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    3.
    发明专利
    未知

    公开(公告)号：AT183197T

    公开(公告)日：1999-08-15

    申请号：AT93105336

    申请日：1993-03-31

    Applicant: HOECHST AG

    Inventor： BREIPOHL GERHARD DR ,  HENKE STEPHAN DR ,  KNOLLE JOCHEN DR ,  SCHOELKENS BERNWARD PROF DR ,  ALPERMANN HANS-GEORG DR ,  GERHARDS HERMANN DR ,  WIRTH KLAUS DR

    IPC: A61K38/00 ,  A61K38/04 ,  A61K38/08 ,  A61P43/00 ,  C07K7/06 ,  C07K7/18

    Abstract: Peptides of the formula I Z - P - A - B - C - E - F - K - (D)Q - G- M- F' - I (I), in which Z is optionally substituted (cyclo)alk(ano)yl(sulphonyl), (C1-C8)-alkoxycarbonyl, (hetero)ar(o)yl(sulphonyl), carbamoyl, P is a direct linkage or a radical II -NR -(U)-CO- (II> in which R is H, methyl or a urethane protective group, U is (cyclo)(aryl)alkylidene, (hetero)arylidene or (CHR )n, R is hydrogen, (cyclo)alkyl, (hetero)aryl, or in which R and R form, together with the atoms carrying them, a ring system; A is defined as P; B is a basic amino acid in the L or D configuration, C is a compound of the formula IIIa or IIIb G'-G'-Gly (IIIa> G'-NH-(CH2)p-CO (IIIb> in which p is 2 to 8 and G' are, independently of one another, a radical of the formula IV -NR -CHR -CO- (IV> in which R and R form, together with the atoms carrying them, a heterocyclic ring system; E is the residue of a neutral, acid or basic, aliphatic or alicyclic-aliphatic amino acid; F are, independently of one another, the radical of a neutral, acid or basic, aliphatic or aromatic amino acid, or a direct linkage; (D)Q is D-Tic, D-Phe, D-Dic, D-Thi or D-Nal, or a radical of the formula (V) in which X is O, S or a direct linkage, and R is H, (cyclo)alkyl or aryl(alkyl), G is defined as G' above or is a direct linkage; F' is defined as F, is a radical -NH-(CH2)q- with q = 2 to 8 or, if G is not a direct linkage, can be a direct linkage, and I is -OH, -NH2 or NHC2H5; K is the radical -NH-(CH2)x-CO- with x = 1-4 or is a direct linkage, and M is defined as F and their physiologically tolerated salts are described. They have excellent bradykinin-antagonistic action. They are obtained by reacting a fragment with a C-terminal free carboxyl group or its activated derivative with an appropriate fragment with an N-terminal free amino group, or by assembling the peptide stepwise, eliminating one or more protective groups temporarily introduced where appropriate to protect other functionalities in the compound obtained in this way, and converting the compounds of the formula I obtained in this way where appropriate into their physiologically tolerated salt.

    New carbamoyl substituted piperidine carbonyl peptide derivatives
    6.
    发明专利
    New carbamoyl substituted piperidine carbonyl peptide derivatives 未知

    公开(公告)号：DE19546938A1

    公开(公告)日：1997-06-19

    申请号：DE19546938

    申请日：1995-12-15

    Applicant: HOECHST AG

    Inventor： WAGNER ADALBERT DR ,  BREIPOHL GERHARD DR ,  HEITSCH HOLGER DR ,  GERHARDS HERMANN DR ,  NOELKEN GERHARD DR ,  WIRTH KLAUS DR ,  SCHOELKENS BERNWARD PROF DR

    IPC: A61K38/00 ,  C07K5/02 ,  C07K7/18 ,  A61K38/06 ,  A61K38/07

    Abstract: 1-Carbamoyl-4-piperidinecarbonyl di- and tripeptides (I) and their salts are new: R = H, 2-6C alkyl, NR R or -N(R )=C(NHR )(NHR ); R = 1-10C alkyl, 2-10C alkenyl, 3-10C alkynyl or -(CH2)m-B-(CH2)n-R (all optionally monosubstituted by CO2R or by 1 or more halo), OR , 3-8C cycloalkyl, 4-10C cycloalkyl-1-4C alkyl, 5-10C cycloalkyl-2-4C alkenyl, 5-10C cycloalkyl-2-4C alkynyl or 6-10C aryl (optionally mono- or disubstituted by halo, 1-4C alkoxy, NO2 or CN); R = H, 1-8C alkyl, 3-8C cycloalkyl, phenyl, benzyl, 1-8C alkoxy-CO- or 1-4C alkyl-6-10C aryloxy-CO-; R = H, 1-6C alkyl, 3-8C cycloalkyl, 2-4C alkenyl or 2-4C alkynyl; R = H, 1-6C alkyl, 3-8C cycloalkyl, phenyl or benzyl; B = O, NR or S; n = 1-5; m = 0-5; o, p = 1-10; A1 = a bond, Phe, 2-, 3- or 4-Cl- or 2-, 3- or 4-F-phenylalanine, Tyr, Tyr(OMe), Thi, Gly, Cha, Leu, Ile, Val, Nle or Phg; A2 = a bond, Gly, Ser, Hser, Lys, Leu, Val, Nle, Ile or Cys; and A3, A4 = a bond or a heterocyclic group of e.g. formula (A) to (C).

    (Aminoalkyl- and acylaminoalkyl-oxy)benzyloxyquinolines, process for their preparation and use as Bradykinin receptor antagonists
    10.
    发明专利
    (Aminoalkyl- and acylaminoalkyl-oxy)benzyloxyquinolines, process for their preparation and use as Bradykinin receptor antagonists 未知

    公开(公告)号：SI0795547T1

    公开(公告)日：2000-10-31

    申请号：SI9730063

    申请日：1997-02-27

    Applicant: HOECHST AG

    Inventor： HEITSCH HOLGER DR ,  WAGNER ADALBERT DR ,  WIRTH KLAUS DR ,  SCHOELKENS BERNWARD PROF DR ,  NOELKEN GERHARD DR

    IPC: A61K31/47 ,  A61P43/00 ,  C07D215/48 ,  C07D215/26

    Abstract: 8-(3-(Aminoalkoxy)-benzyloxy)-quinoline compounds of formula (I) and their salts are new. R1-R3 = H, halo, CHO, COOH, 1-5C alkyl, 6-10C aryl, 1-3C alkyl-(6-10C) aryl, 3-8C cycloalkyl or 1-3C alkoxycarbonyl; R4, R5 = H, halo, NO2, CN, 1-3C alkoxy or 1-3C alkylthio; R6 = H, 1-3C alkyl, 3-5C alkylalkenyl (sic) or 1-3C alkyl-6-10C aryl; R7 = H, 1-6C alkanoyl, alkanoyl (substituted by 1-3C alkoxy, alkylcarbamoyl or aryl), 3-7C alkenoyl, 3-8C cycloalkylcarbonyl, 5-7C cycloalkenylcarbonyl, 1-3C alkoxycarbonyl, aryloxycarbonyl, 6-12C aroyl (optionally substituted by 1-3C alkoxy or halo), alkenoyl (substituted by aryl (optionally substituted by 1-3C alkoxy, 1-3C alkylenedioxy, NO2, CN, halo, 1-3C haloalkyl, hetero-3-8C cycloalkyl (sic), NH2, 1-4C alkylamino, 6-12C heteroaryl-alkanoylamino, aroylamino, 6-12C heteroarylcarbonylamino, 1-5C alkylsulphonylamino, 1-5C alkylureido, alkanoyl, 1-5C alkoxycarbonyl, 1-5C alkylcarbamoyl or arylcarbamoyl), 2-5C acylamino-arylcinnamoyl, 1-3C alkoxycarbonylamino-arylcinnamoyl, 1-4C alkylaminocarbonylaminocinnamoyl, aryl-1-5C alkoxycarbonyl, 1-5C alkylcarbamoyl, arylcarbamoyl, aroylcarbamoyl, alkylsulphonyl, arylsulphonyl, aryl-alkylsulphonyl or phthaloyl (for R6=R7(sic)); n = 1-8; alkyl has 1-6C, aryl has 6-12C, alkanoyl has 2-6C, and alkenoyl has 3-6C unless specified other wise.

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