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1. 发明专利

FI960850A0 未知
公开(公告)号：FI960850A0
公开(公告)日：1996-02-23
申请号：FI960850
申请日：1996-02-23
申请人： BAYER AG
发明人： PAESSENS ARNOLD , BLUNCK MARTIN , RIESS GUENTHER , KLEIM JOERG-PETER , ROESNER MANFRED
IPC分类号： A61K31/34 , C12N9/99 , A61K31/365 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/55 , A61K38/55 , A61K45/00 , A61K45/06 , A61P31/12 , A61P31/18 , A61P37/04 , C07D241/44 , A61K
摘要： Medicaments comprising, in combination, (a) one or more protease inhibitors and (b) one or more cpds. of formula (I) (or their tautomers of formula (Ia)) are new: n = 0-4; R = F, Cl, Br, I, CF3, CF3O, OH, 1-8C alkyl, Cya, TO, TO-R O, TS, TSO, TSO2, NO2, NH2, N3, NHT, NT2, piperidino, morpholino, 1-pyrrolidinyl, 4-methylpiperazinyl, thiomorpholino, imidazolyl, triazolyl, tetrazolyl, Ac, AcO, AcNH, CN, CONH2, COOH, TOCO, HOSO2 or SO2NH2; or Ph, PhO, PhOCO, PhS, PhSO, PhSO2, PhOSO2, PhSO2O, anilinosulphonyl, PhSO2NH, PhCO, 2-, 3- or 4-pyridyl (all opt. substd. by ≤ 5 R ); T = 1-6C alkyl; Cya = 5-8C cycloalkyl; R = 1-4C alkylene; R = F, Cl, Br, I, CN, CF3, CF3O, NO2, NH2, N3, T, Cy, TO, TS, TSO, TSO2, TNH, T2N, TOCO, Ph, PhO or 2-, 3- or 4-pyridyl; R ,R = H, OH, TO, ArO, AcO, CN, NH2, TNH, T2N, ArNH or AcNH; 1-8C alkyl, 2-8C alkenyl, 3-8C alkynyl, Cy, Cy', Cy-R , Cy'-R or TCO (all opt. substd. by F, Cl, Br, I, CN, NH2, SH, OH, AcO, PhCOO, PhCH2O, PhO, TO, TNH, T2N, TS, TSO2, PhSO2, oxo, thioxo, carboxy or carbamoyl); 3-8C alkenyl, 2-8C alkenylcarbonyl, CyCO, Cy''CO, Cy-(1-3C alkyl)carbonyl, 5-6C cycloalkenyl- (1-3C alkyl)carbonyl, 1-8C alkenyloxycarbonyl, 2-8C alkynyloxycarbonyl, 1-8C alkylthiocarbonyl, 2-8C alkenylthiocarbonyl, 1-8C alkylaminocarbonyl, di(1-8C alkyl)aminocarbonyl, TSO2, 2-6C alkenylsulphonyl, 2-8C alkenylaminocarbonyl or di((2-6C)alkenyl)- aminocarbonyl (all opt. substd. by F, Cl, OH, RO, oxo or phenyl); 1-8C alkoxycarbonyl (opt. substd. by F, Cl, Br, OH, RO, RNH, (R)2N or RS); pyrrolidin-1-yl, morpholino-, piperidino-, piperazinyl- or 4-methylpiperazin-1-yl-carbonyl (all opt. substd. by R, 2-6C alkenyl, 1-4C acyl, oxo, thioxo, carboxy or phenyl); Ar, ArCO, ArCS, ArS-CO, ArS-CS, ArOCO, ArSO2, ArNHCO, ArNHCS, aryl(1-5C)alkylaminocarbonyl, Ar', arylalkenyl, arylalkynyl, Ar'CO, arylalkenylcarbonyl, Ar'OCO or Ar'SCO (all opt. substd. by 1-5 R ); or Het, Het', Het-alkenyl, Het'CO, Het-alkenylcarbonyl, HetOCO, HetSCO, HetNHCO, Het'OCO, Het'SCO or Het'NHCO (all opt. substd. by 1-3 R ); Ar = aryl; Ar' = aryl(1-5C)alkyl; Het = heteroaryl; Het' = heteroaryl(1-3C)alkyl; R = 1-4C alkyl; Ac' = 1-6C acyl; Ph = phenyl; Cy = 3-8C cycloalkyl; Cy' = 3-8C cycloalkenyl; Cy'' = 5-8C cycloalkenyl; R , R = H; 1-8C alkyl, 2-8C alkenyl, Cy or Cy' (all opt. substd. by F, Cl, OH, NH2, SH, Ac'O, PhCOO, PhCH2O, PhO, RO, RNH, (R)2N, RS, RSO2, RSO, COOH or CONH2); Ar, aryl(1-3C)alkyl, Het or Het' (all opt. substd. by ≤ 5 R ); or R +R or R +R can be part of an unsatd. or satd. carbo- or heterocyclic ring of 3-8 atoms, which is opt. substd. by F, Cl, OH, NH2, T, 2-6C alkenyl, TO, 2-6C alkynyl, 1-6C acyloxy, benzoyloxy, oxo, thioxo, COOH, CONH2 or Ph); Ac' = 1-4C acyl; X = O, S, Se or NR ; with the exception of cpds. in which (a) R and R are both H, (b) R and R are H and R and R are arylalkyl, and (c) X is O and R and R are H.

2. 发明专利

BR9600809A 未知
公开(公告)号：BR9600809A
公开(公告)日：1997-12-23
申请号：BR9600809
申请日：1996-02-26
申请人： BAYER AG
发明人： PAESSENS ARNOLD , BLUNCK MARTIN , RIESS GUENTHER , KLEIM JOERG-PETER , ROESNER MANFRED
IPC分类号： C12N9/99 , A61K31/34 , A61K31/365 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/55 , A61K38/55 , A61K45/00 , A61K45/06 , A61P31/12 , A61P31/18 , A61P37/04 , C07D241/44 , A61K39/21
摘要： Medicaments comprising, in combination, (a) one or more protease inhibitors and (b) one or more cpds. of formula (I) (or their tautomers of formula (Ia)) are new: n = 0-4; R = F, Cl, Br, I, CF3, CF3O, OH, 1-8C alkyl, Cya, TO, TO-R O, TS, TSO, TSO2, NO2, NH2, N3, NHT, NT2, piperidino, morpholino, 1-pyrrolidinyl, 4-methylpiperazinyl, thiomorpholino, imidazolyl, triazolyl, tetrazolyl, Ac, AcO, AcNH, CN, CONH2, COOH, TOCO, HOSO2 or SO2NH2; or Ph, PhO, PhOCO, PhS, PhSO, PhSO2, PhOSO2, PhSO2O, anilinosulphonyl, PhSO2NH, PhCO, 2-, 3- or 4-pyridyl (all opt. substd. by ≤ 5 R ); T = 1-6C alkyl; Cya = 5-8C cycloalkyl; R = 1-4C alkylene; R = F, Cl, Br, I, CN, CF3, CF3O, NO2, NH2, N3, T, Cy, TO, TS, TSO, TSO2, TNH, T2N, TOCO, Ph, PhO or 2-, 3- or 4-pyridyl; R ,R = H, OH, TO, ArO, AcO, CN, NH2, TNH, T2N, ArNH or AcNH; 1-8C alkyl, 2-8C alkenyl, 3-8C alkynyl, Cy, Cy', Cy-R , Cy'-R or TCO (all opt. substd. by F, Cl, Br, I, CN, NH2, SH, OH, AcO, PhCOO, PhCH2O, PhO, TO, TNH, T2N, TS, TSO2, PhSO2, oxo, thioxo, carboxy or carbamoyl); 3-8C alkenyl, 2-8C alkenylcarbonyl, CyCO, Cy''CO, Cy-(1-3C alkyl)carbonyl, 5-6C cycloalkenyl- (1-3C alkyl)carbonyl, 1-8C alkenyloxycarbonyl, 2-8C alkynyloxycarbonyl, 1-8C alkylthiocarbonyl, 2-8C alkenylthiocarbonyl, 1-8C alkylaminocarbonyl, di(1-8C alkyl)aminocarbonyl, TSO2, 2-6C alkenylsulphonyl, 2-8C alkenylaminocarbonyl or di((2-6C)alkenyl)- aminocarbonyl (all opt. substd. by F, Cl, OH, RO, oxo or phenyl); 1-8C alkoxycarbonyl (opt. substd. by F, Cl, Br, OH, RO, RNH, (R)2N or RS); pyrrolidin-1-yl, morpholino-, piperidino-, piperazinyl- or 4-methylpiperazin-1-yl-carbonyl (all opt. substd. by R, 2-6C alkenyl, 1-4C acyl, oxo, thioxo, carboxy or phenyl); Ar, ArCO, ArCS, ArS-CO, ArS-CS, ArOCO, ArSO2, ArNHCO, ArNHCS, aryl(1-5C)alkylaminocarbonyl, Ar', arylalkenyl, arylalkynyl, Ar'CO, arylalkenylcarbonyl, Ar'OCO or Ar'SCO (all opt. substd. by 1-5 R ); or Het, Het', Het-alkenyl, Het'CO, Het-alkenylcarbonyl, HetOCO, HetSCO, HetNHCO, Het'OCO, Het'SCO or Het'NHCO (all opt. substd. by 1-3 R ); Ar = aryl; Ar' = aryl(1-5C)alkyl; Het = heteroaryl; Het' = heteroaryl(1-3C)alkyl; R = 1-4C alkyl; Ac' = 1-6C acyl; Ph = phenyl; Cy = 3-8C cycloalkyl; Cy' = 3-8C cycloalkenyl; Cy'' = 5-8C cycloalkenyl; R , R = H; 1-8C alkyl, 2-8C alkenyl, Cy or Cy' (all opt. substd. by F, Cl, OH, NH2, SH, Ac'O, PhCOO, PhCH2O, PhO, RO, RNH, (R)2N, RS, RSO2, RSO, COOH or CONH2); Ar, aryl(1-3C)alkyl, Het or Het' (all opt. substd. by ≤ 5 R ); or R +R or R +R can be part of an unsatd. or satd. carbo- or heterocyclic ring of 3-8 atoms, which is opt. substd. by F, Cl, OH, NH2, T, 2-6C alkenyl, TO, 2-6C alkynyl, 1-6C acyloxy, benzoyloxy, oxo, thioxo, COOH, CONH2 or Ph); Ac' = 1-4C acyl; X = O, S, Se or NR ; with the exception of cpds. in which (a) R and R are both H, (b) R and R are H and R and R are arylalkyl, and (c) X is O and R and R are H.

3. 发明专利

HU9600455A2 USE OF QUINOXALINES COMBINED WITH PROTEASE-INHIBITING COMPOUNDS FOR PRODUCING PHARMACEUTICAL COMPOSITIONS FOR TREATING AIDS AND/OR HIV INFECTIONS 未知
公开(公告)号：HU9600455A2
公开(公告)日：1996-12-30
申请号：HU9600455
申请日：1996-02-26
申请人： BAYER AG
发明人： BLUNCK MARTIN , KLEIM JOERG-PETER , PAESSENS ARNOLD , RIESS GUENTHER , ROESNER MANFRED
IPC分类号： A61K31/34 , A61K31/365 , A61K31/425 , C12N9/99 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/55 , A61K38/55 , A61K45/00 , A61K45/06 , A61P31/12 , A61P31/18 , A61P37/04 , C07D241/44 , A61K31/16
摘要： Medicaments comprising, in combination, (a) one or more protease inhibitors and (b) one or more cpds. of formula (I) (or their tautomers of formula (Ia)) are new: n = 0-4; R = F, Cl, Br, I, CF3, CF3O, OH, 1-8C alkyl, Cya, TO, TO-R O, TS, TSO, TSO2, NO2, NH2, N3, NHT, NT2, piperidino, morpholino, 1-pyrrolidinyl, 4-methylpiperazinyl, thiomorpholino, imidazolyl, triazolyl, tetrazolyl, Ac, AcO, AcNH, CN, CONH2, COOH, TOCO, HOSO2 or SO2NH2; or Ph, PhO, PhOCO, PhS, PhSO, PhSO2, PhOSO2, PhSO2O, anilinosulphonyl, PhSO2NH, PhCO, 2-, 3- or 4-pyridyl (all opt. substd. by ≤ 5 R ); T = 1-6C alkyl; Cya = 5-8C cycloalkyl; R = 1-4C alkylene; R = F, Cl, Br, I, CN, CF3, CF3O, NO2, NH2, N3, T, Cy, TO, TS, TSO, TSO2, TNH, T2N, TOCO, Ph, PhO or 2-, 3- or 4-pyridyl; R ,R = H, OH, TO, ArO, AcO, CN, NH2, TNH, T2N, ArNH or AcNH; 1-8C alkyl, 2-8C alkenyl, 3-8C alkynyl, Cy, Cy', Cy-R , Cy'-R or TCO (all opt. substd. by F, Cl, Br, I, CN, NH2, SH, OH, AcO, PhCOO, PhCH2O, PhO, TO, TNH, T2N, TS, TSO2, PhSO2, oxo, thioxo, carboxy or carbamoyl); 3-8C alkenyl, 2-8C alkenylcarbonyl, CyCO, Cy''CO, Cy-(1-3C alkyl)carbonyl, 5-6C cycloalkenyl- (1-3C alkyl)carbonyl, 1-8C alkenyloxycarbonyl, 2-8C alkynyloxycarbonyl, 1-8C alkylthiocarbonyl, 2-8C alkenylthiocarbonyl, 1-8C alkylaminocarbonyl, di(1-8C alkyl)aminocarbonyl, TSO2, 2-6C alkenylsulphonyl, 2-8C alkenylaminocarbonyl or di((2-6C)alkenyl)- aminocarbonyl (all opt. substd. by F, Cl, OH, RO, oxo or phenyl); 1-8C alkoxycarbonyl (opt. substd. by F, Cl, Br, OH, RO, RNH, (R)2N or RS); pyrrolidin-1-yl, morpholino-, piperidino-, piperazinyl- or 4-methylpiperazin-1-yl-carbonyl (all opt. substd. by R, 2-6C alkenyl, 1-4C acyl, oxo, thioxo, carboxy or phenyl); Ar, ArCO, ArCS, ArS-CO, ArS-CS, ArOCO, ArSO2, ArNHCO, ArNHCS, aryl(1-5C)alkylaminocarbonyl, Ar', arylalkenyl, arylalkynyl, Ar'CO, arylalkenylcarbonyl, Ar'OCO or Ar'SCO (all opt. substd. by 1-5 R ); or Het, Het', Het-alkenyl, Het'CO, Het-alkenylcarbonyl, HetOCO, HetSCO, HetNHCO, Het'OCO, Het'SCO or Het'NHCO (all opt. substd. by 1-3 R ); Ar = aryl; Ar' = aryl(1-5C)alkyl; Het = heteroaryl; Het' = heteroaryl(1-3C)alkyl; R = 1-4C alkyl; Ac' = 1-6C acyl; Ph = phenyl; Cy = 3-8C cycloalkyl; Cy' = 3-8C cycloalkenyl; Cy'' = 5-8C cycloalkenyl; R , R = H; 1-8C alkyl, 2-8C alkenyl, Cy or Cy' (all opt. substd. by F, Cl, OH, NH2, SH, Ac'O, PhCOO, PhCH2O, PhO, RO, RNH, (R)2N, RS, RSO2, RSO, COOH or CONH2); Ar, aryl(1-3C)alkyl, Het or Het' (all opt. substd. by ≤ 5 R ); or R +R or R +R can be part of an unsatd. or satd. carbo- or heterocyclic ring of 3-8 atoms, which is opt. substd. by F, Cl, OH, NH2, T, 2-6C alkenyl, TO, 2-6C alkynyl, 1-6C acyloxy, benzoyloxy, oxo, thioxo, COOH, CONH2 or Ph); Ac' = 1-4C acyl; X = O, S, Se or NR ; with the exception of cpds. in which (a) R and R are both H, (b) R and R are H and R and R are arylalkyl, and (c) X is O and R and R are H.

4. 发明专利

HRP960070A2 USE OF QUINOXALINE AND PROTEASE INHIBITORS IN A COMPOSITION FOR THE TREATMENT OF AIDS AND/OR HIV INFECTIONS 未知
公开(公告)号：HRP960070A2
公开(公告)日：1997-10-31
申请号：HRP960070
申请日：1996-02-13
申请人： BAYER AG
发明人： PAESSENS ARNOLD , BLUNCK MARTIN , RIESS GUENTHER , KLEIM JOERG-PETER , ROESNER MANFRED
IPC分类号： A61K31/34 , A61K31/365 , C12N9/99 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/55 , A61K38/55 , A61K45/00 , A61K45/06 , A61P31/12 , A61P31/18 , A61P37/04 , C07D241/44
摘要： Medicaments comprising, in combination, (a) one or more protease inhibitors and (b) one or more cpds. of formula (I) (or their tautomers of formula (Ia)) are new: n = 0-4; R = F, Cl, Br, I, CF3, CF3O, OH, 1-8C alkyl, Cya, TO, TO-R O, TS, TSO, TSO2, NO2, NH2, N3, NHT, NT2, piperidino, morpholino, 1-pyrrolidinyl, 4-methylpiperazinyl, thiomorpholino, imidazolyl, triazolyl, tetrazolyl, Ac, AcO, AcNH, CN, CONH2, COOH, TOCO, HOSO2 or SO2NH2; or Ph, PhO, PhOCO, PhS, PhSO, PhSO2, PhOSO2, PhSO2O, anilinosulphonyl, PhSO2NH, PhCO, 2-, 3- or 4-pyridyl (all opt. substd. by ≤ 5 R ); T = 1-6C alkyl; Cya = 5-8C cycloalkyl; R = 1-4C alkylene; R = F, Cl, Br, I, CN, CF3, CF3O, NO2, NH2, N3, T, Cy, TO, TS, TSO, TSO2, TNH, T2N, TOCO, Ph, PhO or 2-, 3- or 4-pyridyl; R ,R = H, OH, TO, ArO, AcO, CN, NH2, TNH, T2N, ArNH or AcNH; 1-8C alkyl, 2-8C alkenyl, 3-8C alkynyl, Cy, Cy', Cy-R , Cy'-R or TCO (all opt. substd. by F, Cl, Br, I, CN, NH2, SH, OH, AcO, PhCOO, PhCH2O, PhO, TO, TNH, T2N, TS, TSO2, PhSO2, oxo, thioxo, carboxy or carbamoyl); 3-8C alkenyl, 2-8C alkenylcarbonyl, CyCO, Cy''CO, Cy-(1-3C alkyl)carbonyl, 5-6C cycloalkenyl- (1-3C alkyl)carbonyl, 1-8C alkenyloxycarbonyl, 2-8C alkynyloxycarbonyl, 1-8C alkylthiocarbonyl, 2-8C alkenylthiocarbonyl, 1-8C alkylaminocarbonyl, di(1-8C alkyl)aminocarbonyl, TSO2, 2-6C alkenylsulphonyl, 2-8C alkenylaminocarbonyl or di((2-6C)alkenyl)- aminocarbonyl (all opt. substd. by F, Cl, OH, RO, oxo or phenyl); 1-8C alkoxycarbonyl (opt. substd. by F, Cl, Br, OH, RO, RNH, (R)2N or RS); pyrrolidin-1-yl, morpholino-, piperidino-, piperazinyl- or 4-methylpiperazin-1-yl-carbonyl (all opt. substd. by R, 2-6C alkenyl, 1-4C acyl, oxo, thioxo, carboxy or phenyl); Ar, ArCO, ArCS, ArS-CO, ArS-CS, ArOCO, ArSO2, ArNHCO, ArNHCS, aryl(1-5C)alkylaminocarbonyl, Ar', arylalkenyl, arylalkynyl, Ar'CO, arylalkenylcarbonyl, Ar'OCO or Ar'SCO (all opt. substd. by 1-5 R ); or Het, Het', Het-alkenyl, Het'CO, Het-alkenylcarbonyl, HetOCO, HetSCO, HetNHCO, Het'OCO, Het'SCO or Het'NHCO (all opt. substd. by 1-3 R ); Ar = aryl; Ar' = aryl(1-5C)alkyl; Het = heteroaryl; Het' = heteroaryl(1-3C)alkyl; R = 1-4C alkyl; Ac' = 1-6C acyl; Ph = phenyl; Cy = 3-8C cycloalkyl; Cy' = 3-8C cycloalkenyl; Cy'' = 5-8C cycloalkenyl; R , R = H; 1-8C alkyl, 2-8C alkenyl, Cy or Cy' (all opt. substd. by F, Cl, OH, NH2, SH, Ac'O, PhCOO, PhCH2O, PhO, RO, RNH, (R)2N, RS, RSO2, RSO, COOH or CONH2); Ar, aryl(1-3C)alkyl, Het or Het' (all opt. substd. by ≤ 5 R ); or R +R or R +R can be part of an unsatd. or satd. carbo- or heterocyclic ring of 3-8 atoms, which is opt. substd. by F, Cl, OH, NH2, T, 2-6C alkenyl, TO, 2-6C alkynyl, 1-6C acyloxy, benzoyloxy, oxo, thioxo, COOH, CONH2 or Ph); Ac' = 1-4C acyl; X = O, S, Se or NR ; with the exception of cpds. in which (a) R and R are both H, (b) R and R are H and R and R are arylalkyl, and (c) X is O and R and R are H.

5. 发明专利

FI960850A 未知
公开(公告)号：FI960850A
公开(公告)日：1996-08-28
申请号：FI960850
申请日：1996-02-23
申请人： BAYER AG
发明人： PAESSENS ARNOLD , BLUNCK MARTIN , RIESS GUENTHER , KLEIM JOERG-PETER , ROESNER MANFRED
IPC分类号： A61K31/34 , A61K31/365 , C12N9/99 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/55 , A61K38/55 , A61K45/00 , A61K45/06 , A61P31/12 , A61P31/18 , A61P37/04 , C07D241/44
摘要： Medicaments comprising, in combination, (a) one or more protease inhibitors and (b) one or more cpds. of formula (I) (or their tautomers of formula (Ia)) are new: n = 0-4; R = F, Cl, Br, I, CF3, CF3O, OH, 1-8C alkyl, Cya, TO, TO-R O, TS, TSO, TSO2, NO2, NH2, N3, NHT, NT2, piperidino, morpholino, 1-pyrrolidinyl, 4-methylpiperazinyl, thiomorpholino, imidazolyl, triazolyl, tetrazolyl, Ac, AcO, AcNH, CN, CONH2, COOH, TOCO, HOSO2 or SO2NH2; or Ph, PhO, PhOCO, PhS, PhSO, PhSO2, PhOSO2, PhSO2O, anilinosulphonyl, PhSO2NH, PhCO, 2-, 3- or 4-pyridyl (all opt. substd. by ≤ 5 R ); T = 1-6C alkyl; Cya = 5-8C cycloalkyl; R = 1-4C alkylene; R = F, Cl, Br, I, CN, CF3, CF3O, NO2, NH2, N3, T, Cy, TO, TS, TSO, TSO2, TNH, T2N, TOCO, Ph, PhO or 2-, 3- or 4-pyridyl; R ,R = H, OH, TO, ArO, AcO, CN, NH2, TNH, T2N, ArNH or AcNH; 1-8C alkyl, 2-8C alkenyl, 3-8C alkynyl, Cy, Cy', Cy-R , Cy'-R or TCO (all opt. substd. by F, Cl, Br, I, CN, NH2, SH, OH, AcO, PhCOO, PhCH2O, PhO, TO, TNH, T2N, TS, TSO2, PhSO2, oxo, thioxo, carboxy or carbamoyl); 3-8C alkenyl, 2-8C alkenylcarbonyl, CyCO, Cy''CO, Cy-(1-3C alkyl)carbonyl, 5-6C cycloalkenyl- (1-3C alkyl)carbonyl, 1-8C alkenyloxycarbonyl, 2-8C alkynyloxycarbonyl, 1-8C alkylthiocarbonyl, 2-8C alkenylthiocarbonyl, 1-8C alkylaminocarbonyl, di(1-8C alkyl)aminocarbonyl, TSO2, 2-6C alkenylsulphonyl, 2-8C alkenylaminocarbonyl or di((2-6C)alkenyl)- aminocarbonyl (all opt. substd. by F, Cl, OH, RO, oxo or phenyl); 1-8C alkoxycarbonyl (opt. substd. by F, Cl, Br, OH, RO, RNH, (R)2N or RS); pyrrolidin-1-yl, morpholino-, piperidino-, piperazinyl- or 4-methylpiperazin-1-yl-carbonyl (all opt. substd. by R, 2-6C alkenyl, 1-4C acyl, oxo, thioxo, carboxy or phenyl); Ar, ArCO, ArCS, ArS-CO, ArS-CS, ArOCO, ArSO2, ArNHCO, ArNHCS, aryl(1-5C)alkylaminocarbonyl, Ar', arylalkenyl, arylalkynyl, Ar'CO, arylalkenylcarbonyl, Ar'OCO or Ar'SCO (all opt. substd. by 1-5 R ); or Het, Het', Het-alkenyl, Het'CO, Het-alkenylcarbonyl, HetOCO, HetSCO, HetNHCO, Het'OCO, Het'SCO or Het'NHCO (all opt. substd. by 1-3 R ); Ar = aryl; Ar' = aryl(1-5C)alkyl; Het = heteroaryl; Het' = heteroaryl(1-3C)alkyl; R = 1-4C alkyl; Ac' = 1-6C acyl; Ph = phenyl; Cy = 3-8C cycloalkyl; Cy' = 3-8C cycloalkenyl; Cy'' = 5-8C cycloalkenyl; R , R = H; 1-8C alkyl, 2-8C alkenyl, Cy or Cy' (all opt. substd. by F, Cl, OH, NH2, SH, Ac'O, PhCOO, PhCH2O, PhO, RO, RNH, (R)2N, RS, RSO2, RSO, COOH or CONH2); Ar, aryl(1-3C)alkyl, Het or Het' (all opt. substd. by ≤ 5 R ); or R +R or R +R can be part of an unsatd. or satd. carbo- or heterocyclic ring of 3-8 atoms, which is opt. substd. by F, Cl, OH, NH2, T, 2-6C alkenyl, TO, 2-6C alkynyl, 1-6C acyloxy, benzoyloxy, oxo, thioxo, COOH, CONH2 or Ph); Ac' = 1-4C acyl; X = O, S, Se or NR ; with the exception of cpds. in which (a) R and R are both H, (b) R and R are H and R and R are arylalkyl, and (c) X is O and R and R are H.

6. 发明专利

HU9600455D0 USE OF QUINOXALINES COMBINED WITH PROTEASE-INHIBITING COMPOUNDS FOR PRODUCING PHARMACEUTICAL COMPOSITIONS FOR TREATING HIV INFECTIONS 未知
公开(公告)号：HU9600455D0
公开(公告)日：1996-04-29
申请号：HU9600455
申请日：1996-02-26
申请人： BAYER AG
发明人： BLUNCK MARTIN , KLEIM JOERG-PETER , PAESSENS ARNOLD , RIESS GUENTHER , ROESNER MANFRED
IPC分类号： C12N9/99 , A61K31/34 , A61K31/365 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/55 , A61K38/55 , A61K45/00 , A61K45/06 , A61P31/12 , A61P31/18 , A61P37/04 , C07D241/44
摘要： Medicaments comprising, in combination, (a) one or more protease inhibitors and (b) one or more cpds. of formula (I) (or their tautomers of formula (Ia)) are new: n = 0-4; R = F, Cl, Br, I, CF3, CF3O, OH, 1-8C alkyl, Cya, TO, TO-R O, TS, TSO, TSO2, NO2, NH2, N3, NHT, NT2, piperidino, morpholino, 1-pyrrolidinyl, 4-methylpiperazinyl, thiomorpholino, imidazolyl, triazolyl, tetrazolyl, Ac, AcO, AcNH, CN, CONH2, COOH, TOCO, HOSO2 or SO2NH2; or Ph, PhO, PhOCO, PhS, PhSO, PhSO2, PhOSO2, PhSO2O, anilinosulphonyl, PhSO2NH, PhCO, 2-, 3- or 4-pyridyl (all opt. substd. by ≤ 5 R ); T = 1-6C alkyl; Cya = 5-8C cycloalkyl; R = 1-4C alkylene; R = F, Cl, Br, I, CN, CF3, CF3O, NO2, NH2, N3, T, Cy, TO, TS, TSO, TSO2, TNH, T2N, TOCO, Ph, PhO or 2-, 3- or 4-pyridyl; R ,R = H, OH, TO, ArO, AcO, CN, NH2, TNH, T2N, ArNH or AcNH; 1-8C alkyl, 2-8C alkenyl, 3-8C alkynyl, Cy, Cy', Cy-R , Cy'-R or TCO (all opt. substd. by F, Cl, Br, I, CN, NH2, SH, OH, AcO, PhCOO, PhCH2O, PhO, TO, TNH, T2N, TS, TSO2, PhSO2, oxo, thioxo, carboxy or carbamoyl); 3-8C alkenyl, 2-8C alkenylcarbonyl, CyCO, Cy''CO, Cy-(1-3C alkyl)carbonyl, 5-6C cycloalkenyl- (1-3C alkyl)carbonyl, 1-8C alkenyloxycarbonyl, 2-8C alkynyloxycarbonyl, 1-8C alkylthiocarbonyl, 2-8C alkenylthiocarbonyl, 1-8C alkylaminocarbonyl, di(1-8C alkyl)aminocarbonyl, TSO2, 2-6C alkenylsulphonyl, 2-8C alkenylaminocarbonyl or di((2-6C)alkenyl)- aminocarbonyl (all opt. substd. by F, Cl, OH, RO, oxo or phenyl); 1-8C alkoxycarbonyl (opt. substd. by F, Cl, Br, OH, RO, RNH, (R)2N or RS); pyrrolidin-1-yl, morpholino-, piperidino-, piperazinyl- or 4-methylpiperazin-1-yl-carbonyl (all opt. substd. by R, 2-6C alkenyl, 1-4C acyl, oxo, thioxo, carboxy or phenyl); Ar, ArCO, ArCS, ArS-CO, ArS-CS, ArOCO, ArSO2, ArNHCO, ArNHCS, aryl(1-5C)alkylaminocarbonyl, Ar', arylalkenyl, arylalkynyl, Ar'CO, arylalkenylcarbonyl, Ar'OCO or Ar'SCO (all opt. substd. by 1-5 R ); or Het, Het', Het-alkenyl, Het'CO, Het-alkenylcarbonyl, HetOCO, HetSCO, HetNHCO, Het'OCO, Het'SCO or Het'NHCO (all opt. substd. by 1-3 R ); Ar = aryl; Ar' = aryl(1-5C)alkyl; Het = heteroaryl; Het' = heteroaryl(1-3C)alkyl; R = 1-4C alkyl; Ac' = 1-6C acyl; Ph = phenyl; Cy = 3-8C cycloalkyl; Cy' = 3-8C cycloalkenyl; Cy'' = 5-8C cycloalkenyl; R , R = H; 1-8C alkyl, 2-8C alkenyl, Cy or Cy' (all opt. substd. by F, Cl, OH, NH2, SH, Ac'O, PhCOO, PhCH2O, PhO, RO, RNH, (R)2N, RS, RSO2, RSO, COOH or CONH2); Ar, aryl(1-3C)alkyl, Het or Het' (all opt. substd. by ≤ 5 R ); or R +R or R +R can be part of an unsatd. or satd. carbo- or heterocyclic ring of 3-8 atoms, which is opt. substd. by F, Cl, OH, NH2, T, 2-6C alkenyl, TO, 2-6C alkynyl, 1-6C acyloxy, benzoyloxy, oxo, thioxo, COOH, CONH2 or Ph); Ac' = 1-4C acyl; X = O, S, Se or NR ; with the exception of cpds. in which (a) R and R are both H, (b) R and R are H and R and R are arylalkyl, and (c) X is O and R and R are H.

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