HIV replication inhibiting pyrimidines
    2.
    发明授权
    HIV replication inhibiting pyrimidines 有权
    HIV复制抑制嘧啶

    公开(公告)号:US08003789B2

    公开(公告)日:2011-08-23

    申请号:US11930835

    申请日:2007-10-31

    CPC分类号: A61K31/505 A61K31/5513

    摘要: 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.

    摘要翻译: 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。

    HIV inhibiting pyrimidine derivatives
    4.
    发明授权
    HIV inhibiting pyrimidine derivatives 有权
    HIV抑制嘧啶衍生物

    公开(公告)号:US08026248B2

    公开(公告)日:2011-09-27

    申请号:US11111358

    申请日:2005-04-21

    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.

    摘要翻译: 本发明涉及式I化合物在N-氧化物,其药学上可接受的加成盐和立体化学异构形式中的用途,其中A是CH,CR 4或N; n为0〜4; Q是氢或-NR1R2; R1和R2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,其中每个C 1-12烷基可以任选被取代; 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; R 3是氢,芳基,C 1-6烷基羰基,任选取代的C 1-6烷基,C 1-6烷氧基羰基; R4为羟基,卤素,任选取代的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,三卤代甲氧基; R5是氢或C1-4烷基; L是任选取代的C 1-10烷基,C 3-10烯基,C 3-10炔基,C 3-7环烷基; 或L是-X1-R6或-X2-Alk-R7,其中R6和R7是任选取代的苯基; X 1和X 2是-NR 3 - , - NH-NH - , - N - , - O - , - S - , - S(= O) - 或-S(= O) Alk是C1-4烷二基; 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组合物。

    HIV Inhibiting pyrimidine derivatives
    6.
    发明授权
    HIV Inhibiting pyrimidine derivatives 有权
    HIV抑制嘧啶衍生物

    公开(公告)号:US06440986B2

    公开(公告)日:2002-08-27

    申请号:US09749181

    申请日:2000-12-27

    IPC分类号: C07D23928

    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, C1-6alkyloxycarbonyl,; 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 potionally 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.

    摘要翻译: 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0〜4; Q是氢或-NR1R2; R1和R2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,一或二(C1-12烷基)氨基,单或二(C1-12烷基) 其中每个C 1-12烷基可以任选被取代; 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; R 3是氢,芳基,C 1-6烷基羰基,任选取代的C 1-6烷基,C 1-6烷氧基羰基。 R4为羟基,卤素,任选取代的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,三卤代甲氧基; R5是氢或C1-4烷基; L是任选取代的C 1-10烷基,C 3-10烯基,C 3-10炔基,C 3-7环烷基; 或L是-X1-R6或-X2-Alk-R7,其中R6和R7是任选取代的苯基; X1和X2是-NR3-,-NH-NH-,-N = N-,-O - , - S - , - S(= O) - 或-S(= O) Alk是C1-4烷二基; 芳基是取代的苯基; Het是任选取代的脂族或芳族杂环基团: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组合物。

    HIV inhibiting pyrimidine derivative
    7.
    发明授权
    HIV inhibiting pyrimidine derivative 有权
    HIV抑制嘧啶衍生物

    公开(公告)号:US06197779B1

    公开(公告)日:2001-03-06

    申请号:US09276360

    申请日:1999-03-25

    IPC分类号: A61K31506

    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, C1-6alkyloxycarbonyl,; 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 potionally 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.

    摘要翻译: 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0〜4; Q是氢或-NR1R2; R1和R2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,一或二(C1-12烷基)氨基,单或二(C1-12烷基) 其中每个C 1-12烷基可以任选被取代; 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; R 3是氢,芳基,C 1-6烷基羰基,任选取代的C 1-6烷基,C 1-6烷氧基羰基。 R4为羟基,卤素,任选取代的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,三卤代甲氧基; R5是氢或C1-4烷基; L是任选取代的C 1-10烷基,C 3-10烯基,C 3-10炔基,C 3-7环烷基; 或L是-X1-R6或-X2-Alk-R7,其中R6和R7是任选取代的苯基; X1和X2是-NR3-,-NH-NH-,-N = N-,-O - , - S - , - S(= O) - 或-S(= O) Alk是C1-4烷二基; 芳基是取代的苯基; 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组合物。

    2,4-disubstituted triazine derivatives
    9.
    发明授权
    2,4-disubstituted triazine derivatives 失效
    2,4-二取代的三嗪衍生物

    公开(公告)号:US06638932B1

    公开(公告)日:2003-10-28

    申请号:US09831808

    申请日:2001-08-02

    IPC分类号: C07D25116

    摘要: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein —a1═a2—a3═a4— forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently 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)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

    摘要翻译: 本发明涉及配制N-氧化物的化合物,药学上可接受的加成盐,季胺及其立体化学异构形式的用途,其中-a 1 = a 2 -a 3 = a 4 - 与连接的乙烯基形成苯基,吡啶基,嘧啶基,哒嗪基或吡嗪基; n为0〜4; 并在可能的情况下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烷氧基羰基或取代的C 1-6烷基; 每个R 2独立地是羟基,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,多卤甲氧基,多卤甲硫基,-S(= O)p R 4,-NH-S(= O)p R 4,-C(= O)R 4, = O)H,-C(= O)NHNH 2,-NHC(= O)R 4,-C(= NH)R 4或5元杂环; p为1或2; 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L是-X-R 3,其中R 3是任选取代的苯基,吡啶基,嘧啶基,吡嗪基或哒嗪基; X是-NR 1 - , - NH-NH-,-N = N-,-O-,-C(= O) - , - CHOH-,-S-,-S(= O) - 或 - S(= O)2-; 芳基是任选取代的苯基; 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。

    HIV REPLICATION INHIBITING PYRIMIDINES

    公开(公告)号:US20080176880A1

    公开(公告)日:2008-07-24

    申请号:US11930835

    申请日:2007-10-31

    CPC分类号: A61K31/505 A61K31/5513

    摘要: This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl; pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5. R1 is hydrogen, al, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently 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(═CO)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an 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, —C(—O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.