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公开(公告)号:BG104855A
公开(公告)日:2001-05-31
申请号:BG10485500
申请日:2000-10-13
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: A61K31/196 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/47 , A61K31/517 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P43/00 , C07C233/76 , C07C237/22 , C07C311/21 , C07D213/56 , C07D215/36 , C07D239/70 , C07D239/96 , C07C237/52 , C07C235/82 , A61K31/195 , A61K31/44 , A61K31/505 , A61K31/19
Abstract: The invention relates to amides with the general formula and to their tautomeric isomer forms, possible enantiomeric and diastereomeric forms and possible physiologically compatible salts. They are inhibitors of enzymes, especially cysteine proteases such as calpains dependent on cysteineprotease, and its isoenzyme and cathepsin, such as B and L. In the formula `wherein R1 is C1-C6 alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, whereby the rings can still be substituted up to 2 substituentsR4; R2 is -(CH2)m-R8, where R8 is phenyl, cyclohexyl or indolyl and m is 1 to 6; X is a bond, -CH2-, -CH2CH2, -CH2CH2-, -CH=CH-, -C=C-, -CONH-,-SO2NH-; and R1-X together can also be formula wherein R3 means hydrogen and CO-NR6R7, R6 meaning hydrogen, C1-C6 alkyl with branched or unbranched chain; R4 means hydrogen, C1-C4 alkyl with branched or unbranched chain, and -O-C1-C4 alkyl; R5 is hydrogen, C1-C4 alkyl with a branched or unbranched chain and -O-C1-C4 alkyl, and n has the value of 0,1 or 2. 17 claims
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公开(公告)号:BG104831A
公开(公告)日:2001-05-31
申请号:BG10483100
申请日:2000-10-10
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: A61K31/4164 , A61K31/426 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/4709 , A61K31/4725 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P9/04 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P27/12 , A61P43/00 , C07D213/81 , C07D213/82 , C07D233/90 , C07D239/28 , C07D239/30 , C07D239/42 , C07D241/28 , C07D277/20 , C07D277/44 , C07D277/56 , C07D401/04 , C07D401/12 , C07D413/12 , A61K31/44
Abstract: The invention relates to amides of the general formula and their tautomeric and isomeric forms, their possible enantiomers and diastereometric forms and possible physiologically compatible salts, where the variables have the meanings given in the description. The invention also relates to their production and their use as calpain inhibitors. 19 claims
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公开(公告)号:SK15062000A3
公开(公告)日:2001-05-10
申请号:SK15062000
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS-JORG , KNOPP MONIKA
IPC: C07D295/14 , A61K31/18 , A61K31/357 , A61K31/36 , A61K31/40 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/4453 , A61K31/453 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/5375 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C237/32 , C07C311/08 , C07C311/21 , C07D207/06 , C07D207/36 , C07D211/14 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/48 , C07D213/56 , C07D213/71 , C07D213/76 , C07D215/06 , C07D215/36 , C07D215/40 , C07D217/04 , C07D239/28 , C07D295/13 , C07D295/155 , C07D317/54 , C07D317/58 , C07D401/12 , C07D403/04 , C07D498/04 , C07D295/12 , A61K31/50 , C07D215/24 , C07D213/70
Abstract: The invention relates to amides of the general formula (I), which are inhibitors of enzymes, especially cysteine proteases.
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公开(公告)号:TR200003056T2
公开(公告)日:2001-02-21
申请号:TR200003056
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: A61K31/4164 , A61K31/426 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/4709 , A61K31/4725 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P9/04 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P27/12 , A61P43/00 , C07D213/81 , C07D213/82 , C07D233/90 , C07D239/28 , C07D239/30 , C07D239/42 , C07D241/28 , C07D277/20 , C07D277/44 , C07D277/56 , C07D401/04 , C07D401/12 , C07D413/12 , A61K31/44
Abstract: Amides of the general formula Iand their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, their preparation and use as calpain inhibitors.
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公开(公告)号:TR200003004T2
公开(公告)日:2001-02-21
申请号:TR200003004
申请日:1999-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: C07D295/12 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/551 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P43/00 , C07D213/80 , C07D213/81 , C07D213/82 , C07D215/50 , C07D239/42 , C07D295/192 , C07D401/04 , C07D401/14 , C07D405/12 , C07D413/12
Abstract: Heterocyclically substituted amides of the general formula Iwherein the variables as defined in the specification are useful in pharmaceuticals for the treatment of diseases in which increased interleuken-1 levels occur.
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公开(公告)号:DE19934066A1
公开(公告)日:2001-01-25
申请号:DE19934066
申请日:1999-07-23
Applicant: BASF AG
Inventor: KNOPP MONIKA , KOSER STEFAN , SCHAEFER BERND
IPC: C07D277/20 , C07D277/56 , C07D277/12
Abstract: 2-Aminomethyl-4-cyanothiazole (I) and its salts are new. 2-Aminomethyl-4-cyanothiazole (I) and its salts of formula are new. n = 1 or 2; and X = Cl, Br, SO3CF3, HSO4 or 1/2 SO4. Independent claims are included for: (1) the preparation of (I); (2) the preparation of thiazolecarboxylic acid ester intermediates of formula (V); and (3) the new intermediate N-(tert. butoxycarbonyl)-2-aminomethyl-4-cyanothiazole of formula (VII). R1 = 1-10C alkyl or -(CH2)m-Ar; Ar = phenyl (optionally monosubstituted by 1-10C alkyl, 1-4C alkoxy or di-(1-4C alkyl)-amino); and m = 0-2.
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公开(公告)号:CZ20003843A3
公开(公告)日:2001-01-17
申请号:CZ20003843
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: A61K31/197 , A61K31/44 , A61K31/505 , A61P9/10 , A61P19/08 , A61P35/04 , C07C233/76 , C07C235/82 , C07C237/52 , C07C311/21 , C07D213/56 , C07D215/36 , C07D239/96
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公开(公告)号:ID26403A
公开(公告)日:2000-12-21
申请号:ID20002132
申请日:1999-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS-JORG , KNOPP MONIKA
IPC: C07D295/08 , A61K31/16 , A61K31/166 , A61K31/27 , A61K31/395 , A61K31/40 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C229/38 , C07C237/20 , C07C237/22 , C07C237/32 , C07C237/36 , C07D209/14 , C07D213/82 , C07D233/64 , C07D237/32 , C07D237/36 , C07D295/14 , C07D295/155 , C07D237/00
Abstract: 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, morpholine, piperidine, —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, pyridyl, pyrimidyl and pyridazyl, 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 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, 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 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.
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公开(公告)号:BR9909819A
公开(公告)日:2000-12-19
申请号:BR9909819
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JURG , KNOPP MONIKA
IPC: C07D295/14 , A61K31/18 , A61K31/357 , A61K31/36 , A61K31/40 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/4453 , A61K31/453 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/5375 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C237/32 , C07C311/08 , C07C311/21 , C07D207/06 , C07D207/36 , C07D211/14 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/48 , C07D213/56 , C07D213/71 , C07D213/76 , C07D215/06 , C07D215/36 , C07D215/40 , C07D217/04 , C07D239/28 , C07D295/13 , C07D295/155 , C07D317/54 , C07D317/58 , C07D401/12 , C07D403/04 , C07D498/04 , C07D295/12 , A61K31/50 , C07D213/70
Abstract: The invention relates to amides of the general formula (I), which are inhibitors of enzymes, especially cysteine proteases.
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公开(公告)号:BR9909772A
公开(公告)日:2000-12-19
申请号:BR9909772
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JURG , KNOPP MONIKA
IPC: A61K31/4164 , A61K31/426 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/4709 , A61K31/4725 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P9/04 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P27/12 , A61P43/00 , C07D213/81 , C07D213/82 , C07D233/90 , C07D239/28 , C07D239/30 , C07D239/42 , C07D241/28 , C07D277/20 , C07D277/44 , C07D277/56 , C07D401/04 , C07D401/12 , C07D413/12 , A61K31/44
Abstract: Amides of the general formula Iand their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, their preparation and use as calpain inhibitors.
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