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    • 72. 发明授权
    • 1,6-naphthyridine derivatives
    • 1,6-萘啶衍生物
    • US4751228A
    • 1988-06-14
    • US7691
    • 1987-01-28
    • Jorgen KleinschrothKarl MannhardtJohannes HartensteinGerhard SatzingerDieter MusterWolfgang SteinbrecherBernd WagnerHartmut Osswald
    • Jorgen KleinschrothKarl MannhardtJohannes HartensteinGerhard SatzingerDieter MusterWolfgang SteinbrecherBernd WagnerHartmut Osswald
    • A61K31/435A61P3/00A61P7/02A61P9/00A61P9/08A61P9/10C07D213/80C07D471/04
    • C07D213/80C07D471/04
    • The present invention provides 1,6-naphthyridine derivatives of formula ##STR1## wherein R.sup.1 is an unsubstituted or substituted aromatic or heteroaromatic ring or an unsubstituted or substituted condensed aromatic or heterocyclic ring system, R.sup.2 is a straight-chained or branched alkyl radical containing up to 4 carbon atoms, a benzyl radical or a straight-chained or branched, substituted or unsubstituted aminoalkyl radical containing up to 8 carbon atoms, R.sup.3 is a hydrogen atom, a straight-chained or branched alkyl radical or an alkoxycarbonyl radical, in each case containing up to 4 carbon atoms, R.sup.4 is a straight-chained or branched hydrocarbon radical containing up to 21 carbon atoms, which can also contain oxygen, sulphur, nitrogen or halogen atoms and is optionally substituted by carbocyclic or heterocyclic ring systems, or is an amino, cyano, formyl, halogenomethyl or dihalomethyl radical and R.sup.5 is an alkoxycarbonyl radical or an unsubstituted or substituted carboxamide radical with, in each case, up to 21 carbon atoms which can also contain oxygen, sulphur or nitrogen atoms and is optionally substituted by carbocyclic or heterocyclic ring systems or is a carboxyl or cyano group as well as the pharmaceutically acceptable salts thereof.The compounds are useful for blood vessel diseases.The present invention also provides processes for the preparation of these 1,6-naphthyridine derivatives, pharmaceutical compositions containing them, and methods for using them.
    • 本发明提供了式(I)的1,6-萘啶衍生物,其中R 1是未取代或取代的芳族或杂芳环或未取代或取代的稠合芳族或杂环系,R2是直链或支链烷基 含有至多4个碳原子的基团,含有至多8个碳原子的苄基或直链或支链,取代或未取代的氨基烷基,R3是氢原子,直链或支链烷基或烷氧基羰基, 在每种情况下最多含有4个碳原子,R4是含有至多21个碳原子的直链或支链烃基,其也可以含有氧,硫,氮或卤素原子,并且任选地被碳环或杂环系统取代, 或者是氨基,氰基,甲酰基,卤代甲基或二卤甲基,R5是烷氧基羰基或未取代或取代的酰胺基团w 在每种情况下,最多21个碳原子,其也可以含有氧,硫或氮原子,并且任选被碳环或杂环系统取代,或者是羧基或氰基以及其药学上可接受的盐。 这些化合物可用于血管疾病。 本发明还提供制备这些1,6-萘啶衍生物的方法,含有它们的药物组合物及其使用方法。
    • 74. 发明授权
    • Benzo(b)thiophene derivatives
    • BENZO(B)噻吩衍生物
    • US4082770A
    • 1978-04-04
    • US785809
    • 1977-04-08
    • Peter Johannes StossManfred Franz Reinhold HerrmannGerhard Satzinger
    • Peter Johannes StossManfred Franz Reinhold HerrmannGerhard Satzinger
    • C07D333/70C07D333/64
    • C07D333/70
    • The present invention relates to novel benzo(b)thiophene derivatives of the general formula: ##STR1## wherein Y represents a hydrogen or halogen atom; A represents a hydrogen atom or a phenyl group which may be substituted with a halogen atom or a lower alkoxy group; B represents a radical of the formula OR' or NR.sup.2 R.sup.3, wherein R' is an alkyl radical of 1 to 5 carbon atoms which may be substituted with hydroxy, lower alkoxy, phenyl or phenoxy groups or a cycloalkyl or phenyl group which may be substituted by lower alkoxy or halogen atoms; R.sup.2 and R.sup.3, which may be identical or different, represent, if identical, hydrogen, alkyl radicals of 1 to 5 carbon atoms which may be substituted by hydroxy, lower alkoxy, phenoxy, di-lower alkylamino, or phenyl groups; or, if R.sup.2 is hydrogen, R.sup.3 represents either a hydroxyl or an amino group which may be substituted by lower alkyl, dialkyl, alkylidene, phenyl or acyl groups or a lower alkyl group which may be substituted by hydroxy, lower alkoxy, phenoxy, dialkylamino, pyrrolidino, piperidino or morpholino groups; R.sup.3 further is a cycloalkyl or phenyl group, which may be substituted by a halogen or a lower alkoxy radical; R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached, may form an aziridine, pyrrolidine, piperidine, morpholine or piperazine ring which may be substituted by lower alkyl, hydroxyalkyl, phenylalkyl, phenyl or acetyl groups; or A and B together with the C--N group may form a 5, 6, or 7-membered heterocyclic ring.The present invention further relates to the processes for the preparation of these derivatives and to the salts of these compounds with physiologically acceptable inorganic and organic acids such as hydrochloric acid, sulfuric acid, phosphoric acid, fumaric acid, oxalic acid, citric acid, etc., and the quaternary ammonium compounds.