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    SUBSTITUTED PHENYLPROPIONIC ACID DERIVATIVES
    129.
    发明公开
    SUBSTITUTED PHENYLPROPIONIC ACID DERIVATIVES 有权
    替代苯乙烯衍生物

    公开(公告)号：EP1285908A1

    公开(公告)日：2003-02-26

    申请号：EP01932262.7

    申请日：2001-05-25

    申请人： KYORIN PHARMACEUTICAL CO., LTD.

    发明人： MIYACHI, Hiroyuki ,  NOMURA, Masahiro ,  TAKAHASHI, Yukie ,  TANASE, Takahiro ,  MURAKAMI, Kouji ,  SUZUKI, Masahiro

    IPC分类号： C07C69/734 ,  C07C69/738 ,  C07C229/34 ,  C07C233/55 ,  C07C233/81 ,  C07C235/44 ,  C07C235/78 ,  A61K31/192 ,  A61P43/00 ,  A61P3/06 ,  A61P9/10

    CPC分类号： C07C59/68 ,  C07C69/734 ,  C07C69/738 ,  C07C229/34 ,  C07C233/51 ,  C07C233/55 ,  C07C233/87 ,  C07C235/34 ,  C07C235/38 ,  C07C235/52 ,  C07C251/48 ,  C07C323/56

    摘要： The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor α (PPARα) to activate and exhibit potent lipid-decreasing action, and processes for preparing them.
       It relates to substituted phenylpropionic acid derivatives represented by a general formula (1)
    [wherein R 1 denotes a lower alkyl group with carbon atoms of 1 to 4, lower alkoxy group with carbon atoms of 1 to 3, trifluoromethyl group, trifluoromethoxy group, phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents, R 2 denotes a hydrogen atom, lower alkyl group with carbon atoms of 1 to 4 or lower alkoxy group with carbon atoms of 1 to 3, R 3 denotes a lower alkoxy group with carbon atoms of 1 to 3, and the binding mode of A portion denotes -CH 2 CONH-, -NHCOCH 2 -, -CH 2 CH 2 CO-, -CH 2 CH 2 CH 2 -, -CH 2 CH 2 O-, -CONHCH 2 -, -CH 2 NHCH 2 -, -COCH 2 O-, -OCH 2 CO-, -COCH 2 NH- or -NHCH 2 CO-], their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.

    摘要翻译： 本发明提供新的取代的苯基丙酸衍生物，其与作为人过氧化物酶体增殖物激活受体α（PPARα）的配体的受体结合以活化并显示出有力的降脂作用，以及制备它们的方法。 它涉及由通式（1）表示的取代的苯基丙酸衍生物，其中R 1表示碳原子数为1〜4的低级烷基，碳原子数1〜3的低级烷氧基，三氟甲基， 三氟甲氧基，未取代或可具有取代基的苯基，未取代或可具有取代基的苯氧基或未取代或可具有取代基的苄氧基，R 2表示氢原子，碳原子数为1的低级烷基 至4或低级烷氧基，碳原子数为1〜3，R 3表示碳原子数1〜3的低级烷氧基，A部分的结合模式表示-CH 2 CONH - ， - NHCOCH 2 - ， - CH 2 CH 2 CO- ，-CH 2 CH 2 CH 2 - ， - CH 2 CH 2 O-，-CONHCH 2 - ， - CH 2 NHCH 2 - ， - COCH 2 O-，-OCH 2 CO - ， - COCH 2 NH-或-NHCH 2 CO-，其药学上可接受的盐及其水合物，及其制备方法。

    THIOL DERIVATIVE, METALLO-BETA-LACTAMASE INHIBITORS
    130.
    发明公开
    THIOL DERIVATIVE, METALLO-BETA-LACTAMASE INHIBITORS 审中-公开
    巯基衍生物的金属-β-内酰胺酶抑制剂

    公开(公告)号：EP1192128A1

    公开(公告)日：2002-04-03

    申请号：EP00941349.3

    申请日：2000-06-12

    申请人： Merck & Co., Inc.

    发明人： BALKOVEC, James, M. ,  GREENLEE, Mark, L. ,  HAMMOND, Milton, L. ,  HECK, James, V.

    IPC分类号： C07C315/00 ,  C07C53/00 ,  C07C59/147

    CPC分类号： C07D307/91 ,  C07C323/56 ,  C07C327/32 ,  C07D213/56 ,  C07D333/38

    摘要： Thiol derivative compounds, pharmaceutically acceptable salts, and biolabile esters thereof, useful for inhibiting metallo-β-lactamases, bacterial enzymes which confer resistance to clinically relevant ß-lactam antibiotics, characterized by general formula (I): wherein: R1 is selected from straight, branched, unsaturated or alicyclic alkyl, optionally substituted with from 1 to 3 R¿x? groups; and (CH2)nAr, where Ar is an aryl selected from the group consisting of phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl, dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where n is 0, 1, 2 or 3, and where Ar is optionally substituted with 1 to 3 Rx groups; R?2¿ is selected from hydrogen; and a group of formula (II): wherein: R3 is selected from hydrogen; straight, branched, unsaturated or alicyclic alkyl, optionally substituted with from 1 to 3 R¿x? groups; (CH2)nAr, where Ar is an aryl selected from phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where Ar is optionally substituted with 1 to 3 Rx groups, and where n is 0, 1, 2 or 3; and a group of formula (III): wherein: R?4¿ is selected from hydrogen; and straight or branched alkyl; R5 is selected from hydrogen; straight, branched, unsaturated or alicyclic alkyl, optionally substituted with 1 to 3 R¿x? groups, where the alkyl group is optionally interrupted by X, where X is selected from O, S, NH and N(COCH3); allyloxy and 9-fluorenylmethyloxy; and (CH2)nAr, where Ar is selected from phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl, dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where n is 0, 1, 2 or 3, and where Ar is optionally substituted with 1 to 3 Rx groups; and Rx is selected from OR, CN, C(O)NH2, C(O)NHR, C(O)N(R)2, OC(O)NH2, OC(O)R, CHO, SO2NH2, SOR, CF3, C(O)R, COOR, F, Cl, Br, I, OCH2Ph, NHR, N(R)2, NHCOR, NHCO2t-Bu, NHCO2allyl, NH2, and R, where R is hydrogen, C1 to C15 alkyl, or aryl. The invention is further directed to a pharmaceutical composition containing the compound, as well as a method for treating bacterial infections in animals or humans, wherein the composition can be administered in combination with a β-lactam antibiotic.