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    HIV REPLICATION INHIBITING PYRIMIDINES
    2.
    发明申请
    HIV REPLICATION INHIBITING PYRIMIDINES 有权

    公开(公告)号：US20080176880A1

    公开(公告)日：2008-07-24

    申请号：US11930835

    申请日：2007-10-31

    申请人： Bart De Corte ,  Marc Rene De Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken

    发明人： Bart De Corte ,  Marc Rene De Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken

    IPC分类号： A61K31/505 ,  C07D239/42 ,  A61P31/18

    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.

    Trisubstituted 1,3,5-Triazine Derivatives
    3.
    发明授权
    Trisubstituted 1,3,5-Triazine Derivatives 失效
    三取代1,3,5-三嗪衍生物

    公开(公告)号：US6150360A

    公开(公告)日：2000-11-21

    申请号：US276362

    申请日：1999-03-25

    申请人： Frederik Frans Desire Daeyaert ,  Bart De Corte ,  Marc Rene De Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici

    发明人： Frederik Frans Desire Daeyaert ,  Bart De Corte ,  Marc Rene De Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici

    IPC分类号： A61K31/53 ,  A61P31/18 ,  C07D251/42 ,  C07D251/50 ,  C07D251/52 ,  C07D251/66 ,  C07D251/70 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D31/54

    CPC分类号： C07D251/42 ,  C07D251/50 ,  C07D251/52 ,  C07D251/66 ,  C07D251/70 ,  C07D403/12

    摘要： This invention concerns the use of the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR.sup.4 or N; n is 0, 1, 2, 3 or 4; R.sup.1 and R.sup.2 are each independently selected from hydrogen, hydroxy, C.sub.1-12 alkyl, C.sub.1-12 alkyloxy, C.sub.1-12 alkylcarbonyl, C.sub.1-12 -alkyloxycarbonyl, aryl, amino, mono- or di(C.sub.1-12 alkyl)amino, mono- or di(C.sub.1-12 alkyl)aminocarbonyl wherein each of the aforementioned C.sub.1-12 alkyl groups may optionally and each individually be substituted; or R.sup.1 and R.sup.2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C.sub.1-12 alkyl)aminoC.sub.1-4 alkylidene; R.sup.3 is hydrogen, aryl, C.sub.1-6 alkylcarbonyl, optionally substituted C.sub.1-6 alkyl; and each R.sup.4 independently is hydroxy, halo, C.sub.1-6 alkyl, C.sub.1-6 -alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is --X--R.sup.5 or --X--Alk--R.sup.6 ; wherein R.sup.5 and R.sup.6 each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is --NR.sup.3 --, --NH--NH--, --N.dbd.N--, --O--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.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.

    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0,1,2,3或4; R 1和R 2各自独立地选自氢，羟基，C 1-12烷基，C 1-12烷氧基，C 1-12烷基羰基，C 1-12烷氧基羰基，芳基，氨基，单或二（C 1-12烷基）氨基，单或二 C 1-12烷基）氨基羰基，其中每个上述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; 并且每个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。

    HIV replication inhibiting pyrimidines
    6.
    发明授权
    HIV replication inhibiting pyrimidines 有权
    HIV复制抑制嘧啶

    公开(公告)号：US06878717B2

    公开(公告)日：2005-04-12

    申请号：US09430966

    申请日：1999-11-01

    申请人： Bart De Corte ,  Marc Rene De Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken

    发明人： Bart De Corte ,  Marc Rene De Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken

    IPC分类号： C07D239/47 ,  A61K20060101 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/675 ,  A61K31/715 ,  A61P31/18 ,  C07D20060101 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D239/80 ,  C07D401/12 ,  C07D403/12

    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, aryl, 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, polyhalo-methylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)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, —NHC(═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.

    摘要翻译： 本发明涉及下式化合物的用途：N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中-a 1 = -a 2 -a 3 = a < 与所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，取代的C 1-6烷基或取代的C 1-6烷氧基C 1-6烷基羰基; 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，多卤代甲硫基，-S（= O）p R 6，-NH-S（= O）p R 6，-C（= O）R 6， NHC（= O）H，-C（= O）NHNH 2，-NHC（= O）R 6，-C（= NH）R 6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-; Q是氢，C 1-6烷基，卤素，多卤代-C 1-6烷基或任选取代的氨基; 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，多卤甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O） -C（= O）NHNH

    Hiv Inhibiting 1,2,4-Triazin-6-One Derivatives
    7.
    发明申请
    Hiv Inhibiting 1,2,4-Triazin-6-One Derivatives 有权
    HIF抑制1,2,4-三嗪-6-酮衍生物

    公开(公告)号：US20090012092A1

    公开(公告)日：2009-01-08

    申请号：US11573224

    申请日：2005-08-10

    申请人： Georges Joseph Cornelius Hoornaert ,  Amuri Kilonda ,  Jan Heeres ,  Paulus Joannes Lewi ,  Marc Rene de Jonge ,  Frederik Frans Desire Daeyaert ,  Hendrik Maarten Vinkers ,  Lucien Maria Henricus Koymans ,  Paul Adriaan Jan Janssen ,  Frank Xavier Jozef Herwig Arts

    发明人： Georges Joseph Cornelius Hoornaert ,  Amuri Kilonda ,  Jan Heeres ,  Paulus Joannes Lewi ,  Marc Rene de Jonge ,  Frederik Frans Desire Daeyaert ,  Hendrik Maarten Vinkers ,  Lucien Maria Henricus Koymans ,  Paul Adriaan Jan Janssen ,  Frank Xavier Jozef Herwig Arts

    IPC分类号： A61K31/53 ,  C07D253/06 ,  A61P31/18

    CPC分类号： C07D253/075

    摘要： The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(═O)pR6; —NH—S(═O)pR6; —C(═O)R6; —NHC(═O)H; —C(═O)NHNH2; NHC(═O)R6; C(═NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14 —C(═O)—NHR13; —C(═O)—NR13 R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 or X2 represents —NR1—; —NH—NH—; —N═N—; —O—; —C(═O)—; —C1-4alkanediyl-; —CHOH—; —S—; —S(═O)p—; —X4—C1-4alkanediyl-; —C1-4alkanediyl-X4—; or —C1-4alkanediyl-X4—C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式N-氧化物的HIV复制抑制剂，其药学上可接受的加成盐，季胺或其立体化学异构形式，其中环A和环B表示苯基，吡啶基，哒嗪基，嘧啶基或吡嗪基; n和m为1〜4; R1表示氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷氧基羰基; 任选取代的C 1-6烷基; 被C 1-6烷氧基羰基取代的C 1-6烷氧基C 1-6烷基羰基; R2或R4代表氢; 羟基; 光环; 任选取代的C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的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; C 1-6烷基羰基氧基; 羧基; 氰基; 硝基 氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-4烷基; 多卤代1-4烷基氧基; 多卤代 -S（-O）p R 6; -NH-S（-O）p R 6; -C（-O）R 6; -NHC（-O）H; -C（-O）NHNH 2; NHC（-O）R 6; C（-NH）R 6; 或R7; R2a或R3表示氰基; 氨基羰基; 氨基; 光环; NHR13; NR 13 R 14 -C（-O）-NHR 13; -C（ - ） - NR 13 R 14; -C（-O）-R 15; -CH-N-NH-C（-O）-R16; 任选取代的C 1-6烷基; 任选取代的C 1-6烷氧基; 任选取代的C 1-6烷氧基C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7或-X3-R7; X1或X2表示-NR1-; -NH-NH-; -N-N- -O-; -C（-O） - ; -C 1-4烷二基 -CHOH-; -S-; -S（-O）p - ; -X4-C1-4烷二基 -C 1-4烷二基-X4-; 或-C1-4烷二基-X4-C1-4烷二基; 它们作为药物的用途，它们用于制备用于治疗或预防HIV感染的药物的用途; 其制备方法和包含它们的药物组合物。

    HIV replication inhibiting pyrimidines
    8.
    发明授权
    HIV replication inhibiting pyrimidines 有权

    公开(公告)号：US07037917B2

    公开(公告)日：2006-05-02

    申请号：US10634682

    申请日：2003-08-05

    申请人： Bart De Corte ,  Marc Rene De Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken

    发明人： Bart De Corte ,  Marc Rene De Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken

    IPC分类号： C07D239/48 ,  A61K31/506 ,  A61P31/18

    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, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, 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(═O)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, —NHC(═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.