GESELLSCHAFT FÜR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF)
    92.
    发明申请
    GESELLSCHAFT FÜR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) 审中-公开
    GESELLSCHAFTFÜR生物技术公司FORSCHUNG MBH(GBF)

    公开(公告)号:WO2004007476A1

    公开(公告)日:2004-01-22

    申请号:PCT/EP2003/006066

    申请日:2003-06-10

    Inventor: HOEFLE, Gerhard

    Abstract: The invention relates to 5-thiapethilones and 15-disubstituted epothilones according to formula I (I) with the following meanings: X= >C = O or >S = O R 1 = C 1-6 alkyl or C 2-6 alkenyl R 2 = H or C 1-6 alkyl Y - Z = >C=C C- O -C 3 = H, C 1-6 alkyl or C 2-6 alkenyl R 4 = bicycloaryl, bicycloheteroaryl or -C(R 5 ) = CH-R 6 , where R 5 = H or CH 3 and R 6 = aryl or heteroaryl X not being >C=O if R 3 = H.

    Abstract translation: 本发明涉及式I(I)的5-硫代二甲苯酮和15-二取代的埃博霉素,其含义如下:X => C = O或> S = OR 1 = C 1-6烷基或C 2-6烯基R' 2> = H或C 1-6烷基Y -Z = C = C OR OR CO(环氧化物环)R 3 = H,C 1-6烷基或C 2-6烯基R 4 =双环芳基,双环杂芳基 或-C(R 5)= CH-R 6,其中R 5 = H或CH 3且R 6 =芳基或杂芳基X,如果R 3 = H,则不为> C = O。

    PROCESS FOR PREPARING THIAZOLE DERIVATIVE AND THE INTERMEDIATE COMPOUNDS FOR PREPARING THE SAME
    94.
    发明申请
    PROCESS FOR PREPARING THIAZOLE DERIVATIVE AND THE INTERMEDIATE COMPOUNDS FOR PREPARING THE SAME 审中-公开
    制备噻唑衍生物的方法和用于制备噻唑衍生物的中间体化合物

    公开(公告)号:WO2003106442A1

    公开(公告)日:2003-12-24

    申请号:PCT/KR2003/000877

    申请日:2003-05-01

    CPC classification number: C07C323/20 C07D277/26 Y02P20/55

    Abstract: The present invention provides a process for preparing thiazole derivatives of formula (XI), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPARδ), and also provides processes for compounds of formula (VI), (VII), (VIII) and (IX), intermediate compounds for preparation of the above compounds of formula (XI).

    Abstract translation: 本发明提供一种制备活化人过氧化物酶体增殖剂活化受体(hPPARδ)的δ亚型的式(XI)的噻唑衍生物的方法,还提供了式(VI),(VII),(VII), VIII)和(IX),用于制备上述式(XI)化合物的中间体化合物。

    THIAZOLE OR OXAZOLE DERIVATIVES
    100.
    发明申请
    THIAZOLE OR OXAZOLE DERIVATIVES 审中-公开
    噻唑或氧唑衍生物

    公开(公告)号:WO02028844A1

    公开(公告)日:2002-04-11

    申请号:PCT/JP2001/008507

    申请日:2001-09-28

    Abstract: Compounds of the general formula (I), their optical isomers or prodrugs, pharmaceutically acceptable salts of the compounds, the isomers, or the prodrugs, or solvates of the same; and metalloprotease inhibitors containing the compounds, the optical isomers, the prodrugs, the salts, or the solvates: (I) wherein R is hydroxyl or the like; R is optionally substituted lower alkyl or the like; R is hydrogen or the like; R is optionally substituted arylene or the like; R is a group of formula (II) or (III): (III) and R is optionally substituted aryl or the like.

    Abstract translation: 通式(I)的化合物,它们的光学异构体或前体药物,化合物的药学上可接受的盐,异构体或前药或其溶剂合物; 和含有这些化合物的金属蛋白酶抑制剂,光学异构体,前体药物,盐或溶剂合物:(I)其中R 1是羟基等; R 2是任选取代的低级烷基等; R 3是氢等; R 4是任选取代的亚芳基等; R 5是式(II)或(III)的基团:(III),R 6是任选取代的芳基等。

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