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1. 发明申请

WO2004094671A2 METHODS AND PRODUCTS FOR IDENTIFICATION AND ASSESSMENT OF TLR LIGANDS 审中-公开
标题翻译： TLR配置的识别和评估方法和产品
公开(公告)号：WO2004094671A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/012788
申请日：2004-04-22
申请人： COLEY PHARMACEUTICAL GmbH , COLEY PHARMACEUTICAL GROUP, INC. , VOLLMER, Jörg , JURK, Marion , LIPFORD, Grayson, B. , SCHETTER, Christian , FORSBACH, Alexandra , KRIEG, Arthur, M.
发明人： VOLLMER, Jörg , JURK, Marion , LIPFORD, Grayson, B. , SCHETTER, Christian , FORSBACH, Alexandra , KRIEG, Arthur, M.
IPC分类号： C12Q1/68
CPC分类号： C07K14/705
摘要： The invention provides in part novel screening methods and compositions for identifying and distinguishing between candidate immunomodulatory compounds. The invention further provides methods for assessing biological activity of composition containing a known TLR ligand. These latter methods can be used for quality assessment and selection of various lots of test compositions, including pharmaceutical products for clinical use.
摘要翻译：本发明部分提供了用于鉴定和鉴别候选免疫调节化合物的新型筛选方法和组合物。本发明还提供了评估含有已知TLR配体的组合物的生物学活性的方法。这些后一种方法可用于各种批次的测试组合物的质量评估和选择，包括用于临床应用的药物产品。

2. 发明申请

WO2007062107A2 IMMUNOSTIMULATORY OLIGORIBONUCLEOTIDES 审中-公开
标题翻译：免疫抑制剂寡核苷酸
公开(公告)号：WO2007062107A2
公开(公告)日：2007-05-31
申请号：PCT/US2006/045183
申请日：2006-11-22
申请人： COLEY PHARMACEUTICAL GMBH , COLEY PHARMACEUTICAL GROUP, INC. , FORSBACH, Alexandra , VOLLMER, Joerg , LIPFORD, Grayson, B.
发明人： FORSBACH, Alexandra , VOLLMER, Joerg , LIPFORD, Grayson, B.
IPC分类号： C12N15/11 , A61K31/7105 , A61K9/127
CPC分类号： A61K39/39 , A61K31/7105 , A61K2039/55561 , C12N15/117 , C12N2310/17 , C12N2310/315
摘要： The invention provides immunostimulatory compositions and use of those compounds in the preparation of medicaments for the treatment of disease as well as in vitro uses. In particular, the compositions of the invention include immunostimulatory oligoribonucleotides that incorporate a sequence-dependent immunostimulatory sequence motif. Specific modifications involving phosphate linkages, nucleotide analogs, adducts, and combinations thereof are provided. Compositions of the invention, which optionally can include an antigen, can be used alone or together with other treatments to stimulate or enhance an immune response. Also provided are compositions and methods useful for treating a subject having an infection, a cancer, an allergic condition, asthma, airway remodeling, or immunodeficiency. Immnostimulatory oligoribonucleotides of the invention are believed to stimulate Toll-like receptor 8 (TLR8).
摘要翻译：本发明提供免疫刺激组合物和这些化合物在制备用于治疗疾病和体外用途的药物中的用途。特别地，本发明的组合物包括掺入序列依赖性免疫刺激序列基序的免疫刺激性寡核糖核苷酸。提供涉及磷酸键，核苷酸类似物，加合物及其组合的具体修饰。任选地可以包括抗原的本发明的组合物可以单独使用或与其它治疗一起使用以刺激或增强免疫应答。还提供了可用于治疗患有感染，癌症，过敏性疾病，哮喘，气道重塑或免疫缺陷的受试者的组合物和方法。据信本发明的无刺激性寡核糖核苷酸刺激Toll样受体8（TLR8）。

3. 发明申请

WO2005097993A2 IMMUNOSTIMULATORY VIRAL RNA OLIGONUCLEOTIDES 审中-公开
标题翻译：免疫原性病毒RNA寡核苷酸
公开(公告)号：WO2005097993A2
公开(公告)日：2005-10-20
申请号：PCT/US2005/005420
申请日：2005-02-18
申请人： COLEY PHARMACEUTICAL GROUP, INC. , COLEY PHARMACEUTICAL GMBH , LIPFORD, Grayson, B. , FORSBACH, Alexandra
发明人： LIPFORD, Grayson, B. , FORSBACH, Alexandra
IPC分类号： C12N15/11
CPC分类号： A61K39/39 , A61K2039/55561
摘要： Immunostimulatory sequence-specific RNA oligonucleotides corresponding to 3' terminal sequences of single-stranded minus-sense RNA genomic RNAs are provided. Also provided are compositions and methods relating to an immunostimulatory 4-mer RNA motif provided as 5'-C/U-U-G/U-U-3'. Incorporation of this short RNA motif is sufficient to confer new and altered immunostimulatory properties in new and existing oligonucleotides, including CpG oligodeoxynucleotides. Also provided are methods for use of the immunostimulatory RNA oligonucleotides and DNA:RNA chimeric oligonucleotides of the invention to induce an immune response in vitro and in vivo, as well as to treat allergy, asthma, infection, and cancer in a subject. Single-stranded oligoribonucleotides of the invention are believed to signal through a Toll-like receptor (TLR) chosen from TLR9, TLR8, TLR7, and TLR3. The oligoribonucleotides can also be used in a method to screen for TLR antagonists.
摘要翻译：提供了对应于单链负义RNA基因组RNA的3'末端序列的免疫刺激序列特异性RNA寡核苷酸。还提供了与作为5'-C / U-U-G-U-U-3'提供的免疫刺激性4聚体RNA基序有关的组合物和方法。引入这种短RNA基序足以在新的和现有的寡核苷酸（包括CpG寡脱氧核苷酸）中赋予新的和改变的免疫刺激性质。还提供了使用本发明的免疫刺激性RNA寡核苷酸和DNA：RNA嵌合寡核苷酸在体外和体内诱导免疫应答以及治疗受试者中的过敏，哮喘，感染和癌症的方法。据信本发明的单链寡核糖核苷酸通过选自TLR9，TLR8，TLR7和TLR3的Toll样受体（TLR）发出信号。寡核糖核苷酸也可用于筛选TLR拮抗剂的方法中。

4. 发明申请

WO2005007672A2 SMALL MOLECULE TOLL-LIKE RECEPTOR (TLR) ANTAGONISTS 审中-公开
标题翻译：小分子类似受体（TLR）拮抗剂
公开(公告)号：WO2005007672A2
公开(公告)日：2005-01-27
申请号：PCT/US2004/019714
申请日：2004-06-18
申请人： COLEY PHARMACEUTICAL GMBH , COLEY PHARMACEUTICAL GROUP, INC. , LIPFORD, Grayson, B. , FORSBACH, Alexandra , ZEPP, Charles, M.
发明人： LIPFORD, Grayson, B. , FORSBACH, Alexandra , ZEPP, Charles, M.
IPC分类号： C07K
CPC分类号： A61K31/437 , A61K31/122 , A61K31/382 , A61K31/4462 , A61K31/4709 , A61K31/496 , A61K31/517 , A61K31/5415 , A61K31/55 , A61K31/553 , C07D221/10 , C07D239/94 , C07D239/95 , C07D405/12
摘要： The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are 4-primary amino quinolines. Many of the compounds and methods are useful specifically for inhibiting immune stimulation involving at least one of TLR9, TLR8, TLR7, and TLR3. The methods may have use in the treatment of autoimmunity, inflammation, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.
摘要翻译：本发明提供了用于通过Toll样受体调节信号传导的方法和组合物。所述方法包括使TLR表达细胞与具有至少两个环的核心结构的小分子接触。某些化合物是4-伯氨基喹啉。许多化合物和方法专门用于抑制涉及TLR9，TLR8，TLR7和TLR3中的至少一种的免疫刺激。该方法可用于治疗自身免疫，炎症，过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。

5. 发明申请

WO2006080946A2 ABASIC OLIGONUCLEOTIDE AS CARRIER PLATFORM FOR ANTIGEN AND IMMUNOSTIMULATORY AGONIST AND ANTAGONIST 审中-公开
标题翻译：用于抗原和免疫增强剂和拮抗剂的载体寡核苷酸作为载体平台
公开(公告)号：WO2006080946A2
公开(公告)日：2006-08-03
申请号：PCT/US2005/020225
申请日：2005-06-08
申请人： COLEY PHARMACEUTICAL GMBH , LIPFORD, Grayson, B. , FORSBACH, Alexandra , UHLMANN, Eugen , WAGNER, Hermann
发明人： LIPFORD, Grayson, B. , FORSBACH, Alexandra , UHLMANN, Eugen , WAGNER, Hermann
CPC分类号： C07H21/00 , A61K39/0005 , A61K39/385 , A61K2039/6025 , A61K2039/6087 , A61K2039/6093 , A61K2300/00
摘要： Compositions and methods are provided for enhancing delivery of therapeutic agents. More specifically, compositions and methods are provided for improving antigen delivery to antigen-presenting cells. Conjugates between abasic oligonucleotides and antigen are provided, along with methods for their use in vaccination and in the treatment of cancer, infection, and allergy and asthma. Also provided are conjugates between abasic oligonucleotides and various immunostimulatory nucleic acids, including CpG oligonucleotides, as well as methods of use thereof. Also provided are conjugates between abasic oligonucleotides and various other agonists and antagonists of immunostimulation, as well as methods of use thereof.
摘要翻译：提供了用于增强治疗剂递送的组合物和方法。更具体地，提供了用于改善抗原递送细胞的抗原递送的组合物和方法。提供了无碱基寡核苷酸和抗原之间的结合物，以及它们用于疫苗接种和治疗癌症，感染和过敏和哮喘的方法。还提供了脱碱基寡核苷酸与各种免疫刺激核酸（包括CpG寡核苷酸）之间的缀合物，以及其使用方法。还提供了无碱基寡核苷酸与各种其它激动剂和免疫刺激拮抗剂之间的缀合物，以及其使用方法。

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