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    Chemical compounds
    11.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号：US06544960B1

    公开(公告)日：2003-04-08

    申请号：US09530575

    申请日：2000-06-15

    Applicant: Colin David Eldred ,  Andrew Michael Kenneth Pennell

    Inventor： Colin David Eldred ,  Andrew Michael Kenneth Pennell

    IPC: A61K3170

    CPC classification number: C07H19/16 ,  Y02P20/55

    Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine Al receptor.

    Abstract translation: 式（I）的化合物，其中R 2表示C 1-3烷基，卤素或氢; R3表示1-6个碳原子的直链或支链烷基; 条件是当R 3表示C 1-3烷基时，R 2表示C 1-3烷基，R 1不能表示任选被一个或多个选自卤素，C 1-3烷基，三氟甲基，硝基，氰基，-CO 2 R c，-CONRc R d， CORc，-SORe，SO2Re，-SO3H，-SO2NRcRd，-ORc，-NHSO2Re，-NHCORc和-NRcRd; 特别是其生理上可接受的溶剂合物及其盐。 这些化合物是腺苷A1受体的激动剂。

    Adenosine derivatives
    19.
    发明授权
    Adenosine derivatives 失效
    腺苷衍生物

    公开(公告)号：US5998388A

    公开(公告)日：1999-12-07

    申请号：US180442

    申请日：1998-11-06

    Applicant: Frank Ellis ,  Stephen Swanson ,  Richard Peter Charles ,  Brian Cox ,  Andrew Michael Kenneth Pennell ,  Colin David Eldred

    Inventor： Frank Ellis ,  Stephen Swanson ,  Richard Peter Charles ,  Brian Cox ,  Andrew Michael Kenneth Pennell ,  Colin David Eldred

    IPC: C07H19/167 ,  A61K31/7076 ,  A61P9/00 ,  A61P25/00 ,  C07H15/04 ,  C07H19/16 ,  A61K31/70

    CPC classification number: C07H15/04 ,  C07H19/16

    Abstract: This invention relates to novel adenosine derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. Thus the invention provides compounds of formula (I) which are agonists at the adenosine A1 receptor. ##STR1## wherein R.sup.1 represents phenyl optionally substituted by one or more substituents selected from halogen, C.sub.1-3 alkyl, trifluoromethyl, nitro, cyano, --CO.sub.2 R.sup.a.sub.1 --CONR.sup.a R.sup.b, --COR.sup.a, --SOR.sup.c, --SO.sub.2 R.sup.c, --SO.sub.3 H, --SO.sub.2 NR.sup.a R.sup.b, --OR.sup.a, --NHSO.sub.2 R.sup.c, --NHCOR.sup.a and --NR.sup.a R.sup.b,R.sup.2 represents a C.sub.1-6 alkyl or C.sub.3-6 alkenyl group; R.sup.3 represents C.sub.1-3 alkyl;R.sup.a and R.sup.b may each independently represent hydrogen or C.sub.1-3 alkyl or, when --NR.sup.a R.sup.b is directly attached to said phenyl, R.sup.a and R.sup.b together with the nitrogen atom may form a -5 or -6 or membered heterocyclic ring optionally containing a second heteroatom selected from oxygen or nitrogen, which second nitrogen heteroatom may optionally be further substituted by hydrogen or C.sub.1-3 alkyl;R.sup.c represents C.sub.1-3 alkyl;and salts and solvates thereof, in particular physiologically acceptable salts and solvates thereof.

    Abstract translation: PCT No.PCT / EP97 / 02403 Sec。 371日期：1998年11月6日 102（e）日期1998年11月6日PCT提交1997年5月13日PCT公布。 WO97 / 43300 PCT出版物 日期1997年11月20日本发明涉及新型腺苷衍生物，其制备方法，含有它们的药物组合物及其在医药中的用途。 因此，本发明提供了作为腺苷A1受体的激动剂的式（I）化合物。 其中R 1表示任选被一个或多个选自卤素，C 1-3烷基，三氟甲基，硝基，氰基，-CO 2 R 1a -CONR a R b，-COR a，-SOR c，-SO 2 Rc，-SO 3 H，-SO 2 NR a R b，-OR a，-NHSO 2 R c ，-NHCOR a和-NR a R b，R 2表示C 1-6烷基或C 3-6烯基; R 3表示C 1-3烷基; R a和R b可各自独立地表示氢或C 1-3烷基，或当-NR a R b直接与所述苯基连接时，R a和R b与氮原子一起可以形成任选地含有选自第二杂原子的-5或-6元杂环 来自氧或氮，该第二氮杂原子可以任选地被氢或C 1-3烷基进一步取代; Rc表示C1-3烷基; 及其盐和溶剂合物，特别是其生理上可接受的盐和溶剂化物。

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