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    82.
    发明专利
    未知

    公开(公告)号：TR200200181T2

    公开(公告)日：2002-08-21

    申请号：TR200200181

    申请日：2000-07-11

    Applicant: BASF AG

    Inventor： KNOPP MONIKA ,  KOSER STEFAN ,  SCHAFER BERND

    IPC: C07D277/20 ,  C07D277/56

    Abstract: The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ibin whichn=1 or 2 andfor n=1, X is chloride, bromide, triflate and hydrogen sulfate andfor n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula IIis stirred with a cysteine ester of the formula III,in which R is branched or linear C1-10-alkyl orwhere n=0, 1 or 2 and R is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.

    METHOD FOR PRODUCING 4-CYANO-2-AMINOMETHYLTHIAZOL
    84.
    发明专利
    METHOD FOR PRODUCING 4-CYANO-2-AMINOMETHYLTHIAZOL 未知

    公开(公告)号：SK1062002A3

    公开(公告)日：2002-07-02

    申请号：SK1062002

    申请日：2000-07-11

    Applicant: BASF AG

    Inventor： KNOPP MONIKA ,  KOSER STEFAN ,  SCHAFER BERND

    IPC: C07D277/20 ,  C07D277/56

    Abstract: The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ibin whichn=1 or 2 andfor n=1, X is chloride, bromide, triflate and hydrogen sulfate andfor n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula IIis stirred with a cysteine ester of the formula III,in which R is branched or linear C1-10-alkyl orwhere n=0, 1 or 2 and R is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.

    Substituted benzamides, their production and their use as cysteine protease inhibitors
    85.
    发明专利
    Substituted benzamides, their production and their use as cysteine protease inhibitors 未知

    公开(公告)号：AU743245B2

    公开(公告)日：2002-01-24

    申请号：AU3818699

    申请日：1999-04-19

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  MOLLER ACHIM ,  TREIBER HANS-JORG ,  KNOPP MONIKA

    IPC: C07D295/08 ,  A61K31/18 ,  A61K31/27 ,  A61K31/4409 ,  A61K31/4418 ,  A61P9/00 ,  A61P13/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07C233/78 ,  C07C235/42 ,  C07C237/34 ,  C07C311/21 ,  C07D213/56 ,  C07D295/096 ,  A61K31/44

    Abstract: Benzamides of the formula Iand 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, andR2 can be NR5CO-R6 and NHR5SO2-R6, andR3 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, andA 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, andB 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 alsoR5 hydrogen and C1-C4-alkyl andR6 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, andR8 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; andR13 is hydrogen and C1-C6-alkyl, branched or unbranched, andn,p is [sic], independently of one another, a number 0, 1 or 2, andm,o is [sic], independently of one another, a number 0, 1, 2, 3 or 4.

    NEW HETEROCYCLICALLY SUBSTITUTED AMIDES, THEIR PRODUCTION AND THEIR USE
    86.
    发明专利
    NEW HETEROCYCLICALLY SUBSTITUTED AMIDES, THEIR PRODUCTION AND THEIR USE 未知

    公开(公告)号：HU0102146A2

    公开(公告)日：2001-11-28

    申请号：HU0102146

    申请日：1999-05-25

    Applicant: BASF AG

    Inventor： KNOPP MONIKA ,  LUBISCH WILFRIED ,  MOELLER ACHIM ,  TREIBER HANS-JOERG

    IPC: C07D215/08 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61P9/08 ,  A61P9/10 ,  A61P13/12 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/28 ,  A61P27/12 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D209/14 ,  C07D209/44 ,  C07D215/06 ,  C07D217/06 ,  C07D217/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14

    Abstract: Fused heterocyclic-substituted (hetero)aromatic carboxylic acid alkylamides (I) are new. Amides of formula (I) and their tautomers, enantiomers, diastereomers, E- and Z-isomers and salts are new. [Image] A : fused cyclic group such as 1,2,3,4-tetrahydroquinolin-1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, isoindolin-2-yl or indolin-1-yl, all substituted by (R 4) n in the benzene ring; B' : phenyl, naphthyl, pyridyl, pyrimidyl, pyrazyl, pyridazyl, quinolyl, quinazyl, quinoxalyl, thienyl, benzothienyl, benzofuranyl, furanyl or indolyl; R 1H, alkyl, alkoxy, alkenyl, alkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, OH, halo, CF 3, NO 2, NH 2, CN, COOH, COOT, NHC(O)T, NHC(O)Ph, C(O)NHR 11, NHSO 2T, NHSO 2Ph, SO 2T or SO 2Ph; T : 1-4C alkyl; R 2alkyl (optionally substituted by phenyl, cyclohexyl, pyridyl, thienyl, indolyl or naphthyl, themselves all optionally substituted by 1 or 2 R 1 groups); R 3H, COOR 5 or C(O)Z; Z : NR 6R 7, 4-(R 15)-piperazino, R 15-substituted pyrrolidino or R 15-substituted piperidino; R 4H, (CH 2) mNR 8R 9, (CH 2) mQ or O(CH 2) mQ'; Q : 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 15-substituted pyrrolidino, R 15-substituted piperidino, morpholino, 4-(R 8)-1-piperidinyl or R 8-substituted hexamethyleneimino; Q' : 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 8-substituted pyrrolidino, R 15-substituted piperidino, morpholino or 4-(R 8)-1-piperidinyl; R 5, R 8, R 9alkyl (optionally substituted by phenyl, itself optionally substituted by 1 or 2 R 10); R 6H or alkyl; R 7H or alkyl (optionally substituted by phenyl or pyridyl (both optionally substituted by R 10) or by 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 15-substituted pyrrolidino, R 15-substituted piperidino, R 8-substituted 1-imidazolyl, morpholino, 4-(R 8)-1-piperidinyl or -(CH 2) oNR 8R 9); R 10H, T, OT, OH, halo, CF 3, NO 2, NH 2, CN, CONH 2, COOH, COOT, NHC(O)T, NHC(O)Ph, NHSO 2T, NHSO 2Ph, SO 2T or SO 2Ph; R 11H or alkyl; R 15H or as R 8; m : 1-6; n : 0-2; o : 0-4; unless specified otherwise alkyl moieties have 1-6C and alkenyl or alkynyl moieties 2-6C. ACTIVITY : Neuroprotective; spasmolytic; antiischemic; cytoprotective; cardiovascular; antitumor; antiinflammatory; antirheumatic. MECHANISM OF ACTION : Cystiene protease inhibitor; calpain inhibitor; cathepsin inhibitor; interleukin-1 antagonist. No results of biological activity tests are given, although test procedures are described.

    SUBSTITUTED BENZAMIDES, THEIR PRODUCTION AND THEIR USE AS CYSTEINE PROTEASE INHIBITORS
    89.
    发明专利
    SUBSTITUTED BENZAMIDES, THEIR PRODUCTION AND THEIR USE AS CYSTEINE PROTEASE INHIBITORS 未知

    公开(公告)号：HU0101616A2

    公开(公告)日：2001-09-28

    申请号：HU0101616

    申请日：1999-04-19

    Applicant: BASF AG

    Inventor： KNOPP MONIKA ,  LUBISCH WILFRIED ,  MOELLER ACHIM ,  TREIBER HANS-JOERG

    IPC: C07D295/08 ,  A61K31/18 ,  A61K31/27 ,  A61K31/4409 ,  A61K31/4418 ,  A61P9/00 ,  A61P13/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07C233/78 ,  C07C235/42 ,  C07C237/34 ,  C07C311/21 ,  C07D213/56 ,  C07D295/096

    Abstract: Benzamides of the formula Iand 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, andR2 can be NR5CO-R6 and NHR5SO2-R6, andR3 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, andA 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, andB 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 alsoR5 hydrogen and C1-C4-alkyl andR6 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, andR8 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; andR13 is hydrogen and C1-C6-alkyl, branched or unbranched, andn,p is [sic], independently of one another, a number 0, 1 or 2, andm,o is [sic], independently of one another, a number 0, 1, 2, 3 or 4.

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