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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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公开(公告)号:ES2092737T3
公开(公告)日:1996-12-01
申请号:ES93116788
申请日:1993-10-18
Applicant: HOECHST AG
IPC: C07B39/00 , C07C17/14 , C07C22/04 , C07C67/307 , C07C67/343 , C07C69/65 , C07C69/76 , C07C205/12 , C07C255/50 , C07C257/12 , C07C257/20 , C07C311/05 , C07C311/18 , C07C311/53 , C07D275/04 , C07D275/06 , C07D333/24 , C07D333/60 , C07D333/68 , C07D333/70 , C07D471/04 , C07D487/04 , C07D495/04
Abstract: Aromatic bromomethyl compounds play an important role in the synthesis of active substances. They can be obtained in particularly high purity by free-radical bromination of aromatic methyl compounds in the solvent chlorobenzene.
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公开(公告)号:CZ26596A3
公开(公告)日:1996-08-14
申请号:CZ26596
申请日:1996-01-29
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: C07D295/12 , A61K31/155 , A61K31/18 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/08 , A61P13/12 , A61P35/00 , C07C279/22 , C07C311/15 , C07C311/18 , C07C311/29 , C07C311/64 , C07C317/28 , C07C317/46 , C07C323/16 , C07C323/25 , C07C335/32 , C07C381/10 , C07D207/09 , C07D213/40 , C07D213/70 , C07D215/36 , C07D233/42 , C07D233/54 , C07D233/60 , C07D233/84 , C07D235/28 , C07D295/22 , C07D521/00 , C07C319/20 , C07C315/04 , C07C277/08 , A01N1/02
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, SO2NHCONR20, 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; b = 1-10; c = 3-5; d = 0-5; g = 0-4; f, h = 0 or 1; m = 0-2.
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公开(公告)号:DE4432105A1
公开(公告)日:1996-03-14
申请号:DE4432105
申请日:1994-09-09
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 , C07C315/04 , C07C303/36 , A01N1/02 , C07D213/44 , C07D215/12 , C07D217/12
Abstract: Benzoylguanidines of formula (I) and their salts are new. R1 and R3 = H, halogen, CN, NO2, 1-8C alkyl, 3-8C cycloalkyl, Oa(CH2)b(CF2)cCF3, S(O)mR5, SO2NR6R7, SR11, OR11, CR11R12R13 or phenyl, naphthyl, biphenylyl or C- or N-bonded 1-9C heteroaryl gps. opt. substd. by 1-3 of F, Cl, CF3, Me, OMe, OH, NH2, NHMe and NMe2; a = 0 or 1; b = 0-2; c = 0-3; m = 0-2; R5 = 1-8C alkyl, 3-6C alkenyl, CF3 or CnH2n-R8; R6 = H, or as for R5; R7 = H or 1-4C alkyl; or R6+R7 = tetra- or pentamethylene, opt. with a CH2 gp. replaced by O, S, NH, NMe or NCH2Ph; n = 0-4; R8 = 3-7C cycloalkyl, or phenyl opt. substd. by 1-3 of F, Cl, CF3, Me, OMe and NR9R10; R9 and R10 = H or 1-4C alkyl; R11 = 3-8C cycloalkyl; (3-8C)cycloalkyl(1-2C)alkyl; or 1-9C heteroaryl or phenyl opt. substd. by 1-3 of F, Cl, CF3, OMe, OH, NH2, NHMe and NMe2; R12 and R13 = H, 1-4C alkyl or gps. as defined for R11; R2 = CF2R14, CF(R15)(R16), CF(Rf)-R15 or CRf=C(R15)(R16); R14 = 1-4C alkyl or 3-6C cycloalkyl; R15 and R16 = H or 1-4C alkyl; Rf = 1-3C perfluoro-n-alkyl; R4 = H, 1-3C alkyl, F, Cl, Br, I, CN or (CH2)s(CF2)tCF3; s = 0 or 1; t = 0-2.
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公开(公告)号:DE4428480A1
公开(公告)日:1996-03-07
申请号:DE4428480
申请日:1994-08-11
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , WEICHERT ANDREAS DR
IPC: C07C51/363 , C07C69/76 , C07C315/04 , C07C317/44 , C07C63/68 , C07C67/14 , C07C315/00
Abstract: Methylsulphonyl isopropyl benzoate esters of formula (I) are new: R1 = 1-8C alkyl or benzyl. Also claimed is the use of (I) for the prepn. of a benzoylguanidine cpd. of formula (II) (sic).
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公开(公告)号:DE4328352A1
公开(公告)日:1995-03-02
申请号:DE4328352
申请日:1993-08-24
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , LANG HANS-JOCHEN DR , WEICHERT ANDREAS DR , CRAUSE PETER DR , SCHOLZ WOLFGANG DR , ALBUS UDO DR
IPC: A61K31/155 , A61K31/185 , A61P9/00 , A61P9/10 , C07C277/08 , C07C279/20 , C07C279/22 , C07C311/37 , C07C311/59 , C07C315/04 , C07C317/32 , C07C317/44 , C07C323/65 , C07C323/67 , C07D207/327 , C07D215/54 , C07D231/12 , C07D233/60 , C07D233/61 , C07D295/10 , C07D295/155 , C07D521/00 , C07C311/16 , C07C317/14 , C07D401/14 , C07D403/14 , C07C321/30 , A61K49/00
Abstract: Benzoyl-guanidine derivatives (III) are new. (III) are of formula X2-CO-N=C(NH2)2 X2 = R101 = hydrogen, fluoro, chloro, hydroxy, amino or trifluoromethyl; R102 = hydrogen, fluoro, chloro, bromo, cyano, CqF2qCF3, R13SO2, R14R15NCO, R16CO or R17R18NSO2; R13, R14, R16 and R17 = 1-8C alkyl, 3-4C alkenyl, CnH2n-R20, trifluoromethyl or, except for R13, hydrogen; n = 0 or 1; q = 1-5; R20 = 3-6C cycloalkyl or phenyl, optionally substituted by 1-2 of fluoro, chloro, trifluoromethyl, methyl, methoxy or NR21R22; R21 and R22 = hydrogen or methyl; R104 = 1-8C alkyl, CnH2nR20, trifluoromethyl, (iso)quinolyl, pyrrolyl, pyridyl or imidazolyl (all these rings bonded via carbon or nitrogen and optionally substituted by 1 or 2 fluoro, chloro, trifluoromethyl, methoxy, hydroxy or amino (optionally substituted by 1 or 2 methyl)), R87SO2, R88R89NSO2, or R93-ethynyl; R87 = 1-4C alkyl or trifluoromethyl; R88 = hydrogen, 1-4C alkyl, trifluoromethyl, or (CH2)anR90; an = 0 or 1; R90 and R93 = phenyl, optionally substituted as in R20; R103 = any of a wide range of substituents . The full definitions are given in the DEFINITIONS (Full Definitions) Field.
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公开(公告)号:DE4318756A1
公开(公告)日:1994-12-08
申请号:DE4318756
申请日:1993-06-05
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 , C07C311/16 , C07C317/04 , C07C323/16 , C07C335/16 , C07C335/42 , C07C313/04
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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公开(公告)号:DE59004292D1
公开(公告)日:1994-03-03
申请号:DE59004292
申请日:1990-07-18
Applicant: HOECHST AG
Inventor: KLEEMANN HEINZ-WERNER DR , URBACH HANSJOERG DR , WAGNER ADALBERT DR , RUPPERT DIETER DR , LINZ WOLFGANG DR , KRAMER WERNER DR DR
IPC: C12N9/99 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/445 , A61K31/535 , A61K38/55 , A61P9/12 , C07C237/08 , C07C237/22 , C07D211/26 , C07D211/58 , C07D233/54 , C07D233/64 , C07D295/20 , C07D333/24 , C07D401/12 , C07D403/12 , C07D409/12 , C07D521/00 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/078 , C07K14/81 , A61K37/64
Abstract: The present invention relates to compounds of the formula I in which A, R , R , R and n are defined as indicated in the description, to processes for the preparation thereof, to the use thereof as medicines and to pharmaceutical compositions containing these.
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