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    Naphthalene carboxamides
    2.
    发明授权
    Naphthalene carboxamides 失效
    萘甲酰胺

    公开(公告)号：US5389684A

    公开(公告)日：1995-02-14

    申请号：US108038

    申请日：1993-08-17

    Applicant: John Fairhurst ,  David E. Tupper

    Inventor： John Fairhurst ,  David E. Tupper

    IPC: A61K31/165 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61P1/00 ,  A61P3/04 ,  A61P9/12 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07C231/14 ,  C07C235/66 ,  C07C237/48 ,  C07C319/20 ,  C07C323/38 ,  C07C323/62 ,  C07D209/48 ,  C07C233/22

    CPC classification number: C07C323/38 ,  C07C235/66 ,  C07C237/48 ,  C07C2101/14 ,  C07C2101/18

    Abstract: Pharmaceutical compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, nitro or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.6 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1-4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.

    Abstract translation: 下式的药物化合物：烷氧基，卤素或硝基，n为0,1,2或3，R2为氢，C1-4烷基或C2-4烯基，R3为氢，C1-4烷基，C1 -4-烷氧基，C 1-4烷硫基，卤素，硝基或-NR'R“，其中R'和R”各自为氢或C 1-4烷基，R 4和R 5各自为氢，C 1-4烷基，任选取代的苯基 或任选被1至4个C 1-4烷基取代的C 6-9环烷基，R 6是任选取代的苯基，四氢萘基，苯二甲酰亚氨基，糖精，戊二酰氨基，任选被1至4个C 1-4烷基取代的C 6-10环烷基或苯基 或任选被1-4个烷基取代的C 4-9杂取代的环烷基，x为1,2或3，y为0或1，z为0,1,2或3; 及其盐。

    Indolo isoquinoline compounds
    4.
    发明授权
    Indolo isoquinoline compounds 失效
    吲哚异喹啉化合物

    公开(公告)号：US4245095A

    公开(公告)日：1981-01-13

    申请号：US117735

    申请日：1980-02-01

    Applicant: David C. Horwell ,  David E. Tupper

    Inventor： David C. Horwell ,  David E. Tupper

    IPC: C07D471/06 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/475 ,  A61P1/08 ,  A61P25/02 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D209/90 ,  C07D209/94 ,  C07D233/74 ,  C07D471/04

    CPC classification number: C07D471/04 ,  C07D209/90 ,  C07D209/94 ,  C07D471/06

    Abstract: Isoquinoline compounds of the following formula are described: ##STR1## wherein the moiety A-B represents a group of formula:--CH.sub.2 --NR.sup.3 -- or --NR.sup.3 --CH.sub.2 --;wherein R.sup.3 represents hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl, optionally substituted benzyl, C.sub.3-6 alkenyl or C.sub.1-4 alkanoyl;wherein R represents hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or optionally substituted benzyl;wherein R.sup.1 and R.sup.2 each represent hydrogen or taken together represent a chemical bond; and wherein X is hydrogen or halogen; or an acid-addition salt thereof.The compounds are pharmaceuticals and especially useful in the treatment of disorders of the central nervous system.

    Abstract translation: 描述下式的异喹啉化合物：其中A-B部分代表式：-CH 2 -NR 3 - 或-NR 3 -CH 2 - 的基团; 其中R 3表示氢，C 1-6烷基，C 3-6环烷基C 3-6环烷基-C 1-4烷基，任选取代的苄基，C 3-6烯基或C 1-4烷酰基; 其中R表示氢，C 1-6烷基，C 3-6环烷基或任选取代的苄基; 其中R1和R2各自表示氢或一起代表化学键; 并且其中X是氢或卤素; 或其酸加成盐。 这些化合物是药物，特别可用于治疗中枢神经系统疾病。

    Indolo isoquinoline compounds
    5.
    再颁专利
    Indolo isoquinoline compounds 失效
    吲哚异喹啉化合物

    公开(公告)号：USRE31194E

    公开(公告)日：1983-03-29

    申请号：US293588

    申请日：1981-08-17

    Applicant: David C. Horwell ,  David E. Tupper

    Inventor： David C. Horwell ,  David E. Tupper

    IPC: C07D471/06 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/475 ,  A61P1/08 ,  A61P25/02 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D209/90 ,  C07D209/94 ,  C07D233/74 ,  C07D471/04

    CPC classification number: C07D471/04 ,  C07D209/90 ,  C07D209/94 ,  C07D471/06

    Abstract: Isoquinoline compounds of the following formula are described: ##STR1## wherein the moiety A-B represents a group of formula:--CH.sub.2 --NR.sup.3 -- or --NR.sup.3 --CH.sub.2 --;wherein R.sup.3 represents hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl, optionally substituted benzyl, C.sub.3-6 alkenyl or C.sub.1-4 alkanoyl;wherein R represents hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or optionally substituted benzyl;wherein R.sup.1 and R.sup.2 each represent hydrogen or taken together represent a chemical bond; and wherein X is hydrogen or halogen; or an acid-addition salt thereof.The compounds are pharmaceuticals and especially useful in the treatment of disorders of the central nervous system.

    Abstract translation: 描述下式的异喹啉化合物：其中A-B部分代表式-CH 2 -NR 3 - 或-NR 3 -CH 2 - 基团; 其中R 3表示氢，C 1-6烷基，C 3-6环烷基C 3-6环烷基-C 1-4烷基，任选取代的苄基，C 3-6烯基或C 1-4烷酰基; 其中R表示氢，C 1-6烷基，C 3-6环烷基或任选取代的苄基; 其中R1和R2各自表示氢或一起代表化学键; 并且其中X是氢或卤素; 或其酸加成盐。 这些化合物是药物，特别可用于治疗中枢神经系统疾病。

    Organic compounds and their use as pharmaceuticals
    8.
    发明授权
    Organic compounds and their use as pharmaceuticals 失效
    有机化合物及其作为药物的用途

    公开(公告)号：US5015656A

    公开(公告)日：1991-05-14

    申请号：US412691

    申请日：1989-09-26

    Applicant: Maria I. F. Fernandez ,  Terrence M. Hotten ,  David E. Tupper

    Inventor： Maria I. F. Fernandez ,  Terrence M. Hotten ,  David E. Tupper

    IPC: A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61P1/08 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D333/38 ,  C07D409/12

    CPC classification number: C07D409/12 ,  C07D333/38

    Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, hydroxy, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COOH, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge; provided that at least one of R.sup.2 and R.sup.3 is C.sub.1-4 alkoxy or C.sub.2-4 alkenyloxy; and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts and esters thereof.

    2-alkyl-thioergolines and their use for treating anxiety
    9.
    发明授权
    2-alkyl-thioergolines and their use for treating anxiety 失效
    2-烷基硫代高甘醇及其用于治疗焦虑症的用途

    公开(公告)号：US4720498A

    公开(公告)日：1988-01-19

    申请号：US791856

    申请日：1985-10-28

    Applicant: Graham H. Timms ,  David E. Tupper

    Inventor： Graham H. Timms ,  David E. Tupper

    IPC: A61K31/48 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  C07D457/02

    CPC classification number: C07D457/02

    Abstract: There is described a compound of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-4 alkyl, R.sup.2 is hydrogen, C.sub.1-4 alkyl, hydroxy C.sub.1-4 alkyl, C.sub.1-4 alkoxy C.sub.1-4 alkyl, HSC.sub.1-4 alkyl, C.sub.1-4 alkyl-S-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, optionally substituted arylthio or optionally substituted aralkylthio, and R.sup.3 is hydrogen, C.sub.1-4 alkyl, optionally substituted aryl or optionally substituted aralkyl; and salts thereof. The compounds show useful effects on the central nervous system.

    Abstract translation: 描述了式（I）的化合物，其中R 1是氢或C 1-4烷基，R 2是氢，C 1-4烷基，羟基C 1-4烷基，C 1-4烷氧基C 1-4烷基，HSCl 1-4烷基，C 1-4烷基-S-C 1-4烷基，C 1-4烷硫基，任选取代的芳硫基或任选取代的芳烷硫基，R 3是氢，C 1-4烷基，任选取代的芳基或任选取代的芳烷基; 及其盐。 这些化合物对中枢神经系统有效。

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