FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a compound or its pharmaceutically acceptable salt; the compound is a) described by Formula wherein R1 is absent; the index n means an integer from 0 to 2; when n = 0, then X1 means -CH2-; X1 means a member specified in a group consisting of -CH2-, -O-, -N(H)- and -N(Ra)-, wherein Ra is specified in a group consisting of C1-6alkyl; each X2a, X2b and X2c is independently specified in a group consisting of C(H); A means a member specified in a group and (aa), wherein R3 is independently specified in a group consisting of halogen and -Rg, wherein Rg is specified in a group consisting of C1-4alkyl; B means a member specified in a group of compounds and (aaa), wherein R4a is absent; L is absent or means a member specified in a group consisting of C6arylene-C1-6heteroalkylene, C1-6heteroalkylene, C1-6alkylene, C2-6alkenylene, C2-6alkynylene 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, C5-6heteroaryl; C5-6heteroaryl is specified in a group consisting of pyrazol, pyridine and pyrazine, C3-7heterocycloalkyl; C3-7heterocycloalkyl is specified in a group consisting of morpholine, pyrrolidine, piperidine and piperazine, and C3-7cycloalkyl, 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 R6 specified in a group consisting of halogen, -NRpRq, -ORp, -C(O)ORp, -NRpC(O)ORr, -S(O)2Rr, -Rr, -Rs, =O, -Z1-NRpRq and -Z1-Rs; Z1 means C1-6alkylene; each Rp and Rq are independently specified in hydrogen and C1-6alkyl; Rr is specified in a group consisting of C1-6alkyl and phenyl; Rs is specified in a group consisting of phenyl and pyrazole, and 1 pyrimidine ring can be condensed with Rs. 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-XL antiapoptosis 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-XL antiapoptosis protein.
21 cl, 2 tbl, 7 dwg, 66 ex
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Authors
Dates
2015-08-20—Published
2009-12-17—Filed