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1.发明授权3(5)-AMINO-PYRAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 有权3（5） - 氨基 - 吡唑衍生物，它们的制备方法和用途作为抗癌药
公开(公告)号：EP1202733B1
公开(公告)日：2005-10-05
申请号：EP00931906.2
申请日：2000-05-05
发明人： PEVARELLO, Paolo , ORSINI, Paolo , TRAQUANDI, Gabriella , VARASI, Mario , FRITZEN, Edward, L. , WARPEHOSKI, Martha, A. , PIERCE, Betsy, S. , BRASCA, Maria, Grabriella
IPC分类号： A61K31/415 , C07D231/40 , C07D231/16
CPC分类号： C07D403/12 , A61K31/415 , A61K31/4155 , A61K45/06 , C07D231/16 , C07D231/40 , C07D405/12 , C07D409/12
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2.发明授权3(5)-UREIDO-PYRAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 有权3（5） - 脲基 - 吡唑衍生物，它们的制备方法和用途作为抗癌药
公开(公告)号：EP1202734B1
公开(公告)日：2007-05-02
申请号：EP00955241.5
申请日：2000-08-11
发明人： PEVARELLO, Paolo , ORSINI, Paolo , TRAQUANDI, Gabriella , VARASI, Mario , FRITZEN, Edward, L. , WARPEHOSKI, Martha, A. , PIERCE, Betsy, S.
IPC分类号： A61K31/415 , A61K31/496 , C07D231/40 , C07D403/12
CPC分类号： C07D231/40 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/5377
摘要： 3-ureido-pyrazole derivatives represented by formula (I): where R, R1 and R2 are as described herein, or pharmaceutically acceptable salts thereof; are useful, for example, for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
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3.发明公开3(5)-AMINO-PYRAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 有权3（5） - 氨基 - 吡唑衍生物，它们的制备方法和用途作为抗癌药
公开(公告)号：EP1202733A1
公开(公告)日：2002-05-08
申请号：EP00931906.2
申请日：2000-05-05
发明人： PEVARELLO, Paolo , ORSINI, Paolo , TRAQUANDI, Gabriella , VARASI, Mario , FRITZEN, Edward, L. , WARPEHOSKI, Martha, A. , PIERCE, Betsy, S. , BRASCA, Maria, Grabriella
IPC分类号： A61K31/415 , C07D231/40
CPC分类号： C07D403/12 , A61K31/415 , A61K31/4155 , A61K45/06 , C07D231/16 , C07D231/40 , C07D405/12 , C07D409/12
摘要： Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C3-C6 cycloalkyl group optionally substituted by a straight or branched C1-C6 alkyl or arylalkyl group; R1 is a straight or branched C1-C6 alkyl, C2-C4 alkenyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl or arylalkenyl group, each of which may be optionally further substituted as indicated in the description; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
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公开(公告)号：EP1062212B1
公开(公告)日：2004-05-12
申请号：EP99915564.1
申请日：1999-03-04
发明人： MANTEGANI, Sergio , TRAQUANDI, Gabriella , BANDIERA, Tiziano , LANSEN, Jacqueline , VARASI, Mario
IPC分类号： C07D277/42 , C07D233/88 , A61K31/425 , A61K31/415
CPC分类号： C07D417/04 , C07D233/88 , C07D277/40 , C07D277/42
摘要： A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy; R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
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5.发明公开AZAINDOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS ANTITUMOR AGENTS 有权氮杂吲哚衍生物，其制造方法及其作为抗肿瘤药
公开(公告)号：EP1309590A1
公开(公告)日：2003-05-14
申请号：EP01943522.1
申请日：2001-06-13
发明人： LONGO, Antonio , BRASCA, Maria, Gabriella , ORSINI, Paolo , TRAQUANDI, Gabriella , PITTALA', Valeria , VULPETTI, Anna , VARASI, Mario , PEVARELLO, Paolo
IPC分类号： C07D471/04 , A61K31/437 , A61P35/04
CPC分类号： C07D471/04
摘要： Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I), as per the specification, and wherein R is a hydrogen or halogen atom or a group selected from -CN, -OH, -OCOR4, -(CH2)nNH2, -(CH2)nNHR4, -(CH2)nNHCOR4, -(CH2)nNHCONR4R5, -(CH2)nNHCOOR4, or -(CH2)nNHSO2R4, wherein n is either 0 or 1, R4 and R5 are as described in the specification; R1 is hydrogen or an optionally substituted alkyl group; R¿2? is an optionally substituted group selected from alkyl or aryl; R3 is hydrogen or a group selected from -CONR4R5, -COOR4, -CONHOR4, -SO2NHR4, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed; these compounds are useful for treating cell proliferative disorders associated with an altered cell cycle dependent kinase activity.
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6.发明公开PYRAZOLO-QUINAZOLINE DERIVATIVES,PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 有权PYRAZOLOCHINAZOLINDERIVATIVE，方法及其使用AS激酶抑制剂和及其
公开(公告)号：EP1636236A1
公开(公告)日：2006-03-22
申请号：EP04741483.4
申请日：2004-04-27
发明人： TRAQUANDI, Gabriella , BRASCA, Maria Gabriella , D'ALESSIO, Roberto , POLUCCI, Paolo , ROLETTO, Fulvia , VULPETTI, Anna , PEVARELLO, Paolo , PANZERI, Achille , QUARTIERI, Francesca , FERGUSON, Ron , VIANELLO, Paola , FANCELLI, Daniele
IPC分类号： C07D487/04 , C07D487/14 , A61K31/519 , A61P35/00
CPC分类号： C07D487/14 , A61K31/519 , A61K31/5377 , A61K31/551 , C07D231/56 , C07D239/72 , C07D401/10 , C07D403/14 , C07D413/14 , C07D487/04
摘要： Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
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7.发明授权2-AMINO-THIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS ANTITUMOR AGENTS 有权2-氨基噻唑衍生物，其制备方法及其作为抗癌剂的用途
公开(公告)号：EP1124810B1
公开(公告)日：2005-05-04
申请号：EP99955931.3
申请日：1999-10-27
发明人： PEVARELLO, Paolo , AMICI, Raffaella , TRAQUANDI, Gabriella , VILLA, Manuela , VULPETTI, Anna , ISACCHI, Antonella
IPC分类号： C07D277/46 , C07D417/12 , A61K31/426 , A61K31/427 , A61P35/00
CPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , C07D277/46
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8.发明公开3(5)-UREIDO-PYRAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 有权3（5） - 脲基 - 吡唑衍生物，它们的制备方法和用途作为抗癌药
公开(公告)号：EP1202734A1
公开(公告)日：2002-05-08
申请号：EP00955241.5
申请日：2000-08-11
发明人： PEVARELLO, Paolo , ORSINI, Paolo , TRAQUANDI, Gabriella , VARASI, Mario , FRITZEN, Edward, L. , WARPEHOSKI, Martha, A. , PIERCE, Betsy, S.
IPC分类号： A61K31/415 , A61K31/496 , C07D231/40 , C07D403/12
CPC分类号： C07D231/40 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/5377
摘要： 3-ureido-pyrazole derivatives represented by formula (I): where R, R1 and R2 are as described herein, or pharmaceutically acceptable salts thereof; are useful, for example, for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
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9.发明公开PHENYLACETAMIDO-THIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 有权苯乙酰胺基噻唑化合物，工艺作为生产，它们作为抗肿瘤药
公开(公告)号：EP1406899A2
公开(公告)日：2004-04-14
申请号：EP02760213.5
申请日：2002-07-02
发明人： PEVARELLO, Paolo , AMICI, Raffaella , VILLA, Manuela , SALOM, Barbara , VULPETTI, Anna , VARASI, Mario , BRASCA, Maria, Gabriella , TRAQUANDI, Gabriella , NESI, Marcella
IPC分类号： C07D417/12 , C07D277/46 , A61K31/425 , A61P35/00
CPC分类号： C07D417/12 , C07D277/46
摘要： Compounds represented by formula (I), as defined in the description, wherein R is a hydrogen atom or a methyl group and R1 is a group as defined in the specification, or a pharmaceutically acceptable salt thereof, are disclosed; the said compounds are useful in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
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10.发明公开CHROMANE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 审中-公开色，其制造方法相同，它们作为抗肿瘤药
公开(公告)号：EP1379524A2
公开(公告)日：2004-01-14
申请号：EP02719710.2
申请日：2002-01-17
发明人： TRAQUANDI, Gabriella , BRASCA, Maria, Gabriella , ORSINI, Paolo , PIUTTI, Claudia , VULPETTI, Anna , PEVARELLO, Paolo
IPC分类号： C07D405/12 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/4155 , A61P35/00
CPC分类号： C07D401/12 , A61K31/415 , A61K31/47 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： Compounds which are chromane derivatives of formula (I), pharmaceutically acceptable salts, process for their preparation and pharmaceutical compositions thereof are disclosed, as set forth in the specification; these compounds are useful in therapy in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
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