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    3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use
    2.
    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

    Applicant: Philippe Burnier ,  Jacques Froissant ,  Benoit Marabout ,  Frank Marguet ,  Frederic Puech

    Inventor： Philippe Burnier ,  Jacques Froissant ,  Benoit Marabout ,  Frank Marguet ,  Frederic Puech

    IPC: C07D487/02 ,  C07D209/42 ,  A61K31/503

    CPC classification number: C07D487/04 ,  C07D209/42

    Abstract: 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.

    Abstract translation: 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。

    2-amino-N- [[4-(aminocarbonyl)pyrimidin-2-yl]amino]-alkyl]pyrimidine-4-carboxamide derivatives, their preparation and pharmaceutical compositions containing them
    3.
    发明授权
    2-amino-N- [[4-(aminocarbonyl)pyrimidin-2-yl]amino]-alkyl]pyrimidine-4-carboxamide derivatives, their preparation and pharmaceutical compositions containing them 失效
    2-氨基-N - [[4-（氨基羰基）嘧啶-2-基]氨基] - 烷基]嘧啶-4-甲酰胺衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US5330985A

    公开(公告)日：1994-07-19

    申请号：US84493

    申请日：1993-07-01

    Applicant: Pascal George ,  Benoit Marabout ,  Jacques Froissant ,  Jean Pierre Merly

    Inventor： Pascal George ,  Benoit Marabout ,  Jacques Froissant ,  Jean Pierre Merly

    IPC: A61K31/505 ,  A61K9/08 ,  A61K9/20 ,  A61K31/506 ,  A61P13/02 ,  A61P13/08 ,  A61P15/00 ,  A61P43/00 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/495 ,  A61K31/50 ,  C07D403/02 ,  C07D403/06

    CPC classification number: C07D239/42 ,  C07D401/14

    Abstract: A compound which is a pyrimidine-4-carboxamide derivative of the general formula (I) ##STR1## in which n is 0 or 1, m is 0 or 1,R.sub.1 represents a methyl group whenR.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), orR.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a 4-phenoxypiperidin-1-yl group (in which the phenoxy group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), a phenoxymethylpiperidin-1-yl group (in which the phenoxy group optionally carries 1 or 2 C.sub.1 -C.sub.4 alkyl groups) or a 4-phenylpiperazin-1-yl group (in which the phenyl group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), and R.sub.3 represents a hydrogen atom or only when n is 1 a hydroxyl group or a methoxy group, or is an addition salt thereof with an acid, is useful as an .alpha.-adrenergic antagonist.

    Abstract translation: 作为通式（I）的嘧啶-4-甲酰胺衍生物的化合物，其中n为0或1，m为0或1，当R 2表示 苯氧基（C 1 -C 4）烷基（其中苯氧基任选地带有1或2个选自卤素原子和甲氧基的取代基），或者R 1和R 2与它们所连接的氮原子一起形成4-苯氧基哌啶-1 （其中苯氧基任选地带有1或2个选自卤素原子和甲氧基的取代基），苯氧基甲基哌啶-1-基（其中苯氧基任选地带有1或2个C 1 -C 4烷基）或 4-苯基哌嗪-1-基（其中苯基任选地带有1或2个选自卤素原子和甲氧基的取代基），并且R 3表示氢原子或仅当n为1时为羟基或甲氧基，或 是其与酸的加成盐，可用作α-肾上腺素能拮抗剂。

    3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use
    4.
    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

    Applicant: Philippe Burnier ,  Jacques Froissant ,  Benoit Marabout ,  Frank Marguet ,  Frederic Puech

    Inventor： Philippe Burnier ,  Jacques Froissant ,  Benoit Marabout ,  Frank Marguet ,  Frederic Puech

    IPC: A61K31/503 ,  C07D487/02

    CPC classification number: C07D487/04 ,  C07D209/42

    Abstract: 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.

    Abstract translation: 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。

    2-aminopyrimidine-4-carboxamide derivatives, their preparation and their use in therapeutics
    9.
    发明授权
    2-aminopyrimidine-4-carboxamide derivatives, their preparation and their use in therapeutics 失效
    2-氨基嘧啶-4-羧酰胺衍生物，其制备及其在治疗中的应用

    公开(公告)号：US5246939A

    公开(公告)日：1993-09-21

    申请号：US903977

    申请日：1992-06-26

    Applicant: Pascal George ,  Christian Maloizel ,  Benoit Marabout ,  Jean-Pierre Merly

    Inventor： Pascal George ,  Christian Maloizel ,  Benoit Marabout ,  Jean-Pierre Merly

    IPC: A61K31/505 ,  A61K31/506 ,  A61P13/00 ,  A61P13/02 ,  A61P13/08 ,  A61P15/00 ,  C07D211/56 ,  C07D239/42 ,  C07D295/08 ,  C07D401/12 ,  C07D403/12

    CPC classification number: C07D401/12

    Abstract: A compound which is a 2-aminopyrimidine carboxamide derivative represented by formula (I) ##STR1## in which X represents hydrogen, fluorine, chlorine, methyl, 1-methylethyl or methoxy, with the proviso that more than one substituent X may be present in which case each X may be the same or different,n represents 2 or 3,m represents 1, in which case p represents 1, or elsem represents 0, in which case p represents 2,q represents 0 or 1, andR.sub.1 represents a hydrogen atom;or a pharmaceutically acceptable acid addition salt thereof.A compound of formula (I) has .alpha..sub.1 -adrenergic receptor antagonist activity and is useful as a therapeutic substance.

    Abstract translation: 作为式（I）表示的2-氨基嘧啶甲酰胺衍生物的化合物，其中X表示氢，氟，氯，甲基，1-甲基乙基或甲氧基，条件是多于一个取代基X可以 在这种情况下，每个X可以相同或不同，n表示2或3，m表示1，在这种情况下p表示1，或者m表示0，在这种情况下p表示2，q表示0或1， R1表示氢原子。 或其药学上可接受的酸加成盐。 式（I）化合物具有α1-肾上腺素能受体拮抗剂活性，可用作治疗物质。

    2-aminopyrimidine-4-carboxamide derivatives, their preparation and their use in therapy
    10.
    发明授权
    2-aminopyrimidine-4-carboxamide derivatives, their preparation and their use in therapy 失效
    2-氨基嘧啶-4-羧酰胺衍生物，其制备及其在治疗中的应用

    公开(公告)号：US5210086A

    公开(公告)日：1993-05-11

    申请号：US769218

    申请日：1991-10-01

    Applicant: Pascal George ,  Christian Maloizel ,  Benoit Marabout

    Inventor： Pascal George ,  Christian Maloizel ,  Benoit Marabout

    IPC: A61K31/505 ,  A61P13/02 ,  A61P15/00 ,  C07D401/12

    CPC classification number: C07D401/12

    Abstract: A compound which is a 2-aminopyrimidine-4-carboxamide derivative, of the general formula (I) ##STR1## in which m is 0 or 1,p is 0 or 1,q is 1 or 2,n is 2 or 3,R.sub.1 represents a hydrogen atom or a methyl group, and X represents at least one substituent selected from hydrogen, fluorine, chlorine, methoxy, methyl, isopropyl,or a pharmaceutically acceptable addition salt thereof, its preparation and use in therapy.

    Abstract translation: 通式（I）的化合物，其中m为0或1，p为0或1，q为1或2，n为2 或3，R 1表示氢原子或甲基，X表示选自氢，氟，氯，甲氧基，甲基，异丙基或其药学上可接受的加成盐中的至少一种取代基，其制备和用途。

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