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    13.
    发明专利
    未知

    公开(公告)号：ES2162942T3

    公开(公告)日：2002-01-16

    申请号：ES95935916

    申请日：1995-10-07

    Applicant: BASF AG

    Inventor： RIECHERS HARTMUT ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  MULLER STEFAN ,  BAUMANN ERNST

    IPC: C07D251/30 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  C07D239/00 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/60 ,  C07D239/70 ,  C07D239/96 ,  C07D251/12 ,  C07D251/52 ,  C07D257/02 ,  C07D309/00 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048

    Abstract: Heterocyclyl-substd. propanoic acids and their derivs., of formula (I), are new. R = formyl, tetrazolyl, nitrile, COOH or a gp. that can be hydrolysed to COOH; X = N or CR14; R2 = H, OH, NH2, alkylamino, dialkylamino, halo, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; R14 = H or 1-5 C alkyl; R3 = R2 or alkoxyimino; or CR3 + CR14 = 5 or 6 membered alkylene or alkenyl ring (opt. substd. by 1-2 alkyl) in which a methylene can be replaced by O, S, NH or alkylamino; R4, R5 = phenyl or naphthyl (both opt. substd. by one or more halo, NO2, CN, OH, alkyl, haloalkyl, alkoxy, haloalkyloxy, phenoxy, alkylthio, NH2, alkylamine or dialkylamino) or 3-7 C cycloalkyl; or the phenyl or naphthyl gps. are opt. bonded at the O- position (by a bond, CH2, O, S, SO2, ethylene, ethenylene or opt. alkylated amino); R6 = H, 1-8 C alkyl, 2-6 C alkenyl, 3-6 C alkynyl, 3-8 C cycloalkyl (all opt. substd. by 1 or more halo, NO2, CN, alkoxy 3-6 C alkenyloxy, 3-6 C alkynyloxy, alkylthio, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, 3-8 C alkylcarbonylalkyl, alkylamino, dialkylamino, phenyl, Ph or OPh), Ar or Het; Y = S, O or bond; Q = S, O, SO, SO2 or bond; Ph = substd. phenyl, where substits. are halo, NO2, CN, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; Ar = phenyl or naphthyl (both opt. substd. by 1 or more halo, NO2, CN, OH, NH2, alkylamino, dialkylamino or OCH2CH2O); Het = 5 or 6 membered heteroaromatic with 1-3 N atoms and/or one S or O (opt. substd. by 1-4 halo and/or 1 or 2 alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, phenyl, phenoxy or phenyl carbonyl (where the phenyl is opt. substd. by 1-5 halo and/or 1-3 alkyl, haloalkyl, alkoxy, haloalkoxy and/or alkylthio)); alkyl and alkoxy have 1-4 C unless otherwise stated; provided that R6 is not H when Q = bond.

    Amino acid derivatives as endothelin antagonists
    20.
    发明专利
    Amino acid derivatives as endothelin antagonists 未知

    公开(公告)号：NZ319595A

    公开(公告)日：2001-03-30

    申请号：NZ31959596

    申请日：1996-09-26

    Applicant: BASF AG

    Inventor： KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED

    IPC: A61K31/00 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/444 ,  A61K31/505 ,  A61K31/53 ,  A61P5/24 ,  A61P5/36 ,  A61P5/42 ,  A61P9/12 ,  C07D213/74 ,  C07D239/10 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D239/52 ,  C07D239/58 ,  C07D251/46 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D491/056 ,  C07D251/12 ,  C07D403/06

    Abstract: The amino acid derivatives of formula (I) are endothelin antagonists. The compounds may be used in medicaments to treat hypertension, myocardial infarct, angina pectoris, acute kidney failure, renal insufficiency, cerebral vasospasms, cerebral ischemia, subarachnoid hemorrhages, migraine, asthma, atherosclerosis, endotoxic shock, intravascular coagulation, restenosis following angioplasty, benign prostate hyperplasia and ischemic kidney failure. In formula (I); R is COOH or a radical which can be hydrolyzed to COOH; W is nitrogen; R2 is hydrogen, halogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, hydroxyl, mercapto, C1-C4-alkylthio, nitro, amino, C1-C4-alkylamino or C1-C4-dialkylamino, cyano, optionally substituted phenyl, or an optionally substituted five-or six-membered heteroaromatic ring which contains from one to three N atoms and/or one S or O; or R2 can furthermore form with the adjacent carbon atom and X, a 5- or 6-membered alkylene or alkylidene ring in which, in each case, one or two carbon atoms can be replaced by a N, S or O hetero atom and which can be mono- to trisubstituted by the following radicals: halogen, nitro, cyano, hydroxyl, mercapto, C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy, C1-C3 alkylthio, amino, C1-C3 alkylamino, C1-C3 dialkylamino; R3 can have the same meaning as R2, or furthermore form together with the adjacent carbon atom and Y, an optionally substituted 5- or 6-embered alkylene or alkylidene ring in which, in each case, one or two carbon atoms can be replaced by N, O or S; X is nitrogen or CR15, where R15 is hydrogen or C1-C5-alkyl, C1-C5-alkoxy, C1-C5-alkylthio, nitro, phenyl, hydroxyl, mercapto, halogen, amino, C1-C4-alkylamino, C1-C4-dialkylamino or cyano, or CR15 is linked to R2 to form a 5- or 6-membered ring as described above, or CR15 can form together with R3 and its adjacent carbon atom a 5- or 6-membered ring as described above; Y is nitrogen or CR16, where R16 is the same as R15, or CR16 forms together with R3 and its adjacent carbon atom a 5- or 6-membered ring as described above; R4 is hydrogen, C1-C7-alkyl, C3-C7-cycloalkyl, or optionally substituted phenyl or naphthyl; or R4 can be an optionally substituted 5- or 6-membered heteroaromatic ring which contains one N, O or S atom, or R4 and R5 can be phenyl groups which are connected to each other in the ortho positions by a direct linkage, a methylene, ethylene or ethenylene group, an O or S atom or an SO2, NH or N-alkyl group; R5 is C1-C7-alkyl, C3-C7-cycloalkyl or phenyl or naphthyl which can be substituted by 1 to 3 of the following radicals; halogen, nitro, cyano, hydroxyl, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, phenoxy, phenyl, C1-C4-alkylthio, amino, C1-C4-alkylamino or C1-C4-dialkylamino, or the radicals depicted above; or R5 can be an optionally substituted 5- or 6-membered hetero aromatic ring with one N, S or O heteroatoms; or R5 can form together with R4 a tricyclic system, or R5 can be an optionally substituted phenyl or heteroaromatic radical as described above, which is linked in the ortho position to R8 to form a 6-membered ring where Q must be a single bond and R8 must be a CH-R17 group; R6 is hydrogen or C1-C4-alkyl or C1-C4 haloalkyl; Z is a single bond, O, S, sulfinyl or sulfonyl; R7 is hydrogen, or C1-C4 alkyl, C2-C4-alkenyl, C2-C4-alkynyl; Q is a single bond, a C=O, or C(=O)O group; and R8 is hydrogen, C1-C4-alkyl, C2-C4-alkenyl, phenyl or benzyl, and R8 can furthermore be directly connected to R5 as described above, in which case R8 is a CH-R17 group, where R17 is hydrogen, C1-C4-alkyl, phenyl or phenyl which is mono- to trisubstituted by methoxy, or R8 is a radical as depicted above.

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