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公开(公告)号：US5387578A
公开(公告)日：1995-02-07
申请号：US842171
申请日：1992-04-03
申请人： Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
发明人： Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K39/395 , A61K47/00 , A61K47/48 , A61P35/00 , C07H20060101 , C07H15/252 , C07H17/00 , C07H19/24 , A61K37/00 , C07H19/06 , C07K17/06
CPC分类号： C07H15/252 , A61K47/48176 , A61K47/48246 , A61K47/48407 , A61K47/48692 , A61K47/48715 , C07H19/24
摘要： Conjugate of general formula 1:[A--O--W-Z].sub.a -T 1wherein the moity A--O--is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.
摘要翻译： PCT No.PCT / EP91 / 01449 371日期：1992年4月3日 102（e）日期1992年4月3日PCT 1991年8月1日PCT PCT。 公开号WO92 / 02255 通式1：[A-O-W-Z] a-T1的结合物，其中，A-O-是式A-O-H药物的残基，其中-O-H是伯或仲羟基; a为1〜30的整数; W是通式2的基团：其中b是1至4的整数，B表示C1-C3亚烷基，R1和R2各自独立地表示氢，卤素，烷基，苯基或取代的苯基; Z是间隔基，T是载体部分。
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公开(公告)号：US4985548A
公开(公告)日：1991-01-15
申请号：US462549
申请日：1990-01-09
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C46/00 , C07C50/22 , C07C50/38 , C07C225/34 , C07H15/252
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotised followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.
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公开(公告)号：US08227472B2
公开(公告)日：2012-07-24
申请号：US12444792
申请日：2007-10-09
IPC分类号： A61K31/497 , A61K31/445 , A61K31/415 , A01N43/40 , A01N43/56 , C07D403/00 , C07D211/32 , C07D231/54 , C07D487/02
CPC分类号： C07D487/04
摘要： Substituted pyrrolo-pyrazole 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 dysregulated protein kinase activity, like cancer.
摘要翻译： 公开了如说明书中定义的式（I）的取代吡咯并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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24.发明申请SUBSTITUTED DIHYDROPTERIDIN-6-ONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS 失效取代的二氢蝶啶-6-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：US20110053944A1
公开(公告)日：2011-03-03
申请号：US12744770
申请日：2008-11-26
IPC分类号： A61K31/4985 , C07D475/04 , A61P35/00 , A61P37/02
CPC分类号： C07D475/00
摘要： Dihydropteridin-6-one 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）的二氢蝶啶-6-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。
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25.发明授权Anthracycline derivative conjugates, process for their preparation and their use as antitumor compounds 有权蒽环类衍生物缀合物，其制备方法及其作为抗肿瘤化合物的用途公开(公告)号：US08900589B2
公开(公告)日：2014-12-02
申请号：US12502433
申请日：2009-07-14
申请人： Italo Beria , Michele Caruso , John A. Flygare , Vittoria Lupi , Rita Perego , Paul Polakis , Andrew Polson , Matteo Salsa , Susan D. Spencer , Barbara Valsasina , Robert L. Cohen
发明人： Italo Beria , Michele Caruso , John A. Flygare , Vittoria Lupi , Rita Perego , Paul Polakis , Andrew Polson , Matteo Salsa , Susan D. Spencer , Barbara Valsasina , Robert L. Cohen
CPC分类号： C07K16/2863 , A61K47/64 , A61K47/6809 , C07K2317/76
摘要： The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.
摘要翻译： 本发明涉及治疗有用的蒽环类与载体的缀合物，例如天然或合成来源的多克隆和单克隆抗体，蛋白质或肽; 其制备方法，含有它们的药物组合物及其在治疗某些哺乳动物肿瘤中的用途。
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公开(公告)号：US20100010008A1
公开(公告)日：2010-01-14
申请号：US12444792
申请日：2007-10-09
IPC分类号： A61K31/4162 , C07D487/04 , A61P35/00 , A61P25/28 , A61P31/12 , A61P37/00 , C07D401/14 , A61K31/454 , A61K31/496 , C07D403/14
CPC分类号： C07D487/04
摘要： Substituted pyrrolo-pyrazole 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 dysregulated protein kinase activity, like cancer.
摘要翻译： 公开了如说明书中定义的式（I）的取代吡咯并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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27.发明授权Anthracycline derivative conjugates, process for their preparation and their use as antitumor compounds 有权蒽环类衍生物缀合物，其制备方法及其作为抗肿瘤化合物的用途公开(公告)号：US08389697B2
公开(公告)日：2013-03-05
申请号：US13360212
申请日：2012-01-27
申请人： Italo Beria , Michele Caruso , John A. Flygare , Vittoria Lupi , Rita Perego , Paul Polakis , Andrew Polson , Matteo Salsa , Susan D. Spencer , Barbara Valsasina
发明人： Italo Beria , Michele Caruso , John A. Flygare , Vittoria Lupi , Rita Perego , Paul Polakis , Andrew Polson , Matteo Salsa , Susan D. Spencer , Barbara Valsasina
IPC分类号： C07H15/24
CPC分类号： C07K16/2863 , A61K47/64 , A61K47/6809 , C07K2317/76
摘要： The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.
摘要翻译： 本发明涉及治疗有用的蒽环类与载体的缀合物，例如天然或合成来源的多克隆和单克隆抗体，蛋白质或肽; 其制备方法，含有它们的药物组合物及其在治疗某些哺乳动物肿瘤中的用途。
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公开(公告)号：US20120142906A1
公开(公告)日：2012-06-07
申请号：US13308799
申请日：2011-12-01
申请人： Michele Caruso , Vittoria Lupi , Matteo Salsa
发明人： Michele Caruso , Vittoria Lupi , Matteo Salsa
CPC分类号： C07H15/244 , C07H1/00 , C07H19/24
摘要： The present invention provides a process for the preparation of a morpholinyl anthracycline derivative in good yields and purity, including 3′-deamino-3″-4′-anhydro-[2″(S)-methoxy-3″(R)-hydroxy-4″-morpholinyl]doxorubicin (1).
摘要翻译： 本发明提供以良好的产率和纯度制备吗啉基蒽环类衍生物的方法，包括3'-脱氨基-3“-4'-脱水 - [2”（S） - 甲氧基-3“（R） - 羟基 -4“ - 吗啉基]多柔比星（1）。
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29.发明申请ANTHRACYCLINE DERIVATIVE CONJUGATES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR COMPOUNDS 有权蒽醌衍生物偶联物，其制备方法及其作为抗微生物化合物的用途公开(公告)号：US20120130059A1
公开(公告)日：2012-05-24
申请号：US13360212
申请日：2012-01-27
申请人： Italo Beria , Michele Caruso , John A. Flygare , Vittoria Lupi , Rita Perego , Paul Polakis , Andrew Polson , Matteo Salsa , Susan D. Spencer , Barbara Valsasina
发明人： Italo Beria , Michele Caruso , John A. Flygare , Vittoria Lupi , Rita Perego , Paul Polakis , Andrew Polson , Matteo Salsa , Susan D. Spencer , Barbara Valsasina
IPC分类号： C07H15/26 , C07H15/252
CPC分类号： C07K16/2863 , A61K47/64 , A61K47/6809 , C07K2317/76
摘要： The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.
摘要翻译： 本发明涉及治疗有用的蒽环类与载体的缀合物，例如天然或合成来源的多克隆和单克隆抗体，蛋白质或肽; 其制备方法，含有它们的药物组合物及其在治疗某些哺乳动物肿瘤中的用途。
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30.发明授权3-Oxo-2,3-dihydro-1H-indazole-4-carboxamide derivatives as PARP-1 inhibitors 有权3-氧代-2,3-二氢-1H-吲唑-4-甲酰胺衍生物作为PARP-1抑制剂公开(公告)号：US09073893B2
公开(公告)日：2015-07-07
申请号：US14233963
申请日：2012-07-18
申请人： Gianluca Mariano Enrico Papeo , Daniela Borghi , Michele Caruso , Helena Posteri , Mikhail Yurievitch Krasavin
发明人： Gianluca Mariano Enrico Papeo , Daniela Borghi , Michele Caruso , Helena Posteri , Mikhail Yurievitch Krasavin
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D401/10 , C07D403/04 , C07D409/14 , A61K31/4188 , A61K31/454
CPC分类号： C07D401/04 , A61K31/4188 , A61K31/454 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14
摘要： There are provided 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
摘要翻译： 提供了选择性抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性的3-氧代-2,3-二氢-1H-吲唑-4-甲酰胺衍生物 。 因此，本发明的化合物可用于治疗诸如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症的疾病。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及利用包含这些化合物的药物组合物治疗疾病的方法。
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