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1. 发明申请

US20060247290A1 DERIVATIVES OF DIOXAN-2-ALKYL CARBAMATES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS 审中-公开
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：US20060247290A1
公开(公告)日：2006-11-02
申请号：US11426964
申请日：2006-06-28
申请人： Ahmed ABOUABDELLAH , Michele BAS , Gihad DARGAZANLI , Christian HOORNAERT , Adrien LI , Florence MEDAISKO
发明人： Ahmed ABOUABDELLAH , Michele BAS , Gihad DARGAZANLI , Christian HOORNAERT , Adrien LI , Florence MEDAISKO
IPC分类号： A61K31/4184 , A61K31/4178 , C07D405/02
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：对应于通式（I）的化合物：其中R 1表示任选被一个或多个卤素原子或羟基取代的苯基或萘基，氰基，硝基，（C 1）（C 1 -C 3）烷基，（C 1 -C 3 -C 3）烷氧基，三氟甲基，三氟甲氧基，苄氧基，（C 3 H 3） C 1 -C 6环烷基-O-或（C 3 -C 6 -C 6）环烷基（C 1 -C 6） C 1 -C 3烷氧基; R 2表示其中R 3 3表示氢原子的通式为CHR 3 CONHR 4 S的基团，或甲基和R 4代表氢原子或（C 1 -C 3 -C 3）烷基，（C 3 H 3）（C 1 -C 5）环烷基或（吡啶-4-基）甲基; 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）烷基， -C 3 -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。

2. 发明申请

US20110237595A1 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：US20110237595A1
公开(公告)日：2011-09-29
申请号：US13156551
申请日：2011-06-09
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： A61K31/50 , C07D209/08 , C07C271/12 , C07D261/08 , C07D237/08 , C07D217/02 , C07D215/14 , C07D471/04 , C07C269/06 , A61K31/4045 , A61K31/27 , A61K31/42 , A61K31/47 , A61K31/437 , A61P25/20
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。

3. 发明申请

US20070021426A1 DERIVATIVES OF HETEROARYL-ALKYLCARBAMATES, METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 失效
公开(公告)号：US20070021426A1
公开(公告)日：2007-01-25
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： A61K31/505 , A61K31/50 , A61K31/4965 , A61K31/47 , A61K31/325 , A61K31/4245 , A61K31/415 , A61K31/4184 , A61K31/4164
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 wherein A is selected from the group comprising X, Y or Z, and; X represents a methylene group optionally substituted by one or two C1-6-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-3-alkylene groups; Y represents either a C2-alkenylene group optionally substituted by one or two C1-6-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-3-alkylene groups; or a C2-alkynylene group; Z represents a 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; n represents an integer ranging from 1 to 7; R1 represents an R2 group optionally substituted by one or more R3 and/or R4 groups; R2 represents a group chosen from a pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, pyrrolyl, furyl, thienyl, imidazolyl, oxazolyl, thiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, naphthyl, quinolinyl, tetrahydroquinolinyl, isoquinolinyl, tetrahydroisoquinolinyl, 2-oxo-3,4-dihydroquinolinyl, 1-oxo-3,4-dihydroisoquinolinyl, quinazolinyl, quinoxalinyl, phthalazinyl, cinnolinyl, naphthyridinyl, benzofuranyl, dihydrobenzofuranyl, benzothienyl, dihydrobenzothienyl, indolyl, indolinyl, indazolyl, isoinR5R6, —O—(C1-3-alkylene)-O— or phenyl groups, the phenyl group optionally being substituted by one or more halogen atoms; R3 represents a group chosen from halogen atoms or cyano, nitro, C1-6-alkyl, C3-7-cycloalkyl, C1-6-alkoxy, hydroxyl, C1-6-thioalkyl, C1-6-fluoroalkyl, C1-6-fluoroalkoxy, C1-6-fluorothioalkyl, NR5R6, NR5COR6, NR5CO2R6, NR5SO2R6, COR5, CO2R5, CONR5R6, SO2R5, SO2N. R4 represents a group chosen from phenyl, phenyloxy, benzyloxy, naphthyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl groups; it being possible for the R4 group or groups to be substituted by one or more R3 groups which are identical to or different from one another; R5 and R6 represent, independently of one another, a hydrogen atom or a C1-6-alkyl group or form, with the atom or atoms which carry them, a ring chosen from an azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, azepine or piperazine ring, this ring optionally being substituted by a C1-6-alkyl or benzyl group; R7 represents a hydrogen atom or a C1-6-alkyl group, and R8 represents a hydrogen atom or a C1-6-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-3-alkylene group; a salt thereof, or a hydrate or a solvate of said compound or said salt.

4. 发明申请

US20070021405A1 ARYL- AND HETEROARYLPIPERIDINECARBOXYLATE-DERIVATIVES METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 审中-公开
标题翻译： ARYL-和异二氢吡啶羧酸酯衍生物的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：US20070021405A1
公开(公告)日：2007-01-25
申请号：US11465238
申请日：2006-08-17
申请人： Ahmed ABOUABDELLAH , Antonio ALMARIO GARCIA , Christian HOORNAERT , Patrick LARDENOIS , Frank MARGUET
发明人： Ahmed ABOUABDELLAH , Antonio ALMARIO GARCIA , Christian HOORNAERT , Patrick LARDENOIS , Frank MARGUET
IPC分类号： C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D471/04 , C07D207/06 , C07D211/16 , C07D211/52 , C07D401/04 , C07D401/06
摘要： The present invention comprises compounds corresponding to the general formula (I): in which m, n=1 to 3 and m+n=2 to 5; p=1 to 7; A=single bond or X, Y and/or Z; X=optionally substituted methylene; Y=C2-alkenylene, which is optionally substituted, or C2-alkynylene; Z=C3-7-cycloalkyl; R1 represents a group of aryl or heteroaryl type; R2 represents a hydrogen or fluorine atom or a hydroxyl, C1-6-alkoxy or NR8R9 group; R3 represents a hydrogen atom or a C1-6-alkyl group; R4 represents a hydrogen atom or a C1-6-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-3-alkyl group; in the base form or in the form of an addition salt with an acid, of a hydrate or of a solvate. The compounds are useful in the treatment of a number of diseases and/or pathological conditions such as chronic pain, dizziness, vomiting, nausea, eating disorders, neurological and psychiatric pathologies, acute or chronic neurodegenerative diseases, epilepsy, sleep disorders, cardiovascular diseases, renal ischaemia, cancers, disorders of the immune system, allergic diseases, parasitic, viral or bacterial infectious diseases, inflammatory diseases, osteoporosis, eye conditions, pulmonary conditions, gastrointestinal diseases or urinary incontinence.
摘要翻译：本发明包括对应于通式（I）的化合物：其中m，n = 1至3，m + n = 2至5; p = 1〜7; A =单键或X，Y和/或Z; X =任选取代的亚甲基; Y = C 2 - 亚烯基，其任选被取代，或C 2 - 亚炔基; Z = C 3-7 - 环烷基; R 1表示芳基或杂芳基的基团; R 2表示氢或氟原子或羟基，C 1-6 - 烷氧基或NR 8 R 9 >组 R 3表示氢原子或C 1-6 - 烷基; R 4表示氢原子或C 1-6 - 烷基，C 3-7 - 环烷基或C 3-7 环烷基-C 1-3 - 烷基; 以碱的形式或与酸的加成盐，水合物或溶剂化物的形式。这些化合物可用于治疗许多疾病和/或病理状况，例如慢性疼痛，头晕，呕吐，恶心，进食障碍，神经和精神病理学，急性或慢性神经变性疾病，癫痫症，睡眠障碍，心血管疾病，肾缺血，癌症，免疫系统疾病，过敏性疾病，寄生虫，病毒或细菌感染性疾病，炎性疾病，骨质疏松症，眼睛条件，肺部疾病，胃肠道疾病或尿失禁。

5. 发明申请

US20070142350A1 THERAPEUTIC USES OF DERIVATIVES OF PIPERIDINYL- AND PIPERAZINYL-ALKYL CARBAMATES 失效
标题翻译：哌啶基和哌嗪酸亚胺衍生物的治疗用途
公开(公告)号：US20070142350A1
公开(公告)日：2007-06-21
申请号：US11670690
申请日：2007-02-02
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： A61K31/53 , A61K31/519 , A61K31/517 , A61K31/506 , A61K31/4745 , A61K31/4743 , A61K31/4741 , A61K31/497 , A61K31/501
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： Therapeutic uses of a compound corresponding to the general formula (I): in which A=N or CR2; R2=H, F, OH, CN, CF3, C1-6-alkyl, C1-6-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.
摘要翻译：对应于通式（I）的化合物的治疗用途：其中A = N或CR 2; R 2 = H，F，OH，CN，CF 3，C 1-6烷基，C 1-6， /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。

6. 发明申请

US20070021424A1 ARYLOXYALKYLCARBAMATE-TYPE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS 有权
标题翻译： ARYLOXYALKYLCARBAMATE-TYPE衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US20070021424A1
公开(公告)日：2007-01-25
申请号：US11456708
申请日：2006-07-11
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： A61K31/50 , A61K31/4965 , A61K31/53 , A61K31/505 , A61K31/44 , A61K31/325
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， R 4和R 4如本文所定义。本发明还涉及其在治疗中的用途。

7. 发明申请

US20070021403A1 PIPERIDINYLALKYLCARBAMATE DERIVATIVES, METHODS FOR THEIR PREPARATION AND THE THERAPEUTIC USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 失效
标题翻译：哌啶二甲酰胺衍生物，其制备方法及其作为脂肪酸酰胺酶水解酶抑制剂的治疗方法
公开(公告)号：US20070021403A1
公开(公告)日：2007-01-25
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： A61K31/422 , A61K31/454 , C07D413/02
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。

8. 发明申请

US20100035893A1 TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 失效
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：US20100035893A1
公开(公告)日：2010-02-11
申请号：US12573961
申请日：2009-10-06
申请人： Christian HOORNAERT
发明人： Christian HOORNAERT
IPC分类号： A61K31/496 , C07D471/04 , A61P25/00 , A61P29/00 , A61P3/00 , A61P19/10 , A61P9/00 , A61P1/00
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。

9. 发明申请

US20080103197A1 ALKYL-, ALKENYL- AND ALKYNYLCARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS 失效
标题翻译：阿尔茨基，亚苄基和烷基氨基甲酸酯衍生物，其制备及其在治疗中的应用
公开(公告)号：US20080103197A1
公开(公告)日：2008-05-01
申请号：US11874959
申请日：2007-10-19
申请人： Antonio ALMARIO-GARCIA , Pascal GEORGE , Christian HOORNAERT , Adrien Tak LI , Frederic PUECH
发明人： Antonio ALMARIO-GARCIA , Pascal GEORGE , Christian HOORNAERT , Adrien Tak LI , Frederic PUECH
IPC分类号： A61K31/27 , A61P25/16 , C07C269/00
CPC分类号： C07C271/12 , C07C271/24 , C07C2601/18
摘要： The invention relates to a compound of formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to methods of preparation of compounds of formula (I) as well as to their therapeutic application.
摘要翻译：本发明涉及式（I）化合物：其中R 1，R 2，R 3和R 4， SUB>如本文所定义。本发明还涉及式（I）化合物的制备方法及其治疗应用。

10. 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。

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