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1.发明公开Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto 审中-公开三取代的芳基和杂芳基衍生物作为代谢的调节剂，以及预防和治疗相关病症的
公开(公告)号：EP1923390A1
公开(公告)日：2008-05-21
申请号：EP07023527.0
申请日：2004-07-09
发明人： Jones, Robert M. , Semple, Graeme , Xiong, Yifeng , Shin, Young-Jun , Ren, Albert S. , Calderon, Imelda , Choi, Jin Sun Karoline , Fioravanti, Beatriz , Lehmann, Juerg , Bruce, Marc A.
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D239/52 , A61K31/506 , A61K31/5377 , A61K31/505 , A61P3/10
CPC分类号： C07D239/52 , C07D239/54 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism.
Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.摘要翻译： 本发明涉及式（I）的某些三取代的芳基和杂芳基衍生物没有被代谢的调节剂。 因此，本发明的化合物可用于代谢紊乱及其并发症，：如，糖尿病和肥胖的预防或治疗是有用的。
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2.发明授权Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto 有权取代的吡啶和Pyrimidinylderivate新陈代谢的调节和治疗相关疾病
公开(公告)号：EP1911756B9
公开(公告)日：2010-05-26
申请号：EP07023528.8
申请日：2006-01-09
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/506 , A61K31/4545 , A61P3/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
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3.发明公开Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto 有权取代的吡啶和Pyrimidinylderivate新陈代谢的调节和治疗相关疾病
公开(公告)号：EP1911756A3
公开(公告)日：2008-06-18
申请号：EP07023528.8
申请日：2006-01-09
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/506 , A61K31/4545 , A61P3/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to certain substituted pyridinyl and pyrimidinyl derivatives of Fomula ( Ia ) that are modulators of metabolism.
Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.-
4.发明公开Use of GPR119 receptor agonists for increasing bone mass and for treating osteoporosis, as well as combination therapy relating thereto 审中-公开使用GPR119受体激动剂为骨量的增殖和骨质疏松症的治疗以及组合疗法为
公开(公告)号：EP2253311A3
公开(公告)日：2011-06-22
申请号：EP10009066.1
申请日：2007-04-10
IPC分类号： A61K31/00 , A61K31/4375 , A61K31/4439 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/522 , A61K45/06 , A61P19/02 , A61P19/08 , A61P19/10
CPC分类号： A61K31/00 , A61K31/4375 , A61K31/4439 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/522 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.
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5.发明公开Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto 有权取代的吡啶和Pyrimidinylderivate新陈代谢的调节和治疗相关疾病
公开(公告)号：EP1911756A2
公开(公告)日：2008-04-16
申请号：EP07023528.8
申请日：2006-01-09
IPC分类号： C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to certain substituted pyridinyl and pyrimidinyl derivatives of Fomula ( Ia ) that are modulators of metabolism.
Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.摘要翻译： 本发明涉及Fomula（Ia）的某些substituiertem吡啶基和嘧啶衍生物没有被代谢的调节剂。 因此，本发明的化合物可用于代谢相关病症及其并发症，：如，糖尿病和肥胖症的治疗是有用的。
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6.发明公开Use of GPR119 receptor agonists for increasing bone mass and for treating osteoporosis, as well as combination therapy relating thereto 审中-公开使用GPR119受体激动剂为骨量的增殖和骨质疏松症的治疗以及组合疗法为
公开(公告)号：EP2253311A2
公开(公告)日：2010-11-24
申请号：EP10009066.1
申请日：2007-04-10
IPC分类号： A61K31/00 , A61K31/4375 , A61K31/4439 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/522 , A61K45/06 , A61P19/02 , A61P19/08 , A61P19/10
CPC分类号： A61K31/00 , A61K31/4375 , A61K31/4439 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/522 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.
摘要翻译： 本发明涉及使用GPR119受体激动剂的治疗或预防低骨量，颜色为特征的病症：诸如骨质疏松症，以及用于以增加个体骨质量。 本发明进一步涉及在组合使用GPR119受体激动剂的具有二肽基肽酶IV（DPP-IV）抑制剂用于治疗或预防低骨量，颜色为特征的病症：诸如骨质疏松症，以及用于在上增加个体骨质量 ， 甲GPR119受体激动剂和GPR119受体激动剂和DPP-IV抑制剂的组合促进个体骨形成。
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7.发明授权Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto 有权取代的吡啶和Pyrimidinylderivate新陈代谢的调节和治疗相关疾病
公开(公告)号：EP1911756B1
公开(公告)日：2009-10-21
申请号：EP07023528.8
申请日：2006-01-09
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/506 , A61K31/4545 , A61P3/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
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8.发明公开3-phenyl-pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto 审中-公开3-苯基吡唑衍生物作为用于相关疾病的治疗中的5-HT 2A血清素受体调节剂的
公开(公告)号：EP1978019A1
公开(公告)日：2008-10-08
申请号：EP08010784.0
申请日：2005-11-17
发明人： Teegarden, Bradley , Xiong, Yifeng , Strah-Pleynet, Sonja , Jayakumar, Honnappa , Dosa, Peter I. , Feichtinger, Konrad , Casper, Martin , Lehmann, Juerg , Jones, Robert M. , Unett, David J.
IPC分类号： C07D231/16 , C07D231/12 , C07D403/12 , C07D487/08 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61P29/00 , A61K31/4155
CPC分类号： C07D231/12 , A61K31/5377 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula ( Ia ) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT 2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译： 本发明涉及式的某些3-苯基 - 吡唑衍生物（Ia）和其药物组合物做了调制的5-HT 2A血清素受体的活性。 化合物及其药物组合物涉及在血小板聚集，冠状动脉病，心肌梗塞，短暂性缺血发作，心绞痛，中风，心房纤维性颤动，降低血液凝块形成，哮喘或其症状，搅动或风险的治疗有用的方法 症状，行为障碍，药物诱发的精神病，兴奋型精神病，图雷特氏综合征，躁狂性障碍，器质性或NOS精神病，精神障碍，精神病，急性精神分裂症，慢性精神分裂症，NOS精神分裂症和相关病症，和睡眠障碍，睡眠障碍 ，糖尿病相关疾病，进行性多灶性白质脑病等。 因此，本发明涉及一种用于与分开或一起给药其它药物试剂联合治疗5-HT 2A血清素受体介导的病症的方法。
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