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    2.
    发明专利
    未知

    公开(公告)号：DE3782549D1

    公开(公告)日：1992-12-17

    申请号：DE3782549

    申请日：1987-06-20

    Applicant: BASF AG

    Inventor： SCHOLLMEIER KLAUS DR ,  MOELLER ACHIM DR ,  KOERWER WOLFGANG DR ,  DOERPER THOMAS DR ,  HILLEN HEINZ DR ,  DAUM LOTHAR DR ,  EMLING FRANZ DR ,  KEILHAUER GERHARD DR

    IPC: C07K14/52 ,  A61K38/00 ,  A61P35/00 ,  C07K14/00 ,  C07K14/525 ,  C12N15/00 ,  C12N15/09 ,  C12P21/02 ,  C12R1/19 ,  A61K37/02 ,  C07K15/00

    Abstract: (I) and their allelic variations and mutagenically produced derivs. with lymphotoxin or lymphotoxin-like activity, as well as derivs. having an N-terminal immunogenic peptide sequence, are new. (I) is X-Leu-Lys-Pro-Ala-Ala-His-Leu-Ile -Gly-Asp-Pro-Ser-Lys-Gln-Asn-Ser-Leu- Leu-Trp-Arg-Ala-Asn-Thr-Asp-Arg-Ala-Phe-Leu-Gln-Asp-Gly-Phe-Ser-L- eu-Ser-Asn-Asn-Ser-Leu-Leu -Val-Pro-Thr-Ser-Gly-Ile -Tyr-Phe-Val-Tyr-Ser-Gln- -Val-Val-Phe-Ser-Gly-Lys-Ala-Tyr-Ser-Pro-Lys-Ala-Thr- Ser-Ser-Pro-Leu Tyr-Leu-Ala-His-Glu-Val -Gln- Leu-Phe-Ser--Ser-Gln-Tyr-Pro-Phe-His-Val-Pro- Leu-Leu-Ser-Ser-Gln -Lys-Met-Val-Tyr-Pro-Gly- Leu-Gln-Glu-Pro -Trp-Leu-His-Ser-Met-Tyr-His-Gly -Ala-Ala-Phe-Gln-Leu-Thr-Gln-Gly-Asp- Gln-Leu-Ser-Thr -His-Thr-Asp-Gly-Ile-Pro-His-Leu -Val-Leu-Ser-Pro Ser-Thr-Val-Phe-Phe-Gly -Ala-Phe-Ala-Leu, where X = Thr, Ser-Thr, Met-Ser-Thr, Ala-Thr or Ala-Ser-Thr. DNA sequences coding for the polypeptides are also new.

    New 2-substituted 1,2-benzisothiazole derivatives
    6.
    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.

    7.
    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.

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