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heterocyclyl- or 5-carbo substituted pyrimidines for hiv inhibition, and pharmaceutical composition
- 专利权人:
- JANSSEN SCIENCES IRELAND UC;TIBOTEC PHARMACEUTICALS LTD.;Janssen R&D Ireland;TIBOTEC PHARMACEUTICALS
- 发明人:
- Jan Heeres,Jérôme Emile Georges Guillemont,Paulus Joannes Lewi
- 申请号：
- BRPI0515935
- 公开号：
- BRPI0515935B1
- 申请日:
- 2005.09.29
- 申请国别(地区):
- BR
- 年份:
- 2019
- 代理人:
- 摘要：
- "substituted heterocyclyl or 5-carbo pyrimidines for hiv inhibition". hiv replication inhibitors of formula (i), n-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein: - a ^ 1 ^ = a ^ 2 ^ - a ^ 3 ^ = a ^ 4 ^ is -ch = ch = ch = ch-, -n = ch-ch = ch, -n = ch-n = ch-, -n = ch-ch = n, -n = n-ch = ch； -b ^ 1 ^ = b ^ 2 ^ - b ^ 3 ^ = b ^ 4 ^ is -ch = ch-ch = ch, -n = ch-ch = ch, -n = ch-n = ch, -n = ch-ch = n-, -n = n-ch = ch, -n = ch-ch = ch, -n = ch-n = ch, -n = ch-ch = n-, -n = n- ch = ch-； R2 is hydrogen； arila； formyl； optionally substituted C1 -C6 alkyl； C 1-6 alkyloxycarbonyl； r ^ 2 ^ is oh； halo； optionally substituted C 2-6 alkynyl； substituted carbonyl； carboxyl； cn； nitro； amino； substituted amino； polyhalomethyl； polyhlomethylthio； -s (= o) rr ^ 6 ^； c (= nh) r 6 = 6； R2 is cn； amino； substituted amino； optionally substituted C1 -C6 alkyl； halo； optionally substituted C1-6 alkyloxy C1-6 alkyl； optionally substituted C 2-6 alkenyl or optionally substituted C 2-6 alkynyl； -c (= n-o-r8) -C 1-4 alkyl； R 7 or R 3 -R 7； X ~ 1 ~ is -nr ^ 1 ^ -, -o-, -c (=)) -, ch ~ 2 ~, -choh-, s-, -s (= o) -； R2 is cn； amino； optionally substituted C1 -C6 alkyl； -c (= n-o-R 8) - C 1-4 alkyl； R ^ 7 ^； -x ~ 3 -r ^ 7 ^； R4 is halo； oh； optionally substituted C1-6 alkyl； C 2-6 alkenyl or C 2-6 alkynyl； C 3-7 cycloalkyl； C 1-6 alkyloxy； cn； nitro； C 1-6 alkyl polyhalo； polyhalo C 1-6 alkyloxy； substituted carbonyl； formyl； amino； mono- or di (C 1-4 alkyl) amino or R 7； R ^ 5 ^ is -y-c ~ q ~ h ~ 2q-1 or c ~ q ~ h ~ 2q ~ -y-c ~ 2 ~ h ~ 2 ~ r-1； 1 is anila or het； processes for preparing such compounds, pharmaceutical compositions comprising such compounds as active ingredients and the use of such compounds for the prevention or treatment of HIV infection."pirimidinas heterociclil- ou 5-carbo substituídas para inibição de hiv". inibidores de replicação de hiv da fórmula (i), n-óxidos, sais de adição farmaceuticamente aceitáveis, amin
- 来源网站：
- 中国工程科技知识中心
- 来源网址：
- http://www.ckcest.cn/home/
