COMPOUNDS AND METHODS FOR USING Russian patent published in 2015 - IPC C07D417/14 C07D487/04 A61K31/538 A61K31/4709 A61P7/02 A61P35/00 

Abstract RU 2561109 C2

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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RU 2 561 109 C2

Authors

Baehll Dzhonatan Bajldon

Buj Chinkh Tkhien

Kolmen Piter

Dadli Danett A.

Fehjrbrazer Uehjn Dzh.

Flajgehr Dzhon A.

Lessin Gijom Loran

Ndubaku Chudi

Nikolakopulos Dzhordzh

Raj Karl Stiven

Slibs Brehd Ehdmund

Smit Brajan Dzhon

Uotson Kejt Dzheffri

Ehlmor Stiven V.

Petros Ehndrju M.

Sauehrs Ehndrju Dzh.

Kzabotar Piter

Dates

2015-08-20Published

2009-12-17Filed