8-Aza-9-dioxothiaprostanoic acids
    5.
    发明授权
    8-Aza-9-dioxothiaprostanoic acids 失效
    8-氮杂-9-二氧代硫代雄磷酸

    公开(公告)号:US4087435A

    公开(公告)日:1978-05-02

    申请号:US769477

    申请日:1977-02-17

    IPC分类号: C07D275/02

    摘要: Novel 8-aza-9-dioxothiaprostanoic acid compounds, their salts, and derivatives, are prepared from ethyl 7-(3-hydroxymethyl-2-isothiazolidinyl)-5-heptynoate S,S-dioxide by first hydrogenating the triple bond over a Lindlar catalyst, followed by mild oxidation, to produce the corresponding 3-formyl compound, which is condensed with the ylide prepared from dimethyl-(2-oxoheptyl)phosphonate to produce the .alpha.,.beta.-unsaturated ketone, followed by reduction to the corresponding carbinol, and ester hydrolysis. The compounds are useful especially for the treatment of patients with poorly functioning kidneys, as hypotensives, or as platelet aggregation inhibitors.

    摘要翻译: 通过首先在Lindlar上氢化三重键,从7-(3-羟甲基-2-异噻唑烷基)-5-庚炔酸S,S-二氧化物乙酸酯制备新的8-氮杂-9-二氧代硫代雄甾烷酸化合物,其盐和衍生物 催化剂,然后轻度氧化,产生相应的3-甲酰基化合物,其与由二甲基 - (2-氧代庚基)膦酸酯制备的内鎓盐缩合以产生α,β-不饱和酮,随后还原成相应的甲醇, 和酯水解。 该化合物特别适用于治疗肾功能不全的患者,作为低血糖剂或血小板聚集抑制剂。

    11,12-Seco-prostaglandins
    7.
    发明授权
    11,12-Seco-prostaglandins 失效
    前列腺素11,12-半胱氨酸

    公开(公告)号:US4055596A

    公开(公告)日:1977-10-25

    申请号:US704859

    申请日:1976-07-14

    IPC分类号: C07C143/822

    摘要: The invention is concerned with novel 16-aryloxy-, 16-alkoxy-, 16-arylthio- and 16-alkylthio-8-aza-9-dioxothia-11,12-seco-prostaglandins and processes for their preparation. These novel compounds are useful as pharmaceuticals since they can be used in animals for estrus synchronization and treatment of infertility due to persistence of luteal function.

    摘要翻译: 本发明涉及新的16-芳氧基 - ,16-烷氧基 - ,16-芳硫基 - 和16-烷硫基-8-氮杂-9-二氧硫杂十一烷-1,11-前 - 前列腺素及其制备方法。 这些新型化合物可用作药物,因为它们可用于动物用于发情同步和由于黄体功能的持续性导致的不孕症的治疗。

    ((5,6-dichloro-3-oxo-9,9a-d
isubstituted-2,3,9,9a-tetrahydrofluoren-7-yl)oxy)alkanoic acids and
alkanimidamides
    8.
    发明授权
    ((5,6-dichloro-3-oxo-9,9a-d isubstituted-2,3,9,9a-tetrahydrofluoren-7-yl)oxy)alkanoic acids and alkanimidamides 失效
    ((5,6-二氯-3-氧代-9,9a-二取代-2,3,9,9a-四氢芴-7-基)氧基)链烷酸和烷酰胺

    公开(公告)号:US4797391A

    公开(公告)日:1989-01-10

    申请号:US150462

    申请日:1988-02-08

    摘要: The invention relates to novel [(5,6-dichloro-3-oxo-9,9a-disubstituted-2,3,9,9a-tetrahydro-fluoren-7-yl)oxy]alkanoic acids and alkanimidamides, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.

    摘要翻译: 本发明涉及新的[(5,6-二氯-3-氧代-9,9a-二取代-2,3,9,9a-四氢 - 芴-7-基)氧]链烷酸和烷酰胺,其衍生物及其衍生物 盐。 该化合物可用于治疗和预防脑部损伤以及头部创伤,中风(特别是缺血性),呼吸暂停,心跳骤停,雷叶综合征,脑血栓形成,脑栓塞,脑出血,脑肿瘤,脑脊髓炎 ,脊髓损伤,脑积水,术后脑损伤创伤,脑部感染引起的水肿,各种脑震荡和颅内压升高。