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    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

    申请人： Bart De Corte ,  Marc René de Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Frank Xavier Jozef Herwig Arts, legal representative ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken ,  Koenraad Jozef Lodewijk Marcel Andries

    发明人： Bart De Corte ,  Marc René 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 ,  Koenraad Jozef Lodewijk Marcel Andries

    IPC分类号： C07D239/48 ,  A61K31/505 ,  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, 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

    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

    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

    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

    CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/49 ,  C07D239/50 ,  C07D401/12

    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

    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

    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

    IPC分类号： C07D23928

    CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/49 ,  C07D239/50 ,  C07D401/12

    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

    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

    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

    IPC分类号： A61K31506

    CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/49 ,  C07D239/50 ,  C07D401/12

    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。