抗真菌剤
    43.
    发明申请
    抗真菌剤 审中-公开
    抗真菌药物

    公开(公告)号:WO2013047530A1

    公开(公告)日:2013-04-04

    申请号:PCT/JP2012/074580

    申请日:2012-09-25

    摘要:  ルリコナゾールおよび/またはラノコナゾールあるいはその薬学的に許容される塩を有効成分として含む、スキタリジウム属真菌( Scytalidium dimidiatum 、 Scytalidium hyalinum 等)に対する抗真菌剤、好ましくは、スキタリジウム属真菌を原因菌とする表在性真菌症用の抗真菌剤。

    摘要翻译: 一种针对属于Scytalidium的真菌的抗真菌剂(例如,Scytalidium dimidiatum,Scytalidium hyalinum),优选用于由属于Scytalidium的真菌引起的表面真菌病的抗真菌剂,其包含卢立康唑和/或兰考康唑或药物 可接受的盐作为活性成分。

    THIOLACTONE ANTIBIOTICS
    48.
    发明申请
    THIOLACTONE ANTIBIOTICS 审中-公开
    噻吗酮抗生素

    公开(公告)号:WO2012135027A2

    公开(公告)日:2012-10-04

    申请号:PCT/US2012/030354

    申请日:2012-03-23

    摘要: This invention provides a compound having the structure (I) wherein R 1 is H, (II) or (III), wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is (IV), (V), (VI), (VII), (VIII), or (IX), wherein m is an integer from 0 to 8; R 3 is an amino, alkyl, aryl, heteroaryl, diol, piperazine, morpholine, piperidine, triazole, azide or biphenyl, each with or without substitution, branched or unbranched, or (X); and R 4 is alkyl, aryl, or heteroaryl, each with or without substitution, branched or unbranched, R 2 is H, CH 3 , or alkyl, aryl, heteroaryl, pyrrole, diazole, or triazole, each with or without substitution, branched or unbranched, or (XI), wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is (IV), (V), (VI), (VII), or (VIII); and R 6 is azide, methoxy, trifluoromethyl, biphenyl, substituted phenyl, substituted triazole, or alkyl, aryl or heteroaryl, with or without substitution, branched or unbranched, when R 1 is H then R 2 is other than H or CH 3 , and when R 2 is H or CH 3 then R 1 is other than H, or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明提供具有式(I)的化合物,其中R 1为H,(II)或(III),其中n和q独立地为0至8的整数; (IV),(V),(VI),(VII),(VIII)或(IX)所示的化合物,其中m为0至8的整数; 或者(X); R 3是具有或不具有取代基,支链或非支链的氨基,烷基,芳基,杂芳基,二醇,哌嗪,吗啉,哌啶,三唑,叠氮化物或联苯。 R 4是烷基,芳基或杂芳基,各自具有或不具有取代,支链或非支链,R2是H,CH3或烷基,芳基,杂芳基,吡咯,二唑或三唑,各自具有或不具有取代,支链或非支链, 或(XI),其中n和q独立地为0至8的整数; (IV),(V),(VI),(VII)或(VIII)存在的情况; 并且当R 1为H时,R 6为叠氮基,甲氧基,三氟甲基,联苯基,取代的苯基,取代的三唑或烷基,芳基或杂芳基,具有或不具有取代,分支或未分支,则R2不是H或CH3, H或CH 3,然后R 1不是H,或其药学上可接受的盐。

    LIPOIC ACID AND NITROXIDE DERIVATIVES AND USES THEREOF
    49.
    发明申请
    LIPOIC ACID AND NITROXIDE DERIVATIVES AND USES THEREOF 审中-公开
    氯酸和硝酸衍生物及其用途

    公开(公告)号:WO2011141909A3

    公开(公告)日:2012-07-19

    申请号:PCT/IL2011000370

    申请日:2011-05-09

    摘要: The present invention provides bifunctional compounds comprising a poly(ADP-ribose) polymerase (PARP) inhibitor moiety and a reactive oxygen species (ROS) scavenger moiety, more particularly, a lipoic acid or cyclic nitroxide derivative, covalently attached either directly or via a linker, as well as pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions of the invention are useful for prevention, treatment, or management of diseases, disorders and conditions associated with elevated PARP activity or expression.

    摘要翻译: 本发明提供了包含聚(ADP-核糖)聚合酶(PARP)抑制剂部分和活性氧(ROS)清除剂部分,更特别是硫辛酸或环状氮氧自由基衍生物的双官能化合物,其直接或通过连接体共价连接 ,以及包含它们的药物组合物。 本发明的化合物和药物组合物可用于预防,治疗或控制与升高的PARP活性或表达相关的疾病,病症和病况。