申请人:Schoenmakers Ronald
公开号:US08912329B2
公开(公告)日:2014-12-16
The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C≡CH, C≡N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N═CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
本发明涉及一种药物组合物,包括式(1)中的化合物,其中R1是可选取代的苯基、可选取代的
吡啶基或可选取代的
吲哚基;R2是(
CH2)n,其中n为0、1、2、3或4;R3是( )mR3A,其中m为0、1、2、3或4,R3A是甲基、异丙基、叔丁基、O 、OH、可选取代的苯氧基、C≡CH、C≡N、可选取代的苯基、
呋喃基或
噻吩基;A是含有X1的环,X1的含义为O、S、NH、N(
CH3)或 ;X2是O、S或NH;以及式(2)中的化合物,其中R4是可选取代的苯基、可选取代的
吡啶基、可选取代的
吲哚基、—NR7R8;或—NH—N═CH—R9;且取代基R5到R9的含义在说明书中有所说明,特别是
乙硫异烟胺。该药物组合物可用于治疗多药耐药性结核病等疾病。