| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound or its pharmaceutically acceptable salt; the compound is a) described by Formulawherein Ris absent; the index n means an integer from 0 to 2; when n = 0, then Xmeans -CH-; Xmeans a member specified in a group consisting of -CH-, -O-, -N(H)- and -N(R)-, wherein Ris specified in a group consisting of Calkyl; each X, Xand Xis independently specified in a group consisting of C(H); A means a member specified in a groupand(aa), wherein Ris independently specified in a group consisting of halogen and -R, wherein Ris specified in a group consisting of Calkyl; B means a member specified in a group of compoundsand(aaa), wherein Ris absent; L is absent or means a member specified in a group consisting of Carylene-Cheteroalkylene, Cheteroalkylene, Calkylene, Calkenylene, Calkynylene and -O-; heteroalkylene contains 1 or 2 heteroatoms specified in a group consisting of N, O or S; E means hydrogen or halogen; or alternatively, E is specified in a group consisting of phenyl, Cheteroaryl; Cheteroaryl is specified in a group consisting of pyrazol, pyridine and pyrazine, Cheterocycloalkyl; Cheterocycloalkyl is specified in a group consisting of morpholine, pyrrolidine, piperidine and piperazine, and Ccycloalkyl, and if so required 1 ring independently specified in a group consisting of a 5-merous heterocyclic ring containing 2 O heteroatoms, a benzene ring and a 5,6-merous heteroaromatic ring containing 2 N heteroatoms can be condensed with E; E and 1 ring condensed with E if so required are independently protected 0 to 5 times by substitutes Rspecified in a group consisting of halogen, -NRR, -OR, -C(O)OR, -NRC(O)OR, -S(O)R, -R, -R, =O, -Z-NRRand -ZR; Zmeans Calkylene; each Rand Rq are independently specified in hydrogen and Calkyl; Ris specified in a group consisting of Calkyl and phenyl; Ris specified in a group consisting of phenyl and pyrazole, and 1 pyrimidine ring can be condensed with R. Or the compound b) is specified in a group consisting of 2-(1-(benzo[d]thiazol-2-ylcarbamoyl)-1,2,3,4-tetrahydroquinolin-7-yl)-5-(4-methoxyphenyl)-N,N-dimethylthiazol-4-carboxamide, 2-(1-(benzo[d]thiazol-2-ylcarbamoyl)-1,2,3,4-tetrahydroquinolin-7-yl)-5-(4-fluorophenoxy)thiazol-4-carboxamide and N-(benzo[d]thiazol-2-yl)-6-(6-(methylsulphonylcarbamoyl)-5-(3-phenoxypropoxy)pyridin-2-yl)-2H-benzo[b][1,4]oxazine-4(3H)-carboxamide. The invention also refers to specific compounds. The compounds according to the inventions are applicable for a pharmaceutical composition having BCl-Xantiapoptosis protein inhibitory activity. The pharmaceutical composition contains a therapeutically effective amount of the composition of formula a) or b), or its pharmaceutically acceptable salt, and at least one pharmaceutically acceptable diluent, carrier or excipient.EFFECT: new compounds inhibiting BCl-Xantiapoptosis protein.21 cl, 2 tbl, 7 dwg, 66 ex |
