4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds
    1.
    发明授权
    4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds 失效
    4-氧代-4,6,7,8-四氢 - 吡咯并[1,2-a]吡嗪-6-甲酰胺化合物

    公开(公告)号:US07498330B2

    公开(公告)日:2009-03-03

    申请号:US11079638

    申请日:2005-03-14

    CPC分类号: C07D487/04

    摘要: Compound of formula (I): wherein: represents 1-oxidopyridyl substituted by the remainder of the molecule in any one of the positions 2, 3 and 4, m and n, which may be identical or different, each represent an integer of from 1 to 3, R1 represents hydrogen or alkyl, R2 and R3, which may be identical or different, each represent an atom or group selected from hydrogen, halogen, alkyl, hydroxy, acyloxy and alkoxy, or, together with the carbon atom carrying them, form a cycloalkane having from 3 to 6 carbon atoms, R4 and R5 each represent hydrogen, or are adjacent and, together with the carbon atoms carrying them, form a benzo ring, Ar represents aryl or heteroaryl. Medicinal products containing the same which are useful as thrombin inhibitors.

    摘要翻译: 式(I)的化合物:其中:表示由位置2,3和4中的任一个中的分子的其余部分取代的1-氧化吡啶基,m和n可以相同或不同,各自表示1的整数 至3,R 1表示氢或烷基,可以相同或不同的R 2和R 3各自表示选自氢,卤素,烷基,羟基,酰氧基和烷氧基的原子或基团,或者与携带它们的碳原子一起, 形成具有3至6个碳原子的环烷烃,R 4和R 5各自表示氢或邻近,并且与携带它们的碳原子一起形成苯并环,Ar表示芳基或杂芳基。 含有该药物的药物可用作凝血酶抑制剂。

    Bicyclic amino-pyrazinone compounds
    4.
    发明授权
    Bicyclic amino-pyrazinone compounds 失效
    双环氨基 - 吡嗪酮化合物

    公开(公告)号:US06686358B2

    公开(公告)日:2004-02-03

    申请号:US10020433

    申请日:2001-12-14

    IPC分类号: A61K3133

    摘要: A compound of formula (I): wherein: R1 represents hydrogen, or linear or branched (C1-C6)alkyl optionally substituted by one or more identical or different groups selected from aryl, heteroaryl, cycloalkyl and heterocycloalkyl, represents a saturated ring having from 4 to 7 ring members that may contain, in addition to nitrogen, one or two hetero atoms selected from O, S and —NR3 groups, wherein R3 represents hydrogen or linear or branched (C1-C6)alkyl, n represents an integer such that 1≦n≦6, R2 represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as inhibitor of trypsin-related serine proteases and thrombin.

    摘要翻译: 式(I)的化合物:其中:R 1表示氢或任选被一个或多个相同或不同的选自芳基,杂芳基,环烷基和杂环烷基的基团取代的直链或支链(C1-C6)烷基,代表饱和环, 除了氮之外,还可以含有一个或两个选自O,S和-NR 3基团的杂原子的4-7个环成员,其中R 3表示氢或直链或支链(C 1 -C 6)烷基,n表示整数,使得 1 <= N&LE; 6,R2表示说明书中所述的任何一个基团,其异构体和其药学上可接受的酸或碱的加成盐和含有它们的药物可用作胰蛋白酶相关丝氨酸蛋白酶和凝血酶的抑制剂 。

    4-oxo-4,6,7,8-Tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds
    5.
    发明申请
    4-oxo-4,6,7,8-Tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds 审中-公开
    4-氧代-4,6,7,8-四氢 - 吡咯并[1,2-a]吡嗪-6-甲酰胺化合物

    公开(公告)号:US20090131668A1

    公开(公告)日:2009-05-21

    申请号:US12321607

    申请日:2009-01-22

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04

    摘要: Compound of formula (I): wherein: represents 1-oxidopyridyl substituted by the remainder of the molecule in any one of the positions 2, 3 and 4, m and n, which may be identical or different, each represent an integer of from 1 to 3, R1 represents hydrogen or alkyl, R2 and R3, which may be identical or different, each represent an atom or group selected from hydrogen, halogen, alkyl, hydroxy, acyloxy and alkoxy, or, together with the carbon atom carrying them, form a cycloalkane having from 3 to 6 carbon atoms, R4 and R5 each represent hydrogen, or are adjacent and, together with the carbon atoms carrying them, form a benzo ring, Ar represents aryl or heteroaryl. Medicinal products containing the same which are useful as thrombin inhibitors.

    摘要翻译: 式(I)的化合物:其中:表示由位置2,3和4中的任一个中的分子的其余部分取代的1-氧化吡啶基,m和n可以相同或不同,各自表示1的整数 至3,R 1表示氢或烷基,可以相同或不同的R 2和R 3各自表示选自氢,卤素,烷基,羟基,酰氧基和烷氧基的原子或基团,或者与携带它们的碳原子一起, 形成具有3至6个碳原子的环烷烃,R 4和R 5各自表示氢或邻近,并且与携带它们的碳原子一起形成苯并环,Ar表示芳基或杂芳基。 含有该药物的药物可用作凝血酶抑制剂。

    Bicyclic amino-pyrazinone compounds
    6.
    发明授权
    Bicyclic amino-pyrazinone compounds 失效
    双环氨基 - 吡嗪酮化合物

    公开(公告)号:US06277851B1

    公开(公告)日:2001-08-21

    申请号:US09594852

    申请日:2000-06-15

    IPC分类号: A61K3150

    摘要: A compound selected from those of formula (I): wherein: R1 represents hydrogen, optionally substituted alkyl, cycloalkyl or heterocycloalkyl or a group of formula (G): wherein A1 represents single, —CH2—, —CH2—CH2— or —N(CH3)— or oxygen or sulphur, and X1 and X2, which may be identical or different, each represent carbon or nitrogen, R represents hydrogen or linear or branched (C1-C6)alkyl,  represents a saturated ring having from 4 to 7 ring members, n represents integer wherein 1≦n≦6, Ar represents aryl or heteroaryl, its isomers, N-oxydes and pharmaceutically-acceptable acid or base addition salts thereof.

    摘要翻译: 选自式(I)的化合物:其中:R 1表示氢,任选取代的烷基,环烷基或杂环烷基或式(G)的基团:其中A1表示单,-CH 2 - , - CH 2 -CH 2 - 或-N (CH 3) - 或氧或硫,以及可以相同或不同的X 1和X 2各自表示碳或氮,R表示氢或直链或支链(C 1 -C 6)烷基,表示具有4至7个 环成员,n表示其中1≤n≤6的整数,Ar表示芳基或杂芳基,其异构体,N-氧化物及其药学上可接受的酸或碱加成盐。

    4-Oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds
    7.
    发明申请
    4-Oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds 失效
    4-氧代-4,6,7,8-四氢 - 吡咯并[1,2-a]吡嗪-6-甲酰胺化合物

    公开(公告)号:US20050209234A1

    公开(公告)日:2005-09-22

    申请号:US11079638

    申请日:2005-03-14

    CPC分类号: C07D487/04

    摘要: Compound of formula (I): wherein: represents 1-oxidopyridyl substituted by the remainder of the molecule in any one of the positions 2, 3 and 4, m and n, which may be identical or different, each represent an integer of from 1 to 3, R1 represents hydrogen or alkyl, R2 and R3, which may be identical or different, each represent an atom or group selected from hydrogen, halogen, alkyl, hydroxy, acyloxy and alkoxy, or, together with the carbon atom carrying them, form a cycloalkane having from 3 to 6 carbon atoms, R4 and R5 each represent hydrogen, or are adjacent and, together with the carbon atoms carrying them, form a benzo ring, Ar represents aryl or heteroaryl. Medicinal products containing the same which are useful as thrombin inhibitors.

    摘要翻译: 式(I)的化合物:其中:表示由位置2,3和4中的任一个中的分子的其余部分取代的1-氧化吡啶基,m和n可以相同或不同,各自表示1的整数 至3,R 1表示氢或烷基,R 2和R 3可以相同或不同,各自表示原子或基团 选自氢,卤素,烷基,羟基,酰氧基和烷氧基,或者与携带它们的碳原子一起形成具有3至6个碳原子的环烷烃,R 4和R 5 各自表示氢,或者相邻,并且与携带它们的碳原子一起形成苯并环,Ar表示芳基或杂芳基。 含有该药物的药物可用作凝血酶抑制剂。