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    • 4. 发明授权
    • Substituted-pent-4-ynoic acids
    • 取代的戊-4-炔酸
    • US6037367A
    • 2000-03-14
    • US716359
    • 1998-09-14
    • Siegfried B. Christensen, IVJoseph M. KarpinskiJames S. Frazee
    • Siegfried B. Christensen, IVJoseph M. KarpinskiJames S. Frazee
    • C07C47/277C07C49/255C07C59/72C07C69/734C07C69/736C07D233/54C07D239/42C07D257/04C07D271/06C07D271/10C07D277/44C07D285/12A61K31/19
    • C07D233/64C07C47/277C07C49/255C07C59/72C07C69/734C07C69/736C07D239/42C07D257/04C07D271/06C07D271/10C07D277/44C07D285/12C07C2101/08
    • Compounds of formula (I) wherein: R.sub.1 is --(CR.sub.4 R.sub.5).sub.n C(O)O(CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n C(O)NR.sub.4 (CR.sub.4 R.sub.5).sub.m R.sub.6, (CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6, or --(CR.sub.4 R.sub.5).sub.r R.sub.6 : W is alkynyl or 2 carbon atoms; R.sub.3 is H or R.sub.7 ; Z is C(O)R.sub.13, (CH.sub.2).sub.0-1 C(O)OR.sub.13, (CH.sub.2).sub.0-1 C(O)NR.sub.10 R.sub.13, (CH.sub.2).sub.0-1 C(R.sub.8 R.sub.8)OR.sub.8, --NHC(O)R.sub.7, (CH.sub.2).sub.0-1 NR.sub.10 R.sub.13, NH[C(O)C(O)OR.sub.8 ], CH.sub.2 NH[C(O)CNR.sub.10 R.sub.13 ], CH.sub.2 S(O).sub.q R.sub.7, CH[S(O).sub.q R.sub.7 ].sub.2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R.sub.7 is --(CR.sub.4 R.sub.5).sub.q R.sub.11 or C.sub.1-6 alkyl wherein the R.sub.11 or C.sub.1-6 alkyl group is unsubstituted or substituted one or more times by methyl or ethyl unsubstituted or substituted by 1-3 fluorines, --NR.sub.8 R.sub.10, --CO.sub.2 R.sub.8, --O(CH.sub.2q R.sub.8, --NR.sub.8 C(O)R.sub.8 or R.sub.12 ; or the pharmaceutically acceptable salts thereof. ##STR1##
    • PCT No.PCT / US96 / 11613 Sec。 371日期:1998年9月14日 102(e)1998年9月14日PCT PCT 1996年7月12日PCT公布。 出版物WO97 / 03945 (CR4R5)n(O)O(CR4R5)mR6, - (CR4R5)nC(O)NR4(CR4R5)mR6,(CR4R5)nO(CR4R5)的化合物,其中R1为 - (CR4R5)nC mR 6或 - (CR 4 R 5)r R 6:W是炔基或2个碳原子; R3是H或R7; Z是C(O)R 13,(CH 2)0-1 C(O)OR 13,(CH 2)0-1 C(O)NR 10 R 13,(CH 2)0-1C(R 8 R 8)OR 8,-NHC(O) )0-1NR10R13,NH [C(O)C(O)OR 8],CH 2 NH [C(O)CNR 10 R 13],CH 2 S(O)q R 7,CH [S(O)q R 7] 2,二硫戊环,(四唑-5-基) 噻唑-2-基,[1,2,4]噻二唑-5-基,[1,3,4]恶二唑-2-基,咪唑-2-基,恶唑-2-基或(3 - 或5-恶二唑基[1,2,4]; R7是 - (CR4R5)qR11或C1-6烷基,其中R11或C1-6烷基是未取代的或被未取代的或被 1-3个氟,-NR8R10,-CO2R8,-O(CH2qR8,-NR8C(O)R8或R12);或其药学上可接受的盐。