公开(公告)号：AT147375T

公开(公告)日：1997-01-15

申请号：AT93114774

申请日：1993-09-14

Applicant: HOECHST AG

Inventor： LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  KLEEMANN HEINZ-WERNER DR ,  ENGLERT HEINRICH DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR

IPC: A61K31/00 ,  A61K31/155 ,  A61K31/445 ,  A61P1/16 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C311/16 ,  C07C311/21 ,  C07C311/29 ,  C07C317/24 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C323/22 ,  C07C323/65 ,  C07D211/14 ,  C07D211/70 ,  C07D295/14 ,  C07D295/155 ,  A61K31/54 ,  A61K31/45

Abstract: The invention relates to benzoylguanidines of the formula I where R(1) or R(2) is equal to R(3)-S(O)n- or R(4)R(5)N-O2S- and the other substituent R(1) or R(2) is in each case equal to H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O)n or R(4)R(5)N- or 3,4-dehydropiperidine and R(3) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are equal to alkyl or phenylalkyl or phenyl, and in which R(4) and R(5) together can also be a C4-C7-chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can denote a dihydroindol, tetrahydroquinoline or tetrahydroisoquinoline system, and where n is equal to zero, 1 or 2 and their pharmaceutically tolerable salts are outstanding antiarrhythmic agents. They are obtained by a process in which compounds of the formula II in which X stands for a leaving group which can be easily nucleophilically substituted, are reacted with guanidine.

公开(公告)号：DE19518796A1

公开(公告)日：1996-11-28

申请号：DE19518796

申请日：1995-05-22

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: A61K31/165 ,  A61K31/155 ,  A61K31/16 ,  A61P1/16 ,  A61P3/08 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07C277/08 ,  C07C279/22 ,  C07C279/10

Abstract: Fluorocinnamoyl guanidine cpds. of formula (I) and their salts are new. R1-R5 = H or F, provided at least one is F; R6, R7 = H, 1-8C alkyl, 3-8C cycloalkyl, or phenyl (opt. substd. by 1-3 of F, Cl, CF3, Me, OMe and NR9R10; R9, R10 = H, 1-4C alkyl or 1-4C perfluoroalkyl.

公开(公告)号：DE19502795A1

公开(公告)日：1996-08-01

申请号：DE19502795

申请日：1995-01-30

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: C07C279/22 ,  A61K31/155 ,  C07C311/29 ,  C07C311/64 ,  C07C317/28 ,  C07C317/46 ,  C07C323/16 ,  C07C335/32 ,  C07C381/10 ,  C07D207/09 ,  C07D213/40 ,  C07D213/70 ,  C07D215/36 ,  C07D233/54 ,  C07D233/84 ,  C07D235/28 ,  C07D521/00 ,  A01N1/00 ,  A61K31/17 ,  A61K31/18 ,  A61K49/00 ,  C07C277/08 ,  C07C303/40

Abstract: Basic substd. benzoylguanidine derivs. of formula (I) and their salts are new. One of R1-R3 = Xf-CdH2d-B-A-R6 and the others of R1-R3 = H, F, Cl, Br, I, CN, 1-8C alkyl, 2-8C alkenyl, NR35R36 or Zh-CgH2g-R17; R6 = NR7R8, C(=NR9)NR7R8, NR10-C(=NR9)NR7R8 or basic heteroaromatic ring system with 1-9C; R7-R10 = H or 1-4C alkyl; or R7+R8 = C4H8 or CaH2a (opt. with one CH2 replaced by O, S(O)m or NR11; or R8+R9+R10 or R7+R10 = C2H4 or CcH2c (opt. with one CH2 replaced by O, S(O)m or NR11); A = CbH2b (opt. with one or two CH2 replaced by O, CO, CH(OR20), S(O)m, NR20, CONR20, NHCONR20, NR20SO2NHCO, S(=O)(=NR19)NR20 or SO2NR20, or one CH2 replaced by CHR99); R7+R99 form pyrrolidine or piperidine; B = opt. substd. phenylene or naphthylene gp. of formula (i) or (ii); R12, R13 = H, Me, F, Cl, Br, I, CF3 or S(O)mR14; R14, R19 = H or 1-4C alkyl; X = O, CO, CH(OR21), SOm or NR21; R35, R36 = H or 1-6C alkyl; or R35+R36 = (CH2)4-7, with one CH2 opt. replaced by S, NH, NMe or N-benzyl; Z = O, CO, SOm, NR18, CONR18, NHCONR18 or SO2NR18; R17 = H, cyclopropyl, cyclopentyl, cyclohexyl, 1-3C perfluoroalkyl, 1-, 2- or 3-pyrrolyl (opt. substd. by 1-4 of F, Cl, Br, I, CN, 2-8C alkanoyl, 2-8C alkoxycarbonyl, CHO, COOH, CF3, Me and OMe) or 3-8C cycloalkyl or phenyl (both opt. substd. by 1-3 of F, Cl, CF3, Me, OH, OMe, NR37R38, SO2Me and SO2NH2); R11, R18, R20, R21, R37, R38 = H or Me; R4, R5 = H, 1-4C alkyl, F, Cl, OR32, NR33R34 or 1-4C perfluoroalkyl; R32-R34 = H or 1-3C alkyl; a = 5-7; c = 3-5; d = 0-5; g = 0-4; f, h = 0 or 1; m = 0-2.

公开(公告)号：AT138646T

公开(公告)日：1996-06-15

申请号：AT93119781

申请日：1993-12-08

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS DR ,  LANG HANS-JOCHEN DR ,  KLEEMANN HEINZ-WERNER DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR

IPC: A61K31/165 ,  A61K31/155 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C279/22 ,  C07C311/08 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C323/62 ,  C07C323/65 ,  C07D213/56 ,  C07D233/54 ,  C07D239/26 ,  C07D257/02 ,  C07D257/04

Abstract: Benzoylguanidines of the formula I where R(1) is hydrogen, Hal, -NO2, -CN, -CF3, R(4)-SOm or R(5)R(6)N-SO2-, where m is zero to 2, R(4) and R(5) are alk(en)yl or -CnH2n-R(7), n is zero to 4, with R(5) also having the meaning of H, and R(6) is H or (C1-C4)-alkyl, with R(5) and R(6) together being able to be 4 or 5 methylene groups, R(2) is -SR(10), -OR(10), -NHR(10), -NR(10)R(11), -CHR(10)R(12), with R(10) and R(11) being identical or different and being -[CHR(16)]s-(CH2)p-(CHOH)q-(CH2)r-(CH2OH)t-R(21) or -(CH2)p-O(CH2-CH2O)q-R(21), R(12) and R(13) being hydrogen or alkyl, or forming a cycloalkyl together with the carbon atom carrying them, R(14) being H, (cyclo)alkyl or -CnH2n-R(15), R(3) is defined as R(1) or is alkyl, hydrogen or -X-R(22), where X is oxygen, S or NR(16), are described, as are the pharmaceutically tolerated salts thereof. The compounds I possess very good anti-arrhythmic properties but do not have any undesirable salidiuretic properties. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells.

公开(公告)号：CZ9501692A3

公开(公告)日：1996-05-15

申请号：CZ169295

申请日：1995-06-27

Applicant: HOECHST AG

Inventor： SCHWARK JAN-ROBERT DR ,  KLEEMANN HEINZ-WERNER DR ,  LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR

IPC: A61K31/445 ,  A61K31/155 ,  A61K31/165 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  C07C277/00 ,  C07C279/10 ,  C07C279/14 ,  C07C279/22 ,  C07C311/19 ,  C07C311/39 ,  C07C317/44 ,  C07D295/155

CPC classification number: C07D295/155 ,  C07C279/14 ,  C07C311/39

公开(公告)号：CZ9502315A3

公开(公告)日：1996-04-17

申请号：CZ231595

申请日：1995-09-08

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: C07C279/22 ,  A01N1/02 ,  A61K31/155 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61P1/16 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07D213/89 ,  C07D215/60 ,  C07D401/10

CPC classification number: C07D213/89 ,  C07D215/60

公开(公告)号：DE4432101A1

公开(公告)日：1996-03-14

申请号：DE4432101

申请日：1994-09-09

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: A61K31/165 ,  A61K31/155 ,  A61K31/18 ,  A61K31/27 ,  A61K31/275 ,  A61P3/08 ,  A61P3/10 ,  A61P3/12 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/28 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07C229/00 ,  C07C277/08 ,  C07C279/22 ,  C07C317/46 ,  C07C323/44 ,  C07C323/60 ,  C07C323/63 ,  C07C315/04 ,  C07C311/29 ,  A61K31/325 ,  C07C303/36 ,  A01N1/02

Abstract: Benzoyl guanine derivs. of formula(I) and their salts are new. One of the substits. R1-R3 = Y-Ph-Ä(CH2)k-CHR7-CO-R8Ü; and the others = 1-8C alkyl, 2-8C alkenyl, (CH2)mR14, SO2NHC(=Y')NR18R19, H, halo, CN, Z(CH2)p-CqF2q+1, SOuR22, CONR23R24, COR25, SO2NR26R27, OR35 or NR35R36; Ph = phenylene (opt. mono- or di-substd. by Fl, Cl, CF3, Me, OH, OMe or NR37R38); R37, R38 = H or Me; Y = a bond, O, S or NR9; R9 = H or 1-4C alkyl; R7 = OR10 or NR10R11; R10 = H 1-8C alkyl, 1-8C alkanoyl, 1-8C alkoxycarbonyl, benzyl, or benzyloxycarbonyl; R11 = as R10 or trityl; R8 = OR12 or NR12R13; R12, R13 = H, 1-8C alkyl or benzyl; R14 = 3-8C cycloalkyl or phenyl (both opt. substd. by 1-3 F, Cl, CF3, Me, OMe, or NR15R16); R15, R16 = H or Me; Y' = O, S or NR20; R18, R19 = H, 1-8C alkyl, 3-6C alkenyl or (CH2)tR21; or R18+R19 = A; R21 = 5-7C cycloalkyl or phenyl, (both opt. mono- to tri-substd. by F, Cl, OMe or 1-4C alkyl); R20 = as R18 or amidine; Z = a bond, O, S or NR28; R22 = 1-8C alkyl, 3-6C alkenyl, (CH2)nR29 or CF3; R23, R25, R26 = as R22 or H; R24, R27 = H or 1-4C alkyl; or R23+R24, R26+R27 = A; A = (CH2)4 or (CH2)5 (both opt. having a CH2 replaced by O, S, NH, NMe or N-benzyl; R28 = H or 1-3C alkyl; R29 = 3-7C cycloalkyl or phenyl (both opt. substd. by 1-3 F, Cl, CF3, Me, OMe or NR30R31; R30, R31 = H or 1-4C alkyl; R35, R36 = H or 1-6C alkyl; or R35+R36 = (CH2)y (opt. having a CH2 gp. replaced by O, S, NH, NMe or N-benzyl); R4, R5 = H, 1-4C alkyl, F, Cl, OR32, NR33R34 or CrF2r+1; R32-R34 = H or 1-3C alkyl; k, n, t = 0-4; m, u, p = 0-2; q = 1-6; r = 1-4; and y = 4-7.

公开(公告)号：CZ9502316A3

公开(公告)日：1996-03-13

申请号：CZ231695

申请日：1995-09-08

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS DR ,  KLEEMANN HEINZ WERNER DR ,  LANG HANS JOCHEN DR ,  SCHWARK JAN ROBERT DR ,  ALBUS UDO DR ,  SCHOLZ WOLFGANG DR

IPC: A61K31/165 ,  A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/02 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07C22/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/29 ,  C07C311/38 ,  C07C317/44 ,  C07C323/62 ,  C07C317/46 ,  A01N1/02 ,  C07C303/36 ,  C07C315/04

CPC classification number: C07C317/44 ,  C07C279/22

公开(公告)号：DE4421536A1

公开(公告)日：1995-12-21

申请号：DE4421536

申请日：1994-06-20

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: A61K31/165 ,  A01N1/02 ,  A61K31/16 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P31/04 ,  A61P35/00 ,  A61P37/08 ,  C07C277/08 ,  C07C279/22 ,  A61K31/155 ,  C07D521/00

Abstract: Perfluoroalkyl-substd. phenylalkenoyl-guanidine derivs. of formula (I) and their salts are new. Ra and Rb=H, halogen, CN, OH, OR6, 1-8C alkyl, Or(CH2)aRf, 3-8C cycloalkyl or NR7R8; r=0 or 1; a=0-4; Rf=1-8C perfluoroalkyl; R6=1-8C alkyl, 1-4C perfluoroalkyl, 3-8C alkenyl, 3-8C cycloalkyl, or phenyl or benzyl ring-substd. by 0-3 of F, Cl, CF3, Me, OMe and NR9R10; R9 and R10=H, 1-4C alkyl or 1-4C perfluoroalkyl; R7 and R8=gps. as defined for R6, or R7+R8=4 or 5 CH2 gps., one of which is opt. replaced by O, S, NH, NMe or NCH2Ph; x and y=0-2; Rc and Rd=H, halogen, CN, OR6, 1-8C alkyl, Or(CH2)aRf or 3-8C cycloalkyl; R1-R5=H, 1-8C alkyl, Or(CH2)aRf, 3-8C cycloalkyl, halogen or CN; provided that at least one of Ra, Rb, Rc, Rd, R1, R2, R4 and R5 is Or(CH2)aRf, and that R3 is not Or(CH2)aRf.

公开(公告)号：AU1786195A

公开(公告)日：1995-11-16

申请号：AU1786195

申请日：1995-05-03

Applicant: HOECHST AG

Inventor： SCHWARK JAN-ROBERT DR ,  KLEEMAN HEINZ-WERNER DR ,  LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR

IPC: A61K31/165 ,  A61K31/47 ,  A61K31/472 ,  A61P3/08 ,  A61P3/10 ,  A61P9/06 ,  A61P9/10 ,  A61P13/08 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22 ,  C07D215/00 ,  C07D215/48 ,  C07D215/54 ,  C07D215/56 ,  C07D217/00 ,  C07D217/02 ,  C07D217/26 ,  A61K31/135

Abstract: New bicyclic heteroaryl-carboxy-guanidine cpds. and their salts have two fused 6-membered rings contg. up to 4 unsubstd. ring N atoms. The other ring members are C atoms, opt. substd. e.g. by halo, alkyl, alkoxy, alkenyl, alkynyl, amino, carboxyguanidine, cyano, alkylthio, acyl, carboxamido, perfluoroalkyl, (poly)hydroxyalkyl, alkanoylalkyl, aminosulphonyl, (thio)ureidosulphonyl, heteroaryl, phenoxy, phenylthio or phenylamino, where the phenyl rings are opt. substd. by heterocyclyl, (poly)hydroxyalkyl or (poly)hydroxyalkylcarbonyl; or two substits. together form a satd. gp. that completes a fused ring.