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    5,6-dihydronaphtho [1,2-b]pyrans and their use as pharmaceutical compounds
    3.
    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

    申请人： Michael Brunavs ,  Colin P. Dell ,  Peter T. Gallagher ,  William M. Owton ,  Colin W. Smith

    发明人： Michael Brunavs ,  Colin P. Dell ,  Peter T. Gallagher ,  William M. Owton ,  Colin W. Smith

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61P1/16 ,  A61P3/10 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00 ,  C07D311/92 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04

    CPC分类号： C07D405/04 ,  A61K31/35 ,  A61K31/36 ,  A61K31/38 ,  A61K31/40 ,  A61K31/44 ,  C07D311/92 ,  C07D407/04 ,  C07D409/04

    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。

    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

    申请人： Colin P. Dell ,  Colin W. Smith

    发明人： Colin P. Dell ,  Colin W. Smith

    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。

    Pharmaceutical compounds
    7.
    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

    申请人： Colin P. Dell ,  Jai P. Singh ,  Colin W. Smith

    发明人： Colin P. Dell ,  Jai P. Singh ,  Colin W. Smith

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/36 ,  A61K31/381 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61P1/16 ,  A61P3/10 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  C07D311/92 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04

    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。