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1. 发明申请

US20100069405A1 DERIVATIVES OF HETEROARYL-ALKYLCARBAMATES, METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 审中-公开
标题翻译：异喹啉酮的衍生物，其制备方法及其作为脂肪酸氨基水解酶酶抑制剂的用途
公开(公告)号：US20100069405A1
公开(公告)日：2010-03-18
申请号：US12625125
申请日：2009-11-24
申请人： Ahmed Abouabdellah , Regine Bartsch-Li , Christian Hoornaert , Antoine Ravet
发明人： Ahmed Abouabdellah , Regine Bartsch-Li , Christian Hoornaert , Antoine Ravet
IPC分类号： A61K31/27 , C07D213/56 , C07D209/08 , C07C271/12 , C07D261/08 , C07D239/26 , C07D271/06 , C07D215/00 , C07D217/00 , A61K31/4418 , A61K31/404 , A61K31/42 , A61K31/505 , A61K31/47 , A61P25/00
CPC分类号： C07D213/54 , C07C271/12 , C07D209/08 , C07D213/40 , C07D215/04 , C07D215/12 , C07D215/227 , C07D217/14 , C07D231/12 , C07D233/64 , C07D235/06 , C07D239/26 , C07D239/42 , C07D261/14 , C07D273/02 , C07D413/04 , C07D471/04
摘要： The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.
摘要翻译：本发明涉及用于治疗神经系统疾病的化合物和组合物，其引起神经源性和神经性疼痛，炎症性疾病，肾缺血，心血管疾病和由内源性大麻素及其代谢活性产生的其它底物引起的其它病症脂肪酸酰胺水解酶（FAAH）。这些化合物由式（I）表示：其中A，n，R 1，R 7和R 8如本文所定义。

2. 发明授权

US07645757B2 Derivatives of heteroaryl-alkylcarbamates, methods for their preparation and use thereof as fatty acid amido hydrolase enzyme inhibitors 失效
标题翻译：杂芳基 - 烷基氨基甲酸酯的衍生物，其制备方法和用作脂肪酸酰氨基水解酶抑制剂
公开(公告)号：US07645757B2
公开(公告)日：2010-01-12
申请号：US11464355
申请日：2006-08-14
申请人： Ahmed Abouabdellah , Regine Bartsch-Li , Christian Hoornaert , Antoine Ravet
发明人： Ahmed Abouabdellah , Regine Bartsch-Li , Christian Hoornaert , Antoine Ravet
IPC分类号： A61K31/501 , A61K31/541 , A61K31/5355 , A61K31/55 , C07D417/04 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , A61P29/00 , A61P9/00 , A61P3/00
CPC分类号： C07D213/54 , C07C271/12 , C07D209/08 , C07D213/40 , C07D215/04 , C07D215/12 , C07D215/227 , C07D217/14 , C07D231/12 , C07D233/64 , C07D235/06 , C07D239/26 , C07D239/42 , C07D261/14 , C07D273/02 , C07D413/04 , C07D471/04
摘要： The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ishaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula alkylene group; a salt thereof, or a hydrate or a solvate of said compound or said salt; where the variables are as defined in the attached specification.
摘要翻译：本发明涉及用于治疗神经系统疾病的化合物和组合物，所述神经系统疾病引起神经源性和神经性疼痛，炎症性疾病，肾血液贫血，心血管疾病和其它由内源性大麻素和/或由其代谢活动导致的其它底物引起的病症脂肪酸酰胺水解酶（FAAH）。这些化合物由下式表示：其盐，或所述化合物或所述盐的水合物或溶剂合物; 其中变量如规范中所定义。

3. 发明申请

US20060014830A1 Arylalkylcarbamate derivatives production and use thereof in therapy 失效
公开(公告)号：US20060014830A1
公开(公告)日：2006-01-19
申请号：US11186242
申请日：2005-07-21
申请人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Antoine Ravet
发明人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Antoine Ravet
IPC分类号： A61K31/325
CPC分类号： C07C271/12 , C07C271/14 , C07C271/16 , C07C271/18 , C07C271/20 , C07D213/40 , C07D215/12 , C07D217/18 , C07D241/12 , C07D261/08 , C07D285/06 , C07D307/91 , C07D333/20 , C07D333/58
摘要： Compound of the general formula (I) in which n represents an integer ranging from 1 to 7; A is selected from the group consisting of X, Y and Z; X represents a C1-2-alkylene group optionally substituted by one or more C1-12-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-6-alkylene groups; Y represents a C2-alkenylene group optionally substituted by one or more C1-12-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-6-alkylene groups; Z represents a C3-7-cycloalkyl group of formula: m represents an integer ranging from 1 to 5; p and q represent integers and are defined such that p+q is a number ranging from 1 to 5; R1 represents a hydrogen or halogen or a hydroxyl, cyano, nitro, C1-4-alkyl, C1-4-alkoxy, C1-4-thioalkyl, C1-4-fluoroalkyl, C1-4-fluoroalkoxy or C1-4-fluorothioalkyl group; R2 represents a hydrogen or halogen or a cyano, nitro, hydroxyl, C1-4-alkyl, C1-4-alkoxy, C1-4-thioalkyl, C1-4-fluoroalkyl, C1-4-fluoroalkoxy, C1-4-fluorothioalkyl group, or an aryl-type or heteroaryl-type group optionally substituted by one or more substituents; R3 represents a group of general formula CHR4CONHR5 in which R4 represents a hydrogen or a C1-3-alkyl group and R5 represents a hydrogen or a C1-3-alkyl, C3-5-cycloalkyl or C3-7-cycloalkyl-C1-6-alkylene group; in the form of the base, acid addition salt, hydrate or solvate.

4. 发明授权

US07632850B2 Arylalkylcarbamate derivatives and production thereof 失效
标题翻译：芳基烷基氨基甲酸酯衍生物及其制备
公开(公告)号：US07632850B2
公开(公告)日：2009-12-15
申请号：US11186242
申请日：2005-07-21
申请人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Antoine Ravet
发明人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Antoine Ravet
IPC分类号： A61K31/16 , A61K31/165 , C07C233/02 , C07C237/00 , C07D211/70 , C07D213/18 , C07D213/55
CPC分类号： C07C271/12 , C07C271/14 , C07C271/16 , C07C271/18 , C07C271/20 , C07D213/40 , C07D215/12 , C07D217/18 , C07D241/12 , C07D261/08 , C07D285/06 , C07D307/91 , C07D333/20 , C07D333/58
摘要： The present invention provides a compound of the formula (I): in which R1, R2, R3, A and n are described and set forth more fully herein. Also provided are their preparation and their application in therapy.
摘要翻译：本发明提供式（I）化合物：其中R1，R2，R3，A和n被描述并在本文中更全面地阐述。还提供它们的制备及其在治疗中的应用。

5. 发明授权

US09000010B2 Alkyl-heterocycle carbamate derivatives, their preparation and their therapeutic application 有权
标题翻译：烷基杂环氨基甲酸酯衍生物，其制备及其治疗应用
公开(公告)号：US09000010B2
公开(公告)日：2015-04-07
申请号：US13574188
申请日：2011-01-19
申请人： Ahmed Abouabdellah , Antoine Ravet
发明人： Ahmed Abouabdellah , Antoine Ravet
IPC分类号： A61K31/454 , C07D417/12
CPC分类号： C07D417/12 , A61K31/454
摘要： The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
摘要翻译：本发明涉及对应于通式（I）的化合物：其中R 2表示氢，氟，羟基，氰基，三氟甲基，C 1-6 - 烷基，C 1-6 - 烷氧基或-NR 8 R 9; n和m彼此独立地表示等于1,2或3的整数，可以理解，和m + n最多等于5; A表示共价键，氧，C 1-6 - 亚烷基或-O-C 1-6 - 亚烷基; R 1表示任选被取代的苯基或杂环; R 3表示氢，氟，C 1-6 - 烷基或三氟甲基; R4表示任选取代的5元杂环; 以碱的形式或与酸的加成盐; 除去5-羟基-4-（4-氯苯基）哌啶-1-甲酸5-甲基异恶唑-3-基甲酯。本发明还涉及制备式（I）化合物的方法，包括它们的组合物及其治疗应用。

6. 发明授权

US08912218B2 Alkylthiazol carbamate derivatives, preparation thereof and therapeutic use thereof 有权
标题翻译：烷基噻唑氨基甲酸酯衍生物，其制备及其治疗用途
公开(公告)号：US08912218B2
公开(公告)日：2014-12-16
申请号：US13003713
申请日：2009-07-21
申请人： Ahmed Abouabdellah , Jochen Görlitzer , Peter Hamley , Antoine Ravet
发明人： Ahmed Abouabdellah , Jochen Görlitzer , Peter Hamley , Antoine Ravet
IPC分类号： C07D401/04 , C07D417/14
CPC分类号： C07D417/14
摘要： The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.
摘要翻译：本发明涉及式（I）的新产物：其中：R a表示任选取代的H，Hal，芳基或杂芳基; Rb表示H，Rc，-COORc-CO-Rc或-CO-NRcRd; 其中R c代表烷基，环烷基，杂环烷基，芳基和杂芳基，全部任意取代; Rd表示H，烷基或环烷基; 这些产品是所有异构体形式和盐，作为药物，特别是作为MET抑制剂。

7. 发明申请

US20120295909A1 ALKYL-HETEROCYCLE CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION 有权
标题翻译：烷基 - 杂环碳酸酯衍生物，其制备及其治疗应用
公开(公告)号：US20120295909A1
公开(公告)日：2012-11-22
申请号：US13574188
申请日：2011-01-19
申请人： Ahmed Abouabdellah , Antoine Ravet
发明人： Ahmed Abouabdellah , Antoine Ravet
IPC分类号： A61K31/454 , A61K31/427 , A61K31/4709 , A61K31/4725 , A61K31/5377 , A61P25/00 , A61P1/08 , A61P25/18 , A61P25/28 , A61P25/08 , A61P9/00 , A61P35/00 , A61P37/00 , A61P37/08 , A61P33/00 , A61P31/12 , A61P31/04 , A61P29/00 , A61P19/10 , A61P27/02 , A61P1/00 , A61P13/00 , A61P13/10 , C07D417/12
CPC分类号： C07D417/12 , A61K31/454
摘要： The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
摘要翻译：本发明涉及对应于通式（I）的化合物：其中R 2表示氢，氟，羟基，氰基，三氟甲基，C 1-6 - 烷基，C 1-6 - 烷氧基或-NR 8 R 9; n和m彼此独立地表示等于1,2或3的整数，可以理解，和m + n最多等于5; A表示共价键，氧，C 1-6 - 亚烷基或-O-C 1-6 - 亚烷基; R 1表示任选被取代的苯基或杂环; R 3表示氢，氟，C 1-6 - 烷基或三氟甲基; R4表示任选取代的5元杂环; 以碱的形式或与酸的加成盐; 除去5-羟基-4-（4-氯苯基）哌啶-1-甲酸5-甲基异恶唑-3-基甲酯。本发明还涉及制备式（I）化合物的方法，包括它们的组合物及其治疗应用。

8. 发明申请

US20110212963A1 ALKYLTHIAZOL CARBAMATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 有权
标题翻译：阿尔茨海默糖胺衍生物，其制备方法及其治疗方法
公开(公告)号：US20110212963A1
公开(公告)日：2011-09-01
申请号：US13003713
申请日：2009-07-21
申请人： Ahmed Abouabdellah , Jochen Görlitzer , Peter Hamiley , Antoine Ravet
发明人： Ahmed Abouabdellah , Jochen Görlitzer , Peter Hamiley , Antoine Ravet
IPC分类号： A61K31/5377 , C07D417/14 , A61K31/4709 , A61K31/4545 , A61K31/444 , A61K31/506 , C07D413/14 , A61P25/04 , A61P1/00 , A61P9/00 , A61P25/00 , A61P33/00 , A61P31/00 , A61P35/00 , A61P11/00
CPC分类号： C07D417/14
摘要： The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.
摘要翻译：本发明涉及式（I）的新产物：其中：R a表示任选取代的H，Hal，芳基或杂芳基; Rb表示H，Rc，-COORc-CO-Rc或-CO-NRcRd; 其中R c代表烷基，环烷基，杂环烷基，芳基和杂芳基，全部任意取代; Rd表示H，烷基或环烷基; 这些产品是所有异构体形式和盐，作为药物，特别是作为MET抑制剂。

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