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    Novel therapeutic compositions and method involving thiazol-carboxamides
    32.
    发明授权
    Novel therapeutic compositions and method involving thiazol-carboxamides 失效
    涉及噻唑 - 甲酰胺的新型治疗组合物和方法

    公开(公告)号：US3966950A

    公开(公告)日：1976-06-29

    申请号：US539327

    申请日：1975-01-08

    申请人： Odile Le Martret ,  Francois Clemence

    发明人： Odile Le Martret ,  Francois Clemence

    IPC分类号： C07D295/13 ,  A61K20060101 ,  A61K31/425 ,  A61K31/495 ,  C07D20060101 ,  C07D277/20 ,  C07D277/56 ,  C07D295/096 ,  C07D417/12

    CPC分类号： C07D295/13 ,  C07D277/56

    摘要： Novel thiazolcarboxamides of the formula ##EQU1## wherein R is selected from the group consisting of alkyl of 1 to 6 carbon atoms and phenyl, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, n is a whole number from 2 to 5 and X and X.sub.1 are individually selected from the group consisting of hydrogen, halogen, trifluoromethyl and alkyl, alkoxy and alkylthio of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having .alpha.-adrenolytic activity and their preparation.

    摘要翻译： 式O分子式CN-（CH2）n-NNI | R1的新型噻唑羧酰胺其中R选自1至6个碳原子的烷基和苯基，R 1选自氢和1的烷基 至4个碳原子，n为2至5的整数，X和X 1分别选自氢，卤素，三氟甲基和具有1至4个碳原子的烷基，烷氧基和烷硫基，并且其无毒的，药学上 具有α-脱水活性的可接受的酸加成盐及其制备。

    Analgesic 4-substituted indoles
    35.
    发明授权
    Analgesic 4-substituted indoles 失效
    止痛剂4-取代吲哚

    公开(公告)号：US4737505A

    公开(公告)日：1988-04-12

    申请号：US757515

    申请日：1985-07-19

    申请人： Jacques Guillaume ,  Francois Clemence ,  Lucien Nedelec ,  Francoise DeLevallee

    发明人： Jacques Guillaume ,  Francois Clemence ,  Lucien Nedelec ,  Francoise DeLevallee

    IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61P25/04 ,  C07D401/04

    CPC分类号： C07D401/04

    摘要： Novel indole of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 12 carbon atoms, Z is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, cyanoalkyl of 3 to 8 carbon atoms, hydroxyalkyl of 2 to 8 carbon atoms, --(CH.sub.2).sub.n --O--B, ##STR2## aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, CF.sub.3 --, CF.sub.3 O--, --NH.sub.2 and --NO.sub.2 and cycloalkyl alkyl of 4 to 12 carbon atoms, n is one integer from 2 to 8, B is selected from the group consisting of aryl and heteroaryl, both optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, hydroxyalkyl of 1 to 5 carbon atoms, nitro, amino, CF.sub.3 --, alkenyl and alkenyloxy of 2 to 5 carbon atoms and alkynyl and alkynyloxy of 2 to 5 carbon atoms, a and b are both hydrogen or a is hydrogen and b is --OH or alkoxy of 1 to 8 carbon atoms or a and b together form a carbon-carbon bond and the 2-oxo with dotted lines indicates its possible presence with the double bond in the indole ring missing and its non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity of the morphine type.

    摘要翻译： 其中R选自氢，1至8个碳原子的烷基和7至12个碳原子的芳烷基的式VI的新型吲哚，Z选自氢，1至 具有2至8个碳原子的烯基，3至8个碳原子的氰基烷基，2至8个碳原子的羟烷基， - （CH 2）n OB，7-12个碳原子的芳基，其任选被至少一个 由1至5个碳原子的烷基和烷氧基组成的组，卤素，-OH，CF 3 - ，CF 3 O-，-NH 2和-NO 2以及4至12个碳原子的环烷基烷基，n是2至8的一个整数 B选自芳基和杂芳基，两者任选被至少一个由1至5个碳原子的烷基和烷氧基组成的组中的一个取代，卤素，-OH，1-5个碳原子的羟基烷基，硝基 ，2至5个碳原子的氨基，CF 3 - ，链烯基和烯氧基以及2至5个碳原子的炔基和炔氧基，a和ba 氢或a是氢并且b是-OH或1-8个碳原子的烷氧基或a和b一起形成碳 - 碳键，并且具有虚线的2-氧代表示其在吲哚中可能存在双键 戒指及其无毒，药学上可接受的具有吗啡类止痛活性的酸加成盐。

    N-(aminoindanyl)amides as analgesics and antiarrhythmics
    37.
    发明授权
    N-(aminoindanyl)amides as analgesics and antiarrhythmics 失效
    N-（氨基茚满基）酰胺作为镇痛药和抗心律失常药

    公开(公告)号：US4988727A

    公开(公告)日：1991-01-29

    申请号：US409048

    申请日：1989-09-19

    申请人： Francois Clemence ,  Michel Fortin

    发明人： Francois Clemence ,  Michel Fortin

    IPC分类号： C07D295/135 ,  C07D295/155 ,  C07D333/24 ,  C07D333/54

    CPC分类号： C07D295/135 ,  C07D295/155 ,  C07D333/24 ,  C07D333/54

    摘要： A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms possible of compounds of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, one of A and B being ##STR2## and the other being ##STR3## R is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n -- or branched alkylene of 2 to 8 carbon atoms, n is an integer from 0 to 5, Y is selected from the group consisting of naphthyl, indenyl, heterobicyclics and heteromonocyclic containing 5 to 6 ring members, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.2 monoalkylamino and dialkylamino of 1 to 4 alkyl carbon atoms and phenyl optionally substituted with at least one member of the group consisting of halogen and alkyl and alkoxy of 1 to 4 carbon atoms, R.sub.3 and R.sub.4 are individually hydrogen or alkyl or 1 to 5 carbon atoms or taken together with the nitrogen form a heterocyclic of 5 to 6 ring members and optionally containing --O--, --S-- or nitrogen in the ring and their non-toxic, pharmaceutically acceptable acid addition salts having central analgesic and antiarythmic activity among other activities.

    摘要翻译： 选自下列化合物的化合物：其中X选自氢，卤素和1至5个碳原子的烷基和烷氧基，R 1和R 2的所有对映异构体和非对映异构体形式。 分别选自氢和1至5个碳原子的烷基，A和B之一为“IMAGE”，另一个为R 1为氢或1至5个碳原子的烷基，Z为 - （ CH 2）2至8个碳原子的正或支链亚烷基，n为0至5的整数，Y选自萘基，茚基，异双环烯烃和含有5至6个环成员的杂单环，全部任选被 由1至5个碳原子的烷基和烷氧基，卤素，-OH，-CF 3，-NO 2，-NH 2单烷基氨基和1至4个烷基碳原子的二烷基氨基组成的组中的至少一个和任选被至少一个成员取代的苯基 由卤素和烷基组成的组中 具有1至4个碳原子的烷氧基，R 3和R 4独立地为氢或烷基或1至5个碳原子，或与氮一起形成5至6个环成员的杂环，并任选地含有-O - ， - S-或 环中的氮和它们的无毒的药学上可接受的酸加成盐，具有其他活性的中枢镇痛和抗血液活性。