公开(公告)号：JPH11228529A

公开(公告)日：1999-08-24

申请号：JP16270798

申请日：1998-05-08

Applicant: HOECHST AG

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

Abstract: PROBLEM TO BE SOLVED: To obtain a new compound useful for producing drugs for preventing or treating diseases associated with an enhancement of an activity of matrix- decomposed metalloproteinase, concretely, e.g. osteoarthritis. SOLUTION: This compound is one shown by formula I [R is e.g. phenyl, an 1-7C alkyl or OH; R , R and R are each e.g. H, an 1-6C alkyl or picolyl; R and G are each e.g. H, an 1-6C alkyl or 2-6C alkenyl; A is e.g. a covalent bond or O; B is e.g.-(CH2 )m - ((m) is 0, 1 to 3); D is -(CH2 )m - ((m) is 1 to 6); X is -CH=CH-, Oor S], e.g. (R)-(4-chlorobiphenylsulfonyl)citrulline. The objective compound is obtained by reacting a diaminocarboxylic acid of formula II with a sulfonic acid derivative of formula III (Y is e.g. a halogen or imidazoline) in the presence of a base, pref., dehydrater.

公开(公告)号：BR9801604A

公开(公告)日：1999-06-08

申请号：BR9801604

申请日：1998-05-08

Applicant: HOECHST AG

Inventor： THORWART WERNER ,  SCHWAB WILFRIED DR ,  SCHUDOK MANFRED DR ,  HAASE BURKHARD DR ,  NEISES BERNHARD DR ,  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 ,  C07C311/37 ,  C07D239/69 ,  C07D317/68 ,  C07D309/08 ,  C07D209/42 ,  C07D277/68 ,  C07D249/18 ,  C07D215/48 ,  C07D265/30 ,  C07D275/06 ,  A61K31/18 ,  A61K31/495

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：CA2189222A1

公开(公告)日：1997-05-03

申请号：CA2189222

申请日：1996-10-30

Applicant: HOECHST AG

Inventor： BILLEN GUENTER ,  OKYAYUZ-BAKLOUTI ISMAHAN ,  ANAGNOSTOPULOS HIRISTO ,  MUELLNER STEFAN

IPC: A61K31/675 ,  A61P3/00 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/18 ,  A61P33/02 ,  A61P35/00 ,  A61P43/00 ,  C07F9/6561 ,  C07F9/547

Abstract: Alkylxanthine phosphonates and alkylxanthine phosphine oxides and their use as pharmaceuticals A compound of the formula ? (?) where R1 and R3 are identical or different and at least one of the radicals R1 and R3 is a radical of the formula XI (X?) in which E is a covalent bond or a (C1-C5)-alkyl, are suitable for the production of pharmaceuticals for the treatment of muscular atrophy, cachexia, muscular dystrophy, sepsis, septic shock, endotoxic shock, systemic inflammation response syndrome, adult respiratory distress syndrome, cerebral malaria, chronic pneumonia, pulmonary sarcoidosis, reperfusion damage, scar formation, inflammation of the bowel and ulcerative colitis, as a result of infections, acquired immune deficiency syndrome, cancer, trauma and other disorders having increased protein loss, peripheral circulatory disorders, disorders having altered leucocyte adhesion, and also disorders which are accompanied by an increased or unregulated tumor necrosis factor production such as rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis and other arthritic disorders.

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.

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.