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1. 发明申请

WO2012101032A1 TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 审中-公开
标题翻译： TRICYCLIC PYRROLO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：WO2012101032A1
公开(公告)日：2012-08-02
申请号：PCT/EP2012/050773
申请日：2012-01-19
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , CALDARELLI, Marina , ANGIOLINI, Mauro , BERIA, Italo , BRASCA, Maria Gabriella , CASUSCELLI, Francesco , D'ALESSIO, Roberto , LOMBARDI BORGIA, Andrea
发明人： CALDARELLI, Marina , ANGIOLINI, Mauro , BERIA, Italo , BRASCA, Maria Gabriella , CASUSCELLI, Francesco , D'ALESSIO, Roberto , LOMBARDI BORGIA, Andrea
IPC分类号： C07D487/04 , A61K31/519 , A61P19/00 , A61P37/00 , A61P35/00 , A61P17/00
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。

2. 发明申请

WO2007068637A1 SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的取代的吡咯并吡唑衍生物
公开(公告)号：WO2007068637A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/069373
申请日：2006-12-06
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , ORRENIUS, Sten Christian , PERRONE, Ettore , BERIA, Italo , FANCELLI, Daniele , GALVANI, Arturo
发明人： BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , ORRENIUS, Sten Christian , PERRONE, Ettore , BERIA, Italo , FANCELLI, Daniele , GALVANI, Arturo
IPC分类号： C07D487/04 , A61P35/00 , A61K31/41 , A61K31/496 , A61K31/5355
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 5 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：公开了如本说明书中定义的式（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5种药物组合物。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。

3. 发明申请

WO2007068619A1 SUBSTITUTED PYRAZOLO [4,3-C] PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活性的取代的吡唑并[4,3-C]吡啶衍生物
公开(公告)号：WO2007068619A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/069285
申请日：2006-12-06
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , POLUCCI, Paolo , VILLA, Manuela , NESI, Marcella , ANGIOLINI, Mauro , VARASI, Mario
发明人： BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , POLUCCI, Paolo , VILLA, Manuela , NESI, Marcella , ANGIOLINI, Mauro , VARASI, Mario
IPC分类号： C07D471/04 , A61P35/00 , A61K31/496 , A61K31/437 , A61K31/5355
CPC分类号： C07D471/04
摘要： Substituted pyrazolo[4,3-c]pyridine 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）的吡唑并[4,3-c]吡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。

4. 发明申请

WO2012152763A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的取代的吲哚酚衍生物
公开(公告)号：WO2012152763A1
公开(公告)日：2012-11-15
申请号：PCT/EP2012/058389
申请日：2012-05-07
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , LOMBARDI BORGIA, Andrea , CIOMEI, Marina , DONATI, Daniele , NESI, Marcella
发明人： LOMBARDI BORGIA, Andrea , CIOMEI, Marina , DONATI, Daniele , NESI, Marcella
IPC分类号： C07D231/56 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/416 , A61P35/00
CPC分类号： A61K31/416 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D231/56 , C07D295/155 , C07D295/185 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C12N9/12 , C12Y207/10001
摘要： The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. 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：本发明涉及调节蛋白激酶活性的取代吲唑化合物，因此可用于治疗由脱蛋白激酶活性引起的疾病，如癌症。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。

5. 发明申请

WO2009013126A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的取代的吲哚酚衍生物
公开(公告)号：WO2009013126A1
公开(公告)日：2009-01-29
申请号：PCT/EP2008/058861
申请日：2008-07-08
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , LOMBARDI BORGIA, Andrea , MENICHINCHERI, Maria , ORSINI, Paolo , PANZERI, Achille , PERRONE, Ettore , VANOTTI, Ermes , NESI, Marcella , MARCHIONNI, Chiara
发明人： LOMBARDI BORGIA, Andrea , MENICHINCHERI, Maria , ORSINI, Paolo , PANZERI, Achille , PERRONE, Ettore , VANOTTI, Ermes , NESI, Marcella , MARCHIONNI, Chiara
IPC分类号： C07D231/56 , A61K31/33 , A61P35/00
CPC分类号： C07D405/14 , A61K31/496 , A61K45/06 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12
摘要： Substituted indazole 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 deregulated protein kinase activity, like cancer.
摘要翻译：公开了本说明书中定义的式（I）的取代的吲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。

6. 发明申请

WO2008074749A9 INDAZOLE DERIVATIVES AS KINASE INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2008074749A9
公开(公告)日：2008-06-26
申请号：PCT/EP2007/063998
申请日：2007-12-14
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , NESI, Marcella , PERRONE, Ettore , BOSSI, Roberto , POLUCCI, Paolo
发明人： BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , NESI, Marcella , PERRONE, Ettore , BOSSI, Roberto , POLUCCI, Paolo
IPC分类号： A61K31/4162 , A61P35/00
摘要： Substituted indazole derivativesof 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 formula (I).

7. 发明申请

WO2007099171A2 BICYCLO-PYRAZOLES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译： BICYCLO-PYRAZOLES活性为激酶抑制剂
公开(公告)号：WO2007099171A2
公开(公告)日：2007-09-07
申请号：PCT/EP2007/052024
申请日：2007-03-02
申请人： PFIZER ITALIA S.R.L. , BANDIERA, Tiziano , BERTRAND, Jay Aaron , PEVARELLO, Paolo , PERRONE, Ettore , LOMBARDI BORGIA, Andrea , ORRENIUS, Sten Christian , ANGIOLINI, Mauro , FANCELLI, Daniele
发明人： BANDIERA, Tiziano , BERTRAND, Jay Aaron , PEVARELLO, Paolo , PERRONE, Ettore , LOMBARDI BORGIA, Andrea , ORRENIUS, Sten Christian , ANGIOLINI, Mauro , FANCELLI, Daniele
IPC分类号： C07D487/04 , A61K31/4162 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/496 , A61K31/5377
摘要： A compound having formula (I): wherein: R, A, R 1 and R 2 , are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof
摘要翻译：具有式（I）的化合物：其中：R，A，R 1和R 2如本说明书中所定义，及其药物配方和使用方法其

8. 发明申请

WO2007099166A1 PYRAZOLO-PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的吡唑并吡啶衍生物
公开(公告)号：WO2007099166A1
公开(公告)日：2007-09-07
申请号：PCT/EP2007/052011
申请日：2007-03-02
申请人： PFIZER ITALIA S.r.l. , BANDIERA, Tiziano , PERRONE, Ettore , LOMBARDI BORGIA, Andrea , VARASI, Mario
发明人： BANDIERA, Tiziano , PERRONE, Ettore , LOMBARDI BORGIA, Andrea , VARASI, Mario
IPC分类号： C07D471/04 , A61K31/437 , A61P9/00 , A61P25/00 , A61P31/00 , A61P35/00
CPC分类号： C07D471/04
摘要： A compound represented by Formula (I): wherein R and R 1 are as defined in the specification, pharmaceutical formulas thereof, and methods of use thereof.
摘要翻译：由式（I）表示的化合物：其中R和R 1如说明书中所定义，其药物化学式及其使用方法。

9. 发明申请

WO2008145398A1 4-ARYLPYRROLE SUBSTITUTED 2-INDOLINE DERIVATIVES ACTIVE AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂活化的4-ARYLPYRROLE取代的2-吲哚衍生物
公开(公告)号：WO2008145398A1
公开(公告)日：2008-12-04
申请号：PCT/EP2008/004342
申请日：2008-05-31
申请人： PFIZER ITALIA S.R.L. , BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , PAOLUCCI, Paolo , ORRENIUS, Christian , GALVANI, Arturo
发明人： BANDIERA, Tiziano , LOMBARDI BORGIA, Andrea , PAOLUCCI, Paolo , ORRENIUS, Christian , GALVANI, Arturo
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , A61K31/404 , A61P35/00
CPC分类号： C07D403/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The present invention relates to certain 4-arylpyrrole substituted 2-indolinone compounds of Formula (I), which modulate the activity of protein kinases (PKs). The compounds of this invention are therefore useful in treating disorders related to dysregulated PK activity The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及调节蛋白激酶（PK）活性的式（I）的某些4-芳基吡咯取代的2-二氢吲哚酮化合物。因此，本发明的化合物可用于治疗与失调的PK活性相关的疾病。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，以及使用包含这些化合物的药物组合物治疗疾病的方法。

10. 发明申请

WO2015110467A1 PROCESS FOR THE PREPARATION OF SUBSTITUTED N-(5-BENZENESULFONYL-1H-INDAZOL-3-YL)-BENZAMIDES 审中-公开
标题翻译：制备取代的N-（5-苯并呋喃-1H-吲哚-3-基） - 苯甲酸的方法
公开(公告)号：WO2015110467A1
公开(公告)日：2015-07-30
申请号：PCT/EP2015/051133
申请日：2015-01-21
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： ARCARI, Alessandro , D'ARASMO, Germano , LOMBARDI BORGIA, Andrea
IPC分类号： C07D405/14 , C07D231/56 , C07D405/12
CPC分类号： C07D231/56 , C07D405/12 , C07D405/14
摘要： The present invention relates to a process for the preparation of substituted N-(5-benzenesulfonyl-1 H-indazol-3-yl)-benzamides and to the useful intermediate compounds of such process. Such derivatives are described and claimed in WO2008/074749, which also discloses processes for their preparation. The process of the present invention allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis starts from 5-iodo-1 H-indazol-3-ylamine and comprises, as the key steps, the coupling of an activated benzoic acid with a 5-phenylsulfanyl-1 H-indazol-3-ylamine scaffold and the subsequent oxidation of the sulfur atom, followed by further functional group transformations, which furnish the desired products. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, IGF-1R or ALK inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.
摘要翻译：本发明涉及制备取代的N-（5-苯磺酰基-1H-吲唑-3-基） - 苯甲酰胺的方法和该方法的有用的中间体化合物。在WO2008 / 074749中描述和要求保护这些衍生物，其也公开了它们的制备方法。本发明的方法允许以高产率和纯度和有限数量的步骤获得所需的产物。合成从5-碘-1H-吲唑-3-基胺开始，并且作为关键步骤包括活化的苯甲酸与5-苯基硫烷基-1H-吲唑-3-基胺支架的偶联和随后的氧化的硫原子，随后进一步的官能团转化，其提供所需的产物。根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予IGF-1R或ALK抑制活性。因此，这些化合物可用于治疗多种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

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