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1. 发明申请

WO2003008365A3 PHENYLACETAMIDO-THIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 审中-公开
公开(公告)号：WO2003008365A3
公开(公告)日：2003-01-30
申请号：PCT/EP2002/007289
申请日：2002-07-02
申请人： PHARMACIA ITALIA S.P.A. , PEVARELLO, Paolo , AMICI, Raffaella , VILLA, Manuela , SALOM, Barbara , VULPETTI, Anna , VARASI, Mario , BRASCA, Maria, Gabriella , TRAQUANDI, Gabriella , NESI, Marcella
发明人： PEVARELLO, Paolo , AMICI, Raffaella , VILLA, Manuela , SALOM, Barbara , VULPETTI, Anna , VARASI, Mario , BRASCA, Maria, Gabriella , TRAQUANDI, Gabriella , NESI, Marcella
IPC分类号： C07D417/12
摘要： Compounds represented by formula (I), as defined in the description, wherein R is a hydrogen atom or a methyl group and R1 is a group as defined in the specification, or a pharmaceutically acceptable salt thereof, are disclosed; the said compounds are useful in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.

2. 发明申请

WO2003008365A2 PHENYLACETAMIDO-THIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 审中-公开
标题翻译：苯乙烯胺 - 噻唑衍生物，其制备方法及其作为抗菌剂的用途
公开(公告)号：WO2003008365A2
公开(公告)日：2003-01-30
申请号：PCT/EP2002/007289
申请日：2002-07-02
申请人： PHARMACIA ITALIA S.P.A. , PEVARELLO, Paolo , AMICI, Raffaella , VILLA, Manuela , SALOM, Barbara , VULPETTI, Anna , VARASI, Mario , BRASCA, Maria, Gabriella , TRAQUANDI, Gabriella , NESI, Marcella
发明人： PEVARELLO, Paolo , AMICI, Raffaella , VILLA, Manuela , SALOM, Barbara , VULPETTI, Anna , VARASI, Mario , BRASCA, Maria, Gabriella , TRAQUANDI, Gabriella , NESI, Marcella
IPC分类号： C07C49/00
CPC分类号： C07D417/12 , C07D277/46
摘要： Compounds represented by formula (I), as defined in the description, wherein R is a hydrogen atom or a methyl group and R1 is a group as defined in the specification, or a pharmaceutically acceptable salt thereof, are disclosed; the said compounds are useful in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
摘要翻译：其中R为氢原子或甲基，R1为本说明书中定义的基团，或其药学上可接受的盐，由式（I）表示的化合物或其药学上可接受的盐; 所述化合物可用于治疗细胞增殖性疾病，例如，与改变的细胞周期依赖性激酶活性相关的癌症。

3. 发明申请

WO2004014374A1 BICYCLO-PYRAZOLES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：作为激酶抑制剂的双羟基磷酸酯，其制备和包含它们的药物组合物的方法
公开(公告)号：WO2004014374A1
公开(公告)日：2004-02-19
申请号：PCT/EP2003/007000
申请日：2003-07-01
申请人： PHARMACIA ITALIA S.P.A. , VILLA, Manuela , ABRATE, Francesca , FANCELLI, Daniele , VARASI, Mario , VULPETTI, Anna
发明人： VILLA, Manuela , ABRATE, Francesca , FANCELLI, Daniele , VARASI, Mario , VULPETTI, Anna
IPC分类号： A61K31/437
CPC分类号： C07D471/04
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 pyrazole-tetrahydro pyridine derivative. The invention also provides specific pyrazole-tetrahydro pyridines, 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唑 - 四氢吡啶衍生物。本发明还提供特异性的吡唑 - 四氢吡啶，其中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蛋白激酶引起的和/或与其相关的疾病活动如癌症，细胞增殖性疾病，病毒感染，自身免疫性疾病和神经变性疾病。

4. 发明申请

WO2010049768A1 ACRYLAMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION 审中-公开
标题翻译：丙烯酰胺衍生物作为微生物渗透性转换的抑制剂有用
公开(公告)号：WO2010049768A1
公开(公告)日：2010-05-06
申请号：PCT/IB2009/006939
申请日：2009-09-23
申请人： CONGENIA SRL , FANCELLI, Daniele , VARASI, Mario , PLYTE, Simon , BALLARINI, Marco , CAPPA, Anna , CARENZI, Giacomo , MINUCCI, Saverio , PAIN, Gilles , VILLA, Manuela
发明人： FANCELLI, Daniele , VARASI, Mario , PLYTE, Simon , BALLARINI, Marco , CAPPA, Anna , CARENZI, Giacomo , MINUCCI, Saverio , PAIN, Gilles , VILLA, Manuela
IPC分类号： C07C235/38 , C07D213/30 , C07D213/75 , C07D295/135 , C07C235/36 , C07C323/41 , C07D209/08 , C07D211/22 , C07D211/46 , C07D213/32 , C07D213/38 , C07D213/68 , C07D231/12 , C07D231/56 , C07D233/60
CPC分类号： C07C235/38 , C07C235/36 , C07C323/41 , C07C2601/04 , C07C2602/08 , C07D209/08 , C07D211/22 , C07D213/30 , C07D213/36 , C07D213/68 , C07D213/75 , C07D231/12 , C07D231/56 , C07D233/64 , C07D235/06 , C07D235/30 , C07D239/47 , C07D249/18 , C07D257/04 , C07D263/32 , C07D263/56 , C07D295/096 , C07D295/135 , C07D307/42
摘要： Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R', R", W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
摘要翻译：可用作治疗剂的丙烯酰胺衍生物，特别是用于预防和/或治疗与线粒体通透性转换孔（MPTP）的活性相关的疾病和病症，例如以缺血/再灌注，氧化性或退行性组织损伤为特征的疾病，是在此描述。这些化合物属于结构式（I），其中R，R'，R“，W和a如说明书中所定义。本发明还涉及这些化合物的制备，以及包含它们的药物组合物。

5. 发明申请

WO2004013144A1 BICYCLO-PYRAZOLES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：作为激酶抑制剂的双羟基磷酸酯，其制备和包含它们的药物组合物的方法
公开(公告)号：WO2004013144A1
公开(公告)日：2004-02-12
申请号：PCT/EP2003/007851
申请日：2003-07-16
申请人： PHARMACIA ITALIA SPA , VILLA, Manuela , ABRATE, Francesca , FANCELLI, Daniele , VARASI, Mario , VULPETTI, Anna
发明人： VILLA, Manuela , ABRATE, Francesca , FANCELLI, Daniele , VARASI, Mario , VULPETTI, Anna
IPC分类号： C07D487/04
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。

6. 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。

7. 发明申请

WO2004080457A1 BICYCLO-PYRAZOLE DERIVATIVES 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甲基吡唑衍生物，其制备方法和包含它们的药物组合物
公开(公告)号：WO2004080457A1
公开(公告)日：2004-09-23
申请号：PCT/EP2004/050237
申请日：2004-03-02
申请人： PHARMACIA ITALIA S.P.A. , ABRATE, Francesca , FANCELLI, Daniele , VARASI, Mario , VILLA, Manuela
发明人： ABRATE, Francesca , FANCELLI, Daniele , VARASI, Mario , VILLA, Manuela
IPC分类号： A61K31/4162
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4745 , A61K31/55
摘要： Compounds which are pyrrolo-pyrazole derivatives and pharmaceutically acceptable salts thereof, together with the process for their preparation and pharmaceutical compositions thereof are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.
摘要翻译：公开了吡咯并吡唑衍生物及其药学上可接受的盐的化合物及其制备方法及其药物组合物; 这些化合物或组合物可用于治疗由改变的蛋白激酶活性如癌症，细胞增殖性疾病，阿尔茨海默氏病，病毒感染，自身免疫疾病和神经变性疾病引起的和/或与其相关的疾病。

8. 发明申请

WO1997013769A1 DISUBSTITUTED PIPERIDINE DERIVATIVES 审中-公开
标题翻译：分离的哌啶衍生物
公开(公告)号：WO1997013769A1
公开(公告)日：1997-04-17
申请号：PCT/EP1996004075
申请日：1996-09-16
申请人： PHARMACIA S.P.A. , MANTEGANI, Sergio , BANDIERA, Tiziano , VILLA, Manuela , VARASI, Mario , SPECIALE, Carmela
发明人： PHARMACIA S.P.A.
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： Disubstituted piperidine derivatives of formula (I), wherein R1 is hydrogen; bromo; chloro; a linear or branched C1-C5 alkyl group; a linear or branched C1-C5 alkoxy group; or an optionally substituted phenyl group; R2 is hydrogen, a linear or branched C1-C5 alkyl group or an optionally substituted phenyl group; X is CH2, C=O, CHOH or C=NOH; R3 is hydrogen or a linear or branched C1-C5 alkyl group; Y is a (CH2)n group in which n is an integer from 0 to 4, CHOH, C=O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; if the case, either as single isomers or as racemic mixtures, and their pharmaceutically acceptable salts, which possess selective neuroprotective activity, are useful in the treatment of an acute or a degenerative CNS disease. A process for preparing compounds of formula (I) and pharmaceutical compositions comprising them are also described.
摘要翻译：式（I）的二取代的哌啶衍生物，其中R 1是氢; 溴; 氯; 直链或支链C 1 -C 5烷基; 直链或支链C 1 -C 5烷氧基; 或任选取代的苯基; R2是氢，直链或支链C1-C5烷基或任意取代的苯基; X是CH 2，C = O，CHOH或C = NOH; R3是氢或直链或支链C1-C5烷基; Y为（CH 2）n基团，其中n为0至4的整数，CHOH，C = O或CH-A，其中A为任选取代的苯基; A是任选取代的苯基; W是氢或羟基; 如果具有选择性神经保护活性的情况，作为单一异构体或外消旋混合物及其药学上可接受的盐可用于治疗急性或退行性CNS疾病。还描述了制备式（I）化合物的方法和包含它们的药物组合物。

9. 发明专利

IL212250A Acrylamido derivatives useful as inhibitors of the mitochondrial permeability transition 未知
公开(公告)号：IL212250A
公开(公告)日：2015-11-30
申请号：IL21225011
申请日：2011-04-11
申请人： VARASI MARIO , CARENZI GIACOMO , MINUCCI SAVERIO , CONGENIA SRL , FANCELLI DANIELE , PLYTE SIMON , BALLARINI MARCO , CAPPA ANNA , PAIN GILLES , VILLA MANUELA
发明人： VARASI MARIO , CARENZI GIACOMO , MINUCCI SAVERIO , FANCELLI DANIELE , PLYTE SIMON , BALLARINI MARCO , CAPPA ANNA , PAIN GILLES , VILLA MANUELA
IPC分类号： A61K20060101 , A61P20060101 , C07C20060101 , C07D20060101
摘要： Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R', R", W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.

10. 发明专利

IL212250D0 ACRYLAMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION 未知
公开(公告)号：IL212250D0
公开(公告)日：2011-06-30
申请号：IL21225011
申请日：2011-04-11
申请人： VARASI MARIO , CARENZI GIACOMO , MINUCCI SAVERIO , CONGENIA SRL , FANCELLI DANIELE , PLYTE SIMON , BALLARINI MARCO , CAPPA ANNA , PAIN GILLES , VILLA MANUELA
IPC分类号： C07C20060101
摘要： Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R', R", W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.

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