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公开(公告)号:US20090099226A1
公开(公告)日:2009-04-16
申请号:US11920275
申请日:2006-05-15
申请人: Michel Belley , Jason Burch , John Colucci , Julie Farand , Mario Girard , Yongxin Han
发明人: Michel Belley , Jason Burch , John Colucci , Julie Farand , Mario Girard , Yongxin Han
IPC分类号: A61K31/437 , C07D471/04
CPC分类号: C07D471/04
摘要: The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.
摘要翻译: 本发明涉及可用于治疗EP4介导的疾病或病症(例如急性和慢性疼痛,骨关节炎,类风湿性关节炎和癌症)的前列腺素E型受体拮抗剂的喹啉衍生物。 衍生物具有式(I)的以下结构:其中A和B表示氮原子或CH基团,条件是它们不能同时为CH,Q可以表示氮或碳原子,Y和Z 是氮原子,N(O)基或C(R5)基团。 还包括包含式(I)的衍生物的药物组合物。
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公开(公告)号:US08013159B2
公开(公告)日:2011-09-06
申请号:US11920275
申请日:2006-05-15
申请人: Michel Belley , Jason Burch , John Colucci , Julie Farand , Mario Girard , Yongxin Han
发明人: Michel Belley , Jason Burch , John Colucci , Julie Farand , Mario Girard , Yongxin Han
IPC分类号: C07D471/00
CPC分类号: C07D471/04
摘要: The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.
摘要翻译: 本发明涉及可用于治疗EP4介导的疾病或病症(例如急性和慢性疼痛,骨关节炎,类风湿性关节炎和癌症)的前列腺素E型受体拮抗剂的喹啉衍生物。 衍生物具有式(I)的以下结构:其中A和B表示氮原子或CH基团,条件是它们不能同时为CH,Q可以表示氮或碳原子,Y和Z 是氮原子,N(O)基或C(R5)基团。 还包括包含式(I)的衍生物的药物组合物。
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公开(公告)号:US20060167081A1
公开(公告)日:2006-07-27
申请号:US10528419
申请日:2003-10-23
申请人: Xavier Billot , Jean-Luc Beaunard , Yongxin Han , Robert Young , John Colucci , Mario Girard , Marie-Claire Wilson
发明人: Xavier Billot , Jean-Luc Beaunard , Yongxin Han , Robert Young , John Colucci , Mario Girard , Marie-Claire Wilson
IPC分类号: A61K31/4015 , C07D207/24 , A61K31/4025 , C07D403/02
CPC分类号: C07D403/06
摘要: This invention relates to potent selective agonists of the EP, subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译: 本发明涉及EP的有效选择性激动剂,前列腺素E2受体的亚型,它们在治疗青光眼中的用途或制剂以及与患者眼睛中眼内压升高有关的其它病症。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。
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公开(公告)号:US06743802B2
公开(公告)日:2004-06-01
申请号:US10226980
申请日:2002-08-23
IPC分类号: A61K314375
CPC分类号: A61K45/06 , A61K31/435 , A61K31/4375 , C07D471/04 , A61K2300/00
摘要: Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐是可用于治疗哮喘和炎症的磷酸二酯酶4抑制剂。
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公开(公告)号:US06677351B2
公开(公告)日:2004-01-13
申请号:US10154591
申请日:2002-05-24
申请人: Chun Li , Mario Girard , Pierre Hamel , Sebastien Laliberte , Richard Friesen , Yves Girard , Daniel Guay
发明人: Chun Li , Mario Girard , Pierre Hamel , Sebastien Laliberte , Richard Friesen , Yves Girard , Daniel Guay
IPC分类号: A61K31444
CPC分类号: C07D471/04
摘要: Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐是可用于治疗哮喘和炎症的磷酸二酯酶4抑制剂。
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公开(公告)号:US20050070569A1
公开(公告)日:2005-03-31
申请号:US10487047
申请日:2002-08-27
IPC分类号: A61K31/435 , A61K31/436 , A61K31/4375 , A61K45/00 , A61K45/06 , A61P1/04 , A61P7/00 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/14 , A61P11/16 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P39/02 , A61P43/00 , C07D471/04 , C07D519/00 , A61K31/4745
CPC分类号: A61K45/06 , A61K31/435 , A61K31/4375 , C07D471/04 , A61K2300/00
摘要: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐是可用于治疗哮喘和炎症的磷酸二酯酶4抑制剂。
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公开(公告)号:US06200993B1
公开(公告)日:2001-03-13
申请号:US09551040
申请日:2000-04-17
申请人: Bernard Cote , Richard Friesen , Richard Frenette , Mario Girard , Yves Girard , Cedrickx Godbout , Daniel Guay , Pierre Hamel , Marc Blouin , Yves Ducharme , Sylvie Prescott
发明人: Bernard Cote , Richard Friesen , Richard Frenette , Mario Girard , Yves Girard , Cedrickx Godbout , Daniel Guay , Pierre Hamel , Marc Blouin , Yves Ducharme , Sylvie Prescott
IPC分类号: A61K3144
CPC分类号: C07D213/74 , C07D213/76 , C07D213/79 , C07D213/89 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4). or a pharmaceutically acceptable salt or hydrate thereof. The invention also encompasses pharmaceutical compositions and methods for treatment.
摘要翻译: 本发明包括通过通过抑制磷酸二酯酶IV(PDE 4)提高环腺苷-3',5'-单磷酸(cAMP)的水平,可用于治疗包括哮喘在内的疾病的新颖化合物。 其药学上可接受的盐或水合物。本发明还包括药物组合物和治疗方法。
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公开(公告)号:US06450520B1
公开(公告)日:2002-09-17
申请号:US09457314
申请日:1999-12-09
申请人: Mario Girard
发明人: Mario Girard
IPC分类号: B62K2528
CPC分类号: B62K25/286 , B60G2202/116 , B60G2300/12 , B62K2025/041
摘要: A rear suspension (10,64) for mountain bikes comprises a rigid link (46,98) pivotally mounted at opposed ends thereof to a lower rear portion of a main bicycle frame (14,74,96) and at a lower front portion of a bicycle swingarm (16,92). The rigid link (46,98) allows for relative displacements between the main bicycle frame (14,74,96) and the bicycle swingarm (16,92) along two degrees of freedom and, more particularly, for displacements in an area defined by the position of the two pivots (P1,P2) with respect to a rear wheel axle (WA), by the spacing between the two pivots (P1,P2) and also by the possible deformation of a spring (48,66) provided between the main frame (14,74,96) and the swingarm (16,92). A leaf spring (48,66) may be used within a shock absorber system which also includes a damper in order to limit relative displacements between the main frame (14,74,96) and the swingarm (16,92) upon impact of the rear wheel with an obstacle.
摘要翻译: 用于山地自行车的后悬架(10,64)包括刚性连杆(46,98),所述刚性连杆枢转地安装在主自行车车架(14,74,96)的下后部的相对端处,并且在 自行车摇臂(16,92)。 刚性连杆(46,98)允许沿着两个自由度在主自行车车架(14,74,96)和自行车摇臂(16,92)之间的相对位移,更具体地说,用于在由 两个枢轴(P1,P2)相对于后轮轴(WA)的位置由两个枢轴(P1,P2)之间的间隔以及由弹簧(48,66)之间可能的变形而设置在 主框架(14,74,96)和摆臂(16,92)。 一个弹簧(48,66)可以用在减震器系统内,该减震器系统还包括阻尼器,以便在主框架(14,74,96)和摆臂(16,92)的冲击之后限制主框架 后轮有障碍物。
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公开(公告)号:US06399636B2
公开(公告)日:2002-06-04
申请号:US09810119
申请日:2001-03-16
申请人: Richard Freisen , Yves Ducharme , Bernard Cote , Marc Blouin , Evelyn Martins , Daniel Guay , Pierre Hamel , Mario Girard , Richard Frenette , Sebastien Laliberte
发明人: Richard Freisen , Yves Ducharme , Bernard Cote , Marc Blouin , Evelyn Martins , Daniel Guay , Pierre Hamel , Mario Girard , Richard Frenette , Sebastien Laliberte
IPC分类号: A61K314439
CPC分类号: C07D417/06
摘要: Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.
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公开(公告)号:US5733909A
公开(公告)日:1998-03-31
申请号:US784663
申请日:1997-01-21
申请人: Cameron Black , Mario Girard , Daniel Guay , Zhaoyin Wang
发明人: Cameron Black , Mario Girard , Daniel Guay , Zhaoyin Wang
IPC分类号: C07C317/44 , A01N41/10 , A61K31/535 , C07C311/29
CPC分类号: C07C317/44
摘要: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
摘要翻译: 本发明包括可用于治疗环氧合酶-2介导的疾病的新颖的式I化合物。 本发明还包括用于治疗包含式I化合物的环氧合酶-2介导的疾病的某些药物组合物。
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