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    New 2-substituted 1,2-benzisothiazole derivatives
    2.
    发明专利
    New 2-substituted 1,2-benzisothiazole derivatives 未知

    公开(公告)号：DE19746612A1

    公开(公告)日：1999-04-29

    申请号：DE19746612

    申请日：1997-10-22

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED DR ,  DULLWEBER UTA DR ,  STARCK DOROTHEA DR ,  STEINER GERD DR ,  BACH ALFRED DR ,  EMLING FRANZ DR ,  GARCIA-LADONA FRANCISCO JAVIER ,  TESCHENDORF HANS-JUERGEN DR ,  WIECKE KARSTEN DR

    IPC: A61K31/428 ,  A61P25/24 ,  A61P43/00 ,  C07D275/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  A61K31/445 ,  A61K31/44 ,  A61K31/425

    Abstract: 2-Substituted 1,2-benzisothiazole derivatives (I) and their acid salts are new. 2-Substituted 1,2-benzisothiazole derivatives of formula (I) and their enantiomers, diastereomers, tautomers and acid salts are new. R , R = independently 1-6C alkyl; R , R = independently H, 1-6C alkyl, OH, 1-6C alkoxy, F, Cl, Br, I, CF3, NR R , CO2R , NO2, CN, pyrrolo, or phenyl-(1-4C alkyl), which may itself be ring-substituted by F, Cl, Br, I, 1-4C alkyl, 1-4C alkoxy, CF3, OH, NH2, CN or NO2; R , R = independently H, 1-6C alkyl, benzoyl, CO2-tert.-butyl, (1-4C alkyl)carbonyl or together form a 5- or 6-membered ring, which may contain a second N atom (e.g. piperazinyl); R = H or 1-6C alkyl; A = 1-10C alkylene or 2-10C alkylene containing one or more Z groups; Z = O, S, NR , cyclopropyl, CHOH, or a double or triple bond; B = 4-piperidine, 4-(1,2,3,6-tetrahydropyridine), 4-piperazine or one of these rings N-bound to A via a methylene group; Ar = phenyl (optionally substituted by 1-6C alkyl, 1-6C alkoxy, OH, F, Cl, Br, I, CF3, NR R , CO2R , CN or phenyl), tetralinyl, indanyl, other condensed aromatic moieties e.g. naphthalinyl (optionally substituted by 1-4C alkyl or 1-4C alkoxy), anthracenyl, or a 5- or 6-membered aromatic heterocycle with 1 or 2 O or N heteroatoms, which can be anellated with other aromatic groups.

    4.
    发明专利
    未知

    公开(公告)号：DE19636769A1

    公开(公告)日：1998-03-12

    申请号：DE19636769

    申请日：1996-09-10

    Applicant: BASF AG

    Inventor： STEINER GERD DR ,  LUBISCH WILFRIED DR ,  BACH ALFRED DR ,  EMLING FRANZ DR ,  WICKE KARSTEN DR ,  TESCHENDORF HANS-JUERGEN DR ME ,  BEHL BERTHOLD DR ,  KERRIGAN FRANK DR ,  CHEETHAM SHARON DR

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14 ,  A61K31/44 ,  A61K31/38 ,  A61K31/505

    Abstract: The invention concerns 3-substituted 3,4,5,6,7,8-hexahydro-pyrido[4,3':4,5]thieno-[2,3-d]pyrimidine derivatives of formula (I) in which: R designates a hydrogen atom, a C1-C4 alkyl group, an acetyl or benzoyl group, a phenylalkyl C1-C4 group - the aromatic optionally being substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano or nitro groups - a naphthylalkyl C1-C3 group, a phenylalkanone C2-C3 group or a phenylcarbamoylalkyl C2 group, wherein the phenyl group can be substituted by halogen; R designates a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which can optionally be mono-, di- or tri-substituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and can optionally be anellated with a benzene nucleus, which can optionally be mono- or di-substituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and can optionally contain 1 nitrogen atom, or with a 5- or 6-member ring which can contain between 1 and 2 oxygen atoms, or can be substituted by a phenyl-C1-C2 alkyl or alkoxy group, wherein the phenyl group can be substituted by halogen, a methyl, trifluoromethyl or methoxy group; A designates NH or an oxygen atom; B designates hydrogen or methyl; C designates hydrogen, methyl or hydroxy; X designates a nitrogen atom; Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH; Z designates a nitrogen atom, a carbon atom or CH, wherein the bond between Y and Z can also be a double bond; and n is the number 2, 3 or 4, and their physiologically compatible salts. These compounds are suitable as medicaments for treating diseases in which the serotonin concentration is reduced and in which the activity of the presynaptic receptors 5-HT1B, 5-HT1A, 5HT1D is to be blocked within a therapeutic context without greatly influencing other receptors. Such diseases include, for example, depression.

    5.
    发明专利
    未知

    公开(公告)号：DE19532050A1

    公开(公告)日：1997-03-06

    申请号：DE19532050

    申请日：1995-08-31

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED DR ,  BEHL BERTHOLD DR ,  HOFMANN HANS PETER DR ,  TESCHENDORF HANS-JUERGEN DR ME

    IPC: A61K31/00 ,  A61K31/495 ,  A61K31/498 ,  A61P25/04 ,  C07D401/14 ,  C07D403/04

    Abstract: Pyrrolyl tetrahydroquinoxalin diones of formula (I) and their tautomeric and isomeric forms, and their physiologically acceptable salts, in which the variables are: R - hydrogène, cyclohexyl radical, an aliphatic radical with 1 to 4 atoms which can bear the radical COOR , where R is hydrogen or C1-C4 alkyl, R -COOH, -COO-C1-C4, -COO-(CH2)m-Ph, -CONR R and (a), where m may be a whole number from 1 to 6, R is hydrogen, -C1-C4 alkyl or OH and R is hydrogen, -C1-C4 alkyl, -(CH2)m-Ph or (b), where all the phenyl or pyridyl rings contained in R may be substituted by up to 3 of the following radicals: -C1-C4 alkyl, halogen, -O-C1-C4 alkyl, -OCF3, -NO2, -CN, -COOR or -CONHR ; R is -CF3, -NO2, -CN and R is hydrogen; or R and R together may be an anellated benzole ring. The compounds are suitable as medicaments in human and veterinary medicine.

    Substituted benzamide, process of its preparation and use thereof as cysteine protease inhibitor
    9.
    发明专利
    Substituted benzamide, process of its preparation and use thereof as cysteine protease inhibitor 未知

    公开(公告)号：CZ20003890A3

    公开(公告)日：2001-11-14

    申请号：CZ20003890

    申请日：1999-04-19

    Applicant: BASF AG

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

    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 ,  A61P9/10

    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.

    10.
    发明专利
    未知

    公开(公告)号：DK0572852T3

    公开(公告)日：1999-06-28

    申请号：DK93107984

    申请日：1993-05-17

    Applicant: BASF AG

    Inventor： HOFMANN HANS PETER DR ,  LUBISCH WILFRIED DR ,  BEHL BERTHOLD DR

    IPC: 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

    Abstract: Quinoxaline-2,3-(1H,4H)diones of the general formula I in which the variables have the following meaning: R is hydrogen; an aliphatic radical having up to 12 C atoms, which can carry one of the following substituents: phenyl, cyclopentyl, cyclohexyl or a group -CO-R , -CO-O-R or -CO-NH-R , where R denotes hydrogen, C1-C4-alkyl, phenyl, benzyl or 1-phenylethyl; a cycloaliphatic radical having up to 12 C atoms, or a phenyl group, where the cyclic groups contained in R can carry up to three of the following substituents: C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, halogen, nitro, cyano, -CO-O-R and -CO-NH-R ; R is a pyrrol-1-yl group which can carry up to two of the following substituents: C1-C4-alkyl, phenyl, phenylsulphonyl, nitro, cyano and one of the groups -CO-O-R , -CO-NH-R , -CH2-O-R , -O-R and -CH=NO-R ; R is identical or different radicals from the following: C1-C4-alkyl, C1-C4-alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and one of the groups -CO-O-R and -CO-NH-R and a fused benzene ring; n is 0 to 3. Quinoxaline-2,3-(1H,4H)diones I' in which R has the meaning mentioned. The compounds I and I' are suitable as medicines for human and veterinary medicine.

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