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1. 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。

2. 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。

3. 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。

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

WO9847913A3 INHIBITION OF HIV-1 REPLICATION BY A TAT RNA-BINDING DOMAIN PEPTIDE ANALOG 审中-公开
标题翻译：通过TAT RNA结合域抑制HIV-1复制模型
公开(公告)号：WO9847913A3
公开(公告)日：1999-01-21
申请号：PCT/US9807533
申请日：1998-04-16
申请人： UNIV NEW JERSEY MED , WANG JIHONG , STEIN STANLEY , LEIBOWITZ MICHAEL J , RABSON ARNOLD B
发明人： WANG JIHONG , STEIN STANLEY , LEIBOWITZ MICHAEL J , RABSON ARNOLD B
IPC分类号： A61K38/00 , C07K14/16 , C07K7/00
CPC分类号： C07K14/005 , A61K38/00 , C12N2740/16322
摘要： The peptidic compounds, R-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-X-(biotin)-NH2 wherein R is the residue of a carboxylic acid and X is a cysteine or lysine residue, analogs thereof, and the biologically and pharmaceutically acceptable salts thereof, contain the 9-amino acid sequence from the basic domain of the Tat protein responsible for specific interaction with TAR RNA, or an analog thereof. The cysteine or lysine residue provides an attachment site for biotin which acts as a cellular uptake enhancer. These peptides bind a fragment of TAR RNA (ΔTAR) avidly and specifically, as measured in an electrophoretic gel shift assay. Further, they inhibit tat gene-induced expression of a stably transfected CAT (chloramphenicol acety transferase) reporter gene linked to the HIV-1 LTR in a model cell assay, but do not inhibit phorbol ester-induced expression of CAT, thereby demonstrating a Tat-dependent mechanism of inhibition. Inhibition of HIV-1 replication after acute infection of MT2 cells was demonstrated by absence of HIV-induced syncytium formation and cytotoxicity, as well as by suppression of reverse transcriptase production. These results indicate that these peptides are capable of competing with the TAR RNA-binding domain of Tat protein and thus are useful as therapeutic agents in the treatment of AIDS.

6. 发明申请

WO03018609A3 APPLICATION OF PEPTIDE CONJUGATES TO ALZHEIMER'S DISEASE 审中-公开
标题翻译：肽共轭物在阿尔茨海默病中的应用
公开(公告)号：WO03018609A3
公开(公告)日：2003-10-16
申请号：PCT/US0226889
申请日：2002-08-23
申请人： STEIN STANLEY
发明人： STEIN STANLEY
IPC分类号： A61K38/08 , A61K47/48 , G01N33/68 , A61K51/00
CPC分类号： G01N33/6896 , A61K38/08 , A61K47/64 , G01N2800/2821
摘要： A chemical compound and a method for its use in the diagnosis and treatment of Alzheimer's disease in which the at least the sequence of the D-isomers of the amino acids (phenylalanine-phenylalanine-valine-leucine-lysine) is capable of crossing the blood brain barrier, recognizing the formation of plaques characteristic of the pathogenesis of Alzheimer's disease, and intefering with the formation of fibril from beta amyloid peptide effecting an inhibition of the disease process.
摘要翻译：一种化合物及其用于诊断和治疗阿尔茨海默氏病的方法，其中氨基酸（苯丙氨酸 - 苯丙氨酸 - 缬氨酸 - 亮氨酸 - 赖氨酸）的D-异构体的至少一个序列能够穿过血液识别阿尔茨海默氏病发病机理特征性斑块的形成，以及从β-淀粉样肽形成纤维形成影响疾病过程的抑制。

7. 发明申请

WO2007047967A3 DETOXIFICATION DEPOT FOR ALZHEIMER'S DISEASE 审中-公开
标题翻译：脱氧核糖核酸阿尔茨海默病
公开(公告)号：WO2007047967A3
公开(公告)日：2007-11-29
申请号：PCT/US2006041110
申请日：2006-10-20
申请人： SENICURE LLC , STEIN STANLEY , SUNDARAM PAZHANI , KASINATHAN CHINNASWAMY
发明人： STEIN STANLEY , SUNDARAM PAZHANI , KASINATHAN CHINNASWAMY
IPC分类号： A61K39/395
CPC分类号： C07K14/4711 , A61K9/0024 , A61K38/08 , A61K47/665 , A61K47/6903 , B82Y5/00
摘要： The invention is directed to a device that is placed inside an Alzheimer's disease (AD) patient for the purpose of extracting and accumulating neurotoxic beta-amyloid peptides (nt-bAP) from body fluids. AD is the consequence of a process in which nt-bAP aggregates to form fibrils and plaques which can cause nerve damage. Since nt-bAP can cross the blood-brain barrier (BBB), the concentration in the central nervous system and in the periphery are in equilibrium. By sequestering nt-bAP, our device will act as a "sink." It should draw nt-bAP across the BBB, reducing the concentration of soluble nt- bAP in the brain, thereby halting or slowing plaque deposition in the brain. Since plaques and possibly soluble, aggregated nt-bAP are the cause of nerve damage in AD, this process should be therapeutically effective. The device can be a depot containing a fragment of nt-bAP which intrinsically retains the ability to bind but not to be toxic.
摘要翻译：本发明涉及放置在阿尔茨海默氏病（AD）患者体内的装置，用于从体液中提取和积累神经毒性β-淀粉样肽（nt-bAP）。 AD是nt-bAP聚集形成可引起神经损伤的原纤维和斑块的过程的结果。由于nt-bAP可以穿过血脑屏障（BBB），因此中枢神经系统和外周的浓度处于平衡状态。通过隔离nt-bAP，我们的设备将充当“接收器”。它应该通过BBB吸取nt-bAP，减少大脑中可溶性nt-bAP的浓度，从而阻止或减缓大脑中的斑块沉积。由于斑块和可能的可溶性聚集的nt-bAP是AD中神经损伤的原因，所以该过程应该是治疗有效的。该装置可以是含有nt-bAP片段的仓库，其本质上保留了结合但不具有毒性的能力。

8. 发明申请

WO0197865A3 MULTIPLE PHASE CROSS-LINKED COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：多相交联组合物及其用途
公开(公告)号：WO0197865A3
公开(公告)日：2003-03-27
申请号：PCT/US0119451
申请日：2001-06-19
申请人： UNIV NEW JERSEY MED , STEIN STANLEY , QIU BO
发明人： STEIN STANLEY , QIU BO
IPC分类号： A61K9/00 , A61K9/66 , A61K47/34
CPC分类号： A61K9/0024 , A61K47/34
摘要： The present invention is directed to pharmaceutical compositions, and method for preparing pharmaceutical compositions, comprising a cross-linked matrix physically entrapping at least one therapeutic agent. The matrix may comprise one or more phases in addition to an aqueous phase, such as a solid and/or oil phase. The matrix of the invention has at least one controlled release in-vivo kinetic profile, and may have additional profiles for the same agent. The matrix may also comprise more than one therapeutic agent, and each additional therapeutic agent may have one or more controlled release in-vivo kinetic profile.
摘要翻译：本发明涉及药物组合物和制备药物组合物的方法，其包含物理捕获至少一种治疗剂的交联基质。除水相外，基质还可以包含一个或多个相，例如固相和/或油相。本发明的基质具有至少一个受控释放的体内动力学特征，并且可以具有用于相同试剂的附加特征。所述基质还可包含多于一种治疗剂，并且每种其它治疗剂可具有一种或多种受控释放的体内动力学特征。

9. 发明申请

WO0107013A9 THIOAMIDE MOIETY-CONTAINING POLYMER DRUG CONJUGATES 审中-公开
标题翻译：含有酰胺的含MOIETY聚合物药物的药物
公开(公告)号：WO0107013A9
公开(公告)日：2002-11-14
申请号：PCT/US0020090
申请日：2000-07-24
申请人： UNIV NEW JERSEY MED , STEIN STANLEY , ZHANG GUOBAO , QIU BO
发明人： STEIN STANLEY , ZHANG GUOBAO , QIU BO
IPC分类号： A61K47/48
CPC分类号： A61K47/60
摘要： This invention pertains to disulfide-linked conjugates of therapeutic agents containing at least one thioamide group with polymer comprising at least one thiol group, so as to provide a controlled release pharmaceutical composition for administration to animals for the prophylaxis or treatment of various conditions or diseases. The therapeutic agent conjugate may comprise an inactive or weakly active prodrug form which may be converted into the original therapeutic compound by the natural action of reducing agents in vivo . The composition may comprise a mixture of polymers each with a different thioamide-containing agent attached, or a polymer conjugated with a mixture of thioamide-containing agents. Modified properties of the therapeutic compound potentially provided by the polymer itself, as well as by other compounds also appended to the polymer, include but are not limited to greater water solubility, longer in vivo half-life (due to larger size of the conjugate), slower release from a sustained-release depot (due to larger size of the conjugate), better oral bioavailability and tissue-specific targeting.
摘要翻译：本发明涉及含有至少一种硫代酰胺基团的治疗剂与包含至少一种硫醇基团的聚合物的二硫键连接的缀合物，以提供用于预防或治疗各种病症或疾病的用于给予动物的控释药物组合物。治疗剂缀合物可以包含无活性或弱活性的前药形式，其可以通过体内还原剂的天然作用转化为原始治疗化合物。组合物可以包含各自与不同含硫代酰胺的试剂连接的聚合物的混合物，或与含硫代酰胺的试剂的混合物缀合的聚合物。由聚合物本身可能提供的治疗化合物以及也附加到聚合物上的其它化合物的治疗化合物的改进性质包括但不限于更大的水溶性，更长的体内半衰期（由于缀合物的较大尺寸）缓释片段缓慢释放（由于缀合物尺寸较大），更好的口服生物利用度和组织特异性靶向。

10. 发明申请

WO0107013A2 MATERIALS AND PROCESSES FOR CONTROLLED RELEASE OF THIOAMIDE MOIETY-CONTAINING THERAPEUTIC AGENTS BY LINKING TO THIOL-CONTAINING POLYMERS 审中-公开
标题翻译：通过连接含THIOL的聚合物控制释放含有硫氧化物的含药物治疗药物的材料和方法
公开(公告)号：WO0107013A2
公开(公告)日：2001-02-01
申请号：PCT/US0020090
申请日：2000-07-24
申请人： UNIV NEW JERSEY MED , STEIN STANLEY , ZHANG GUOBAO , QIU BO
发明人： STEIN STANLEY , ZHANG GUOBAO , QIU BO
IPC分类号： A61K47/48 , A61K9/00
CPC分类号： A61K47/60
摘要： This invention pertains to disulfide-linked conjugates of therapeutic agents containing at least one thioamide group with polymer comprising at least one thiol group, so as to provide a controlled release pharmaceutical composition for administration to animals for the prophylaxis or treatment of various conditions or diseases. The therapeutic agent conjugate may comprise an inactive or weakly active prodrug form which may be converted into the original therapeutic compound by the natural action of reducing agents in vivo . The composition may comprise a mixture of polymers each with a different thioamide-containing agent attached, or a polymer conjugated with a mixture of thioamide-containing agents. Modified properties of the therapeutic compound potentially provided by the polymer itself, as well as by other compounds also appended to the polymer, include but are not limited to greater water solubility, longer in vivo half-life (due to larger size of the conjugate), slower release from a sustained-release depot (due to larger size of the conjugate), better oral bioavailability and tissue-specific targeting.
摘要翻译：本发明涉及含有至少一种硫代酰胺基团的治疗剂与包含至少一种硫醇基团的聚合物的二硫键连接的缀合物，以提供用于预防或治疗各种病症或疾病的用于给予动物的控释药物组合物。治疗剂缀合物可以包含无活性或弱活性的前药形式，其可以通过体内还原剂的天然作用转化为原始治疗化合物。组合物可以包含各自与不同含硫代酰胺的试剂连接的聚合物的混合物，或与含硫代酰胺的试剂的混合物缀合的聚合物。由聚合物本身可能提供的治疗化合物以及也附加到聚合物上的其它化合物的治疗化合物的改进性质包括但不限于更大的水溶性，更长的体内半衰期（由于到更大尺寸的缀合物），缓释片段的缓慢释放（由于缀合物的较大尺寸），更好的口服生物利用度和组织特异性靶向。

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