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1.发明授权Acrylamido derivatives useful as inhibitors of the mitochondrial permeability transition 有权丙烯酰胺衍生物可用作线粒体通透性转换的抑制剂公开(公告)号：US08470831B2
公开(公告)日：2013-06-25
申请号：US13123852
申请日：2009-09-23
申请人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
发明人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
IPC分类号： A61K31/4965 , A61K31/445 , A61K31/4178 , A61K31/416 , A61K31/22 , A61K31/19 , A61K31/18 , A61K31/167 , C07D295/12 , C07D241/04 , C07D211/32 , C07D403/06 , C07D231/56 , C07D295/096 , C07C69/017 , C07C65/19 , C07C311/13 , C07C233/88
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。
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2.发明申请ACRYLOMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION 有权丙烯酰胺衍生物有助于作为MITOCHENDRIAL渗透性转换的抑制剂公开(公告)号：US20130245019A1
公开(公告)日：2013-09-19
申请号：US13874081
申请日：2013-04-30
申请人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
发明人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
IPC分类号： C07C235/38 , C07D213/36 , C07D209/08 , C07D233/64 , C07D263/32 , C07C323/41 , C07D235/30 , C07D263/56 , C07D235/06 , C07D231/56 , C07D249/18 , C07D213/68 , C07D211/22 , C07D239/47 , C07D295/135 , C07D295/096 , C07D213/30
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。
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3.发明授权Acrylomido derivatives useful as inhibitors of the mitochondrial permeability transition 有权Acrylomido衍生物可用作线粒体通透性转换的抑制剂公开(公告)号：US08669261B2
公开(公告)日：2014-03-11
申请号：US13874081
申请日：2013-04-30
申请人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
发明人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
IPC分类号： A61K31/4965 , A61K31/445 , A61K31/4178 , A61K31/416 , A61K31/22 , A61K31/19 , A61K31/18 , A61K31/167
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。
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4.发明申请ACRYLAMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION 有权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：US20110195977A1
公开(公告)日：2011-08-11
申请号：US13123852
申请日：2009-09-23
申请人： Daniele Fancelli , Varasi Mario , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
发明人： Daniele Fancelli , Varasi Mario , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
IPC分类号： A61K31/4965 , A61K31/445 , A61K31/4178 , A61K31/416 , A61K31/22 , A61K31/19 , A61K31/18 , A61K31/167 , C07D295/12 , C07D241/04 , C07D211/32 , C07D403/06 , C07D231/56 , C07C69/017 , C07C65/19 , C07C311/13 , C07C233/88 , C07D295/096 , A61P25/28 , A61P3/10 , A61P25/00 , A61P25/16
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。
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5.发明申请Bicyclo-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开作为激酶抑制剂活性的双环吡唑衍生物，其制备方法和包含它们的药物组合物公开(公告)号：US20070037790A1
公开(公告)日：2007-02-15
申请号：US10548332
申请日：2004-03-02
IPC分类号： A61K31/55 , A61K31/4745
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。
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6.发明申请Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开作为激酶抑制剂活性的双环吡唑，其制备方法和包含它们的药物组合物公开(公告)号：US20060135508A1
公开(公告)日：2006-06-22
申请号：US10522253
申请日：2003-07-16
IPC分类号： A61K31/55 , A61K31/4745 , C07D487/02 , C07D471/02
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。
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7.发明申请Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开作为激酶抑制剂活性的双环吡唑，其制备方法和包含它们的药物组合物公开(公告)号：US20060100233A1
公开(公告)日：2006-05-11
申请号：US10522254
申请日：2003-07-01
IPC分类号： A61K31/4745 , C07D471/02
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。
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![Substituted pyrazolo[4,3-C]pyridine derivatives active as kinase inhibitors](/abs-image/US/2012/05/08/US08173659B2/abs.jpg.150x150.jpg)
8.发明授权Substituted pyrazolo[4,3-C]pyridine derivatives active as kinase inhibitors 有权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：US08173659B2
公开(公告)日：2012-05-08
申请号：US13085889
申请日：2011-04-13
申请人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
发明人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
IPC分类号： A61K31/496 , A61K31/437
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。
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9.发明申请Arylmethyl-carbonylamino-thiazole derivatives and their use as antitumor agents 审中-公开芳基甲基 - 羰基氨基 - 噻唑衍生物及其作为抗肿瘤剂的用途公开(公告)号：US20050004120A1
公开(公告)日：2005-01-06
申请号：US10902326
申请日：2004-07-29
申请人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
发明人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
IPC分类号： C07D277/20 , A61K20060101 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/5377 , A61P20060101 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/08 , A61P19/02 , A61P25/28 , A61P31/12 , A61P35/00 , A61P37/02 , C07D20060101 , C07D277/04 , C07D277/46 , C07D401/00 , C07D417/12 , C07D417/14
CPC分类号： A61K31/426 , C07D277/46
摘要： A method of modulating apoptosis or treating diseases associated with protein kinases by administering to a mammal in need thereof of an effective amount of 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are as defined herein, or pharmaceutically acceptable salts thereof.
摘要翻译： 通过向有需要的哺乳动物施用有效量的由式（I）或（II）表示的2-氨基-1,3-噻唑衍生物来调节凋亡或治疗与蛋白激酶相关的疾病的方法：其中R，R 1 ，R2和R3如本文所定义，或其药学上可接受的盐。
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10.发明授权Arylmethyl-carbonylamino-thiazole derivatives and their use as antitumor agents 失效芳基甲基 - 羰基氨基 - 噻唑衍生物及其作为抗肿瘤剂的用途公开(公告)号：US06784198B1
公开(公告)日：2004-08-31
申请号：US10048474
申请日：2002-07-18
申请人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
发明人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
IPC分类号： A61K31425
CPC分类号： A61K31/426 , C07D277/46
摘要： 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof are useful as, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
摘要翻译： 由式（I）或（II）表示的2-氨基-1,3-噻唑衍生物：其中R，R 1，R 2和R 3在本文中定义，或其药学上可接受的盐可用作例如癌症的治疗， 细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病或神经变性疾病。
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