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1. 发明授权

EP0853616B1 BICYCLIC 4-ARALKYLAMINOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS 失效
标题翻译：双环4- aralkylaminopyrimidine衍生物作为酪氨酸激酶抑制剂
公开(公告)号：EP0853616B1
公开(公告)日：2001-09-19
申请号：EP97925987.6
申请日：1997-06-03
申请人： PHARMACIA & UPJOHN S.p.A.
发明人： BRASCA, Maria, Gabriella , BALLINARI, Dario , LONGO, Antonio , BUZZETTI, Franco
IPC分类号： C07D239/94 , C07D473/34 , A61K31/70 , A61K31/505
CPC分类号： C07D473/34 , C07D239/94
摘要： Novel and known bicyclic 4-aralkylaminopyrimidine derivatives of formula (I) wherein A is a benzene or imidazole ring; B is a benzene, tetralin, indane or 2-oxindole ring R is (C1-C4)perfluoroalkyl, phenyl, phenyl-(C1-C4)alkyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkoxy-(C1-C4)alkyl, (C2-C4)acyloxy-(C1-C4)alkyl, halobenzoyloxy-(C1-C4)alkyl, carboxy, carbamoyl, (C1-C4)alkoxycarbonyl, cyano, (C1-C4)alkylcarbonyl, carboxy-(C1-C4)alkyl, carbamoyl-(C1-C4)alkyl, (C1-C4)alkoxycarbonyl-(C1-C4)alkyl, halo-(C1-C4)alkyl, amino-(C1-C4)alkyl, mono- or di-(C1-C4)alkylamino-(C1-C4)alkyl, sulfo-(C1-C4)alkyl or sulfamido-(C1-C4)alkyl; each of R1 and R2, which may be the same or different, is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or -NR5R6 in which each of R5 and R6, which may be the same or different, is H or C1-C4 alkyl; each of R3 and R4, which may the same or different, is hydrogen, C1-C4 alkyl, halogen, hydroxy, C1-C4 alkoxy, C1-C4 alkoxycarbonyl, nitro, cyano or CF3; and the pharmaceutically acceptable salts thereof, are tyrosine kinase inhibitors.

2. 发明公开

EP0802914A1 ARYL AND HETEROARYL PURINE COMPOUNDS 失效
标题翻译：芳和HETEROARYLPURIN衍生物
公开(公告)号：EP0802914A1
公开(公告)日：1997-10-29
申请号：EP96934673.0
申请日：1996-10-14
申请人： PHARMACIA & UPJOHN S.p.A.
发明人： BUZZETTI, Franco , BRASCA, Maria, Gabriella , LONGO, Antonio , BALLINARI, Dario
IPC分类号： A61K31 , A61P25 , A61P35 , A61P37 , A61P43 , C07D471 , C07D473
CPC分类号： C07D473/00 , C07D471/04 , C07D473/30 , C07D473/34 , C07D473/38
摘要： Novel bicyclic condensed pyrimidine compounds having general formula (I) wherein X is -CH2-, -NH-(CH2)n-, -O-(CH2)n- or -S-(CH2)n- in which n is zero or 1; A is a 4,5-fused imidazole ring N-substituted by R3 which is hydrogen, C1-C4 alkyl or benzyl, or A is a 2,3-fused pyridine ring C-substituted by R4 which is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or NR5R6 in which each of R5 and R6 independently is H or C1-C4 alkyl; B is a bicyclic ring chosen from tetralin, indane and 2-oxindole; each of R1 and R2, independently, is hydrogen, C1-C4 alkyl, halogen, hydroxy, C1-C4 alkoxy, C1-C4 alkoxycarbonyl, nitro, cyano or CF3; and the pharmaceutically acceptable salts thereof; and wherein, when at the same time, A is pyridine and B is a tetralin ring, R4 is H, C1-C4 alkyl, C1-C4 alkoxy or halogen and X is as defined above, then each of R1 and R2 is other than H; and wherein, when at the same time, A is imidazole, X is -NH-(CH2)n- as defined above, and B is an indan ring unsubstituted or substituted by one or more of halogen, hydroxy, C1-C4 alkoxy and nitro, then R3 is other than C1-C4 alkyl or benzyl, are provided.

3. 发明授权

EP0658159B1 ARYLIDENE AND HETEROARYLIDENE OXINDOLE DERIVATIVES AS TYROSINE KINASE INHIBITORS 失效
标题翻译： ARYLIDEN-UND HETEROARYLIDEN-OXINDOL DERIVATE ALS TYROSIN KINASE INHIBITOREN
公开(公告)号：EP0658159B1
公开(公告)日：2000-08-23
申请号：EP94918379.2
申请日：1994-05-26
申请人： PHARMACIA & UPJOHN S.p.A.
发明人： BUZZETTI, Franco , LONGO, Antonio , BRASCA, Maria, Gabriella , ORZI, Fabrizio , CRUGNOLA, Angelo , BALLINARI, Dario , MARIANI, Mariangela
IPC分类号： C07D401/06 , A61K31/40 , C07D209/34
CPC分类号： C07D401/06 , C07C255/36 , C07C255/37 , C07C255/41 , C07C327/42 , C07C2602/10 , C07D209/18 , C07D209/34 , C07D215/14
摘要： Arylidene and heteroarylidene oxindole derivatives of formula (I) wherein, subject to provisos, Y is a bicyclic ring system chosen from naphthalene, tetralin, quinoline and isoquinoline; R is hydrogen or an oxo (=O) group when Y is tetralin; or R is hydrogen when Y is naphthalene, quinoline or isoquinoline; each of R?1 and R2¿ independently is hydrogen, C¿1?-C6 alkyl or C2-C6 alkanoyl; m is zero, 1 or 2; n is zero, 1, 2 or 3; each of R?3 and R4¿ independently is hydrogen, halogen, cyano, C¿1?-C6 alkyl, carboxy, nitro or -NR?6R7¿ in which each of R?6 and R7¿ independently is hydrogen or C¿1?-C6 alkyl; R?5¿ is hydrogen or C¿1?-C6 alkyl; and their pharmaceutically acceptable salts, which are useful as tyrosine kinase inhibitors.
摘要翻译：羟吲哚，丙烯酰胺，硫代丙烯酰胺和丙烯腈化合物及其药学上可接受的盐，其可用作酪氨酸激酶抑制剂。

4. 发明授权

EP0802914B1 ARYL- AND HETEROARYL- PURINE AND PYRIDOPYRIMIDINE DERIVATIVES 失效
标题翻译：芳基和杂嘌呤和PYRIDOPYRIMIDIN-衍生物
公开(公告)号：EP0802914B1
公开(公告)日：2001-06-06
申请号：EP96934673.3
申请日：1996-10-14
申请人： PHARMACIA & UPJOHN S.p.A.
发明人： BUZZETTI, Franco , BRASCA, Maria, Gabriella , LONGO, Antonio , BALLINARI, Dario
IPC分类号： C07D473/34 , C07D473/30 , C07D473/38 , C07D473/00 , C07D471/04 , A61K31/52
CPC分类号： C07D473/00 , C07D471/04 , C07D473/30 , C07D473/34 , C07D473/38
摘要： Novel bicyclic condensed pyrimidine compounds having general formula (I) wherein X is -CH2-, -NH-(CH2)n-, -O-(CH2)n- or -S-(CH2)n- in which n is zero or 1; A is a 4,5-fused imidazole ring N-substituted by R3 which is hydrogen, C1-C4 alkyl or benzyl, or A is a 2,3-fused pyridine ring C-substituted by R4 which is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or NR5R6 in which each of R5 and R6 independently is H or C1-C4 alkyl; B is a bicyclic ring chosen from tetralin, indane and 2-oxindole; each of R1 and R2, independently, is hydrogen, C1-C4 alkyl, halogen, hydroxy, C1-C4 alkoxy, C1-C4 alkoxycarbonyl, nitro, cyano or CF3; and the pharmaceutically acceptable salts thereof; and wherein, when at the same time, A is pyridine and B is a tetralin ring, R4 is H, C1-C4 alkyl, C1-C4 alkoxy or halogen and X is as defined above, then each of R1 and R2 is other than H; and wherein, when at the same time, A is imidazole, X is -NH-(CH2)n- as defined above, and B is an indan ring unsubstituted or substituted by one or more of halogen, hydroxy, C1-C4 alkoxy and nitro, then R3 is other than C1-C4 alkyl or benzyl, are provided.

5. 发明授权

EP0752985B1 HYDROSOLUBLE 3-ARYLIDENE-2-OXINDOLE DERIVATIVES AS TYROSINE KINASE INHIBITORS 失效
标题翻译：水溶性3- arylidenes -2-羟吲哚类衍生物作为酪氨酸激酶抑制剂
公开(公告)号：EP0752985B1
公开(公告)日：1999-08-04
申请号：EP95943238.6
申请日：1995-12-22
申请人： PHARMACIA & UPJOHN S.p.A.
发明人： BUZZETTI, Franco , BRASCA, Maria, Gabriella , LONGO, Antonio , BALLINARI, Dario
IPC分类号： C07D209/34 , A61K31/40
CPC分类号： C07D401/06 , C07D209/34
摘要： Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R1 is hydrogen, C¿1?-C6 alkyl or C2-C6 alkanoyl; one of R?2 and R3¿ independently is hydrogen and the other is a substituent selected from: a C¿1?-C6 alkyl group substituted by 1, 2 or 3 hydroxy groups; -SO3R?4¿ in which R4 is hydrogen or C¿1?-C6 alkyl unsubtituted or substituted by 1, 2 or 3 hydroxy groups; -SO2NHR?5¿ in which R5 is as R4 defined above or a -(CH¿2?)n-N(C1-C6 alkyl)2 group in which n is 2 or 3; -COOR?6¿ in which R6 is C1-C6 alkyl unsubtituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; -CONHR7 in which R7 is hydrogen, phenyl or C¿1?-C6 alkyl substituted by 1, 2 or 3 hydroxy groups or by phenyl; -NHSO2R?8¿ in which R8 is C1-C6 alkyl or phenyl unsubtituted or substituted by halogen or by C1-C4 alkyl; -N(R9)2, -NHR?9 or -OR9¿ wherein R9 is C2-C6 alkyl substituted by 1, 2 or 3 hydroxy groups; -NHCOR?10, -OOCR10¿ or -CH¿2OOCR?10 in which R10 is C1-C6 alkyl substituted by 1, 2 or 3 hydroxy groups; -NHCONH2; -NH-C(NH2)=NH; -C(NH2)=NH; -CH2NHC(NH2)=NH; -CH2NH2; -OPO(OH)2; -CH2OPO(OH)2; -PO(OH)2; or (a), (b), (c), or (d) group, wherein p is 1, 2 or 3 and Z is -CH2-, -O- or (e), in which R11 is hydrogen or is as R9 defined above; and the pharmaceutically acceptable salts thereof, are disclosed.

6. 发明公开

EP0853616A1 BICYCLIC 4-ARALKYLAMINOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS 失效
标题翻译：双环4- aralkylaminopyrimidine衍生物作为酪氨酸激酶抑制剂
公开(公告)号：EP0853616A1
公开(公告)日：1998-07-22
申请号：EP97925987.0
申请日：1997-06-03
申请人： PHARMACIA & UPJOHN S.p.A.
发明人： BRASCA, Maria, Gabriella , BALLINARI, Dario , LONGO, Antonio , BUZZETTI, Franco
IPC分类号： A61K31 , A61P25 , A61P35 , A61P43 , C07D239 , C07D473
CPC分类号： C07D473/34 , C07D239/94
摘要： Novel and known bicyclic 4-aralkylaminopyrimidine derivatives of formula (I) wherein A is a benzene or imidazole ring; B is a benzene, tetralin, indane or 2-oxindole ring R is (C1-C4)perfluoroalkyl, phenyl, phenyl-(C1-C4)alkyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkoxy-(C1-C4)alkyl, (C2-C4)acyloxy-(C1-C4)alkyl, halobenzoyloxy-(C1-C4)alkyl, carboxy, carbamoyl, (C1-C4)alkoxycarbonyl, cyano, (C1-C4)alkylcarbonyl, carboxy-(C1-C4)alkyl, carbamoyl-(C1-C4)alkyl, (C1-C4)alkoxycarbonyl-(C1-C4)alkyl, halo-(C1-C4)alkyl, amino-(C1-C4)alkyl, mono- or di-(C1-C4)alkylamino-(C1-C4)alkyl, sulfo-(C1-C4)alkyl or sulfamido-(C1-C4)alkyl; each of R1 and R2, which may be the same or different, is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or -NR5R6 in which each of R5 and R6, which may be the same or different, is H or C1-C4 alkyl; each of R3 and R4, which may the same or different, is hydrogen, C1-C4 alkyl, halogen, hydroxy, C1-C4 alkoxy, C1-C4 alkoxycarbonyl, nitro, cyano or CF3; and the pharmaceutically acceptable salts thereof, are tyrosine kinase inhibitors.

7. 发明公开

EP0752985A1 HYDROSOLUBLE 3-ARYLIDENE-2-OXINDOLE DERIVATIVES AS TYROSINE KINASE INHIBITORS 失效
标题翻译：水溶性3- arylidenes -2-羟吲哚类衍生物作为酪氨酸激酶抑制剂
公开(公告)号：EP0752985A1
公开(公告)日：1997-01-15
申请号：EP95943238.0
申请日：1995-12-22
申请人： PHARMACIA & UPJOHN S.p.A.
发明人： BUZZETTI, Franco , BRASCA, Maria, Gabriella , LONGO, Antonio , BALLINARI, Dario
IPC分类号： A61K31 , A61P3 , A61P9 , A61P11 , A61P35 , A61P43 , C07D209 , C07D401
CPC分类号： C07D401/06 , C07D209/34
摘要： Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R1 is hydrogen, C¿1?-C6 alkyl or C2-C6 alkanoyl; one of R?2 and R3¿ independently is hydrogen and the other is a substituent selected from: a C¿1?-C6 alkyl group substituted by 1, 2 or 3 hydroxy groups; -SO3R?4¿ in which R4 is hydrogen or C¿1?-C6 alkyl unsubtituted or substituted by 1, 2 or 3 hydroxy groups; -SO2NHR?5¿ in which R5 is as R4 defined above or a -(CH¿2?)n-N(C1-C6 alkyl)2 group in which n is 2 or 3; -COOR?6¿ in which R6 is C1-C6 alkyl unsubtituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; -CONHR7 in which R7 is hydrogen, phenyl or C¿1?-C6 alkyl substituted by 1, 2 or 3 hydroxy groups or by phenyl; -NHSO2R?8¿ in which R8 is C1-C6 alkyl or phenyl unsubtituted or substituted by halogen or by C1-C4 alkyl; -N(R9)2, -NHR?9 or -OR9¿ wherein R9 is C2-C6 alkyl substituted by 1, 2 or 3 hydroxy groups; -NHCOR?10, -OOCR10¿ or -CH¿2OOCR?10 in which R10 is C1-C6 alkyl substituted by 1, 2 or 3 hydroxy groups; -NHCONH2; -NH-C(NH2)=NH; -C(NH2)=NH; -CH2NHC(NH2)=NH; -CH2NH2; -OPO(OH)2; -CH2OPO(OH)2; -PO(OH)2; or (a), (b), (c), or (d) group, wherein p is 1, 2 or 3 and Z is -CH2-, -O- or (e), in which R11 is hydrogen or is as R9 defined above; and the pharmaceutically acceptable salts thereof, are disclosed.

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