5,6;8,9-Tetrahydro-7H-dibenz(d,f)azonines
    15.
    发明授权
    5,6;8,9-Tetrahydro-7H-dibenz(d,f)azonines 失效
    5,6; 8,9-四氢-7H-二苯并(d,f)吖嗪

    公开(公告)号:US4415495A

    公开(公告)日:1983-11-15

    申请号:US238501

    申请日:1981-02-24

    CPC分类号: C07D225/08

    摘要: The present invention provides 5,6;8,9-tetrahydro-7H-dibenz(d,f)azonine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are hydrogen or halogen atoms or lower alkyl or alkoxy radicals, R.sup.3 is a hydrogen atom or a lower alkyl radical, R.sup.4 is a hydrogen atom or a lower alkyl or alkanoyl radical and n is 1 or 2; and the pharmaceutically acceptable salts thereof formed with inorganic and organic acids; but excluding 6-benzyl-2,12-dimethoxy-1-hydroxy-7-methyl-5,6;8,9-tetrahydro-7H-dibenz(d,f)azonine in which case R.sup.1, R.sup.2 and R.sup.4 are hydrogen, n is 1 and R.sup.3 is methyl. The lower alkyl, alkanoyl and alkoxy radicals are straight chained or branched radicals containing 1 to 5 carbon atoms.The present invention also provides a process for the preparation of these compounds, as well as pharmaceutical compositions containing them.

    摘要翻译: 本发明提供下式的5,6,8,9-四氢-7H-二苯并(d,f)吖嗪衍生物:其中R 1和R 2相同或不同,为氢或卤原子或更低级 烷基或烷氧基,R3是氢原子或低级烷基,R4是氢原子或低级烷基或烷酰基,n是1或2; 和其与无机酸和有机酸形成的药学上可接受的盐; 但不包括6-苄基-2,12-二甲氧基-1-羟基-7-甲基-5,6; 8,9-四氢-7H-二苯并吖嗪(d,f)吖嗪,其中R1,R2和R4是氢 ,n为1,R 3为甲基。 低级烷基,烷酰基和烷氧基是含有1至5个碳原子的直链或支链基团。 本发明还提供了制备这些化合物的方法以及含有它们的药物组合物。

    Process for the preparation of
4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2)
    18.
    发明授权
    Process for the preparation of 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) 失效
    制备4-氨基-1-苯基-c-乙氧基羰基 - 环己烯的方法(2)

    公开(公告)号:US4008233A

    公开(公告)日:1977-02-15

    申请号:US528107

    申请日:1974-11-29

    摘要: This invention relates to 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are hydrogen or alkyl having 1 to 4 carbon atoms, or one of the two groups is allyl, phenalkyl having 7 to 9 carbon atoms or .alpha.-methyl-.beta.-hydroxyethyl; or R.sub.1 and R.sub.2 together form a morpholino group, piperazino group substituted at the 4- position by methyl, benzyl, phenyl, 3-chlorophenyl, 4-chlorophenyl, 2-phenethyl or benzoyl, or a piperidino group substituted at the 4- position by hydroxyl, phenyl, 2-methoxyphenyl, 4-methoxyphenyl, methyl or benzyl and medically acceptable addition compounds derived from inorganic and organic acids or lower alkyl halides. The compounds of the present invention are prepared by separation of 4-amino-1-phenyl-1-ethoxycarbonyl-cyclohexenes-(2), described in U.S. Patent Application Ser. No. 226,509, filed Feb. 15, 1972, into the two possible geometrical isomers. The instant compounds, the 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) of formula I, exhibit marked analgesic and neuroleptic activities and are useful for the alleviation and reduction of pain.

    摘要翻译: 本发明涉及式I的4r-氨基-1t-苯基-c-乙氧基羰基 - 环己烯 - (2):其中R 1和R 2相同或不同,为氢或具有1至4个碳原子的烷基, 或两个基团中的一个为烯丙基,具有7至9个碳原子的苯基烷基或α-甲基-β-羟乙基; 或R 1和R 2一起形成吗啉代基,在4-位上被甲基,苄基,苯基,3-氯苯基,4-氯苯基,2-苯乙基或苯甲酰基取代的哌嗪基或在4-位取代的哌啶子基, 羟基,苯基,2-甲氧基苯基,4-甲氧基苯基,甲基或苄基,以及衍生自无机和有机酸或低级烷基卤的医药上可接受的加成化合物。 本发明的化合物是通过分离美国专利申请序列号中描述的4-氨基-1-苯基-1-乙氧基羰基 - 环己烯 - (2)制备的。 1972年2月15日提交的226,509号的两种可能的几何异构体。 本发明化合物,式I的4r-氨基-1t-苯基1c-乙氧基羰基 - 环己烯 - (2)表现出明显的镇痛和精神安定活性,并且可用于缓解和减轻疼痛。

    Method for treating cardiovascular circulatory insufficiencies and
hypotonia with 2-hydroxyphenyl-1-oxa-4-azaspiroalkane derivatives
    19.
    发明授权
    Method for treating cardiovascular circulatory insufficiencies and hypotonia with 2-hydroxyphenyl-1-oxa-4-azaspiroalkane derivatives 失效
    用2-羟基苯基-1-氧杂-4-氮杂螺环烷衍生物治疗心血管循环功能不全和低血压的方法

    公开(公告)号:US3989836A

    公开(公告)日:1976-11-02

    申请号:US557134

    申请日:1975-03-10

    IPC分类号: C07D263/52 A61K31/42

    CPC分类号: C07D263/52

    摘要: Novel 2-hydroxy-phenyl-1-oxa-4-azaspiroalkane derivatives, the preparation thereof, and pharmaceutical compositions containing these 2-hydroxyphenyl-1-oxa-4-azaspiroalkane derivatives are disclosed. These derivatives possess unexpectedly valuable thereapeutic properties which make them outstandingly useful for the treatment of cardiovascular circulatory insufficiencies and hypotonic states.

    摘要翻译: 公开了新的2-羟基 - 苯基-1-氧杂-4-氮杂螺环烷衍生物,其制备方法和含有这些2-羟基苯基-1-氧杂-4-氮杂螺环烷衍生物的药物组合物。 这些衍生物具有出人意料的有价值的治疗性质,使其在治疗心血管循环功能不全和低渗状态方面非常有用。