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公开(公告)号:AT114320T
公开(公告)日:1994-12-15
申请号:AT90115455
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
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.
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公开(公告)号:DE59102259D1
公开(公告)日:1994-08-25
申请号:DE59102259
申请日:1991-11-11
Applicant: HOECHST AG
Inventor: HEITSCH HOLGER DR , HENNING RAINER DR , LINZ WOLFGANG DR , SCHOELKENS BERNWARD PROF DR , 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.
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公开(公告)号:DK0417473T3
公开(公告)日:1993-12-13
申请号:DK90115230
申请日:1990-08-08
Applicant: HOECHST AG
Inventor: LINZ WOLFGANG DR , SCHOLZ WOLFGANG DR , URBACH HANSJOERG DR , SCHOELKENS BERNWARD PROF DR , WIEMER GABRIELE DR , HENNING RAINER DR , TEETZ VOLKER DR
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.
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34.
公开(公告)号:AT94409T
公开(公告)日:1993-10-15
申请号:AT90115230
申请日:1990-08-08
Applicant: HOECHST AG
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公开(公告)号:DE4131325A1
公开(公告)日:1993-04-01
申请号:DE4131325
申请日:1991-09-20
Applicant: HOECHST AG
Inventor: HEITSCH HOLGER DR , WAGNER ADALBERT DR , KLEEMANN HEINZ-WERNER DR , GERHARDS HERMANN DR , SCHOELKENS BERNWARD PROF DR
IPC: C07D235/08 , C07D409/06 , C07D471/04 , C07D487/04 , C07D519/00
Abstract: Fused imidazole derivs. of formula (I) and their physiologically acceptable salts are new. In (I) X = a monocyclic gp. with 3, 4 or 5 ring atoms or a bicyclic gp. with 8-10 ring atoms, which is completely or partially hydrogenated and in which one or more CH or CH2 gps. are replaced with N, NH or O; R1 = 1-10C alkyl, 3-10C alkenyl, 3-10C alkynyl, (these 3 gps. being opt. mono-substd. with CO2R6 and opt. having 1 to all of their H atoms replaced with F), etc.. R2, R3, R4 and R5 = each H, halogen, OH, CN, NO2, sulpho, formyl, benzoyl, 1-8C acyl, 1-8C acyloxy, SH, etc.. R6 = H, 1-8C alkyl (in which 1 to all H atoms are opt. replaced with F) 3-8C cycloalkyl, Ph, benzyl; L = 1-3C alkane diyl; R12 and R13 = each H, halogen, NO2, 1-4C alkyl or 1-2C alkoxy; q = 0-1; A = either a heterocycle with 5-10 ring atoms, which is mono or bicyclic and in which up to 9 ring atoms are C and which is opt. substd. with up to 6 (esp. up to 3) opt. different gps. R14 and R15; or A is opt. substd. biphenyl.
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公开(公告)号:AT252567T
公开(公告)日:2003-11-15
申请号:AT97107623
申请日:1997-05-09
Applicant: HOECHST AG
Inventor: WAGNER ADALBERT DR , HEITSCH HOLGER DR , NOELKEN GERHARD DR , WIRTH KLAUS DR , SCHOELKENS BERNWARD PROF DR
IPC: C07D277/60 , A61K31/38 , A61K31/395 , A61K31/41 , A61K31/425 , A61K31/428 , A61K31/53 , A61P43/00 , C07D253/10 , C07D277/62 , C07D277/64 , C07D277/66 , C07D277/68 , C07D277/70 , C07D277/74 , C07D277/82 , C07D417/12
Abstract: Sulphur-containing bradykinin antagonist compounds of formula (I) and their salts are claimed: one of X1-X3 = COR , and the other X1-X4 = N, CR ; R ,R = H, halo, 1-6C alkyl, OR , SR , NHR , 6-12C aryl, (6-12C aryl)(1-3C alkyl), C(O)OR , C(O)H, 2-5C alkenyl, NO2, SO3R , CN, C(O)NHR , where alkyl, aryl, alkenyl may be substituted by C(O)(O)o(1-5C alkyl), OR , SR , NO2, CN, NHR , halo; R = (II); R ,R = e.g. H; R -R = H, 1-5C alkyl, 3-5C alkenyl, etc.; A = amino acid e.g. methionine, alanine, phenylalanine, etc.; R = H, C(O)(O)o(1-5C alkyl), C(O)(O)o(11-3C alkyl)(6-10C aryl); R = e.g. C(O)DE; D = 2-5C alkendiyl, 1-8C alkandiyl, (CH2)nYo(CH2)m, etc., where any of the groups are optionally substituted by e.g. OR ; E = H, 6-10C aryl, 1-9C heteroaryl, etc.;Y = O, S, NR ; n,m = 0-6; o = 0 or 1.
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公开(公告)号:DK0560177T3
公开(公告)日:2003-04-14
申请号:DK93103301
申请日:1993-03-02
Applicant: HOECHST AG
Inventor: BECKER REINHARD DR , HENNING RAINER DR , WAGNER ADALBERT DR , SCHOELKENS BERNWARD PROF DR , HEITSCH HOLGER DR , GERHARDS HERMANN DR
IPC: A61K31/4164 , A61K31/64 , A61P9/10 , A61P9/12 , C07D233/84 , A61K31/415 , 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.
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公开(公告)号:GR3033415T3
公开(公告)日:2000-09-29
申请号:GR20000401105
申请日:2000-05-16
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
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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公开(公告)号:DE59209292D1
公开(公告)日:1998-05-28
申请号:DE59209292
申请日:1992-01-01
Applicant: HOECHST AG
Inventor: WAGNER ADALBERT DR , ENGLERT HEINRICH DR , KLEEMANN HEINZ-WERNER DR , GERHARDS HERMANN DR , SCHOELKENS BERNWARD PROF DR , BECKER REINHARD DR , LINZ WOLFGANG DR , CAILLE JEAN-CLAUDE , VEVERT JEAN-PAUL
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
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.
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公开(公告)号:DE19620508A1
公开(公告)日:1997-11-27
申请号:DE19620508
申请日:1996-05-22
Applicant: HOECHST AG
Inventor: WAGNER ADALBERT DR , HEITSCH HOLGER DR , NOELKEN GERHARD DR , WIRTH KLAUS DR , SCHOELKENS BERNWARD PROF DR
IPC: C07D277/60 , A61K31/38 , A61K31/395 , A61K31/41 , A61K31/425 , A61K31/428 , A61K31/53 , A61P43/00 , C07D253/10 , C07D277/62 , C07D277/64 , C07D277/66 , C07D277/68 , C07D277/70 , C07D277/74 , C07D277/82 , C07D417/12 , C07D521/00
Abstract: Sulphur-containing bradykinin antagonist compounds of formula (I) and their salts are claimed: one of X1-X3 = COR , and the other X1-X4 = N, CR ; R ,R = H, halo, 1-6C alkyl, OR , SR , NHR , 6-12C aryl, (6-12C aryl)(1-3C alkyl), C(O)OR , C(O)H, 2-5C alkenyl, NO2, SO3R , CN, C(O)NHR , where alkyl, aryl, alkenyl may be substituted by C(O)(O)o(1-5C alkyl), OR , SR , NO2, CN, NHR , halo; R = (II); R ,R = e.g. H; R -R = H, 1-5C alkyl, 3-5C alkenyl, etc.; A = amino acid e.g. methionine, alanine, phenylalanine, etc.; R = H, C(O)(O)o(1-5C alkyl), C(O)(O)o(11-3C alkyl)(6-10C aryl); R = e.g. C(O)DE; D = 2-5C alkendiyl, 1-8C alkandiyl, (CH2)nYo(CH2)m, etc., where any of the groups are optionally substituted by e.g. OR ; E = H, 6-10C aryl, 1-9C heteroaryl, etc.;Y = O, S, NR ; n,m = 0-6; o = 0 or 1.
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