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31. 发明申请

US20100210476A1 Pyrrolo[2,3-b]Pyridine Derivatives Active as Kinase Inhibitors and Pharmaceutical Compositions Comprising Them 有权
标题翻译：吡咯并[2,3-b]吡啶衍生物作为激酶抑制剂和药物组合物
公开(公告)号：US20100210476A1
公开(公告)日：2010-08-19
申请号：US12766230
申请日：2010-04-23
申请人： Barbara Salom , Matteo D'Anello , Maria Gabriella Brasca , Patrizia Giordano , Katia Martina , Francesco Angelucci , Frederick Arthur Brookfield , William John Trigg , Edward Andrew Boyd , Jonathan Anthony Larard
发明人： Barbara Salom , Matteo D'Anello , Maria Gabriella Brasca , Patrizia Giordano , Katia Martina , Francesco Angelucci , Frederick Arthur Brookfield , William John Trigg , Edward Andrew Boyd , Jonathan Anthony Larard
IPC分类号： C40B40/04 , A61K31/437 , A61K31/5377 , A61K31/496 , A61P35/00 , A61P25/28 , A61P31/12 , A61P13/08 , A61P17/06 , A61P9/10 , A61P19/02 , A61P35/04 , A61P37/06 , A61P17/14
CPC分类号： C07D471/04
摘要： Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds 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; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了吡咯并[2,3-b]吡啶衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化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。还公开了在SPS条件下制备本发明化合物的方法和包含其中多个化合物的化学文库。

32. 发明授权

US06328953B1 Polymeric derivatives of camptothecins 失效
标题翻译：喜树碱的聚合衍生物
公开(公告)号：US06328953B1
公开(公告)日：2001-12-11
申请号：US09509534
申请日：2000-03-31
申请人： Francesco Angelucci , Fabrizio Orzi , Gabriele Fachin , Valeria Caiolfa , Moreno Zamai , Antonino Suarato
发明人： Francesco Angelucci , Fabrizio Orzi , Gabriele Fachin , Valeria Caiolfa , Moreno Zamai , Antonino Suarato
IPC分类号： A61K31435
CPC分类号： A61K47/58
摘要： The invention relates to polymeric conjugates of 20-O-[glycyl-aminoacyl-glycyl]-camptothecins and a process for producing the same.
摘要翻译：本发明涉及20-O- [甘氨酰 - 酰基 - 甘氨酰] - 喜树碱的聚合物缀合物及其制备方法。

33. 发明授权

US5776458A Anthracycline-conjugates 失效
标题翻译：蒽环霉素共轭物
公开(公告)号：US5776458A
公开(公告)日：1998-07-07
申请号：US412220
申请日：1995-03-27
申请人： Francesco Angelucci , Daniela Ruggieri , Stefania Stefanelli , Antonino Suarato , Laura Bersani
发明人： Francesco Angelucci , Daniela Ruggieri , Stefania Stefanelli , Antonino Suarato , Laura Bersani
IPC分类号： A61K47/48 , C07H15/252 , A61K39/395 , A61K39/00 , C07K16/00 , C07K17/00
CPC分类号： C07H15/252 , A61K47/48407
摘要： The present invention provides anthracycline conjugates with carriers such as monoclonal polyclonal antibodies, proteins or peptides, or other synthetic carriers. These anthracycline conjugates provide pharmaceutical compositions which are useful for treating certain mammalian tumors. The compounds of the present invention have higher potency than anthracyclines, and improved therapeutic efficacy and reduced toxic effects.
摘要翻译：本发明提供了与载体例如单克隆多克隆抗体，蛋白质或肽或其它合成载体的蒽环霉素缀合物。这些蒽环霉素缀合物提供可用于治疗某些哺乳动物肿瘤的药物组合物。本发明的化合物具有比蒽环类药更高的效力，并且具有改善的治疗功效和降低的毒性作用。

34. 发明授权

US5571785A Biologically active compounds 失效
标题翻译：生物活性化合物
公开(公告)号：US5571785A
公开(公告)日：1996-11-05
申请号：US351474
申请日：1994-12-20
申请人： Francesco Angelucci , Maria Grandi , Antonino Suarato
发明人： Francesco Angelucci , Maria Grandi , Antonino Suarato
IPC分类号： C07K17/08 , A61K47/48 , A61P35/00 , C07H15/24 , C07K5/107 , C07K9/00 , A61K38/16 , A61K31/70
CPC分类号： A61K47/48176 , Y02P20/582
摘要： The present invention provides polymer-bound anthracyclines of formula A which consists essentially of three units represented by formulae 1, 2 and 3: ##STR1## wherein: Gly represents glycine;n is 0 or 1;x is from 70 to 98 mol %,y is from 1 to 29 mol %,z is from 1 to 29 mol %,R.sub.1 is a C.sub.1 -C.sub.6 alkyl group substituted by one or more hydroxy groups;Y is an amino acid residue or a peptide spacer;[NH--D] is the residue of an anthracycline aminoglycoside [NH.sub.2 --D]; andZ is a hydroxy group or a residue of formula --NHR.sub.1 wherein R.sub.1 is as defined above. Methods for their preparation and pharmaceutical compositions containing them are also provided.
摘要翻译： PCT No.PCT / EP94 / 01100 Sec。 371日期1994年12月20日第 102（e）1994年12月20日PCT PCT 1994年4月8日PCT公布。第WO94 / 26311号公报日期1994年11月24日本发明提供式A的聚合物键合蒽环类药物，其基本上由式1，2和3表示的三个单元组成：其中：Gly表示甘氨酸; n为0或1; x为70〜98摩尔％，y为1〜29摩尔％，z为1〜29摩尔％，R1为被一个或多个羟基取代的C1-C6烷基。 Y是氨基酸残基或肽间隔基; [NH-D]是蒽环类氨基糖苷[NH2-D]的残基; 并且Z是羟基或式-NHR1的残基，其中R 1如上所定义。还提供了它们的制备方法和含有它们的药物组合物。

35. 发明授权

US5387578A New linker for bioactive agents 失效
标题翻译：生物活性剂的新接头
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。

36. 发明授权

US5362831A Polymer-bound paclitaxel derivatives 失效
标题翻译：聚合物结合紫杉醇衍生物
公开(公告)号：US5362831A
公开(公告)日：1994-11-08
申请号：US77065
申请日：1993-06-16
申请人： Nicola Mongelli , Francesco Angelucci , Enrico Pesenti , Antonino Suarato , Giovanni Biasoli
发明人： Nicola Mongelli , Francesco Angelucci , Enrico Pesenti , Antonino Suarato , Giovanni Biasoli
IPC分类号： A61K38/00 , A61K38/02 , A61K47/48 , A61P35/00 , C07D305/14 , C07K5/062 , C07K5/065 , C07K5/083 , C07K5/087 , C07K5/103 , C07K5/107 , A61K31/765 , C80F222/38
CPC分类号： A61K47/48176 , C07D305/14
摘要： A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：一种聚合物共轭物，其基本上由以下组成：90至99.9摩尔％的由式（IMAGE）表示的单元，为0.1至5摩尔％的由式IMA图示的单元，其中R 1和R 2之一是式，另一个是氢原子; 其中R是苯基或叔丁氧基，R3是H或乙酰基，A和A1可以相同或不同，表示化学单键，选自βAla，Gly，Phe-Gly，Phe-Phe-，Leu-Gly，Val-Ala，Phe-Ala，Leu-Phe，Leu-Ala，Phe-Leu-Gly的氨基酸残基或肽间隔子， Phe-Phe-Leu，Leu-Leu-Gly，Phe-Tyr-Ala，Phe-Gly-Phe，Phe-Phe-Gly，Phe-Leu-Gly-Phe，Gly-Phe-Leu-Gly-Phe， Ala，Phe-Gly-βAla，Phe-Phe-βAla，Leu-Gly-βAla，Val-Ala-βAla，Phe-Ala-βAla，Leu-Phe-βAla，Leu-Gly-βAla ，Phe-Leu-Gly-β-Ala，Phe-Phe-LeuβAla，Leu-Leu-Gly-βAla，Phe-Tyr-Ala-βAla，Phe-Gly-Phe-β，Phe-Phe-Glyβ Ala，Phe-Leu-Gly-Phe-β-Ala或Gly-Phe-Leu-Gly-Phe-β-Ala。与紫杉醇或其已知的类似物相比，该化合物具有抗肿瘤活性并显示改善的水溶性和降低的毒性。还描述了其制备方法和含有它们的药物组合物。

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