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ПИРРОЛОПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ ЗЛОКАЧЕСТВЕННОЙ ОПУХОЛИ
专利权人:
THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
发明人:
WANG Xiaodong,ВАНГ Ксяодонг,LIU Jing,ЛЮ Джинг,ZHANG Weihe,ЗХАНГ Вейхе,FRYE Stephen,ФРИЕ Стивен,KIREEV Dmitri,КИРЕЕВ Дмитрий
申请号:
RU2014115847
公开号:
RU0002631655C2
申请日:
2012.10.01
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
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 -R5R6, 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 exИзобретение относится к новым соединениям формулы I или их фармацевтически приемлемой соли, пригодным для применения для лечения злокачественной опухоли, выбранной из группы, состоящей из миелоидного лейкоза, лимфобластного лейкоза, меланомы, злокачественной опухоли молочной железы, легкого, толстой кишки, печени, желудка, почки, яичника, матки и головного мозга. В формуле Iод
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