公开(公告)号：DE3926822A1

公开(公告)日：1991-02-21

申请号：DE3926822

申请日：1989-08-14

Applicant: HOECHST AG

Inventor： BREIPOHL GERHARD DR ,  HENKE STEPHAN DR ,  KNOLLE JOCHEN DR ,  SCHOELKENS BERNWARD PROF ,  GERHARDS HERMANN DR

IPC: A61K38/00 ,  A61K38/08 ,  A61P43/00 ,  C07K1/06 ,  C07K7/06 ,  C07K7/08 ,  C07K7/18

Abstract: Peptides of the formula I A-B-C-E-F-K-(D)-Phe-G-M-F'-I (1> in which A is hydrogen, alkyl, alkanoyl, alkoxycarbonyl, alkylsulphonyl, cycloalkyl, aryl, aryloyl, arylsulphonyl, heteroaryl or an amino acid, each of which can optionally be substituted, B is a basic amino acid, C is a di- or tripeptide, E is the residue of an aromatic amino acid, F is, independently of one another, an amino acid which is optionally substituted in the side chain or is a direct bond, G is an amino acid, F' is defined as F or can be -NH-(CH2)2-8 or optionally a direct bond, I is -OH, -NH2 or -NHC2H5, and K is a radical -NH-(CH2)1-4-CO- or is a direct bond, act as bradykinin antagonists. Their therapeutic uses comprise all pathological states promoted, induced or assisted by bradykinin and bradykinin-related peptides. The peptides of the formula I are prepared by known methods of peptide synthesis.

公开(公告)号：DE4023215A1

公开(公告)日：1992-01-23

申请号：DE4023215

申请日：1990-07-21

Applicant: HOECHST AG

Inventor： HENNING RAINER DR ,  WAGNER ADALBERT DR ,  GERHARDS HERMANN DR ,  SCHOELKENS BERNWARD PROF

IPC: A61K31/415 ,  A61K31/4164 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  A61K31/495 ,  A61K31/505 ,  A61P1/16 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P43/00 ,  C07D233/56 ,  C07D233/90 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: Substd. azole derivs. of formula (I) and their physiologically acceptable salts are new. In (I) X, Y and Z are each N or CR2 R1 is 2-10C alkyl, 3-10C alkenyl, 3-10C alkynyl, -(CH2)mB(CH2nR4 (these 4 gps. opt. monosubstd. with CO2R3 and opt. have 1-all H atoms replaced by F), OR3, 3-8C cycloalkyl, 5-10C cycloalkylalkynyl, or benzyl (opt. mono or disubstd. on the Ph ring with halogen, 1-4C alkoxy and/or NO2), R2 = H, halogen, CvF2v+1, SF5, pentafluoro phenyl CN, phenyl, -(CH2)nF, -(CH2)nONO2, -CH2N3, -(CH2)nNO2, phthalimido (CH2)n-, R3 = H, 1-8C alkyl (in which 1 to all H are replaced by F), 3-8C cycloalkyl, Ph or benzyl, R4 = H, 1-6C alkyl, 3-8C cycloalkyl, 2-4C alkenyl, or 2-4C alkynyl, A = a mono or bicyclic unsatd. or partially hydrogenated heterocycle gp. with 5-10 ring atom of which up to 9 are C, and opt. substd. with up to 3 opt. different R14 gps. or -(CH2)n-1-(CHR6CH2)0-1, R14 where R14 = halogen, oxo, nitroso, NO2, amino, CN, OH, 1-6C alkyl, 1-4C alkanoyl, 1-4C alkanoyloxy. B = O, NR7 or S, W = O or S, L = 1-3C alkanediyl, R26 and R27 are each H, halogen, NO2, 1-4C alkyl or 1-2C alkoxy, n = 1-5, o = 1-10, q = 0-1.

公开(公告)号：DE4036706A1

公开(公告)日：1992-05-21

申请号：DE4036706

申请日：1990-11-17

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER DR ,  HENNING RAINER DR ,  LINZ WOLFGANG DR ,  SCHOELKENS BERNWARD PROF ,  URBACH HANSJOERG DR

IPC: A61K31/41 ,  A61K31/415 ,  A61K31/495 ,  A61K31/675 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D403/10

Abstract: The invention relates to a method for the treatment of cardiac and of vascular hypertrophy and/or hyperplasia by administration of angiotensin II receptor blockers, preferably of the imidazole, pyrrole, pyrazole, triazole or tetrazole type.

公开(公告)号：DE4013270A1

公开(公告)日：1991-10-31

申请号：DE4013270

申请日：1990-04-26

Applicant: HOECHST AG

Inventor： BREIPOHL GERHARD DR ,  HENKE STEPHAN DR ,  KNOLLE JOCHEN DR ,  SCHOELKENS BERNWARD PROF ,  HOCK FRANZ DR

IPC: A61K38/00 ,  A61K38/08 ,  A61K38/17 ,  A61P29/00 ,  A61P37/08 ,  C07K1/02 ,  C07K7/06 ,  C07K7/18

Abstract: Peptides of the formula I A-B-C-E-F-K-(D)-Tic-G-M-F'-I (I> in which A is hydrogen, alkyl, alkanoyl, alkoxycarbonyl, alkylsulphonyl, cycloalkyl, aryl, arylsulphonyl, heteroaryl or an amino acid, each of which can optionally be substituted, B is a basic amino acid, C is a di- or tripeptide, E is the residue of an aliphatic or alicyclic-aliphatic amino acid, F is, independently of one another, an amino acid which is optionally substituted in the side chain or is a direct bond, G is an amino acid, F' is defined as F, can be -NH-(CH2)2-8 or a direct bond, I is -OH, -NH2 or -NHC2H5, and K is a radical -NH-(CH2)1-4-CO-, or is a direct bond, have a bradykinin-antagonistic action. Their therapeutic uses comprise all pathological states which are mediated, induced or assisted by bradykinin and bradykinin-related peptides. The peptides of the formula I are prepared by known methods of peptide synthesis.

公开(公告)号：DE3926606A1

公开(公告)日：1991-02-14

申请号：DE3926606

申请日：1989-08-11

Applicant: HOECHST AG

Inventor： LINZ WOLFGANG DR ,  SCHOELKENS BERNWARD PROF ,  SCHOLZ WOLFGANG DR ,  WIEMER GABRIELE DR ,  URBACH HANS-JOERG DR ,  HENNING RAINER DR ,  TEETZ VOLKER DR

IPC: A61K38/55 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07C237/12 ,  C07K5/06

Abstract: The invention relates to a method for the treatment of cardiac and of vascular hypertrophy and hyperplasia by administration of angiotensin converting enzyme inhibitors. Administration of compounds of the formula I (I) in which n is 1 or 2, R, R1, R2 and R3 are identical or different and each is hydrogen or an organic radical, and R4 and R5 form, together with the atoms carrying them, a mono-, bi- or tricyclic heterocyclic ring system, is preferred. The invention additionally relates to angiotensin converting enzyme inhibitors and to agents containing these for administration for the treatment of the abovementioned diseases.