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    Novel 10.beta.-alkynyl-steroids
    3.
    发明授权
    Novel 10.beta.-alkynyl-steroids 失效
    新型10个β-炔基 - 类固醇

    公开(公告)号：US4987128A

    公开(公告)日：1991-01-22

    申请号：US18199

    申请日：1987-02-24

    申请人： Lucien Nedelec ,  Francois Nique ,  Anne-Marie Moura

    发明人： Lucien Nedelec ,  Francois Nique ,  Anne-Marie Moura

    IPC分类号： A61K31/585 ,  A61P9/00 ,  C07J1/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J43/00 ,  C07J53/00

    CPC分类号： C07J21/006 ,  C07J1/007 ,  C07J21/003 ,  C07J33/005 ,  C07J43/006

    摘要： Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R.sub.2 is methyl or ethyl, X and Y taken together form a member selected from the group consisting of ##STR2## Alk is alkyl of 1 to 8 carbon atoms or X is hydroxy and Y is ##STR3## or X is optionally acylated or etherified hydroxy and Y is selected from the group consisting of --CH.sub.2 --CH.sub.2 --CH.sub.2 --OH, hydrogen, R.sub.4, and --CH.sub.2 --CH.sub.2 --COOM, M is selected from the group consisting of hydrogen, --NH.sub.4 and alkali metal and R.sub.4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, the dotted lines indicate the optional presence of a second carbon-carbon bond when R.sub.6 and R.sub.7 and the carbon to which they are attached do not form cyclopropyl and the wavy lines indicate that R.sub.6 and R.sub.7 may be in the .alpha. or .beta. position with the proviso that R is not hydrogen when R.sub.6 and R.sub.7 are hydrogen, R.sub.2 is methyl, X is optionally acylated or etherified hydroxy, Y is hydrogen or R.sub.4 and the dotted lines are not a second carbon-carbon bond having aldosterone antagonistic activity and increased hydrosodic diuresis with organic potassium conservation with little secondary hormone effects.

    摘要翻译： 新颖的式10的β-炔基 - 类固醇，其中R选自氢，任选取代的烷基和1至8个碳原子的烷氧基，任选取代的碳原子数2〜8的烯基和炔基，任选地 取代的芳基和芳烷基，任意酯化的羧基，二烷基氨基与1至6个碳原子的烷基，卤素和1至7个烷基碳原子的三烷基甲硅烷基，R 6和R 7与它们所连接的碳原子一起形成环丙基或R6是氢 并且R 7是R 1，R 1选自氢，任选取代的1至6个碳原子的烷基，任选取代的烯基和2至6个碳原子的炔基和乙酰硫基，R 2是甲基或乙基，X和Y一起 形成选自由以下组成的组中的一个成员：Alk为1至8个碳原子的烷基或X为羟基，Y为X或X任选被酰化或醚化羟基，Y选自gro 其由-CH 2 -CH 2 -CH 2 -OH，氢，R 4和-CH 2 -CH 2 -COOM组成，M选自氢，-NH 4和碱金属，R 4选自由以下组成的组： 1至6个碳原子和2至6个碳原子的烯基和炔基，虚线表示当R6和R7以及它们所连接的碳不形成环丙基时，任选存在第二碳 - 碳键，波浪线 表示R6和R7可以在α或β位置，条件是当R6和R7是氢时，R不是氢，R2是甲基，X是任选被酰化或醚化羟基，Y是氢或R4，虚线是 不是具有醛固酮拮抗活性的第二个碳 - 碳键和具有少量次生激素效应的有机钾保护的增加的水溶性利尿。

    Novel 10-substituted steroids and their use in the induction of aldosterone antagonistic activity
    4.
    发明授权
    Novel 10-substituted steroids and their use in the induction of aldosterone antagonistic activity 失效

    公开(公告)号：US4701449A

    公开(公告)日：1987-10-20

    申请号：US768867

    申请日：1985-08-23

    申请人： Vesperto Torelli ,  Lucien Nedelec ,  Martine Moguilewski ,  Anne-Marie Moura

    发明人： Vesperto Torelli ,  Lucien Nedelec ,  Martine Moguilewski ,  Anne-Marie Moura

    IPC分类号： A61K31/58 ,  A61P9/04 ,  A61P9/10 ,  C07J1/00 ,  C07J5/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J53/00 ,  A61K31/585 ,  A61K31/56

    CPC分类号： C07J1/0011 ,  C07J1/0022 ,  C07J1/0033 ,  C07J1/0037 ,  C07J1/0044 ,  C07J21/00 ,  C07J21/003 ,  C07J21/006 ,  C07J31/003 ,  C07J31/006 ,  C07J33/005 ,  C07J41/0038 ,  C07J41/0094 ,  C07J43/006 ,  C07J51/00 ,  C07J53/007

    摘要： Novel 10-substituted steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 8 carbon atoms, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 8 carbon atoms, aryl and substituted aryl, aralkyl and substituted aralkyl, protected hydroxy, optionally esterified carboxy, --NH.sub.2, protected amino, mono and di-alkyl amino of 1 to 4 alkyl carbon atoms, halogen and trialkylsilyl, R.sub.2 is methyl or ethyl, R.sub.6 and R.sub.7 together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 6 carbon atoms, acetylthio and alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 6 carbon atoms, X is optionally acylated or etherified hydroxyl and Y is selected from the group consisting of hydrogen, R.sub.4, --CH.sub.2 --CH.sub.2 COOM and --CH.sub.2 --CH.sub.2 --CH.sub.2 OH, M is hydrogen, alkali metal or --NH.sub.4 or X and Y together form a member of the group consisting of ##STR2## or X is --OH and Y is ##STR3## R.sub.4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, Alk is alkyl of 1 to 8 carbon atoms, the dotted lines in the 1(2) and 6(7) indicate the optional presence of a second carbon-carbon bond with the proviso that when R.sub.6 and R.sub.7 form cyclopropyl, there is no 6(7) second bond, the dotted line in 10-substituent indicates the optional presence of a third carbon-carbon bond, the wavy lines at R.sub.6 and R.sub.7 indicate the possible .alpha.- or .beta.-position with the proviso that R is not hydrogen when R.sub.6 and R.sub.7 are hydrogen R.sub.2 is methyl, X is hydroxy or acetoxy and Y is hydrogen, the dotted lines at 1(2) and 6(7) do not represent a second bond and the dotted line in the 10-substituent is a third carbon-carbon bond useful as aldosterone antagonists and for increasing hydrosodium diuresis while preserving organic potassium with reduced hormonal side effects.

    Guanidinoalkyl-1,1-bisphosphonic acid derivatives, process for their preparation and their use
    6.
    发明授权
    Guanidinoalkyl-1,1-bisphosphonic acid derivatives, process for their preparation and their use 失效
    胍基烷基-1,1-二膦酸衍生物，其制备方法及其应用

    公开(公告)号：US5294608A

    公开(公告)日：1994-03-15

    申请号：US988890

    申请日：1992-12-10

    申请人： Hans-Jochen Lang ,  Christoph Naumann ,  Denis Carniato ,  Anne-Marie Moura ,  Ryoichi Satoh ,  Masakazu Katoh

    发明人： Hans-Jochen Lang ,  Christoph Naumann ,  Denis Carniato ,  Anne-Marie Moura ,  Ryoichi Satoh ,  Masakazu Katoh

    IPC分类号： A61K31/66 ,  A61K31/155 ,  A61K31/663 ,  A61P3/00 ,  A61P19/10 ,  C07F9/38 ,  C07F9/40 ,  C07F9/6506 ,  A61K31/675

    CPC分类号： C07F9/405 ,  C07F9/3873 ,  C07F9/65068

    摘要： The invention describes tautomeric compounds of the formula Ia, Ib or Ic ##STR1## and/or their physiologically tolerable salts, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are a hydrogen atom, substituted (C.sub.1 -C.sub.7)-alkyl, (C.sub.3 -C.sub.10)-cycloalkyl, substituted phenyl or (C.sub.1 -C.sub.4)-alkylphenyl, R.sup.2 is substituted phosphoric acid, R.sup.2 and R.sup.3, R.sup.2 and R.sup.5 or R.sup.4 and R.sup.5 form a monocyclic 5- to 7-membered saturated or unsaturated heterocyclic ring which is mono- or polysubstituted, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a hydrogen atom or (C.sub.1 -C.sub.5)-alkyl, X is a hydrogen atom, hydroxyl or halogen, l and n are an integer from 0 to 7, m is an integer from 0 to 2, and the sum of the numbers l, m and n is less than or equal to 10, a process for the preparation of the compounds of the formula Ia, Ib or Ic, pharmaceuticals and their use for the prophylaxis or treatment of osteoporosis.

    摘要翻译： 本发明描述了式Ia，Ib或Ic（Ia）的互变异构化合物和/或其生理上可耐受的盐，其中R 1，R 2，R 3，R 4，R 5 ，R6和R7是氢原子，取代的（C1-C7） - 烷基，（C3-C10） - 环烷基，取代的苯基或（C1-C4） - 烷基苯基，R2是取代的磷酸，R2和R3，R2和R5 或R 4和R 5形成单或多取代的单环5-至7-元饱和或不饱和杂环，R 8，R 9，R 10和R 11为氢原子或（C 1 -C 5） - 烷基，X为氢原子 ，羟基或卤素，l和n是0至7的整数，m是0至2的整数，数字1，m和n的和小于或等于10，制备 式Ia，Ib或Ic的化合物，药物及其用于预防或治疗骨质疏松症的用途。

    Benzocyclohexanes and analgesic compositions thereof
    7.
    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.