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1. 发明申请

WO2012051581A3 INTESTINAL PEPTIDE TARGETING LIGANDS 审中-公开
标题翻译： INTESTINAL PEPTIDE TARGTING LIGANDS
公开(公告)号：WO2012051581A3
公开(公告)日：2014-04-03
申请号：PCT/US2011056449
申请日：2011-10-14
申请人： UNIV RUTGERS , SINKO PATRICK J , ZHANG XIAOPING , SZEKELY ZOLTAN
发明人： SINKO PATRICK J , ZHANG XIAOPING , SZEKELY ZOLTAN
IPC分类号： C07K4/00 , C07K7/00
CPC分类号： C07K7/08 , A61K38/08 , A61K45/06 , A61K47/60 , A61K47/62 , A61K47/6925 , C07K7/06
摘要： Peptide ligands for transporting therapeutic agents across the intestinal epithelial barrier that ordinarily are inadequately absorbed and must be delivered by alternative means, which contain an isolated amino acid sequence wherein at least one pair of amino acids are of an opposite charge and the pair members are separated by a spacer of 1-12 amino acid residues including at least one hydrophobic amino acid, and wherein the length of the amino acid sequence is greater than 5 and less than 20 amino acids. Pharmaceutical compositions for gastro-intestinal delivery and methods for the gastrointestinal delivery of poorly absorbed therapeutic agents are also disclosed.
摘要翻译：通过肠上皮屏障传递治疗剂的肽配体，其通常未被充分吸收并且必须通过替代手段递送，其中所述替代方法含有分离的氨基酸序列，其中至少一对氨基酸具有相反电荷，并且所述成对体被分离通过包含至少一个疏水性氨基酸的1-12个氨基酸残基的间隔区，并且其中氨基酸序列的长度大于5个且小于20个氨基酸。还公开了用于胃肠输送的药物组合物和用于胃肠递送不良吸收的治疗剂的方法。

2. 发明申请

WO2010107831A8 NANOCARRIER COMPOSITIONS AND METHODS 审中-公开
标题翻译： NANOCARRIER组合物和方法
公开(公告)号：WO2010107831A8
公开(公告)日：2011-05-19
申请号：PCT/US2010027532
申请日：2010-03-16
申请人： UNIV RUTGERS , SINKO PATRICK J , STEIN STANLEY , GUNASEELAN SIMI , POOYAN SHAHRIAR , PALOMBO MATTHEW SEAN , ZHANG XIAOPING
发明人： SINKO PATRICK J , STEIN STANLEY , GUNASEELAN SIMI , POOYAN SHAHRIAR , PALOMBO MATTHEW SEAN , ZHANG XIAOPING
IPC分类号： A61K47/42
CPC分类号： A61K47/42 , A61K9/5169
摘要： This invention provides multimeric nanocarrier for in vivo delivery of a bioactive agent, comprising at least two peptide monomers reversibly or irreversibly linked with one or more of said bioactive agents, wherein said two or more of said peptide monomers are covalently linked by a biodegradable difunctional moiety, as well as methods of using this nanocarrier.
摘要翻译：本发明提供了用于体内递送生物活性剂的多聚体纳米载体，其包含与一种或多种所述生物活性剂可逆地或不可逆地连接的至少两种肽单体，其中所述两种或多种所述肽单体通过可生物降解的双官能部分共价连接，以及使用该纳米载体的方法。

3. 发明申请

WO2006089156A3 DRUG-POLYMER CONJUGATES COUPLED TO A PEPTIDIC CARRIER 审中-公开
标题翻译：与聚合物载体相结合的药物聚合物
公开(公告)号：WO2006089156A3
公开(公告)日：2009-04-16
申请号：PCT/US2006005729
申请日：2006-02-16
申请人： UNIV RUTGERS , SINKO PATRICK J , STEIN STANLEY , GUNASEELAN SIMI , POOYAN SHAHRIAR , WAN LI
发明人： SINKO PATRICK J , STEIN STANLEY , GUNASEELAN SIMI , POOYAN SHAHRIAR , WAN LI
IPC分类号： A61K38/00
CPC分类号： A61K47/64 , A61K47/60
摘要： Monodisperse macromolecular conjugate compositions of a peptidic carrier irreversibly or reversibly conjugated with one or more effectors and one or more therapeutic agents, wherein at least one effector or therapeutic agent is attached to a pendant reactive group on said peptidic carrier via a water-soluble polymer. Monodispersity is obtained through the use of orthogonal and separate conjugation reactions.
摘要翻译：肽载体的单分散大分子缀合物组合物与一种或多种效应物和一种或多种治疗剂不可逆地或可逆地缀合，其中至少一种效应物或治疗剂通过水溶性聚合物连接到所述肽载体上的侧链反应性基团上。通过使用正交和分离的共轭反应获得单分散性。

4. 发明申请

WO2006069344A3 CONTROLLED RELEASE HYDROGELS 审中-公开
标题翻译：控制释放水凝胶
公开(公告)号：WO2006069344A3
公开(公告)日：2006-08-10
申请号：PCT/US2005046891
申请日：2005-12-22
申请人： UNIV RUTGERS , SINKO PATRICK J , STEIN STANLEY , LALLOO ANITA
发明人： SINKO PATRICK J , STEIN STANLEY , LALLOO ANITA
IPC分类号： A61K9/127 , A61K9/14
CPC分类号： A61K9/127 , A61K9/0019 , A61K9/0024 , A61K31/4745 , A61K47/34
摘要： Formulations and methods for their preparation including a hydrogel including a crosslinked matrix comprising a polymer, and a one or more liposomes containing a therapeutic agent.
摘要翻译：用于其制备的制剂和方法包括含有包含聚合物的交联基质和含有治疗剂的一种或多种脂质体的水凝胶。

5. 发明申请

WO2009123768A3 NANOCARRIER AND NANOGEL COMPOSITIONS 审中-公开
标题翻译：纳米胶和纳米胶组合物
公开(公告)号：WO2009123768A3
公开(公告)日：2009-12-03
申请号：PCT/US2009002164
申请日：2009-04-06
申请人： UNIV RUTGERS , SINKO PATRICK J , STEIN STANLEY , KUTSCHER HILLIARD , DESHMUKH MANJEET , MENJOGE ANUPA , SINGH YASHVEER
发明人： SINKO PATRICK J , STEIN STANLEY , KUTSCHER HILLIARD , DESHMUKH MANJEET , MENJOGE ANUPA , SINGH YASHVEER
IPC分类号： A61K9/16
CPC分类号： A61K9/06 , A61K9/10 , A61K9/14 , A61K9/1641 , A61K9/48 , A61K9/51 , A61K31/704 , A61K47/10 , A61K47/51 , A61K47/56 , A61K47/60 , A61K47/64 , A61K47/6925 , A61K49/003 , A61K49/0043 , A61K49/0054 , Y10T428/2982
摘要： Novel classes of multi-arm polyalkylene oxide-based materials including PEG nanocarriers, nanogel particles, and aggregated nanogel particles are disclosed. These classes of compositions may be associated with therapeutic agents and targeting moieties, or visibility enhancing agents, and may have a modified surface structure. In some embodiments the PEG-based materials can be made to provide relatively high drug loads with improved solubility and targeted delivery.
摘要翻译：公开了新型的多臂聚环氧烷基材料，包括PEG纳米载体，纳米凝胶颗粒和聚集的纳米凝胶颗粒。这些类型的组合物可以与治疗剂和靶向部分或可见性增强剂相关联，并且可以具有改性的表面结构。在一些实施方案中，可以制备基于PEG的材料以提供具有改善的溶解度和靶向递送的相对高的药物负载。

6. 发明申请

WO0210746A2 PHARMACOKINETIC TOOL AND METHOD FOR PREDICTING METABOLISM OF A COMPOUND IN A MAMMAL 审中-公开
标题翻译：药物动力学工具和用于预测化合物在代谢中的代谢的方法
公开(公告)号：WO0210746A2
公开(公告)日：2002-02-07
申请号：PCT/US0123867
申请日：2001-07-30
申请人： LION BIOSCIENCE AG , LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , HOLME KEVIN , IZHIKEVICH TATYANA , DOERR STEVENS JULIE , LECLUYSE EDWARD , THAKKER DHIREN R , GRASS GEORGE M
发明人： LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , HOLME KEVIN , IZHIKEVICH TATYANA , DOERR-STEVENS JULIE , LECLUYSE EDWARD , THAKKER DHIREN R , GRASS GEORGE M
IPC分类号： G01N33/15 , C12Q1/02 , G06F19/00 , G01N33/48
CPC分类号： G06F19/704 , G16H10/40 , G16H50/50
摘要： A system for simulating metabolism of a compound in a mammal is disclosed that includes a metabolism simulation model of a mammalian liver. This model has equations which when executed on a computer, calculate the rate of metabolism of the compound in the cells of the mammalian liver and a rate of transport of the compound into the cells, wherein the simulation model determines an amount of the metabolism product. The rate of metabolism may be a rate of depletion of the compound. The metabolism product may be an amount of the compound remaining after the compound's first passage through the mammalian liver (This is not necessarily limited to first pass, nor would it need to be limited to the liver. Intestinal metabolism could also be modeled). The rate of metabolism may alternatively be a rate of accumulation of a metabolite of the compound.
摘要翻译：公开了一种用于模拟哺乳动物中化合物代谢的系统，其包括哺乳动物肝脏的代谢模拟模型。该模型具有在计算机上执行时计算化合物在哺乳动物肝细胞中的代谢速率和化合物进入细胞的速率的方程式，其中模拟模型确定新陈代谢产物的量。代谢速率可能是化合物的消耗速率。代谢产物可以是化合物首次通过哺乳动物肝脏后残留的化合物的量（这不一定限于第一次通过，也不需要限于肝脏，也可以建模肠代谢）。代谢速率可以是化合物代谢物的积累速率。

7. 发明申请

WO0015178A2 PHARMACOKINETIC-BASED DRUG DESIGN TOOL AND METHOD 审中-公开
标题翻译：基于药物动力学的药物设计工具和方法
公开(公告)号：WO0015178A2
公开(公告)日：2000-03-23
申请号：PCT/US9921001
申请日：1999-09-14
申请人： NAVICYTE INC , GRASS GEORGE M , LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , WEHRLI JOHN E
发明人： GRASS GEORGE M , LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , WEHRLI JOHN E
IPC分类号： G01N33/50 , A01N37/18 , A01N43/04 , A01N61/00 , A61K20060101 , A61K31/522 , A61P31/12 , C07B61/00 , C07B63/00 , C12M1/00 , C12M3/00 , C12Q1/00 , G01N15/00 , G01N31/00 , G01N33/15 , G01N33/48 , G01N33/53 , G01N33/543 , G06F9/455 , G06F17/30 , G06F17/50 , G06F19/00 , G06G7/60 , G06N3/00 , G06N7/00 , A61K
CPC分类号： C40B30/02 , C40B50/02 , Y02A90/26
摘要： The present invention relates to a pharmacokinetic-based design and selection tool (PK tool) and methods for predicting absoption of an administered compound of interest. The methods utilize the tools, and optionally a separately operable component or subsystem thereof. The PK tool includes as computer-readable components: (1) input/output system; (2) physiologic-based simulation model of one or more segments of a mammalian system of interest having one or more physiological barriers to absorption that is based on the selected route of administration; and (3) simulation engine having a differential equation solver. The invention also provides methods for optimizing as well as enabling minimal input requirements a physiologic-based simulation model for predicting in vivo absorption, and optionally one or more additional properties, from either in vitro or in vivo data. The PK tool of the invention may be provided as a computer system, as an article of manufacture in the form of a computer-readable medium, or a computer program product and the like. Subsystems and individual components of the PK tool also can be utilized and adapted in a variety of disparate applications for predicting the fate of an administered compound. The PK tool and methods of the invention can be used to screen and design compound libraries, select and design drugs, as well as predict drug efficacy in mammals from in vitro and/or in vivo data of one or more compounds of interest. The PK tool and methods of the invention also find use in selecting, designing, and preparing drug compounds, and multi-compound drugs and drug formulations (i.e., drug delivery system) for preparation of medicaments for use in treating mammalian disorders.
摘要翻译：本发明涉及基于药代动力学的设计和选择工具（PK工具）以及用于预测所施用化合物的吸收的方法。该方法利用工具，以及可选的单独可操作的组件或子系统。 PK工具包括计算机可读组件：（1）输入/输出系统; （2）基于所选择的给药途径的具有一种或多种吸收生理屏障的哺乳动物系统的一个或多个区段的基于生理学的模拟模型; 和（3）具有微分方程求解器的模拟引擎。本发明还提供用于优化的方法以及实现最小输入需求，用于从体外或体内数据预测体内吸收以及任选的一种或多种另外的性质的生理学模拟模型。本发明的PK工具可以作为计算机系统提供，作为计算机可读介质或计算机程序产品等形式的制品。 PK工具的子系统和各个组分也可以用于各种不同的应用中并用于预测给药化合物的命运。本发明的PK工具和方法可用于筛选和设计化合物库，选择和设计药物，以及从一种或多种感兴趣的化合物的体外和/或体内数据预测哺乳动物的药物功效。本发明的PK工具和方法还可用于选择，设计和制备药物化合物，以及用于制备用于治疗哺乳动物疾病的药物的多重复合药物和药物制剂（即药物递送系统）。

8. 发明申请

WO0210741A3 REGIONAL INTESTINAL PERMEABILITY MODEL 审中-公开
标题翻译：区域内渗透性模型
公开(公告)号：WO0210741A3
公开(公告)日：2003-09-04
申请号：PCT/US0123762
申请日：2001-07-30
申请人： LION BIOSCIENCE AG , GRASS GEORGE M , LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , ATHWAL JEHANGIR , SAGE CARLETON , BREMER TROY , HOLME KEVIN , YONG LEE , LEE KYOUNG
发明人： GRASS GEORGE M , LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , ATHWAL JEHANGIR , SAGE CARLETON , BREMER TROY , HOLME KEVIN , YONG LEE , LEE KYOUNG
IPC分类号： C12Q1/02 , G01N33/483 , G06F19/00
CPC分类号： G06F19/704 , G06F19/707 , G16H10/40 , G16H50/50
摘要： Permeability models and methods for creating the models are disclosed. The models include receiving as an input in vitro permeability and structure data for a particular compound. Then the data is mapped to at least one permeability. In some models the data is, mapped to a plurality of permeabilities, each associated with a specific region in a mammalian GI tract. Some models may take into consideration solubility, permeability and at least one molecular descriptor associated with the compound of interest.
摘要翻译：披露了渗透性模型和创建模型的方法。这些模型包括作为特定化合物的体外渗透性和结构数据的输入。然后将数据映射到至少一个磁导率。在一些模型中，数据被映射到多个渗透性，每个渗透性与哺乳动物胃肠道中的特定区域相关联。一些模型可以考虑溶解度，渗透性和与感兴趣的化合物相关联的至少一个分子描述符。

9. 发明申请

WO0015178A9 COMPUTER IMPLEMENTED PHARMACOKINETICS METHOD AND PROGRAM 审中-公开
标题翻译：计算机实现药物动力学方法和程序
公开(公告)号：WO0015178A9
公开(公告)日：2001-10-04
申请号：PCT/US9921001
申请日：1999-09-14
申请人： NAVICYTE INC , GRASS GEORGE M , LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , WEHRLI JOHN E
发明人： GRASS GEORGE M , LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , WEHRLI JOHN E
IPC分类号： G01N33/50 , A01N37/18 , A01N43/04 , A01N61/00 , A61K20060101 , A61K31/522 , A61P31/12 , C07B61/00 , C07B63/00 , C12M1/00 , C12M3/00 , C12Q1/00 , G01N15/00 , G01N31/00 , G01N33/15 , G01N33/48 , G01N33/53 , G01N33/543 , G06F9/455 , G06F17/30 , G06F17/50 , G06F19/00 , G06G7/60 , G06N3/00 , G06N7/00
CPC分类号： C40B30/02 , C40B50/02 , Y02A90/26
摘要： The present invention relates to a pharmacokinetic-based design and selection tool (PK tool) and methods for predicting absoption of an administered compound of interest. The methods utilize the tools, and optionally a separately operable component or subsystem thereof. The PK tool includes as computer-readable components: (1) input/output system; (2) physiologic-based simulation model of one or more segments of a mammalian system of interest having one or more physiological barriers to absorption that is based on the selected route of administration; and (3) simulation engine having a differential equation solver. The invention also provides methods for optimizing as well as enabling minimal input requirements a physiologic-based simulation model for predicting in vivo absorption, and optionally one or more additional properties, from either in vitro or in vivo data. The PK tool of the invention may be provided as a computer system, as an article of manufacture in the form of a computer-readable medium, or a computer program product and the like. Subsystems and individual components of the PK tool also can be utilized and adapted in a variety of disparate applications for predicting the fate of an administered compound. The PK tool and methods of the invention can be used to screen and design compound libraries, select and design drugs, as well as predict drug efficacy in mammals from in vitro and/or in vivo data of one or more compounds of interest. The PK tool and methods of the invention also find use in selecting, designing, and preparing drug compounds, and multi-compound drugs and drug formulations (i.e., drug delivery system) for preparation of medicaments for use in treating mammalian disorders.
摘要翻译：本发明涉及基于药代动力学的设计和选择工具（PK工具）和用于预测目标化合物的吸收的方法。这些方法利用工具，以及可选的单独可操作的组件或子系统。 PK工具包括计算机可读组件：（1）输入/输出系统; （2）基于所选择的给药途径的具有一种或多种吸收生理屏障的哺乳动物感兴趣系统的一个或多个区段的基于生理学的模拟模型; 和（3）具有微分方程求解器的模拟引擎。本发明还提供用于优化的方法以及使得能够最小化输入需求用于从体外或体内数据预测体内吸收以及任选的一种或多种另外的性质的基于生理学的模拟模型。本发明的PK工具可以作为计算机系统提供，作为计算机可读介质或计算机程序产品等形式的制品。 PK工具的子系统和各个组分也可用于各种不同的应用中，用于预测给药化合物的命运。本发明的PK工具和方法可用于筛选和设计化合物库，选择和设计药物，以及从一种或多种感兴趣的化合物的体外和/或体内数据预测哺乳动物的药物功效。本发明的PK工具和方法还可用于选择，设计和制备用于制备用于治疗哺乳动物疾病的药物的药物化合物和多重复合药物和药物制剂（即药物递送系统）。

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