公开(公告)号：US20060025566A1

公开(公告)日：2006-02-02

申请号：US11149731

申请日：2005-06-10

申请人： Hamid Hoveyda ,  Mark Peterson ,  Graeme Fraser ,  Mahesh Ramaseshan

发明人： Hamid Hoveyda ,  Mark Peterson ,  Graeme Fraser ,  Mahesh Ramaseshan

IPC分类号： C07K5/12

CPC分类号： C07K5/0827 ,  A61K38/00 ,  C07D273/00 ,  C07D498/08 ,  C07K5/0808 ,  C07K5/0812

摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and 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, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

公开(公告)号：US20080051383A1

公开(公告)日：2008-02-28

申请号：US11774185

申请日：2007-07-06

申请人： Graeme Fraser ,  Hamid Hoveyda ,  Mark Peterson

发明人： Graeme Fraser ,  Hamid Hoveyda ,  Mark Peterson

IPC分类号： A61K31/33 ,  A61P1/00

CPC分类号： A61K31/33

摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective agonists of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Such compounds are useful as medicaments for treatment and prevention of a range of medical conditions characterized by disturbed gastrointestinal motility including, but not limited to, post-surgical gastroparesis and post-operative ileus in combination with opioid-induced bowel dysfunction. These agents are effective for multiple disorders at dose levels equivalent to those required to treat a single disorder.

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，同种型及其变体）的选择性激动剂的新的构象定义的大环化合物。 这些化合物可用作治疗和预防特征为紊乱的胃肠蠕动的一系列医学病症的药物，包括但不限于手术后胃轻瘫和与阿片样物质诱导的肠功能障碍联合的术后肠梗阻。 这些药剂对于与治疗单一病症所需的剂量水平相当的剂量水平对多种疾病有效。

公开(公告)号：US20170029429A1

公开(公告)日：2017-02-02

申请号：US15259922

申请日：2016-09-08

申请人： Hamid Hoveyda ,  Guillaume Dutheuil ,  Graeme Fraser ,  Marie-Odile Roy ,  Mohamed El Bousmaqui ,  Frédéric Batt

发明人： Hamid Hoveyda ,  Guillaume Dutheuil ,  Graeme Fraser ,  Marie-Odile Roy ,  Mohamed El Bousmaqui ,  Frédéric Batt

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  Y02P20/55

摘要： The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.

摘要翻译： 本发明涉及式I的新型化合物及其在治疗性治疗中的用途。 本发明还涉及使用N-sp 3保护基团的5,6,7，（8-取代的） - 四氢 - [1,2,4]三唑并[4,3-a]吡嗪的手性合成。 本发明还提供用于合成式I化合物的中间体。

公开(公告)号：US20110105389A1

公开(公告)日：2011-05-05

申请号：US12916205

申请日：2010-10-29

申请人： Hamid R. Hoveyda ,  Eric Marsault ,  Helmut Thomas ,  Graeme Fraser ,  Sylvie Beaubien ,  Axel Mathieu ,  Julien Beignet ,  Marc-André Bonin ,  Serge Phoenix ,  David Drutz ,  Mark Peterson ,  Sophie Beauchemin ,  Martin Brassard ,  Martin Vezina

发明人： Hamid R. Hoveyda ,  Eric Marsault ,  Helmut Thomas ,  Graeme Fraser ,  Sylvie Beaubien ,  Axel Mathieu ,  Julien Beignet ,  Marc-André Bonin ,  Serge Phoenix ,  David Drutz ,  Mark Peterson ,  Sophie Beauchemin ,  Martin Brassard ,  Martin Vezina

IPC分类号： A61K38/12 ,  C07K5/08 ,  C07K5/087 ,  A61K38/26 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/32 ,  A61P9/00 ,  A61P1/00 ,  A61P3/00 ,  A61P1/16 ,  A61P5/00 ,  A61P25/30

CPC分类号： C07K5/0808 ,  A61K38/00 ,  C07K5/0804 ,  C07K5/0812

摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (GRLN, growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, obesity and obesity-associated disorders, appetite or eating disorders, addictive disorders, cardiovascular disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders, central nervous system disorders and inflammatory disorders.

摘要翻译： 本发明提供已被证明是生长素释放肽受体（GRLN，生长激素促分泌素受体，GHS-R1a和亚型，同种型和/或其变体）的选择性调节剂的新型构象定义的大环化合物。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的拮抗剂或反向激动剂，并且用作治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌紊乱，肥胖症和肥胖相关疾病，食欲或饮食 疾病，成瘾性疾病，心血管疾病，胃肠道疾病，遗传疾病，过度增殖性疾病，中枢神经系统疾病和炎症性疾病。

公开(公告)号：US20070021331A1

公开(公告)日：2007-01-25

申请号：US11149512

申请日：2005-06-10

申请人： Graeme Fraser ,  Hamid Hoveyda ,  Mark Peterson

发明人： Graeme Fraser ,  Hamid Hoveyda ,  Mark Peterson

IPC分类号： A61K38/12 ,  A61K31/55 ,  A61K31/4545 ,  A61K31/395

CPC分类号： C07K5/0827 ,  A61K31/395 ,  A61K31/4545 ,  A61K31/55 ,  A61K38/06 ,  A61K38/12 ,  C07K5/0808 ,  C07K5/0812 ,  Y02A50/395

摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and 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, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory 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，同种型及其变体）的选择性调节剂的新型构象定义的大环化合物。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的激动剂，并且用作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，肥胖症和肥胖相关疾病， 中枢神经系统疾病，遗传疾病，过度增殖性疾病和炎症性疾病。

公开(公告)号：US20050054562A1

公开(公告)日：2005-03-10

申请号：US10872142

申请日：2004-06-18

申请人： Graeme Fraser ,  Eric Marsault ,  Mark Peterson ,  Hamid Hoveyda ,  Sylvie Beaubien ,  Kamel Benakli

发明人： Graeme Fraser ,  Eric Marsault ,  Mark Peterson ,  Hamid Hoveyda ,  Sylvie Beaubien ,  Kamel Benakli

IPC分类号： A61K38/12 ,  A61K38/22 ,  C07K5/08 ,  C07K5/087 ,  C07K5/097 ,  A61K31/365

CPC分类号： C07C213/08 ,  A61K38/12 ,  A61K38/2214 ,  C07C41/18 ,  C07C67/343 ,  C07D273/00 ,  C07D413/06 ,  C07D498/04 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/0827

摘要： The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

摘要翻译： 本发明涉及式（I）的新型大环化合物及其药学上可接受的盐，水合物或溶剂化物：其中R1，R2，R3，R4，R5，R6，n1，m，pZ1，Z2和Z3为 在规范中描述。 本发明还涉及作为胃动素受体的拮抗剂的式（I）的化合物，并且可用于治疗与该受体相关并与运动功能障碍相关的病症。