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    • 4. 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
    • 5. 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
    • 6. 发明授权
      US06448254B1 Substituted amides, their production and their use 失效
    • Substituted amides, their production and their use
    • 取代酰胺，其生产和使用
    • US06448254B1
    • 2002-09-10
    • US09647677
    • 2000-10-03
    • Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
    • Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
    • C07C31121
    • C07D213/56 , C07C311/21 , C07D215/36 , C07D239/70 , C07D239/96
    • Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the following meanings: R1 [sic] can be C1-C6-alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, where the rings can additionally be substituted by up to 2 radicals R4 [sic], and R2 [sic] is —(CH2)m—R8 [sic], where R8 [sic] can be phenyl, cyclohexyl- or indolyl and m=1 to 6, and X is a bond, —CH2—, —CH2CH2—, —CH═CH—, —C≡C—, —CONH—, —SO2NH— [sic], and and [sic] R1—X [sic] together are also  and R3 [sic] is hydrogen and CO—NR6R7 [sic], R4 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched and unbranched, and —O—C1-C4-alkyl [sic]; R5 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched or unbranched, and —O—C1-C4-alkyl [sic]; R6 [sic] is hydrogen, C1-C6-alkyl, which is branched and unbranched, and R7 [sic] is hydrogen, C1-C6-alkyl, which is branched or unbranched, and n is is [sic] a number 0, 1 or 2.
    • 通式I的酰胺及其互变异构体和异构体形式，可能的对映异构体和非对映体形式，以及可能的生理上可耐受的盐，其中变量具有以下含义：R 1 [C 1-6]可以是C 1 -C 6 - 烷基，苯基，萘基 ，喹啉基，吡啶基，嘧啶基，哒嗪基，喹唑啉基和喹喔啉基，其中环可以另外被至多2个基团R 4 [sic]取代，并且R 2是 - （CH 2）m -R 8 [sic]，其中R 8 [ ]可以是苯基，环己基或吲哚基并且m = 1至6，X是键，-CH 2 - ， - CH 2 CH 2 - ， - CH = CH - ， - C≡C - ， - CONH - ， - SO 2 NH- ]，并且R 1-X [sic]一起也是且R 3 [sic]是氢且CO-NR 6 R 7 [sic]，R 4 [sic]是氢，C 1 -C 4 - 烷基[ 非支链和-O-C 1 -C 4 - 烷基[sic]; R 5 [sic]是氢，C 1 -C 4 - 烷基[sic]，其是支链或非支链的，和-O-C 1 -C 4 - 烷基[ R 6是氢，C 1 -C 6 - 烷基，其是支链和非支链的，并且R 7 [sic]是氢，C 1 -C 6 - 烷基，其是支链或 不分支，而且是数字0，1或2。
    • 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
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