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1. 发明申请

WO2012113774A1 THIAZOLYLPHENYL-BENZENESULFONAMIDO DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的噻唑啉基苯并呋喃氨基衍生物
公开(公告)号：WO2012113774A1
公开(公告)日：2012-08-30
申请号：PCT/EP2012/052906
申请日：2012-02-21
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , PULICI, Maurizio , TRAQUANDI, Gabriella , MARCHIONNI, Chiara , SCOLARO, Alessandra , COLOMBO, Nicoletta
发明人： PULICI, Maurizio , TRAQUANDI, Gabriella , MARCHIONNI, Chiara , SCOLARO, Alessandra , COLOMBO, Nicoletta
IPC分类号： C07D417/04 , A61K31/44 , A61P35/00
CPC分类号： C07D417/04 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K45/06 , C07D417/14 , A61K2300/00
摘要： Thiazolylphenyl-benzenesulfonamido 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）的噻唑基苯基 - 苯磺酰胺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。

2. 发明申请

WO2012016993A1 DERIVATIVES OF PYRAZOLOPHENYL-BENZENESULFONAMIDE COMPOUNDS AND USE THEREOF AS ANTITUMOR AGENTS 审中-公开
标题翻译：吡唑并苯基芳香胺化合物的衍生物及其作为抗菌剂的用途
公开(公告)号：WO2012016993A1
公开(公告)日：2012-02-09
申请号：PCT/EP2011/063325
申请日：2011-08-02
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , PULICI, Maurizio , MARCHIONNI, Chiara , TRAQUANDI, Gabriella , SCOLARO, Alessandra , DONATI, Daniele
发明人： PULICI, Maurizio , MARCHIONNI, Chiara , TRAQUANDI, Gabriella , SCOLARO, Alessandra , DONATI, Daniele
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D451/04 , C07D471/04 , A61P35/00 , A61K31/4439
CPC分类号： A61K31/4439 , A61K31/437 , A61K31/4545 , A61K31/506 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D451/04 , C07D471/04
摘要： Substituted pyrazolophenyl-benzenesulfonamide compounds of formula (I) are described, wherein m, R1, R2, R3, and R4 are defined in the description, which modulate the activity of protein kinases, These compounds find utility in treating diseases caused by deregulated protein kinase activity, such as cancer and cell proliferative disorders.
摘要翻译：描述了式（I）的取代的吡唑并苯基 - 苯磺酰胺化合物，其中m，R 1，R 2，R 3和R 4在描述中定义，其调节蛋白激酶的活性。这些化合物可用于治疗由失调蛋白激酶活动，如癌症和细胞增殖性疾病。

3. 发明申请

WO2010010154A1 3,4-DIARYLPYRAZOLES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的3,4-二氨基吡唑
公开(公告)号：WO2010010154A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/059506
申请日：2009-07-23
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , PULICI, Maurizio , ZUCCOTTO, Fabio , BADARI, Alessandra , NUVOLONI, Stefano , CERVI, Giovanni , TRAQUANDI, Gabriella , BIONDARO, Sonia , TRIFIRO', Paolo , MARCHIONNI, Chiara , MODUGNO, Michele
发明人： PULICI, Maurizio , ZUCCOTTO, Fabio , BADARI, Alessandra , NUVOLONI, Stefano , CERVI, Giovanni , TRAQUANDI, Gabriella , BIONDARO, Sonia , TRIFIRO', Paolo , MARCHIONNI, Chiara , MODUGNO, Michele
IPC分类号： C07D401/04 , C07D403/04 , C07D407/14 , C07D409/14 , A61K31/4439 , A61P35/00
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/506 , A61K31/635 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D513/14
摘要： 3,4-diarylpyrazole 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3,4-二芳基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。

4. 发明申请

WO2011092088A1 SULFONAMIDO DERIVATIVES OF 3,4-DIARYLPYRAZOLES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的3,4-二氨基吡唑的磺酰胺衍生物
公开(公告)号：WO2011092088A1
公开(公告)日：2011-08-04
申请号：PCT/EP2011/050654
申请日：2011-01-19
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , PULICI, Maurizio , MARCHIONNI, Chiara , TRAQUANDI, Gabriella
发明人： PULICI, Maurizio , MARCHIONNI, Chiara , TRAQUANDI, Gabriella
IPC分类号： C07D401/04 , A61K31/4439 , A61P35/00
CPC分类号： C07D401/04 , A61K31/4439
摘要： Compounds which are sulfonamido 3,4-diarylpyrazole derivatives, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is their use as prodrugs.
摘要翻译：公开了作为磺酰胺基3,4-二芳基吡唑衍生物的化合物或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; 这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的艾滋病发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了它们作为前药的用途。

5. 发明申请

WO2010145998A1 SUBSTITUTED PYRIMIDINYLPYRROLOPYRIDINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 审中-公开
标题翻译：取代的吡咯烷基吡咯并吡啶酮衍生物，其制备方法及其作为激酶抑制剂的用途
公开(公告)号：WO2010145998A1
公开(公告)日：2010-12-23
申请号：PCT/EP2010/058223
申请日：2010-06-11
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , MARCHIONNI, Chiara , ZUCCOTTO, Fabio , BADARI, Alessandra , ANGIOLINI, Mauro , CARENZI, Davide , CALDARELLI, Marina , PULICI, Maurizio
发明人： MARCHIONNI, Chiara , ZUCCOTTO, Fabio , BADARI, Alessandra , ANGIOLINI, Mauro , CARENZI, Davide , CALDARELLI, Marina , PULICI, Maurizio
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , A61K31/506 , A61K45/06 , A61N5/00
摘要： Pyrimidinylpyrrolopyridinone 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）的嘧啶基吡咯并吡喃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。

6. 发明申请

WO2010070060A1 BICYCLIC PYRAZOLES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的双相PYRAZOLES
公开(公告)号：WO2010070060A1
公开(公告)日：2010-06-24
申请号：PCT/EP2009/067438
申请日：2009-12-17
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , PULICI, Maurizio , MARCHIONNI, Chiara , PIUTTI, Claudia , GASPARRI, Fabio
发明人： PULICI, Maurizio , MARCHIONNI, Chiara , PIUTTI, Claudia , GASPARRI, Fabio
IPC分类号： C07D513/04 , A61K31/429 , A61K31/542 , A61P35/00
CPC分类号： C07D513/04
摘要： 3,4-diaryl-bicyclicpyrazole 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：公开了本说明书中定义的式（I）的3,4-二芳基 - 双环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。

7. 发明申请

WO2010069966A1 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：WO2010069966A1
公开(公告)日：2010-06-24
申请号：PCT/EP2009/067206
申请日：2009-12-15
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , MENICHINCHERI, Maria , BERTRAND, Jay, Aaron , MARCHIONNI, Chiara , NESI, Marcella , ORSINI, Paolo , PANZERI, Achille
发明人： MENICHINCHERI, Maria , BERTRAND, Jay, Aaron , MARCHIONNI, Chiara , NESI, Marcella , ORSINI, Paolo , PANZERI, Achille
IPC分类号： C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , A61K31/416 , A61K31/454 , A61K31/496 , A61P35/00
CPC分类号： C07D405/12 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12
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。

8. 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。

9. 发明申请

WO2002100863A1 CORTICOTROPIN RELEASING FACTOR ANTAGONISTS 审中-公开
标题翻译： CORTICOTROPIN释放因子拮抗剂
公开(公告)号：WO2002100863A1
公开(公告)日：2002-12-19
申请号：PCT/GB2002/002656
申请日：2002-06-11
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
发明人： DI FABIO, Romano , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K51/0459 , C07B2200/05 , C07D239/70 , C07D239/94 , C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -COR 4 , nitro, -NR 3 R 4 cyano, or a group R 5 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 3 R 4 or cyano; R 2 corresponds to a group CHR 6 R 7 ; R 3 is hydrogen, C1-C6 alkyl; R 4 independently from R 3 , has the same meanings; R 5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R 5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R 6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R 6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R 7 independently from R 6 , has the same meanings; X is carbon or nitrogen; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供式（I）化合物，其包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素， C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自：C 1 -C 6烷氧基和羟基的基团取代; R7独立于R6，具有相同的含义; X是碳或氮; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

10. 发明申请

WO2002088095A1 FUSED PYRIMIDINES AS ANTAGONISTS OF THE CORTICOTROPIN RELEASING FACTOR (CRF) 审中-公开
标题翻译：作为抗氧化剂释放因子（CRF）的拮抗剂的FUSED PYRIMININES
公开(公告)号：WO2002088095A1
公开(公告)日：2002-11-07
申请号：PCT/GB2002/002029
申请日：2002-04-30
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , CAPELLI, Anna, Maria , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
发明人： CAPELLI, Anna, Maria , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
IPC分类号： C07D239/70
CPC分类号： C07D487/04 , A61K51/0459 , A61K51/0463 , A61K51/0465 , C07D239/70 , C07D239/94 , C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein the variables are as defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供了式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中变量如本说明书所定义，其制备方法，含有它们的药物组合物及其在治疗由促肾上腺皮质激素释放因子（CRF）。

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