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    • 7. 发明申请
    • 9-HALOGEN-'DELTA'2-PROSTAGLANDINE DERIVATIVES, PREPARATION PROCESS AND UTILIZATION THEREOF AS DRUGS
    • 9-恶嗪-2β-丙氨酸衍生物,其制备方法和作为药物的利用
    • WO1985002841A1
    • 1985-07-04
    • PCT/DE1984000280
    • 1984-12-21
    • SCHERING AKTIENGESELLSCHAFTSKUBALLA, WernerRADÜCHEL, BerndVORBÜGGEN, HelmutELGER, WalterLOGE, Olaf
    • SCHERING AKTIENGESELLSCHAFT
    • C07C177/00
    • C07C405/0041C07C405/00
    • 9-halogen- DELTA -prostaglandine derivatives having the general formula (I), wherein Hal may be a fluorine or chlorine atom in alpha or beta position; R1 may be the rest OR2, R2 being a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic rest, or the rest NHR3, R3 being an acid rest or the rest R2; A may represent a group -CH2-CH2- or cis-CH=CH-; B may represent -CH2-CH2-, trans-CH=CH- or -C=C-; W may represent a free or functionally modified hydroxymethylene or group, the respective OH groups being in position alpha or beta ; D and E may represent together a direct bound or D may represent a straight or branched chain alkylene group with 1 to 10 atoms of carbon, which may optionally be substituted by fluorine atoms; E may represent an oxygen atom or sulphur, a direct bound, -C=C- bound or a group -CR6=CR7, R6 representing an hydrogen atom or an alkyl group and R7 representing an oxygen atom, an alkyl group or a halogen atom; R4 is a free or functionally modified hydroxy group; R5 represents an oxygen atom, an alkyl group, an halogen substituted alkyl, cycloalkyl, aryl optionally substituted or a heterocyclic group and, if R2 is a hydrogen atom, the salts thereof with physiologically acceptable bases.
    • 具有通式(I)的9-卤素-Δta-前列环素衍生物,其中Hal可以是α或β位的氟或氯原子; R 1可以是其余的OR 2,R 2是氢原子,烷基,环烷基,芳基或杂环基,或其余的NHR 3,R 3是酸基或其余的R 2; A可以表示基团-CH 2 -CH 2 - 或顺式-CH = CH-; B可以表示-CH 2 -CH 2 - ,反式-CH = CH-或-C = C-; W可以代表游离或官能改性的羟基亚甲基或基团,各个OH基团位于α或β位置; D和E可以一起代表直接键合,或者D可以表示具有1-10个碳原子的直链或支链亚烷基,该烷基可以任选被氟原子取代; E可以表示氧原子或硫,直接键合-C = C-结合或基团-CR 6 = CR 7,R 6表示氢原子或烷基,R 7表示氧原子,烷基或卤素原子 ; R4是游离或官能改性的羟基; R5表示氧原子,烷基,卤素取代的烷基,环烷基,任选取代的芳基或杂环基,如果R2是氢原子,则其与生理上可接受的碱的盐。