首页> 外国专利> 15-Acyloxy-prostaglandin analogues - with hypotensive activity without undesired smooth muscle side effects (BE 24.7.78)

15-Acyloxy-prostaglandin analogues - with hypotensive activity without undesired smooth muscle side effects (BE 24.7.78)

机译:15-乙酰氧基-前列腺素类似物-具有降压活性,而无不希望的平滑肌副作用(BE 24.7.78)

摘要

Prostaglandin analogues of formula (I), suitable salts and esters are new. In (I), one of R1 and R2 is H and the other is OH, or R1+R2 is O, R3 is 1-10C alkyl (opt. substd. by 1-5C alkoxy or by aryloxy, furyloxy or benzyloxy which may in turn be substd. by one or more 1-3C alkyl gps.), or 3-7C cycloalkyl, aryl or furyl opt. substd. by one or more 1-3C alkyl gps.; and R is H or is not 10C alkyl. (I) have hypotensive activity which is superior to that of the corresp. non-acylated cpds. Undesired smooth muscle side-effects are not observed. Specific cpds. (I) include 9-keto-15alpha-acetoxy-16,16-dimethyl-18-oxa-prost-4,13-dienoic acid. In an example, this was prepd. by acylating the corresp. 15alpha-hydroxy cpd. with acetic anhydride in the presence of pyridine.
机译:式(I)的前列腺素类似物,合适的盐和酯是新的。在(I)中,R 1和R 2之一为H,另一个为OH,或R 1 + R 2为O,R 3为1-10C烷基(优选1-5C烷氧基或芳氧基,呋喃氧基或苄氧基)依次由一个或多个1-3C烷基gps。或3-7C环烷基,芳基或呋喃基取代。取代一个或多个1-3C烷基gps。并且R是H或不是> 10 C烷基。 (I)的降压活性优于相应的降压活性。非酰化的cpds。没有观察到不希望的平滑肌副作用。特定的cpds。 (I)包括9-酮基15α-乙酰氧基-16,16-二甲基-18-氧杂-prost-4,13-二烯酸。在一个示例中,这是准备好的。通过酰化对应物15α-羟基cpd。在吡啶存在下用乙酸酐洗涤。

著录项

  • 公开/公告号FR2378009A2

    专利类型

  • 公开/公告日1978-08-18

    原文格式PDF

  • 申请/专利权人 HOECHST AG;

    申请/专利号FR19780001790

  • 发明设计人

    申请日1978-01-23

  • 分类号C07C177/00;A61K31/19;

  • 国家 FR

  • 入库时间 2022-08-22 21:42:47

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