏松症，烧伤或促进伤口愈合。

    CHRH antagonists with low histamine release
    10.
    发明授权
    CHRH antagonists with low histamine release 失效
    低组胺释放的CHRH拮抗剂

    公开(公告)号：US5470947A

    公开(公告)日：1995-11-28

    申请号：US371552

    申请日：1989-06-26

    申请人： Karl A. Folkers ,  Anders Ljungqvist ,  Dong-Mei Feng ,  Minoru Kubota ,  Pui-Fun L. Tang ,  Cyril Y. Bowers

    发明人： Karl A. Folkers ,  Anders Ljungqvist ,  Dong-Mei Feng ,  Minoru Kubota ,  Pui-Fun L. Tang ,  Cyril Y. Bowers

    IPC分类号： A61K38/04 ,  A61K38/00 ,  A61P15/00 ,  C07K7/06 ,  C07K7/23

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

    摘要： Antide is the decapeptide, N--Ac--D--2--Nal,D--pClPhe, D--3--Pal, Ser,NicLys, D--NicLys, Leu, ILys, Pro, D--Ala,NH.sub.2 which is an antagonist of luteinizing hormone releasing hormone (LHRH). This decapeptide, like others of the present invention, has high antiovulatory activity (AOA) and releases negligible histamine. Antide is scheduled for scale-up, safety testing and evaluation in the experimental primate and in clinical medicine. Numerous other peptides having structures related to Antide were prepared and tested. These peptides had variations primarily in positions 5, 6, 7, and 8. Of these, N--Ac--D--2--Nal, D--pClPhe,D--3--Pal,Ser,PicLys,cis--DpzACAla, Leu,ILys,pro,D--Ala--NH.sub.2 was one of the most potent and had higher antiovulatory activity than Antide, i.e. 73%/0.25 ug and 100%/0.5 ug vs. 36%/0.5 ug and 100%/1.0 ug. Antide showed significant, (p

    摘要翻译： Antide是黄素化拮抗剂的十肽，N-Ac-D-2-Nal，D-pClPhe，D-3-Pal，Ser，NicLys，D-NicLys，Leu，ILys，Pro，D-Ala，NH2 激素释放激素（LHRH）。 这种十肽与本发明的其它物质一样，具有高的抗疟药活性（AOA），释放出可忽略的组胺。 Antide计划在实验灵长类动物和临床医学中进行放大，安全测试和评估。 制备并测试了许多具有与Antide有关的结构的其它肽。 这些肽主要在第5,6,7和8号位置有变化。其中，N-Ac-D-2-Nal，D-pClPhe，D-3-Pal，Ser，PicLys，cis-DpzACAla，Leu，ILys ，pro-D-Ala-NH2是最有效的并且具有比Antide更高的抗肿瘤活性，即73％/ 0.25ug和100％/ 0.5ug，而36％/ 0.5ug和100％/1.0μg。 当在50ng激动剂[D-3-Qal6] -LHRH之前以10μg，44小时的剂量注射时，Antide显示显着的（p <0.001）作用持续时间。 Antide在600ug（73％）和1200μg（100％）下显示口服AOA，水和玉米油口服制剂之间的差异可以忽略不计。