ANTIPROLIFERATIVE AGENTS FOR THE TREATMENT OF PAH Russian patent published in 2022 - IPC C07D471/04 C07D487/04 A61K31/4375 A61K31/519 A61P35/00 A61P9/12 

Abstract RU 2786588 C1

FIELD: organic chemistry.

SUBSTANCE: invention relates to organic chemistry, namely to a compound of formula I or a pharmaceutically acceptable salt thereof, where A represents CH or N; R1 is C1-C2 alkyl; R2 is C1-C4 alkyl; R3 is a 5-7 membered heterocyclyl containing 1 heteroatom selected from nitrogen or oxygen, C3-C8 cycloalkyl, where each of the 5-7 membered heterocyclyl is optionally substituted with 1 R5, where each of the C3-C8 cycloalkyl is optionally substituted with 1 R5 and further optionally substituted with 1 -N(R6)2; R4 is a fragment having the structure

each R5 is independently selected from the group consisting of -F, -OH, C1-C4 alkyl, C1-C4 fluoroalkyl, C1-C4 alkoxy-C1-C4 alkyl-; each R6 is independently selected from the group consisting of H and C1-C2 alkyl; each R7 is independently H or C1-C2 alkyl; and each R8 is independently H. The invention also relates to specific compounds, the crystalline form of 3-acetyl-1-cyclopentyl-7-{[(3S,4R)-3-hydroxytetrahydro-2H-pyran-4-yl]amino}- 4-methyl-1,6-naphthyridin-2(1H)-one, a pharmaceutical composition based on a compound of formula I or said specific compounds, a method for treating a disease or disorder that would benefit from inhibition of CDK4 and/or CDK6 or abnormal cell growth, use compounds of formula I or specific specified compounds, the method for inhibition of CDK.

EFFECT: inhibition of CDK4 and/or CDK6 by a compound of formula I useful in the treatment of diseases such as pulmonary hypertension, pulmonary arterial hypertension, pulmonary hypertension with left heart disease, pulmonary hypertension with lung disease and/or hypoxemia, pulmonary hypertension due to chronic thrombotic and/or embolic disease; and a disease associated with pulmonary hypertension, including sarcoidosis, histiocytosis X, lymphangiomatosis, and pulmonary vascular compression or abnormal cell growth.

44 cl, 1 dwg, 17 tbl, 34 ex

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RU 2 786 588 C1

Authors

Bhattacharya, Samit Kumar

Behenna, Douglas Carl

Cameron, Kimberly O.

Chen, Ping

Curto, John M.

Freeman-Cook, Kevin Daniel

Jalaie, Mehran

Kania, Robert Steven

Lian, Yajing

Nair, Sajiv Krishnan

Palmer, Cynthia Louise

Pettersson, Martin Youngjin

Rui, Eugene Yuanjin

Sammons, Matthew Forrest

Yang, Qingyi

Zhang, Liying

Dates

2022-12-22Published

2020-04-15Filed