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

    Pharmaceutical compounds
    2.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号：US5410061A

    公开(公告)日：1995-04-25

    申请号：US962365

    申请日：1992-10-16

    申请人： Jeremy Gilmore ,  John R. Harris

    发明人： Jeremy Gilmore ,  John R. Harris

    IPC分类号： A61K31/47 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14 ,  C07D401/10 ,  A61K31/475

    CPC分类号： C07D401/12 ,  C07D401/14

    摘要： A compound having pharmaceutical activity, of the formula ##STR1## in which A is hydrogen or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x is 0 or 1 to 4, R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl and R.sup.3 is --CN, --COOH, tetrazolyl or --CONHSO.sub.2 R.sup.4 where R.sup.4 is optionally substituted phenyl, and ##STR2## where R.sup.5 and R.sup.6 are each hydrogen, C.sub.1-4 alkyl or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x, R.sup.1, R.sup.2 and R.sup.3 are as defined above, and R.sup.7 is hydrogen, C.sub.1-4 alkyl or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x is 1 to 4, and R.sup.1, R.sup.2 and R.sup.3 are as defined above;provided that when A is hydrogen at least one of R.sup.5, R.sup.6 and R.sup.7is --(CR.sup.1 R.sup.2).sub.x R.sup.3, and provided that when ##STR3## A is --(CR.sup.1 R.sup.2).sub.x R.sup.3 and x is 1 to 4 then R.sup.3 is --CONHSO.sub.2 R.sup.4 ;and salts and esters thereof.

    摘要翻译： 具有药物活性的化合物，其中A为氢或 - （CR 1 R 2）x R 3，其中x为0或1至4，R 1和R 2为氢或C 1-4烷基，R 3为 - CN，-COOH，四唑基或-CONHSO 2 R 4，其中R 4是任选取代的苯基，和其中R 5和R 6各自是氢，C 1-4烷基或 - （CR 1 R 2）x R 3，其中x，R 1，R 2 和R 3如上所定义，并且R 7是氢，C 1-4烷基或 - （CR 1 R 2）x R 3，其中x是1至4，并且R 1，R 2和R 3如上定义; 条件是当A为氢时，R 5，R 6和R 7中的至少一个为 - （CR 1 R 2）x R 3，并且条件是当A为 - （CR 1 R 2）x R 3且x为1至4时，R 3为-CONHSO 2 R 4; 及其盐和酯。

    Pharmaceutical compounds
    3.
    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。

    Benzodiazepine compounds and their use as pharmaceuticals
    4.
    发明授权
    Benzodiazepine compounds and their use as pharmaceuticals 失效
    苯并二氮杂类化合物及其作为药物的用途

    公开(公告)号：US5051516A

    公开(公告)日：1991-09-24

    申请号：US562055

    申请日：1990-08-02

    申请人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    发明人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    IPC分类号： C07D277/20 ,  A61K31/00 ,  A61K31/55 ,  A61P25/18 ,  A61P25/20 ,  C07D277/56 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D277/56

    摘要： Pharmaceutical thiazolo-[1,5]benzodiazepines of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula formula ##STR2## where R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, benzyl or ZO--C.sub.2-6 alkyl where Z is hydrogen or an acyl group, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio; and in which ##STR3## represents a thiazole ring selected from ##STR4## and acid addition salts thereof. The compounds have central nervous system activity.

    Isothiocyanato-azobenzene-sulfonic, arsonic and substituted-glutamic acid haptens
    8.
    发明授权
    Isothiocyanato-azobenzene-sulfonic, arsonic and substituted-glutamic acid haptens 失效
    异硫氰酸 - 偶氮苯磺酸，芳香和取代谷氨酸半抗原

    公开(公告)号：US4442032A

    公开(公告)日：1984-04-10

    申请号：US325513

    申请日：1981-11-27

    申请人： Robin G. Simmonds

    发明人： Robin G. Simmonds

    IPC分类号： G01N33/53 ,  A61K39/385 ,  C07C331/28 ,  C07F9/76 ,  G01N33/531 ,  C07C107/06 ,  C07C113/04 ,  C09B29/12 ,  C09B33/044

    CPC分类号： G01N33/531 ,  C07F9/76 ,  Y10S530/806 ,  Y10S530/807 ,  Y10S534/03

    摘要： Compounds of formula (I) ##STR1## in which n is 1 or 2, R.sup.1 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, halo or hydroxy, m is 0, 1 or 2, R.sup.2 is an immunogenic determinant and x is 1 or 2, provided that when n is 1, x is 1 or 2 and there is one diazo moiety at the 3-position or two diazo moieties at the 3- and 5-positions, with respect to the isothiocyanate group, and the hydroxy group is at the 4-position; and provided that when n is 2, x is 1 and the diazo moiety is at the 4-position and the hydroxy groups are at the 3- and 5-positions, are described. The compounds are useful in the preparation of immunoglobulin conjugates for employment in diagnostic techniques.

    摘要翻译： 式（I）化合物其中n为1或2，R 1为C 1-4烷基，C 1-4烷氧基，硝基，氨基，卤素或羟基，m为0,1或2，R 2为 免疫原性决定簇，x为1或2，条件是当n为1时，x为1或2，并且在3-位有一个重氮部分或3-和5-位上的两个重氮部分相对于 异硫氰酸酯基，羟基为4-位; 并且条件是当n为2时，x为1，重氮部分为4-位，羟基为3-和5-位。 该化合物可用于制备用于诊断技术的免疫球蛋白缀合物。

    Method of treating hypersensitivity disease with benzoxazole derivatives
    9.
    发明授权
    Method of treating hypersensitivity disease with benzoxazole derivatives 失效
    用苯并恶唑衍生物治疗超敏反应疾病的方法

    公开(公告)号：US4416892A

    公开(公告)日：1983-11-22

    申请号：US368079

    申请日：1982-04-14

    申请人： William Dawson

    发明人： William Dawson

    IPC分类号： A61K31/42

    CPC分类号： A61K31/42 ,  Y10S514/826 ,  Y10S514/849 ,  Y10S514/861

    摘要： The invention relates to a method for the prophylactic or therapeutic treatment of an immediate hypersensitivity disease, which comprises administering to a mammal, including a human, a compound of the following formula ##STR1## in which the group --CHR.sup.1 R.sup.2 is in the 5- or 6- position of the benzoxazole nucleus, R.sup.1 is hydrogen or C.sub.1-4 alkyl, R.sup.2 is selected from the group --COOH or a salt or ester thereof, the group --CONH.sub.2 and the group --CH.sub.2 OH, and in which R.sup.4 is a phenyl group optionally substituted by one or two groups selected from halogen, C.sub.1-4 alkoxy, C.sub.1-4 alkyl and C.sub.1-4 haloalkyl, or optionally substituted in two adjacent positions by methylenedioxy.

    摘要翻译： 本发明涉及一种用于预防或治疗即时超敏反应疾病的方法，该方法包括向哺乳动物（包括人）施用下列式的化合物，其中基团-CHR1R2为 苯并恶唑核的5-或6-位，R 1是氢或C 1-4烷基，R 2选自-COOH或其盐或酯，基团-CONH 2和基团-CH 2 OH，其中R 4是 任选被一个或两个选自卤素，C 1-4烷氧基，C 1-4烷基和C 1-4卤代烷基的基团取代的苯基，或在亚邻二氧基的两个相邻位置任意取代。

    Pyrazolo [3,4-b][1,5]benzodiazepine compounds
    10.
    发明授权
    Pyrazolo [3,4-b][1,5]benzodiazepine compounds 失效
    吡唑并[3,4-b] [1,5]苯并二氮杂化合物

    公开(公告)号：US4404137A

    公开(公告)日：1983-09-13

    申请号：US193200

    申请日：1980-10-02

    申请人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    发明人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    IPC分类号： A61K31/00 ,  A61P1/08 ,  A61P25/18 ,  A61P25/20 ,  C07D231/38 ,  C07D487/04 ,  A61K31/55

    CPC分类号： C07D231/38 ,  C07D487/04

    摘要： Compounds are described of the formula ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, halogen, C.sub.1-4 haloalkyl, C.sub.1-4 alkanoyl, nitro, amino, C.sub.2-4 acylamino, cyano, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 haloalkoxy or a group of the formula --SO.sub.2 N(R.sup.8).sub.2, --SO.sub.2 R.sup.8 or --SO.sub.3 R.sup.8 where R.sup.8 is C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or optionally substituted phenyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.9 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkanoyl, benzyl, cyano or optionally substituted phenyl, where R.sup.10 is hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl and where n is 0 or 1; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, benzyl, C.sub.1-6 alkanoyl, C.sub.1-4 carbalkoxy or benzoyl; and in which R.sup.7 is one of the values of R.sup.6 or halogen, nitro, cyano, amino or C.sub.1-4 acylamino. The compounds are active as pharmaceuticals and particularly in the treatment of disorders of the central nervous system. Intermediate compounds in which R.sup.5 is thiol, hydroxy, or amino are also described.

    摘要翻译： 化合物描述为式“IMAGE”或其酸加成盐; 其中R 1，R 2，R 3和R 4独立地表示氢，C 1-4烷基，C 2-4烯基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，卤素，C 1-4卤代烷基，C 1-4烷酰基，硝基 ，氨基，C2-4酰氨基，氰基，羟基，C1-4烷氧基，C1-4烷硫基，C1-4卤代烷氧基或式-SO2N（R8）2，-SO2R8或-SO3R8的基团，其中R8为C1-4 烷基，C 1-4卤代烷基或任选取代的苯基; 其中R 5是下式的基团，其中R 9是氢，C 1-4烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，C 1-4卤代烷基，C 2-4链烯基，C 1-4烷酰基 苄基，氰基或任选取代的苯基，其中R 10是氢，C 1-4烷基或任选取代的苯基，其中n是0或1; 其中R 6是氢，C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，C 1-4卤代烷基，苄基，C 1-6烷酰基，C 1-4烷氧基或苯甲酰基; 并且其中R 7是R 6或卤素，硝基，氰基，氨基或C 1-4酰氨基的值之一。 这些化合物作为药物是有活性的，特别是用于治疗中枢神经系统疾病。 还描述了其中R 5为硫醇，羟基或氨基的中间体化合物。