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92 条记录 (耗时 0.074 秒)

    Antifungal 4-substituted 5,6-dihydro-4h-pyrrolo[1,2-a][1,4] benzodiazepines
    52.
    发明授权
    Antifungal 4-substituted 5,6-dihydro-4h-pyrrolo[1,2-a][1,4] benzodiazepines 有权
    抗真菌剂4-取代的5,6-二氢-4H-吡咯并[1,2-a] [1,4]苯并二氮杂卓

    公开(公告)号：US07202240B2

    公开(公告)日：2007-04-10

    申请号：US10399596

    申请日：2001-10-17

    申请人： Terence Gilkerson ,  Roger John Nash ,  Jozel Frans Elisabetha Van Gestel ,  Lieven Meerpoel

    发明人： Terence Gilkerson ,  Roger John Nash ,  Jozel Frans Elisabetha Van Gestel ,  Lieven Meerpoel

    IPC分类号： A61K31/55 ,  A61P31/10 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/55 ,  A61K31/551

    摘要： The present invention concerns compounds for use as a medicine having the formula (I), the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 represents hydrogen, C1-6 alkyl, C1-4alkylthio, C1-4alkyloxy, or halo; R2 represents hydrogen or C1-6alkyl; R3 represents phenyl substituted with halo, cyano, C1-4alkyloxy, C1-4alkylthio, C1-6alkyl, haloC1-6alkyl; 2-thienyl; or 3-thienyl, R4 represents hydrogen; or R2 and R4 form an extra bond, which are active against dermatophytes, and their preparation; it further relates to compositions comprising them, as well as their use as a medicine.

    摘要翻译： 本发明涉及用作具有式（I）的药物，N-氧化物形式，其盐，季胺及其立体化学异构形式的化合物，其中R 1表示氢， C 1-4烷基，C 1-4烷基硫基，C 1-4烷基氧基或卤素; R 2表示氢或C 1-6烷基; R 3表示被卤素，氰基，C 1-4烷氧基，C 1-4烷基硫基，C 1-6烷基取代的苯基 烷基，卤代C 1-6烷基; 2-噻吩基; 或3-噻吩基，R 4表示氢; 或R 2和R 4形成对皮肤癣菌有活性的额外的结合，及其制备; 它还涉及包含它们的组合物以及它们作为药物的用途。

    Amino acid ester containing azole antifungals
    58.
    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。

    Antifungal ethers
    59.
    发明授权
    Antifungal ethers 有权
    抗真菌醚

    公开(公告)号：US06583136B1

    公开(公告)日：2003-06-24

    申请号：US09980560

    申请日：2002-02-04

    申请人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx

    发明人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx

    IPC分类号： A61K3155

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

    摘要： The present invention concerns compounds of formula the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein D represents a tetrahydrofuran or dioxolane ring substituted with aryl and azolmethyl; —A—B— represents an optionally substituted bivalent radical of formula —N═CH—, —CH═N—, —CH═CH—, —CH2—CH2; Alk represents C1-6alkanediyl; Y represents optionally substituted C1-6alkanediyl; R1 and R2 represent hydrogen, C1-6alkyl or arylC1-6alkyl; or R1 and R2 may be taken together to form an optionally substituted heterocyclic radical selected from morpholinyl, pyrrolidinyl, piperidinyl, homopiperidinyl, piperazinyl or phthalimid-1-yl; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; having broad-spectrum antifungal activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其盐，季胺和立体化学异构形式，其中D表示被芳基和唑甲取代的四氢呋喃或二氧戊环; -A-B-表示式-N = CH-，-CH = N - ， - CH = CH - ， - CH 2 -CH 2 - 的任选取代的二价基团; Alk表示C1-6烷二基; Y表示任选取代的C 1-6烷二基; R 1和R 2表示氢，C 1-6烷基或芳基C 1-6烷基; 或者R1和R2可以一起形成选自吗啉基，吡咯烷基，哌啶基，高哌啶基，哌嗪基或邻苯二甲酰亚胺-1-基的任选取代的杂环基; 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; 具有广谱抗真菌活性; 其制剂，含有它们的组合物及其作为药物的用途。