SMALL MOLECULE INHIBITORS OF THE PHOSPHORYLATED BCL-2-ASSOCIATED DEATH PROMOTER (BAD) Russian patent published in 2023 - IPC C07D211/06 C07D241/04 C07D213/53 C07D295/96 C07D295/155 C07D295/192 C07D307/52 C07D333/20 C07D413/04 A61K31/445 A61K31/496 A61P35/00 

Abstract RU 2799873 C2

FIELD: pharmaceutical industry.

SUBSTANCE: invention relates to new compounds of general formula (I)

where each R1 is independently OH, NR10R11, with each of R10 and R11 independently selected from C1-6 alkyl; n is 1, 2 or 3; R2a and R2b together with the nitrogen atom to which they are attached form a piperazine substituted with one R6 substituent; each R6 is independently selected from phenyl which may be substituted with 1–2 substituents selected from halo, C1-2 alkyl; R3 is phenyl, naphthyl, 5–6 membered heteroaryl containing 1 heteroatom selected from O, N and S, any of which is optionally substituted with one R7 substituent selected from halo, -O(C1-4 alkyl), -C1-4 haloalkyl or -C(O)NR8R9; each of R8 and R9 is independently selected from H or C3-6 cycloalkyl; or a pharmaceutically acceptable salt thereof.

EFFECT: obtaining new compounds being the inhibitors of Bcl-2-associated death promoter (BAD) phosphorylation that have anti-apoptotic activity and are useful in the treatment of cancer, in particular, breast cancer, endometrial cancer, ovarian cancer, liver cancer, colon cancer, prostate cancer, or pancreatic cancer.

14 cl, 22 dwg, 2 tbl, 9 ex

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RU 2 799 873 C2

Authors

Lobi, Piter Edvard

Pandej, Vidzhej Kumar

Kanchugarakoppal Subbegovda, Rangappa

Salundi, Bassappa

Chakrabkhavi Dkhanandzhaya, Mokhan

Rangappa, Shobit

Venkatachalaiakh, Shrinivasa

Dates

2023-07-13Published

2018-04-18Filed