发明名称 Thiophene carboxamide deriv. prepn.
摘要 Derivs. are of formula (I), in which R1 is CHO, CH2OH, CH2O-1-4C alkyl, CO-1-3C alkyl, CH(OH)-1-3C alkyl, or COOH; R2 is 1-4C alkyl, CHO, CH2OH, CH2O-1-4C alkyl, CO-1-3C alkyl, CH(OH)-1-3C alkyl, or COOH; R3 is 1-4C alkyl and X is pyrrolidinyl or pyrrolidinyl-methyl. They act on the central nervous system, blocking post-synaptic dopamine receptors in treatment of vomiting, depression, anxiety and certain psychotic conditions, and are made by (a) oxidn. of a cpd. (I) in which R1 or R2 is 1-4C alkyl or CHO; or (b) redn. of a cpd. (I) in which R1 or R2 is CHO or CO-1-3C alkyl, or (c) alkylation of a cpd. (I) in which R1 and/or R2 is CH2OH; or (d) reaction of a cpd. (II) in which Z is halogen, OH or OR and R is an active gp. with an amine of formula X-NH2.
申请公布号 ES2008630(A6) 申请公布日期 1989.07.16
申请号 ES19880003044 申请日期 1988.10.06
申请人 LLLY S.A.;LILLY INDISTRIES LIMITED 发明人 FERNANDEZ FERNANDEZ M. ISABEL;HOTTEN TERRENCE M.;TUPPER DAVID EDWARD
分类号 A61K31/40;C07D409/12;(IPC1-7):C07D409/12 主分类号 A61K31/40
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