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    • 61. 发明授权
      US07276500B2 Substituted amides, their preparation and use 失效
    • Substituted amides, their preparation and use
    • US07276500B2
    • 2007-10-02
    • US10690400
    • 2003-10-20
    • Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
    • Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
    • A61K31/5377 , A61K31/496 , A61K31/4439 , A61K31/444 , A61K31/44 , C07D213/82
    • C07D213/82 , A61K31/195 , A61K31/5375 , C07C229/38 , C07C237/22 , C07C237/32 , C07C2601/14 , C07D295/155
    • An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine [sic], morpholine [sic], piperidine [sic], —NR5R6 and  and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl [sic], pyridyl [sic], pyrimidyl [sic] and pyridazyl [sic], it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH═CH—, —C≡C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by by [sic] a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, —NHSO2-C1-C4-alkyl and —SO2—C1-C4-alkyl; and Y is phenyl [sic], pyridine, pyrimidine and pyrazine and R4 is hydrogen, COOR9 and CO-Z in which Z is NR10R11 and R9 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R10 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which itself may also be substituted by one or two R12 radicals, and R11 is hydrogen, C1-C6-alkyl, branched or unbranched, which may also be and [sic] substituted by a phenyl ring which may also carry an R9 radical, and R12 can be hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, J, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, —NHCO—C1-C4-alkyl, —NHCO-phenyl, —NHSO2—C1-C4-alkyl, NHSO2-phenyl, —SO2—C1-C4-alkyl and —SO2-phenyl, R13 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R14 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and n is a number 0, 1 or 2, and m, q are, independently of one another, a number 0, 1, 2, 3 or 4.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 62. 发明授权
      US06436925B1 Substituted benzamides, their production and their use as cysteine protease inhibitors 失效
    • Substituted benzamides, their production and their use as cysteine protease inhibitors
    • US06436925B1
    • 2002-08-20
    • US09647673
    • 2000-10-03
    • Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
    • Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
    • C07D29508
    • C07D295/096 , C07C233/78 , C07C235/42 , C07C237/34 , C07C311/21 , C07D213/56
    • Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be aromatic rings and heteroaromatic rings such as naphthyl, quinolyl, quinoxyl, benzimidazolyl, benzothienyl, quinazolyl, phenyl, thienyl, imidazolyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by by [sic] R9 and up to 2 R8 radicals, and B a bond, —(CH2)m—, —(CH2)m—O—(CH2)o—, —(CH2)o—S—(CH2)m—, —(CH2)o—SO—(CH2)m—, —(CH2)o—SO2—(CH2)m—, —CH═CH—, —C≡C—, —CO—CH═CH—, —(CH2)o—CO—(CH2)m—, —(CH2)m—NHCO—(CH2)o—, —(CH2)m—CONH—(CH2)o—, —(CH2)m—NHSO2—(CH2)o—, —NH—CO—CH═CH—, —(CH2)m—SO2NH—(CH2)o—, A—B together also R5 hydrogen and C1-C4-alkyl and R6 is hydrogen, phenyl, naphthyl, C1-C6-alkyl, linear or branched, it being possible for a C atom in the chain to be substituted by a phenyl ring which itself may also be substituted by one or two R4 radicals, and R8 can be hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, —NHCO—C1-C4-alkyl, phenyl, NHCO-phenyl, —NHSO2—C1-C4-alkyl, —NHSO2-phenyl, —SO2—C1-C4-alkyl, pyridine [sic] and SO2-phenyl, R9 hydrogen, —CHR14—(CH2)p—R12 where R12 pyrrolidine [sic], morpholine [sic], piperidine [sic], hexahydroazepine [sic], homopiperazine [sic],  and R10 [lacuna] C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring which is in turn substituted by by [sic] a maximum of two R11 radicals, where R11 is hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, —NHSO2—C1-C4-alkyl and —SO2—C1-C4-alkyl; and R13 is hydrogen and C1-C6-alkyl, branched or unbranched, and n,p is [sic], independently of one another, a number 0, 1 or 2, and m,o is [sic], independently of one another, a number 0, 1, 2, 3 or 4.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 67. 发明授权
      US5852017A 2,3(1H,4H)-quinoxalinediones 失效
    • 2,3(1H,4H)-quinoxalinediones
    • 2,3（1H，4H） - 喹喔啉
    • US5852017A
    • 1998-12-22
    • US880507
    • 1997-06-23
    • Wilfried Lubisch , Berthold Behl , Hans Peter Hofmann
    • Wilfried Lubisch , Berthold Behl , Hans Peter Hofmann
    • A61K31/495 , A61K31/498 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , C07D241/44 , C07D241/52 , C07D401/04 , C07D403/04 , C07D487/12 , C07D487/14
    • C07D403/04 , C07D241/52 , C07D487/14
    • 2,3(1H,4H)-quinoxalinediones of the formula I ##STR1## where R.sup.1 is hydrogen, an aliphatic radical which has up to 12 carbons and can be substituted by one of the following: phenyl, cyclopentyl, cyclohexyl or --CO--R.sup.3, --CO--O--R.sup.3 or --CO--NH--R.sup.3, where R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl, benzyl or 1-phenylethyl, a cycloaliphatic radical with up to 12 carbons or phenyl, where the cyclic groups in R.sup.1 can have up to three of the following substituents: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, halogen, nitro, cyano, --CO--O--R.sup.3 and --CO--NH--R.sup.3 ; R.sup.2 is 1-pyrrolyl which can have up to two of the following substituents: C.sub.1 -C.sub.4 -alkyl, phenyl, phenylsulfonyl, nitro, cyano and --CO--O--R.sup.3, --CO--NH--R.sup.3, --CH.sub.2 --O--R.sup.3, --O--R.sup.3 and --CH.dbd.NO--R.sup.3 R radicals are identical or different and are the following: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and --CO--O--R.sup.3 and --CO--NH--R.sup.3 as well as a fused-on benzene ring; n is 0-3, and 2,3(1H,4H)-quinoxalinediones I' ##STR2## where R.sup.1 has the stated meanings, are suitable as drugs in the treatment of neurodegenerative disorders and neurotoxic disturbances of the central nervous system.
    • 式I的2,3（1H，4H） - 喹喔啉，其中R 1是氢，具有至多12个碳原子并且可以被下列之一取代的脂族基团：苯基，环戊基，环己基或-CO -R 3，-CO-O-R 3或-CO-NH-R 3，其中R 3是氢，C 1 -C 4烷基，苯基，苄基或1-苯基乙基，具有至多12个碳的脂环族基团或苯基， R1中的基团可以具有多达三个以下取代基：C 1 -C 4 - 烷基，C 1 -C 4 - 卤代烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 卤代烷氧基，卤素，硝基，氰基，-CO-O-R 3和 -CO-NH-R3; R2是可以具有至多两个以下取代基的1-吡咯基：C 1 -C 4烷基，苯基，苯基磺酰基，硝基，氰基和-CO-O-R 3，-CO-NH-R 3，-CH 2 -O-R 3 ，-O-R3和-CH = NO-R3R基团是相同或不同的，如下：C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，三氟甲基，三氯甲基，三氟甲氧基，三氯甲氧基，氟，氯，溴，碘 ，硝基，氰基和-CO-O-R 3和-CO-NH-R 3以及稠合的苯环; n为0-3，并且具有所述含义的2,3（1H，4H） - 喹喔啉酮I'，其中R 1具有所述含义，适合作为治疗神经变性疾病和中枢神经系统的神经毒性紊乱的药物。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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