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MIKROBICIDNI PIRIMIDINI ILI TRIAZINI ZA PREVENCIJU PRIJENOSA HIV SEKSUALNIM PUTEM
专利权人:
TIBOTEC PHARMACEUTICALS LTD.
发明人:
VAN ROEY, JENS (MARCEL),DE BETHUNE, MARIE-PIERRE T.M.M.G,STOFFELS, PAUL
申请号:
HRP20041177
公开号:
HRP20041177B1
申请日:
2004.12.10
申请国别(地区):
HR
年份:
2013
代理人:
摘要:
Microbial activity of some non nucleoside inhibitors containing pyridine or tributylamine. Current compounds inhibit systemic infection in people living with HIV. In particular, these compounds can prevent the human body from sexually transmitted HIV. 1. Requirement 1: use the compound in formula (1),(2) Or (3),One of the formula compounds (1) is equivalent to nitrous oxide, a pharmaceutically acceptable additive salt or a stereochemical isomerization formula, when y is Cr5 or N; a is ch, Cr4 or N; n is 0, 1, 2, 3 or 4; q is - nr1r2 orwhen Y is CR5, then Q can also be hydrogen, each of R1 and R2 is independently selected from hydrogen, hydroxy, C1-2 alkyl, C1-12 alkyloxy, C1-12 alkylcarbonyl, C1-12 alkyloxycarbonyl, aryl, amino, mono- or di (C1-12 alkyl) amino, mono- or di (C1-12 alkyl) aminocarbonyl, where each of said C1-12 alkyl groups can be optionally and individually separately, substituted with one or two substituents each of which is independently selected from hydroxy, C1-6 alkyloxy, C1-6 hydroxyalkyloxy, carboxyl, C1-6 alkyloxycarbonyl, cyano, amino, imino, aminocarbonyl, aminocarbonylamino, mono- or di (C1-6 alkyl) amino,aryl and Het, or R1 and R2 together can form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono or di (C1-12 alkyl) C1-4 aminoalkylidene; R 3 is hydrogen, aryl, C 1-6 alkylcarbonyl, C 1-6 alkyl, C 1-6 alkyloxycarbonyl, C 1-6 alkyl substituted with C 1-6 alkyloxycarbonyl and each R 4 is independently hydroxy, halo, C 1-6 alkyl, C 1-6 alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy or,when Y is CR5, then R4 may also represent C1-6 alkyl substituted with cyano or aminocarbonyl, R5 is hydrogen or C1-4 alkyl; L is -X1-R6 or X2-Alk-R7 where each of R6 and R7 is independently phenyl or phenyl substituted with 1, 2, 3, 4 or 5 substituents, each of which is independently selected from halo, hydroxy, C1-6 alkyl, C1-6 alkyloxy, C1-6 alkylcarbonyl, C1-6 alkyloxycarbonyl, formyl, cyano, nitro, amino and trifluoromethyl
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