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    Triazolones as apolipoprotein-B synthesis inhibitors
    1.
    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。

    Water soluble azoles as broad-spectrum antifungals
    2.
    发明授权
    Water soluble azoles as broad-spectrum antifungals 有权
    水溶性唑类作为广谱抗真菌剂

    公开(公告)号：US06384030B1

    公开(公告)日：2002-05-07

    申请号：US09700251

    申请日：2000-11-09

    申请人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx ,  Louis Jozef Elisabeth Van der Veken ,  Jan Heeres ,  Frank Christopher Odds

    发明人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx ,  Louis Jozef Elisabeth Van der Veken ,  Jan Heeres ,  Frank Christopher Odds

    IPC分类号： C07D40514

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

    摘要： The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein L represent a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkanediyl; is 1, 2 or 3; Y is O, S or NR2; R1 represents hydrogen, aryl, Het1, or an optionally substituted C1-6alkyl; each R2 independently represents hydrogen or C1-6alkyl; or in case R1 and R2 are attached to the same nitrogen atom, they may be taken together to form a heterocyclic radical; or they may be taken together to form an azido radical; each R3 independently represents hydrogen, hydroxy or C1-4alkyloxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; Het1 represents an optionally substituted monocyclic or bicyclic heterocyclic radical; Het2 is the same as Het1 and may also be piperazinyl, homopiperazinyl, 1,4-dioxanyl, morpholinyl, thiomorpholinyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen or C1-4alkyl; or R6 and R7 taken together form a bivalent radical of formula —N═CH— (i), —CH═N— (ii), —CH═CH— (iii), —CH2—CH2 (iv), wherein one hydrogen atom in the radicals (i) and (ii) may be replaced with a C1-4alkyl radical and one or more hydrogen atoms in radicals (iii) and (iv) may be replaced by a C1-4alkyl radical; D represents a trisubstituted 1,3-dioxolane derivative; as antifungals; their processes for preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物形式的新化合物，其药学上可接受的加成盐和立体化学异构形式，其中L代表甲酰基的基团，每个Alk独立地表示任选取代的C 1-6烷二基; 是1，2或3; Y是O，S或NR2; R 1表示氢，芳基，Het1或任选取代的C 1-6烷基; 每个R 2独立地表示氢或C 1-6烷基; 或者在R1和R2连接到相同的氮原子的情况下，它们可以一起形成杂环基; 或者它们可以一起形成叠氮基; 每个R 3独立地表示氢，羟基或C 1-4烷氧基; 芳基表示苯基，萘基，1,2,3,4-四氢 - 萘基，茚基或茚满基; 每个所述芳基可任选被取代; Het1表示任选取代的单环或双环杂环基; Het2与Het1相同，也可以是哌嗪基，高哌嗪基，1,4-二氧杂环己基，吗啉基，硫代吗啉基; R6代表氢或C1-4烷基; R7代表氢或C1-4烷基; 或者R 6和R 7一起形成式-N = CH-（ⅰ），-CH = N-（ⅱ），-CH = CH-（ⅲ），-CH 2 -CH 2（ⅳ）的二价基团，其中一个氢 基团（i）和（ii）中的原子可以被C 1-4烷基取代，并且基团（iii）和（iv）中的一个或多个氢原子可被C 1-4烷基取代; D表示三取代的1,3-二氧戊环衍生物; 作为抗真菌剂; 其制备方法，含有它们的组合物及其作为药物的用途。

    Apolipoprotein-B synthesis inhibitors
    3.
    发明授权
    Apolipoprotein-B synthesis inhibitors 失效
    载脂蛋白-B合成抑制剂

    公开(公告)号：US5929075A

    公开(公告)日：1999-07-27

    申请号：US817247

    申请日：1997-04-09

    申请人： Jan Heeres ,  Leo Jacobus Jozef Backx ,  Robert Jozef Maria Hendrickx ,  Luc Alfons Leo Van der Eycken ,  Didier Robert Guy Gabriel de Chaffoy de Courcelles

    发明人： Jan Heeres ,  Leo Jacobus Jozef Backx ,  Robert Jozef Maria Hendrickx ,  Luc Alfons Leo Van der Eycken ,  Didier Robert Guy Gabriel de Chaffoy de Courcelles

    IPC分类号： C07D405/12 ,  A61K31/41 ,  A61K31/495 ,  A61P3/06 ,  A61P9/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D407/14

    CPC分类号： C07D417/14 ,  C07D405/14 ,  C07D413/14

    摘要： The present invention provides novel compounds of formula ##STR1## the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula:--N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d), --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.

    摘要翻译： PCT No.PCT / EP95 / 04111 Sec。 371日期1997年04月9日 102（e）日期1997年4月9日PCT 1995年10月19日PCT PCT。 第WO96 / 13499号公报 日期：1996年5月9日本发明提供了新型式的化合物N-氧化物，其立体化学异构形式及其药学上可接受的酸加成盐，其中A和B一起形成下式的二价基团-N = CH- （a）中，-CH = N-（b），-CH 2 -CH 2 - （c），-CH = CH-（d），-C（= O）-CH 2 - （e） O） - （f）; R1是氢，C1-6烷基或卤素; R2是氢或卤素; R3是氢; C 1-8烷基; C 3-6环烷基或被羟基，氧代，C 3-6环烷基或芳基取代的C 1-8烷基。 Het是五或六元任选取代的杂环。 公开了作为药物的使用，特别是作为降脂剂的用途以及用于制备化合物和组合物的药物组合物和方法。

    Triazolones as apolipoprotein-B synthesis inhibitors
    5.
    发明授权
    Triazolones as apolipoprotein-B synthesis inhibitors 失效
    三唑酮作为载脂蛋白-B合成抑制剂

    公开(公告)号：US5922718A

    公开(公告)日：1999-07-13

    申请号：US930847

    申请日：1997-10-07

    申请人： Jan Heeres ,  Leo Jacobus Josef Backx ,  Paul August Clement Luyts ,  Didier Robert Guy Gabriel de Chaffoy de Courcelles

    发明人： Jan Heeres ,  Leo Jacobus Josef Backx ,  Paul August Clement Luyts ,  Didier Robert Guy Gabriel de Chaffoy de Courcelles

    IPC分类号： C07D405/14 ,  A61K31/495 ,  A61P3/06 ,  C07D405/06 ,  C07D521/00 ,  C07D403/14

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

    摘要： The present invention concerns novel compounds of formula (I). ##STR1## wherein R.sup.1 is C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-7 cycloalkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; Alk represents C.sub.1-3 alkanediyl; --A-- represents a bivalent radical of formula --CH.dbd.CH--N.dbd.CH-- (a), --N.dbd.CH--N.dbd.CH-- (b), --CH.dbd.N--N.dbd.CH-- (c), --CH.dbd.CH--CH.dbd.N-- (d); in said bivalent radicals a hydrogen atom may be replaced by C.sub.1-6 alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; 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： PCT No.PCT / EP96 / 01585第 371日期1997年10月7日第 102（e）日期1997年10月7日PCT 1996年4月12日PCT PCT。 WO96 / 33193 PCT出版物 日期：1996年10月24日本发明涉及新的式（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。

    HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
    8.
    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。