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1. 发明授权

US06753340B2 (4,2-disubstituted-thiazol-5-yl)amine compounds as PDE7 inhibitors 失效
标题翻译：（4,2-二取代 - 噻唑-5-基）胺化合物作为PDE7抑制剂
公开(公告)号：US06753340B2
公开(公告)日：2004-06-22
申请号：US10401392
申请日：2003-03-27
申请人： Fabrice Vergne , Patrick Bernardelli , Edwige Lorthiois , Pierre Ducrot
发明人： Fabrice Vergne , Patrick Bernardelli , Edwige Lorthiois , Pierre Ducrot
IPC分类号： C07D27742
CPC分类号： C07D417/04 , C07D277/42
摘要： A compound selected from those of formula (I): wherein R1a, R1b, R2, R3, are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of phosphosdiesterase-7 (PDE-7).
摘要翻译：选自式（I）的化合物：其中R1a，R1b，R2，R3如说明书中所定义，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和含有它们的药物可用作磷酸二酯酶-7（PDE-7）的特异性抑制剂。

2. 发明授权

US06852720B2 Thiazol-2-yl-imine compounds as PDE-7 inhibitors 失效
标题翻译：噻唑-2-基亚胺化合物作为PDE-7抑制剂
公开(公告)号：US06852720B2
公开(公告)日：2005-02-08
申请号：US10402235
申请日：2003-03-27
申请人： Fabrice Vergne , Patrick Bernardelli , Edwige Lorthiois , Pierre Ducrot
发明人： Fabrice Vergne , Patrick Bernardelli , Edwige Lorthiois , Pierre Ducrot
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/517 , A61P1/00 , A61P5/00 , A61P11/06 , A61P15/08 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/00 , A61P43/00 , C07D277/42 , C07D417/04 , C07D401/04 , C07D401/14 , C07D403/04
CPC分类号： C07D417/04 , C07D277/42
摘要： A compound selected from those of formula (I): wherein: R1, R2, R3 are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as inhibitors of phosphosdiesterase-7.
摘要翻译：选自式（I）的化合物：其中：R1，R2，R3如说明书中所定义，并且任选地，其旋光异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用作磷酸二酯酶-7的抑制剂。

3. 发明申请

US20070049558A1 New Spirotricyclic Derivatives and Their Use as Phosphodiesterase-7 Inhibitors 审中-公开
标题翻译：新型Spirotricyclic衍生物及其作为磷酸二酯酶抑制剂的用途
公开(公告)号：US20070049558A1
公开(公告)日：2007-03-01
申请号：US11551687
申请日：2006-10-20
申请人： Patrick Bernardelli , Pierre Ducrot , Edwige Lorthiois , Fabrice Vergne
发明人： Patrick Bernardelli , Pierre Ducrot , Edwige Lorthiois , Fabrice Vergne
IPC分类号： A61K31/519 , C07D487/04 , C07F9/6512
CPC分类号： C07D239/70 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12
摘要： The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods for preparing them and their use for the treatment of disorders for which therapy by a PDE7 inhibitor is relevant.
摘要翻译：本发明提供了具有下列式（I），（II）和（III）的PDE7抑制剂的化合物，其中X 1，X 2，X 3， 3 X，X 4，X，Y，Z，A和Z 1如说明书中所定义，其制备方法及其用于治疗的方法的PDE7抑制剂治疗相关的疾病。

4. 发明授权

US07214676B2 Spirotricyclic derivatives and their use as phosphodiesterase-7 inhibitors 失效
标题翻译： Spirotricyclic衍生物及其作为磷酸二酯酶-7抑制剂的用途
公开(公告)号：US07214676B2
公开(公告)日：2007-05-08
申请号：US10852404
申请日：2004-05-24
申请人： Patrick Bernardelli , Pierre Ducrot , Edwige Lorthiois , Febrice Vergne
发明人： Patrick Bernardelli , Pierre Ducrot , Edwige Lorthiois , Febrice Vergne
IPC分类号： A61K31/535 , A61K31/497 , A61K31/517 , C07D273/01
CPC分类号： C07D239/70 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12
摘要： The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods for preparing them and their use for the treatment of disorders for which therapy by a PDE7 inhibitor is relevant.
摘要翻译：本发明提供了具有下列式（I），（II）和（III）的PDE7抑制剂的化合物，其中X 1，X 2，X 3， 3 X，X 4，X，Y，Z，A和Z 1如说明书中所定义，其制备方法及其用于治疗的方法的PDE7抑制剂治疗相关的疾病。

5. 发明授权

US07122565B2 Thiadiazoles and oxadiazoles and their use as phosphodiesterase-7 inhibitors 失效
标题翻译：噻二唑和恶二唑及其作为磷酸二酯酶-7抑制剂的用途
公开(公告)号：US07122565B2
公开(公告)日：2006-10-17
申请号：US09968371
申请日：2001-10-01
申请人： Fabrice Vergne , Pierre Ducrot , Charles Andrianjara , Patrick Bernardelli , Edwige Lorth Ois
发明人： Fabrice Vergne , Pierre Ducrot , Charles Andrianjara , Patrick Bernardelli , Edwige Lorth Ois
IPC分类号： C07D285/135 , A61K31/433
CPC分类号： C07D285/135 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/02
摘要： The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following Formula I: in which, Y is S or O, R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted, R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted, R3 is X2—R′3, in which X2 is a binding group and R′3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted, or their pharmaceutically acceptable derivatives, a compound of Formula I, for their preparation, and processes for pharmaceutical compositions containing methods of using the compounds for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.
摘要翻译：本发明提供具有下式I的1,3,4-噻二唑和1,3,4-恶二唑：其中Y是S或O，R 1是烷基，烯基，炔基，环烷基，杂环烷基，环烯基，芳基，杂芳基或多环基团，任选取代的R 2是烷基，烯基，炔基，环烷基，杂环烷基，任选取代的环烯基或芳基，R 3 >其中X 2是结合基团，并且R'3'是X 2 - ， - 环烷基，杂环烷基，环烯基，芳基，杂芳基或多环基团; 任选取代的，或其药学上可接受的衍生物，式I化合物及其制备方法，以及含有使用该化合物治疗PDE7抑制剂治疗相关疾病的方法的药物组合物的方法。

6. 发明申请

US20050014816A1 Thiophene amino acid derivatives, process for preparing them and pharmaceutical compositions containing them 审中-公开
标题翻译：噻吩氨基酸衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US20050014816A1
公开(公告)日：2005-01-20
申请号：US10884059
申请日：2004-07-02
申请人： Delphine Compere , Anne-Claude Dublanchet , Karine Courte , Stephane Blais , Pierre Ducrot , Philippe Cluzeau , Alexis Denis
发明人： Delphine Compere , Anne-Claude Dublanchet , Karine Courte , Stephane Blais , Pierre Ducrot , Philippe Cluzeau , Alexis Denis
IPC分类号： A61K31/381 , A61K31/4436 , A61P11/00 , C07D333/34 , C07D333/38 , C07D409/10 , C07
CPC分类号： C07D333/38 , C07D409/10
摘要： The invention provides compounds of Formula (I), stereoisomers thereof, or pharmaceutically acceptable salts of said compounds or stereoisomers, wherein R1, R2, m, p, q, R7 and R8 are as defined below, as well as compositions comprising the same, processes for making the same, and methods of using the same to treat a variety of diseases, including, those requiring interaction with metalloproteases, and more specifically with macrophage metalloelastase (MMP-12), and for the prevention and treatment of respiratory pathologies such as chronic obstructive bronchopneumopathy (COPD), emphysema, chronic bronchitis, chronic pulmonary inflammation, asthma, cystic fibrosis, acute respiratory distress syndrome (ARDS), respiratory allergies including allergic rhinitis, and also diseases associated with the production of TNFα including severe fibrotic pulmonary disease, pulmonary sarcoidosis and silicosis. The compounds of the present invention also show inhibitory activity on metalloprotease-13 (MMP-13), making them useful for the treatment of pathologies involving this enzyme, such as cancer, osteoporosis, osteoarthritis, arthritis, rheumatoid arthritis, atherosclerosis, multiple sclerosis and cardiac insufficiency.
摘要翻译：本发明提供式（I）化合物，其立体异构体或所述化合物或立体异构体的药学上可接受的盐，其中R 1，R 2，m，p，q，R 7和R 8如下所定义，以及包含其的组合物，制备相同的方法，以及使用它们治疗各种疾病的方法，包括需要与金属蛋白酶相互作用的那些疾病，更具体地涉及巨噬细胞金属弹性蛋白酶（MMP-12），以及用于预防和治疗呼吸道病症如慢性阻塞性支气管肺病（COPD），肺气肿，慢性支气管炎，慢性肺部炎症，哮喘，囊性纤维化，急性呼吸窘迫综合征（ARDS），包括过敏性鼻炎在内的呼吸系统过敏，以及包括严重纤维性肺病在内的TNFα产生相关疾病，肺结节病和矽肺。本发明的化合物还显示对金属蛋白酶-13（MMP-13）的抑制活性，使其可用于治疗涉及该酶的病理学，例如癌症，骨质疏松症，骨关节炎，关节炎，类风湿性关节炎，动脉粥样硬化，多发性硬化和心功能不全

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