2-ALKYL-6-CYCLOAMINO-3-(PYRIDIN-4-YL)IMIDAZO[1,2-B]-PYRIDAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF
    3.
    发明申请
    2-ALKYL-6-CYCLOAMINO-3-(PYRIDIN-4-YL)IMIDAZO[1,2-B]-PYRIDAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF 审中-公开
    2-氨基-6-环丙氨基-3-(吡啶-4-基)咪唑并[1,2-B] - 吡啶衍生物,其制备方法及其治疗应用

    公开(公告)号:US20110312934A1

    公开(公告)日:2011-12-22

    申请号:US13058665

    申请日:2009-08-12

    CPC分类号: C07D487/04 C07D519/00

    摘要: The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R2 is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-4-alkyl, C1-4-alkyloxy-C-M-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl>C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-alkyl, C1-4-fluoroalkyl group; R3 is a hydrogen atom or a substituent selected from halogen atoms and the C1-3 alkyl, —NR4R5, hydroxyl or C1-4 alkyloxy groups; A is a C1-7-alkylene group optionally substituted by one or two Ra groups; B is a C1-7-alkylene group optionally substituted by one or two Rb groups; L is either a nitrogen atom optionally substituted by an Rc or Rd group or a carbon atom substituted by an Re1 group and an Rd group or by two Re2 groups; Rd is a group selected from a hydrogen atom or a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkylthio-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C1-6-fluoroalkyl, hydroxy-C1-6-alkyl group; Rf is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl, C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-allyl, C1-6-fluoroalkyl or benzyl group. The invention also relates to a method for preparing same and to the therapeutic application thereof.

    摘要翻译: 本发明涉及通式(I)的2-烷基-6-环氨基-3-(吡啶-4-基)咪唑并[1,2-b]哒嗪衍生物,其中:R2是C1-6烷基,C3 7-环烷基,C 3-7 - 环烷基-C 1-4 - 烷基,C 1-4 - 烷氧基-C1-烷基,C 3-7 - 环烷氧基-C 1-4 - 烷基,C 3-7 - 环烷基-C 1-4 - 烷氧基 C 1-4烷基,羟基-C 1-6 - 烷基,C 1-4 - 氟代烷基; R3是氢原子或选自卤素原子和C1-3烷基,-NR4R5,羟基或C1-4烷氧基的取代基; A是任选被一个或两个R a基团取代的C 1-7 - 亚烷基; B是任选被一个或两个Rb基团取代的C 1-7 - 亚烷基; L是任选被Rc或Rd基团取代的氮原子或被Re 1基团和Rd基团取代的碳原子或两个Re 2基团; Rd是选自氢原子或C 1-6 - 烷基,C 3-7 - 环烷基,C 3-7 - 环烷基-C 1-6 - 烷基,C 1-6 - 烷硫基-C 1-6 - 烷基,C 1-6 - 烷氧基-C 1-6 - 烷基,C 1-6 - 氟代烷基,羟基-C 1-6 - 烷基; R f是C 1-6 - 烷基,C 3-7 - 环烷基,C 3-7 - 环烷基-C 1-6 - 烷基,C 1-6 - 烷氧基-C 1-6 - 烷基,C 3-7 - 环烷氧基-C 1-4 - 烷基 C 3-7 - 环烷基-C 1-4 - 烷氧基-C 1-4 - 烷基,羟基-C 1-6 - 烯丙基,C 1-6 - 氟烷基或苄基。 本发明还涉及其制备方法及其治疗应用。

    3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide Derivatives, Their Preparation and Therapeutic Use
    5.
    发明申请
    3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide Derivatives, Their Preparation and Therapeutic Use 有权
    3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-B]吲哚-1-甲酰胺衍生物及其制备和治疗用途

    公开(公告)号:US20080249098A1

    公开(公告)日:2008-10-09

    申请号:US12140608

    申请日:2008-06-17

    IPC分类号: A61K31/5025 A61P25/00

    CPC分类号: C07D487/04 C07D209/42

    摘要: A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4) alkyl or (C1-C4) alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.

    摘要翻译: 本发明的主题是通式(I)的化合物,其中X表示氢或卤素原子; R 1表示氢原子或(C 1 -C 4 -C 4)烷基; R 2和R 3各自独立地表示氢原子或(C 1 -C 4)烷基, 或者R 2和R 3形式,与携带它们的氮原子一起形成吡咯烷基,哌啶基,吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基,1-氧化吡啶基,喹啉基,异喹啉基,嘧啶基,吡嗪基或哒嗪基的杂芳族基团,杂芳基可以携带一个或多个卤素原子和/或一个或多个(C 1 C 1 -C 4烷基或(C 1 -C 4 -C 4)烷氧基; 以碱的形式,与酸,溶剂合物或水合物的加成盐,包含它们的药物组合物,其制备方法和合成中间体。

    Oxazolidin-2-one derivatives, preparation method therefor and
therapeutical use thereof
    6.
    发明授权
    Oxazolidin-2-one derivatives, preparation method therefor and therapeutical use thereof 失效
    恶唑烷-2-酮衍生物及其制备方法及其治疗用途

    公开(公告)号:US5969146A

    公开(公告)日:1999-10-19

    申请号:US51539

    申请日:1998-04-13

    CPC分类号: C07D413/04

    摘要: Compounds derived from oxazolidin-2-one of formula (I) ##STR1## in which: R.sub.1 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a fluoroalkyl group, a hydroxyfluoroalkyl group, a cyanoalkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenylmethyl group or an R.sub.3 A- group in which R.sub.3 is a cycloalklyl or cyclooxyalkyl group which is unsubstituted or substituted by a hydroxyl group and A is a --CH.sub.2 or --CH.sub.2 --CH.sub.2 radical,R.sub.2 represents a hydrogen atom or a methyl group,X represents an oxygen or sulphur atom or an NR.sub.4 group where R.sub.4 is an alkyl group or a hydrogen atom, andZ represents an oxygen atom or a --CH.dbd.CH or --CH.sub.2 --CH.sub.2 group,their process of preparation and their applications in therapeutics.

    摘要翻译: PCT No.PCT / FR96 / 01511 Sec。 371日期:1998年4月13日 102(e)1998年4月13日PCT PCT 1996年10月8日PCT公布。 公开号WO97 / 13768 日期1997年04月17日衍生自式(I)的恶唑烷-2-酮的化合物,其中:R1表示氢原子,烷基,羟基烷基,氟代烷基,羟基氟烷基,氰基烷基,取代或 未取代的苯基,取代或未取代的苯基甲基或R3A-基团,其中R3是未被取代或被羟基取代的环烯基或环氧烷基,A是-CH2或-CH2-CH2基,R2表示氢 原子或甲基,X表示氧或硫原子或NR4基团,其中R4是烷基或氢原子,Z表示氧原子或-CH = CH或-CH2-CH2基团,它们的方法 制剂及其在治疗中的应用。

    3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use
    7.
    发明授权
    3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use 有权
    3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-B]吲哚-1-甲酰胺衍生物,其制备和治疗用途

    公开(公告)号:US07402682B2

    公开(公告)日:2008-07-22

    申请号:US11427508

    申请日:2006-06-29

    CPC分类号: C07D487/04 C07D209/42

    摘要: A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4)alkyl or (C1-C4)alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.

    摘要翻译: 本发明的主题是通式(I)的化合物,其中X表示氢或卤素原子; R 1表示氢原子或(C 1 -C 4 -C 4)烷基; R 2和R 3各自独立地表示氢原子或(C 1 -C 4)烷基, 或者R 2和R 3形式,与携带它们的氮原子一起形成吡咯烷基,哌啶基,吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基,1-氧化吡啶基,喹啉基,异喹啉基,嘧啶基,吡嗪基或哒嗪基的杂芳族基团,杂芳基可以携带一个或多个卤素原子和/或一个或多个(C 1 C 1 -C 4烷基或(C 1 -C 4 -C 4)烷氧基; 以碱的形式,与酸,溶剂合物或水合物的加成盐,包含它们的药物组合物,其制备方法和合成中间体。

    3-heteroaryl-3, 5-dihydro-4-oxo-4H-pyridazino[4, 5-b]indole-1-carboxamide derivatives their preparations and therapeutic use
    8.
    发明授权
    3-heteroaryl-3, 5-dihydro-4-oxo-4H-pyridazino[4, 5-b]indole-1-carboxamide derivatives their preparations and therapeutic use 有权
    3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-b]吲哚-1-甲酰胺衍生物的制备和治疗用途

    公开(公告)号:US07109194B2

    公开(公告)日:2006-09-19

    申请号:US10499725

    申请日:2002-11-20

    CPC分类号: C07D487/04 C07D209/42

    摘要: The invention concerns compounds of general formula (I), wherein: X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1–C4)alkyl group; R2 and R3, represent each, independently of each other, a hydrogen atom or a (C1–C4)alkyl group, or R2 and R3 form, with the atom which bears them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl, pyridazinyl type, the heteroaromatic group may represent one or several halogen atoms and/or one or several (C1–C4)alkyl, (C1–C4)alkoxyl groups; in the form of bases, addition salts to acids, solvates or hydrates. The invention also concerns pharmaceutical compositions containing same, methods for preparing same and synthesis intermediates

    摘要翻译: 本发明涉及通式(I)的化合物,其中:X表示氢或卤素原子; R 1表示氢原子或(C 1 -C 4 -C 4)烷基; R 2和R 3各自独立地表示氢原子或(C 1 -C 4)烷基, 或者R 2和R 3形式,其中带有它们的原子,吡咯烷基,哌啶基,吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基,1-氧化吡啶基,喹啉基,异喹啉基,嘧啶基,吡嗪基,哒嗪基类的杂芳族基团,杂芳基可以表示一个或多个卤素原子和/或一个或多个(C 1 H 3) -C 1-4烷基,(C 1 -C 4 -C 4)烷氧基; 以碱的形式,与酸,溶剂化物或水合物的加成盐。 本发明还涉及含有其的药物组合物,其制备方法和合成中间体

    3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use
    10.
    发明授权
    3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use 有权
    3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-b]吲哚-1-甲酰胺衍生物,其制备和治疗用途

    公开(公告)号:US07569567B2

    公开(公告)日:2009-08-04

    申请号:US12140608

    申请日:2008-06-17

    IPC分类号: A61K31/503 C07D487/02

    CPC分类号: C07D487/04 C07D209/42

    摘要: A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4) alkyl or (C1-C4) alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.

    摘要翻译: 本发明的主题是通式(I)的化合物,其中X表示氢或卤素原子; R1表示氢原子或(C1-C4)烷基; R2和R3各自独立地表示氢原子或(C1-C4)烷基,或者R2和R3与携带它们的氮原子一起形成吡咯烷基,哌啶基,吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基,1-氧化吡啶基,喹啉基,异喹啉基,嘧啶基,吡嗪基或哒嗪基的杂芳族基团,杂芳基可以携带一个或多个卤素原子和/或一个或多个(C 1 -C 4)烷基 或(C 1 -C 4)烷氧基; 以碱的形式,与酸,溶剂合物或水合物的加成盐,包含它们的药物组合物,其制备方法和合成中间体。