公开(公告)号：GR3021397T3

公开(公告)日：1997-01-31

申请号：GR960402615

申请日：1996-10-17

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS DR ,  LANG HANS-JOCHEN ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/33 ,  A61K31/435 ,  A61K31/44 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/02 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P15/04 ,  A61P43/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/37 ,  C07C315/04 ,  C07C317/32 ,  C07C317/44 ,  C07C323/60 ,  C07D213/56

Abstract: Benzoylguanidines of the formula I with R(1) equal to R(4)-SOm or R(5)R(6)N-SO2- with R(4) and R(5) equal to alk(en)yl, -CnH2n-R(7), and with R(7) equal to cycloalkyl or phenyl, where R(5) can also mean H, R(6) equals H or C1-C4-alkyl, R(2) is hydrogen, (cyclo)alk(en)(yn)yl, aryl and hetaryl R(3) is defined as R(2), and their pharmaceutically tolerated salts, are described. Compounds I are obtained by reacting compounds of the formula II with guanidine, in which L is a leaving group which can easily undergo nuclophilic substitution. Compounds I are outstandingly suitable as antiarrhythmic drugs with cardioprotective component for the treatment and prophylaxis of infarct and for treating angina pectoris, and they also greatly reduce preventively the pathophysiological processes in the development of ischaemia-induced damage. Furthermore, I are distinguished by a potent inhibitory action on cell proliferation. They can thus be used as antiatherosclerotics, remedies for the late complications of diabetes, cancers, fibrotic disorders such as pulmonary, hepatic or renal fibrosis. They are effective inhibitors of the cellular sodium-proton antiporter (Na /H exchanger).

公开(公告)号：ES2092729T3

公开(公告)日：1996-12-01

申请号：ES93110195

申请日：1993-06-25

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS DR ,  LANG HANS-JOCHEN ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/33 ,  A61K31/435 ,  A61K31/44 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/02 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P15/04 ,  A61P43/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/37 ,  C07C315/04 ,  C07C317/32 ,  C07C317/44 ,  C07C323/60 ,  C07D213/56

Abstract: Benzoylguanidines of the formula I with R(1) equal to R(4)-SOm or R(5)R(6)N-SO2- with R(4) and R(5) equal to alk(en)yl, -CnH2n-R(7), and with R(7) equal to cycloalkyl or phenyl, where R(5) can also mean H, R(6) equals H or C1-C4-alkyl, R(2) is hydrogen, (cyclo)alk(en)(yn)yl, aryl and hetaryl R(3) is defined as R(2), and their pharmaceutically tolerated salts, are described. Compounds I are obtained by reacting compounds of the formula II with guanidine, in which L is a leaving group which can easily undergo nuclophilic substitution. Compounds I are outstandingly suitable as antiarrhythmic drugs with cardioprotective component for the treatment and prophylaxis of infarct and for treating angina pectoris, and they also greatly reduce preventively the pathophysiological processes in the development of ischaemia-induced damage. Furthermore, I are distinguished by a potent inhibitory action on cell proliferation. They can thus be used as antiatherosclerotics, remedies for the late complications of diabetes, cancers, fibrotic disorders such as pulmonary, hepatic or renal fibrosis. They are effective inhibitors of the cellular sodium-proton antiporter (Na /H exchanger).

公开(公告)号：DE59304166D1

公开(公告)日：1996-11-21

申请号：DE59304166

申请日：1993-06-25

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS DR ,  LANG HANS-JOCHEN ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/33 ,  A61K31/435 ,  A61K31/44 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/02 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P15/04 ,  A61P43/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/37 ,  C07C315/04 ,  C07C317/32 ,  C07C317/44 ,  C07C323/60 ,  C07D213/56

Abstract: Benzoylguanidines of the formula I with R(1) equal to R(4)-SOm or R(5)R(6)N-SO2- with R(4) and R(5) equal to alk(en)yl, -CnH2n-R(7), and with R(7) equal to cycloalkyl or phenyl, where R(5) can also mean H, R(6) equals H or C1-C4-alkyl, R(2) is hydrogen, (cyclo)alk(en)(yn)yl, aryl and hetaryl R(3) is defined as R(2), and their pharmaceutically tolerated salts, are described. Compounds I are obtained by reacting compounds of the formula II with guanidine, in which L is a leaving group which can easily undergo nuclophilic substitution. Compounds I are outstandingly suitable as antiarrhythmic drugs with cardioprotective component for the treatment and prophylaxis of infarct and for treating angina pectoris, and they also greatly reduce preventively the pathophysiological processes in the development of ischaemia-induced damage. Furthermore, I are distinguished by a potent inhibitory action on cell proliferation. They can thus be used as antiatherosclerotics, remedies for the late complications of diabetes, cancers, fibrotic disorders such as pulmonary, hepatic or renal fibrosis. They are effective inhibitors of the cellular sodium-proton antiporter (Na /H exchanger).

公开(公告)号：ES2108144T3

公开(公告)日：1997-12-16

申请号：ES93101841

申请日：1993-02-05

Applicant: HOECHST AG

Inventor： LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  ENGLERT HEINRICH DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C311/21 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07D295/155 ,  C07D295/22 ,  C07D295/26

公开(公告)号：DE59307360D1

公开(公告)日：1997-10-23

申请号：DE59307360

申请日：1993-02-05

Applicant: HOECHST AG

Inventor： LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  ENGLERT HEINRICH DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C311/21 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07D295/155 ,  C07D295/22 ,  C07D295/26

公开(公告)号：AT158278T

公开(公告)日：1997-10-15

申请号：AT93101841

申请日：1993-02-05

Applicant: HOECHST AG

Inventor： LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  ENGLERT HEINRICH DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C311/21 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07D295/155 ,  C07D295/22 ,  C07D295/26

公开(公告)号：DK0556673T3

公开(公告)日：1998-04-14

申请号：DK93101841

申请日：1993-02-05

Applicant: HOECHST AG

Inventor： SCHOLZ WOLFGANG DR ,  LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  ENGLERT HEINRICH DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C311/21 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07D295/155 ,  C07D295/22 ,  C07D295/26

公开(公告)号：DE59302959D1

公开(公告)日：1996-07-25

申请号：DE59302959

申请日：1993-02-05

Applicant: HOECHST AG

Inventor： LANG HANS-JOCHEN DR ,  MANIA DIETER DR ,  WEICHERT ANDREAS DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  ENGLERT HEINRICH DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P35/04 ,  C07C217/44 ,  C07C311/16 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65

Abstract: There are described benzoylguanidines of the formula I where R(1) is equal to R(4)-SOm or R(5)R(6)N-SO2-, where R(4) and R(5) are equal to alk(en)yl, -CnH2n-R(7), and where R(7) is equal to cycloalkyl or phenyl, where R(5) also denotes H, R(6) is equal to H or C1-C4-alkyl, R(2) is hydrogen, halogen, alkyl, -O-(CH2)mCpF2p+1, -X-R(10), where X is equal to O, S, NR(11), R(10) is equal to H, (cyclo)alkyl(methyl), -CnH2n-R(12) where R(12) is equal to phenyl, R(3), inter alia, is defined as R(1), and their pharmaceutically tolerable salts. The compounds I are prepared by reaction of compounds of the formula II in which L represents a leaving group which can be easily substituted nucleophilically, with guanidine. Compounds I are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infract treatment and for the treatment of angina pectoris, where they also preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage. They are moreover distinguished by a strong inhibitory action on cell proliferation. They can therefore be used as antiatherosclerotics, agents against diabetic late complications, cancers, fibrotic disorders such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys. They are effective inhibitors of the cellular sodium/protons antiporter (Na /H exchanger).

公开(公告)号：GR3025523T3

公开(公告)日：1998-02-27

申请号：GR970403172

申请日：1997-11-26

Applicant: HOECHST AG

Inventor： LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  ENGLERT HEINRICH DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C311/21 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07D295/155 ,  C07D295/22 ,  C07D295/26

公开(公告)号：DK0577024T3

公开(公告)日：1997-02-24

申请号：DK93110195

申请日：1993-06-25

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS DR ,  LANG HANS-JOCHEN ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/33 ,  A61K31/435 ,  A61K31/44 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/02 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P15/04 ,  A61P43/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/37 ,  C07C315/04 ,  C07C317/32 ,  C07C317/44 ,  C07C323/60 ,  C07D213/56

Abstract: Benzoylguanidines of the formula I with R(1) equal to R(4)-SOm or R(5)R(6)N-SO2- with R(4) and R(5) equal to alk(en)yl, -CnH2n-R(7), and with R(7) equal to cycloalkyl or phenyl, where R(5) can also mean H, R(6) equals H or C1-C4-alkyl, R(2) is hydrogen, (cyclo)alk(en)(yn)yl, aryl and hetaryl R(3) is defined as R(2), and their pharmaceutically tolerated salts, are described. Compounds I are obtained by reacting compounds of the formula II with guanidine, in which L is a leaving group which can easily undergo nuclophilic substitution. Compounds I are outstandingly suitable as antiarrhythmic drugs with cardioprotective component for the treatment and prophylaxis of infarct and for treating angina pectoris, and they also greatly reduce preventively the pathophysiological processes in the development of ischaemia-induced damage. Furthermore, I are distinguished by a potent inhibitory action on cell proliferation. They can thus be used as antiatherosclerotics, remedies for the late complications of diabetes, cancers, fibrotic disorders such as pulmonary, hepatic or renal fibrosis. They are effective inhibitors of the cellular sodium-proton antiporter (Na /H exchanger).