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41. 发明授权

US08026258B2 Aryloxyalkylcarbamate-type derivatives, preparation method thereof and use of same in therapeutics 有权
标题翻译：芳氧基烷基氨基甲酸酯型衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US08026258B2
公开(公告)日：2011-09-27
申请号：US12691384
申请日：2010-01-21
申请人： Ahmed Abouabdellah , Antonio Almario Garcia , Jacques Froissant , Christian Hoornaert
发明人： Ahmed Abouabdellah , Antonio Almario Garcia , Jacques Froissant , Christian Hoornaert
IPC分类号： A61K31/445 , A61K31/472
CPC分类号： C07D207/08 , C07C271/16 , C07D211/22 , C07D211/46 , C07D213/65 , C07D215/20 , C07D215/28 , C07D217/24 , C07D401/12
摘要： The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.
摘要翻译：本发明涉及式（I）化合物：其中m，n，X，Y，R 1，R 2，R 3和R 4如本文所定义。本发明还涉及其在治疗中的用途。

42. 发明申请

US20110071161A1 TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：三唑酰胺羧酰胺衍生物，其制备方法及其治疗方法
公开(公告)号：US20110071161A1
公开(公告)日：2011-03-24
申请号：US12956764
申请日：2010-11-30
申请人： Christian HOORNAERT
发明人： Christian HOORNAERT
IPC分类号： A61K31/496 , C07D471/04 , A61P29/00 , A61P1/08 , A61P3/00 , A61P3/06 , A61P25/00 , A61P25/08 , A61P19/10 , A61P27/02 , A61P1/00 , A61P13/00 , A61P13/10
CPC分类号： C07D471/04
摘要： The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
摘要翻译：本发明涉及通式（I）的三唑并吡啶甲酰胺衍生物：其中X，A，R 1和R 2如本文所定义。本发明还涉及其制备方法及其治疗用途。

43. 发明授权

US07868007B2 Triazolopyridine carboxamide derivatives, preparation thereof and therapeutic use thereof 失效
标题翻译：三唑并吡啶甲酰胺衍生物，其制备及其治疗用途
公开(公告)号：US07868007B2
公开(公告)日：2011-01-11
申请号：US12573961
申请日：2009-10-06
申请人： Christian Hoornaert
发明人： Christian Hoornaert
IPC分类号： A61K31/4353 , A61K31/496 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
摘要翻译：本发明涉及通式（I）的三唑并吡啶甲酰胺衍生物：其中X，A，R 1和R 2如本文所定义。本发明还涉及其制备方法及其治疗用途。

44. 发明授权

US07781590B2 Piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase enzyme inhibitors 失效
标题翻译：哌啶基烷基氨基甲酸酯衍生物，其制备方法及其作为脂肪酸酰氨基水解酶抑制剂的治疗用途
公开(公告)号：US07781590B2
公开(公告)日：2010-08-24
申请号：US11465825
申请日：2006-08-21
申请人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Jean Jeunesse
发明人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Jean Jeunesse
IPC分类号： C07D421/00 , C07D211/26
CPC分类号： C07D207/09 , C07D205/04 , C07D211/26 , C07D211/58
摘要： The present invention comprises peridinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
摘要翻译：本发明包括哌啶基烷基氨基甲酸酯衍生物，其制备方法及其作为脂肪酸酰氨基水解酶（FAAH）酶抑制剂的治疗用途。这些衍生物通过与大麻素和香草素受体的相互作用发挥各种药理活性。通过抑制FAAH酶的代谢活性，不会产生常常负责多种疾病和其他病理状况发生的化合物，并且疾病的发病率大大降低。

45. 发明申请

US20100041651A1 TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES AND TRIAZOLOPYRIMIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 失效
标题翻译：三唑酰胺羧酰胺衍生物和三唑基吡啶羧酰胺衍生物，其制备方法及其治疗方法
公开(公告)号：US20100041651A1
公开(公告)日：2010-02-18
申请号：US12573959
申请日：2009-10-06
申请人： Luc EVEN , Christian HOORNAERT
发明人： Luc EVEN , Christian HOORNAERT
IPC分类号： A61K31/437 , C07D471/04 , A61K31/5377 , A61K31/496 , A61P25/00 , A61P29/00 , A61P3/00 , A61P19/10 , A61P27/00 , A61P11/00 , A61P1/00 , A61P13/10
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
摘要翻译：本发明涉及三唑并吡啶甲酰胺衍生物和通式（I）的三唑并嘧啶甲酰胺衍生物：其中X，A，R 1和R 2如本文所定义。本发明还涉及其制备方法及其治疗用途。

46. 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。

47. 发明申请

US20090286868A1 DERIVATIVES OF DIOXAN-2-ALKYL CARBAMATES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS 有权
标题翻译：二氧化-2-烷基碳酸酯的衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US20090286868A1
公开(公告)日：2009-11-19
申请号：US12510326
申请日：2009-07-28
申请人： Ahmed Abouabdellah , Michele Bas , Gihad Dargazanli , Christian Hoornaert , Adrien Tak Li , Florence Medaisko
发明人： Ahmed Abouabdellah , Michele Bas , Gihad Dargazanli , Christian Hoornaert , Adrien Tak Li , Florence Medaisko
IPC分类号： A61K31/335 , C07D319/06
CPC分类号： C07D319/06 , C07C235/06 , C07D405/12
摘要： A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3-C6)cycloalkyl-O— or (C3-C6)cycloalkyl(C1-C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1-C3)alkyl, (C3-C5)cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases.
摘要翻译：氰基，硝基，（C1-C3）烷基，（C1-C3）烷氧基，三氟甲基，（C1-C3）烷氧基，三氟甲氧基，苄氧基，（C3-C6）环烷基-O-或（C3-C6）环烷基（C1-C3）烷氧基; R 2表示通式CHR 3 CONHR 4的基团，其中R 3表示氢原子或甲基，R 4表示氢原子或（C 1 -C 3）烷基，（C 3 -C 5）环烷基或（吡啶-4-基）甲基组; 或2,2,2-三氟乙基; 或（咪唑-2-基）甲基; 或（苯并咪唑-2-基）甲基; 或任选被一个或多个卤素原子取代的苯基或氰基，硝基，（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，三氟甲基或三氟甲氧基; n表示1〜3的数; 以碱的形式，与酸的加成盐，水合物或溶剂合物的形式。还公开并要求保护的是由其衍生的药物组合物及其治疗各种疾病的治疗用途。

48. 发明申请

US20090143365A1 DERIVATIVES OF ALKYLPIPERAZINE- AND ALKYLHOMOPIPERAZINE-CARBOXYLATES, PREPARATION METHOD THEREOF AND USE OF SAME AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 失效
标题翻译：烷基哌嗪和烷基二磷杂环己烷羧酸酯的衍生物，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：US20090143365A1
公开(公告)日：2009-06-04
申请号：US12334798
申请日：2008-12-15
申请人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Tak Adrien Li
发明人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Tak Adrien Li
IPC分类号： A61K31/551 , C07D241/04 , A61K31/495 , A61K31/496 , A61P9/00 , A61P37/00 , A61P1/00 , A61P31/00 , A61P35/00 , A61P25/00 , C07D413/02 , C07D243/08
CPC分类号： C07D295/185 , C07D209/16 , C07D215/20 , C07D215/26 , C07D231/12 , C07D239/26 , C07D243/08 , C07D295/205
摘要： The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
摘要翻译：本发明包括烷基哌嗪和烷基高哌嗪羧酸盐及其衍生物，其制备方法及其作为脂肪酸酰氨基水解酶（FAAH）酶抑制剂的治疗用途。这些衍生物通过与大麻素和香草素受体的相互作用发挥各种药理活性。通过抑制FAAH酶的代谢活性，不会产生常常引起疾病发病和其他病理状况的化合物，并且疾病的发病率大大降低。

49. 发明申请

US20060089344A1 Derivatives of piperidinyl-and piperazinyl-alkyl carbamates, preparation methods thereof and application of same in therapeutics 失效
标题翻译：哌啶基和哌嗪基 - 烷基氨基甲酸酯的衍生物，其制备方法和在治疗中的应用
公开(公告)号：US20060089344A1
公开(公告)日：2006-04-27
申请号：US11262211
申请日：2005-10-28
申请人： Ahmed Abouabdellah , Philippe Burnier , Christian Hoornaert , Jean Jeunesse , Frederic Puech
发明人： Ahmed Abouabdellah , Philippe Burnier , Christian Hoornaert , Jean Jeunesse , Frederic Puech
IPC分类号： A61K31/519 , A61K31/517 , A61K31/496 , C07D417/14 , C07D413/14 , C07D403/14
CPC分类号： C07D211/26 , C07D213/38 , C07D295/13 , C07D401/04 , C07D401/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Compound corresponding to the general formula (I): in which A=N or CR2; R2═H, F, OH, CN, CF3, C1-6-alkyl, C12-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3═CHR4CONHR5; R4═H or C1-6-alkyl; R5═H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate. Therapeutic uses thereof
摘要翻译：对应于通式（I）的化合物：其中A = N或CR 2; R 2 -H，F，OH，CN，CF 3，C 1-6烷基，C 12〜 /烷氧基; 当A = N时，n = 2或3，m = 2; 当A = CR 2时，n = 1,2或3，m = 1或2。 B =共价键或C 1-8 - 亚烷基; R 1 =任选取代的杂芳基; R 3 -CHR 4 CONHR 5 5; R 4 -H或C 1-6 - 烷基; R 5 -H，C 1-6 - 烷基，C 3-7 - 环烷基，C 3-7 环烷基-C 1 -C 6 - 亚烷基; 以碱的形式，酸加成盐，水合物或溶剂化物。其治疗用途

50. 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.

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