发明名称 Prodrug derivatives of thyrotropin-releasing hormone (TRH)
摘要 PCT No. PCT/DK90/00228 Sec. 371 Date Mar. 20, 1992 Sec. 102(e) Date Mar. 20, 1992 PCT Filed Sep. 3, 1990 PCT Pub. No. WO91/03487 PCT Pub. Date Mar. 21, 1991.Compounds of formula (I), wherein R1 is selected from the group consisting of an alkyl group, an aralkyl group, an alkenyl group, a cycloalkyl group, in which the alkyl, aralkyl, alkenyl or cycloalkyl group is unsubstituted or substituted with one or more substituents selected from the group consisting of a halogen atom, e.g. Cl or Br, a hydroxyl group or a straight or branched-chain alkoxy group containing from 1 to 6 carbon atoms; and the pharmaceutically acceptable acid addition salts thereof. Such compounds are prodrugs of TRH and are characterized by having a higher lipophilicity than TRH and possessing a high resistance toward degradation by TRH-inactivating enzymes. Such compounds will after administration be converted into TRH.
申请公布号 US5405834(A) 申请公布日期 1995.04.11
申请号 US19920842181 申请日期 1992.03.20
申请人 BUNDGAARD, HANS;MOSS, JUDI 发明人 BUNDGAARD, HANS;MOSS, JUDI
分类号 A61K38/22;A61K38/00;A61K38/04;A61P5/00;A61P5/12;C07K1/113;C07K5/08;C07K5/097;(IPC1-7):C07K7/04;A61K37/24;A61K37/43 主分类号 A61K38/22
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