PYRROLOPYRIMIDINE COMPOUNDS FOR MALIGNANT TUMOUR TREATMENT Russian patent published in 2017 - IPC C07D487/04 A61K31/519 A61P35/00 

Abstract RU 2631655 C2

FIELD: pharmacology.

SUBSTANCE: in formula I , one of X and X' is N, and the other X and X' is C; one of the dashed lines in formula I is a single bond, and the other dashed line in formula I is a double bond; R1 is phenyl which may be substituted with 1 to 2 substituents selected from halogen atoms, S(O)2R, where R is a 5-6-member cycloalkyl in which one CH2 group is optionally replaced by an oxygen atom; NRaRb, -CH2NRaRb, 1,1-cyclopropyl-NRaRb, S(O)2NRaRb, wherein each Ra and Rb are hydrogen or both Ra and Rb are 4-6-member heterocycloalkyl which may further contain NH, N-CH3, O (oxygen) as a heteroatom and may be substituted by halogen atoms; R2 is -R5'R6, where R5' is a covalent bond or C1-C3alkyl, and R6 is C6cycloalkyl, and wherein R6 is optionally substituted one to two times with independently selected polar groups selected from amino or hydroxy; R3 is -NR7R8, where one of R7 and R8 is selected from H, C1-C6alkyl, and the other R7 and R8 is selected from C1-C6alkyl, C3-C6thcycloalkyl-C1-C6alkyl, each of which is optionally substituted once with a polar group selected from hydroxy; or R2 and R3 together form a linking group, wherein the linking group is -NH-(CH2)4-C(=O)-NH-(CH2)3-, R4 is H and R5 is H or a pharmaceutically acceptable salt thereof. The compounds are selected from IA or IB structure, where R1-R5 have the values indicated in paragraph 1.

EFFECT: possibility to use for treatment of a malignant tumour selected from the group consisting of myeloid leukemia, lymphoblastic leukemia, melanoma, malignant breast, lung, colon, liver, stomach, kidney, ovary, uterus and brain.

14 cl, 3 tbl, 5 ex

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RU 2 631 655 C2

Authors

Wang Xiaodong

Liu Jing

Zhang Weihe

Frye Stephen

Kireev Dmitri

Dates

2017-09-26Published

2012-10-01Filed