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    Biocidal benzylbiphenyl derivatives
    1.
    发明授权
    Biocidal benzylbiphenyl derivatives 失效
    杀生物苄基联苯衍生物

    公开(公告)号：US06440440B1

    公开(公告)日：2002-08-27

    申请号：US09647015

    申请日：2000-09-22

    申请人： Lieven Meerpoel ,  Mark Arthur Josepha Van der Flaas ,  Louis Jozef Elisabeth Van Der Veken ,  Jan Heeres

    发明人： Lieven Meerpoel ,  Mark Arthur Josepha Van der Flaas ,  Louis Jozef Elisabeth Van Der Veken ,  Jan Heeres

    IPC分类号： A01N4340

    CPC分类号： C07D211/58 ,  A01N33/04 ,  A01N33/12 ,  A01N43/40 ,  C07C211/27 ,  C07C211/28 ,  C07D211/26 ,  C07D211/70

    摘要： This invention concerns compounds of formula. stereochemically isomeric forms thereof, acid or base addition salts thereof, N-oxides thereof, or quaternary ammonium derivatives thereof, wherein the dotted line is an optional bond; X is a direct bond when the dotted line represents a bond, or X is hydrogen or hydroxy, when the dotted line does not represent a bond; R1, R2, R5 and R6 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, —SO3H, and the like; R3 and R4 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, nitro, amino, cyano, trifluoromethyl, or trifluoromethoxy; L is a radical of formula wherein A1 is a direct bond or C1-6alkanediyl; A2 is C2-6alkanediyl; and R7 to R11 are hydrogen, C1-6alkyl, aminoC1-6alkyl and the like; having biocidal properties; their preparation, compositions containing them and their use as a biocide.

    摘要翻译： 本发明涉及其化学式为其立体化学异构形式，其酸或碱加成盐，其N-氧化物或其季铵衍生物，其中虚线为任选的键; 当虚线不表示键时，X是直链键，当虚线表示键时，X表示氢或羟基; R 1，R 2，R 5和R 6各自独立地选自氢，卤素，羟基，C 1-4烷基，C 1-4烷氧基，-SO 3 H等; R 3和R 4各自独立地选自氢，卤素，羟基，C 1-4烷基，C 1-4烷氧基，硝基，氨基，氰基，三氟甲基或三氟甲氧基; L是公式的基数A1 直接键或C1-6烷二基; A2是C2-6烷二基; 并且R 7至R 11为氢，C 1-6烷基，氨基C 1-6烷基等; 具有杀生物性; 它们的制备方法，含有它们的组合物以及它们作为杀生物剂的用途。

    2,4,4-trisubstituted-1,3-dioxolane antifungals
    2.
    发明授权
    2,4,4-trisubstituted-1,3-dioxolane antifungals 有权
    2,4,4-三取代-1,3-二氧戊环抗真菌剂

    公开(公告)号：US06387906B1

    公开(公告)日：2002-05-14

    申请号：US09462588

    申请日：2000-01-07

    申请人： Lieven Meerpoel ,  Jan Heeres ,  Frank Christopher Odds ,  Hugo Florent Adolf Vanden Bossche ,  Louis Jozef Elisabeth Van der Veken

    发明人： Lieven Meerpoel ,  Jan Heeres ,  Frank Christopher Odds ,  Hugo Florent Adolf Vanden Bossche ,  Louis Jozef Elisabeth Van der Veken

    IPC分类号： C07D40514

    CPC分类号： C07D249/08 ,  A61K31/496 ,  A61K31/506 ,  A61K31/53 ,  C07D231/12 ,  C07D233/56

    摘要： The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or 3; X is N or CH; each R1 independently is halo, nitro, cyano, amino, hydroxy, C1-4alkyl, C1-4alkyloxy or trifluoromethyl; R2 is hydrogen; C3-7alkenyl; C3-7alkynyl, aryl; C3-7cycloalkyl; optionally substituted C1-6alkyl R3 and R4 each independently are hydrogen, C1-6alkyl, C3-7cycloalkyl or aryl; or R3 and R4 taken together form a bivalent radical —R3—R4— of formula: wherein R5a, R5b, R5c, R5d each independently are hydrogen, C1-6alkyl or aryl; and aryl is optionally substituted phenyl; as antifungals; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及式N-氧化物形式的新型化合物，其药学上可接受的酸加成盐或其立体化学异构形式，其中n为0,1,2或3; X是N或CH;每个R 1独立地是卤素，硝基，氰基，氨基，羟基，C 1-4烷基，C 1-4烷氧基或三氟甲基; R2是氢; C3-7烯基; C 3-7炔基，芳基; C 3-7环烷基; 任选取代的C 1-6烷基R 3和R 4各自独立地为氢，C 1-6烷基，C 3-7环烷基或芳基; 或R 3和R 4一起形成下式的二价基团-R 3 -R 4 - 其中R 5a，R 5b，R 5c，R 5d各自独立地是氢，C 1-6烷基或芳基; 芳基是任选取代的苯基; 作为抗真菌剂; 其制剂，含有它们的组合物及其作为药物的用途。

    Water soluble azoles as broad-spectrum antifungals
    3.
    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。

    Amino acid ester containing azole antifungals
    6.
    发明授权
    Amino acid ester containing azole antifungals 有权
    氨基酸酯含唑类抗真菌剂

    公开(公告)号：US06512116B2

    公开(公告)日：2003-01-28

    申请号：US09848989

    申请日：2001-05-04

    申请人： Lieven Meerpoel ,  Jan Heeres ,  Robert Jozef Maria Hendrickx

    发明人： Lieven Meerpoel ,  Jan Heeres ,  Robert Jozef Maria Hendrickx

    IPC分类号： C07D40514

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

    摘要： The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts thereof and stereochemically isomeric forms thereof, wherein —A—B— forms a bivalent radical of formula —N═CH— (a), —CH═N— (b), —CH═CH— (c), L represents the acyl moiety of an amino acid; D is an azole containing 1,3- or 1,4-dioxolane derivative as broad-spectrum antifungals; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的新化合物，其药学上可接受的加成盐和其立体化学异构形式，其中-AB-形成式-N = CH-（a），-CH = N-（ b），-CH = CH-（c），L表示氨基酸的酰基部分; D是含有1,3-或1,4-二氧戊环衍生物作为广谱抗真菌剂的唑类; 其制剂，含有它们的组合物及其作为药物的用途。

    Amino acid ester containing azole antifungals
    7.
    发明授权
    Amino acid ester containing azole antifungals 有权
    氨基酸酯含唑类抗真菌剂

    公开(公告)号：US06262052B1

    公开(公告)日：2001-07-17

    申请号：US09355369

    申请日：1999-07-26

    申请人： Lieven Meerpoel ,  Jan Heeres ,  Robert Jozef Maria Hendrickx

    发明人： Lieven Meerpoel ,  Jan Heeres ,  Robert Jozef Maria Hendrickx

    IPC分类号： A61K31496

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

    摘要： The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts thereof and stereochemically isomeric forms thereof, wherein —A—B— forms a bivalent radical of formula —N═CH— (a), —CH═N— (b), —CH═CH— (c), L represents the acyl moiety of an amino acid; D is an azole containing 1,3- or 1,4-dioxolane derivative as broad-spectrum antifungals; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的新化合物，其药学上可接受的加成盐和其立体化学异构形式，其中-AB-形成式-N = CH-（a），-CH = N-（ b），-CH = CH-（c），L表示氨基酸的酰基部分; D是含有1,3-或1,4-二氧戊环衍生物作为广谱抗真菌剂的唑类; 其制剂，含有它们的组合物及其作为药物的用途。

    Amino acid ester containing azole antifungals
    8.
    发明授权
    Amino acid ester containing azole antifungals 有权
    氨基酸酯含唑类抗真菌剂

    公开(公告)号：US06703506B2

    公开(公告)日：2004-03-09

    申请号：US10298038

    申请日：2002-11-15

    申请人： Lieven Meerpoel ,  Jan Heeres ,  Robert Jozef Maria Hendrickx

    发明人： Lieven Meerpoel ,  Jan Heeres ,  Robert Jozef Maria Hendrickx

    IPC分类号： C07D40514

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

    摘要： The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts thereof and stereochemically isomeric forms thereof, wherein —A—B— forms a bivalent radical of formula —N═CH— (a), —CH═N— (b), —CH═CH— (c), L represents the acyl moiety of an amino acid; D is an azole containing 1,3- or 1,4-dioxolane derivative as broad-spectrum antifungals; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的新化合物，其药学上可接受的加成盐和其立体化学异构形式，其中-AB-形成式-N = CH-（a），-CH = N-（ b），-CH = CH-（c），L表示氨基酸的酰基部分; D是含有1,3-或1,4-二氧戊环衍生物作为广谱抗真菌剂的唑类; 其制剂，含有它们的组合物及其作为药物的用途。