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1. 发明授权

US5410054A Heteroaryl quinolines as inhibitors of leukotriene biosynthesis 失效
标题翻译：杂芳基喹啉作为白三烯生物合成的抑制剂
公开(公告)号：US5410054A
公开(公告)日：1995-04-25
申请号：US95131
申请日：1993-07-20
申请人： Rick Friesen , Robert N. Young , Yves Girard , Marc Blouin , Daniel Dube
发明人： Rick Friesen , Robert N. Young , Yves Girard , Marc Blouin , Daniel Dube
IPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , C07D493/08 , C07D215/12 , C07D215/16 , C07D217/18 , C07D217/22
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , C07D493/08
摘要： Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
摘要翻译：具有式I的化合物：I是抑制白三烯生物合成。这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。它们也可用于治疗心绞痛，脑痉挛，肾小球性肾炎，肝炎，内毒素血症，葡萄膜炎和同种异体移植物排斥和预防动脉粥样硬化斑块的形成。

2. 发明申请

US20060040981A1 Use of phosphodiesterase-4 inhibitors as enhancers of cognition 审中-公开
标题翻译：使用磷酸二酯酶-4抑制剂作为认知的增强剂
公开(公告)号：US20060040981A1
公开(公告)日：2006-02-23
申请号：US10536250
申请日：2003-11-19
申请人： Daniel Dube , Michel Gallant , Patrick Lacombe , Yves Girard , Dwight Macdonald , Richard Friesen , Yves Ducharme , Bernard Cote , Marc Blouin , Evelyn Martins , Daniel Guay , Pierre Hamel , Mario Girard , Richard Frenette , Sebastien Laliberte , Annette Robichaud , Anthony Mastracchio , Helene Perrier
发明人： Daniel Dube , Michel Gallant , Patrick Lacombe , Yves Girard , Dwight Macdonald , Richard Friesen , Yves Ducharme , Bernard Cote , Marc Blouin , Evelyn Martins , Daniel Guay , Pierre Hamel , Mario Girard , Richard Frenette , Sebastien Laliberte , Annette Robichaud , Anthony Mastracchio , Helene Perrier
IPC分类号： A61K31/4709 , A61K31/47
CPC分类号： A61K31/4709 , A61K31/277 , A61K31/4375 , A61K31/44 , A61K31/47
摘要： The present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of a phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and effective amount of a phosphodiesterase-4 inhibitor.
摘要翻译：本发明涉及增强健康受试者的认知的方法，其包括施用安全认知增加量的磷酸二酯酶-4抑制剂。特别地，本发明涉及增加健康受试者的记忆，学习，保留，召回，意识和判断的方法，包括施用安全有效量的磷酸二酯酶-4抑制剂。

3. 发明授权

US06204275B1 PDE IV inhibiting compounds, compositions and methods of treatment 失效
标题翻译： PDE IV抑制化合物，组合物和治疗方法
公开(公告)号：US06204275B1
公开(公告)日：2001-03-20
申请号：US09513149
申请日：2000-02-25
申请人： Richard Friesen , Yvbes Ducharme , Daniel Dube , Yves Girard , Richard Frenette , Chun Li , Marc Blouin , Nathalie Chauret , Laird Trimble
发明人： Richard Friesen , Yvbes Ducharme , Daniel Dube , Yves Girard , Richard Frenette , Chun Li , Marc Blouin , Nathalie Chauret , Laird Trimble
IPC分类号： C07D40102
CPC分类号： C07D213/30 , C07D213/89 , C07D417/14
摘要： The invention encompasses compounds 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 IV). The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.
摘要翻译：本发明包括通过抑制磷酸二酯酶IV（PDE IV）提高环腺苷-3'，5'-单磷酸（cAMP）的水平，可用于治疗疾病（包括哮喘）的式I化合物。本发明还包括通过抑制PDE IV治疗疾病的某些药物组合物和方法，导致cAMP升高，包括使用式I化合物。

4. 发明授权

US5710170A Tri-aryl ethane derivatives as PDE IV inhibitors 失效
标题翻译：三芳基乙烷衍生物作为PDE IV抑制剂
公开(公告)号：US5710170A
公开(公告)日：1998-01-20
申请号：US763566
申请日：1996-12-10
申请人： Daniel Guay , Yves Girard , Yves Ducharme , Marc Blouin , Pierre Hamel , Mario Girard
发明人： Daniel Guay , Yves Girard , Yves Ducharme , Marc Blouin , Pierre Hamel , Mario Girard
IPC分类号： C07D213/30 , C07D213/34 , C07D213/89 , A61K31/415 , A61K31/44 , C07D233/64
CPC分类号： C07D213/30 , C07D213/34 , C07D213/89
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 IV). ##STR1## The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.
摘要翻译：本发明包括通过抑制磷酸二酯酶IV（PDE IV）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型式I化合物。本发明还包括通过抑制PDE IV治疗疾病的某些药物组合物和方法，导致cAMP升高，包括使用式I化合物。

5. 发明授权

US06200993B1 Heterosubstituted pyridine derivatives as PDE4 inhibitors 失效
标题翻译：异取代吡啶衍生物作为PDE4抑制剂
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。

6. 发明授权

US07153968B2 8-(biaryl)quinoline PDE4 inhibitors 失效
标题翻译： 8-（联芳）喹啉PDE4抑制剂
公开(公告)号：US07153968B2
公开(公告)日：2006-12-26
申请号：US10517416
申请日：2003-06-23
申请人： Daniel Dube , Michel Gallant , Patrick Lacombe , Denis Deschenes , Laurence Dube , Yves Girard , Dwight Macdonald
发明人： Daniel Dube , Michel Gallant , Patrick Lacombe , Denis Deschenes , Laurence Dube , Yves Girard , Dwight Macdonald
IPC分类号： C07D219/08 , C07D215/12 , A61K31/47
CPC分类号： C07D215/04 , C07D215/06 , C07D215/12 , C07D215/14 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/12 , C07D471/04 , C07F7/0812 , C07F9/60
摘要： 8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues. In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.
摘要翻译： 8-（联芳）喹啉，其中8-位上的双芳基与喹啉基团呈元间关系，是可用于治疗哮喘，慢性支气管炎，慢性阻塞性肺疾病，嗜酸性肉芽肿，银屑病的PDE4抑制剂其他良性或恶性增殖性皮肤疾病，内毒素性休克，马匹中的扁桃体炎，马蹄痛，败血性休克，溃疡性结肠炎，克罗恩病，心肌和脑的再灌注损伤，炎症性关节炎，慢性肾小球肾炎，特应性皮炎，荨麻疹，成人呼吸窘迫综合征，动物慢性阻塞性肺病，尿崩症，过敏性鼻炎，过敏性结膜炎，春季结膜炎，动脉再狭窄或动脉粥样硬化，动脉粥样硬化，神经源性炎症，疼痛，咳嗽，类风湿关节炎，强直性脊柱炎，移植排斥反应，移植物抗宿主病，分泌过多的胃酸，细菌，真菌诱导的败血症，病毒诱导 d败血症，真菌诱发的败血症休克，病毒诱导的败血性休克，炎症介导的慢性组织变性，细胞因子介导的慢性组织变性，骨关节炎，癌症，恶病质，肌肉消瘦，抑郁，记忆障碍，肿瘤生长或正常组织的癌性侵袭。另一方面，本发明涉及一种增强健康受试者认知的方法，其包括施用安全认知增加量的磷酸二酯酶-4抑制剂。特别地，本发明涉及一种在健康受试者中增强记忆，学习，保留，召回，意识和判断的方法，包括施用安全和认知增加量的磷酸二酯酶-4抑制剂。

7. 发明申请

US20050234238A1 8-(Biaryl)quinoline pde4 inhibitors 失效
标题翻译： 8-（双芳基）喹啉pde4抑制剂
公开(公告)号：US20050234238A1
公开(公告)日：2005-10-20
申请号：US10517416
申请日：2003-06-23
申请人： Daniel Dube , Michel Gallant , Patrick Lacombe , Denis Deschenes , Laurence Dube , Yves Girard , Dwight Macdonald
发明人： Daniel Dube , Michel Gallant , Patrick Lacombe , Denis Deschenes , Laurence Dube , Yves Girard , Dwight Macdonald
IPC分类号： A61P29/00 , C07D215/04 , C07D215/12 , C07D401/04 , C07D401/10 , C07D403/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/02 , C07D471/04 , C07F7/08 , C07F9/60 , C07D41/02 , C07D43/14
CPC分类号： C07D215/04 , C07D215/06 , C07D215/12 , C07D215/14 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/12 , C07D471/04 , C07F7/0812 , C07F9/60
摘要： 8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues. In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.
摘要翻译： 8-（联芳）喹啉，其中8-位上的双芳基与喹啉基团呈元间关系，是可用于治疗哮喘，慢性支气管炎，慢性阻塞性肺疾病，嗜酸性肉芽肿，银屑病的PDE4抑制剂其他良性或恶性增殖性皮肤疾病，内毒素性休克，马匹中的扁桃体炎，马蹄痛，败血性休克，溃疡性结肠炎，克罗恩病，心肌和脑的再灌注损伤，炎症性关节炎，慢性肾小球肾炎，特应性皮炎，荨麻疹，成人呼吸窘迫综合征，动物慢性阻塞性肺病，尿崩症，过敏性鼻炎，过敏性结膜炎，春季结膜炎，动脉再狭窄或动脉粥样硬化，动脉粥样硬化，神经源性炎症，疼痛，咳嗽，类风湿关节炎，强直性脊柱炎，移植排斥反应，移植物抗宿主病，分泌过多的胃酸，细菌，真菌诱导的败血症，病毒诱导 d败血症，真菌诱发的败血症休克，病毒诱导的败血性休克，炎症介导的慢性组织变性，细胞因子介导的慢性组织变性，骨关节炎，癌症，恶病质，肌肉消瘦，抑郁，记忆障碍，肿瘤生长或正常组织的癌性侵袭。另一方面，本发明涉及一种增强健康受试者认知的方法，其包括施用安全认知增加量的磷酸二酯酶-4抑制剂。特别地，本发明涉及一种在健康受试者中增强记忆，学习，保留，召回，意识和判断的方法，包括施用安全和认知增加量的磷酸二酯酶-4抑制剂。

8. 发明授权

US5252599A Heteroarylnaphthalene hydroxy acids as inhibitors of leukotriene biosynthesis 失效
标题翻译：杂芳基萘羟基酸作为白三烯生物合成的抑制剂
公开(公告)号：US5252599A
公开(公告)日：1993-10-12
申请号：US936810
申请日：1992-08-27
申请人： Yves Girard , Rejean Fortin , Daniel Delorme , Daniel Dube , Pierre Hamel , Yves Ducharme , John W. Gillard
发明人： Yves Girard , Rejean Fortin , Daniel Delorme , Daniel Dube , Pierre Hamel , Yves Ducharme , John W. Gillard
IPC分类号： C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D493/08 , A61K31/35 , C07D309/10
CPC分类号： C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D493/08
摘要： Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
摘要翻译：具有式I的化合物：I是抑制白三烯生物合成。这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。它们也可用于治疗心绞痛，脑痉挛，肾小球性肾炎，肝炎，内毒素血症，葡萄膜炎和同种异体移植物排斥和预防动脉粥样硬化斑块的形成。

9. 发明申请

US20060058316A1 4-Oxo-1-3-substituted phenyl-1,4-dihydro-1,8-naphthyridine-3-carboxamide phosphodiesterase-4 inhibitors 失效
标题翻译： 4-氧代-1,3-取代的苯基-1,4-二氢-1,8-二氮杂萘-3-甲酰胺磷酸二酯酶-4抑制剂
公开(公告)号：US20060058316A1
公开(公告)日：2006-03-16
申请号：US10534582
申请日：2003-11-19
申请人： Daniel Dube , Michel Gallant , Patrick Lacombe , Renee Aspiotis , Laurence Dube , Yves Girard , Dwight Macdonald
发明人： Daniel Dube , Michel Gallant , Patrick Lacombe , Renee Aspiotis , Laurence Dube , Yves Girard , Dwight Macdonald
IPC分类号： A61K31/506 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
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 and useful for the enhancement of cognition.
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并且可用于增强认知的磷酸二酯酶4抑制剂。

10. 发明授权

US5428060A Heteroarylnaphthalene lactones as inhibitors of leukotriene biosynthesis 失效
标题翻译：杂芳基萘内酯作为白三烯生物合成的抑制剂
公开(公告)号：US5428060A
公开(公告)日：1995-06-27
申请号：US936809
申请日：1992-08-27
申请人： Yves Ducharme , John W. Gillard , Rejean Fortin , Daniel Dube , Yves Girard , Pierre Hamel , Daniel Delorme
发明人： Yves Ducharme , John W. Gillard , Rejean Fortin , Daniel Dube , Yves Girard , Pierre Hamel , Daniel Delorme
IPC分类号： C07D405/14 , C07D407/14 , C07D409/14 , C07D493/08 , A61K31/36 , A61K31/365
CPC分类号： C07D405/14 , C07D407/14 , C07D409/14 , C07D493/08
摘要： Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
摘要翻译：具有式I的化合物：I是抑制白三烯生物合成。这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。它们也可用于治疗心绞痛，脑痉挛，肾小球性肾炎，肝炎，内毒素血症，葡萄膜炎和同种异体移植物排斥和预防动脉粥样硬化斑块的形成。

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