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11. 发明申请

US20070185143A1 Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors 有权
标题翻译：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：US20070185143A1
公开(公告)日：2007-08-09
申请号：US10557565
申请日：2004-04-27
申请人： Gabriella Traquandi , Maria Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
发明人： Gabriella Traquandi , Maria Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： A61K31/505
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 maybe 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（Ia）或（Ib）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; 本发明的化合物可用于治疗与抑制性蛋白激酶活性相关的疾病如癌症“。

12. 发明授权

US08981089B2 Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors 有权
标题翻译：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：US08981089B2
公开(公告)日：2015-03-17
申请号：US13972659
申请日：2013-08-21
申请人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： C07D487/04 , C07D403/14 , C07D413/14 , C07D487/14 , C07D231/56 , C07D239/72
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.
摘要翻译：公开了说明书中定义的式（Ia）或（Ib）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。

13. 发明授权

US08541429B2 Pyrazolo quinazoline derivatives, process for their preparation and their use as kinase inhibitors 有权
标题翻译：吡唑喹啉衍生物，其制备方法及其作为激酶抑制剂的用途
公开(公告)号：US08541429B2
公开(公告)日：2013-09-24
申请号：US12262933
申请日：2008-10-31
申请人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： A01N43/54 , A61K31/505
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.
摘要翻译：公开了说明书中定义的式（Ia）或（Ib）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。

14. 发明申请

US20090124605A1 Pyrazolo-Quinazoline Derivatives, Process for Their Preparation and Their Use as Kinase Inhibitors 有权
标题翻译：吡唑并喹唑啉衍生物，其制备方法及其用作激酶抑制剂
公开(公告)号：US20090124605A1
公开(公告)日：2009-05-14
申请号：US12262933
申请日：2008-10-31
申请人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： A61K31/551 , A61K31/519 , C12N9/99 , C07D487/04 , A61K31/496 , A61P25/28 , A61P17/06 , A61P37/06 , A61P37/00 , A61P35/00 , C07D401/14 , C07D413/14 , A61K31/5377
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.
摘要翻译：公开了说明书中定义的式（Ia）或（Ib）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。

15. 发明申请

US20130338148A1 PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 审中-公开
公开(公告)号：US20130338148A1
公开(公告)日：2013-12-19
申请号：US13972659
申请日：2013-08-21
申请人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： A61K31/551 , C07D401/10 , C07D487/14 , A61K31/519 , A61K31/5377 , C07D231/56 , C07D487/04
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.

16. 发明授权

US07482354B2 Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors 有权
标题翻译：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：US07482354B2
公开(公告)日：2009-01-27
申请号：US10557565
申请日：2004-04-27
申请人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： A61K31/505 , A01N43/54 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
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.
摘要翻译：公开了说明书中定义的式（Ia）或（Ib）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; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

17. 发明申请

US20090136513A1 BICYCLO-PYRAZOLES ACTIVE AS KINASE INHIBITORS 有权
标题翻译： BICYCLO-PYRAZOLES活性为激酶抑制剂
公开(公告)号：US20090136513A1
公开(公告)日：2009-05-28
申请号：US12281602
申请日：2007-03-02
申请人： Tiziano Bandiera , Jay Aaron Bertrand , Paolo Pevarello , Ettore Perrone , Andrea Lombardi Borgia , Sten Christian Orrenius , Mauro Angiolini , Daniele Fancelli
发明人： Tiziano Bandiera , Jay Aaron Bertrand , Paolo Pevarello , Ettore Perrone , Andrea Lombardi Borgia , Sten Christian Orrenius , Mauro Angiolini , Daniele Fancelli
IPC分类号： A61K31/4162 , C07D487/04 , A61K31/5377 , A61K39/395 , A61P35/00 , A61K31/496
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/496 , A61K31/5377
摘要： A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.
摘要翻译：具有式（I）的化合物：其中：R，A，R 1和R 2如说明书中所定义，及其药物配方及其使用方法作为激酶抑制剂。

18. 发明授权

US06414013B1 Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention 失效
标题翻译：噻吩化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US06414013B1
公开(公告)日：2002-07-02
申请号：US09596550
申请日：2000-06-19
申请人： Daniele Fancelli , Paolo Pevarello , Mario Varasi
发明人： Daniele Fancelli , Paolo Pevarello , Mario Varasi
IPC分类号： A61K3138
CPC分类号： C07D409/12 , C07D333/38 , C07D333/68 , C07D413/12 , C07D473/00 , C07D495/04
摘要： Compounds which are 3-aminocarbonyl-2-carboxamido-thiophene derivatives of formula (I): wherein R1 and R2 are, independently from each other, hydrogen, halogen or an optionally substituted group selected from aryl, straight or branched C1-C6 alkyl or aryl C1-C6 alkyl; or, taken together with the thiophene bond to which they are linked, R1 and R2 form a —(CH2)m—(NR4)n—(CH2)p— group wherein m and p are, each independently, an integer form 1 to 3, n is 0 or 1 and m+n+p is an integer from 3 to 5; and R4 is hydrogen or an optionally substituted straight or branched C1-C6 alkyl group; R3 is a group, optionally further substituted, selected from: i) straight or branched C1-C8 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C2-C6 alkylcarbonyl; ii) aryl; iii) 3 to 7 membered carbocycle; iv) 5 to 7 membered heterocycle with from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur; or a pharmaceutically acceptable salt thereof; are useful in the treatment of diseases associated with an altered protein kinase activity such as cancer, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.
摘要翻译：作为式（I）的3-氨基羰基-2-甲酰氨基 - 噻吩衍生物的化合物：其中R 1和R 2彼此独立地为氢，卤素或任选取代的基团，其选自芳基，直链或支链C 1 -C 6烷基或芳基C1-C6烷基; 或者与它们所连接的噻吩键一起，R 1和R 2形成 - （CH 2）m - （NR 4）n - （CH 2）p - 基团，其中m和p各自独立地是1〜 3，n为0或1，m + n + p为3〜5的整数，且R 4为氢或任选取代的直链或支链C 1 -C 6烷基; R 3是任选进一步取代的，选自：i）直链或支链C 1 -C 8烷基，C 2 -C 6烯基，C 2 -C 6炔基或C 2 -C 6烷基羰基; ii）芳基; iii）3至7元碳环; iv）具有1至3个选自氮，氧和硫的杂原子的5至7元杂环; 或其药学上可接受的盐; 可用于治疗与改变的蛋白激酶活性如癌症，阿尔茨海默病，病毒感染，自身免疫疾病和神经变性疾病相关的疾病。

19. 发明授权

US09012487B2 Bicyclo-pyrazoles active as kinase inhibitors 有权
标题翻译：作为激酶抑制剂活化的双环吡唑
公开(公告)号：US09012487B2
公开(公告)日：2015-04-21
申请号：US12281602
申请日：2007-03-02
申请人： Tiziano Bandiera , Jay Aaron Bertrand , Paolo Pevarello , Ettore Perrone , Andrea Lombardi Borgia , Sten Christian Orrenius , Mauro Angiolini , Daniele Fancelli
发明人： Tiziano Bandiera , Jay Aaron Bertrand , Paolo Pevarello , Ettore Perrone , Andrea Lombardi Borgia , Sten Christian Orrenius , Mauro Angiolini , Daniele Fancelli
IPC分类号： C07D487/04 , A61K31/496 , A61K31/5377 , A61K31/4162
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/496 , A61K31/5377
摘要： A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.
摘要翻译：具有式（I）的化合物：其中：R，A，R 1和R 2如说明书中所定义，及其药物配方及其使用方法作为激酶抑制剂。

20. 发明申请

US20060135508A1 Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开
标题翻译：作为激酶抑制剂活性的双环吡唑，其制备方法和包含它们的药物组合物
公开(公告)号：US20060135508A1
公开(公告)日：2006-06-22
申请号：US10522253
申请日：2003-07-16
申请人： Manuela Villa , Francesca Abrate , Daniele Fancelli , Mario Varasi , Anna Vulpetti
发明人： Manuela Villa , Francesca Abrate , Daniele Fancelli , Mario Varasi , Anna Vulpetti
IPC分类号： A61K31/55 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： C07D487/04 , A61K31/415 , A61K45/06 , C07D471/04 , A61K2300/00
摘要： The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a pyrrolo-pyrazole or pyrazolo-azepine. The invention also provides specific pyrrolo-pyrazoles and pyrazolo-azepines, useful intermediates, a library comprising at least two of them, a process for their preparation and the pharmaceutical compositions containing them, which are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.
摘要翻译：本发明提供了治疗由变化的蛋白激酶活性引起和/或与其相关的疾病的方法，其包括向有需要的哺乳动物施用有效量的吡咯并吡唑或吡唑并氮。本发明还提供特定的吡咯并吡唑和吡唑并氮杂，有用的中间体，包含其中至少两个的文库，其制备方法和含有它们的药物组合物，其可用于治疗由和/或与改变的蛋白激酶活性如癌症，细胞增殖性病症，病毒感染，自身免疫疾病和神经变性疾病有关。

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