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公开(公告)号：US20070142414A1
公开(公告)日：2007-06-21
申请号：US11303114
申请日：2005-12-16
IPC分类号： A61K31/506 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： Compounds represented by formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译： 由式（I）表示的化合物，其中A，R 1，R 2，R 3，R 4， R 5和R 6如本说明书中所定义，其药物组合物及其使用方法。
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12.发明授权Azaindolylidene derivatives as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 失效作为激酶抑制剂的亚芴基亚芴基衍生物，其制备方法和包含它们的药物组合物公开(公告)号：US07371862B2
公开(公告)日：2008-05-13
申请号：US11271191
申请日：2005-11-11
申请人： Ermes Vanotti , Francesco Angelucci , Alberto Bargiotti , Maria Gabriella Brasca , Antonella Ermoli , Maria Menichincheri
发明人： Ermes Vanotti , Francesco Angelucci , Alberto Bargiotti , Maria Gabriella Brasca , Antonella Ermoli , Maria Menichincheri
IPC分类号： C07D471/02 , C07D233/00
CPC分类号： C07D471/04
摘要： The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell proliferation or to disregulated protein kinase.
摘要翻译： 本发明涉及下式的化合物或其药学上可接受的盐，前体药物，溶剂合物或旋光异构体，含有该化合物的药物组合物及其用于治疗与细胞增殖失调或失调的蛋白激酶相关的疾病的用途。
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13.发明申请Azaindolylidene derivatives as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 失效作为激酶抑制剂的亚芴基亚芴基衍生物，其制备方法和包含它们的药物组合物公开(公告)号：US20070112020A1
公开(公告)日：2007-05-17
申请号：US11271191
申请日：2005-11-11
申请人： Ermes Vanotti , Francesco Angelucci , Alberto Bargiotti , Maria Brasca , Antonella Ermoli , Maria Menichincheri
发明人： Ermes Vanotti , Francesco Angelucci , Alberto Bargiotti , Maria Brasca , Antonella Ermoli , Maria Menichincheri
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell proliferation or to disregulated protein kinase.
摘要翻译： 本发明涉及下式的化合物或其药学上可接受的盐，前体药物，溶剂合物或旋光异构体，含有该化合物的药物组合物及其用于治疗与细胞增殖失调或失调的蛋白激酶相关的疾病的用途。
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公开(公告)号：US20050288238A1
公开(公告)日：2005-12-29
申请号：US10878212
申请日：2004-06-28
申请人： Mauro Angiolini , Sylvie Ducki , Maria Menichincheri , Nicola Mongelli , Ermes Vanotti , Marina Ciomei
发明人： Mauro Angiolini , Sylvie Ducki , Maria Menichincheri , Nicola Mongelli , Ermes Vanotti , Marina Ciomei
IPC分类号： A61K31/225 , A61K31/704 , C07C67/02 , C07C67/293 , C07C69/007 , C07C69/013 , C07C69/618 , C07D213/55 , C07D233/54 , C07D263/32 , C07D277/30 , C07H15/24
CPC分类号： C07D233/64 , C07C67/08 , C07C67/29 , C07C67/293 , C07C69/007 , C07C69/013 , C07C69/618 , C07C2602/12 , C07D213/55 , C07D263/32 , C07D277/30 , 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.
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公开(公告)号：US08673893B2
公开(公告)日：2014-03-18
申请号：US13611679
申请日：2012-09-12
申请人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： A61K31/415 , A61K31/535 , A61K31/445
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。
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公开(公告)号：US20100292207A1
公开(公告)日：2010-11-18
申请号：US12668745
申请日：2008-07-08
申请人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： A61K31/416 , C07D403/12 , C07D231/56 , C07D405/14 , C07D405/12 , C07D413/14 , C07D403/14 , C07D413/12 , A61K31/497 , A61K31/5513 , A61K31/454 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P27/02 , A61P17/06 , A61P35/04 , A61P9/00 , A61P11/00
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。
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17.发明申请Tetracyclic pyrazole derivatives as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开作为激酶抑制剂的四环吡唑衍生物，其制备方法和包含它们的药物组合物公开(公告)号：US20060264493A1
公开(公告)日：2006-11-23
申请号：US10545768
申请日：2004-02-03
申请人： Ermes Vanotti , Giovanni Cervi , Maurizio Pulici , Maria Menichincheri , Mario Varasi , Paola Vianello
发明人： Ermes Vanotti , Giovanni Cervi , Maurizio Pulici , Maria Menichincheri , Mario Varasi , Paola Vianello
IPC分类号： A61K31/4162 , C07D487/02
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。
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公开(公告)号：US5912263A
公开(公告)日：1999-06-15
申请号：US964889
申请日：1997-11-05
申请人： Maria Menichincheri , Walter Ceccarelli , Marina Ciomei , Domenico Fusar Bassini , Nicola Mongelli , Ermes Vanotti
发明人： Maria Menichincheri , Walter Ceccarelli , Marina Ciomei , Domenico Fusar Bassini , Nicola Mongelli , Ermes Vanotti
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14
CPC分类号： C07D305/14
摘要： Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.
摘要翻译： 在式（I）的紫杉烷衍生物骨架（紫杉醇编号）的13位修饰的紫杉烷衍生物，其中R，Ra，Rb，Rc，R 1，R 2，R 3是合适的有机残基可以是抗肿瘤剂。
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公开(公告)号：US20100056556A1
公开(公告)日：2010-03-04
申请号：US12528656
申请日：2008-02-18
IPC分类号： A61K31/4375 , C07D471/12 , C07D471/02 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , C07D471/14
摘要： Heteroarylpyridinone derivatives represented by formula (I) wherein R1, R2, R3, R4, R5, 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 5和X如本说明书中所定义，其组成及其使用方法。 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。
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公开(公告)号：US08299057B2
公开(公告)日：2012-10-30
申请号：US12668745
申请日：2008-07-08
申请人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： A61K31/035 , A61K31/55 , A61K31/535 , A61K31/497 , A61K31/445 , A61K31/415 , C07D413/10 , C07D231/56 , C07D243/08
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。
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