公开(公告)号：US08450342B2

公开(公告)日：2013-05-28

申请号：US12709222

申请日：2010-02-19

申请人： Laurent Meijer ,  Karima Bettayeb ,  Herve Galons ,  Luc Demange ,  Nassima Oumata

发明人： Laurent Meijer ,  Karima Bettayeb ,  Herve Galons ,  Luc Demange ,  Nassima Oumata

IPC分类号： A61K31/437 ,  C07D471/14

CPC分类号： C07D471/04

摘要： The invention relates to trisubstituted or tetrasubstituted imidazo[4,5b]pyridines, to their uses as well as to a process for manufacturing them.The compounds of the invention are imidazo[4,5b]pyridines.The first general synthesis of 3,5,7 imidazo[4,5b]pyridines is disclosed in the description.The invention founds application, in particular, in the pharmaceutical field.

摘要翻译： 本发明涉及三取代或四取代的咪唑并[4,5-b]吡啶，其用途以及制备方法。 本发明的化合物是咪唑并[4,5-b]吡啶。 3,5,7咪唑并[4,5b]吡啶的第一个一般合成在本说明书中公开。 本发明尤其涉及制药领域。

公开(公告)号：US20100331343A1

公开(公告)日：2010-12-30

申请号：US12880774

申请日：2010-09-13

申请人： Daniel PERRISSOUD ,  Jean Martinez ,  Aline Moulin ,  Jean-Alain Fehrentz ,  Damien Boeglin ,  Luc Demange

发明人： Daniel PERRISSOUD ,  Jean Martinez ,  Aline Moulin ,  Jean-Alain Fehrentz ,  Damien Boeglin ,  Luc Demange

IPC分类号： A61K31/496 ,  A61P5/00 ,  A61P25/28 ,  A61P25/22 ,  A61P9/12 ,  A61P3/10 ,  A61P19/08 ,  A61P1/04 ,  A61P25/24 ,  A61P15/14 ,  A61P21/00 ,  A61P3/04 ,  A61P13/12 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/444 ,  A61K31/4545

CPC分类号： A61K31/4439 ,  A61K31/4196 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/497 ,  A61K45/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  A61K2300/00

摘要： The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

摘要翻译： 本发明提供新颖的三唑衍生物作为根据式（I）的生长激素促分泌素受体的生长素释放肽类似物配体，其可用于治疗或预防由GHS受体介导的哺乳动物，优选人类的生理和/或病理生理学状况。 本发明还提供了可用于调节这些受体的GHS受体拮抗剂和激动剂，并且可用于治疗上述病症，特别是生长迟缓，恶病质，短期，中期和/或长期调节能量平衡; 短期，中期和/或长期调节（刺激和/或抑制）食物摄入; 脂肪形成，肥胖和/或肥胖; 体重增加和/或减少; 糖尿病，I型糖尿病，II型糖尿病，肿瘤细胞增殖; 炎症，炎症反应，胃后肠梗阻，术后肠梗阻和/或胃切除术（生长激素释放肽替代疗法）。

公开(公告)号：US20070037857A1

公开(公告)日：2007-02-15

申请号：US11502473

申请日：2006-08-11

申请人： Daniel Perrissoud ,  Jean Martinez ,  Aline Moulin ,  Jean-Alain Fehrentz ,  Damien Boeglin ,  Luc Demange

发明人： Daniel Perrissoud ,  Jean Martinez ,  Aline Moulin ,  Jean-Alain Fehrentz ,  Damien Boeglin ,  Luc Demange

IPC分类号： A61K31/4439 ,  A61K31/4196

CPC分类号： A61K31/4439 ,  A61K31/4196 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/497 ,  A61K45/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  A61K2300/00

摘要： The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

摘要翻译： 本发明提供新颖的三唑衍生物作为根据式（I）的生长激素促分泌素受体的生长素释放肽类似物配体，其可用于治疗或预防由GHS受体介导的哺乳动物，优选人类的生理和/或病理生理学状况。 本发明还提供了可用于调节这些受体的GHS受体拮抗剂和激动剂，并且可用于治疗上述病症，特别是生长迟缓，恶病质，短期，中期和/或长期调节能量平衡; 短期，中期和/或长期调节（刺激和/或抑制）食物摄入; 脂肪形成，肥胖和/或肥胖; 体重增加和/或减少; 糖尿病，I型糖尿病，II型糖尿病，肿瘤细胞增殖; 炎症，炎症反应，胃后肠梗阻，术后肠梗阻和/或胃切除术（生长激素释放肽替代疗法）。

公开(公告)号：US08710089B2

公开(公告)日：2014-04-29

申请号：US12880774

申请日：2010-09-13

申请人： Daniel Perrissoud ,  Jean Martinez ,  Aline Moulin ,  Jean-Alain Fehrentz ,  Damien Boeglin ,  Luc Demange

发明人： Daniel Perrissoud ,  Jean Martinez ,  Aline Moulin ,  Jean-Alain Fehrentz ,  Damien Boeglin ,  Luc Demange

IPC分类号： A01N43/64 ,  A61K31/41 ,  C07D249/08

CPC分类号： A61K31/4439 ,  A61K31/4196 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/497 ,  A61K45/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  A61K2300/00

摘要： The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

摘要翻译： 本发明提供新颖的三唑衍生物作为根据式（I）的生长激素促分泌素受体的生长素释放肽类似物配体，其可用于治疗或预防由GHS受体介导的哺乳动物，优选人类的生理和/或病理生理学状况。 本发明还提供了可用于调节这些受体的GHS受体拮抗剂和激动剂，并且可用于治疗上述病症，特别是生长迟缓，恶病质，短期，中期和/或长期调节能量平衡; 短期，中期和/或长期调节（刺激和/或抑制）食物摄入; 脂肪形成，肥胖和/或肥胖; 体重增加和/或减少; 糖尿病，I型糖尿病，II型糖尿病，肿瘤细胞增殖; 炎症，炎症反应，胃后肠梗阻，术后肠梗阻和/或胃切除术（生长激素释放肽替代疗法）。

公开(公告)号：US07829724B2

公开(公告)日：2010-11-09

申请号：US11502473

申请日：2006-08-11

申请人： Daniel Perrissoud ,  Jean Martinez ,  Aline Moulin ,  Jean-Alain Fehrentz ,  Damien Boeglin ,  Luc Demange

发明人： Daniel Perrissoud ,  Jean Martinez ,  Aline Moulin ,  Jean-Alain Fehrentz ,  Damien Boeglin ,  Luc Demange

IPC分类号： C07D249/08 ,  A01N43/64 ,  A61K31/41

CPC分类号： A61K31/4439 ,  A61K31/4196 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/497 ,  A61K45/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  A61K2300/00

摘要： The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

摘要翻译： 本发明提供新颖的三唑衍生物作为根据式（I）的生长激素促分泌素受体的生长素释放肽类似物配体，其可用于治疗或预防由GHS受体介导的哺乳动物，优选人类的生理和/或病理生理学状况。 本发明还提供了可用于调节这些受体的GHS受体拮抗剂和激动剂，并且可用于治疗上述病症，特别是生长迟缓，恶病质，短期，中期和/或长期调节能量平衡; 短期，中期和/或长期调节（刺激和/或抑制）食物摄入; 脂肪形成，肥胖和/或肥胖; 体重增加和/或减少; 糖尿病，I型糖尿病，II型糖尿病，肿瘤细胞增殖; 炎症，炎症反应，胃后肠梗阻，术后肠梗阻和/或胃切除术（生长激素释放肽替代疗法）。