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    Alkyl-heterocycle carbamate derivatives, their preparation and their therapeutic application
    3.
    发明授权
    Alkyl-heterocycle carbamate derivatives, their preparation and their therapeutic application 有权
    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。

    Alkylthiazol carbamate derivatives, preparation thereof and therapeutic use thereof
    4.
    发明授权
    Alkylthiazol carbamate derivatives, preparation thereof and therapeutic use thereof 有权
    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。

    ALKYL-HETEROCYCLE CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
    8.
    发明申请
    ALKYL-HETEROCYCLE CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION 有权
    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。

    DERIVATIVES OF HETEROARYL-ALKYLCARBAMATES, METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS
    10.
    发明申请
    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.