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公开(公告)号:AT165351T
公开(公告)日:1998-05-15
申请号:AT91122406
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:DK0455133T3
公开(公告)日:1997-08-25
申请号:DK91106663
申请日:1991-04-25
Applicant: HOECHST AG
Inventor: HENKE STEPHAN DR , HOCK FRANZ DR , BREIPOHL GERHARD DR , KNOLLE JOCHEN DR , SCHOELKENS BERNWARD PROF DR
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.
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公开(公告)号:DK0413277T3
公开(公告)日:1995-04-18
申请号:DK90115455
申请日:1990-08-11
Applicant: HOECHST AG
Inventor: GERHARDS HERMANN DR , KNOLLE JOCHEN DR , HENKE STEPHAN DR , BREIPOHL GERHARD DR , SCHOELKENS BERNWARD PROF 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:AT108656T
公开(公告)日:1994-08-15
申请号:AT91119183
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:DK0795547T3
公开(公告)日:2000-09-18
申请号:DK97103163
申请日:1997-02-27
Applicant: HOECHST AG
Inventor: SCHOELKENS BERNWARD PROF DR , HEITSCH HOLGER DR , WAGNER ADALBERT DR , WIRTH KLAUS 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:GR3031543T3
公开(公告)日:2000-01-31
申请号:GR990402630
申请日:1999-10-15
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
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.
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公开(公告)号:DE19610784A1
公开(公告)日:1997-09-25
申请号:DE19610784
申请日:1996-03-19
Applicant: HOECHST AG
Inventor: WAGNER ADALBERT DR , HEITSCH HOLGER DR , NOELKEN GERHARD DR , WIRTH KLAUS DR , SCHOELKENS BERNWARD PROF DR
IPC: C07D237/28 , A61K31/345 , A61K31/47 , A61K31/495 , A61K31/53 , A61P43/00 , C07D215/04 , C07D215/26 , C07D239/72 , C07D239/74 , C07D241/36 , C07D241/44 , C07D253/04 , C07D253/065 , C07D257/10 , C07D237/30 , C07D241/40 , C07D253/10 , C07D257/12 , C07C205/07
Abstract: Fluoroalkyl- and fluoroalkoxy-substituted benzyloxy-azaheterocyclic compounds of formula (I) and their salts are new: X1-X3 = N or CR ; R , R = H or halo; R , R = H, halo, 1-5C alkyl or 2-5C alkenyl; R = 2-5C alkenediyl, halo, OR , SR , NHR , -COOR or COOH; 1-6C alkyl, 6-12C aryl or 6-12C aryl-1-3C alkyl (all optionally substituted by e.g. OR , SR , NO2, CN, NHR or halo); R , R = H, 1-5C alkyl, 3-5C alkenyl or 6-12C aryl-1-3C alkyl; R = 1-5C alkyl or 1-5C alkoxy (both substituted by 1 or more F or Cl); B = amino acid; D = 2-5C alkanediyl, 1-5C alkanediyl or -(CH2)n-Yp-(CH2)m-; E = O or S; Y = O, S or NR ; n, m = 0-3; o = 1-3; and p = 0 or 1.
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公开(公告)号:GR3023172T3
公开(公告)日:1997-07-30
申请号:GR970400829
申请日:1997-04-18
Applicant: HOECHST AG
Inventor: BREIPOHL GERHARD DR , HENKE STEPHAN DR , KNOLLE JOCHEN DR , SCHOELKENS BERNWARD PROF DR , HOCK FRANZ DR
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.
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公开(公告)号:DE19537334A1
公开(公告)日:1997-04-10
申请号:DE19537334
申请日:1995-10-09
Applicant: HOECHST AG
Inventor: TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR , SCHOELKENS BERNWARD PROF DR , KLEMM PETER DR , HUELS CHRISTOPH DR , SEIFFGE DIRK DR
IPC: C07D295/20 , A61K31/215 , A61K31/33 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/495 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/08 , C07D207/16 , C07D211/34 , C07D211/62 , C07D405/00 , C07H15/203 , C07H15/207 , C07H17/00 , C07H19/04 , C07H15/26 , C07H1/00
Abstract: Piperidine and pyrrolidine derivs. of formula (I) are new. Z = pyranoside, pyranosyl residue bound via. the 6-position, alkyl pyranoside bound via the 6-position, furanoside, furanosyl residue bound via the 5-position, alkyl furanoside bound via the 5-position or a polyalcohol; A = O, CH2 or S; R ,R = H, (CH2)mX or CH2O(CH2)mX ; or R + R = 5- or 6-membered carbocycle or heterocycle with at least one substit. R ,R or R ; E = N, C or CH; R = (CH2)pCOOH, (COOH)2, (CH2)pCH(COOH)2, (CH2)p(COOH)2, (CH2)pC(CH2-C6H5)(COOH)2, CONHC(COOH)2 or a gp. of formula (a)-(d); m = 1-20; p = 0-10; q, r = 0-3;m = 1-3; provided that q + r + n = 4 or 5; R -R = H, OH, O(CH2)wX or CH2O(CH2)wX ; w = 1-19; Y ,Y = O, NH or S; and X -X = H, NH2, COOH, OH, CH2OH, CH2NH2, 1-20C alkyl or 6-10C aryl.
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公开(公告)号:AT149519T
公开(公告)日:1997-03-15
申请号:AT91106663
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
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.
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