2,4-Disubstituted-5-oxo-5H-dibenzo[a,d]cycloheptenes
    9.
    发明授权
    2,4-Disubstituted-5-oxo-5H-dibenzo[a,d]cycloheptenes 失效
    2,4-二取代-5-氧代-5H-二苯并{8α,d {9环庚烯

    公开(公告)号:US4172949A

    公开(公告)日:1979-10-30

    申请号:US920047

    申请日:1978-06-28

    摘要: Compounds of the formula ##STR1## wherein R is hydrogen or methyl; R.sup.1 is hydrogen, C.sub.1 to C.sub.8 linear or branched alkyl or C.sub.1 to C.sub.8 linear or branched alkanoyl; X is oxygen or sulfur; R.sup.2 is selected from the group hydrogen, C.sub.1 to C.sub.18 linear or branched alkyl and the radicals --(CH.sub.2).sub.n --NR.sup.3 R.sup.4, --CH.sub.2 --CH(OH)--CH.sub.2 --OH or a ketal thereof formed from the aldehyde or ketone R.sup.5 R.sup.6 CO, wherein R.sup.3 and R.sup.4 are each independently C.sub.1 to C.sub.6 linear or branched alkyl or R.sup.3 and R.sup.4 taken together with the nitrogen atom of the first radical are attached to form a 5- or 6-membered heterocyclic ring, R.sup.5 and R.sup.6 are each independently hydrogen, C.sub.1 to C.sub.6 linear or branched alkyl, phenyl or benzyl or R.sup.5 and R.sup.6 taken together represent an alkylene bridge of from 4 to 6 carbon atoms; n is an integer of from 2 to 4; and the dotted line represents an optional double bond; and the pharmaceutically acceptable salts thereof. The compounds have anti-inflammatory, analgesic and anti-pyretic activities and, accordingly, are useful in the treatment of inflammation, pain and/or pyrexia.

    摘要翻译: 式(I)的化合物,其中R是氢或甲基; R1是氢,C1至C8直链或支链烷基或C1至C8直链或支链烷酰基; X是氧或硫; R2选自氢,C1至C18直链或支链烷基和由醛或酮R5R6CO形成的基团 - (CH2)n-NR3R4,-CH2-CH(OH)-CH2-OH或其缩酮,其中 R 3和R 4各自独立地为C 1至C 6直链或支链烷基或与第一基团的氮原子一起的R 3和R 4连接以形成5-或6-元杂环,R 5和R 6各自独立地为氢,C 1 C 6直链或支链烷基,苯基或苄基或R 5和R 6一起表示4至6个碳原子的亚烷基桥; n为2〜4的整数, 虚线表示任选的双键; 及其药学上可接受的盐。 这些化合物具有抗炎,止痛和抗热解活性,因此可用于治疗炎症,疼痛和/或发热。

    Esters of 2-substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes having
pharmaceutical activity, and methods and compositions for the use
thereof
    10.
    发明授权
    Esters of 2-substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes having pharmaceutical activity, and methods and compositions for the use thereof 失效
    具有药物活性的2-取代-5-氧代-5H-二苯并[8α,d {9环庚烯的酯,及其用途的方法和组合物

    公开(公告)号:US4112114A

    公开(公告)日:1978-09-05

    申请号:US830264

    申请日:1977-09-02

    摘要: Esters of 2-substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where R' is --CH.sub.2 --CH.dbd.CH.sub.2, --CH.sub.2 --CH(OH)--CH.sub.2 OH, ##STR2## where Y is either O or S, or ##STR3## where R.sup.4 and R.sup.5 are independently hydrogen, alkyl having 1 to 6 carbon atoms, phenyl, or benzyl, or together R.sup.4 and R.sup.5 form an alkylene bridge having 4, 5 or 6 carbon atoms; one of R.sup.2 and R.sup.3 is hydrogen and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and/or pyrexia.

    摘要翻译: 由下式表示的2-取代-5-氧代-5H-二苯并[a,d]环庚烯的酯:其中R'是-CH 2 -CH = CH 2,-CH 2 -CH(OH)-CH 2 OH, 其中Y是O或S,或者其中R4和R5独立地是氢,具有1-6个碳原子的烷基,苯基或苄基,或者一起R4和R5形成具有4,5或6个亚烷基的桥 碳原子 R2和R3中的一个是氢,另一个是氢,甲基或乙基,或者一起R2和R3是亚甲基。 该化合物具有抗炎,镇痛和解热活性,因此可用于治疗炎症,疼痛和/或发热。