Quinoline derivatives as anti-inflammatory agents
    72.
    发明申请
    Quinoline derivatives as anti-inflammatory agents 失效
    喹啉衍生物作为抗炎剂

    公开(公告)号:US20060084677A1

    公开(公告)日:2006-04-20

    申请号:US11291867

    申请日:2005-11-30

    IPC分类号: A61K31/47 C07D215/60

    CPC分类号: C07D215/36

    摘要: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a CH2, CH(OH), C(O), C═NOR4, NR5, O, S, S(O), or S(O)2, and the other substituents are as defined in the specification; or prodrugs, individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents

    摘要翻译: 本发明涉及通常为抗炎和止痛化合物的化合物,其由式I表示:其中A是CH 2,CH(OH),C(O),C- NOR 4,NR 5,O,S,S(O)或S(O)2,其它取代基如所定义 在规范中; 或前药,各异构体,异构体的混合物及其药学上可接受的盐。 本发明还涉及含有这些化合物的药物组合物及其用作治疗剂的方法

    Tetrahydroquinoline derivatives
    73.
    发明申请

    公开(公告)号:US20040236109A1

    公开(公告)日:2004-11-25

    申请号:US10482707

    申请日:2004-01-02

    IPC分类号: C07D215/36 C07D215/60

    摘要: The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; YnullX is (CO)nullO, (SO)2nullO, NHC(O)nullO, NHC(S)nullO, OC(O)nullO, bond-O, C(O)nullNH, S(O)2nullNH, NHC(O)nullNH, NHC(S)nullNH, OC(O)nullNH, bond-NH, NHnullC(O), OnullC(O), NHnullS(O)2, or OnullS(O)2 or YnullX is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8, R9-aminocarbonyl(1-4C)alkyl, R8, R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-10C)aryl, (3-9C)heteroaryl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, (1-4C)(di)alkylamino(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkylthio(1-4C)alkyl, (1-4C)alkylcarbonylamino(1-4C)alkyl, (1-4C)alkoxycarbonyl(1-4C)alkyl, (1-4C)alkoxycarbonylamino(1-4C)alkyl, (3-6C)cycloalkyl, (2-6C)heterocycloylkyl, or R8 and R9 may be joined in a (2-6C)heterocycloalkyl ring. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to control fertility. 1

    Therapeutic amides
    74.
    发明申请
    Therapeutic amides 有权
    治疗酰胺

    公开(公告)号:US20040132618A1

    公开(公告)日:2004-07-08

    申请号:US10613914

    申请日:2003-07-03

    CPC分类号: C07D215/227 C07D241/44

    摘要: The invention provides compounds of the formula: 1 wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering a compound of the above formula or a salt thereof to a mammal in need thereof.

    摘要翻译: 本发明提供下式的化合物:其中A,X,Y和Z如说明书中所定义。 这些化合物是有效的抗肿瘤剂。 本发明还提供了包含上式化合物或其盐的药物组合物,可用于制备上式化合物的中间体,以及包括将上式化合物或其盐施用于有需要的哺乳动物的治疗方法 。

    Antitumor agents
    75.
    发明申请
    Antitumor agents 有权
    抗肿瘤剂

    公开(公告)号:US20030144321A1

    公开(公告)日:2003-07-31

    申请号:US10210781

    申请日:2002-07-31

    CPC分类号: C07D215/227

    摘要: The invention provides compounds of formula I: 1 wherein Y is F, Cl, Br, methyl or methoxy; and pharmaceutically acceptable salts thereof. The compounds are effective antitumor agents. The invention also provides pharmaceutical compositions comprising a compound of formula I or a salt thereof, intermediates useful for preparing a compound of formula I, and therapeutic methods comprising administering a compound of formula I or a salt thereof to a mammal in need thereof.

    摘要翻译: 本发明提供式I化合物:其中Y是F,Cl,Br,甲基或甲氧基; 及其药学上可接受的盐。 这些化合物是有效的抗肿瘤剂。 本发明还提供了包含式I化合物或其盐的药物组合物,可用于制备式I化合物的中间体,以及包括将式I化合物或其盐施用于有需要的哺乳动物的治疗方法。

    4-amino quinolines and naphthyridines and their use as medicines
    79.
    发明授权
    4-amino quinolines and naphthyridines and their use as medicines 失效
    4-氨基喹啉和萘啶并用作药物

    公开(公告)号:US5026711A

    公开(公告)日:1991-06-25

    申请号:US362105

    申请日:1989-06-06

    摘要: Compounds represented by the general formula: ##STR1## in which R.sub.1 and R.sub.2 are selected from hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl , phenyl or benzyl or R.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a C.sub.4 -C.sub.8 saturated heterocycle, R.sub.3 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or C.sub.7 -C.sub.9 phenyl-alkyl, R.sub.4 is selected from hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 and R.sub.6 are selected from hydrogen or halogen, C.sub.1 -C.sub.3 or alkoxy, nitro or trifluoromethyl; Z is selected from OH, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.4 alkyl, benzyl, C.sub.4 -C.sub.6 aryl with or without a heteroatom, or NR.sub.8 R.sub.9, R.sub.8 and R.sub.9 being selected from hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; R.sub.10 is selected from hydrogen, C.sub.1 -C.sub.4 alkyl or phenyl; n is 0, 1 or 3, p is 0 or 1 and one of the symbols A, B, C, D represents N and the others CH or A, B, C, D all represent CH and their acid addition salts, and their salts with bases. The compounds are useful in the prevention and treatment of cardiovascular diseases, as anti-allergic drugs, in the prevention and treatment of infectious states, and for the treatment of anxiety.

    摘要翻译: 由以下通式表示的化合物:其中R 1和R 2选自氢,C 1 -C 6烷基或C 2 -C 6烯基,苯基或苄基或R 1和R 2与它们所连接的氮原子一起形成C4 -C8饱和杂环,R3选自氢,C1-C6烷基,苯基或C7-C9苯基 - 烷基,R4选自氢或C1-C4烷基,R5和R6选自氢或卤素,C1-C3或 烷氧基,硝基或三氟甲基; Z选自OH,C 1 -C 6烷氧基,C 1 -C 4烷基,苄基,具有或不具有杂原子的C 4 -C 6芳基,或NR 8 R 9,R 8和R 9选自氢,C 1 -C 4烷基,苯基或苄基; R 10选自氢,C 1 -C 4烷基或苯基; n为0,1或3,p为0或1,符号A,B,C,D中的一个为N,其余CH或A,B,C,D全部为CH及其酸加成盐, 与碱的盐。 该化合物可用于预防和治疗心血管疾病,作为抗过敏药物,预防和治疗感染状态以及治疗焦虑症。