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1. 发明申请

WO2008138131A4 BONE TARGETED ALKALINE PHOSPHATASE, KITS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2008138131A4
公开(公告)日：2008-11-20
申请号：PCT/CA2008/000923
申请日：2008-05-12
申请人： ENOBIA PHARMA INC. , CRINE, Philippe , BOILEAU, Guy , LOISEL, Thomas, P. , LEMIRE, Isabelle , LEONARD, Pierre , HEFT, Robert , LANDY, Hal
发明人： CRINE, Philippe , BOILEAU, Guy , LOISEL, Thomas, P. , LEMIRE, Isabelle , LEONARD, Pierre , HEFT, Robert , LANDY, Hal
IPC分类号： C12N15/55 , A61K38/46 , A61P19/08 , C12N15/85 , C12N5/10 , C12N9/16
摘要： A bone targeted alkaline phosphatase comprising a polypeptide having the structure : Z-sALP-Y-spacer-X-W n -V, wherein sALP is the extracellular domain of the alkaline phosphatase; wherein V is absent or is an amino acid sequence of at least one amino acid; X is absent or is an amino acid sequence of at least one amino acid; Y is absent or is an amino acid sequence of at least one amino acid; Z is absent or is an amino acid sequence of at least one amino acid; and W n is a polyaspartate or a polyglutamate wherein n = 10 to 16. Kits and methods of use thereof.

2. 发明申请

WO2005103263A1 BONE DELIVERY CONJUGATES AND METHOD OF USING SAME TO TARGET PROTEINS TO BONE 审中-公开
标题翻译：骨递送缀合物及使用该方法将蛋白质靶向骨骼的方法
公开(公告)号：WO2005103263A1
公开(公告)日：2005-11-03
申请号：PCT/CA2005/000615
申请日：2005-04-21
申请人： ENOBIA PHARMA INC. , CRINE, Philippe , BOILEAU, Guy , LEMIRE, Isabelle , LOISEL, Thomas, P.
发明人： CRINE, Philippe , BOILEAU, Guy , LEMIRE, Isabelle , LOISEL, Thomas, P.
IPC分类号： C12N15/57
CPC分类号： C07K7/06 , A61K38/00 , A61K47/645 , C07K14/51 , C07K2319/01 , C07K2319/23 , C12N9/16 , C12N9/6421 , C12N9/6494 , C12Y301/03001 , C12Y304/24011
摘要： A bone delivery conjugate having a structure selected from the group consisting of :A) X-D n -Y-protein-Z; and B) Z-protein-Y- D n -X, wherein X is absent or is an amino acid sequence of at least one amino acid; Y is absent or is an amino acid sequence of at least one amino acid; Z is absent or is an amino acid sequence of at least one amino acid; and D n is a poly aspartate wherein n = 10 to 16. Compositions comprising same and uses thereof.
摘要翻译：具有选自以下的结构的骨递送缀合物：A）X-D n -Y蛋白-Z; 和B）Z-蛋白-Y-D n -X，其中X不存在或是至少一个氨基酸的氨基酸序列; Y不存在或是至少一个氨基酸的氨基酸序列; Z不存在或是至少一个氨基酸的氨基酸序列; 并且D n是聚天冬氨酸，其中n = 10至16.包含其的组合物及其用途。

3. 发明申请

WO2004050620A2 DERIVATIVES OF SUCCINIC AND GLUTARIC ACIDS AND ANALOGS THEREOF USEFUL AS INHIBITORS OF PHEX 审中-公开
标题翻译：化合物和葡萄糖的衍生物及其类似物作为PHEX的抑制剂有用
公开(公告)号：WO2004050620A2
公开(公告)日：2004-06-17
申请号：PCT/CA2003/001893
申请日：2003-12-03
申请人： BIOMEP INC. , GRAVEL, Denis , RATEMI, Elaref, S. , HATAM, Mostafa , BOILEAU, Guy , CRINE, Philippe , LEMIRE, Isabelle
发明人： GRAVEL, Denis , RATEMI, Elaref, S. , HATAM, Mostafa , BOILEAU, Guy , CRINE, Philippe , LEMIRE, Isabelle
IPC分类号： C07D209/00
CPC分类号： C07K5/0819 , C07C233/05 , C07C259/06 , C07D209/16 , C07D209/20 , C07D213/40 , C07F9/4006 , C07F9/5728 , C07F9/653 , C07K5/06104 , C07K5/06113 , C07K5/06191
摘要： The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula (I), useful as inhibitors of PHEX. These derivatives are useful for promoting generation of bone mass and treating or preventing diseases or conditions associated with a phosphate metabolism defect. Methods for preparation and intermediates are also disclosed.
摘要翻译：本发明涉及具有以下通式（I）的琥珀酸和戊二酸及其类似物的衍生物，其可用作PHEX的抑制剂。这些衍生物可用于促进骨量的产生和治疗或预防与磷酸盐代谢缺陷相关的疾病或病症。还公开了制备方法和中间体。

4. 发明申请

WO2011134084A1 METHODS, COMPOSITIONS, AND KITS FOR THE TREATMENT OF MATRIX MINERALIZATION DISORDERS 审中-公开
标题翻译：用于治疗基质矿化症的方法，组合物和工具
公开(公告)号：WO2011134084A1
公开(公告)日：2011-11-03
申请号：PCT/CA2011/050258
申请日：2011-04-29
申请人： ENOBIA PHARMA INC. , CRINE, Philippe , LEONARD, Pierre
发明人： CRINE, Philippe , LEONARD, Pierre
IPC分类号： A61K47/48 , A61K31/7088 , A61K38/17 , A61K38/46 , A61K48/00 , A61P19/08 , C12N9/16 , C12N15/55 , C12N15/867
CPC分类号： C12N9/96 , A61K31/7088 , A61K38/465 , A61K47/6811
摘要： The present invention provides methods, compositions, and kits for the treatment of matrix mineralization disorders such as hypophosphatasia. In particular, the present invention provides polypeptides having a soluble alkaline phosphatase fused to an Fc domain of an immunoglobulin. Such polypeptides can be administered to patients, e.g., subcutaneously, to treat hypophosphatasia using enzyme replacement therapy. The invention also features nucleic acids encoding such polypeptides and the use of the nucleic acids for treating matrix mineralization disorders.
摘要翻译：本发明提供了用于治疗基质矿化病症例如hypophosphatasia的方法，组合物和试剂盒。特别地，本发明提供了具有与免疫球蛋白的Fc结构域融合的可溶性碱性磷酸酶的多肽。可以将这样的多肽施用于患者，例如皮下，以使用酶替代疗法治疗次磷酸化。本发明还包括编码这种多肽的核酸和用于治疗基质矿化病症的核酸的用途。

5. 发明申请

WO2013059491A1 COMPOSITIONS COMPRISING ALKALINE PHOSPHATASE AND/OR NATRIURETIC PEPTIDE AND METHODS OF USE THEREOF 审中-公开
标题翻译：包含碱性磷酸酶和/或NATRIURETIC PEPTIDE的组合物及其使用方法
公开(公告)号：WO2013059491A1
公开(公告)日：2013-04-25
申请号：PCT/US2012/060869
申请日：2012-10-18
申请人： ALEXION PHARMA INTERNATIONAL SàRL , VANDERBILT UNIVERSITY , CRINE, Philippe , ELEFTERIOU, Florent
发明人： CRINE, Philippe , ELEFTERIOU, Florent
IPC分类号： A61K39/00 , A61K38/00 , A61P13/06 , C12N9/16
CPC分类号： C07K14/58 , A61K38/16 , A61K38/2278 , A61K38/465 , C07K2319/30 , C12N9/16
摘要： The present invention provides methods, compositions, and kits for the treatment of neurocutaneous syndromes, such as neurofibromatosis type I; disorders associated with overactivation of FGFR3, such as achondroplasia; bone or cartilage disorders; or vascular smooth muscle disorders; or for the elongation of bone. In some embodiments, the present invention provides polypeptides having an alkaline phosphatase peptide fused to an Fc domain of an immunoglobulin or a natriuretic peptide fused to an Fc domain of an immunoglobulin. Such polypeptides can be administered to subjects, e.g., subcutaneously, to treat a neurocutaneous syndrome, a disorder associated with overactivation of FGFR3, a bone or cartilage disorder, or a vascular smooth muscle disorder, or to elongate bone. The invention also features nucleic acid molecules encoding such polypeptides and the use of the nucleic acid molecules for treating neurocutaneous syndromes, disorders associated with overactivation of FGFR3, bone or cartilage disorders, or vascular smooth muscle disorders, or for elongating bone.
摘要翻译：本发明提供了用于治疗神经皮肤综合征的方法，组合物和试剂盒，例如I型神经纤维瘤病; 与FGFR3过度活化相关的疾病，如软骨发育不全; 骨或软骨疾病; 或血管平滑肌障碍; 或用于骨的伸长。在一些实施方案中，本发明提供了具有与免疫球蛋白的Fc结构域融合的碱性磷酸酶肽的多肽，或与免疫球蛋白的Fc结构域融合的利尿钠肽。这样的多肽可以被给予例如皮下的受试者，以治疗神经皮肤综合征，与FGFR3的过度活化相关的病症，骨或软骨疾病或血管平滑肌病症或细长的骨骼。本发明还具有编码这种多肽的核酸分子以及核酸分子用于治疗神经皮肤综合征，与FGFR3过度活化相关的病症，骨或软骨疾病或血管平滑肌病症或延长骨骼的用途。

6. 发明申请

WO2012088608A1 COMPOSITIONS COMPRISING NATRIURETIC PEPTIDES AND METHODS OF USE THEREOF 审中-公开
标题翻译：包含NATRIURETIC PEPTIDES的组合物及其使用方法
公开(公告)号：WO2012088608A1
公开(公告)日：2012-07-05
申请号：PCT/CA2011/050807
申请日：2011-12-23
申请人： ENOBIA CANADA LIMITED PARTNERSHIP , CRINE, Philippe , JOUBERT, Simon , PARAT, Marie
发明人： CRINE, Philippe , JOUBERT, Simon , PARAT, Marie
IPC分类号： C12N15/16 , A61K38/17 , A61K47/48 , A61P19/08 , C07K14/575 , C07K19/00 , C12N15/62
CPC分类号： C07K14/58 , A61K31/7088 , A61K38/2242 , C07K2319/22 , C07K2319/30 , C07K2319/31
摘要： The present invention provides methods, compositions, and kits for the treatment of disorders associated with overactivation of FGFR3, such as achondroplasia; bone or cartilage disorders; or vascular smooth muscle disorders, or for the elongation of bone. In some embodiments, the present invention provides polypeptides having a natriuretic peptide fused to an Fc domain of an immunoglobulin. Such polypeptides can be administered to subjects, e.g., subcutaneously, to treat a disorder associated with overactivation of FGFR3, a bone or cartilage disorder, or a vascular smooth muscle disorder, or to elongate bone. The invention also features nucleic acid molecules encoding such polypeptides and the use of the nucleic acid molecules for treating disorders associated with overactivation of FGFR3, bone or cartilage disorders, or vascular smooth muscle disorders, or for elongating bone.
摘要翻译：本发明提供了用于治疗与FGFR3的过度活化相关的疾病的方法，组合物和试剂盒，例如软骨发育不良; 骨或软骨疾病; 或血管平滑肌障碍，或用于骨的伸长。在一些实施方案中，本发明提供了具有与免疫球蛋白的Fc结构域融合的利尿钠肽的多肽。可以将这样的多肽施用于受试者，例如皮下，以治疗与FGFR3过度活化，骨或软骨疾病或血管平滑肌病症或细长骨骼相关的病症。本发明还具有编码这种多肽的核酸分子以及核酸分子用于治疗与FGFR3，骨或软骨障碍或血管平滑肌病或过度活化骨骼相关的疾病的用途。

7. 发明申请

WO2013058833A1 COMPOSITIONS COMPRISING ALKALINE PHOSPHATASE AND/OR NATRIURETIC PEPTIDE AND METHODS OF USE THEREOF 审中-公开
标题翻译：包含碱性磷酸酶和/或NATRIURETIC PEPTIDE的组合物及其使用方法
公开(公告)号：WO2013058833A1
公开(公告)日：2013-04-25
申请号：PCT/US2012/039004
申请日：2012-05-22
申请人： ENOBIA CANADA LIMITED PARTNERSHIP , VANDERBIL T UNIVERSITY , CRINE, Philippe , ELEFTERIOU, Florent
发明人： CRINE, Philippe , ELEFTERIOU, Florent
IPC分类号： A61K39/00 , A61K38/00 , A61P13/06 , C12N9/16
CPC分类号： C07K14/58 , A61K38/16 , A61K38/2278 , A61K38/465 , C07K2319/30 , C12N9/16
摘要： The present invention provides methods, compositions, and kits for the treatment of neurocutaneous syndromes, such as neurofibromatosis type I disorders associated with overactivation of FGFR3, such as achondroplasia; bone or cartilage disorders; or vascular smooth muscle disorders; or for the elongation of bone. Polypeptides having an alkaline phosphatase peptide fused to an Fc domain of an immunoglobulin or a natriuretic peptide fused to an Fc domain of an immunoglobulin can be administered to subjects, e.g., subcutaneously, to treat a neurocutaneous syndromes. The invention also features nucleic acid molecules encoding such polypeptides and the use of the nucleic acid molecules for treating neurocutaneous syndromes.
摘要翻译：本发明提供了用于治疗神经性皮肤综合征的方法，组合物和试剂盒，例如与FGFR3过度活化相关的神经纤维瘤病I型障碍，例如软骨发育不良; 骨或软骨疾病; 或血管平滑肌障碍; 或用于骨的伸长。具有与免疫球蛋白的Fc结构域融合的碱性磷酸酶肽的多肽或与免疫球蛋白的Fc结构域融合的利尿钠肽可以给予受试者，例如皮下，以治疗神经皮肤综合征。本发明还具有编码这种多肽的核酸分子以及核酸分子用于治疗神经皮肤综合征的用途。

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