公开(公告)号：US20140135344A1

公开(公告)日：2014-05-15

申请号：US14129838

申请日：2012-06-26

申请人： Siji Zheng ,  Bo Tan ,  Linyong Fu ,  Xiaoyi Liu ,  Shaoqing Yuan ,  Zhihui Cao

发明人： Siji Zheng ,  Bo Tan ,  Linyong Fu ,  Xiaoyi Liu ,  Shaoqing Yuan ,  Zhihui Cao

IPC分类号： C07D215/227

CPC分类号： C07D215/227 ,  A61K9/0056 ,  A61K9/2018 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/496

摘要： A method for preparing an aripiprazole type I microcrystal, including the following steps: dissolving aripiprazole in an acidifier, acquiring a medicament-having acid solution; adding an alkalizer while stirring, then adding water or aqueous ethanol 10 to 60 wt % while stirring, and separating by precipitation the aripiprazole type I microcrystal. Furthermore, a method for preparing a solid preparation having the aripiprazole type I microcrystal, an aripiprazole microcrystal having an average particle size of less than 24 μm, and a solid preparation having the microcrystal. The method for preparing the aripiprazole type I microcrystal allows reduced pollution and loss, great safety, easy and convenient, reduced use of organic solvents, obviated need for demanding process conditions (such as cooling condition) and apparatus, low cost, and facilitated applicability in industrialized manufacturing. This solid preparation provides great stability, solubility, and bioavailability, reduced individual differences, and reduced content of related substances.

摘要翻译： 一种制备阿立哌唑I型微晶的方法，包括以下步骤：将阿立哌唑溶解在酸化剂中，获得药物的酸溶液; 在搅拌的同时加入碱化剂，然后在搅拌下加入10至60重量％的水或乙醇水溶液，并通过沉淀阿立哌唑I型微晶分离。 此外，制备具有阿立哌唑I型微晶体的固体制剂，平均粒径小于24μm的阿立哌唑微晶体和具有微晶体的固体制剂的方法。 制备阿立哌唑I型微晶的方法可减少污染和损失，安全性，方便，减少有机溶剂的使用，避免了苛刻的工艺条件（如冷却条件）和设备的需求，低成本，便于适用性 工业化制造业。 这种固体制剂提供极大的稳定性，溶解度和生物利用度，减少个体差异，并减少相关物质的含量。

公开(公告)号：US20050009750A1

公开(公告)日：2005-01-13

申请号：US10885225

申请日：2004-07-06

申请人： Matthew Sleeman ,  J. Murison ,  Zhihui Cao

发明人： Matthew Sleeman ,  J. Murison ,  Zhihui Cao

IPC分类号： C07H21/04 ,  C07K14/71 ,  A61K38/17

CPC分类号： C07K14/71 ,  C07H21/04

摘要： Isolated fibroblast growth factor receptor 5 (FGFR5) polypeptides are provided, together with polynucleotides encoding such polypeptides. Also provided are modulators of FGFR5 gene expression and binding molecules that specifically bind to, and agonize or antagonize, FGFR5 polypeptide function. Binding molecules include antibodies, and functional fragments thereof, as well as scFv and Camelidae heavy chain IgG that specifically bind to FGFR5 thereby modulating the activity of FGFR5. Such binding agents and modulators of FGFR5 gene expression may be employed for the treatment of disorders including: osteopontin-mediated diseases; autoimmune diseases, such as systemic lupus erythematosus; bone disorders such as osteoporosis and osteopetrosis; and cancers, including cellular carcinomas such as hepatocellular carcinomas.

公开(公告)号：US20060115483A1

公开(公告)日：2006-06-01

申请号：US11154977

申请日：2005-06-15

申请人： Matthew Sleeman ,  J. Murison ,  Zhihui Cao

发明人： Matthew Sleeman ,  J. Murison ,  Zhihui Cao

IPC分类号： C07K14/82 ,  C07K16/30 ,  C07H21/04 ,  C12P21/06 ,  A61K39/395

CPC分类号： C07K16/2863 ,  C07K14/71 ,  C07K2317/74 ,  C07K2317/75 ,  C07K2317/76 ,  C07K2319/30

摘要： Isolated fibroblast growth factor receptor 5 (FGFR5) polypeptides are provided, together with polynucleotides encoding such polypeptides. Also provided are modulators of FGFR5 gene expression and binding molecules that specifically bind to, and agonize or antagonize, FGFR5 polypeptide function. Binding molecules include antibodies, and functional fragments thereof, as well as scFv and Camelidae heavy chain IgG that specifically bind to FGFR5 thereby modulating the activity of FGFR5. Such binding agents and modulators of FGFR5 gene expression may be employed for the treatment of disorders including: osteopontin-mediated diseases; autoimmune diseases, such as systemic lupus erythematosus; bone disorders such as osteoporosis and osteopetrosis; and cancers, including cellular carcinomas such as hepatocellular carcinomas.

摘要翻译： 分离的成纤维细胞生长因子受体5（FGFR5）多肽与编码这种多肽的多核苷酸一起提供。 还提供了FGFR5基因表达的调节剂和特异性结合并激动或拮抗FGFR5多肽功能的结合分子。 结合分子包括抗体及其功能片段，以及特异性结合FGFR5的scFv和骆驼科重链IgG，从而调节FGFR5的活性。 FGFR5基因表达的这种结合剂和调节剂可用于治疗疾病，包括：骨桥蛋白介导的疾病; 自身免疫性疾病，如系统性红斑狼疮; 骨质疏松症和骨硬化等骨质疏松症; 和癌症，包括细胞癌如肝细胞癌。

公开(公告)号：US20050112642A1

公开(公告)日：2005-05-26

申请号：US10954094

申请日：2004-09-29

申请人： Matthew Sleeman ,  J. Murison ,  Zhihui Cao

发明人： Matthew Sleeman ,  J. Murison ,  Zhihui Cao

IPC分类号： A61K38/00 ,  C07H21/04 ,  C07K14/71 ,  C07K16/28 ,  C12Q1/68

CPC分类号： C07H21/04 ,  A61K38/00 ,  A61K2039/505 ,  C07K14/71 ,  C07K16/2863 ,  C07K2319/00

摘要： Isolated fibroblast growth factor receptor 5 (FGFR5) polypeptides are provided, together with polynucleotides encoding such polypeptides. Also provided are modulators of FGFR5 gene expression and binding molecules that specifically bind to, and agonize or antagonize, FGFR5 polypeptide function. Binding molecules include antibodies, and functional fragments thereof, as well as scFv and Camelidae heavy chain IgG that specifically bind to FGFR5 thereby modulating the activity of FGFR5. Such binding agents and modulators of FGFR5 gene expression may be employed for the treatment of disorders including: osteopontin-mediated diseases; autoimmune diseases, such as systemic lupus erythematosus; bone disorders such as osteoporosis and osteopetrosis; and cancers, including cellular carcinomas such as hepatocellular carcinomas.

摘要翻译： 分离的成纤维细胞生长因子受体5（FGFR5）多肽与编码这种多肽的多核苷酸一起提供。 还提供了FGFR5基因表达的调节剂和特异性结合并激动或拮抗FGFR5多肽功能的结合分子。 结合分子包括抗体及其功能片段，以及特异性结合FGFR5的scFv和骆驼科重链IgG，从而调节FGFR5的活性。 FGFR5基因表达的这种结合剂和调节剂可用于治疗疾病，包括：骨桥蛋白介导的疾病; 自身免疫性疾病，如系统性红斑狼疮; 骨质疏松症和骨硬化等骨质疏松症; 和癌症，包括细胞癌如肝细胞癌。

公开(公告)号：US09073857B2

公开(公告)日：2015-07-07

申请号：US14129838

申请日：2012-06-26

申请人： Siji Zheng ,  Bo Tan ,  Linyong Fu ,  Xiaoyi Liu ,  Shaoqing Yuan ,  Zhihui Cao

发明人： Siji Zheng ,  Bo Tan ,  Linyong Fu ,  Xiaoyi Liu ,  Shaoqing Yuan ,  Zhihui Cao

IPC分类号： C07D215/227 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  A61K31/496

CPC分类号： C07D215/227 ,  A61K9/0056 ,  A61K9/2018 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/496

摘要： A method for preparing an aripiprazole type I microcrystal, including the following steps: dissolving aripiprazole in an acidifier, acquiring a medicament-having acid solution; adding an alkalizer while stirring, then adding water or aqueous ethanol 10 to 60 wt % while stirring, and separating by precipitation the aripiprazole type I microcrystal. Furthermore, a method for preparing a solid preparation having the aripiprazole type I microcrystal, an aripiprazole microcrystal having an average particle size of less than 20 μm, and a solid preparation having the microcrystal. The method for preparing the aripiprazole type I microcrystal allows reduced pollution and loss, great safety, easy and convenient, reduced use of organic solvents, obviated need for demanding process conditions (such as cooling condition) and apparatus, low cost, and facilitated applicability in industrialized manufacturing. This solid preparation provides great stability, solubility, and bioavailability, reduced individual differences, and reduced content of related substances.

摘要翻译： 一种制备阿立哌唑I型微晶的方法，包括以下步骤：将阿立哌唑溶解在酸化剂中，获得药物的酸溶液; 在搅拌的同时加入碱化剂，然后在搅拌下加入10至60重量％的水或乙醇水溶液，并通过沉淀阿立哌唑I型微晶分离。 此外，制备具有阿立哌唑I型微晶体，平均粒径小于20μm的阿立哌唑微晶体和具有微晶体的固体制剂的固体制剂的制备方法。 制备阿立哌唑I型微晶的方法可减少污染和损失，安全性，方便，减少有机溶剂的使用，避免了苛刻的工艺条件（如冷却条件）和设备的需求，低成本，便于适用性 工业化制造业。 这种固体制剂提供极大的稳定性，溶解度和生物利用度，减少个体差异，并减少相关物质的含量。

公开(公告)号：US20070110752A1

公开(公告)日：2007-05-17

申请号：US11591993

申请日：2006-11-01

申请人： J. Murison ,  Zhihui Cao

发明人： J. Murison ,  Zhihui Cao

IPC分类号： A61K39/395 ,  A61K48/00

CPC分类号： C07K14/71 ,  A61K38/00 ,  C12N15/1138 ,  C12N2310/11

摘要： Isolated fibroblast growth factor receptor 5 (FGFR5) polypeptides are provided, together with polynucleotides encoding such polypeptides. Also provided are modulators of FGFR5 gene expression and binding molecules that specifically bind to, and agonize or antagonize, FGFR5 polypeptide finction. Binding molecules include antibodies, and functional fragments thereof, as well as scFv and Camelidae heavy chain IgG that specifically bind to FGFR5 thereby modulating the activity of FGFR5. Such binding agents and modulators of FGFR5 gene expression may be employed for the treatment of disorders including: osteopontin-mediated diseases; autoimmune diseases, such as systemic lupus erythematosus; bone disorders such as osteoporosis and osteopetrosis; and cancers, including cellular carcinomas such as hepatocellular carcinomas.

摘要翻译： 分离的成纤维细胞生长因子受体5（FGFR5）多肽与编码这种多肽的多核苷酸一起提供。 还提供了FGFR5基因表达的调节剂和特异性结合并激动或拮抗FGFR5多肽功能的结合分子。 结合分子包括抗体及其功能片段，以及特异性结合FGFR5的scFv和骆驼科重链IgG，从而调节FGFR5的活性。 FGFR5基因表达的这种结合剂和调节剂可用于治疗疾病，包括：骨桥蛋白介导的疾病; 自身免疫性疾病，如系统性红斑狼疮; 骨质疏松症和骨硬化等骨质疏松症; 和癌症，包括细胞癌如肝细胞癌。