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INHIBITORS OF TYPE ErbB INHIBITORS
专利权人:
ERREJ BAJOFARMA INK.
发明人:
LISSIKATOS Dzhozef P. (US),ЛИССИКАТОС Джозеф П. (US),MARMSATER Fredrik P. (US),МАРМСАТЕР Фредрик П. (US),CHAO CHzhan (US),ЧАО Чжань (US),GRESCHUK Dzhuli Mari (US),ГРЕСЧУК Джули Мари (US),VEJDONG Lyu (,ВЕЙДОНГ Лью (US),ХЕННИНГС Дэвид Д. (US)
申请号:
RU2011122539/04
公开号:
RU0002592703C2
申请日:
2006.11.15
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to novel compounds of formula 10 and method for production thereof. Compounds possess properties of receptor tyrosine kinase type I inhibitors and can be used in treating hyperproliferative disorders. Invention also relates to novel intermediate compounds of formula 8 and 9 and to method of producing compounds 9. Compounds 10 and 8 correspond to common formulas (8) (10), where each R6, R8 and R8a are independently hydrogen or C1-C6alkyl, where said alkyl is optionally substituted OR15; or R8 and R8a together with atom to which they are connected, three-six-Member carbocyclic ring is formed; and R15 is hydrogen or C1-C6alkyl. Connection 9 corresponds to general formula (9), where A represents O; E represents , where X is CH; D1, D2 and D3 independently represent N or CR19; D4 and D5 are independently N or CR19 and D6 represents O, S or NR20, at least one of D4 and D5 is not CR19; D7, D8, D9 and D10 represent independently N or CR19, wherein at least one of D7, D8, D9 and D10 represents N; R1 represents H or C1-C6alkyl; each R2 independently represents halogen, cyano, trifluoromethyl, difluoromethyl, ftormetil or C1-C6alkyl; each R6, R8 and R8a are independently hydrogen or C1-C6alkyl, where said alkyl is optionally substituted by OR15, or R8 and R8a together with atom, to which they are bonded, 3-6-member carbocyclic ring is formed; R15 represents H or C1-C6alkyl; each R19 independently represents H, halogen or C1-C6alkyl; each R20 is independently hydrogen or C1-C4alkyl, j is 0 and n represents 0, 1 or 2.EFFECT: method of preparing compound of formula 10 involves condensation of compound of formula 8 with compound of formula 2 (2) in presence of acid in acceptable solvent, followed by thiourea of formula 9 cyclization, preferably in water solution of NaOH in tetrahydrofuran with addition of thozilchloride TsCl.9 cl, 1 tbl, 281 exИзобретение относится к новым соединениям формулы 10 и способу их получения. Соединения
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