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81. 发明专利

AU1499897A Ortho-subatituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them 未知
公开(公告)号：AU1499897A
公开(公告)日：1997-09-11
申请号：AU1499897
申请日：1997-02-28
申请人： HOECHST AG
发明人： ALBUS UDO , BRENDEL JOACHIM , KLEEMANN HEINZ-WERNER , LANG HANS JOCHEN , SCHOLZ WOLFGANG , SCHWARK JAN-ROBERT , WEICHERT ANDREAS
IPC分类号： A61K31/165 , A01N1/02 , A61K31/155 , A61P9/00 , A61P9/08 , A61P9/10 , A61P35/00 , A61P43/00 , C07C279/22
摘要： 2-Alkoxy-benzoylguanidines of formula (I) and their salts are new. R1-R3 = 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, Ar, SR13, OR13, NHR13, NR13R14, CHR13R15, C(R15)(R16)OH, CCR18, CR19=CHR18 or (CR20R21)k-CO-(CR22R23)l-R24; R4 = 1-4C alkyl; Ar = phenyl, naphthyl, biphenylyl, or 1-9C heteroaryl (bonded via C or N) all optionally mono- to - tri-substituted by Z; Z = F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; X = O, S or NR5; R5 = H, 1-4C alkyl or CdH2d-R6; R6 = phenyl, biphenylyl, naphthyl (all optionally mono- to tri-substituted by Z') or 3-8C cycloalkyl; Z' = 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 by Z); R11, R12 = as R10, H, or 1-4C alkyl; R13, R14 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)j-R17, (CH2)g-O-(CH2CH2O)h-R24; R15, R16 = H or 1-6C alkyl; or CR15R16 = 3-8C cycloalkyl; R17 = H or CH3; R18 = phenyl, 1-9C heteroaryl (optionally mono- to tri-substituted by Z'), 1-6C alkyl (optionally mono- to tri-substituted by OH) or 3-8C cycloalkyl; R19 - R23 = H or CH3; R24 = H, 1-6C alkyl, 3-8C cycloalkyl or CmH2m-R18; a = 0 or 1; b, f = 0-2; c =0-3; d, g, h, i, k, l = 0-4; j, m = 1-4;

82. 发明专利

MX9701163A GUANIDINAS DE ACIDOS TIOFENILALQUENILCARBOXILICOS SUSTITUIDAS, PROCEDIMIENTO PARA SU PREPARACION, SU EMPLEO COMO MEDICAMENTO O AGENTE DE DIAGNOSTICO, ASI COMO MEDICAMENTO QUE LAS CONTIENE. 未知
公开(公告)号：MX9701163A
公开(公告)日：1997-08-30
申请号：MX9701163
申请日：1997-02-14
申请人： HOECHST AG
发明人： SCHWARK JAN-ROBERT , BRENDEL JOACHIM , KLEEMANN HEINZ-WERNER , LANG HANS JOCHEN , WEICHERT ANDREAS , ALBUS UDO , SCHOLZ WOLFGANG
IPC分类号： C07D333/24 , A61K31/38 , A61K31/381 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P35/00 , A61P43/00 , C07C279/22 , C07D333/02 , C07D333/34 , C07D333/22
摘要： Se describen guanidinas de ácidos tiofenilalquenilcarboxílicos sustituidas de la formula I en donde R(1) a R(5) tienen los significados indicados en las reivindicaciones, son medicamentos antiarrítmicos extraordinariamente activos con un componente cardioprotector y son extraordinariamente adecuados para la profilaxis del infarto y el tratamiento del infarto, así como para el tratamiento de la angina de pecho, inhibiendo o reduciendo fuertemente también de forma preventiva los procesos patofiosiologicos en la aparicion de lesiones inducidas por isquemias, en especial en el desencadenamiento de arritmias del corazon inducidas por isquemias.

83. 发明专利

AU1477397A Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them 未知
公开(公告)号：AU1477397A
公开(公告)日：1997-08-28
申请号：AU1477397
申请日：1997-02-19
申请人： HOECHST AG
发明人： ALBUS UDO , BRENDEL JOACHIM , KLEEMANN HEINZ-WERNER , LANG HANS-JOCHEN , SCHOLZ WOLFGANG , SCHWARK JAN-ROBERT , WEICHERT ANDREAS
IPC分类号： 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 , A01N1/00
摘要： 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.

84. 发明专利

NO973850D0 未知
公开(公告)号：NO973850D0
公开(公告)日：1997-08-21
申请号：NO973850
申请日：1997-08-21
申请人： HOECHST AG
发明人： SCHWARK JAN-ROBERT , BRENDEL JOACHIM , KLEEMANN HEINZ-WERNER , LANG HANS JOCHEN , WEICHERT ANDREAS , JANSEN HANS-WILLI , SCHOLZ WOLFGANG
IPC分类号： C07D213/65 , A01N1/00 , A61K31/155 , A61K31/165 , A61K31/44 , A61K31/4406 , A61P3/06 , A61P9/00 , A61P9/06 , A61P9/10 , A61P13/02 , A61P15/00 , A61P25/00 , A61P43/00 , C07C277/08 , C07C279/20 , C07C279/22 , C07C
摘要： Phenyl-substituted alkenyl-carboxylic acid guanidide compounds of formula (I) are new. T = a group (i); Ra = H, F, Cl, Br, I , CN, OH, OR6, 1-4C alkyl, Or-(CH2)aCbF2b+1, 3-8C cycloalkyl or NR7R8; r = 0 or 1; a = 0 - 4; b = 1 - 4; R6 = 1-4C alkyl, 1-4C perfluoroalkyl, 3-6C alkenyl, 3-8C cycloalkyl, phenyl or benzyl; where the phenyl nucleus is optionally substituted by 1 - 3 F, Cl, CF3, CH3, OCH3 or NR9R10 groups; R9, R10 = H, 1-4C alkyl or 1-4C perfluoroalkyl; R7, R8 = as for R6; or R7+R8 = (CH2)4 or (CH2)5, where one of the CH2 groups may be replaced by O, S, NH, N-CH3 or N-benzyl; Rb, Rc, Rd = as for Ra; x, y = 0 - 2; Rf = H, F, Cl, Br, I, CN, OR12, 1-8C alkyl, Op-(CH2)f-CgF2g+1, 3-8C cycloalkyl or 1-9C heteroaryl; p = 0 or 1; f = 0 - 4; g = 1 - 8; R12 = 1-8C alkyl, 1-4C perfluoroalkyl, 3-8C alkenyl, 3-8C cycloalkyl, phenyl or benzyl; where the phenyl nucleus may be substituted by 1 - 3 F, Cl, CF3, CH3, OCH3 or NR13R14 groups; R13, R14 = H, 1-4C alkyl or 1-4C perfluoroalkyl; Re = as for Rf; R1 = as for T, or is H, Ok-CmH2m+1, On-(CH2)p-CqF2q+1, F, Cl, Br, I, CN, CO-N=C(NH2)2, SOr1R17, SOr2-NR31R32, Ou-(CH2)v-C6H5, Ou2-(1-9C heteroaryl) (sic) or Su2-(1-9C heteroaryl) (sic); k, n = 0 or 1; m = 0-8; q = 1 - 8; p = 0-4; r1, r2 = 0 - 2; R31, R32 = H, 1-8C alkyl or 1-8C perfluoroalkyl, or R31+R32 = (CH2)4 or (CH2)5, where one of the CH2 groups may be replaced by O, S, NH, N-CH3 or N-benzyl; R17 = 1-8C alkyl; u, u2 = 0 or 1; v = 0- 4. The phenyl nucleus may be substituted by 1-3 F, Cl, CF3, CH3, OCH3, (CH2)w-NR21R22, NR18R19 or 1-9C heteroaryl groups ÄsicÜ. R18, R19, R21, R22 = 1-4C alkyl or 1-4C perfluoroalkyl; w = 1 - 4; The heterocycle of the 1-9C heteroaryl may be substituted by 1 - 3 F, Cl, CF3, CH3 or OCH3 groups. R2, R3, R4 and R5 = as for R1; or R1+R2 or R2+R3 = CH-CH=CH-CH, which is optionally substituted by 1 - 3 F, Cl, CF3, CH3, OCH3, (CH2)w2-NR24R25 or NR26R27; R24, R25, R26, R27 = H, 1-4C alkyl or 1-4C perfluoroalkyl; w2 = 1 - 4; provided that T is present 2-3 times in the molecule.

85. 发明专利

CA2197628A1 SUBSTITUTED THIOPHENYLALKENYLCARBOXYLIC ACID GUANIDIDES, PROCESS FOR THEIR PREPARATION, THEIR USE AS A MEDICAMENT OR DIAGNOSTIC, AND MEDICAMENT CONTAINING THEM 未知
公开(公告)号：CA2197628A1
公开(公告)日：1997-08-16
申请号：CA2197628
申请日：1997-02-14
申请人： HOECHST AG
发明人： SCHWARK JAN-ROBERT , BRENDEL JOACHIM , KLEEMAN HEINZ-WERNER , LANG HANS JOCHEN , WEICHERT ANDREAS , ALBUS UDO , SCHOLZ WOLFGANG
IPC分类号： C07D333/24 , A61K31/38 , A61K31/381 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P35/00 , A61P43/00 , C07C279/22 , C07D333/02 , C07D333/34 , C07D333/30 , C07D333/06 , A61K31/395
摘要： Substituted thiophenylalkenylcarboxylic acid guanidides, processes for their preparation, their use as a medicament or diagnostic, and a medicament containing them. There are described substituted thiophenylalkenylcarboxylic acid guanidides of the formula I (see fig. I) in which R(1) to R(5) have the meanings given in the claims, which are outstandingly active antiarrhythmic pharmaceuticals having a cardioprotective component and are outstandingly suitable for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they also inhibit or greatly reduce the pathophysiological processes in the formation of ischemicallyinduced damage, in particular in the initiation of ischemically induced cardiac arrhythmias, in a preventive manner.

88. 发明专利

NO970406L 未知
公开(公告)号：NO970406L
公开(公告)日：1997-08-01
申请号：NO970406
申请日：1997-01-30
申请人： HOECHST AG
发明人： KLEMANN HEINZ-WERNER , BRENDEL JOACHIM , SCHWARK JAN-ROBERT , WEICHERT ANDREAS , LANG HANS JOCHEN , ALBUS UDO , SCHOLZ WOLFGANG
IPC分类号： A61K31/165 , A61K31/155 , A61K31/17 , A61K31/18 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P43/00 , C07C279/22 , C07C311/21 , C07C311/60 , C07C311/47

89. 发明专利

MX9605538A BENZOIL-GUANIDINAS SUSTITUIDAS CON SULFONILAMINO, PROCEDIMIENTO PARA SU PREPARACION, SU EMPLEO COMO MEDICAMENTO O PARA DIAGNOSTICO, ASI COMO EL MEDICAMENTO QUE LAS CONTIENE. 未知
公开(公告)号：MX9605538A
公开(公告)日：1997-05-31
申请号：MX9605538
申请日：1996-11-13
申请人： HOECHST AG
发明人： KLEEMANN HEINZ WERNER , BRENDEL JOACHIM , SCHWARK JAN-ROBERT , WEICHERT ANDREAS , LANG HANS JOCHEN , ALBUS UDO , SCHOLZ WOLFGANG
IPC分类号： A61K31/18 , C07D213/65 , A61K31/44 , A61P1/16 , A61P3/08 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C303/34 , C07C303/40 , C07C307/10 , C07C311/08 , C07D213/62 , C07C279/22
摘要： La invencion se refiere a benzoil-guanidinas de la formula I: en donde R(1) a R(6) tienen los significados indicados en las reivindicaciones, son medicamentos antiarrítmicos extraordinariamente eficaces con un componente cardioprotector y son extraordinariamente adecuados para la profilaxis del infarto y el tratamiento del infarto, así como para el tratamiento de la angina de pecho, inhibiendo o reduciendo fuertemente también previene los procesos patofisiologicos en la formacion de lesiones inducidas por isquemia, en particular en el desencadenamiento de arritmias del corazon inducidas por isquemia.

90. 发明专利

AU7180496A Substituted benzenedicarboxylic acid diguanides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them 未知
公开(公告)号：AU7180496A
公开(公告)日：1997-05-29
申请号：AU7180496
申请日：1996-11-18
申请人： HOECHST AG
发明人： KLEEMANN HEINZ-WERNER , BRENDEL JOACHIM , SCHWARK JAN-ROBERT , WEICHERT ANDREAS , LANG HANS JOCHEN , ALBUS UDO , SCHOLZ WOLFGANG
IPC分类号： A61K31/165 , A61P1/16 , A61P3/08 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07C279/20 , C07C279/22 , A01N1/02 , A61K31/135
摘要： Benzenedicarboxylic acid diguanidide compounds of formula (I) and their salts are new. One of R1-R4 = -CO-N=C(NH2)2; and the others are as follows; R1 = H, 1-4C alkyl, F, Cl, OR32, NR33R34 or CF3; R2, R4 = H, halo, OH, CN, CF3, 1-8C alkyl, 2-8C alkenyl, (CH2)mR14, 1-, 2- or 3-pyrrolyl (optionally substituted by 1-4 of halo, CN, 2-8C alkanoyl, 2-8C alkoxycarbonyl, CHO, COOH, CF3, Me and OMe), SO2R22, CONH2, CONHMe, CONMe2, COR28, SO2NH2, SO2NHMe, SO2NMe2, OR35 or NR35R36; R3 = H, SR25, OR25, NR25R26 or CR25R26R27; R5 =1-4C alkyl, halo, (CH2)yCF3, O(CH2)yCF3, or phenyl (optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, NH2, NHMe and NMe2); R32-R34 = H or 1-4C alkyl; m, y = 0-2; R14 = phenyl (optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, NH2, NHMe or NMe2) or 3-8C cycloalkyl; R22, R28 = Me or CF3; R23, R24, R29, R30 = H or Me; R35, R36 = H or 1-6C alkyl; or R35+R36 = 4-7 (CH2)(4-7) optionally with one CH2 replaced by O, S, NH, NMe or N-benzyl; R25 = H, 1- 8C alkyl, phenyl (optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, OH, NH2, NHMe and NMe2) or 1-9C heteroaryl (optionally substituted by 1-3 of F, Cl, CF3, Me, OMe, OH, NH2, NHMe and NMe2); R26, R27 = groups as defined for R25, or H, 1-8C alkyl (sic).

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