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1. 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。

2. 发明授权

US06376617B1 Bioactive derivatives of camptothecin 失效
标题翻译：喜树碱的生物活性衍生物
公开(公告)号：US06376617B1
公开(公告)日：2002-04-23
申请号：US09308667
申请日：1999-06-03
申请人： Francesco Angelucci , Gabriele Fachin , Valeria Caiolfa , Antonino Suarato
发明人： Francesco Angelucci , Gabriele Fachin , Valeria Caiolfa , Antonino Suarato
IPC分类号： C08F22056
CPC分类号： A61K47/58 , A61K47/65
摘要： Water soluble polymeric conjugates of camptothecin consist essentially of N-(2-hydroxypropyl)methacryloylamide units linked via a spacer group to a residue of a camptothecin such as irinotecan or its non-soluble metabolite, 7-ethyl-10-hydroxy-camptothecin. The conjugates possess enhance antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation and the pharmaceutical compositions containing them are also described.
摘要翻译：喜树碱的水溶性聚合物缀合物基本上由通过间隔基团连接到喜树碱的残基例如伊立替康或其不溶性代谢物7-乙基-10-羟基喜树碱的N-（2-羟丙基）甲基丙烯酰胺单元组成。缀合物相对于游离药物具有增强的抗肿瘤活性和降低的毒性。还描述了其制备方法和含有它们的药物组合物。

3. 发明授权

US5773522A Polymer-bound camptothecin derivatives 失效
标题翻译：聚合物键合的喜树碱衍生物
公开(公告)号：US5773522A
公开(公告)日：1998-06-30
申请号：US448330
申请日：1995-06-08
申请人： Francesco Angelucci , Antonino Suarato
发明人： Francesco Angelucci , Antonino Suarato
IPC分类号： A61K47/48 , C08F220/36 , C08F220/56 , C08F220/60 , C08F20/56 , A01N43/42 , C08F120/56
CPC分类号： A61K47/48176 , A61K47/4823 , A61K47/48338
摘要： A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2-hydroxypropyl) methacryloylamide units represented by formula 1: ##STR1## (ii) from 1 to 40 mol % of 20-0-(N-methacryloylglycyl-aminoacyl) camptothecin units represented by formula 2 ##STR2## wherein �A! is a spacer group having respective terminal amino and carbonyl groups which are separated by at least three atoms and O-CPT represents a residue of a camptothecin, the C-20 hydroxy group of the camptothecin being linked to the terminal carbonyl group of the spacer group �A!; and (iii) from 0 to 10 mol % of N-methacryloylglycine or N-(2-hydroxy-propyl)methacryloylglycinamide units represented by formula 3: ##STR3## wherein Z represents hydroxy or a residue of formula --NH--CH.sub.2 --CH(OH)--CH.sub.3.
摘要翻译： PCT No.PCT / EP94 / 03154 Sec。 371日期：1995年6月8日 102（e）日期1995年6月8日PCT 1994年9月21日PCT公布。公开号WO95 / 10304 日期1995年04月20日一种聚合共轭物基本上由以下组成：（i）60至99mol％由式1表示的N-（2-羟丙基）甲基丙烯酰胺单元：乙酰丙酰基甘氨酰 - 氨酰基）喜树碱单元由式2 其中[A]是具有分别具有至少三个原子的末端氨基和羰基的间隔基，O-CPT表示喜树碱的残基，喜树碱的C 20羟基与末端羰基连接的间隔基[A]; 和（iii）0至10摩尔％的由式3表示的N-甲基丙烯酰基甘氨酸或N-（2-羟基 - 丙基）甲基丙烯酰基甘氨酰胺单元：其中Z表示羟基或式-NH-CH2-CH （OH）-CH 3。

4. 发明授权

US5473055A 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：US5473055A
公开(公告)日：1995-12-05
申请号：US263832
申请日：1994-06-22
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 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08
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,Gly-.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， βAla，Phe-Gly-βAla，Phe-Phe-βAla，Leu-Gly-βAla，Val-Ala-Ala，Phe-Ala-Ala，Leu-Phe-βAla，Leu-Gly-β Ala，Phe-Leu-Gly-βAla，Phe-Phe-LeuβAla，Leu-Leu-Gly-βAla，Phe-Tyr-Ala-βAla，Phe-Gly-Phe-β，Phe-Phe-Gly β-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，这些化合物具有抗肿瘤活性，。还描述了其制备方法和含有它们的药物组合物。

5. 发明授权

US5719265A 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：US5719265A
公开(公告)日：1998-02-17
申请号：US508209
申请日：1995-07-27
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 , A61K38/04
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##
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; 0〜9.9摩尔％的由式表示的单元

6. 发明授权

US5569720A Polymer-bound paclitaxel derivatives 失效
公开(公告)号：US5569720A
公开(公告)日：1996-10-29
申请号：US508210
申请日：1995-07-27
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 , C08F20/56 , C08F8/30 , C08F8/32
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,Gly-.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.

7. 发明授权

US4906743A 4-demethoxy-4-amino-anthracyclines 失效
公开(公告)号：US4906743A
公开(公告)日：1990-03-06
申请号：US181506
申请日：1988-04-14
申请人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
发明人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
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 diazotized 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.

8. 发明申请

US20050107543A1 Fluoro linkers and their use as linkers for enzyme-activated drug conjugates 审中-公开
标题翻译：氟接头及其作为酶活化药物偶联物的接头的用途
公开(公告)号：US20050107543A1
公开(公告)日：2005-05-19
申请号：US10486477
申请日：2002-07-29
申请人： Francesco Angelucci , Antonino Suarato , Michele Caruso , Alessandra Scolaro , Enrico Pesenti , Daniela Faiardi
发明人： Francesco Angelucci , Antonino Suarato , Michele Caruso , Alessandra Scolaro , Enrico Pesenti , Daniela Faiardi
IPC分类号： C07D491/22 , A61K38/00 , A61K47/48 , A61P35/00 , A61P35/02 , C07C271/22 , C07D207/46 , C07D209/48 , C07K5/10 , C07K7/06 , C07F7/02 , C08G63/48 , C08G63/91
CPC分类号： C07C271/22 , Y02P20/55
摘要： The present invention provides compounds or formula (1) R1—HN—CH2—CF2—(CH2)l—CR3R4—CO—R2, wherein: l is 0, 1 or 2, R1 is a labile amino protecting group, R2 is hydroxy group or the residue or an activated ester or halogen atom; R3 and R4 are independently hydrogen atom or C1-C4 alkyl chain. There are also provided their preparation and the water-soluble conjugates based on these linkers, endowed with selective anticancer activity.
摘要翻译：本发明提供化合物或式（1）R 1 -HN-CH 2 -CF 2 - （CH 2）其中：l是0,1或2，其中：l是0,1或2，其中：l是0,1或2，或2，R 1是不稳定的氨基保护基团，R 2是羟基或残基或活化的酯或卤素原子; R 3和R 4独立地是氢原子或C 1 -C 4烷基链。还提供了它们的制备和基于这些接头的水溶性缀合物，具有选择性的抗癌活性。

9. 发明授权

US5547667A Linker for bioactive agents 失效
标题翻译：生物活性剂接头
公开(公告)号：US5547667A
公开(公告)日：1996-08-20
申请号：US328697
申请日：1994-10-25
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 , A61K39/44 , C07K17/06 , C07K15/252 , C07K19/06
CPC分类号： C07H15/252 , A61K47/48176 , A61K47/48246 , A61K47/48407 , A61K47/48692 , A61K47/48715 , C07H19/24
摘要： Conjugates of general formula 1:[A--O--W--Z].sub.a --T 1wherein the moiety 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：通式1的缀合物：[A-O-W-Z] a-T1，其中A-O-部分是式A-O-H的药物的残基，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。

10. 发明授权

US5412081A New 4'-epi-4'-amino anthracyclines 失效
标题翻译：新的4'-epi-4'-氨基蒽环类
公开(公告)号：US5412081A
公开(公告)日：1995-05-02
申请号：US1229
申请日：1993-01-06
申请人： Francesco Angelucci , Alberto Bargiotti , Daniela Faiardi , Stefania Stefanelli , Antonino Suarato
发明人： Francesco Angelucci , Alberto Bargiotti , Daniela Faiardi , Stefania Stefanelli , Antonino Suarato
IPC分类号： C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides having the general formula 1 and 2: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, fluorine, hydroxy or amino; R.sub.2 and R.sub.3 represent hydroxy or one of R.sub.2 and R.sub.3 is a hydrogen atom, a nitro or an amino group and the other of R.sub.2 and R.sub.3 is a HYDROXY group, exhibit activity against LoVo and LoVo/Dx in vitro.
摘要翻译：具有通式1和2的蒽环酸苷：其中R 1选自氢，氟，羟基或氨基; R2和R3代表羟基或R2和R3之一是氢原子，硝基或氨基，R2和R3中的另一个是羟基，体外表现出对LoVo和LoVo / Dx的活性。

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