首页> 外国专利> Compounds derived from pyrimidine - 2.4 - dione and Co. - 2.4 - dione and Pharmaceutical composition comprising such compounds to treat Diseases mediated by HIV, AIDS or Arc

Compounds derived from pyrimidine - 2.4 - dione and Co. - 2.4 - dione and Pharmaceutical composition comprising such compounds to treat Diseases mediated by HIV, AIDS or Arc

机译:衍生自嘧啶-2.4-二酮和钴-2.4-二酮的化合物以及包含此类化合物的药物组合物,用于治疗HIV,AIDS或Arc介导的疾病

摘要

Relating to compounds of formula (i), where a is chr3 = ChR2, ch2r3ch2r2, CH2; r1 is alkyl, (ii) (C1 - C6); R2 is H, alkyl (C1 - C3), haloalquilo (C1 - C3), alquenilo (C2 - C6), nrarb X1, among others; is o or s; x2 is or if it is chr3 = ChR2, X2 or NRD; R3 is H or alkyl (C1 - C3); R4 is Halogen, alkyl (C1 - Cycloalkyl (C6), C3 C6), haloalquilo (C1 - C6) or alkoxy (C1 - C6), ra and RB are h,Alkyl (C1 - C3) or acyl (C1 - C6); Rd is H, alkyl or acyl (C1 - C3) (C1 - C6); ar is phenyl substituted by 1 to 3 halogeno, cyano, alkoxy (C1 - C6); n is 1 to 3. Preferred compounds are: 3 - [6 - bromo - 3 - (2 - [- 1 - methyl - tetrahydro - pyrimidin-2-yl) - 2 - phenoxy] - 5 - fluoro chloro BENZONITRILE, 3 - [3 - (4 - amino - 2 - oxo - 2H - pyrimidine - 1 - methyl) - 6 Bromine Fluorine - 2 - phenoxy] - 5 - chloro BENZONITRILE; among others.It also relates to a Pharmaceutical Composition and a preparation method thereof. These compounds inhibit hiv-1 reverse transcriptase, and are useful in the Prevention and Treatment of HIV, AIDS and / or Arc
机译:关于式(i)的化合物,其中a是chr 3 = ChR 2,ch 2r 3 ch 2r 2,CH 2; r1是烷基,(ii)(C1-C6); R 2是H,烷基(C 1 -C 3),卤代alquilo(C 1 -C 3),alquenilo(C 2 -C 6),nrarb X 1等。是o或s; x2是或如果chr3 = ChR2,X2或NRD; R3是H或烷基(C1-C3); R 4是卤素,烷基(C 1-环烷基(C 6,C 3 -C 6),卤代烷基(C 1 -C 6)或烷氧基(C 1 -C 6),ra和RB是h,烷基(C 1 -C 3)或酰基(C 1 -C 6)。 ; Rd是H,烷基或酰基(C1-C3)(C1-C6); ar是被1-3个卤素,氰基,烷氧基(C1-C6)取代的苯基; n为1-3。优选的化合物为:3-[6-溴-3-(2-[-1-甲基-四氢-嘧啶-2-基)-2-苯氧基]-5-氟氯苯甲腈,3- [3-(4-氨基-2-氧代-2H-嘧啶-1-甲基)-6溴氟-2-苯氧基]-5-氯苯甲腈;它还涉及药物组合物及其制备方法。这些化合物抑制hiv-1逆转录酶,可用于预防和治疗HIV,AIDS和/或Arc

著录项

  • 公开/公告号PE02962009A1

    专利类型

  • 公开/公告日2009-03-27

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG;

    申请/专利号PE20080000903

  • 申请日2008-05-27

  • 分类号A61K31/505;A61P31/18;C07D233/72;C07D233/78;C07D239/22;C07D239/54;C07D239/545;C07D239/553;

  • 国家 PE

  • 入库时间 2022-08-21 19:26:03

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