申请人:Schoenmakers Ronald
公开号:US20120101080A1
公开(公告)日:2012-04-26
The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R
1
is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R
2
is (CH
2
)
n
wherein n is 0, 1, 2, 3 or 4; R
3
is (CH
2
)
m
R
3A
wherein m is 0, 1, 2, 3 or 4, and R
3A
is methyl, isopropyl, tert-butyl, OCH
3
, OH, optionally substituted phenoxy, C≡CH, C≡N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X
1
with the meaning O, S, NH, N(CH
3
) or CH
2
; and X
2
is O, S or NH; and a compound of formula (2) wherein R
4
is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR
7
R
8
; or —NH—N═CH—R
9
; and substituents R
5
to R
9
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,其中包含式(1)的化合物,其中R1是可选取代苯基,可选取代吡啶基或可选取代吲哚基;R2是(CH2)n,其中n为0、1、2、3或4;R3是(CH2)mR3A,其中m为0、1、2、3或4,R3A是甲基、异丙基、叔丁基、OCH3、OH、可选取代苯氧基、C≡CH、C≡N、可选取代苯基、呋喃基或噻吩基;A是一个含有X1环,X1的含义是O、S、NH、N(CH3)或CH2;X2是O、S或NH;以及式(2)的化合物,其中R4是可选取代苯基,可选取代吡啶基,可选取代吲哚基,—NR7R8;或—NH—N═CH—R9;和取代基R5至R9在说明书中有所示,特别是乙硫异烟胺。该药物组合物在治疗多药耐药结核病方面具有用途。