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11. 发明申请

WO2003055861A1 BENZOCYCLODECANE DERIVATIVES WITH ANTITUMOR ACTIVITY 审中-公开
标题翻译：具有抗肿瘤活性的苯并四氢吡喃衍生物
公开(公告)号：WO2003055861A1
公开(公告)日：2003-07-10
申请号：PCT/EP2002/014514
申请日：2002-12-18
申请人： PHARMACIA ITALIA SPA , ANGIOLINI, Mauro , DUCKI, Sylvie , MENICHINCHERI, Maria , MONGELLI, Nicola , VANOTTI, Ermes , CIOMEI, Marina
发明人： ANGIOLINI, Mauro , DUCKI, Sylvie , MENICHINCHERI, Maria , MONGELLI, Nicola , VANOTTI, Ermes , CIOMEI, Marina
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , C07C45/673 , C07C49/747 , C07C67/08 , C07C67/29 , C07C67/293 , C07C69/007 , C07C69/013 , C07C69/618 , C07C2602/12 , C07D213/56 , C07D263/32 , C07D277/30 , C07H15/203 , C07C69/16
摘要： A compound which is a benzocyclodecane of the formula I wherein: ----- at positions 8-9 and 11-12 independently represents a single or double bond, -R1 is =O, or -OR7, R7 is H, C1-C7 alkanoyl, benzoyl, C1-C10 alkyl, C2-C10 alkenyl or COCH=CHR8, R8 is aryl or heterocyclyl;-R2 and -R3 are H, =O or -OR9, R9 is H, C1-C7 alkanoyl or benzoyl; when at position 11-12 there is a single bond, then -R4 represents=O, =CH2, =CHCOOR10, R10 is C1-C10 alkyl or aryl; =CH(OCH3), -OR9; -CH2OR11, R11 is H or a sugar residue, -COR12 , R12 is H, -OH or -OR10; or when at position 11-12 there is a double bond, then -R4 is -CH2OR11 or -COR12; - R5 and -R6 are H or, when at position 8-9 there is a single bond, taken together form a cyclopropane ring; R13 is H or 1-3 substituents selected from C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy, aryloxy, cyano, nitro, amino, C1-C10 alkylamino, arylamino, C1-C7 alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C1-C6 alkylcarbonyl, C1-C6 alkylaminosulfonyl and arylaminosulfonyl group; with the provisos that if R1 and R4 =O, then one of R2, R3, R5, R6 and R13 is not H atom; or a pharmaceutically acceptable salt thereof. These benzocyclodecane derivatives are endowed with antitumor activity; a process and new intermediates for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.
摘要翻译：作为式I的苯并环十一烷的化合物，其中： - 在8-9和11-12位，独立地表示单键或双键，-R1为=或-OR7，R7为H，C1- C7烷酰基，苯甲酰基，C1-C10烷基，C2-C10烯基或COCH = CHR8，R8是芳基或杂环基; -R2和-R3是H，= O或-OR9，R9是H，C1-C7烷酰基或苯甲酰基; 当在11-12位存在单键时，则-R 4表示= O，= CH 2，= CHCOOR 10，R 10是C 1 -C 10烷基或芳基; = CH（OCH 3），-OR 9; -CH 2 OR 11，R 11为H或糖残基，-COR 12，R 12为H，-OH或-OR 10; 或者当在11-12位存在双键时，则-R 4是-CH 2 OR 11或-COR 12; -R 5和-R 6是H或当在8-9位存在单键时，一起形成环丙烷环; R 13是H或1-3个选自C 1 -C 6烷基，C 2 -C 6烯基，苯基，苯基C 1 -C 6烷基，卤素，羟基，C 1 -C 6烷氧基，芳氧基，氰基，硝基，氨基，C 1 -C 10烷基氨基，芳基氨基，C 1 -C 7烷酰基氨基，芳酰氨基，羟基羰基，氨基羰基，C 1 -C 6烷基羰基，C 1 -C 6烷基氨基磺酰基和芳基氨基磺酰基; 条件是如果R1和R4 = O，则R2，R3，R5，R6和R13之一不是H原子; 或其药学上可接受的盐。这些苯并环十一烷衍生物具有抗肿瘤活性; 还提供了其制备方法和新的中间体，含有它们的药物组合物及其在预防，控制和治疗癌症中的用途。

12. 发明申请

WO2008104475A1 ISOQUINOLINOPYRROLOPYRIDINONES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的活性氧化丙烯吡咯烷酮
公开(公告)号：WO2008104475A1
公开(公告)日：2008-09-04
申请号：PCT/EP2008/051948
申请日：2008-02-18
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , VANOTTI, Ermes , MENICHINCHERI, Maria , SCOLARO, Alessandra
发明人： VANOTTI, Ermes , MENICHINCHERI, Maria , SCOLARO, Alessandra
IPC分类号： A61K31/437
CPC分类号： C07D471/04 , C07D471/14
摘要： Heteroarylpyridinone derivatives represented by formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions comprising them and their use as therapeutic agents in the treatment of cancer and cell proliferation disorders.
摘要翻译：由式（I）表示的杂芳基吡啶酮衍生物，其中R 1，R 2，R 3，R 4，R 4，并且X如说明书，其组成，及其使用方法中所定义。特别地，描述了异喹啉基吡咯并吡啶酮，包含它们的药物组合物及其在治疗癌症和细胞增殖障碍中作为治疗剂的用途。

13. 发明申请

WO2005013986A1 PYRIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的吡啶衍生物衍生物
公开(公告)号：WO2005013986A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008811
申请日：2004-08-06
申请人： PHARMACIA ITALIA S.P.A. , VANOTTI, Ermes , D'ALESSIO, Roberto , TIBOLLA, Marcellino , VARASI, Mario , MONTAGNOLI, Alessia , SANTOCANALE, Corrado , MARTINA, Katia , MENICHINCHERI, Maria
发明人： VANOTTI, Ermes , D'ALESSIO, Roberto , TIBOLLA, Marcellino , VARASI, Mario , MONTAGNOLI, Alessia , SANTOCANALE, Corrado , MARTINA, Katia , MENICHINCHERI, Maria
IPC分类号： A61K31/444
CPC分类号： C07D471/04 , A61K31/444 , A61K31/4745 , A61K45/06 , A61K2300/00
摘要： Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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：公开了式（I）的吡啶基吡咯衍生物及其药学上可接受的盐，以及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

WO2004071507A1 TETRACYCLIC PYRAZOLE DERIVATIVES AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：作为激酶抑制剂的四环吡唑衍生物，其制备和包含它们的药物组合物的方法
公开(公告)号：WO2004071507A1
公开(公告)日：2004-08-26
申请号：PCT/EP2004/050071
申请日：2004-02-03
申请人： PHARMACIA ITALIA S.P.A. , VANOTTI, Ermes , CERVI, Giovanni , PULICI, Maurizio , MENICHINCHERI, Maria , VARASI, Mario , VIANELLO, Paola
发明人： VANOTTI, Ermes , CERVI, Giovanni , PULICI, Maurizio , MENICHINCHERI, Maria , VARASI, Mario , VIANELLO, Paola
IPC分类号： A61K31/4162
CPC分类号： C07D487/04 , A61K31/4162 , A61K45/06 , 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 tetracyclic pyrazole. The invention also provides specific tetracyclic pyrazole derivatives, 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，该方法包括向有需要的哺乳动物施用有效量的四环吡唑。本发明还提供具体的四环吡唑衍生物，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，其可用于治疗由改变的和/或与之相关的疾病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。

15. 发明申请

WO2008065054A1 TRICYCLIC INDOLES AND (4,5-DIHYDRO) INDOLES 审中-公开
标题翻译：三聚吲哚和（4,5-二羟基）吲哚
公开(公告)号：WO2008065054A1
公开(公告)日：2008-06-05
申请号：PCT/EP2007/062762
申请日：2007-11-23
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , VANOTTI, Ermes , CALDARELLI, Marina , CASUSCELLI, Francesco , FORTE, Barbara , MENICHINCHERI, Maria , SCOLARO, Alessandra , TRAQUANDI, Gabriella , VIANELLO, Paola
发明人： VANOTTI, Ermes , CALDARELLI, Marina , CASUSCELLI, Francesco , FORTE, Barbara , MENICHINCHERI, Maria , SCOLARO, Alessandra , TRAQUANDI, Gabriella , VIANELLO, Paola
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4162 , A61K31/4745 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, ----- means either simple or double carbon-carbon bond and R 1 , R 2 and R 3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.
摘要翻译：本发明提供式（I）的三环吲哚和（4,5-二氢）吲哚或其药学上可接受的盐：其中环A表示稠合吡唑，吡啶或嘧啶，-----表示简单或双碳 - 碳键和R 1，R 2和R 3是如说明书中所定义的。本发明的另外的目的是制备式（I）化合物，包含它们的药物组合物和治疗细胞增殖性疾病的方法的方法。事实上，式（I）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，特别是Cdc7和AKT激酶活性，如癌症。

16. 发明申请

WO2004024711A1 SUBSTITUTED PYRIDINE DERIVATIVES AS ANTITUMOR AGENT 审中-公开
标题翻译：取代的吡啶衍生物作为抗菌剂
公开(公告)号：WO2004024711A1
公开(公告)日：2004-03-25
申请号：PCT/EP2003/009572
申请日：2003-08-26
申请人： PHARMACIA ITALIA S.P.A. , ANGIOLINI, Mauro , MENICHINCHERI, Maria , FUSAR BASSINI, Domenico , GUDE, Markus
发明人： ANGIOLINI, Mauro , MENICHINCHERI, Maria , FUSAR BASSINI, Domenico , GUDE, Markus
IPC分类号： C07D401/04
CPC分类号： C07D213/73 , C07D213/74
摘要： The present invention relates to novel substituted pyridine derivatives active as Telomerase inhibitors, to the use of them as therapeutic agents, in particular as antitumoral agents, to a process for their preparation and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及作为端粒酶抑制剂活性的新型取代的吡啶衍生物，其用作治疗剂，特别是作为抗肿瘤剂的制剂方法和包含它们的药物组合物。

17. 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。

18. 发明申请

WO2003024529A1 SIMPLIFIED SARCODICTYN DERIVATIVES AS ANTI-TUMOR AGENTS 审中-公开
标题翻译：简单的SARCODICTYN衍生物作为抗肿瘤剂
公开(公告)号：WO2003024529A1
公开(公告)日：2003-03-27
申请号：PCT/EP2002/010038
申请日：2002-09-06
申请人： PHARMACIA ITALIA SPA , UNIVERSITA DEGLI STUDI DI MILANO , MONGELLI, Nicola , MENICHINCHERI, Maria , CIOMEI, Marina , GENNARI, Cesare , TELSER, Joachim , BEUMER, Raphael
发明人： MONGELLI, Nicola , MENICHINCHERI, Maria , CIOMEI, Marina , GENNARI, Cesare , TELSER, Joachim , BEUMER, Raphael
IPC分类号： A61P35/00
CPC分类号： C07D263/34 , C07C69/013 , C07C69/618 , C07C2602/32 , C07D233/90 , C07D277/30
摘要： There are provided sarcodictyin derivatives or pharmaceutically acceptable salts thereof, which are characterized by a simplified chemical structure and have anti-tumor activity. A process for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.
摘要翻译：提供了莽草苷衍生物或其药学上可接受的盐，其特征在于化学结构简单并具有抗肿瘤活性。还提供了其制备方法，含有它们的药物组合物及其在预防，控制和治疗癌症中的用途。

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