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    • 6. 发明申请
    • 7-[CARBOXYALKYL OR ALKENYL]-6-[ALKYL OR ALKENYL] 3-OXO-2,4-DIOXOBICYCLO-[3.2.1] OCTANE AND DERIVATIVES THEREOF
    • 7- [羧甲基或烷基] -6- [烷基或亚苄基] 3-氧代-2,4-二氧代环己基 - [3.2.1]其衍生物及其衍生物
    • WO1995018103A1
    • 1995-07-06
    • PCT/US1994014012
    • 1994-12-05
    • ALLERGAN, INC.
    • ALLERGAN, INC.BURK, Robert, M.KRAUSS, Achim, H.WOODWARD, David, F.
    • C07C405/00
    • C07D307/00C07D319/08C07D493/08
    • The present invention relates to 7-[carboxyalkyl or alkenyl]-6-[alkyl or alkenyl]-3-oxo-2,4-dioxobicyclo[3.2.1] octanes and derivatives thereof. In particular, hydroxyl, nitro, amino, amido, azido, oxime, thiol, ether and thiol ether derivatives of said carboxy group are contemplated. In particular, 7-[6-carboxy-2-hexenyl]-6-[3-hydroxy-1-octenyl] of 3-oxo-2,4-dioxobicyclo-[3.2.1] octane and derivatives thereof are disclosed. These compounds are useful as ocular hypotensives and as (a) thromboxane mimetics for the prevention of hemorrhaging as follows: during surgery; tooth extraction; hemorrhaging associated with gastro-intestinal diseases and conditions such as hemorrhoids, inflammatory bowel diseases and gastric and peptic ulcers; as a result of stroke; as a complication in retinal diseases resulting in impaired vision and associated with menstruation, childbirth and uterine dysfunction and (b) selective vasoconstrictors for treating systemic hypotension, e.g. in restoring normal blood pressure in hemorrhagic, anaphylactic, or septic shock victims; to provide local anti-inflammatory effects in the eye, skin and nose; to limit plasma exudation in burns, etc. and optimizing blood-born delivery of drugs and diagnostics in encapsulating vehicles.
    • 本发明涉及7- [羧基烷基或烯基] -6- [烷基或链烯基] -3-氧代-2,4-二氧代双环[3.2.1]辛烷及其衍生物。 特别地,考虑到所述羧基的羟基,硝基,氨基,酰胺基,叠氮基,肟,硫醇,醚和硫醇醚衍生物。 特别地,公开了3-氧代-2,4-二氧双环[3.2.1]辛烷及其衍生物的7- [6-羧基-2-己烯基] -6- [3-羟基-1-辛烯基]。 这些化合物可用作眼睛低血压剂和(a)用于预防出血的凝血恶烷模拟物如下:手术期间; 拔牙; 与胃肠道疾病和痔疮,炎性肠病和胃和消化性溃疡等疾病相关的出血; 作为中风的结果; 视网膜疾病并发症,导致视力受损,并伴有月经,分娩和子宫功能障碍,以及(b)用于治疗全身性低血压的选择性血管收缩剂,例如, 恢复出血性,过敏性或败血性休克患者的正常血压; 在眼睛,皮肤和鼻子中提供局部消炎作用; 限制血浆渗透等等,并优化血液输送药物和封装车辆中的诊断。