公开(公告)号：DE19609827A1

公开(公告)日：1997-09-18

申请号：DE19609827

申请日：1996-03-13

Applicant: HOECHST AG

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

IPC: C07D215/48 ,  A61K31/47 ,  A61P43/00 ,  C07D215/26 ,  C07D215/24 ,  C07D209/48 ,  C07D401/12

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.

公开(公告)号：DE19603767A1

公开(公告)日：1997-08-07

申请号：DE19603767

申请日：1996-02-02

Applicant: HOECHST AG

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

IPC: C07D207/08 ,  C07D207/20 ,  C07D401/12 ,  C07D409/14 ,  C07D401/10 ,  A61K31/40 ,  A61K31/445 ,  C07D209/52 ,  C07D215/48

Abstract: Pyrrolidine derivatives of formula (I), and their salts are new: R1 = OH, 1-10C alkoxy, 3-10C alkenyloxy, 1-3C alkyl-(6-10C)aryloxy or NR6R7; R2 = 1-10C alkyl, 2-10C alkenyl, 3-10C alkynyl or (CH2)m-B-(CH2)nR5 (all optionally substituted by a COR1 group, or optionally substituted by one or more halo); (6-10C)aryl-(1-3C)alkyl or (6-10C)-aryl (both optionally ring substituted by 1-2 halo, 1-4C alkoxy, NO2 or CN); or 3-8C cycloalkyl, (4-10C)cycloalkyl-(1-4C)alkyl, (5-10C)cycloalkyl-(2-4C)alkenyl or (5-10C)cycloalkyl-(2-4C)alkynyl; R3 = H, 1-8C alkyl, 3-8C cycloalkyl, (6-10C)aryl-(1-3C)alkyl, 2-6C alkenyl or 3-6C alkynyl; or R2 + R3 = 2-4C alkylene, optionally substituted by halo; R4 = H, 1-6C alkyl, (6-10C)aryl-(1-3C)alkyl, 3-10C alkenyl, COO-(1-6C)alkyl, COO-(1-6C)alkyl-(6-10C)aryl or C(=NH)NH2; R5 = H, or a group of formula (i): R6, R7 = H, 1-10C alkyl, (6-10C)aryl-(1-3C)alkyl, 1-10C alkylamino or 1-10C alkylguanidino; R8 = 6-10C aryl or (6-10C)aryl-(1-3C)alkyl (both optionally substituted by one or more COR1, halo, NO2, CN, 1-4C alkoxy or amino); or 1-6C alkyl, 3-8C cycloalkyl or (2-6C)alkenyl; R9 = NH(CH2)oNHR4, O(CH2)oNH2 or O(CH2)oNH-C(=NH)NH2; A = a single or double bond; B = O, NR3 or S; Y = a direct bond, or an amino acid; m = 1-5; n = 1-5; o = 1-10.

公开(公告)号：DE59108573D1

公开(公告)日：1997-04-10

申请号：DE59108573

申请日：1991-04-25

Applicant: HOECHST AG

Inventor： BREIPOHL GERHARD DR ,  HENKE STEPHAN DR ,  KNOLLE JOCHEN DR ,  SCHOELKENS BERNWARD PROF DR ,  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：DE59007747D1

公开(公告)日：1995-01-05

申请号：DE59007747

申请日：1990-08-11

Applicant: HOECHST AG

Inventor： HENKE STEPHAN DR ,  BREIPOHL GERHARD DR ,  KNOLLE JOCHEN DR ,  SCHOELKENS BERNWARD PROF DR ,  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：DE58907889D1

公开(公告)日：1994-07-21

申请号：DE58907889

申请日：1989-11-21

Applicant: HOECHST AG

Inventor： HENKE STEPHAN DR ,  ANAGNOSTOPULOS HIRISTO ,  BREIPOHL GERHARD DR ,  KNOLLE JOCHEN DR ,  STECHEL JENS DR ,  SCHOELKENS BERNWARD PROF DR ,  FEHLHABER HANS-WOLFRAM DR

IPC: A61K38/17 ,  A61K38/00 ,  A61K38/08 ,  A61P9/00 ,  A61P9/02 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07K1/06 ,  C07K7/06 ,  C07K7/08 ,  C07K7/18 ,  C07K99/20

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 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, 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, have bradykinin-antagonistic action. Their therapeutic uses comprise all pathological states which are promoted, induced or sustained 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：AT107318T

公开(公告)日：1994-07-15

申请号：AT89121498

申请日：1989-11-21

Applicant: HOECHST AG

Inventor： HENKE STEPHAN DR ,  ANAGNOSTOPULOS HIRISTO ,  BREIPOHL GERHARD DR ,  KNOLLE JOCHEN DR ,  STECHEL JENS DR ,  SCHOELKENS BERNWARD PROF DR ,  FEHLHABER HANS-WOLFRAM DR

IPC: A61K38/17 ,  A61K38/00 ,  A61P9/00 ,  A61P9/02 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07K1/06 ,  C07K7/06 ,  C07K7/08 ,  C07K7/18 ,  C07K99/20

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 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, 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, have bradykinin-antagonistic action. Their therapeutic uses comprise all pathological states which are promoted, induced or sustained 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：DE59002721D1

公开(公告)日：1993-10-21

申请号：DE59002721

申请日：1990-08-08

Applicant: HOECHST AG

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

IPC: A61K38/55 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07C237/12 ,  C07K5/06 ,  A61K37/64 ,  A61K37/02

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.

公开(公告)号：DE4036645A1

公开(公告)日：1992-05-21

申请号：DE4036645

申请日：1990-11-16

Applicant: HOECHST AG

Inventor： KLEEMANN HEINZ-WERNER DR ,  GERHARDS HERMANN DR ,  SCHOELKENS BERNWARD PROF DR

IPC: A61K31/41 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/495 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/88 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/10 ,  C07D409/10 ,  C07D411/10 ,  C07D413/10

Abstract: Azoles of the formula in which X, Y and Z represent N or CR , L denotes alkylene, A denotes an aromatic or heterocyclic radical and T denotes a bond or a bivalent radical and R , R and E are as defined in the description. A process for their preparation, compositions containing these compounds and their application as medicines are also described.