发明授权
- 专利标题: HIV inhibiting pyrimidine derivatives
- 专利标题(中): HIV抑制嘧啶衍生物
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申请号: US11111358申请日: 2005-04-21
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公开(公告)号: US08026248B2公开(公告)日: 2011-09-27
- 发明人: Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
- 申请人: Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
- 申请人地址: BE Beerse
- 专利权人: Janssen Pharmaceutica N.V.
- 当前专利权人: Janssen Pharmaceutica N.V.
- 当前专利权人地址: BE Beerse
- 优先权: EP98201587 19980514; EP98203948 19981125
- 主分类号: A01N43/54
- IPC分类号: A01N43/54 ; A61K31/505 ; C07D239/02 ; C07D401/00 ; C07D403/00 ; C07D405/00 ; C07D409/00 ; C07D411/00 ; C07D413/00 ; C07D417/00 ; C07D419/00
摘要:
This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.
公开/授权文献
- US20050197354A1 HIV inhibiting pyrimidine derivatives 公开/授权日:2005-09-08