摘要:
A sleep inducing agent comprising, as an active component, a prostaglandin derivative represented by formula (1), wherein X represents a halogen atom, Y represents a group represented by (CH2)m, a cis-vinylene group or a phenylene group, Z represents an ethylene group, a trans-vinylene group, OCH2 or S(O)nCH2, R is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with a C1-4 alkyl group, a C4-13 cycloalkylalkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, an C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R represents a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl, m is an integer of 1 to 3, and n is 0, 1 or 2, or a pharmaceutically acceptable salt or hydrate thereof.
摘要:
A sleep-inducing preparation which comprises as an effective ingredient a prostaglandin derivative represented by the formula: wherein X is a halogen atom, Y is a group represented by (CH 2 ) m , a cis-vinylene group or a phenylene group, Z is an ethylene group, a trans-vinylene group, OCH 2 or S(O) n CH 2 , R 1 is a C 3-10 cycloalkyl group, a C 3-10 cycloalkyl group substituted with C 1-4 alkyl group(s), a C 4-13 cycloalkylalkyl group, a C 5-10 alkyl group, a C 5-10 alkenyl group, a C 5-10 alkynyl group or a bridged cyclic hydrocarbon group, R 2 is a hydrogen atom, a C 1-10 alkyl group or a C 3-10 cycloalkyl group, m is an integer of 1 to 3, and n is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.
摘要:
Prostaglandin derivative represented by Formula (I): wherein R 1 is a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or a cycloalkyl group having 3 to 10 carbon atoms, and R 2 is a cycloalkyl group having 3 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms substituted by a methyl group, an alkyl group having 1 to 3 carbon atoms substituted by a cycloalkyl group having 3 to 10 carbon atoms, a branched alkyl group having 5 to 10 carbon atoms or a branched alkenyl group having 5 to 10 carbon atoms, X is a halogen atom substituted at the α- or β-configuration, and A is an ethylene group, a vinylene group or an ethynylene group, salts thereof, and a pharmaceutical composition for lowering intraocular pressure containing them as an effective ingredient. These compounds are useful as lowering agents of intraocular pressure with no or remarkably reduced side-effects such as transient ocular hypertension and the like.
摘要:
To produce a prostaglandin E in a short time and in a high yield while minimizing the formation of isomers. A process for producing a prostaglandin E represented by general formula (I) wherein A represents an arbitrary group not participating in the reaction; B represents vinylene or ethynylene; R⁴ and R⁵ may be the same or different from each other and each represents hydrogen or a protective group for a hydroxyl group; and R⁶ and R⁷ represent each an arbitrary group not participating in the reaction, which comprises reacting an allyl ester of a prostaglandin E represented by general formula (II) wherein R¹ and R² may be the same or different from each other and each represents hydrogen or lower alkyl; R³ represents hydrogen, lower alkyl, alkenyl or aryl; and R⁴, R⁵, R⁶, R⁷, A and B are each as defined above, with one or two compounds selected from the group consisting of bases and formic acid in the presence of a complex compound or a complex salt of 0-valent or divalent palladium atom.
摘要翻译:在短时间内以高产率产生前列腺素E,同时最小化异构体的形成。 一种制备由通式(I)表示的前列腺素E的方法,其中A表示不参与反应的任意基团; B代表亚乙烯基或亚乙炔基; R 4和R 5可以彼此相同或不同,并且各自表示氢或羟基的保护基; R 6和R 7各自表示不参与反应的任意基团,其包括使通式(II)表示的前列腺素E的烯丙酯与其中R 1和R 2可以是 相同或不同,各自表示氢或低级烷基; R 3表示氢,低级烷基,烯基或芳基; 和R 4,R 5,R 6,R 7,A和B各自如上所定义,在一个或多个存在下存在下,一种或两种选自碱和甲酸的化合物 络合物或0价或二价钯原子的络盐。