HETEROARYL DERIVATIVE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, A METHOD FOR PRODUCTION THEREOF AND A PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAID ACTIVE SUBSTANCE Russian patent published in 2020 - IPC C07D471/04 C07D487/04 A61K31/519 A61P35/00 A61P19/02 A61P17/06 A61P3/10 A61P5/14 A61P1/04 

Abstract RU 2719367 C2

FIELD: medicine.

SUBSTANCE: invention refers to a new compound of formula 1, its (S) isomer or its pharmaceutically acceptable salt and to versions of its production method. Compounds are characterized by selective inhibition of PI3 kinase selected from the group consisting of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ.The compounds can be used for healthy functional nutrition for preventing or relieving the disease associated with PI3 kinase. In the compound of formula 1

,

is a single bond or a double bond; A is a carbon (C) or nitrogen (N) atom; R1 represents a hydrogen atom (H) or -NH2; R2 is H, -CN, C1-5 linear or branched alkyl, unsubstituted C3-7 cycloalkyl or halogen atom; R3 is H; R4 is H or C1-5 linear or branched alkyl; or R3 and R4 can form 5-member unsubstituted heterocycloalkyl containing one heteroatom N, together with atoms conjugated therewith; and R5 is

, , or ,

where n is an integer in range of 0~3, R6 is an unsubstituted or substituted phenyl or unsubstituted or substituted 6-member heteroaryl containing one heteroatom N, said substituted phenyl and substituted heteroaryl contain one or two substitutes selected from a group consisting of a halogen atom, C1-2 linear or branched alkyl, R7 denotes H, a halogen atom or unsubstituted 6-member heteroaryl containing one heteroatom N, and R8 is H or halogen.

EFFECT: compounds can be used for preventing or treating a disease selected from a group consisting of cancer selected from the following group: blood malignant growths, ovarian cancer, cervical cancer, breast cancer, colon and rectal cancer, hepatic cancer, stomach cancer, pancreatic cancer, colon cancer, peritoneal metastases, skin cancer, bladder cancer, prostate cancer, thyroid cancer, lung cancer, osteosarcoma, fibrous tumor and brain tumor; an autoimmune disease selected from a group consisting of rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type 1 diabetes, thyroid hyperfunction, myasthenia gravis, Crohn's disease, ankylosing spondylitis, psoriasis, autoimmune atrophic gastritis and Sjögren syndrome; respiratory disease, selected from a group consisting of chronic obstructive pulmonary disease (COPD), rhinitis, asthma, chronic bronchitis, chronic inflammatory pulmonary disease, silicosis, pulmonary sarcoidosis, pleurisy, alveolitis, vasculitis, emphysema, pneumonia and bronchiectasis.

20 cl, 3 tbl, 103 ex

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RU 2 719 367 C2

Authors

Lee, Ge Hyeong

Lim, Hee-Jong

Cho, Heeyeong

Park, Woo Kyu

Kim, Seong Hwan

Choi, Jung Hwan

Dates

2020-04-17Published

2016-06-01Filed