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1. 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。

2. 发明授权

US06410563B1 Substituted 8-arylquinoline phosphodiesterase-4 inhibitors 失效
标题翻译：取代的8-芳基喹啉磷酸二酯酶-4抑制剂
公开(公告)号：US06410563B1
公开(公告)日：2002-06-25
申请号：US09741517
申请日：2000-12-20
申请人： Denis Deschenes , Daniel Dube , Michel Gallant , Yves Girard , Patrick Lacombe , Dwight MacDonald , Anthony Mastracchio , Helene Perrier
发明人： Denis Deschenes , Daniel Dube , Michel Gallant , Yves Girard , Patrick Lacombe , Dwight MacDonald , Anthony Mastracchio , Helene Perrier
IPC分类号： A61K314709
CPC分类号： C07D401/10 , C07D215/12 , C07D215/14 , C07D401/14 , C07D405/12 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.
摘要翻译：新的取代的8-芳基喹啉，其中8位的芳基含有取代的取代的烯基，是PDE4抑制剂。

3. 发明授权

US06919353B2 Substituted 8-arylquinolune PDE4 inhibitors 失效
标题翻译：取代的8-芳基喹啉PDE4抑制剂
公开(公告)号：US06919353B2
公开(公告)日：2005-07-19
申请号：US10478791
申请日：2002-06-26
申请人： Daniel Dube , Yves Girard , Dwight MacDonald , Anthony Mastracchio , Michel Gallant , Patrick Lacombe , Denis Deschenes
发明人： Daniel Dube , Yves Girard , Dwight MacDonald , Anthony Mastracchio , Michel Gallant , Patrick Lacombe , Denis Deschenes
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/675 , A61K45/00 , A61P1/00 , A61P1/04 , A61P7/00 , A61P7/12 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P11/14 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/14 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P39/02 , A61P43/00 , C07D215/12 , C07D215/14 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/08 , C07D405/10 , C07D405/14 , C07D413/08 , C07D413/10 , C07D417/08 , C07D417/10 , C07D417/12 , C07F9/60 , C07F9/6571 , C07F9/6574
CPC分类号： C07D401/08 , C07D215/12 , C07D215/14 , C07D401/12 , C07D401/14 , C07D405/08 , C07D405/14 , C07D413/08 , C07D417/08 , C07D417/12 , C07F9/60 , C07F9/657181
摘要： 8-arylquinolines of formula (I) wherein the aryl group at the 8-position contains a meta two atom bridge to an optionally substituted phenyl or pyridyl group, are PDE4 inhibitors useful to treat asthma, chronic bronchitis, chronic obstructive pulmonary disease, arthritis, respiratory distress syndrome, allergic rhinitis, neurogenic inflammation, pain, rheumatoid arthritis, and other diseases. R1-R7 and Ar are as in claim 1.
摘要翻译：式（I）的8-芳基喹啉，其中8位上的芳基含有任选取代的苯基或吡啶基的间二原子桥，是可用于治疗哮喘，慢性支气管炎，慢性阻塞性肺病，关节炎的PDE4抑制剂，呼吸窘迫综合征，过敏性鼻炎，神经源性炎症，疼痛，类风湿性关节炎等疾病。 R 1〜R 7和Ar如权利要求1所述。

4. 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。

5. 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。

6. 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。

7. 发明授权

US07342024B2 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：US07342024B2
公开(公告)日：2008-03-11
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： A01N43/42 , A61K31/44 , 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

8. 发明授权

US07238706B2 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：US07238706B2
公开(公告)日：2007-07-03
申请号：US10764229
申请日：2004-01-23
申请人： Daniel Dube , Laurence Dube , Michel Gallant , Patrick Lacombe , Renee Aspiotis , Yves Girard , Dwight Macdonald
发明人： Daniel Dube , Laurence Dube , Michel Gallant , Patrick Lacombe , Renee Aspiotis , Yves Girard , Dwight Macdonald
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02
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 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。

9. 发明申请

US20050107402A1 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：US20050107402A1
公开(公告)日：2005-05-19
申请号：US10764229
申请日：2004-01-23
申请人： Daniel Dube , Laurence Dube , Michel Gallant , Patrick Lacombe , Renee Aspiotis , Yves Girard , Dwight Macdonald
发明人： Daniel Dube , Laurence Dube , Michel Gallant , Patrick Lacombe , Renee Aspiotis , Yves Girard , Dwight Macdonald
IPC分类号： A61K31/4375 , A61K31/4745 , A61K31/506 , A61P25/00 , C07D221/00 , C07D471/02 , C07D471/04
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 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. 发明申请

US20120035214A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：US20120035214A1
公开(公告)日：2012-02-09
申请号：US13262781
申请日：2010-04-01
申请人： Daniel J. McKay , Melissa Arbour , Renee Aspiotis , Austin Chen , Pierre-Andre Fournier , Michel Gallant , Yongxin Han , Helene Juteau , Patrick Lacombe , Sebastien Laliberte , Sophie Lauzon , Carmela Molinaro , Paul O'Shea , Yeeman Ramtohul , Daniel Simard , Dwight MacDonald , Bruce Mackay , Christophe Mellon , Krista Morley , Chit Tsui , Sarah Jennifer Dolman , Greg Hughes , Jacob Janey
发明人： Daniel J. McKay , Melissa Arbour , Renee Aspiotis , Austin Chen , Pierre-Andre Fournier , Michel Gallant , Yongxin Han , Helene Juteau , Patrick Lacombe , Sebastien Laliberte , Sophie Lauzon , Carmela Molinaro , Paul O'Shea , Yeeman Ramtohul , Daniel Simard , Dwight MacDonald , Bruce Mackay , Christophe Mellon , Krista Morley , Chit Tsui , Sarah Jennifer Dolman , Greg Hughes , Jacob Janey
IPC分类号： A61K31/451 , C07D401/04 , C07D401/10 , C07D211/26 , C07D211/28 , C07D401/12 , A61K31/4545 , A61K31/454 , A61P9/12 , A61P9/04 , A61P9/10 , A61P27/06 , A61P25/22 , A61P25/00 , A61P13/12 , C07D211/22
CPC分类号： C07D211/26 , C07D211/22 , C07D211/28 , C07D211/52 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14
摘要： The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
摘要翻译：本发明涉及联芳基哌啶基肾素抑制剂化合物及其在治疗心血管事件和肾功能不全中的用途。

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