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1. 发明申请

WO2011076732A1 COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING GASTROINTESTINAL DISORDERS 审中-公开
标题翻译：化合物，药物组合物和用于治疗胃肠疾病的方法
公开(公告)号：WO2011076732A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070234
申请日：2010-12-20
申请人： EUROSCREEN S.A. , HOVEYDA, Hamid , BRANTIS, Cyrille Evangelos , DUTHEUIL, Guillaume , ZOUTE, Ludivine , SCHILS, Didier , FRASER, Graeme
发明人： HOVEYDA, Hamid , BRANTIS, Cyrille Evangelos , DUTHEUIL, Guillaume , ZOUTE, Ludivine , SCHILS, Didier , FRASER, Graeme
IPC分类号： A61K31/415 , A61K31/426 , A61K31/433 , A61K31/4439 , A61P1/00 , A61P1/12
CPC分类号： A61K31/426 , A61K31/415 , A61K31/433 , A61K31/4439
摘要： The present invention relates to compounds of formula (I) useful in treating and/or preventing gastrointestinal disorders.
摘要翻译：本发明涉及可用于治疗和/或预防胃肠道疾病的式（I）化合物。

2. 发明申请

WO2013050424A1 NOVEL CHIRAL N-ACYL-5,6,7,(8-SUBSTITUTED)-TETRAHYDRO-[1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR MEDIATED DISORDERS AND CHIRAL SYNTHESIS THEREOF 审中-公开
标题翻译：选择性NK-3受体拮抗剂的新颖的正丙氨酰-5,6,7（8-取代的） - 羟基 - [1,2,4]三唑并[4,3-a]吡啶，药物组合物，使用方法在NK-3受体介导的疾病和其合成的CHIRAL
公开(公告)号：WO2013050424A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069546
申请日：2012-10-03
申请人： EUROSCREEN S.A. , HOVEYDA, Hamid , DUTHEUIL, Guillaume , FRASER, Graeme , ROY, Marie-Odile , EL BOUSMAQUI, Mohamed , BATT, Frédéric
发明人： HOVEYDA, Hamid , DUTHEUIL, Guillaume , FRASER, Graeme , ROY, Marie-Odile , EL BOUSMAQUI, Mohamed , BATT, Frédéric
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
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。

3. 发明申请

WO2004111077A1 MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR 审中-公开
标题翻译：大肠杆菌受体的巨噬细胞拮抗剂
公开(公告)号：WO2004111077A1
公开(公告)日：2004-12-23
申请号：PCT/CA2004/000913
申请日：2004-06-18
申请人： TRANZYME PHARMA INC. , FRASER, Graeme , MARSAULT, Eric , PETERSON, Mark , HOVEYDA, Hamid , BEAUBIEN, Sylvie , BENAKLI, Kamel
发明人： FRASER, Graeme , MARSAULT, Eric , PETERSON, Mark , HOVEYDA, Hamid , BEAUBIEN, Sylvie , BENAKLI, Kamel
IPC分类号： C07K5/12
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 R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n 1 , m, p Z 1 , Z 2 , and Z 3 are as describe in the specification. The invention also relates to compounds 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）化合物，并且可用于治疗与该受体相关并伴有或具有运动功能障碍的病症。

4. 发明申请

WO2008130464A1 MACROCYCLIC GHRELIN RECEPTOR MODULATORS AND METHODS OF USING THE SAME 审中-公开
标题翻译：大分子GHRELIN受体调节剂及其使用方法
公开(公告)号：WO2008130464A1
公开(公告)日：2008-10-30
申请号：PCT/US2008/001754
申请日：2008-02-08
申请人： TRANZYME PHARMA, INC. , HOVEYDA, Hamid , FRASER, Graeme , BEAUCHEMIN, Sophie , BRASSARD, Martin , DRUTZ, David , MARSAULT, Éric , OUELLET, Luc , PETERSON, Mark, L. , WANG, Zhigang , BENAKLI, Kamel
发明人： HOVEYDA, Hamid , FRASER, Graeme , BEAUCHEMIN, Sophie , BRASSARD, Martin , DRUTZ, David , MARSAULT, Éric , OUELLET, Luc , PETERSON, Mark, L. , WANG, Zhigang , BENAKLI, Kamel
IPC分类号： C07D273/00 , C07K5/12 , A61K38/00 , A61P1/00
CPC分类号： A61K31/395 , C07C215/42 , C07C215/54 , C07C271/16 , C07C2601/14 , C07D273/00 , C07D413/06 , C07D498/04 , C07D498/16
摘要： The present invention provides novel conformationally-defined macrocyclic compounds that can function as 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, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
摘要翻译：本发明提供新的构象定义的大环化合物，其可以作为生长素释放肽受体（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。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，骨骼疾病，遗传疾病，过度增殖性疾病和炎症性疾病。

5. 发明申请

WO2011053821A1 MACROCYCLIC GHRELIN RECEPTOR ANTAGONISTS AND INVERSE AGONISTS AND METHODS OF USING THE SAME 审中-公开
标题翻译：巨噬细胞GHRELIN受体拮抗剂和反相激素及其使用方法
公开(公告)号：WO2011053821A1
公开(公告)日：2011-05-05
申请号：PCT/US2010/054797
申请日：2010-10-29
申请人： TRANZYME PHARMA, INC. , HOVEYDA, Hamid , MARSAULT, Éric , THOMAS, Helmut , FRASER, Graeme , BEAUBIEN, Sylvie , MATHIEU, Axel , BEIGNET, Julien , BONIN, Marc-André , PHOENIX, Serge , DRUTZ, David , PETERSON, Mark , BEAUCHEMIN, Sophie , BRASSARD, Martin , VÉZINA, Martin
发明人： HOVEYDA, Hamid , MARSAULT, Éric , THOMAS, Helmut , FRASER, Graeme , BEAUBIEN, Sylvie , MATHIEU, Axel , BEIGNET, Julien , BONIN, Marc-André , PHOENIX, Serge , DRUTZ, David , PETERSON, Mark , BEAUCHEMIN, Sophie , BRASSARD, Martin , VÉZINA, Martin
IPC分类号： C07K5/12 , A61K38/12 , A61P25/00 , A61P35/00 , A61P5/00 , A61P3/00 , A61P1/00 , A61P29/00 , A61P9/00
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0804 , C07K5/0812
摘要： The present invention provides novel conformationalIy- defined macrocyclic compounds of formula (I) 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/或变体）的选择性调节剂的式（I）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，过度增生性疾病，中枢神经系统疾病和炎症性疾病。

6. 发明申请

WO2006137974A2 MACROCYCLIC GHRELIN RECEPTOR ANTAGONISTS AND INVERSE AGONISTS AND METHODS OF USING THE SAME 审中-公开
标题翻译：巨噬细胞GHRELIN受体拮抗剂和反相激素及其使用方法
公开(公告)号：WO2006137974A2
公开(公告)日：2006-12-28
申请号：PCT/US2006/015698
申请日：2006-04-26
申请人： TRANZYME PHARMA, INC. , FRASER, Graeme , HOVEYDA, Hamid
发明人： FRASER, Graeme , HOVEYDA, Hamid
CPC分类号： 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/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, cardiovascular disorders, obesity and obesity-associated disorders, gastrointestinal 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，同种型和/或变体）的选择性调节剂的新的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/或内分泌疾病，心血管疾病，肥胖症和肥胖相关疾病，胃肠道疾病，遗传疾病，过度增殖性疾病和炎症性疾病。

7. 发明申请

WO2006046977A1 MACROCYCLIC GHRELIN RECEPTOR ANTAGONISTS AND METHODS OF USING THE SAME 审中-公开
标题翻译：大环素GHRELIN受体拮抗剂及其使用方法
公开(公告)号：WO2006046977A1
公开(公告)日：2006-05-04
申请号：PCT/US2005/020887
申请日：2005-06-13
申请人： TRANZYME PHARMA, INC. , FRASER, Graeme , HOVEYDA, Hamid
发明人： FRASER, Graeme , HOVEYDA, Hamid
IPC分类号： C07K5/12 , A61K38/12 , A61P1/14
CPC分类号： C07K5/0808 , A61K38/06 , C07K5/0812 , C07K5/0827
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/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists 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, cardiovascular disorders, obesity and obesity-associated disorders, gastrointestinal 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，同种型和/或变体）的选择性调节剂的新的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，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，心血管疾病，肥胖症和肥胖相关疾病，胃肠道疾病，遗传疾病，过度增殖性疾病和炎症性疾病。

8. 发明申请

WO2006009674A1 MACROCYCLIC MODULATORS OF THE GHRELIN RECEPTOR 审中-公开
标题翻译： GHRELIN受体的大分子调节剂
公开(公告)号：WO2006009674A1
公开(公告)日：2006-01-26
申请号：PCT/US2005/020857
申请日：2005-06-13
申请人： TRANZYME PHARMA, INC. , HOVEYDA, Hamid , PETERSON, Mark , FRASER, Graeme , RAMASESHAN, Mahesh
发明人： HOVEYDA, Hamid , PETERSON, Mark , FRASER, Graeme , RAMASESHAN, Mahesh
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.
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。

9. 发明申请

WO2006009645A8 METHODS OF USING MACROCYCLIC MODULATORS OF THE GHRELIN RECEPTOR 审中-公开
公开(公告)号：WO2006009645A8
公开(公告)日：2006-01-26
申请号：PCT/US2005/020654
申请日：2005-06-13
申请人： TRANZYME PHARMA, INC. , FRASER, Graeme , HOVEYDA, Hamid , PETERSON, Mark
发明人： FRASER, Graeme , HOVEYDA, Hamid , PETERSON, Mark
IPC分类号： C07K5/12 , A61K38/12 , A61P1/14
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.

10. 发明申请

WO2008033328A2 MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR TREATMENT OF GASTROINTESTINAL DYSMOTILITY DISORDERS 审中-公开
标题翻译：胃动素受体治疗胃肠道憩室病的大环内酯类拮抗剂
公开(公告)号：WO2008033328A2
公开(公告)日：2008-03-20
申请号：PCT/US2007/019705
申请日：2007-09-11
申请人： TRANZYME PHARMA, INC. , MARSAULT, Éric , FRASER, Graeme , BENAKLI, Kamel , ST-LOUIS, Carl , ROUILLARD, Alain , THOMAS, Helmut
发明人： MARSAULT, Éric , FRASER, Graeme , BENAKLI, Kamel , ST-LOUIS, Carl , ROUILLARD, Alain , THOMAS, Helmut
IPC分类号： C07K5/08 , A61P1/00
CPC分类号： C07K5/0812 , A61K38/00 , C07C271/16 , C07D273/00 , C07D413/06 , C07D417/12 , Y02P20/582
摘要： The present invention provides conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.
摘要翻译：本发明提供了结构上定义的大环化合物，其与motilin受体包括其亚型，同种型和/或变体结合和/或是其功能调节剂。这些大环化合物至少具有足够的药理学性质，可用作一系列疾病适应症的治疗剂。特别是，这些化合物可用于治疗和预防特征在于高血脂酸过多和/或胃肠过度运动的病症，包括但不限于腹泻，癌症治疗相关性腹泻，癌症诱导的腹泻，化学疗法诱导的腹泻，放射性肠炎，辐射诱发的腹泻，压力诱发的腹泻，慢性腹泻，AIDS相关的腹泻，C。其他类型的腹泻，消化不良，肠易激综合征，化疗引起的恶心和呕吐（呕吐）以及手术后恶心和呕吐以及功能性胃肠疾病。此外，这些化合物还可用于治疗特征在于胃或肠吸收不良的疾病和病症，如短肠综合征，乳糜泻和恶病质。这些化合物也可用于治疗炎症性疾病和胃肠道病症，如炎症性肠病，溃疡性结肠炎，克罗恩氏病和胰腺炎。因此，还提供了治疗这些病症的方法和包括本发明化合物的药物组合物。

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