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。

    4-oxo-4,6,7,8-Tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds
    2.
    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。

    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 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。

    Octahydro-2H-pyrido[1,2-a]pyrazine compounds
    9.
    发明授权
    Octahydro-2H-pyrido[1,2-a]pyrazine compounds 失效
    八氢-2H-吡啶并[1,2-a]吡嗪化合物

    公开(公告)号:US06992085B2

    公开(公告)日:2006-01-31

    申请号:US10195019

    申请日:2002-07-12

    IPC分类号: A61K31/4985 C07D471/04

    CPC分类号: C07D471/04

    摘要: A compound selected from those of formula (I): wherein: Ra represents linear or branched (C1–C6)alkylene, X represents a group selected from W1, —C(W1)—W2—, —W2—C(W1)—, —W2—C(W1)W2—, —W2—Ra— and —CH(OR1)— wherein W1, W2 and R1 are as defined in the description, when Y represents aryl or heteroaryl, or X represents a group selected from single bond, —C(W1)—, —W2—C(W1)—, —W2—Ra and —CH(OR1)— wherein W1, W2, Ra and R1 are as defined hereinbefore, when Y represents a fused bicyclic group, of formula: wherein: A represents nitrogen-containing heterocycle having from 4 to 7 ring members that is unsaturated or partially saturated and optionally contains a second hetero atom, B represents phenyl ring optionally substituted by one or more groups as defined in the description, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, medicinal products containing the same are useful in the treatment of cognitive deficiencies.

    摘要翻译: 选自式(I)的化合物:其中:R a表示直链或支链(C 1 -C 6 -C 6)亚烷基,X表示选自W SUB -C(W 1) - W 2 - , - W 2 -C(W 1) ) - ,-W 2 -C(W 1)W 2 - , - W 2

    Beta-carboline compounds
    10.
    发明授权
    Beta-carboline compounds 失效
    β-咔啉化合物

    公开(公告)号:US06350757B1

    公开(公告)日:2002-02-26

    申请号:US09621742

    申请日:2000-07-21

    IPC分类号: C07D47114

    CPC分类号: C07D471/04

    摘要: A compound selected from those of formula (I): wherein: represents single or double bond, R1 represents hydrogen, alkyl, —R6-aryl, —R6-cycloalkyl, —R6-heterocycle, —CO2R7—, —COR8, or —CONHR8, wherein R6, R7, and R8 are as defined in the description, R2 represents cyano, mono- or di-alkylaminoalkylaminocarbonyl, —CO2R8, —CONHR8, —NR8R9, —NHCO2R7, or —COR8 wherein R7, R8, and R9 are as defined in the description, R3 and R4 together form (C3-C10)cycloalkyl, R5 represents hydrogen, alkyl, or arylalkyl, Ra, Rb, Rc, Rd, which may be identical or different, represent a group as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of CNS disorders.

    摘要翻译: 选自式(I)的化合物:其中:CUSTOM-CHARACTER FILE =“US06350757-20020226-P00900.TIF”ID =“CUSTOM-CHARACTER-00001”>表示单键或双键,R1表示氢,烷基, -R6-芳基,-R6-环烷基,-R6-杂环,-CO2R7-,-COR8或-CONHR8,其中R6,R7和R8如说明书中所定义,R 2表示氰基,单或二烷基氨基烷基氨基羰基 ,-CO 2 R 8,-CONHR 8,-NR 8 R 9,-NHCO 2 R 7或-COR 8,其中R 7,R 8和R 9如说明书中所定义,R 3和R 4一起形成(C 3 -C 10)环烷基,R 5表示氢,烷基或芳烷基 可以相同或不同的R a,R b,R c,R d表示本说明书中定义的基团,其异构体及其药学上可接受的酸或碱加成盐,以及含有该基团的药物,其可用于 治疗中枢神经系统疾病。