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公开(公告)号：CZ292521B6
公开(公告)日：2003-10-15
申请号：CZ360097
申请日：1997-11-13
Applicant: HOECHST AG
Inventor： STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , HULS CHRISTOPH DR , SEIFFGE DIRK DR
IPC: C07D233/76 , A61K31/415 , A61K31/4166 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/54 , C07D233/72 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/08 , C07K5/10 , C07K5/117
Abstract: In the present invention there are disclosed compounds of the general formula I, in which the symbols B, D, E, R, W, Y, Z, b, c, d, e, f, g, and h have specific meanings, are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4, which belongs to the group of integrins. The invention describes the use of compounds of the general formula I, for the preparation of medicaments intended for the treatment and prophylaxis of diseases, which are caused by an un desired extent of leucocyte adhesion and/or leucocyte migration or which are associated with leucocyte adhesion and/or leucocyte migration or in which cell-cell or cell-matrix interactions play a part which are based on interactions of VLA-4 receptors with their ligands, for example of inflammatory processes, rheumatoid arthritis or allergic disorders. Further described are novel compounds of the formula I per se, and pharmaceutical preparations containing these novel compounds.
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公开(公告)号：SI0842943T1
公开(公告)日：2003-08-31
申请号：SI9730524
申请日：1997-11-10
Applicant: HOECHST AG
Inventor： STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , KNOLLE JOCHEN DR , BARTNIK ECKART DR , HUELS CHRISTOPH DR
IPC: A61K31/415 , A61K31/4166 , A61K31/4178 , A61K31/421 , A61K31/426 , A61K38/00 , A61K38/06 , C07D233/00 , A61K38/07 , A61K38/39 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/32 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/86 , C07D257/00 , C07D403/12 , C07D405/12 , C07K5/02 , C07K5/023 , C07K5/078 , C07K5/08 , C07K5/097 , C07K5/10 , C07K5/117 , C07K7/06 , C07K14/78
Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer (or mixture) forms, or their salts for inhibiting the adhesion and/or migration of leukocytes or inhibiting VLA-4 receptors is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = 1-6C alkylene, 3-7C cycloalkylene, (1-6C) alkylene-phenylene, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally substituted); B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenylene; D = CR2R3, NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, 3-8C cycloalkyl, Ar or Ar-alkyl ; R1 = X-NH-C(=NH)-(CH2)p or X1-NH-(CH2)p; p = 0-3; X = H, 1-6C alkyl, (1-6C) alkylcarbonyl, Ar-(1-6C) alkoxycarbonyl, CN, OH, etc.; X1 = X etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, alkenyl, alkynyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar-alkyl or 3-8C cycloalkyl; b, c, d, f = 0 or 1, but not all 0; e, g, h= 0-6; Ar = optionally substituted 6-14C aryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.
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公开(公告)号：DK0842945T3
公开(公告)日：2003-06-10
申请号：DK97119636
申请日：1997-11-10
Applicant: HOECHST AG
Inventor： HUELS CHRISTOPH DR , SEIFFGE DIRK DR , WEHNER VOLKMAR DR , STILZ HANS ULRICH DR
IPC: C07D277/20 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/54 , C07D233/72 , C07D277/34 , C07K5/06 , C07K5/078 , C07K5/097 , C07K5/107 , C07K5/11 , C07K5/117
Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer or mixture forms, or their salts as medicaments is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = direct bond, 3-12C cycloalkylene, (1-6C) alkylene-(3-12C) cycloalkylene, phenylene, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally mono- or disubstituted) etc.; B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenylene; D = CR2R3, NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het '-alkyl (where alkyl residues are optionally substituted by one or more F); R1 = SR21, SSR21, SOR22, SO2R22, S-OR21, SO-OR21, SO2-OR21, SCOR21, SCOOR22, SCSSR22, OCOR21, OCSR21, OCOOR22, OSO2R22, OSO-R22, OP(O)(OR21)2, P(O)(OR21)2, P(O)(R22)OR21, CN, halo etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl, alkenyl, alkynyl, alkenylcarbonyl, alkynylcarbonyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl or (3-8C) cycloalkylalkyl; R21 = H, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het'-alkyl (where alkyl residues are optionally substituted by one or more F); b, c, d, f = 0 or 1 provided not all are 0; e, g,h = 0-6; Ar = optionally substituted 6-14C aryl; Het' = optionally substituted heteroaryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.
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公开(公告)号：AT233276T
公开(公告)日：2003-03-15
申请号：AT97119638
申请日：1997-11-10
Applicant: HOECHST AG
Inventor： STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , KNOLLE JOCHEN DR , BARTNIK ECKART DR , HUELS CHRISTOPH DR
IPC: C07D233/00 , A61K31/415 , A61K31/4166 , A61K31/4178 , A61K31/421 , A61K31/426 , A61K38/00 , A61K38/06 , A61K38/07 , A61K38/39 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/32 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/86 , C07D257/00 , C07D403/12 , C07D405/12 , C07K5/02 , C07K5/023 , C07K5/078 , C07K5/08 , C07K5/097 , C07K5/10 , C07K5/117 , C07K7/06 , C07K14/78
Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer (or mixture) forms, or their salts for inhibiting the adhesion and/or migration of leukocytes or inhibiting VLA-4 receptors is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = 1-6C alkylene, 3-7C cycloalkylene, (1-6C) alkylene-phenylene, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally substituted); B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenylene; D = CR2R3, NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, 3-8C cycloalkyl, Ar or Ar-alkyl ; R1 = X-NH-C(=NH)-(CH2)p or X1-NH-(CH2)p; p = 0-3; X = H, 1-6C alkyl, (1-6C) alkylcarbonyl, Ar-(1-6C) alkoxycarbonyl, CN, OH, etc.; X1 = X etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, alkenyl, alkynyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar-alkyl or 3-8C cycloalkyl; b, c, d, f = 0 or 1, but not all 0; e, g, h= 0-6; Ar = optionally substituted 6-14C aryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.
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Patent Agency Ranking
公开(公告)号：BR9705726A
公开(公告)日：1999-07-20
申请号：BR9705726
申请日：1997-11-14
Applicant: HOECHST AG
Inventor： STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , HUELS CHRISTOPH DR , SEIFFGE DIRK DR
IPC: C07D233/76 , A61K31/415 , A61K31/4166 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/54 , C07D233/72 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/08 , C07K5/10 , C07K5/117 , C07K5/00 , A61K38/04
Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer or mixture forms, or their salts is for inhibiting the adhesion and/or migration of leukocytes or inhibiting VLA-4 receptors is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = 1-6C alkylene, 3-12C cycloalkylene, (1-6C), phenylene-(1-6C)alkyl, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally mono- or disubstituted) etc.; B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenyl; D = CR2R3. NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het'-alkyl (where alkyl residues are optionally substituted); R1 = H, 1-10C alkyl (optionally fluorinated), cycloalkyl, cycloalkylalkyl, O or S etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl, alkenyl, alkynyl, alkenylcarbonyl, alkynylcarbonyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar-alkyl or 3-8C cycloalkyl; b, c, d, f = 0 or 1, but not all 0; e, g, h= 0-6; Ar = optionally substituted 6-14C aryl; Het' = optionally substituted heteroaryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.
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公开(公告)号：CZ9704113A3
公开(公告)日：1998-07-15
申请号：CZ411397
申请日：1997-12-18
Applicant: HOECHST AG , GENENTECH INC
Inventor： WEHNER VOLKMAR DR , STILZ HANS ULRICH DR , PEYMAN ANUSCHIRWAN DR , KNOLLE JOCHEN DR , RUXER JEAN-MARIE DR , CARNIATO DENIS DR , LEFRANCOIS JEAN-MICHEL , GADEK THOMAS RICHARD DR , MCDOWELL ROBERT DR
IPC: C07D239/00 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/33 , A61K31/395 , A61K31/415 , A61K31/4184 , A61K31/47 , A61K31/472 , A61K31/55 , A61K38/04 , A61P9/00 , A61P19/08 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C279/20 , C07C279/24 , C07C311/64 , C07C313/30 , C07C327/00 , C07D217/24 , C07D233/04 , C07D235/16 , C07D243/06 , C07D253/06 , C07D253/08 , C07D263/52 , C07D267/08 , C07D277/60 , C07D471/02 , C07D471/04 , C07D487/04 , C07K5/04
CPC classification number: C07D487/04
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公开(公告)号：CZ9704112A3
公开(公告)日：1998-07-15
申请号：CZ411297
申请日：1997-12-18
Applicant: HOECHST AG , GENENTECH INC
Inventor： WEHNER VOLKMAR DR , STILZ HANS ULRICH DR , PEYMAN ANUSCHIRWAN DR , SCHEUNEMANN KARLHEINZ DR , RUXER JEAN-MARIE DR , CARNIATO DENIS DR , LEFRANCOIS JEAN-MICHEL , GADEK THOMAS RICHARD DR , MCDOWELL ROBERT DR
IPC: C07D295/18 , A61K31/33 , A61K31/415 , A61K31/4184 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/536 , A61K31/5375 , A61K31/55 , A61K31/66 , A61P9/00 , A61P19/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D235/30 , C07D239/84 , C07D243/06 , C07D243/24 , C07D253/06 , C07D253/08 , C07D263/52 , C07D265/12 , C07D265/18 , C07D267/08 , C07D277/60 , C07D279/00 , C07D471/04 , C07D521/00 , C07F9/6561
CPC classification number: C07D243/24
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公开(公告)号：CZ9703601A3
公开(公告)日：1998-06-17
申请号：CZ360197
申请日：1997-11-13
Applicant: HOECHST AG
Inventor： STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , HULS CHRISTOPH DR , SEIFFGE DIRK DR
IPC: C07D277/20 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/54 , C07D233/72 , C07D277/34 , C07K5/06 , C07K5/078 , C07K5/097 , C07K5/107 , C07K5/11 , C07K5/117 , C07K5/08 , C07D207/00 , C07D213/00
CPC classification number: C07K5/1016 , A61K38/00 , C07K5/1019 , Y02A50/411
Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer or mixture forms, or their salts as medicaments is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = direct bond, 3-12C cycloalkylene, (1-6C) alkylene-(3-12C) cycloalkylene, phenylene, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally mono- or disubstituted) etc.; B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenylene; D = CR2R3, NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het '-alkyl (where alkyl residues are optionally substituted by one or more F); R1 = SR21, SSR21, SOR22, SO2R22, S-OR21, SO-OR21, SO2-OR21, SCOR21, SCOOR22, SCSSR22, OCOR21, OCSR21, OCOOR22, OSO2R22, OSO-R22, OP(O)(OR21)2, P(O)(OR21)2, P(O)(R22)OR21, CN, halo etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl, alkenyl, alkynyl, alkenylcarbonyl, alkynylcarbonyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl or (3-8C) cycloalkylalkyl; R21 = H, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het'-alkyl (where alkyl residues are optionally substituted by one or more F); b, c, d, f = 0 or 1 provided not all are 0; e, g,h = 0-6; Ar = optionally substituted 6-14C aryl; Het' = optionally substituted heteroaryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.
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公开(公告)号：DE19647380A1
公开(公告)日：1998-05-20
申请号：DE19647380
申请日：1996-11-15
Applicant: HOECHST AG
Inventor： STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , KNOLLE JOCHEN DR , BARTNIK ECKART DR , HUELS CHRISTOPH DR
IPC: C07D233/00 , A61K31/415 , A61K31/4166 , A61K31/4178 , A61K31/421 , A61K31/426 , A61K38/00 , A61K38/06 , A61K38/07 , A61K38/39 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/32 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/86 , C07D257/00 , C07D403/12 , C07D405/12 , C07K5/02 , C07K5/023 , C07K5/078 , C07K5/08 , C07K5/097 , C07K5/10 , C07K5/117 , C07K7/06 , C07K14/78 , C07K5/06 , A61K38/05 , C07D239/20
Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer (or mixture) forms, or their salts for inhibiting the adhesion and/or migration of leukocytes or inhibiting VLA-4 receptors is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = 1-6C alkylene, 3-7C cycloalkylene, (1-6C) alkylene-phenylene, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally substituted); B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenylene; D = CR2R3, NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, 3-8C cycloalkyl, Ar or Ar-alkyl ; R1 = X-NH-C(=NH)-(CH2)p or X1-NH-(CH2)p; p = 0-3; X = H, 1-6C alkyl, (1-6C) alkylcarbonyl, Ar-(1-6C) alkoxycarbonyl, CN, OH, etc.; X1 = X etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, alkenyl, alkynyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar-alkyl or 3-8C cycloalkyl; b, c, d, f = 0 or 1, but not all 0; e, g, h= 0-6; Ar = optionally substituted 6-14C aryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.
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