公开(公告)号：ES2204888T3

公开(公告)日：2004-05-01

申请号：ES92115500

申请日：1992-09-10

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER DR ,  WAGNER ADALBERT DR ,  KLEEMANN HEINZ-WERNER DR ,  GERHARDS HERMANN DR ,  SCHOLKENS BERNWARD PROF DR

IPC: A61K31/33 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/495 ,  A61K31/505 ,  A61P9/10 ,  A61P9/12 ,  C07D235/06 ,  C07D235/08 ,  C07D235/22 ,  C07D235/24 ,  C07D403/10 ,  C07D409/06 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of the formula (I) in which the symbols have the following meaning: X represents a monocyclic radical having 3, 4 or 5 ring atoms, R , R , R , R , R , R and R is, for example, an alkyl radical q is zero or 1 L is, for example, the methylene group A is the radical, for example, of a heterocycle are highly effective as antagonists of angiotensin II receptors. They can be used as pharmaceuticals or diagnostics.

公开(公告)号：CZ284783B6

公开(公告)日：1999-03-17

申请号：CS397990

申请日：1990-08-13

Applicant: HOECHST AG

Inventor： HENKE STEPHAN DR ,  BREIPOHL GERHARD DR ,  KNOLLE JOCHEN DR ,  SCHOLKENS 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：DK0450566T3

公开(公告)日：1995-10-30

申请号：DK91105178

申请日：1991-04-02

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT DR ,  HENNING RAINER DR ,  GERHARDS HERMANN DR ,  SCHOELKENS BERNWARD DR ,  JEAN-PAUL VEVERT ,  JEAN-CLAUDE CAILLE

IPC: A61K31/415 ,  A61K31/38 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/423 ,  A61K31/437 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/495 ,  A61K31/505 ,  A61K31/519 ,  A61P9/12 ,  A61P29/00 ,  A61P43/00 ,  C07D233/64 ,  C07D233/84 ,  C07D233/90 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D471/04 ,  C07D487/04

Abstract: The invention relates to compounds of the formula in which X, Y and Z are identical or different and are N or CR , R and R are as defined in the description, L is an alkylene radical, q = 0 or 1, and A is the radical of a fused heterobicycle. The invention furthermore relates to a method for the preparation of the abovementioned compounds, to compositions containing them, and to their use.

公开(公告)号：ES2065445T3

公开(公告)日：1995-02-16

申请号：ES90115455

申请日：1990-08-11

Applicant: HOECHST AG

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

IPC: A61K38/00 ,  A61K38/08 ,  A61P43/00 ,  C07K1/06 ,  C07K7/06 ,  C07K7/08 ,  C07K7/18 ,  A61K37/02

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：BR9300761A

公开(公告)日：1993-09-14

申请号：BR9300761

申请日：1993-03-05

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER DR ,  HENNING RAINER DR ,  WAGNER ADALBERT DR ,  GERHARDS HERMANN DR ,  BECKER REINHARD DR ,  SCHOELKENS BERNWARD DR

IPC: A61K31/415 ,  A61K31/4164 ,  A61K31/64 ,  A61P9/10 ,  A61P9/12 ,  C07D233/84 ,  C07D233/86 ,  C07D233/90

Abstract: Compounds of the formula (I) in which R is, for example, ethyl, R is, for example, methyl, n is, for example, zero, R is, for example, COOH and R is, for example, SO2NHCONHCH3 are highly active antagonists of angiotensin II receptors.

公开(公告)号：CS1092A3

公开(公告)日：1992-07-15

申请号：CS1092

申请日：1992-01-03

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT DR ,  ENGLERT HEINRICH DR ,  KLEEMANN HEINZ-WERNER DR ,  GERHARDS HERMANN DR ,  SCHOLKENS BERNWARD PROF DR ,  BECKER REINHARD DR ,  LINZ WOLFGANG DR

IPC: A61K31/40 ,  A61K31/415 ,  A61K31/425 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/64 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D207/34 ,  C07D207/36 ,  C07D233/54 ,  C07D233/66 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D233/90 ,  C07D249/02 ,  C07D255/02 ,  C07D257/02 ,  C07D257/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D453/02 ,  C07D521/00 ,  C07D231/10 ,  C07D207/30 ,  C07D249/04 ,  C07D249/08 ,  A61K31/41

Abstract: Azole derivative of the general formula (I) in which A, L, O, R , X, Y, Z and q have the meanings given, a process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have, for example, the following meanings: R = (C2-C10)-alkyl Z = nitrogen X and Y = independently of one another CR L = -CH2- q = zero or 1 A = biphenyl radical which is substituted, for example, by R R = halogen or hydrogen R = SO2-NH-CO-OR and R = phenyl, are highly active antagonists of angiotensin II receptors.

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：CS9100906A2

公开(公告)日：1991-11-12

申请号：CS90691

申请日：1991-04-02

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT DR ,  HENNING RAINER DR ,  GERHARDS HERMANN DR ,  SCHOLKENS BERNHARD DR

IPC: A61K31/415 ,  A61K31/38 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/423 ,  A61K31/437 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/495 ,  A61K31/505 ,  A61K31/519 ,  A61P9/12 ,  A61P29/00 ,  A61P43/00 ,  C07D233/64 ,  C07D233/84 ,  C07D233/90 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D471/04 ,  C07D487/04

Abstract: The invention relates to compounds of the formula in which X, Y and Z are identical or different and are N or CR , R and R are as defined in the description, L is an alkylene radical, q = 0 or 1, and A is the radical of a fused heterobicycle. The invention furthermore relates to a method for the preparation of the abovementioned compounds, to compositions containing them, and to their use.

公开(公告)号：DE3721723A1

公开(公告)日：1989-01-12

申请号：DE3721723

申请日：1987-07-01

Applicant: HOECHST AG

Inventor： BARTMANN WILHELM PROF DR ,  GUNTRUM EBERHARD DR ,  URBACH HANSJOERG DR ,  WEGMANN HELMUT DR ,  GERHARDS HERMANN DR ,  KAISER JOACHIM DR ,  SCHACHT ULRICH DR

IPC: C07D217/24 ,  C07D217/04 ,  A61K31/47 ,  C07D217/06 ,  C07D217/16 ,  C07D217/20

Abstract: The invention relates to 6-oxodecahydroisoquinoline derivatives of the formula I in which R and R have the meanings indicated. In animal experiments, the compounds of the formula I show both a hypotensive action and an action on the central nervous system.

公开(公告)号：DE2853996A1

公开(公告)日：1980-07-03

申请号：DE2853996

申请日：1978-12-14

Applicant: HOECHST AG

Inventor： LATTRELL RUDOLF DIPL CHEM DR ,  BARTMANN WILHELM DIPL CHEM DR ,  GERHARDS HERMANN DR

IPC: C07D209/08 ,  C07D209/34 ,  C07D215/38 ,  C07D401/12 ,  A61K31/495

Abstract: Phenylpiperazine derivs. of formula (I) and their physiologically acceptable salts are new: (R1 = H or 1-6C alkyl; R2 = H or >=1 of the substits. 1-6C alkyl or alkoxy, halo, CF3, OH, NO2, NH2 or methylenedioxy; R3 = H, OH or 1-6c alkanoyloxy; and n = 1 or 2). (I) have psychotropic and cardio-vascular activities; specifically they are used to treat hypertension and as neuropleptics. Some cpds. have little or no cataleptic activity. They are formulated conventionally pref. for administration at 50-500 mg/day orally, or 10-200 mg/day by injection.