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31.发明申请SUBSTITUTED DIHYDROPTERIDIN-6-ONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 失效取代的二氢蝶啶-6-酮衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US20110053944A1
公开(公告)日：2011-03-03
申请号：US12744770
申请日：2008-11-26
IPC分类号： A61K31/4985 , C07D475/04 , A61P35/00 , A61P37/02
CPC分类号： C07D475/00
摘要： Dihydropteridin-6-one derivatives of formula (I) 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.
摘要翻译： 公开了说明书中定义的式（I）的二氢蝶啶-6-酮衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。
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32.发明授权3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents 失效3（5） - 氨基 - 吡唑衍生物，其制备方法及其作为抗肿瘤剂的用途公开(公告)号：US06218418B1
公开(公告)日：2001-04-17
申请号：US09667603
申请日：2000-09-22
申请人： Paolo Pevarello , Paolo Orsini , Gabriella Traquandi , Mario Varasi , Edward L. Fritzen , Martha A. Warpehoski , Betsy S. Pierce , Maria Gabriella Brasca
发明人： Paolo Pevarello , Paolo Orsini , Gabriella Traquandi , Mario Varasi , Edward L. Fritzen , Martha A. Warpehoski , Betsy S. Pierce , Maria Gabriella Brasca
IPC分类号： A61K31415
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): where R is a C3-C6 cycloalkyl group, which may optionally be substituted by a straight or branched C1-C6 alkyl group, and R1 is a straight or branched C1-C6 alkyl group or a C2-C4 alkenyl, cycloalkyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl and arylalkenyl, which may be optionally substituted; 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.
摘要翻译： 由式（I）表示的3-氨基 - 吡唑衍生物的化合物：其中R是可以被直链或支链C1-C6烷基取代的C3-C6环烷基，R1是直链或支链C1-C6 烷基或C 2 -C 4烯基，环烷基，芳基，芳基烷基，芳基羰基，芳氧基烷基和芳基烯基，其可以任选被取代; 或其药学上可接受的盐。该化合物可用于治疗癌症，细胞增殖性疾病，阿尔茨海默氏病，病毒感染，自身免疫性疾病或神经变性疾病。
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公开(公告)号：US20140155421A1
公开(公告)日：2014-06-05
申请号：US14112559
申请日：2012-04-05
申请人： Maria Gabriella Brasca , Tiziano Bandiera , Jay Aaron Bertrand , Paola Gnocchi , Danilo Mirizzi , Marcella Nesi , Achille Panzeri
发明人： Maria Gabriella Brasca , Tiziano Bandiera , Jay Aaron Bertrand , Paola Gnocchi , Danilo Mirizzi , Marcella Nesi , Achille Panzeri
IPC分类号： A61K31/506 , C07F5/02 , C07D405/14 , C07D403/04
CPC分类号： A61K31/506 , C07D403/04 , C07D405/14 , C07F5/025
摘要： The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明涉及调节蛋白激酶活性的式（I）的取代的嘧啶基 - 吡咯化合物，因此可用于治疗由失调蛋白激酶活性引起的疾病，尤其是Janus激酶。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物。
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公开(公告)号：US08623876B2
公开(公告)日：2014-01-07
申请号：US13495688
申请日：2012-06-13
IPC分类号： A61K31/497 , A01N43/40 , A61K31/445 , A01N43/56 , A61K31/415 , C07D211/32 , C07D231/54 , C07D487/02
CPC分类号： C07D487/04
摘要： Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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 dysregulated protein kinase activity, like cancer.
摘要翻译： 公开了如说明书中定义的式（I）的取代吡咯并吡唑衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。
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公开(公告)号：US20130344031A1
公开(公告)日：2013-12-26
申请号：US14010819
申请日：2013-08-27
申请人： Maria Gabriella Brasca , Raffaella Amici , Daniele Fancelli , Marcella Nesi , Paolo Orsini , Fabrizio Orzi , Patrick Roussel , Anna Vulpetti , Paolo Pevarello
发明人： Maria Gabriella Brasca , Raffaella Amici , Daniele Fancelli , Marcella Nesi , Paolo Orsini , Fabrizio Orzi , Patrick Roussel , Anna Vulpetti , Paolo Pevarello
IPC分类号： C07D487/04 , A61K31/454 , A61N5/10 , A61K31/4162 , A61K45/06 , A61K31/5377 , A61K31/496
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , A61N5/10
摘要： Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
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36.发明授权Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors 有权取代的吡唑并喹唑啉衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US08614220B2
公开(公告)日：2013-12-24
申请号：US12520842
申请日：2007-12-17
申请人： Michele Caruso , Italo Beria , Maria Gabriella Brasca , Ron Ferguson , Helena Posteri , Barbara Valsasina
发明人： Michele Caruso , Italo Beria , Maria Gabriella Brasca , Ron Ferguson , Helena Posteri , Barbara Valsasina
IPC分类号： A61K31/519 , C07D239/70
CPC分类号： C07D487/04 , C07D295/135 , C07D295/155 , C40B40/04 , C40B50/14
摘要： Pyrazolo-quinazoline derivatives of formula (I) 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.
摘要翻译： 公开了说明书中定义的式（I）的吡唑并喹唑啉衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。
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37.发明授权Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors 失效取代的二氢蝶啶-6-酮衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US08598172B2
公开(公告)日：2013-12-03
申请号：US12744770
申请日：2008-11-26
IPC分类号： A61K31/495 , C07D475/00
CPC分类号： C07D475/00
摘要： Dihydropteridin-6-one derivatives of formula (I) 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.
摘要翻译： 公开了说明书中定义的式（I）的二氢蝶啶-6-酮衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。
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公开(公告)号：US08586598B2
公开(公告)日：2013-11-19
申请号：US13265918
申请日：2010-04-23
IPC分类号： A61K31/505 , C07D491/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.
摘要翻译： 本发明涉及新型的水溶性盐和cdk抑制剂游离碱的结晶形式。 这种结晶盐例如是富马酸盐，L-苹果酸盐，马来酸盐，琥珀酸盐，己二酸盐，丙二酸盐，乙醇酸盐，磷酸盐，甲磺酸盐，L-乳酸盐，盐酸盐，二盐酸盐，三盐酸盐。 这种新盐形式的水合物和多晶型物，其制备方法，其在治疗中的用途和含有它们的药物组合物在本申请中也被要求保护和描述。
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39.发明申请TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 有权三聚吡咯衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US20130296305A1
公开(公告)日：2013-11-07
申请号：US13980168
申请日：2012-01-19
申请人： Marina Caldarelli , Mauro Angiolini , Italo Beria , Maria Gabriella Brasca , Francesco Casuscelli , Roberto D'Alessio , Andrea Lombardi Borgia
发明人： Marina Caldarelli , Mauro Angiolini , Italo Beria , Maria Gabriella Brasca , Francesco Casuscelli , Roberto D'Alessio , Andrea Lombardi Borgia
IPC分类号： C07D487/04 , A61K31/55 , A61K45/06 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519 , A61K31/55 , A61K45/06 , C07C67/00 , C07D207/34 , C07D209/42 , C07D401/04 , C12N9/99
摘要： The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明涉及式（I）的三环吡咯衍生物，其调节蛋白激酶的活性，因此可用于治疗由失调的蛋白激酶活性引起的疾病。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物的方法。
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40.发明授权Substituted pyrrolo-pyrimidine derivatives, process for their preparation and their use as kinase inhibitors 有权取代的吡咯并嘧啶衍生物，其制备方法及其作为激酶抑制剂的用途公开(公告)号：US08426417B2
公开(公告)日：2013-04-23
申请号：US12679716
申请日：2008-09-25
申请人： Michele Caruso , Italo Beria , Maria Gabriella Brasca , Helena Posteri , Marina Caldarelli , Walter Ceccarelli , Barbara Valsasina
发明人： Michele Caruso , Italo Beria , Maria Gabriella Brasca , Helena Posteri , Marina Caldarelli , Walter Ceccarelli , Barbara Valsasina
IPC分类号： C07D403/04 , C07D471/04 , A61K31/506
CPC分类号： C07D403/04 , C07D401/14 , C07D405/14 , C07D471/04
摘要： Substituted pyrrolo-pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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 dysregulated protein kinase activity, like cancer.
摘要翻译： 公开了如本说明书中定义的式（I）的取代的吡咯并 - 嘧啶衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。
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