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    71.
    发明专利
    未知

    公开(公告)号：NO20005929L

    公开(公告)日：2000-11-23

    申请号：NO20005929

    申请日：2000-11-23

    Applicant: BASF AG

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

    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 ,  A61K31/44

    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.

    73.
    发明专利
    未知

    公开(公告)号：NO20005265L

    公开(公告)日：2000-10-19

    申请号：NO20005265

    申请日：2000-10-19

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  TREIBER HANS-JOERG ,  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.

    Use of pyrimidine derivatives for the prophylaxis and therapy of cerebral ischemia
    80.
    发明专利
    Use of pyrimidine derivatives for the prophylaxis and therapy of cerebral ischemia 未知

    公开(公告)号：NZ512767A

    公开(公告)日：2003-05-30

    申请号：NZ51276799

    申请日：1999-12-24

    Applicant: BASF AG

    Inventor： SZABO LASZLO ,  EMLING FRANZ ,  GARCIA-LADONA FRANCISCO JAVIER ,  HOFMANN HANS-PETER ,  UNGER LILIANE ,  STEINER GERD ,  SCHELLHAAS KURT ,  LUBISCH WILFRIED ,  HOLZENKAMP UTA ,  STARCK DOROTHEA ,  KNOPP MONIKA

    IPC: C07D495/04 ,  A61K31/505 ,  A61K31/519 ,  A61P9/10 ,  C07D495/14 ,  A61K31/513 ,  A61K31/55

    Abstract: The use of pyrimidine derivatives of the formula (I) where: A is NH or oxygen; B is hydrogen or methyl; D is methyl; E is ¥ C ¥ Nr3R4 or Q% O D and E are together ûCH2-CH2-NR1-CH2-, -CH2-NR1-CH2- or -CH2-NR1-CH2-CH2-; X is nitrogen; Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH; Z is nitrogen, carbon or CH, with it also being possible for the bond between Y and Z to be a double bond, N is the number 2, 3 or 4; R1 is hydrogen, a C1-C4-alkyl group, and acetyl or benzoyl group, a phenylalkyl C1-C4-alkyl group, an acetyl or benzoyl group, a phenylalkyl C1-C4 radical, with the aromatic moiety optionally being substituted by halogen, or C1-C4-alkyl, trifluoromethyl, hydroxy, C1-C4-alkoxy, amino, cyano or nitro groups, a napthylalkyl C1-C3 radical, a phenylalkanone C2-C3 radical or a phenylcarbamoylalkyl C2 radical, with it being possible for the phenyl group to be substituted by halogen; R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is optional monosubstituted, disubstituted or trisubstituted by halogen atoms, C1-C4-alkyl or be substituted by halogen, a C1-C4-alkyl group, a methoxy group and by a nitro or amino group; R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is optionally monosubstituted, disubstituted or trisubstituted by halogen atoms, C1-C4-alkyl or trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4-alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which can optionally be fused to a benzene nucleus which can optionally be monosubstituted or disubstituted by halogen atoms, C1-C4-alkyl or hydroxyl, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitro groups and which can optionally contain 1 nitrogen atom, or to a 5- or 6-membered ring which can contain 1-2 oxygen atoms, or can be substituted by a phenyl-C1-C2-alkyl- or ûalkoxy group, with it being possible for the phenyl radical to be substituted by halogen, or a methyl, trifluoromethyl or methoxy group; R3 and R4 are, independently of each other, hydrogen or a C1-C4-alkyl group, and of their physiologically tolerated salts for producing medicaments for the prophylaxis and treatment of cerebral ischemia and strokes.

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