[EN] 3 -AMINO- PYRAZOLE DERIVATIVES USEFUL AGAINST TUBERCULOSIS<br/>[FR] DÉRIVÉS DE 3-AMINO-PYRAZOLE UTILES CONTRE LA TUBERCULOSE
申请人:GLAXO GROUP LTD
公开号:WO2012049161A1
公开(公告)日:2012-04-19
A compound of Formula (I) or a pharmaceutically acceptable salt thereof: (I), Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, -CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
化合物的化学式(I)或其药学上可接受的盐:(I),其中:Het是一个5到10个成员的杂芳环;X是N且Y是CR5;或X是C且Y是S;Z从N和CH中选择;R1从H和C1-2烷基中选择;R2从H,C1-2烷基,OH,-CH2OH和C1-2烷氧基中选择;每个R3独立地从OH,C1-3烷基,F,Cl,Br,NH2和C1-3烷氧基中选择;R4从C1-3烷基和卤代C1-3烷基中选择;R5从H,C1-3烷基和卤代C1-3烷基中选择;R6和R7要么i)各自独立地从H,C1-3烷基和C1-3烷氧基中选择;要么ii)R6和R7与它们附着的环一起形成一个9个成员的双环环;p为0-3;RA从H和C1-3烷基中选择,提供了含有它们的组合物,它们在治疗中的用途,例如在结核病治疗中的用途,以及这类化合物的制备方法。