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    • 6. 发明授权
    • Trisubstituted 1,3,5,-triazine derivatives
    • 三取代1,3,5, - 三嗪衍生物
    • US06372729B1
    • 2002-04-16
    • US09634340
    • 2000-08-08
    • Frederik Frans Desiré DaeyaertBart De CorteMarc René De JongeJan HeeresChih Yung HoPaul Adriaan Jan JanssenRobert W. KavashLucien Maria Henricus KoymansMichael Joseph KuklaDonald William Ludovici
    • Frederik Frans Desiré DaeyaertBart De CorteMarc René De JongeJan HeeresChih Yung HoPaul Adriaan Jan JanssenRobert W. KavashLucien Maria Henricus KoymansMichael Joseph KuklaDonald William Ludovici
    • C07D25166
    • C07D251/42C07D251/50C07D251/52C07D251/66C07D251/70C07D403/12
    • 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, 1, 2, 3 or 4; R1 and R2 are each independently 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 of the aforementioned C1-12alkyl groups may optionally and each individually 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; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X-Alk-R6; wherein R5 and R6 each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; 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 pharmaceutical compositions comprising them.
    • 本发明涉及N-氧化物,其药学上可接受的加成盐和立体化学异构形式的化合物的用途,其中A是CH,CR 4或N; n为0,1,2,3或4; R1和R2各自独立地选自氢,羟基,C1-12烷基,C1-12烷氧基,C1-12烷基羰基,C1-12烷氧基羰基,芳基,氨基,单或二(C1-12烷基)氨基,单或二(C1- 12烷基)氨基羰基,其中各个上述C 1-12烷基可以任选地和各自独立地被取代; 或R 1和R 2可以一起形成吡咯烷基,哌啶基,吗啉基,叠氮基或单或二(C 1-12烷基)氨基C 1-4亚烷基; R3是氢,芳基,C1-6烷基羰基,任选取代的C 1-6烷基; 每个R 4独立地是羟基,卤素,C 1-6烷基,C 1-6烷氧基,氰基,氨基羰基,硝基,氨基,三卤代甲基或三卤代甲氧基; L是-X-R5或-X-Alk-R6; 其中R 5和R 6各自独立地为茚满基,吲哚基或苯基; 所述二氢化茚基,吲哚基或苯基中的每一个可以被取代; 并且X是-NR 3 - , - NH-NH - , - N = N - , - O - , - S - , - S(= O) - 或-S(= O) 芳基是任选取代的苯基; Het是任选取代的脂族或芳族杂环基; 用于制造用于治疗患有HIV(人类免疫缺陷病毒)感染的受试者的药物。 它还涉及作为式(I)化合物的亚组的新化合物,其制备方法和包含它们的药物组合物。
    • 10. 发明授权
    • HIV replication inhibiting pyrimidines
    • HIV复制抑制嘧啶
    • US08003789B2
    • 2011-08-23
    • US11930835
    • 2007-10-31
    • Bart De CorteMarc René de JongeJan HeeresChih Yung HoPaul Adriaan Jan JanssenFrank Xavier Jozef Herwig Arts, legal representativeRobert W. KavashLucien Maria Henricus KoymansMichael Joseph KuklaDonald William LudoviciKoen Jeanne Alfons Van AkenKoenraad Jozef Lodewijk Marcel Andries
    • Bart De CorteMarc René de JongeJan HeeresChih Yung HoPaul Adriaan Jan JanssenRobert W. KavashLucien Maria Henricus KoymansMichael Joseph KuklaDonald William LudoviciKoen Jeanne Alfons Van AkenKoenraad Jozef Lodewijk Marcel Andries
    • C07D239/48A61K31/505A61K31/506A61P31/18
    • A61K31/505A61K31/5513
    • This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, 13 NHC(═O)R6,—C(═NH)R6, aryl; for the treatment of subjects suffering from HIV infection.
    • 本发明涉及式I化合物的N-氧化物,药学上可接受的加成盐,季胺,其立体化学异构体形式的用途,其中-a1 = a2-a3 = a4形成苯基,吡啶基,嘧啶基,哒嗪基,吡嗪基, 乙烯基; n为0〜5; R 1是氢,芳基,甲酰基,C 1-6烷基羰基,C 1-6烷基,C 1-6烷氧基羰基,取代的C 1-6烷基,取代的C 1-6烷氧基C 1-6烷基羰基; R2是羟基,卤素,任选取代的C 1-6烷基,C 2-6烯基或C 2-6炔基,C 3-7环烷基,C 1-6烷氧基,C 1-6烷氧基羰基,羧基,氰基,硝基,氨基,单或二(C 1-6烷基)氨基 ,多卤代甲基,多卤代甲氧基,多卤甲硫基,-S(= O)pR 6,-NH-S(= O)pR 6,-C(= O)R 6,-NHC(= O)H,-C(= O)NHNH 2, NHC(= O)R 6,-C(= NH)R 6,5元杂环; L是任选取代的C 1-10烷基,C 2-10烯基,C 2-10炔基或C 3-7环烷基; 或-X-R 3; Q是氢,C 1-6烷基,卤素,多卤代-C 1-6烷基,任选取代的氨基; Y表示羟基,卤素,C 3-7环烷基,任选取代的C 1-6烷基,C 2-6烯基或C 2-6炔基,C 1-6烷氧基,C 1-6烷氧基羰基,羧基,氰基,硝基,氨基,单 - 或二(C 1-6烷基)氨基 ,多卤甲基,多卤代甲氧基,多卤甲硫基,-S(= O)pR 6,-NH-S(= O)pR 6,-C(= O)R 6,-NHC(= O)H,-C(= O)NHNH 2, NHC(= O)R 6,-C(= NH)R 6,芳基; 用于治疗患有艾滋病毒感染的受试者。