BICYCLIC TETRAHYDROTHIAZEPINE DERIVATIVES USEFUL FOR TREATING NEOPLASTIC AND/OR INFECTIOUS DISEASES Russian patent published in 2020 - IPC C07D281/10 C07D417/12 C07D417/14 A61K31/55 A61P35/00 

Abstract RU 2730524 C2

FIELD: organic chemistry.

SUBSTANCE: invention relates to an immunomodulator which is a compound of formula (I) or a pharmaceutically acceptable salt thereof, where X1 is S; S(O) or S(O)2; X2 is N or C(R4); R1 denotes H or methyl; R2 denotes phenyl; pyridinyl; quinolinyl or thiadiazolyl, where R2 is optionally substituted with one or more R5, which are identical or different; R5 is halogen; CN; OR6; C(O)N(R6R6a); T1 or C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with one or more halogens which are the same or different; R6, R6a are independently selected from a group consisting of H and C1-6 alkyl, where C1-6 alkyl is optionally substituted with one or more halogens, which are identical; T1 is C3-7 cycloalkyl; oxadiazolyl; thiadiazolyl; triazolyl or morpholinyl, where T1 is optionally substituted with one R7; R7 represents C1-6 alkyl; R3 is R3a; OR3a; NHR3a or NHC(O)R3a; R3a is T2; C1-12 alkyl; C2-12 alkenyl or C2-12 alkynyl, where C1-12 alkyl; C2-12 alkenyl and C2-12 alkynyl are optionally substituted with one or three R9, which are identical or different; R9 is halogen; OR10; C(O)N(R10R10a); N(R10)C(O)R10a; T2 or C1-12 alkyl; R10, R10a are independently selected from a group consisting of H or C1-12 alkyl, where C1-12 alkyl is optionally substituted with one R11; T2 is phenyl; C3-7 cycloalkyl; oxanyl; morpholinyl; oxazolyl; pyridinyl; oxolanyl or oxaspiroheptanyl, where T2 is optionally substituted with one or two R12, which are identical or different; R12 is halogen; OR13; OC(O)N(R13R13a); T3 or C1-6 alkyl, where C1-6 alkyl is optionally substituted with one to three R14, which are identical or different; R13, R13a are independently selected from a group consisting of H; C1-6 alkyl; C2-6 alkenyl and C2-6 alkynyl, where C1-6 alkyl is optionally substituted with one or more R14, which are identical; R11, R14 are independently selected from a group consisting of halogen; OR15; C(O)N(R15R15a); or N(R15)C(O)R15a; R15, R15a are independently selected from a group, consisting of H and C1-6 alkyl ; T3 is phenyl or morpholinyl; R4 is H; F; Cl or N (CH3)2; R18 is H or C1-6 alkyl, where C1-6 alkyl is optionally substituted with one R19; R19 is N (R20)C(O)OR20a; R20, R20a are independently selected from a group consisting of H and C1-6 alkyl. Invention also relates to a pharmaceutical composition based on the compound of formula (I).

EFFECT: technical result is obtaining novel compounds and a pharmaceutical composition based thereon, which can be used in medicine for treating cancer.

23 cl, 47 tbl

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RU 2 730 524 C2

Authors

Ermann Monika

Lametshvandtner Gyunter

Amoutseg Patrisia Leoni

Kraft Rassell Styuart

Khanke Tomas

Dzhejms Timoti Robin

Dzhouns Severin Daniel

Lojbner Khans

Loke Puj Leng

Shternberger Ina

Shtyutts Anton

Ver Roland

Uittejker Mark

Dates

2020-08-24Published

2016-02-29Filed