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    Benzocyclohexanes and analgesic compositions thereof
    2.
    发明授权
    Benzocyclohexanes and analgesic compositions thereof 失效

    公开(公告)号：US5068244A

    公开(公告)日：1991-11-26

    申请号：US312885

    申请日：1989-02-17

    申请人： Anne-Marie Moura ,  Francois Clemence ,  Daniel Frechet ,  Michel Fortin

    发明人： Anne-Marie Moura ,  Francois Clemence ,  Daniel Frechet ,  Michel Fortin

    IPC分类号： A61K31/165 ,  A61K31/33 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61P7/10 ,  A61P9/06 ,  A61P9/12 ,  A61P25/04 ,  A61P25/28 ,  C07C67/00 ,  C07C209/00 ,  C07C209/16 ,  C07C209/60 ,  C07C211/42 ,  C07C215/44 ,  C07C215/70 ,  C07C217/74 ,  C07C233/79 ,  C07C235/14 ,  C07C271/52 ,  C07D295/12 ,  C07D295/135 ,  C07D333/54 ,  C07D333/60 ,  C07D521/00

    CPC分类号： C07D295/135 ,  C07D333/60

    摘要： Novel all possible enantiomeric and diastereoisomeric forms of compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2, --NH.sub.2 and mono and dialkylamino of 1 to 5 alkyl carbon atoms, n is 1 or 2, A and B have the trans configuration, one of A and B being ##STR2## R.sub.2 is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2)--.sub.n2, n.sub.2 being an integer from 0 to 5 or branched alkylene of 2 to 8 carbon atoms or --CH.sub.2 --O--, Y is selected from the group consisting of phenyl, naphthyl, indenyl, heteromonocycle of 5 to 6 ring atoms and heterobicycle, all optionally having at least one substituent and the other of A and B is ##STR3## R.sub.4 and R.sub.5 individually being selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen to which they are attached form a 5 to 6 ring heterocycle optionally containing a heteroatom selected from the group consisting of --O--, --S-- and --NH-- with the proviso 1) A is ##STR4## wherein R.sub.4 l and R.sub.5 have the above definitions and B is ##STR5## wherein R.sub.2, Z and Y have the above definition or 2) Z is --(CH.sub.2).sub.n2 -- and n.sub.2 is 0,2,3,4 or 5 or branched alkylene of 2 to 8 carbon atoms or --CH.sub.2 O-- yr 3) Y is phenyl substituted with at least one member of the group consisting of alkyl of 1 to 5 carbon atoms, alkoxy of 2 to 5 carbon atoms, --NH.sub.2 and mono and dialkylamino or 4) Y is naphthyl, indenyl, heteromonocycle of 5 to 6 ring atoms or heterobicycle, all optionally substituted with at least one substituent, except unsubstituted benzothiophene or 5) R.sub.1 is --NO.sub.2 or 6) R.sub.2 is alkyl of 4 to 5 carbon atoms or 7) R.sub.1 is hydrogen, n.sub.1 is 1, A is ##STR6## Y is selected from the group consisting of 3,4-dimethoxy-phenyl, 4-nitro-phenyl and benzothienyl and B is pyrrolidinyl or 8) R.sub.1 is hydrogen, n.sub.1 is 2, A is ##STR7## Y is selected from the group consisting of 3,4-dimethoxy-phenyl, 3,4-dichloro-phenyl, 4-trifluoromethyl-phenyl, 4-nitro-phenyl and benzothienyl and B is pyrrolidinyl and their non-toxic, pharmaceutically acceptable acid addition salts having central analgesic properties and a strong affinity for opiate receptors.

    Decahydroquinolines and central analgesic method of use thereof
    6.
    发明授权
    Decahydroquinolines and central analgesic method of use thereof 失效
    十氢喹啉和中枢镇痛药的使用方法

    公开(公告)号：US4877796A

    公开(公告)日：1989-10-31

    申请号：US084456

    申请日：1987-08-12

    申请人： Francois Clemence ,  Odile Le Martret ,  Francoise Delevallee ,  Michel Fortin

    发明人： Francois Clemence ,  Odile Le Martret ,  Francoise Delevallee ,  Michel Fortin

    IPC分类号： A61K31/47 ,  A61P7/06 ,  A61P7/10 ,  A61P9/06 ,  A61P9/12 ,  A61P25/04 ,  C07D215/40 ,  C07D401/12 ,  C07D409/12

    CPC分类号： C07D215/40

    摘要： A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms of a decahydroquinoline of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and akyl of 1 to 5 carbon atoms, A is selected from the group consisting of --(CH.sub.2).sub.n --, --CH.sub.2 O-- and alkylene substituted with alkyl having a total of 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthyl, optionally substituted indenyl, optionally substituted heteromonocycle of 5 to 6 members and optionally substituted heterobicycle with the proviso that when Z is o-alkoxy-phenyl, A is not --(CH.sub.2).sub.n -- in which n is O, and their non-toxic, pharmaceutically acceptable acid addition salts and their quaternary ammonium salts and intermediates having analgesic, diuretic, hypotensive, anti-arrithmic and anti-cerebral-ischaemic properties.

    摘要翻译： 选自下式的化合物：其中R 1为1至5个碳原子的烷基，R 2选自氢和1至5个碳原子的烷基的所有对映异构体和非对映异构体形式的十氢喹啉的化合物 原子，A选自 - （CH 2）n - ， - CH 2 O-和被具有总共2至8个碳原子的烷基取代的亚烷基，n是0至5的整数，Z选自 由任选取代的苯基，任选取代的萘基，任选取代的茚基，任选取代的5至6个成员的异单环和任选取代的杂双环，条件是当Z是邻 - 烷氧基 - 苯基时，A不是 - （CH2）n-，其中 n是O，它们的无毒的药学上可接受的酸加成盐及其季铵盐和具有止痛，利尿，降压，抗对数和抗脑缺血性质的中间体。

    Novel indanes
    7.
    发明授权
    Novel indanes 失效
    新的indanes

    公开(公告)号：US5234944A

    公开(公告)日：1993-08-10

    申请号：US970776

    申请日：1992-11-03

    申请人： Francois Clemence ,  Odile Le Martret ,  Francoise Delevallee ,  Michel Fortin

    发明人： Francois Clemence ,  Odile Le Martret ,  Francoise Delevallee ,  Michel Fortin

    IPC分类号： C07D295/135 ,  C07D311/96

    CPC分类号： C07D295/135 ,  C07D311/96

    摘要： A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula ##STR1## wherein R.sub.6 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 hydrogen or alkyl of 1 to 5 carbon atoms or taken together with the carbon atoms to which they are attached form a cycloalkyl of 3 to 6 carbon atoms optionally containing a heteroatom selected from the group consisting of --S--, --O-- and --N--, one of A and B has the formula ##STR2## and the other has the formula ##STR3## R is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Z is selected from the group consisting of --(CH.sub.2).sub.n --, branched alkylene of 2 to 8 carbon atoms and --CH.sub.2 O--, n is an integer of 0 to 5, X, X' and X" are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 4 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.2, mono and dialkylamino of 1 to 4 alkyl carbon atoms and sulfamino, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom to which they are attached form a 5 to 6 member heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR4## R.sub.1 ' is hydrogen or alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having a strong affinity for optical receptors, central analgesic, diuretic, anti-arrythmic, hypotensive and cerebral anti-ischemic activity.

    摘要翻译： 选自下组的对映异构体和非对映异构体形式的化合物及其混合物，其中R 6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分别为 氢或1至5个碳原子的烷基或与它们所连接的碳原子一起形成3至6个碳原子的环烷基，任选地含有选自-S - ， - O-和-N - ，A和B中的一个具有式，另一个具有式（Ia）的化合物，其选自氢和1至5个碳原子的烷基，Z选自 - （ CH 2）n支链亚烷基，-CH 2 O-，n为0〜5的整数，X，X'和X“分别选自氢，烷基和烷氧基的1 至4个碳原子，卤素，-OH，-CF 3，-NO 2，-NH 2，1至4个烷基的单和二烷基氨基 碳原子和磺氨基，R3和R4分别选自氢和1至5个碳原子的烷基，或与它们所连接的氮原子一起形成5至6个成员杂环，任选地含有 由-O-，-S-和R IMA'组成的基团是氢或1至4个碳原子的烷基，它们对光学受体具有强亲和力的无毒的药学上可接受的酸加成盐，中枢性镇痛药，利尿剂， 抗焦虑，降压和脑抗缺血活性。

    N-(aminoindanyl)amides as analgesics and antiarrhythmics
    8.
    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。