Therapy for diabetic complications
    6.
    发明授权
    Therapy for diabetic complications 失效
    治疗糖尿病并发症

    公开(公告)号:US5281619A

    公开(公告)日:1994-01-25

    申请号:US34011

    申请日:1993-03-22

    IPC分类号: A61K31/35

    CPC分类号: A61K31/35

    摘要: This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: ##STR1## in which n, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are variables.

    摘要翻译: 本发明提供了一种治疗哺乳动物糖尿病并发症的方法,其包括施用式I化合物:(*化学结构*)(I),其中n,R1,R2,R3和R4是可变的。

    5,6-dihydronaphtho [1,2-b]pyrans and their use as pharmaceutical
compounds
    7.
    发明授权
    5,6-dihydronaphtho [1,2-b]pyrans and their use as pharmaceutical compounds 失效
    5,6-二氢萘并[1,2-b]吡喃及其作为药物化合物的用途

    公开(公告)号:US5622987A

    公开(公告)日:1997-04-22

    申请号:US461342

    申请日:1995-06-05

    摘要: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1 -4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an alkyl group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an alkyl group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.12, --N(COR.sup.11).sub.2 or --N.dbd.CHOCH.sub.2 R.sup.11 where R.sup.11 and R.sup.12 are each hydrogen or C.sub.1-4 alkyl optionally substituted with carboxy, --N.dbd.CH--NR.sup.13 R.sup.14 where R.sup.13 is hydrogen or C.sub.1-4 alkyl and R.sup.14 is C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted heteroaryl, ##STR2## where X is C.sub.2-4 alkylene, or --NHSO.sub.2 R.sup.15 where R.sup.15 is C.sub.1-4 alkyl, trifluoromethyl or optionally substituted phenyl; and salts thereof.

    摘要翻译: 式“IMAGE”的药物化合物,其中n为0,1或2,R 1连接在7,8,9或10位的任何位置,每个R 1为卤素,羧基,三氟甲基,羟基,C 1-4烷基 C 1-4烷氧基,C 1-4烷硫基,羟基-C 1-4烷基,羟基-C 1-4烷氧基,含氮杂环基,硝基,三氟甲氧基,-COOR 5,其中R 5为烷基,-COR 6,-CONR 6 R 7或 - NR 6 R 7,其中R 6和R 7各自为氢或C 1-4烷基; R 2是选自噻吩基,吡啶基,苯并噻吩基,喹啉基,苯并呋喃基或苯并咪唑基的苯基,萘基或杂芳基,所述苯基,萘基和杂芳基任选被取代,或R 2是任选被C 1-4烷基取代的呋喃基; R 3是腈,羧基,-COOR 8,其中R 8是烷基,或-CONR 9 R 10,其中R 9和R 10各自是氢或C 1-4烷基; 并且R 4为-NR 11 R 12,-NR 11 COR 12,-N(COR 11)2或-N = CHOCH 2 R 11,其中R 11和R 12各自为氢或任选被羧基取代的C 1-4烷基,-N = CH-NR 13 R 14,其中R 13为氢或C1- 4烷基和R 14是C 1-4烷基,任选取代的苯基或任选取代的杂芳基,其中X是C 2-4亚烷基或-NHSO 2 R 15,其中R 15是C 1-4烷基,三氟甲基或任选取代的苯基; 及其盐。

    Pharmaceutical compounds
    10.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号:US5284868A

    公开(公告)日:1994-02-08

    申请号:US951629

    申请日:1992-09-25

    CPC分类号: C07D405/04 C07D311/92

    摘要: A pharmaceutical compound of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 5, 6, 7, 8, 9 or 10, and each R.sup.1 is halo, trifluoromethyl, C.sub.1-4 alkoxy, hydroxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, trifluoromethoxy, carboxy, --COOR.sup.5 where R.sup.5 is an ester group, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl; R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl, or R.sup.11 SO.sub.2 -- where R.sup.11 is C.sub.1-4 alkyl or optionally substituted phenyl; and R.sup.4 is --NR.sup.12 R.sup.13, --NHCOR.sup.12, --N(COR.sup.12).sub.2 or --N.dbd.CHOCH.sub.2 R.sup.12 where R.sup.12 and R.sup.13 are each hydrogen or C.sub.1-4 alkyl optionally substituted with carboxy, ##STR2## where X is C.sub.2-4 alkylene, or --NHSO.sub.2 R.sup.14 where R.sup.14 is C.sub.1-4 alkyl or optionally substituted phenyl; provided that when n is 0, R.sup.3 is nitrile and R.sup.4 is --NH.sub.2, R.sup.2 is not phenyl or phenyl substituted in the para-position with a single chloro, hydroxy or methoxy substituent; and salts thereof.

    摘要翻译: 式(*化学结构*)(I)的药物化合物,其中n为0,1或2,R 1在任何位置5,6,7,8,9或10处连接,并且每个R 1为卤素 三氟甲基,C 1-4烷氧基,羟基,硝基,C 1-4烷基,C 1-4烷硫基,羟基-C 1-4烷基,羟基-C 1-4烷氧基,三氟甲氧基,羧基,-COOR 5,其中R 5为酯基, CONR 6 R 7或-NR 6 R 7,其中R 6和R 7各自为氢或C 1-4烷基; R 2是选自噻吩基,吡啶基,苯并噻吩基,喹啉基,苯并呋喃基或苯并咪唑基的苯基,萘基或杂芳基,所述苯基,萘基和杂芳基任选被取代,或R 2是任选被C 1-4烷基取代的呋喃基; R3是腈,羧基,-COOR8,其中R8是酯基,-CONR9R10,其中R9和R10各自是氢或C1-4烷基,或R11SO2-,其中R11是C1-4烷基或任选取代的苯基; 并且R 4为-NR 12 R 13,-NHCOR 12,-N(COR 12)2或-N = CHOCH 2 R 12,其中R 12和R 13各自为氢或任选被羧基取代的C 1-4烷基,(*化学结构*)其中X为C 2-4亚烷基 或-NHSO 2 R 14,其中R 14是C 1-4烷基或任选取代的苯基; 条件是当n为0时,R3为腈,R4为-NH2,R2不为苯基或在对位被苯基取代的苯基与单个氯,羟基或甲氧基取代基取代; 及其盐。