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1. 发明申请

WO2011103552A9 AMP DERIVATIVES FOR TREATING CARDIAC DISEASES 审中-公开
标题翻译：用于治疗心脏病的AMP衍生物
公开(公告)号：WO2011103552A9
公开(公告)日：2012-04-26
申请号：PCT/US2011025680
申请日：2011-02-22
申请人： UNIV CONNECTICUT , US HEALTH , LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V , KUMAR THATIKONDA SANTHOSH
发明人： LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V , KUMAR THATIKONDA SANTHOSH
IPC分类号： C07F9/6561 , A61K31/675 , A61P9/04
CPC分类号： A61K31/675 , A61K31/683 , C07F9/65616
摘要： Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)- methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C-P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.
摘要翻译：描述了磷酸酯和膦酸盐的N-甲基钴胺衍生物，包括它们的前药类似物。含有（N） - 甲氰胺（二环[3.1.0]己烷）环体系的2-氯-AMP衍生物代替核糖的MRS2339激活P2X受体，配体门控离子通道。基于由于C-P键的稳定性增加体内半衰期的期望，使用Michaelis-Arbuzov和Wittig反应合成MRS2339的膦酸酯类似物。当通过小型渗透泵（Alzet）将其转运给小鼠（心力衰竭的遗传模型）时，一些类似物通过超声心动图来源的分数缩短（FS）评估，显着增加了体内完整的心脏收缩功能车辆输注小鼠。用于治疗心力衰竭的碳环核苷酸类似物的范围已经扩大。

2. 发明申请

WO2011103552A2 COMPOSITIONS AND METHODS TO TREAT CARDIAC DISEASES 审中-公开
标题翻译：组合物和治疗心脏病的方法
公开(公告)号：WO2011103552A2
公开(公告)日：2011-08-25
申请号：PCT/US2011025680
申请日：2011-02-22
申请人： UNIV CONNECTICUT , US HEALTH , LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V
发明人： LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V
IPC分类号： C07F9/6561
CPC分类号： A61K31/675 , A61K31/683 , C07F9/65616
摘要： Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)- methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C-P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.
摘要翻译：描述了膦酸盐和次膦酸盐，其包括其前体药物类似物的N-甲基碳酰胺衍生物。含有（N） - 甲氰胺（双环[3.1.0]己烷）环系的2-氯-AMP衍生物MRS2339代替核糖，活化P2X受体，配体门控离子通道。基于由于C-P键的稳定性而增加的体内半衰期的期望，使用Michaelis-Arbuzov和Wittig反应合成MRS2339的膦酸酯类似物。当通过小型渗透泵（Alzet）将氯雷斯特林过度表达的小鼠（心力衰竭的遗传模型）施用时，一些类似物显着增加体内完整的心脏收缩功能，如通过超声心动图来源的分数缩短（FS）评估的，与车辆输注小鼠。用于治疗心力衰竭的碳环核苷酸类似物的范围已经扩大。

3. 发明申请

WO2011063156A2 ACID SALT FORMS OF POLYMER-DRUG CONJUGATES AND ALKOXYLATION METHODS 审中-公开
标题翻译：聚合物 - 药物共轭物的酸盐形式和烷氧基化方法
公开(公告)号：WO2011063156A2
公开(公告)日：2011-05-26
申请号：PCT/US2010057289
申请日：2010-11-18
申请人： NEKTAR THERAPEUTICS , CHONG ANTHONY O , LEE SEOJU , JOSHI BHALCHANDRA V , BRAY BRIAN , NIE SHAOYONG , SPENCE PATRICK , KOZLOWSKI ANTONI , MCMANUS SAMUEL , TIPNIS SACHIN , LAVATY GREG , SWALLOW DAVID
发明人： CHONG ANTHONY O , LEE SEOJU , JOSHI BHALCHANDRA V , BRAY BRIAN , NIE SHAOYONG , SPENCE PATRICK , KOZLOWSKI ANTONI , MCMANUS SAMUEL , TIPNIS SACHIN , LAVATY GREG , SWALLOW DAVID
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： C08G65/331 , A61K31/4745 , A61K47/60 , C07C51/412 , C07C53/18 , C07D491/22 , C08G65/329 , C08G65/33396 , C08G65/48 , C08L2203/02
摘要： Among other aspects, provided herein is a mixed-acid salt of a water-soluble polymer-drug conjugate, along with related methods of making and using the same. The mixed-sail acid salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding predominantly pure acid salt or free base forms of the polymer-drug conjugate. The mixed acid salt is reproducibly prepared and recovered, and provides surprising advantages over non-mixed acid salt forms of the water-soluble polymer drug conjugate.
摘要翻译：在其他方面中，本文提供了水溶性聚合物 - 药物缀合物的混合酸盐以及制备和使用它们的相关方法。混合帆酸盐是稳定形成的，并且似乎比聚合物 - 药物缀合物的相应主要纯酸盐或游离碱形式更耐水解降解。混合酸盐可重现地制备和回收，并且与非混合酸盐形式的水溶性聚合物药物缀合物相比，提供了令人惊讶的优点。

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