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    21.
    发明专利
    未知

    公开(公告)号：ES2143122T3

    公开(公告)日：2000-05-01

    申请号：ES96116938

    申请日：1996-10-22

    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

    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

    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.

    26.
    发明专利
    未知

    公开(公告)号：DK0700899T3

    公开(公告)日：1999-10-18

    申请号：DK95113847

    申请日：1995-09-04

    Applicant: HOECHST AG

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

    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.

    27.
    发明专利
    未知

    公开(公告)号：ES2134878T3

    公开(公告)日：1999-10-16

    申请号：ES94108280

    申请日：1994-05-30

    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: A61K31/165 ,  A61K31/155 ,  A61K31/166 ,  A61K31/395 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4418 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P43/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/15 ,  C07C317/32 ,  C07C317/44 ,  C07C317/48 ,  C07C323/62 ,  C07D207/337 ,  C07D213/30 ,  C07D213/53 ,  C07D213/54 ,  C07D213/58 ,  C07D213/65 ,  C07D215/14 ,  C07D217/16 ,  C07D231/12 ,  C07D233/06 ,  C07D233/61 ,  C07D233/64 ,  C07D241/26 ,  C07D241/28

    Abstract: There are described benzoylguanidines of the formula I in which: R(1) is R(6)-CO or R(7)R(8)N-CO, where R(6), R(7) and R(8) are (perfluoro)alk(en)yl, -(CH)2n-R(9), R(9) is cycloalkyl, phenyl, biphenylyl or naphthyl, where R(7) and R(8) can together be 4 or 5 methylene groups, of which one CH2 group can be replaced by oxygen, S, NH, N-CH3 or N-benzyl; R(2) is defined as R(1), or is H, Hal, CN, NO2, (perfluoro)alk(en)yl, -(CH)2 R(15) where R(15) is cycloalkyl, phenyl, biphenylyl or naphthyl, or R(2) is (C1-C9)-heteroaryl, or R(2) is SR(18), -OR(18), -NR(18)R(19), -CR(18)R(19)R(20); R(18) = -(CH2)-heteroaryl, R(19), R(20) are defined as R(18) or are H, (perfluoro)-alkyl, or R(2) is R(21)-SOm or R(22)R(23)N-SO2-, where R(21) is (perfluoro)alk(en)yl, -CH2-R(24), R(24) is cycloalkyl, phenyl, biphenylyl or naphthyl, R(22) is H, (perfluoro)alk(en)yl, -(CH2)n-R(29), R(29) is (C3-C8)-cycloalkyl, phenyl, biphenylyl or naphthyl, R(23) is H, (perfluoro)alkyl, where R(22) and R(23) can together be 4 or 5 methylene groups, of which one CH2 group can be replaced by oxygen, S, NH, N-CH3 or N-benzyl; or R(33)X-, where R(2) is X is oxygen, S, NR(34), (D=O)A-, NR(34)C=MN R(35)-, where M is oxygen, S, A = oxygen, NR(34), D = C, SO R(33) and R(35) are (perfluoro)alk(en)yl, -(CH2)n-R(36), where R(36) is cycloalkyl, phenyl, biphenylyl or naphthyl, R(34) = H, (perfluoro)alkyl, where A and N are bonded to the phenyl ring of the benzoylguanidine parent structure; or R(2) is -SR(40), -OR(40), -NHR(40)R(41), -CHR(40)R(42), -C=CR(45) where R(40), R(41) are identical or different, and are -(CH2)p-(CHOH)q-(CH2)r-(CHOH)t-R(51) or -(CH2)p-O-(CH2-CH2O)q-R(51), R(51) is hydrogen or methyl, R(42), R(43) are hydrogen or alkyl or, together with the carbon atom carrying them, form a (C3-C8)-cycloalkyl; R(44) is H, (C1-C6)-alkyl, (C3-C8)-cycloalkyl, -CeH2e-R(45) where R(45) is phenyl, heteroaryl or alkyl, R(46), R(47), R(48), R(49) and R(50) are hydrogen or methyl; or R(2) is R(55)-NH-SO2-, R(3), R(4) and R(5) are independently of one another defined as R(1) or R(2); and their pharmaceutically tolerable salts.0

    28.
    发明专利
    未知

    公开(公告)号：AT181322T

    公开(公告)日：1999-07-15

    申请号：AT94108280

    申请日：1994-05-30

    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: A61K31/165 ,  A61K31/155 ,  A61K31/166 ,  A61K31/395 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4418 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P43/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/15 ,  C07C317/32 ,  C07C317/44 ,  C07C317/48 ,  C07C323/62 ,  C07D207/337 ,  C07D213/30 ,  C07D213/53 ,  C07D213/54 ,  C07D213/58 ,  C07D213/65 ,  C07D215/14 ,  C07D217/16 ,  C07D231/12 ,  C07D233/06 ,  C07D233/61 ,  C07D233/64 ,  C07D241/26 ,  C07D241/28

    Abstract: There are described benzoylguanidines of the formula I in which: R(1) is R(6)-CO or R(7)R(8)N-CO, where R(6), R(7) and R(8) are (perfluoro)alk(en)yl, -(CH)2n-R(9), R(9) is cycloalkyl, phenyl, biphenylyl or naphthyl, where R(7) and R(8) can together be 4 or 5 methylene groups, of which one CH2 group can be replaced by oxygen, S, NH, N-CH3 or N-benzyl; R(2) is defined as R(1), or is H, Hal, CN, NO2, (perfluoro)alk(en)yl, -(CH)2 R(15) where R(15) is cycloalkyl, phenyl, biphenylyl or naphthyl, or R(2) is (C1-C9)-heteroaryl, or R(2) is SR(18), -OR(18), -NR(18)R(19), -CR(18)R(19)R(20); R(18) = -(CH2)-heteroaryl, R(19), R(20) are defined as R(18) or are H, (perfluoro)-alkyl, or R(2) is R(21)-SOm or R(22)R(23)N-SO2-, where R(21) is (perfluoro)alk(en)yl, -CH2-R(24), R(24) is cycloalkyl, phenyl, biphenylyl or naphthyl, R(22) is H, (perfluoro)alk(en)yl, -(CH2)n-R(29), R(29) is (C3-C8)-cycloalkyl, phenyl, biphenylyl or naphthyl, R(23) is H, (perfluoro)alkyl, where R(22) and R(23) can together be 4 or 5 methylene groups, of which one CH2 group can be replaced by oxygen, S, NH, N-CH3 or N-benzyl; or R(33)X-, where R(2) is X is oxygen, S, NR(34), (D=O)A-, NR(34)C=MN R(35)-, where M is oxygen, S, A = oxygen, NR(34), D = C, SO R(33) and R(35) are (perfluoro)alk(en)yl, -(CH2)n-R(36), where R(36) is cycloalkyl, phenyl, biphenylyl or naphthyl, R(34) = H, (perfluoro)alkyl, where A and N are bonded to the phenyl ring of the benzoylguanidine parent structure; or R(2) is -SR(40), -OR(40), -NHR(40)R(41), -CHR(40)R(42), -C=CR(45) where R(40), R(41) are identical or different, and are -(CH2)p-(CHOH)q-(CH2)r-(CHOH)t-R(51) or -(CH2)p-O-(CH2-CH2O)q-R(51), R(51) is hydrogen or methyl, R(42), R(43) are hydrogen or alkyl or, together with the carbon atom carrying them, form a (C3-C8)-cycloalkyl; R(44) is H, (C1-C6)-alkyl, (C3-C8)-cycloalkyl, -CeH2e-R(45) where R(45) is phenyl, heteroaryl or alkyl, R(46), R(47), R(48), R(49) and R(50) are hydrogen or methyl; or R(2) is R(55)-NH-SO2-, R(3), R(4) and R(5) are independently of one another defined as R(1) or R(2); and their pharmaceutically tolerable salts.0

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