公开(公告)号：HU9801045A2

公开(公告)日：1999-06-28

申请号：HU9801045

申请日：1998-05-08

Applicant: HOECHST AG

Inventor： BILLEN GUENTER ,  HAASE BURKHARD ,  NEISES BERNHARD ,  SCHUDOK MANFRED ,  SCHWAB WILFRIED ,  THORWART WERNER

IPC: C07D295/18 ,  A61K31/195 ,  A61K31/215 ,  A61K31/27 ,  A61K31/275 ,  A61K31/33 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/48 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/02 ,  A61P9/10 ,  A61P19/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C311/13 ,  C07C311/19 ,  C07C311/22 ,  C07C311/29 ,  C07C323/59 ,  C07D207/16 ,  C07D207/34 ,  C07D207/38 ,  C07D209/46 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D215/14 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D233/74 ,  C07D235/08 ,  C07D235/24 ,  C07D241/24 ,  C07D249/08 ,  C07D249/12 ,  C07D261/10 ,  C07D261/18 ,  C07D275/04 ,  C07D277/06 ,  C07D277/28 ,  C07D307/24 ,  C07D307/54 ,  C07D307/58 ,  C07D307/68 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/12 ,  C07D513/04 ,  C07C311/18

Abstract: Phenyl-, thienyl- or furanyl-substituted N( alpha )-sulphonyl-diaminocarboxylic acid derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 of 1-7C alkyl, 3-7C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN, NO2, COOH, alkyl-O-CO-, OCH2O, NR4R5CO and NR4R5); Het = pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thienyl, thiazolyl, oxazolyl, isoxazolyl, pyridinyl, pyrimidinyl, indolyl, benzothiophenyl, benzimidazolyl, benzoxazolyl, benzothiazolyl or benzotriazolyl (all optionally substituted as for phenyl in Ar); R2,R4,R5 = H, alkyl, carboxyalkyl, Ar-(CH2)o- or picolyl; or NR4R5 = 4-7 membered ring, optionally having one C replaced by O, S or NH; o = 0-2; R3,G = H, alkyl, 3-6C cycloalkyl, 2-6C alkenyl, Ar-(CH2)m-, Het-(CH2)m-, R6CO-, R6OCO-, R6CH(NH2)CO-, NR7R8CO-, R6SO2-, R6SO2NR7CO-. R'6-NHC(=NR'7)- or a heterocyclic group of formula (i); or N(G)R3 = succinimido, maleimido, 2-oxo-pyrrolidino, 1H-1-pyrrolyl, 1H-1-imidazolyl or 2-oxo-2,3-dihydro-1H-1-pyrrolyl, all monosubstituted by R7; phthalimido or 2-oxo-1-indolinyl, both monosubstituted by R10 in the benzene ring; 1-indolyl; 1-benzimidazolyl; pyrrolidino, piperidino, perhydroazepino or perhydroazocino; or a group of formula (ii)-(vi); one ring C in (iv) is optionally replaced by O, S, SO2 or NR2; m = 0-3; r = 1 or 2; R6 = H, alkyl (optionally substituted as for Ar or by 3-6C cycloalkyl), 3-6C cycloalkyl (optionally substituted as for Ar), 2-6C alkenyl (optionally substituted as for Ar, or by Ar or Het (both optionally having a third substituent as above)); Ar-(CH2)m (in which Ar optionally has a third substituent as above and may further be substituted by OCF3, SO2NH2, NHCOCF3 or benzyl; and (CH2)m is optionally substituted by COOH), naphthyl, adamantyl or Het-(CH2)m-; R7 = H or alkyl; R8 = H, alkyl, Ar-(CH2)m- or Het-(CH2)m-; or NR7R8 = optionally substituted 4-7 membered ring, optionally having one C replaced by O, S or NH; R'6,R'7 = as R6,R7; or alkyl-CO-, NO2 or Ar-(CH2)m-SO2-; W = N, S or O; R10 = one or the optional substituents of Ar; A = direct bond, O, CH=CH or C IDENTICAL C; B = (CH2)m, O(CH2)q or CH=CH; q = 1-5; D = (CH2)s, optionally with one C replaced by optionally substituted NH, O or S; s = 1-6; X = CH=CH, O or S; R9 = H; or can also be alkyl, phenyl, succinimidyl, benzotriazolyl or benzyl if G = H; unless specified otherwise alkyl moieties have 1-6C.

公开(公告)号：PT877019E

公开(公告)日：2002-05-31

申请号：PT98108040

申请日：1998-05-02

Applicant: HOECHST AG

Inventor： THORWART WERNER ,  NEISES BERNHARD ,  SCHUDOK MANFRED ,  SCHWAB WILFRIED ,  HAASE BURKHARD ,  BILLEN GUNTER

IPC: C07D295/18 ,  A61K31/195 ,  A61K31/215 ,  A61K31/27 ,  A61K31/275 ,  A61K31/33 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/48 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/02 ,  A61P9/10 ,  A61P19/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C311/13 ,  C07C311/19 ,  C07C311/22 ,  C07C311/29 ,  C07C323/59 ,  C07D207/16 ,  C07D207/34 ,  C07D207/38 ,  C07D209/46 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D215/14 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D233/74 ,  C07D235/08 ,  C07D235/24 ,  C07D241/24 ,  C07D249/08 ,  C07D249/12 ,  C07D261/10 ,  C07D261/18 ,  C07D275/04 ,  C07D277/06 ,  C07D277/28 ,  C07D307/24 ,  C07D307/54 ,  C07D307/58 ,  C07D307/68 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/12 ,  C07D513/04 ,  C07D209/42 ,  C07D249/18 ,  C07D215/48 ,  C07D295/20 ,  C07D239/42 ,  A61K31/18 ,  A61K31/63

Abstract: Phenyl-, thienyl- or furanyl-substituted N( alpha )-sulphonyl-diaminocarboxylic acid derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 of 1-7C alkyl, 3-7C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN, NO2, COOH, alkyl-O-CO-, OCH2O, NR4R5CO and NR4R5); Het = pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thienyl, thiazolyl, oxazolyl, isoxazolyl, pyridinyl, pyrimidinyl, indolyl, benzothiophenyl, benzimidazolyl, benzoxazolyl, benzothiazolyl or benzotriazolyl (all optionally substituted as for phenyl in Ar); R2,R4,R5 = H, alkyl, carboxyalkyl, Ar-(CH2)o- or picolyl; or NR4R5 = 4-7 membered ring, optionally having one C replaced by O, S or NH; o = 0-2; R3,G = H, alkyl, 3-6C cycloalkyl, 2-6C alkenyl, Ar-(CH2)m-, Het-(CH2)m-, R6CO-, R6OCO-, R6CH(NH2)CO-, NR7R8CO-, R6SO2-, R6SO2NR7CO-. R'6-NHC(=NR'7)- or a heterocyclic group of formula (i); or N(G)R3 = succinimido, maleimido, 2-oxo-pyrrolidino, 1H-1-pyrrolyl, 1H-1-imidazolyl or 2-oxo-2,3-dihydro-1H-1-pyrrolyl, all monosubstituted by R7; phthalimido or 2-oxo-1-indolinyl, both monosubstituted by R10 in the benzene ring; 1-indolyl; 1-benzimidazolyl; pyrrolidino, piperidino, perhydroazepino or perhydroazocino; or a group of formula (ii)-(vi); one ring C in (iv) is optionally replaced by O, S, SO2 or NR2; m = 0-3; r = 1 or 2; R6 = H, alkyl (optionally substituted as for Ar or by 3-6C cycloalkyl), 3-6C cycloalkyl (optionally substituted as for Ar), 2-6C alkenyl (optionally substituted as for Ar, or by Ar or Het (both optionally having a third substituent as above)); Ar-(CH2)m (in which Ar optionally has a third substituent as above and may further be substituted by OCF3, SO2NH2, NHCOCF3 or benzyl; and (CH2)m is optionally substituted by COOH), naphthyl, adamantyl or Het-(CH2)m-; R7 = H or alkyl; R8 = H, alkyl, Ar-(CH2)m- or Het-(CH2)m-; or NR7R8 = optionally substituted 4-7 membered ring, optionally having one C replaced by O, S or NH; R'6,R'7 = as R6,R7; or alkyl-CO-, NO2 or Ar-(CH2)m-SO2-; W = N, S or O; R10 = one or the optional substituents of Ar; A = direct bond, O, CH=CH or C IDENTICAL C; B = (CH2)m, O(CH2)q or CH=CH; q = 1-5; D = (CH2)s, optionally with one C replaced by optionally substituted NH, O or S; s = 1-6; X = CH=CH, O or S; R9 = H; or can also be alkyl, phenyl, succinimidyl, benzotriazolyl or benzyl if G = H; unless specified otherwise alkyl moieties have 1-6C.

公开(公告)号：AU736700B2

公开(公告)日：2001-08-02

申请号：AU6482498

申请日：1998-05-08

Applicant: HOECHST AG

Inventor： THORWART WERNER ,  SCHWAB WILFRIED ,  SCHUDOK MANFRED ,  HAASE BURKHARD ,  NEISES BERNHARD ,  BILLEN GUNTER

IPC: C07D295/18 ,  A61K31/195 ,  A61K31/215 ,  A61K31/27 ,  A61K31/275 ,  A61K31/33 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/48 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/02 ,  A61P9/10 ,  A61P19/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C311/13 ,  C07C311/19 ,  C07C311/22 ,  C07C311/29 ,  C07C323/59 ,  C07D207/16 ,  C07D207/34 ,  C07D207/38 ,  C07D209/46 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D215/14 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D233/74 ,  C07D235/08 ,  C07D235/24 ,  C07D241/24 ,  C07D249/08 ,  C07D249/12 ,  C07D261/10 ,  C07D261/18 ,  C07D275/04 ,  C07D277/06 ,  C07D277/28 ,  C07D307/24 ,  C07D307/54 ,  C07D307/58 ,  C07D307/68 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/12 ,  C07D513/04 ,  C07D261/08 ,  C07D209/34 ,  C07D241/12 ,  C07D241/18 ,  C07D213/06 ,  C07D307/34 ,  C07D333/04 ,  A61K31/18 ,  A61K31/405 ,  A61K31/17 ,  A61K31/24 ,  A61K31/495 ,  A61K31/505 ,  A61K31/335

Abstract: Phenyl-, thienyl- or furanyl-substituted N( alpha )-sulphonyl-diaminocarboxylic acid derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 of 1-7C alkyl, 3-7C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN, NO2, COOH, alkyl-O-CO-, OCH2O, NR4R5CO and NR4R5); Het = pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thienyl, thiazolyl, oxazolyl, isoxazolyl, pyridinyl, pyrimidinyl, indolyl, benzothiophenyl, benzimidazolyl, benzoxazolyl, benzothiazolyl or benzotriazolyl (all optionally substituted as for phenyl in Ar); R2,R4,R5 = H, alkyl, carboxyalkyl, Ar-(CH2)o- or picolyl; or NR4R5 = 4-7 membered ring, optionally having one C replaced by O, S or NH; o = 0-2; R3,G = H, alkyl, 3-6C cycloalkyl, 2-6C alkenyl, Ar-(CH2)m-, Het-(CH2)m-, R6CO-, R6OCO-, R6CH(NH2)CO-, NR7R8CO-, R6SO2-, R6SO2NR7CO-. R'6-NHC(=NR'7)- or a heterocyclic group of formula (i); or N(G)R3 = succinimido, maleimido, 2-oxo-pyrrolidino, 1H-1-pyrrolyl, 1H-1-imidazolyl or 2-oxo-2,3-dihydro-1H-1-pyrrolyl, all monosubstituted by R7; phthalimido or 2-oxo-1-indolinyl, both monosubstituted by R10 in the benzene ring; 1-indolyl; 1-benzimidazolyl; pyrrolidino, piperidino, perhydroazepino or perhydroazocino; or a group of formula (ii)-(vi); one ring C in (iv) is optionally replaced by O, S, SO2 or NR2; m = 0-3; r = 1 or 2; R6 = H, alkyl (optionally substituted as for Ar or by 3-6C cycloalkyl), 3-6C cycloalkyl (optionally substituted as for Ar), 2-6C alkenyl (optionally substituted as for Ar, or by Ar or Het (both optionally having a third substituent as above)); Ar-(CH2)m (in which Ar optionally has a third substituent as above and may further be substituted by OCF3, SO2NH2, NHCOCF3 or benzyl; and (CH2)m is optionally substituted by COOH), naphthyl, adamantyl or Het-(CH2)m-; R7 = H or alkyl; R8 = H, alkyl, Ar-(CH2)m- or Het-(CH2)m-; or NR7R8 = optionally substituted 4-7 membered ring, optionally having one C replaced by O, S or NH; R'6,R'7 = as R6,R7; or alkyl-CO-, NO2 or Ar-(CH2)m-SO2-; W = N, S or O; R10 = one or the optional substituents of Ar; A = direct bond, O, CH=CH or C IDENTICAL C; B = (CH2)m, O(CH2)q or CH=CH; q = 1-5; D = (CH2)s, optionally with one C replaced by optionally substituted NH, O or S; s = 1-6; X = CH=CH, O or S; R9 = H; or can also be alkyl, phenyl, succinimidyl, benzotriazolyl or benzyl if G = H; unless specified otherwise alkyl moieties have 1-6C.

公开(公告)号：AU6482498A

公开(公告)日：1998-11-12

申请号：AU6482498

申请日：1998-05-08

Applicant: HOECHST AG

Inventor： THORWART WERNER ,  SCHWAB WILFRIED ,  SCHUDOK MANFRED ,  HAASE BURKHARD ,  NEISES BERNHARD ,  BILLEN GUNTER

IPC: C07D295/18 ,  A61K31/195 ,  A61K31/215 ,  A61K31/27 ,  A61K31/275 ,  A61K31/33 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/48 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/02 ,  A61P9/10 ,  A61P19/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C311/13 ,  C07C311/19 ,  C07C311/22 ,  C07C311/29 ,  C07C323/59 ,  C07D207/16 ,  C07D207/34 ,  C07D207/38 ,  C07D209/46 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D215/14 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D233/74 ,  C07D235/08 ,  C07D235/24 ,  C07D241/24 ,  C07D249/08 ,  C07D249/12 ,  C07D261/10 ,  C07D261/18 ,  C07D275/04 ,  C07D277/06 ,  C07D277/28 ,  C07D307/24 ,  C07D307/54 ,  C07D307/58 ,  C07D307/68 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/12 ,  C07D513/04 ,  C07D261/08 ,  C07D209/34 ,  C07D241/12 ,  C07D241/18 ,  C07D213/06 ,  C07D307/34 ,  C07D333/04 ,  A61K31/18 ,  A61K31/405 ,  A61K31/17 ,  A61K31/24 ,  A61K31/495 ,  A61K31/505 ,  A61K31/335

Abstract: Phenyl-, thienyl- or furanyl-substituted N( alpha )-sulphonyl-diaminocarboxylic acid derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 of 1-7C alkyl, 3-7C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN, NO2, COOH, alkyl-O-CO-, OCH2O, NR4R5CO and NR4R5); Het = pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thienyl, thiazolyl, oxazolyl, isoxazolyl, pyridinyl, pyrimidinyl, indolyl, benzothiophenyl, benzimidazolyl, benzoxazolyl, benzothiazolyl or benzotriazolyl (all optionally substituted as for phenyl in Ar); R2,R4,R5 = H, alkyl, carboxyalkyl, Ar-(CH2)o- or picolyl; or NR4R5 = 4-7 membered ring, optionally having one C replaced by O, S or NH; o = 0-2; R3,G = H, alkyl, 3-6C cycloalkyl, 2-6C alkenyl, Ar-(CH2)m-, Het-(CH2)m-, R6CO-, R6OCO-, R6CH(NH2)CO-, NR7R8CO-, R6SO2-, R6SO2NR7CO-. R'6-NHC(=NR'7)- or a heterocyclic group of formula (i); or N(G)R3 = succinimido, maleimido, 2-oxo-pyrrolidino, 1H-1-pyrrolyl, 1H-1-imidazolyl or 2-oxo-2,3-dihydro-1H-1-pyrrolyl, all monosubstituted by R7; phthalimido or 2-oxo-1-indolinyl, both monosubstituted by R10 in the benzene ring; 1-indolyl; 1-benzimidazolyl; pyrrolidino, piperidino, perhydroazepino or perhydroazocino; or a group of formula (ii)-(vi); one ring C in (iv) is optionally replaced by O, S, SO2 or NR2; m = 0-3; r = 1 or 2; R6 = H, alkyl (optionally substituted as for Ar or by 3-6C cycloalkyl), 3-6C cycloalkyl (optionally substituted as for Ar), 2-6C alkenyl (optionally substituted as for Ar, or by Ar or Het (both optionally having a third substituent as above)); Ar-(CH2)m (in which Ar optionally has a third substituent as above and may further be substituted by OCF3, SO2NH2, NHCOCF3 or benzyl; and (CH2)m is optionally substituted by COOH), naphthyl, adamantyl or Het-(CH2)m-; R7 = H or alkyl; R8 = H, alkyl, Ar-(CH2)m- or Het-(CH2)m-; or NR7R8 = optionally substituted 4-7 membered ring, optionally having one C replaced by O, S or NH; R'6,R'7 = as R6,R7; or alkyl-CO-, NO2 or Ar-(CH2)m-SO2-; W = N, S or O; R10 = one or the optional substituents of Ar; A = direct bond, O, CH=CH or C IDENTICAL C; B = (CH2)m, O(CH2)q or CH=CH; q = 1-5; D = (CH2)s, optionally with one C replaced by optionally substituted NH, O or S; s = 1-6; X = CH=CH, O or S; R9 = H; or can also be alkyl, phenyl, succinimidyl, benzotriazolyl or benzyl if G = H; unless specified otherwise alkyl moieties have 1-6C.

公开(公告)号：PL326218A1

公开(公告)日：1998-11-23

申请号：PL32621898

申请日：1998-05-08

Applicant: HOECHST AG

Inventor： THORWART WERNER ,  SCHWAB WILFRIED ,  SCHUDOK MANFRED ,  HAASE BURKHARD ,  NEISES BERNHARD ,  BILLEN GUENTER

IPC: C07D295/18 ,  A61K31/195 ,  A61K31/215 ,  A61K31/27 ,  A61K31/275 ,  A61K31/33 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/48 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/02 ,  A61P9/10 ,  A61P19/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C311/13 ,  C07C311/19 ,  C07C311/22 ,  C07C311/29 ,  C07C323/59 ,  C07D207/16 ,  C07D207/34 ,  C07D207/38 ,  C07D209/46 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D215/14 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D233/74 ,  C07D235/08 ,  C07D235/24 ,  C07D241/24 ,  C07D249/08 ,  C07D249/12 ,  C07D261/10 ,  C07D261/18 ,  C07D275/04 ,  C07D277/06 ,  C07D277/28 ,  C07D307/24 ,  C07D307/54 ,  C07D307/58 ,  C07D307/68 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/12 ,  C07D513/04 ,  C07C311/27 ,  C07D307/64 ,  C07D333/34 ,  A61K31/18

Abstract: Phenyl-, thienyl- or furanyl-substituted N( alpha )-sulphonyl-diaminocarboxylic acid derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 of 1-7C alkyl, 3-7C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN, NO2, COOH, alkyl-O-CO-, OCH2O, NR4R5CO and NR4R5); Het = pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thienyl, thiazolyl, oxazolyl, isoxazolyl, pyridinyl, pyrimidinyl, indolyl, benzothiophenyl, benzimidazolyl, benzoxazolyl, benzothiazolyl or benzotriazolyl (all optionally substituted as for phenyl in Ar); R2,R4,R5 = H, alkyl, carboxyalkyl, Ar-(CH2)o- or picolyl; or NR4R5 = 4-7 membered ring, optionally having one C replaced by O, S or NH; o = 0-2; R3,G = H, alkyl, 3-6C cycloalkyl, 2-6C alkenyl, Ar-(CH2)m-, Het-(CH2)m-, R6CO-, R6OCO-, R6CH(NH2)CO-, NR7R8CO-, R6SO2-, R6SO2NR7CO-. R'6-NHC(=NR'7)- or a heterocyclic group of formula (i); or N(G)R3 = succinimido, maleimido, 2-oxo-pyrrolidino, 1H-1-pyrrolyl, 1H-1-imidazolyl or 2-oxo-2,3-dihydro-1H-1-pyrrolyl, all monosubstituted by R7; phthalimido or 2-oxo-1-indolinyl, both monosubstituted by R10 in the benzene ring; 1-indolyl; 1-benzimidazolyl; pyrrolidino, piperidino, perhydroazepino or perhydroazocino; or a group of formula (ii)-(vi); one ring C in (iv) is optionally replaced by O, S, SO2 or NR2; m = 0-3; r = 1 or 2; R6 = H, alkyl (optionally substituted as for Ar or by 3-6C cycloalkyl), 3-6C cycloalkyl (optionally substituted as for Ar), 2-6C alkenyl (optionally substituted as for Ar, or by Ar or Het (both optionally having a third substituent as above)); Ar-(CH2)m (in which Ar optionally has a third substituent as above and may further be substituted by OCF3, SO2NH2, NHCOCF3 or benzyl; and (CH2)m is optionally substituted by COOH), naphthyl, adamantyl or Het-(CH2)m-; R7 = H or alkyl; R8 = H, alkyl, Ar-(CH2)m- or Het-(CH2)m-; or NR7R8 = optionally substituted 4-7 membered ring, optionally having one C replaced by O, S or NH; R'6,R'7 = as R6,R7; or alkyl-CO-, NO2 or Ar-(CH2)m-SO2-; W = N, S or O; R10 = one or the optional substituents of Ar; A = direct bond, O, CH=CH or C IDENTICAL C; B = (CH2)m, O(CH2)q or CH=CH; q = 1-5; D = (CH2)s, optionally with one C replaced by optionally substituted NH, O or S; s = 1-6; X = CH=CH, O or S; R9 = H; or can also be alkyl, phenyl, succinimidyl, benzotriazolyl or benzyl if G = H; unless specified otherwise alkyl moieties have 1-6C.

公开(公告)号：CA2237052A1

公开(公告)日：1998-11-09

申请号：CA2237052

申请日：1998-05-07

Applicant: HOECHST AG

Inventor： THORWART WERNER ,  BILLEN GUENTER ,  SCHWAB WILFRIED ,  NEISES BERNHARD ,  SCHUDOK MANFRED ,  HAASE BURKHARD

IPC: C07D295/18 ,  A61K31/195 ,  A61K31/215 ,  A61K31/27 ,  A61K31/275 ,  A61K31/33 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/48 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/02 ,  A61P9/10 ,  A61P19/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C311/13 ,  C07C311/19 ,  C07C311/22 ,  C07C311/29 ,  C07C323/59 ,  C07D207/16 ,  C07D207/34 ,  C07D207/38 ,  C07D209/46 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D215/14 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D233/74 ,  C07D235/08 ,  C07D235/24 ,  C07D241/24 ,  C07D249/08 ,  C07D249/12 ,  C07D261/10 ,  C07D261/18 ,  C07D275/04 ,  C07D277/06 ,  C07D277/28 ,  C07D307/24 ,  C07D307/54 ,  C07D307/58 ,  C07D307/68 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/12 ,  C07D513/04 ,  C07D235/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D249/18 ,  A61K31/18 ,  C07D295/205 ,  C07D239/42 ,  C07D209/44 ,  C07D215/48 ,  C07D239/54 ,  C07C311/64 ,  C07D317/68

Abstract: Substituted diaminocarboxylic acids Compounds of the formula I (see fig. I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

公开(公告)号：HU9801045D0

公开(公告)日：1998-07-28

申请号：HU9801045

申请日：1998-05-08

Applicant: HOECHST AG

Inventor： BILLEN GUENTER ,  HAASE BURKHARD ,  NEISES BERNHARD ,  SCHUDOK MANFRED ,  SCHWAB WILFRIED ,  THORWART WERNER

IPC: C07D295/18 ,  A61K31/195 ,  A61K31/215 ,  A61K31/27 ,  A61K31/275 ,  A61K31/33 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/48 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/02 ,  A61P9/10 ,  A61P19/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C311/13 ,  C07C311/19 ,  C07C311/22 ,  C07C311/29 ,  C07C323/59 ,  C07D207/16 ,  C07D207/34 ,  C07D207/38 ,  C07D209/46 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D215/14 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D233/74 ,  C07D235/08 ,  C07D235/24 ,  C07D241/24 ,  C07D249/08 ,  C07D249/12 ,  C07D261/10 ,  C07D261/18 ,  C07D275/04 ,  C07D277/06 ,  C07D277/28 ,  C07D307/24 ,  C07D307/54 ,  C07D307/58 ,  C07D307/68 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/12 ,  C07D513/04

Abstract: Phenyl-, thienyl- or furanyl-substituted N( alpha )-sulphonyl-diaminocarboxylic acid derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 of 1-7C alkyl, 3-7C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN, NO2, COOH, alkyl-O-CO-, OCH2O, NR4R5CO and NR4R5); Het = pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thienyl, thiazolyl, oxazolyl, isoxazolyl, pyridinyl, pyrimidinyl, indolyl, benzothiophenyl, benzimidazolyl, benzoxazolyl, benzothiazolyl or benzotriazolyl (all optionally substituted as for phenyl in Ar); R2,R4,R5 = H, alkyl, carboxyalkyl, Ar-(CH2)o- or picolyl; or NR4R5 = 4-7 membered ring, optionally having one C replaced by O, S or NH; o = 0-2; R3,G = H, alkyl, 3-6C cycloalkyl, 2-6C alkenyl, Ar-(CH2)m-, Het-(CH2)m-, R6CO-, R6OCO-, R6CH(NH2)CO-, NR7R8CO-, R6SO2-, R6SO2NR7CO-. R'6-NHC(=NR'7)- or a heterocyclic group of formula (i); or N(G)R3 = succinimido, maleimido, 2-oxo-pyrrolidino, 1H-1-pyrrolyl, 1H-1-imidazolyl or 2-oxo-2,3-dihydro-1H-1-pyrrolyl, all monosubstituted by R7; phthalimido or 2-oxo-1-indolinyl, both monosubstituted by R10 in the benzene ring; 1-indolyl; 1-benzimidazolyl; pyrrolidino, piperidino, perhydroazepino or perhydroazocino; or a group of formula (ii)-(vi); one ring C in (iv) is optionally replaced by O, S, SO2 or NR2; m = 0-3; r = 1 or 2; R6 = H, alkyl (optionally substituted as for Ar or by 3-6C cycloalkyl), 3-6C cycloalkyl (optionally substituted as for Ar), 2-6C alkenyl (optionally substituted as for Ar, or by Ar or Het (both optionally having a third substituent as above)); Ar-(CH2)m (in which Ar optionally has a third substituent as above and may further be substituted by OCF3, SO2NH2, NHCOCF3 or benzyl; and (CH2)m is optionally substituted by COOH), naphthyl, adamantyl or Het-(CH2)m-; R7 = H or alkyl; R8 = H, alkyl, Ar-(CH2)m- or Het-(CH2)m-; or NR7R8 = optionally substituted 4-7 membered ring, optionally having one C replaced by O, S or NH; R'6,R'7 = as R6,R7; or alkyl-CO-, NO2 or Ar-(CH2)m-SO2-; W = N, S or O; R10 = one or the optional substituents of Ar; A = direct bond, O, CH=CH or C IDENTICAL C; B = (CH2)m, O(CH2)q or CH=CH; q = 1-5; D = (CH2)s, optionally with one C replaced by optionally substituted NH, O or S; s = 1-6; X = CH=CH, O or S; R9 = H; or can also be alkyl, phenyl, succinimidyl, benzotriazolyl or benzyl if G = H; unless specified otherwise alkyl moieties have 1-6C.