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    Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use in medicaments
    2.
    发明授权
    Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use in medicaments 有权
    取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，它们的制备及其在药物中的用途

    公开(公告)号：US06596742B1

    公开(公告)日：2003-07-22

    申请号：US09655373

    申请日：2000-09-05

    申请人： Stefan Petry ,  Karl Schoenafinger ,  Guenter Mueller ,  Karl-Heinz Baringhaus

    发明人： Stefan Petry ,  Karl Schoenafinger ,  Guenter Mueller ,  Karl-Heinz Baringhaus

    IPC分类号： A61K314245

    CPC分类号： C07D271/113

    摘要： Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 in any optically isomeric form, and their physiologically acceptable salts, where R1 is C1-C6-alkyl, C3-C9-cycloalkyl, both of which may be unsubstituted or substituted, and R2 and R3 independently of one another are hydrogen, C6-C10-aryl, C3-C8-cycloalkyl, C6-C10-aryloxymethyl, O-benzyl, O—C6-C10-aryl, O—C3-C8-cycloalkyl, O—C1-C6-alkyl, SO2—NH—C1-C6-alkyl, SO2—NH-(2,2,6,6-tetramethylpiperidin-4-yl), SO2—NH—C3-C8-cycloalkyl, SO2—N(C1-C6-alkyl)2 or COX, where X is O—C1-C6-alkyl, NH—C1-C6-alkyl, NH—C3-C8-cycloalkyl or N(C1-C6-alkyl)2, with the proviso that the substitutents R2 and R3 may in some instances be unsubstituted or substituted and are not both simultaneously hydrogen. A process for their preparation, and their inhibitory effect on the hormone-sensitive lipase, HSL.

    摘要翻译： 以任何光学异构体形式的取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮及其生理上可接受的盐，其中R 1是C 1 -C 6 - 烷基，C 3 -C 9 - 环烷基， 两者可以是未取代的或取代的，R 2和R 3彼此独立地是氢，C 6 -C 10 - 芳基，C 3 -C 8 - 环烷基，C 6 -C 10 - 芳氧基甲基，O-苄基，O-C 6 -C 10 - 芳基， O-C 3 -C 8 - 环烷基，O-C 1 -C 6烷基，SO 2 -NH-C 1 -C 6烷基，SO 2 -NH-（2,2,6,6-四甲基哌啶-4-基），SO 2 -NH- C 3 -C 8 - 环烷基，SO 2 -N（C 1 -C 6 - 烷基）2或COX，其中X是O-C 1 -C 6烷基，NH-C 1 -C 6烷基，NH-C 3 -C 8环烷基或N -C 1-6 - 烷基）2，条件是取代基R2和R3在一些情况下可以是未取代的或取代的，并且不同时是氢。 其制备方法及其对激素敏感性脂肪酶HSL的抑制作用。

    Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use as pharmaceuticals
    3.
    发明授权
    Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use as pharmaceuticals 有权
    取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，它们的制备及其作为药物的用途

    公开(公告)号：US06369088B2

    公开(公告)日：2002-04-09

    申请号：US09799082

    申请日：2001-03-06

    申请人： Karl Schoenafinger ,  Stefan Petry ,  Guenter Mueller ,  Karl-Heinz Baringhaus

    发明人： Karl Schoenafinger ,  Stefan Petry ,  Guenter Mueller ,  Karl-Heinz Baringhaus

    IPC分类号： C07D271113

    CPC分类号： C07D271/113 ,  C07D413/10 ,  C07D413/12

    摘要： Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 are described, in which R1 is substituted C1-C6-alkyl and C3-C9-cycloalkyl, R2, R3, R4 and R5 are hydrogen, halogen, nitro, C1-C4-alkyl, C1-C9-alkyloxy, substituted C6-C10-aryl-C1-C4-alkyloxy, C6-C10-aryloxy, C6-C10-aryl, C3-C8-cycloalkyl or O—C3—C8-cycloalkyl, or 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, with the proviso that R2, R3, R4 and R5 are not simultaneously hydrogen, and at least one of the radicals R2, R3, R4 or R5 is the radical 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, wherein R6=hydrogen, C1-C4-alkyl or substituted C6-C10-aryl-C1-C4-alkyl, A=a single bond, COn, SOn or CONH, n=1 or 2, R7=hydrogen, substituted C1-C18-alkyl, C2-C18-alkenyl, C6-C10-aryl-C1-C4-alkyl, C5-C8-cycloalkyl-C1-C4-alkyl, C5-C8-cycloalkyl, C6-C10-aryl-C2-C6-alkenyl, C6-C10-aryl, biphenylyl, biphenylyl-C1-C4-alkyl, indanyl, or the group Het-(CH2)r—, wherein r=0, 1, 2 or 3 and Het=a saturated or unsaturated 5-7-membered heterocycle, which may be optionally benzo-fused and optionally substituted, and proceses for their preparation. The compounds of formula 1 show an inhibitory effect on hormone-sensitive lipase, HSL.

    摘要翻译： 描述了式1的取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，其中R 1是取代的C 1 -C 6 - 烷基和C 3 -C 9 - 环烷基，R 2，R 3，R 4和 R 5是氢，卤素，硝基，C 1 -C 4 - 烷基，C 1 -C 9 - 烷氧基，取代的C 6 -C 10 - 芳基-C 1 -C 4 - 烷氧基，C 6 -C 10 - 芳氧基，C 6 -C 10 - 芳基，C 3 -C 8 - 或O-C 3 -C 8 - 环烷基或2-氧代吡咯烷-1-基，2,5-二甲基吡咯-1-基或NR6-A-R7，条件是R2，R3，R4和R5不同时为氢， 并且基团R 2，R 3，R 4或R 5中的至少一个是基团2-氧代吡咯烷-1-基，2,5-二甲基吡咯-1-基或NR6-A-R7，其中R6 =氢，C1-C4- 烷基或取代的C 6 -C 10 - 芳基-C 1 -C 4烷基，A =单键，COn，SO n或CONH，n = 1或2，R 7 =氢，取代的C 1 -C 18烷基，C 2 -C 18 - 烯基， C 6 -C 10 - 芳基-C 1 -C 4烷基，C 5 -C 8 - 环烷基-C 1 -C 4烷基，C 5 -C 8 - 环烷基，C 6 -C 10 - 芳基-C 2 -C 6 - 烯基，C 6 -C 10 - 芳基，联苯基， 联苯基-C 1 -C 4烷基，二氢化茚基或Het-（CH 3）