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145 条记录 (耗时 0.084 秒)

    Substituted diamino-1,3,5-triazine derivatives
    42.
    发明授权
    Substituted diamino-1,3,5-triazine derivatives 失效
    取代的二氨基-1,3,5-三嗪衍生物

    公开(公告)号：US06858609B2

    公开(公告)日：2005-02-22

    申请号：US10002456

    申请日：2001-11-15

    申请人： Paul A. J. Janssen ,  Jan Heeres ,  Henri E. L. Moereels ,  Michael Joseph Kukla ,  Donald W. Ludovici

    发明人： Paul A. J. Janssen ,  Jan Heeres ,  Henri E. L. Moereels ,  Michael Joseph Kukla ,  Donald W. Ludovici

    IPC分类号： A61K31/53 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07D251/18 ,  C07D251/22 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D251/42

    CPC分类号： C07D403/06 ,  C07D251/18 ,  C07D251/48 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12

    摘要： This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H7)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; 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： 本发明涉及配制药学上可接受的酸加成盐及其立体化学异构形式的化合物，其中R 1和R 2各自独立地选自氢; 羟基; 氨基; 任选取代的C 1-6烷基; C 1-6烷氧基; C 1-6烷基羰基; C 1-6烷氧基羰基; Ar <1>; 单或二（C 1-6烷基）氨基; 单或二（C 1-6烷基） - 氨基羰基; 二氢-2（3H7） - 呋喃酮; 或R 1和R 2一起可以形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-6烷基）氨基-C 1-4亚烷基; R 3是氢，Ar 1，C 1-6烷基羰基，C 1-6烷基，C 1-6烷氧基羰基，被C 1-6烷氧基羰基取代的C 1-6烷基; R 4，R 5，R 6，R 7和R 8各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，氨基羰基，硝基，氨基， 三卤甲基或三卤代甲氧基; L是任选取代的C 1-10烷基; C3-10烯基; C3-10炔基; C 3-7环烷基; Ar 1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。 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 5-carbo- or heterocyclic substituted pyrimidines
    44.
    发明授权
    HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines 有权
    HIV抑制5-碳环或杂环取代的嘧啶

    公开(公告)号：US07531548B2

    公开(公告)日：2009-05-12

    申请号：US11576068

    申请日：2005-09-29

    申请人： Jerôme Emile Georges Guillemont ,  Jan Heeres ,  Paulus Joannes Lewi

    发明人： Jerôme Emile Georges Guillemont ,  Jan Heeres ,  Paulus Joannes Lewi

    IPC分类号： C07D239/48 ,  C07D239/50 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  A61K31/505 ,  A61P31/18

    CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12

    摘要： HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O)rR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(═O)—, CH2, —CHOH—, —S—, —S(═O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X3—R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhalo C1-6alkyl; polyhalo C1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; R5 is —Y—CqH2q-L or —CqH2q—Y—CrH2r-L; L is aryl or Het; processes for the preparation of these compounds, pharmaceutical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.

    摘要翻译： 式（I）的HIV复制抑制剂N-氧化物，药学上可接受的加成盐，季胺或其立体异构形式，其中-a1 = a2-a3 = a4-是-CH-CH-CH-CH-，-N -CH-CH-CH-，-N-CH-N-CH-，-N-CH-CH-N - ，-NN-CH-CH-; -b1 = b2-b3 = b4-是-CH-CH-CH-CH-，-N-CH-CH-CH-，-N-CH-N-CH-，-N-CH-CH-N-， -NN-CH-CH-; R1是氢; 芳基; 甲酰基 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; R2是OH; 光环; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; 取代的羰基; 羧基; CN; 硝基 氨基; 取代氨基; 多卤甲基 多卤甲硫基 -S（-O）r R 6; C（-NH）R 6; R2a为CN; 氨基; 取代氨基; 任选取代的C 1-6烷基; 光环; 任选取代的C 2-6烷氧基; 取代的羰基; -CH-N-NH-C（-O）-R16; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7或-X3-R7; X 1是-NR 1 - ， - O - ， - C（-O） - ，CH 2，-CHOH - ， - S - ， - S（-O） R3为CN; 氨基; C 1-6烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH-N-NH-C（-O）-R16; 取代的C 1-6烷基; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7; -X3-R7; R4是卤素; 哦; 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; CN; 硝基 多卤代C1-6烷基; 多卤C 1-6烷氧基; 取代的羰基; 甲酰基 氨基; 单或二（C 1-4烷基）氨基或R 7; R5是-Y-CqH2q-L或-CqH2q-Y-CrH2r-L; L是芳基或Het; 制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物以及这些化合物用于预防或治疗HIV感染的用途。

    Hiv Inhibiting Bicyclic Pyrimdine Derivatives
    46.
    发明申请
    Hiv Inhibiting Bicyclic Pyrimdine Derivatives 有权

    公开(公告)号：US20080085907A1

    公开(公告)日：2008-04-10

    申请号：US11718181

    申请日：2005-10-27

    申请人： Jerome Guillemont ,  Mikael Paugam ,  Bruno Delest ,  Jan Heeres ,  Paulus Lewi ,  Paul Adriaan Janssen ,  Frank Javier Arts

    发明人： Jerome Guillemont ,  Mikael Paugam ,  Bruno Delest ,  Jan Heeres ,  Paulus Lewi ,  Paul Adriaan Janssen ,  Frank Javier Arts

    IPC分类号： C07D473/36 ,  A61K31/519 ,  A61K31/52 ,  A61P31/18 ,  C07D487/04 ,  C07D239/70 ,  C07D473/32

    CPC分类号： C07D487/04 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/34

    摘要： HIV replication inhibitors of formula (1) N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl: optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4 alkyl; R7 or —X—R4; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16: substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4 alkyl; R7; —X—R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; -A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.

    Triazolones as apolipoprotein-B synthesis inhibitors
    49.
    发明授权
    Triazolones as apolipoprotein-B synthesis inhibitors 失效
    新型三唑酮作为载脂蛋白-B合成抑制剂

    公开(公告)号：US06197972B1

    公开(公告)日：2001-03-06

    申请号：US09251989

    申请日：1999-02-17

    申请人： Jan Heeres ,  Leo Jacobus Jozef Backx ,  Paul August Clement Luyts

    发明人： Jan Heeres ,  Leo Jacobus Jozef Backx ,  Paul August Clement Luyts

    IPC分类号： C07D40506

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

    摘要： The present invention concerns novel compounds of formula (I). wherein R1 is C1-10alkyl, C3-7cycloalkyl or C1-6alkyl substituted with C3-7cycloalkyl; R2 is hydrogen or C1-6alkyl; Alk represents C1-3alkanediyl; —A— represents a bivalent radical of formula —CH═CH—N═CH— (a), —N═CH—N═CH— (b), —CH═N—N═CH— (c), —CH═CH—CH═N— (d); in said bivalent radicals a hydrogen atom may be replaced by C1-6alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C1-6alkyl or C1—6alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof. The present invention further comprises the pharmaceutical compositions comprising compounds of formula (I), the preparation thereof as well as the use as a medicine in the treatment of hyperlipidemia.

    摘要翻译： 本发明涉及新的式（I）化合物，其中R 1是C 1-10烷基，C 3-7环烷基或被C 3-7环烷基取代的C 1-6烷基; R2是氢或C1-6烷基; Alk表示C1-3烷二基; -A-表示式-CH = CH-N = CH-（a），-N = CH-N = CH-（b），-CH = NN = CH-（c），-CH = CH -CH = N-（d）; 在所述二价基团中，氢原子可被C 1-6烷基取代; 和Ar是未取代的苯基; 被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的苯基; 未取代的萘基; 或被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的萘基; 其立体化学异构形式及其药学上可接受的酸加成盐。 本发明还包含包含式（I）化合物，其制备方法以及用作治疗高脂血症药物的药物组合物。