公开(公告)号：WO2010014689A1

公开(公告)日：2010-02-04

申请号：PCT/US2009/052080

申请日：2009-07-29

Applicant: PHASEBIO PHARMACEUTICALS, INC. ,  DAGHER, Sue ,  PRIOR, Chris ,  SADEGHI, Homayoun

Inventor： DAGHER, Sue ,  PRIOR, Chris ,  SADEGHI, Homayoun

IPC: A01N25/00 ,  A61K47/00

CPC classification number: A61K38/39 ,  A61K9/0019 ,  A61K9/19

Abstract: The present invention provides stable pharmaceutical compositions or formulations, including solution and non-solution phase formulations, and methods of preparing the same. The formulations of the invention may improve the stability and/or solubility of various pharmaceutically-active ingredients, including biological molecules and small drug compounds, and may be tailored to a variety of storage conditions. The formulations of the invention may provide an alternative to lyophilization, or may be employed together with lyophilization or other methods of stabilization. Generally, the compositions comprise a pharmaceutically active ingredient, such as a biological molecule or small drug compound, and a pharmaceutically acceptable carrier. The carrier comprises an Elastin-Like Peptide (ELP) in an amount and form (e.g., soluble or insoluble form) effective for stabilizing the pharmaceutically active ingredient.

Abstract translation: 本发明提供稳定的药物组合物或制剂，包括溶液和非溶液相制剂，及其制备方法。 本发明的制剂可以改善各种药物活性成分（包括生物分子和小药物化合物）的稳定性和/或溶解性，并且可以针对各种储存条件进行调整。 本发明的制剂可以提供冷冻干燥的替代方案，或者可以与冷冻干燥或其它稳定方法一起使用。 通常，组合物包含药物活性成分，例如生物分子或小药物化合物和药学上可接受的载体。 载体包含有效稳定药物活性成分的量和形式（例如可溶性或不溶性形式）的弹性蛋白样肽（ELP）。

公开(公告)号：WO2008033395A3

公开(公告)日：2008-05-15

申请号：PCT/US2007019809

申请日：2007-09-11

Applicant: BIOREXIS PHARMACEUTICAL CORP ,  SADEGHI HOMAYOUN ,  PRIOR CHRISTOPHER PHILIP

Inventor： SADEGHI HOMAYOUN ,  PRIOR CHRISTOPHER PHILIP

IPC: C07K14/435

CPC classification number: C07K14/79 ,  C07K14/575 ,  C07K14/70582 ,  C07K2319/00

Abstract: The present invention discloses fusion proteins comprising a transferrin moiety and a melanocortin or melanocortin receptor agonist moiety. In one embodiment of the invention, the transferrin moiety is modified to exhibit reduced or no glycosylation. In another embodiment, the transferrin moiety is modified to exhibit reduced or no binding to a transferrin receptor. The fusion protein of the invention can optionally comprise a linker peptide and/or a second therapeutic peptide such as GLP-1 or exendin-4. Also disclosed are methods of treating or preventing a disease or condition in a subject by administering a fusion protein of the invention.

Abstract translation: 本发明公开了包含转铁蛋白部分和黑皮质素或黑皮质素受体激动剂部分的融合蛋白。 在本发明的一个实施方案中，转铁蛋白部分被修饰以显示减少或不糖基化。 在另一个实施方案中，转铁蛋白部分被修饰以显示减少或不结合转铁蛋白受体。 本发明的融合蛋白可任选地包含接头肽和/或第二治疗肽如GLP-1或毒蜥外泌肽-4。 还公开了通过施用本发明的融合蛋白来治疗或预防受试者的疾病或病症的方法。

公开(公告)号：WO2006096515A3

公开(公告)日：2006-12-07

申请号：PCT/US2006007617

申请日：2006-03-06

Applicant: BIOREXIS PHARMACEUTICAL CORP ,  SADEGHI HOMAYOUN ,  TURNER ANDREW J ,  PRIOR CHRISTOPHER P ,  BALLANCE DAVID J

Inventor： SADEGHI HOMAYOUN ,  TURNER ANDREW J ,  PRIOR CHRISTOPHER P ,  BALLANCE DAVID J

IPC: A61K38/26 ,  A61K38/40 ,  C07K5/00 ,  C07K14/76 ,  C12N15/16 ,  C12N15/17 ,  C12N15/18

CPC classification number: C07K14/605 ,  A61K38/26 ,  A61K47/644 ,  C07K14/79 ,  C07K2319/00

Abstract: Modified fusion proteins of a transferrin moiety, a GLP-1 moiety and a linker moiety, with increased productivity, bioactivity and serum half-life are disclosed. Preferred fusion proteins include those modified so that the transferrin moiety exhibits no or reduced glycosylation. The fusion proteins of the invention are useful for the treatment of Type 2 diabetes, Type 1 diabetes, obesity, congestive heart failure, and non-fatty liver disease.

Abstract translation: 公开了转铁蛋白部分，GLP-1部分和连接体部分的经修饰的融合蛋白，其具有提高的生产力，生物活性和血清半衰期。 优选的融合蛋白包括经修饰的融合蛋白，使得转铁蛋白部分不显示或减少糖基化。 本发明的融合蛋白可用于治疗2型糖尿病，1型糖尿病，肥胖症，充血性心力衰竭和非脂肪肝疾病。

公开(公告)号：WO2005021579A3

公开(公告)日：2005-08-04

申请号：PCT/US2004027949

申请日：2004-08-30

Applicant: BIOREXIS PHARMACEUTICAL CORP ,  SADEGHI HOMAYOUN ,  TURNER ANDREW J

Inventor： SADEGHI HOMAYOUN ,  TURNER ANDREW J

IPC: A61K38/00 ,  A61K38/08 ,  C07K20060101 ,  C12N5/02 ,  C12P21/04

CPC classification number: C07K14/79 ,  A61K38/00 ,  C07K7/06 ,  C07K7/08 ,  C07K2319/31

Abstract: EPM peptides, including EPM peptide-fusion proteins with increased serum half-life or serum stability are disclosed. Compositions comprising the EPM peptides or fusion proteins and methods of treating or preventing disorders by administering a therapeutically or prophylactically effective amount of an EPM peptide or fusion protein to a patient in need thereof are also disclosed.

Abstract translation: 公开了EPM肽，包括具有增加的血清半衰期或血清稳定性的EPM肽 - 融合蛋白。 还公开了包含EPM肽或融合蛋白的组合物以及通过向有需要的患者施用治疗或预防有效量的EPM肽或融合蛋白来治疗或预防病症的方法。

公开(公告)号：WO2011020091A1

公开(公告)日：2011-02-17

申请号：PCT/US2010/045605

申请日：2010-08-16

Applicant: PHASEBIO PHARMACEUTICALS, INC. ,  SADEGHI, Homayoun ,  TURNER, Andrew ,  DAGHER, Suzanne

Inventor： SADEGHI, Homayoun ,  TURNER, Andrew ,  DAGHER, Suzanne

IPC: A61K38/00 ,  A61K38/24

CPC classification number: A61K38/2278 ,  A61K38/39 ,  A61K2300/00

Abstract: The present invention provides modified Vasoactive Intestinal Peptides (VIPs), encoding polynucleotides and vectors, as well as pharmaceutical compositions comprising the same. The invention further provides methods of making and using the modified VIP agents. In accordance with the invention the VIP exhibits an extended circulatory half-life, receptor-binding or biological potency, and/or altered receptor binding profile with respect to unmodified VIP.

Abstract translation: 本发明提供了修饰的血管活性肽肽（VIPs），编码多核苷酸和载体，以及包含其的药物组合物。 本发明还提供了制备和使用经修饰的VIP试剂的方法。 根据本发明，VIP相对于未修饰的VIP显示出延长的循环半衰期，受体结合或生物效力和/或改变的受体结合特征。

公开(公告)号：WO2008012629A3

公开(公告)日：2008-05-08

申请号：PCT/IB2007002047

申请日：2007-07-13

Applicant: BIOREXIS PHARMACEUTICAL CORP ,  SADEGHI HOMAYOUN ,  PRIOR CHRISTOPHER PHILIP ,  BALLANCE DAVID JAMES ,  TURNER ANDREW JOHN

Inventor： SADEGHI HOMAYOUN ,  PRIOR CHRISTOPHER PHILIP ,  BALLANCE DAVID JAMES ,  TURNER ANDREW JOHN

IPC: C07K14/575 ,  A61K38/22 ,  C07K19/00 ,  C12N15/62 ,  C12N15/63

CPC classification number: C07K14/57563 ,  C07K2319/03

Abstract: The invention provides fusion proteins comprising an exendin-4 fused to a transferrin (Tf) via a polypeptide linker, as well as corresponding nucleic acid molecules, vectors, host cells, and pharmaceutical compositions. The invention also provides the use of the exendin-4/Tf fusion proteins for treatment of Type Il diabetes, obesity, and to reduce body weight.

Abstract translation: 本发明提供了包含通过多肽接头与转铁蛋白（Tf）融合的毒蜥外泌肽-4的融合蛋白，以及相应的核酸分子，载体，宿主细胞和药物组合物。 本发明还提供了毒蜥外泌肽-4 / Tf融合蛋白用于治疗II型糖尿病，肥胖症和降低体重的用途。

公开(公告)号：WO2008021412A3

公开(公告)日：2008-02-21

申请号：PCT/US2007/018099

申请日：2007-08-14

Applicant: BIOREXIS PHARMACEUTICAL CORPORATION ,  SADEGHI, Homayoun ,  TURNER, Andrew, John ,  PRIOR, Christopher, Philip

Inventor： SADEGHI, Homayoun ,  TURNER, Andrew, John ,  PRIOR, Christopher, Philip

IPC: A61K47/48 ,  C07K14/56 ,  C07K14/565 ,  C07K14/79 ,  C12N15/62

Abstract: Fusion proteins of transferrin and IFNβ with increased serum half-life or serum stability are disclosed- Preferred fusion proteins include those modified so that the transferrin moiety exhibits no or reduced glycosylation, binding to iron and/or binding to the transferrin receptor.

公开(公告)号：WO2006049983A3

公开(公告)日：2007-02-01

申请号：PCT/US2005038531

申请日：2005-10-27

Applicant: BIOREXIS PHARMACEUTICAL CORP ,  PRIOR CHRISTOPHER P ,  SADEGHI HOMAYOUN ,  BALLANCE DAVID J ,  TURNER ANDREW

Inventor： PRIOR CHRISTOPHER P ,  SADEGHI HOMAYOUN ,  BALLANCE DAVID J ,  TURNER ANDREW

IPC: C07K14/00 ,  C07H17/00 ,  C12P21/06

CPC classification number: C07K14/575 ,  C07K2319/01

Abstract: Modified fusion proteins of transferring and therapeutic proteins or peptides including, with increased serum half-life or serum stability are disclosed. Preferred fusion proteins include those modified so that the transferrin moiety exhibits no or reduced glycosylation, binding to iron and/or binding to the transferrin receptor.

Abstract translation: 公开了转移和治疗性蛋白质或肽的修饰融合蛋白，包括具有增加的血清半衰期或血清稳定性。 优选的融合蛋白包括经修饰的融合蛋白，使得转铁蛋白部分不显示或降低糖基化，结合铁和/或结合转铁蛋白受体。

公开(公告)号：WO2004078777A2

公开(公告)日：2004-09-16

申请号：PCT/US2004/006462

申请日：2004-03-04

Applicant: BIOREXIS PHARMACEUTICAL CORPORATION ,  SADEGHI, Homayoun ,  PRIOR, Christopher, P. ,  BALLANCE, David, J.

Inventor： SADEGHI, Homayoun ,  PRIOR, Christopher, P. ,  BALLANCE, David, J.

IPC: C07K

CPC classification number: C07K1/1075 ,  C07K14/521 ,  C07K14/575 ,  C07K14/605 ,  C07K14/79

Abstract: The present invention provides modified therapeutic polypeptides or peptides partially or completely protected from DPP activity. The modified polypeptides or peptides comprise at least one additional amino acid at the amino terminus. The modified therapeutic polypeptides or peptides are useful in the treatment of diseases such as diabetes.

Abstract translation: 本发明提供经DPP活性部分或完全保护的修饰的治疗性多肽或肽。 修饰的多肽或肽在氨基末端包含至少一个另外的氨基酸。 修饰的治疗性多肽或肽可用于治疗疾病如糖尿病。

公开(公告)号：WO2004019872A2

公开(公告)日：2004-03-11

申请号：PCT/US2003/026778

申请日：2003-08-28

Applicant: BIOREXIS PHARMACEUTICAL CORPORATION ,  PRIOR, Christopher, P. ,  SADEGHI, Homayoun ,  TURNER, Andrew

Inventor： PRIOR, Christopher, P. ,  SADEGHI, Homayoun ,  TURNER, Andrew

IPC: A61K

CPC classification number: C07K14/70582 ,  C07K14/79 ,  C07K2319/035

Abstract: Pharmaceutical compositions containing modified fusion proteins of transferrin and therapeutic proteins or peptides with increased serum half-life or increased serum stability are disclosed. Preferred fusion proteins include those modified so that the transferrin moiety exhibits no or reduced glycosylation, but does exhibit binding to iron and/or the transferrin receptor. Such fusion proteins may be administered orally.

Abstract translation: 公开了含有转铁蛋白的修饰融合蛋白和具有增加的血清半衰期或增加的血清稳定性的治疗性蛋白质或肽的药物组合物。 优选的融合蛋白包括那些经过修饰以使转铁蛋白部分不显示或减少糖基化，但显示与铁和/或转铁蛋白受体结合的融合蛋白。 这种融合蛋白可以口服给药。