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    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    41.
    发明申请
    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    HEPATITIS C病毒的大肠抑制剂

    公开(公告)号：US20090247512A1

    公开(公告)日：2009-10-01

    申请号：US11995869

    申请日：2008-01-16

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Carl Erik Daniel Jonsson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Susana Ayesa Alvarez ,  Bjorn Olof Classon ,  Hans Kristian Wallberg

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Carl Erik Daniel Jonsson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Susana Ayesa Alvarez ,  Bjorn Olof Classon ,  Hans Kristian Wallberg

    IPC分类号： A61K31/427 ,  C07D245/04 ,  A61K31/4709 ,  A61K31/538 ,  A61P31/04

    CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D413/12 ,  C07D487/04

    摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from wherein said ring system may optionally be substituted with 1-3 substituents; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each of which may be optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from N, O or S, and being optionally substituted with 1-3 substituents pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

    摘要翻译： 式（I）的HCV复制抑制剂及其N-氧化物，盐或立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，C为C; R1是-OR6，-NH-SO2R7; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基或C 3-7环烷基; n为3,4,5或6; R4和R5与它们所连接的氮原子一起形成双环体系，其选自其中所述环系可以任选被1-3个取代基取代; R6是氢; 芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R7是芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 芳基是苯基或萘基，每个可以任选被1-3个取代基取代; Het是含有1至4个独立地选自N，O或S的杂原子的5或6元饱和的，部分不饱和的或完全不饱和的杂环，并且任选被1-3个取代基取代，含有化合物（I）的药物组合物和 制备化合物（I）。 还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。

    HIV INHIBITING 2-(4-CYANOPHENYL)-6-HYDROXYLAMINOPYRIMIDINES
    44.
    发明申请
    HIV INHIBITING 2-(4-CYANOPHENYL)-6-HYDROXYLAMINOPYRIMIDINES 有权
    HIV抑制2-（4-氰基苯基）-6-羟基氨基嘧啶

    公开(公告)号：US20100121060A1

    公开(公告)日：2010-05-13

    申请号：US12690673

    申请日：2010-01-20

    申请人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck

    发明人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck

    IPC分类号： C07D239/48

    CPC分类号： C07D239/48 ,  C07D405/12

    摘要： HIV replication inhibitors of formula pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

    摘要翻译： 式可复用的药学上可接受的加成盐的HIV复制抑制剂; 或其立体化学异构体形式，其中R 1为卤素; R2和R3各自独立地为C1-6烷基; 含有这些化合物作为活性成分的药物组合物和制备这些化合物和组合物的方法。

    Hiv Prodrugs Cleavable by Cd26
    45.
    发明申请
    Hiv Prodrugs Cleavable by Cd26 审中-公开
    Hiv前驱物可被Cd26切割

    公开(公告)号：US20080214648A1

    公开(公告)日：2008-09-04

    申请号：US10555712

    申请日：2004-05-10

    申请人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck ,  Jan Balzarini

    发明人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck ,  Jan Balzarini

    IPC分类号： A61K31/40 ,  C07D493/04 ,  C07D207/12 ,  A61P31/18 ,  A61K31/34

    CPC分类号： C07D493/04 ,  A61K38/00 ,  A61K47/64 ,  C07H15/252 ,  C07K5/06052 ,  C07K5/06113 ,  C07K5/0808 ,  C07K5/1008 ,  C07K5/101 ,  C07K5/1019 ,  C07K5/1021 ,  C07K7/06 ,  C07K9/003

    摘要： The present invention provides new prodrugs which are conjugates of a therapeutic compound and a peptide wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present prodrugs have the formula the stereoisomeric forms and salts thereof, wherein n is 1 to 5; Y is proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine; X is selected from any amino acid in the D- or L-configuration; X and Y in each repeat of [Y-X] are chosen independently from one another and independently from other repeats; Z is a direct bond or a bivalent straight or branched saturated hydrocarbon group having from 1 to 4 carbon atoms; R1 is an aryl, heteroaryl, aryloxy, heteroaryloxy, aryloxyC1-4alkyl, heterocycloalkyloxy, heterocycloalkylC1-4alkyloxy, heteroaryloxyC1-4alkyl, heteroarylC1-4alkyloxy; R2 is arylC1-4alkyl; R3 is C1-10alkyl, C2-6alkenyl or C3-7cycloalkylC1-4alkyl; R4 is hydrogen or C1-4alkyl. The present invention furthermore provides the use of said prodrugs as medicines as well as a method of producing said prodrugs.

    摘要翻译： 本发明提供了新的前体药物，其是治疗化合物和肽的缀合物，其中缀合物可被二肽基肽酶切割，更优选通过CD26，也称为DPPIV（二肽基氨基二肽酶IV））。 本发明的前药具有式的立体异构形式及其盐，其中n为1至5; Y是脯氨酸，丙氨酸，羟脯氨酸，二羟脯氨酸，噻唑烷羧酸（硫脯氨酸），脱氢脯氨酸，哌可酸（L-高脯氨酸），氮杂环丁烷羧酸，氮丙啶羧酸，甘氨酸，丝氨酸，缬氨酸，亮氨酸，异亮氨酸和苏氨酸; X选自D-或L-构型中的任何氨基酸; [Y-X]的每个重复中的X和Y彼此独立地独立地选自其它重复; Z是直接键或具有1至4个碳原子的二价直链或支链饱和烃基; R 1是芳基，杂芳基，芳氧基，杂芳氧基，芳氧基C 1-4烷基，杂环烷氧基，杂环烷基C 1-4烷氧基，杂芳氧基C 1-4烷基，杂芳基C 1-4烷氧基; R 2是芳基C 1-4烷基; R 3是C 1-10烷基，C 2-6链烯基或C 3-7环烷基C SUB 1-4烷基; R 4是氢或C 1-4烷基。 本发明还提供所述前体药物作为药物的用途以及制备所述前体药物的方法。

    SMALL MOLECULE ENTRY INHIBITORS
    46.
    发明申请
    SMALL MOLECULE ENTRY INHIBITORS 有权

    公开(公告)号：US20090203743A1

    公开(公告)日：2009-08-13

    申请号：US12430547

    申请日：2009-04-27

    申请人： Dominique Louis Surleraux ,  Piet Tom Wigernick ,  Markieke Christiane Voets ,  Sandrine Marie Vendeville ,  Herman Augustinus De Kock ,  Bernhard Joanna Vergouwen

    发明人： Dominique Louis Surleraux ,  Piet Tom Wigernick ,  Markieke Christiane Voets ,  Sandrine Marie Vendeville ,  Herman Augustinus De Kock ,  Bernhard Joanna Vergouwen

    IPC分类号： A61K31/4184 ,  C07D405/14 ,  C07D401/14 ,  A61K31/4439 ,  A61P31/18

    CPC分类号： C07D401/12 ,  A61K31/415 ,  C07D235/30 ,  C07D235/32 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D493/04

    摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(═O)—, —C(═S)—, —S(═O)2—, C1-6alkanediyl-C(═O)—, C1-6alkanediyl-C(═S)— or C1-6alkanediyl-S(═O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxy-carbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2′ R12 is H, —NH2, —NR5AR6, —C1-6alkyl or alkyl-W—R14, wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het1, Het2, or amino wherein said amino is optionally mono- or di-substituted with C1-4alkyl and R13 is H, C1-6-alkyl, optionally substituted by aryl, Het1, Het2, hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with C1-4alkyl.

    HIV inhibiting 2-(4-cyanophenyl)-6-hydroxylaminopyrimidines
    48.
    发明授权
    HIV inhibiting 2-(4-cyanophenyl)-6-hydroxylaminopyrimidines 有权
    HIV抑制2-（4-氰基苯基）-6-羟氨基嘧啶

    公开(公告)号：US08119801B2

    公开(公告)日：2012-02-21

    申请号：US12690673

    申请日：2010-01-20

    申请人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck

    发明人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck

    IPC分类号： C07D239/48

    CPC分类号： C07D239/48 ,  C07D405/12

    摘要： HIV replication inhibitors of formula pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

    摘要翻译： 式可复用的药学上可接受的加成盐的HIV复制抑制剂; 或其立体化学异构体形式，其中R 1为卤素; R2和R3各自独立地为C1-6烷基; 含有这些化合物作为活性成分的药物组合物和制备这些化合物和组合物的方法。

    HIV inhibiting 2-(4-cyanophenylamino) pyrimidine oxide derivatives
    49.
    发明授权
    HIV inhibiting 2-(4-cyanophenylamino) pyrimidine oxide derivatives 有权
    HIV抑制2-（4-氰基苯基氨基）嘧啶氧化物衍生物

    公开(公告)号：US07935711B2

    公开(公告)日：2011-05-03

    申请号：US11814958

    申请日：2006-02-20

    申请人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck

    发明人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck

    IPC分类号： C07D239/48 ,  A61K31/505

    CPC分类号： C07D239/48

    摘要： HIV replication inhibitors of formula (I) a pharmaceutically acceptable addition salt; or a stereochemically isomeric form thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl. Pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

    摘要翻译： 式（I）的HIV复制抑制剂药学上可接受的加成盐; 或其立体化学异构体形式，其中R 1为卤素; R2和R3各自独立地为C1-6烷基。 含有这些化合物作为活性成分的药物组合物和制备这些化合物和组合物的方法。