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1. 发明申请

WO2013096901A8 PHARMACEUTICAL FORMULATIONS FOR FUMAGILLIN DERIVATIVE-PHF CONJUGATES 审中-公开
标题翻译： FUMAGILLIN衍生物 - PHF结合物的药物制剂
公开(公告)号：WO2013096901A8
公开(公告)日：2014-08-07
申请号：PCT/US2012071477
申请日：2012-12-21
申请人： MERSANA THERAPEUTICS INC , AKULLIAN LAURA , LIU GUI , LOWINGER TIMOTHY B , MCGILLICUDDY DENNIS , STEVENSON CHERI , VAN DUZER JOHN , YIN MAO , YURKOVETSKIY ALEKSANDR
发明人： AKULLIAN LAURA , LIU GUI , LOWINGER TIMOTHY B , MCGILLICUDDY DENNIS , STEVENSON CHERI , VAN DUZER JOHN , YIN MAO , YURKOVETSKIY ALEKSANDR
IPC分类号： C07D303/12
CPC分类号： A61K47/48192 , A61K47/60 , C07D303/22
摘要： The invention described herein provides a mixture comprising polymer molecules or salts thereof, wherein a polymer molecule in the mixture comprises covalently bound subunits L, K, and M wherein the average molecular weight of the polymer molecules in the mixture is about 50 kDa to about 200 kDa, wherein the mole percentage of subunit M, relative to the total amount of subunits in the mixture, is about 90.5 to about 96 mol%, v1 herein the mole percentage of subunit K, relative to the total amount of subunits in the mixture, is about 2.8 to about 7.3 mol%, and wherein the mole percentage of subunit L, is about relative to the total amount of subunits in the mixture, 1. 2 to about 2. 2 mol%.
摘要翻译：本文描述的本发明提供了包含聚合物分子或其盐的混合物，其中该混合物中的聚合物分子包含共价结合的亚单位L，K和M，其中混合物中聚合物分子的平均分子量为约50kDa至约200 kDa，其中相对于混合物中亚单位总量的亚单位M的摩尔百分数为约90.5至约96mol％，v1为亚单位K的摩尔百分数，相对于混合物中亚单位的总量，为约2.8至约7.3摩尔％，并且其中亚单位L的摩尔百分比约为混合物中亚单位总量的1. 2至约2.2摩尔％。

2. 发明申请

WO2012171020A1 PROTEIN-POLYMER-DRUG CONJUGATES 审中-公开
标题翻译：蛋白聚合物药物结合
公开(公告)号：WO2012171020A1
公开(公告)日：2012-12-13
申请号：PCT/US2012/041931
申请日：2012-06-11
申请人： MERSANA THERAPEUTICS, INC. , YURKOVETSKIY, Aleksandr , YIN, Mao , LOWINGER, Timothy, B. , THOMAS, Joshua, D. , HAMMOND, Charles, E. , STEVENSON, Cheri, A. , BODYAK, Natalya, D. , CONLON, Patrick, R. , GUMEROV, Dmitry, R.
发明人： YURKOVETSKIY, Aleksandr , YIN, Mao , LOWINGER, Timothy, B. , THOMAS, Joshua, D. , HAMMOND, Charles, E. , STEVENSON, Cheri, A. , BODYAK, Natalya, D. , CONLON, Patrick, R. , GUMEROV, Dmitry, R.
IPC分类号： A61K47/48 , C07K5/02 , C07K7/06 , A61P35/00
CPC分类号： A61K47/6849 , A61K31/4745 , A61K47/59 , A61K47/64 , A61K47/6803 , A61K47/6883 , C07K7/02 , C07K16/32 , C08G65/33396 , C08G65/334
摘要： A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L D -D, the protein based recognition-molecule being connected to the polymeric carrier by L p . Each occurrence of D is independently a therapeutic agent having a molecular weight ≤ 5 kDa. L D and L p are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
摘要翻译：本文提供药物缀合物。缀合物包含基于蛋白质的识别分子（PBRM）和被一个或多个-LD-D取代的聚合物载体，基于蛋白质的识别分子通过Lp连接到聚合物载体上。每次出现的D独立地是分子量= 5kDa的治疗剂。 LD和Lp分别是将治疗剂和PBRM分别连接到聚合物载体的接头。还公开了可用于与PBRM缀合以形成本文所述的聚合物 - 药物-PBRM缀合物的聚合物支架，包含缀合物的组合物，其制备方法，以及用缀合物或其组合物治疗各种病症的方法。

3. 发明申请

WO2010138719A1 POLYAL DRUG CONJUGATES COMPRISING VARIABLE RATE-RELEASING LINKERS 审中-公开
标题翻译：包括可变速率释放链接器的聚合药物
公开(公告)号：WO2010138719A1
公开(公告)日：2010-12-02
申请号：PCT/US2010/036413
申请日：2010-05-27
申请人： MERSANA THERAPEUTICS, INC. , YURKOVETSKIY, Aleksandr , YIN, Mao , LIU, Gui , AKULLIAN, Laura, C. , KANE, John, J. , STEVENSON, Cheri, A. , HAMMOND, Charles, E. , PETTER, Russell, C. , VAN DUZER, John, H. , LOWINGER, Timothy, B.
发明人： YURKOVETSKIY, Aleksandr , YIN, Mao , LIU, Gui , AKULLIAN, Laura, C. , KANE, John, J. , STEVENSON, Cheri, A. , HAMMOND, Charles, E. , PETTER, Russell, C. , VAN DUZER, John, H. , LOWINGER, Timothy, B.
IPC分类号： A61K31/74
CPC分类号： C07D519/04 , A61K47/59 , C07D491/22 , G01N2500/00 , Y10T436/145555
摘要： Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.
摘要翻译：描述包含可变速率释放连接体的多价 - 药物共轭物以及制备这种缀合物的方法。也描述了这种多种药物共轭物的用途。

4. 发明申请

WO2013096901A1 PHARMACEUTICAL FORMULATIONS FOR FUMAGILLIN DERIVATIVE-PHF CONJUGATES 审中-公开
标题翻译： FUMAGILLIN衍生物 - PHF结合物的药物制剂
公开(公告)号：WO2013096901A1
公开(公告)日：2013-06-27
申请号：PCT/US2012/071477
申请日：2012-12-21
申请人： MERSANA THERAPEUTICS, INC. , AKULLIAN, Laura , LIU, Gui , LOWINGER, Timothy B. , MCGILLICUDDY, Dennis , STEVENSON, Cheri , VAN DUZER, John , YIN, Mao , YURKOVETSKIY, Aleksandr
发明人： AKULLIAN, Laura , LIU, Gui , LOWINGER, Timothy B. , MCGILLICUDDY, Dennis , STEVENSON, Cheri , VAN DUZER, John , YIN, Mao , YURKOVETSKIY, Aleksandr
IPC分类号： C07D303/12
CPC分类号： A61K47/48192 , A61K47/60 , C07D303/22
摘要： The invention described herein provides a mixture comprising polymer molecules or salts thereof, wherein a polymer molecule in the mixture comprises covalently bound subunits L, K, and M wherein the average molecular weight of the polymer molecules in the mixture is about 50 kDa to about 200 kDa, wherein the mole percentage of subunit M, relative to the total amount of subunits in the mixture, is about 90.5 to about 96 mol%, v1 herein the mole percentage of subunit K, relative to the total amount of subunits in the mixture, is about 2.8 to about 7.3 mol%, and wherein the mole percentage of subunit L, is about relative to the total amount of subunits in the mixture, 1. 2 to about 2. 2 mol%.
摘要翻译：本文描述的本发明提供了包含聚合物分子或其盐的混合物，其中该混合物中的聚合物分子包含共价结合的亚单位L，K和M，其中混合物中聚合物分子的平均分子量为约50kDa至约200 kDa，其中相对于混合物中亚单位总量的亚单位M的摩尔百分数为约90.5至约96mol％，v1为亚单位K的摩尔百分数，相对于混合物中亚单位的总量，为约2.8至约7.3摩尔％，并且其中亚单位L的摩尔百分比约为混合物中亚单位总量的1. 2至约2.2摩尔％。

5. 发明申请

WO2009073445A2 BIOCOMPATIBLE BIODEGRADABLE FUMAGILLIN ANALOG CONJUGATES 审中-公开
标题翻译：生物可降解的FUMAGILLIN模拟结合
公开(公告)号：WO2009073445A2
公开(公告)日：2009-06-11
申请号：PCT/US2008/084539
申请日：2008-11-24
申请人： MERSANA THERAPEUTICS, INC. , STEVENSON, Cheri, A. , AKULLIAN, Laura, C. , PETTER, Russell C. , KANE, John, J. , HAMMOND, Charles, E. , YIN, Mao , YURKOVETSKIY, Aleksandr
发明人： STEVENSON, Cheri, A. , AKULLIAN, Laura, C. , PETTER, Russell C. , KANE, John, J. , HAMMOND, Charles, E. , YIN, Mao , YURKOVETSKIY, Aleksandr
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： C07D303/40 , A61K47/59 , C07D303/18 , C07D303/22 , C07D303/36 , C07D405/14 , C07D487/08
摘要： Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog.
摘要翻译：烟曲霉素类似物聚合物缀合物，制备烟曲霉素类似物聚合物共轭物的方法，包含烟曲霉素类似物的聚合物缀合物的组合物，以及用于治疗癌症的方法或治疗血管发生疾病的方法，包括向有需要的受试者施用有效量的烟曲霉素类似物。还描述了新的烟曲霉素类似物，制备烟曲霉素类似物的方法，包含至少一种烟曲霉素类似物的组合物，以及用于治疗癌症的方法或治疗血管发生疾病，包括向有需要的受试者施用有效量的烟曲霉素类似物。

6. 发明申请

WO2010068759A1 PHARMACEUTICAL FORMULATIONS OF BIODEGRADABLE BIOCOMPATIBLE CAMPTOTHECIN-POLYMER CONJUGATES 审中-公开
标题翻译：生物可降解生物活性聚合物共聚物的药物制剂
公开(公告)号：WO2010068759A1
公开(公告)日：2010-06-17
申请号：PCT/US2009/067505
申请日：2009-12-10
申请人： MERSANA THERAPEUTICS, INC. , ROLKE, James , PETTER, Russell, C. , YIN, Mao , YURKOVETSKIY, Aleksandr , LIU, Gui , FARHAN, Emile
发明人： ROLKE, James , PETTER, Russell, C. , YIN, Mao , YURKOVETSKIY, Aleksandr , LIU, Gui , FARHAN, Emile
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K47/48215 , A61K31/44 , A61K47/59
摘要： A camptothecin/polymer dual phase drug release system is described that is stable in both liquid and lyophilized states. The polymer contains acetals and/or ketals.
摘要翻译：描述了在液体和冻干状态下稳定的喜树碱/聚合物双相药物释放系统。聚合物含有缩醛和/或缩酮。

7. 发明申请

WO2011120053A1 MODIFIED POLYMERS FOR DELIVERY OF POLYNUCLEOTIDES, METHOD OF MANUFACTURE, AND METHODS OF USE THEREOF 审中-公开
标题翻译：用于输送多核苷酸的改性聚合物，其制造方法及其使用方法
公开(公告)号：WO2011120053A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/030225
申请日：2011-03-28
申请人： MERSANA THERAPEUTICS, INC. , YURKOVETSKIY, Aleksandr , YIN, Mao , LOWINGER, Timothy, B. , CABRAL, Carolina, B. , STEVENSON, Cheri, A. , HAMMOND, Charles, E.
发明人： YURKOVETSKIY, Aleksandr , YIN, Mao , LOWINGER, Timothy, B. , CABRAL, Carolina, B. , STEVENSON, Cheri, A. , HAMMOND, Charles, E.
IPC分类号： C08L59/00 , C07D401/00 , A61K31/785 , A61K47/48
CPC分类号： C08L59/00 , A61K47/59 , A61K48/0041 , C12N15/111 , C12N2310/11 , C12N2310/12 , C12N2310/14 , C12N2320/32
摘要： A polynucleotide delivery vehicle comprising a modified polymer is provided herein, the modified polymer having the following formula (I) in which W 1, W 2, W 3, W 4 , W 5 , W 6 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 , Z 9 , R 1 , R 2 , R 3 , R 4 , R 5 , n 1 , n 2 , n 3 , n 4 , n 5 , and n 6 are defined herein. Also disclosed are methods of delivering a polynucleotide to the cytoplasm of a selected tissue type or cell type and methods of reducing expression of a gene in a cell or a subject in need thereof with the modified polymer.
摘要翻译：本文提供了包含改性聚合物的多核苷酸递送载体，具有下式（I）的改性聚合物，其中W1，W2，W3，W4，W5，W6，Z1，Z2，Z3，Z4，Z5，Z9，R1， R2，R3，R4，R5，n1，n2，n3，n4，n5和n6定义如下。还公开了将多核苷酸递送至所选组织类型或细胞类型的细胞质的方法以及在有需要的细胞或受试者中用改性聚合物降低基因表达的方法。

8. 发明申请

WO2009073445A3 BIOCOMPATIBLE BIODEGRADABLE FUMAGILLIN ANALOG CONJUGATES 审中-公开
标题翻译：生物可降解的FUMAGILLIN模拟结合
公开(公告)号：WO2009073445A3
公开(公告)日：2010-01-28
申请号：PCT/US2008084539
申请日：2008-11-24
申请人： MERSANA THERAPEUTICS INC , AKULLIAN LAURA C , PETTER RUSSELL C , KANE JOHN J , HAMMOND CHARLES E , YIN MAO , YURKOVETSKIY ALEKSANDR , STEVENSON CHERI A
发明人： AKULLIAN LAURA C , PETTER RUSSELL C , KANE JOHN J , HAMMOND CHARLES E , YIN MAO , YURKOVETSKIY ALEKSANDR , STEVENSON CHERI A
IPC分类号： A61K47/48 , A61P35/00 , C07D303/22
CPC分类号： C07D303/40 , A61K47/59 , C07D303/18 , C07D303/22 , C07D303/36 , C07D405/14 , C07D487/08
摘要： Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog.
摘要翻译：烟曲霉素类似物聚合物共轭物，制备烟曲霉素类似物聚合物共轭物的方法，包含烟曲霉素类似物的聚合物缀合物的组合物，以及用于治疗癌症的方法或治疗血管发生疾病的方法，包括向有需要的受试者施用有效量的烟曲霉素类似物。还描述了新的烟曲霉素类似物，制备烟曲霉素类似物的方法，包含至少一种烟曲霉素类似物的组合物，以及用于治疗癌症的方法或治疗血管发生疾病，包括向有需要的受试者施用有效量的烟曲霉素类似物。

9. 发明申请

US20090199156A1 CONSTRAINT LANGUAGE EDITING FOR GENERATING MODEL-RELATED CONSTRAINT EXPRESSIONS 有权
标题翻译：用于生成与模型相关的约束表达式的约束语言编辑
公开(公告)号：US20090199156A1
公开(公告)日：2009-08-06
申请号：US12362829
申请日：2009-01-30
申请人： Ying Li , Jing Luo , Jia Yin Mao , Jie Qiu
发明人： Ying Li , Jing Luo , Jia Yin Mao , Jie Qiu
IPC分类号： G06F9/44
CPC分类号： G06F8/427 , G06F8/35
摘要： A method and navigation helper for generating constraint language codes for navigation in a constraint language editor. The constraint language editor generates model/instance-related constraint expressions according to the loaded model/instance and related constraints. The navigation is a path implementing the constraints. The method includes parsing the loaded model/instance; calculating a possible association related to the element through the type of the navigation-related element in the model/instance; and calculating a possible navigation path according to the association. A method for generating constraint language codes in a constraint language editor and the constraint language editor includes loading the model/instance; loading constraint patterns for storing parameters and a constraint code template; invoking corresponding helpers, according to the types of parameters stored in the constraint patterns; and generating constraint codes according to the generated parameters and the constraint code template.
摘要翻译：一种用于在约束语言编辑器中生成用于导航的约束语言代码的方法和导航帮助器。约束语言编辑器根据加载的模型/实例和相关约束生成与模型/实例相关的约束表达式。导航是实现约束的路径。该方法包括解析加载的模型/实例; 通过模型/实例中的导航相关元素的类型计算与元素相关的可能关联; 以及根据所述关联来计算可能的导航路径。一种用于在约束语言编辑器中生成约束语言代码的方法，所述约束语言编辑器包括加载所述模型/实例; 加载用于存储参数的约束模式和约束代码模板; 根据存储在约束模式中的参数类型调用相应的助手; 并根据生成的参数和约束代码模板生成约束码。

10. 发明申请

US20080003177A1 Radioactive arsenic-containing compounds and their uses in the treatment of tumors 失效
标题翻译：放射性含砷化合物及其在肿瘤治疗中的应用
公开(公告)号：US20080003177A1
公开(公告)日：2008-01-03
申请号：US11881901
申请日：2007-07-30
申请人： Chun-Ying Huang , Ming-Shiuan Wu , Te-Wei Lee , Te-Jung Chen , Kwo-Ping Chang , Shyh-Yi Chyi , Yin-Mao Hsu , Kuo-Hsien Fan , Wei-Chuan Hsu , Ying-Kai Fu , Charng-Feng Kao , Shiang-Rong Chang , Chih-Hsien Chang
发明人： Chun-Ying Huang , Ming-Shiuan Wu , Te-Wei Lee , Te-Jung Chen , Kwo-Ping Chang , Shyh-Yi Chyi , Yin-Mao Hsu , Kuo-Hsien Fan , Wei-Chuan Hsu , Ying-Kai Fu , Charng-Feng Kao , Shiang-Rong Chang , Chih-Hsien Chang
IPC分类号： A61K51/02 , A61P35/00
CPC分类号： A61K51/02 , A61K41/009 , A61K51/121
摘要： This invention provides a process for producing a radioactive arsenic-containing compound, comprising the steps of: (i) subjecting an arsenic-containing compound to a neutron irradiation treatment, said arsenic-containing compound being selected from a group consisting of As2O3, As2S3, As2S2, and a combination thereof, such that the arsenic element contained in the arsenic-containing compound is converted to a radioactive arsenic isotope; and (ii) recovering the resultant product from step (i). This invention also provides a pharmaceutical composition comprising a therapeutically effective amount of the radioactive arsenic-containing compound and a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the treatment of tumors/cancers such as hematological malignancies and solid tumors.
摘要翻译：本发明提供了一种制备放射性含砷化合物的方法，包括以下步骤：（i）对含砷化合物进行中子照射处理，所述含砷化合物选自： 2 3 3 3 3 SUB>及其组合，使含砷化合物中所含的砷元素转化为放射性砷同位素; 和（ii）从步骤（i）中回收所得产物。本发明还提供包含治疗有效量的放射性含砷化合物和药学上可接受的载体的药物组合物。药物组合物可用于治疗肿瘤/癌症如血液恶性肿瘤和实体瘤。

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