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公开(公告)号:CZ9603382A3
公开(公告)日:1998-05-13
申请号:CZ338296
申请日:1996-11-18
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , BRENDEL JOACHIM DR , SCHWARK JAN-ROBERT DR , WEICHERT ANDREAS DR , LANG HANS JOCHEN DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: A61K31/165 , A61P1/16 , A61P3/08 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C279/20 , C07C279/22
CPC classification number: C07C279/22
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公开(公告)号:DK0556672T3
公开(公告)日:1998-03-02
申请号:DK93101840
申请日:1993-02-05
Applicant: HOECHST AG
Inventor: LINZ WOLFGANG DR , SCHOLZ WOLFGANG DR , LANG HANS-JOCHEN DR , ENGLERT HEINRICH DR , ALBUS UDO DR , MANIA DIETER DR
IPC: A61K31/155 , A61K31/165 , A61K31/445 , A61P1/16 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P35/00 , C07C279/22 , C07D213/65 , C07D295/14 , C07D295/155
Abstract: There are described benzoylguanidines of the formula I in which R(1) or R(2) is an amino group -NR(3)R(4), where R(3) and R(4) are equal to H, (cyclo)alkyl or R(3) is equal to phenyl-(CH2)p- where p = 0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) together can also be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF3, CmF2m+1-CH2-, benzyl or phenoxy, and their pharmaceutically tolerable salts. The compounds according to the invention have very good antiarrhythmic properties, such as they show, for example, in the case of oxygen deficiency symptoms. The compounds are used as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage, in particular during the induction of ischaemically induced cardiac arrhythmias.
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公开(公告)号:GR3024927T3
公开(公告)日:1998-01-30
申请号:GR970402568
申请日:1997-10-03
Applicant: HOECHST AG
Inventor: LANG HANS-JOCHEN DR , KLEEMANN HEINZ-WERNER DR , SCHOLZ WOLFGANG DR , ALBUS UDO DR
IPC: A61K31/165 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , C07C277/08 , C07C279/22 , C07C311/15 , C07C317/44 , C07C317/46 , C07C323/62 , C07D241/28
Abstract: There are described benzoylguanidines of the formula I where R(1) is H, Hal, -NO2, -C IDENTICAL N, Xo-(CH2)p-(CF2)q-CF3, R(5)- SOm, R(6)-CO- or R(6)R(7)NO-SO2-, where X is O, S, NR(14), m is 0-2, o is 0, 1, p is 0-2, q is 0-6, R(5) and R(6) are alk(en)yl, -CnH2n-R(8), CF3, n is 0-4, R(8) is cycloalkyl, phenyl, R(6) also being H, R(2) is where Y is O, -S- or -NR(12)-; R(11), R(12) = H, alkyl, and h is zero or 1, and i, j and k are 0-4, but where h, i and k are not simultaneously zero, R(3) is defined as R(1), or is alkyl, -X-R(13) where X is O, S, NR(14), R(14) is H, alkyl, R(13) is H, (cyclo)alkyl, -CbH2b-R(15) where b is 0-4, R(15) is phenyl, R(4) is H, -OR(16) or -NR(16)R(17) where R(16), R(17) are H, alkyl and their pharmaceutically tolerable salts. They are obtained from a compound II by reaction with guanidine, in which R(1) to R(4) have the meaning indicated and L is a leaving group which can be easily nucleophilically substituted. The compounds are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they also preventively inhibit or severely decrease the pathophysiological processes in the formation of ischaemically induced damage, in particular in the elicitation of ischaemically induced cardiac arrhythmias.
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公开(公告)号:AT161532T
公开(公告)日:1998-01-15
申请号:AT94111575
申请日:1994-07-25
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , LANG HANS-JOCHEN DR , SCHWARK JAN-ROBERT DR , WEICHERT ANDREAS DR , SCHOLZ WOLFGANG DR , ALBUS UDO DR
IPC: C07D233/64 , A01N1/02 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P13/08 , A61P13/12 , A61P15/00 , A61P25/28 , A61P35/00 , A61P43/00 , C07C279/22 , C07D207/333 , C07D207/337 , C07D213/30 , C07D231/12 , C07D233/54 , C07D233/58 , C07D521/00
Abstract: The invention relates to benzoylguanidines of the formula I where R(1) is H, Hal, -NO2, -C IDENTICAL N, Xo-(CH2)p-(CF2)q-CF3, R(5)SOm, R(6)-CO-, R(6)R(7)N-CO- or R(6)R(7)N-SO2-, where X is oxygen, S, NR(14), m is zero, 1 or 2, o is zero, 1, p is zero, 1, 2, q is zero, 1, 2, 3, 4, 5, 6, R(5) and R(6) are alk(en)yl, -CnH2n-R(8), CF3, n is zero, 1, 2, 3 or 4, R(8) is cycloalkyl, phenyl, where R(6) also has the meaning of H, R(7) is H or alkyl; R(2) is R(11) is (C1-C9)-heteroaryl, Y is oxygen, -S- or NR(12)-, R(12) is H, (C1-C4)-alkyl; R(3) is defined as R(1), or is alkyl, -X-R(13) where X is oxygen, S, NR(14), R(14) is H, (C1-C3)-alkyl, R(13) is H, (cyclo)alkyl, -CbH2b-R(15) where b is zero to 4 and R(15) is phenyl; R(4) is hydrogen, -OR(16), -NR(16)R(17) or CrF2r+1 where R(16), R(17) independently are hydrogen, (C1-C3)-alkyl, r is 1-4 and their pharmaceutically tolerable salts. The compounds I are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and for infarct treatment and for the treatment of angina pectoris.
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公开(公告)号:ID17038A
公开(公告)日:1997-12-04
申请号:ID971869
申请日:1997-06-02
Applicant: HOECHST AG
Inventor: WEICHERT ANDREAS DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , LANG HANS JOCHEN DR , SCHWARK JAN-ROBERT DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: A61K31/165 , A01N1/02 , A01N47/44 , A61K31/155 , A61P3/00 , A61P3/06 , A61P7/04 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P35/00 , C07C279/22 , C07C319/20 , C07C323/62
Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: R = H; F; Cl; Br; I; CN; NO2; 1-8 C alkyl; 1-8 C alkoxy; 3-8 C cycloalkyl; 3-8 C cycloalkoxy; Xa-(CH2)b-(CF2)c-CF3; SR ; OR ; CR R R ; Ph, etc.;R or R = OCOR and the other = R ;R , R = H; 1-4C alkyl; 1-4C alkoxy; etc.;X = e.g. O; a = 0 or 1;b = 0-2;c = 0-3;R = -CfH2f-Q;Q = e.g. 3-8 C cycloalkyl;f = 0-2; R , R = H; 1-4 C alkyl; or R ; R = e.g. 1-8C alkyl.
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公开(公告)号:DE19608161A1
公开(公告)日:1997-09-11
申请号:DE19608161
申请日:1996-03-04
Applicant: HOECHST AG
Inventor: WEICHERT ANDREAS DR , ALBUS UDO DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , LANG HANS-JOCHEN DR , SCHOLZ WOLFGANG DR , SCHWARK JAN-ROBERT DR
IPC: A61K31/165 , A01N1/02 , A61K31/155 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/08 , A61P25/00 , A61P35/00 , A61P43/00 , C07C279/10 , C07C279/20 , C07C279/22 , C07C277/08 , C07D215/02 , C07D217/02 , C07D213/04
Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: where R1 = H, F, Cl, Br, I, CN, NO2, 1-8C alkyl, 1-8C alkoxy, 3-8C cycloalkyl, 3-8C cycloalkoxy, Xa-(CH2)b-(CF2)c-CF3, SR10, OR10, CR10R11R12; or phenyl, naphthyl, biphenylyl, or 1-9C (sic) heteroaryl bonded via C or N and all optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; or SR13, OR13, NHR13, NR13R14, CHR13R15, CR15R16-OH, C IDENTICAL CR18, CR19=CHR18, ÄCR20R21Ük-CO, ÄCR22R23Ül-R24; one of R2, R3 = hydroxy the other as R1; R4 = 1-4C alkyl, 1-4C alkoxy, F, Cl, Br, I or (CH2)n-(CF2)o-CF3; X = O, S, NR5; a = 0-1; b = 0-2; c = 0-3; R5 = H, 1-4C alkyl, CdH2d-R6; d = 0-4; R6 = 3-8C cycloalkyl; or phenyl, biphenylyl or naphthyl (each optionally mono- to tri-substituted with F, Cl, CF3, methyl, methoxy, or NR7R8); R7, R8 = H or 1-4C alkyl; R10 = CfH2f-3-8C cycloalkyl; or phenyl optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; f = 0-2; R11, R12 = as R10, H or 1-4C alkyl; k = 0-4; l = 0-4; R13, R14 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)j-R17, or (CH2)g-O-(CH2CH2O)h-R24; R17 = H, CH3; g, h, i = 0-4; j = 1-4; R15, R16 = H or 1-6C alkyl; or CR15R16 = 3-8C cycloalkyl; R18 = phenyl optionally mono- to tri-substituted with F, Cl, CF3, CH3, OCH3 or NR25R26; or 3-8C cycloalkyl; or 1-9C (sic) heteroaryl optionally substituted as for phenyl; or 1-6C alkyl optionally substituted by 1-3 OH; R25, R26 = H or 1-4C alkyl; R19-R23 = H or CH3; R24 = H, 1-6C alkyl, 3-8C cycloalkyl, CmH2m-R18; m = 1-4; n = 0-1; and o = 0-1.
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公开(公告)号:ID16042A
公开(公告)日:1997-08-28
申请号:ID970554
申请日:1997-02-24
Applicant: HOECHST AG
Inventor: ALBUS UDO DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ WERNER DR , LANG HANS JOCHEN DR , SCHOLZ WOLFGANG DR , SCHWARK JAN ROBERT DR , WEICHERT ANDREAS DR
IPC: A61K31/165 , A61K31/155 , A61P1/16 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C279/10 , C07C279/20 , C07C279/22 , C07C279/02
Abstract: Ortho-substituted benzoylguanidines of formula (I) and their salts are new: R2, R3 = H, Cl, Br, I, 1-8C alkyl, 3-8C cycloalkyl or OR5; provided that one, but not both of R2 or R3 = H; R5 = 1-8C alkyl, or CdH2d-(3-8C cycloalkyl); and d = 0-2.
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公开(公告)号:DE19540995A1
公开(公告)日:1997-05-07
申请号:DE19540995
申请日:1995-11-03
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , BRENDEL JOACHIM DR , SCHWARK JAN-ROBERT DR , WEICHERT ANDREAS DR , LANG HANS-JOCHEN DR , ALBUS UDO DR , SCHOLZ WOLFGANG DR
IPC: A61K31/165 , A61K31/18 , A61P1/16 , A61P3/08 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P41/00 , A61P43/00 , C07C279/18 , C07C313/02 , C07C313/06 , C07C381/10 , C07C311/21 , C07C311/15 , C07C303/40 , C07C317/48 , A61K49/00
Abstract: Sulphonimidamides of formula R1N=S(O)(R2)N(R4)(R3) (I) and their salts are new: at least one of R1-R3 = a benzoylguanidine group of formula (a) optionally substituted in the phenyl ring by 1-4 of 1-8C alkyl, 2-8C alkenyl, (CH2)mR14, halo, CN, CF3, R22SO2, R23R24NCO, R25CO, R26R27NSO2, OR35, SR35 or NR35R36; m = 0-2; R14 = 3-8C cycloalkyl, phenyl optionally substituted by 1-3 of F, Cl, CF3, Me, OMe or NR15R16; R15, R16 = H or Me; R22, R23, R25, R26 = 1-8C alkyl, 2-8C alkenyl, (CH2)nR29 or CF3; or R23+R24, R26+R27 = 5-6 methylene groups with optionally one CH2 replaced by O, S, NH, NMe or N-benzyl; or R23, R25, R26 = H; n = 0-4; R29 = 3-7C cycloalkyl, phenyl optionally substituted by 1-3 of F, Cl, CF3, Me, OMe or NR30R31; R30, R31 = H or 1-4C alkyl; R24, R27 = H or 1-4C alkyl; R35, R36 = H or 1-6C alkyl; or R35+R36 = 4-7 methylene groups with optionally one CH2 replaced by O, S, NH, NMe or N-benzyl; or R35 = phenyl optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, SO2R5, SO2NR6R7 or NR32R33; R5 = 1-6C alkyl; R6, R7 = H or 1-4C alkyl; R32, R33 = H or 1-4C alkyl; or R35 = 1-9C heteroaryl optionally substituted by 1-3 of F, Cl, CF3, CH3, OMe, OH, NH2, NHMe or N(Me)2; the remaining R1-R3 = 1-8C alkyl or (CH2)pR10; or the remaining R1, R2 = H; p = 0-4; R10 = phenyl optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, SO2NR17R8 or SO2R9; R17, R8 = H or 1-4C alkyl; R9 = 1-4C alkyl; and R4 = H or 1-4C alkyl.
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公开(公告)号:GR3022136T3
公开(公告)日:1997-03-31
申请号:GR960403574
申请日:1996-12-20
Applicant: HOECHST AG
Inventor: LANG HANS-JOCHEN DR , KLEEMANN HEINZ-WERNER DR , SCHOLZ WOLFGANG DR , ALBUS UDO DR
IPC: A61K31/165 , A61K31/415 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/47 , A61K31/472 , A61P9/06 , A61P9/08 , A61P9/10 , C07C279/22 , C07C311/08 , C07C317/44 , C07C323/62 , C07D207/32 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/66 , C07D213/68 , C07D213/70 , C07D215/20 , C07D215/26 , C07D217/02 , C07D217/24 , C07D233/54 , C07D249/08 , C07D521/00
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公开(公告)号:DE19526381A1
公开(公告)日:1997-01-23
申请号:DE19526381
申请日:1995-07-19
Applicant: HOECHST AG
Inventor: WEICHERT ANDREAS DR , BRENDEL JOACHIM DR , KLEEMANN HEINZ-WERNER DR , LANG HANS JOCHEN DR , SCHWARK JAN-ROBERT DR , SCHOLZ WOLFGANG DR , ALBUS UDO DR
IPC: A61K49/00 , A01N1/02 , A61K31/155 , A61K31/165 , A61K31/18 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P41/00 , C07C303/40 , C07C311/16 , C07C315/04 , C07C317/44
Abstract: Benzoyl-guanidine derivs. of formula (I) and their salts are new: R1 = R4-SOm, R5R6N-SO2-, -Op-(CH2)q-(CF2)r-CF3, -SR10, -OR10 or -CR10R11R12; m = 1-2; R4, R5 = 1-8C alkyl, 3-6C alkenyl, CF3 or -CnH2n-R7; n = 0-4; R6 = H or 1-4C alkyl; R7 = 3-8C cycloalkyl or Ph (opt. substd. with 1-3 substits. from F, Cl, CF3, Me, OMe and NR8R9; R8, R9 = H or 1-4C alkyl; R5 = H; or R5 + R6 = 4-5C methylene group (with opt. replacement of a CH2 by O, S, NH, NMe or N-benzyl; ; p = 0-1; q = 0-2; r = 0-3;R10, R11, R12 = H, 1-8C alkyl, CsH2s-(3-8C cycloalkyl) or an aromatic gp. chosen from pyridyl, pyrrolyl, quinolyl, isoquinolyl, imidazolyl or Ph (in which the aromatic system may be opt. 1-3 times substd. by F, Cl, CF3, Me, OMe, OH, NH2, NHMe or N(Me)2; s = 0-2; R2 = -(CH2)u-(CF2)t-CF3; t = 0-3; u = 0-1; R3 = H or as for R1.
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