公开(公告)号：WO2006105201A2

公开(公告)日：2006-10-05

申请号：PCT/US2006011474

申请日：2006-03-28

Applicant: TRIMERIS INC ,  WRING STEPHEN ,  FRICK LLOYD ,  SCHNEIDER STEPHEN ,  ZHANG HUYI ,  DI JIE ,  HEILMAN DAVID

Inventor： WRING STEPHEN ,  FRICK LLOYD ,  SCHNEIDER STEPHEN ,  ZHANG HUYI ,  DI JIE ,  HEILMAN DAVID

IPC: C07K14/16

CPC classification number: C07K14/005 ,  A61K38/00 ,  A61K39/00 ,  A61K47/543 ,  C12N2740/16122

Abstract: Provided is a conjugate comprised of HIV gp41 -derived peptide operatively linked to fatty acid, and pharmaceutical compositions and medicaments containing the conjugate. Also provided are methods for producing a conjugate according to the present invention which include, but are not limited to, covalently coupling a linker to the HIV gp41 -derived peptide, wherein the linker is covalently coupled to fatty acid.

Abstract translation: 提供了由可操作地连接到脂肪酸的HIV gp41衍生的肽组成的缀合物，以及含有缀合物的药物组合物和药物。 还提供了用于制备根据本发明的缀合物的方法，其包括但不限于将接头共价偶联到HIV gp41衍生的肽，其中所述接头共价偶联到脂肪酸上。

公开(公告)号：WO2004029073A3

公开(公告)日：2004-08-12

申请号：PCT/US0330285

申请日：2003-09-26

Applicant: TRIMERIS INC

Inventor： BRAY BRIAN ,  KANG MYUNG-CHOL ,  TVERMOES NICOLAI ,  KINDER DANIEL ,  LACKEY JOHN WILLIAM

IPC: C07K7/00 ,  A61K38/00 ,  A61K47/48 ,  C07K14/16 ,  A61K39/21 ,  A61K39/385

CPC classification number: C07K14/005 ,  A61K38/00 ,  A61K47/60 ,  C12N2740/16122

Abstract: Provided are conjugates comprising a polymer having operably bound thereto no less than two molecules of synthetic peptide derived from HIV gp41; methods of using these conjugates to inhibit transmission of HIV to a target cell by adding an amount of effective to inhibit infection of the cell by the virus; and methods of producing the conjugates by operably binding each molecule of synthetic peptide, via a reactive functionality, to the polymer.

Abstract translation: 提供了包含与其可操作结合的聚合物不少于两个分子的衍生自HIV gp41的合成肽的缀合物; 通过加入一定量的有效抑制病毒对细胞的感染来使用这些缀合物来抑制HIV向靶细胞的传播的方法; 以及通过经由反应性官能团将每个合成肽分子可操作地结合到聚合物来产生缀合物的方法。

公开(公告)号：WO2004028457A2

公开(公告)日：2004-04-08

申请号：PCT/US2003/030287

申请日：2003-09-26

Applicant: TRIMERIS, INC.

Inventor： DI, Jie ,  HEILMAN, David ,  BRAY, Brian

IPC: A61K

CPC classification number: A61K9/0019 ,  A61K38/162 ,  A61K47/10 ,  A61K47/26

Abstract: Provided is a pharmaceutical composition comprising a solution comprised of synthetic peptide in a final concentration of not less than 70 mg/ml in admixture with a polyol; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the polyol is in a final concentration of no less than 5 weight % and no more than 75 weight % of the pharmaceutical composition. Also provided is a synthetic peptide-containing pharmaceutical composition as a unit dose comprising an aqueous formulation comprised of synthetic peptide in a final concentration of not less than 70 mg/ml in admixture with a polyol; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the polyol is in a final concentration of no less than 5 weight % and no more than 75 weight % of the pharmaceutical composition. Further provided is a method of treating HIV infection by administering to an HIV-infected individual a pharmaceutical composition according to the present invention.

Abstract translation: 本发明提供一种药物组合物，其包含与多元醇混合的终浓度不小于70mg / ml的合成肽的溶液; 其中所述合成肽是HIV融合抑制剂，并且其中所述多元醇的终浓度不低于所述药物组合物的5重量％且不大于75重量％。 还提供了含合成肽的药物组合物作为单位剂量，其包含由多元醇混合而成的最终浓度不小于70mg / ml的合成肽的水性制剂; 其中所述合成肽是HIV融合抑制剂，并且其中所述多元醇的终浓度不低于所述药物组合物的5重量％且不大于75重量％。 还提供了通过向HIV感染个体施用根据本发明的药物组合物来治疗HIV感染的方法。

公开(公告)号：WO0103723A9

公开(公告)日：2002-07-25

申请号：PCT/US0018772

申请日：2000-07-10

Applicant: TRIMERIS INC ,  BARNEY SHAWN ,  GUTHRIE KELLY I ,  MERUTKA GENE ,  ANWER MOHMED K ,  LAMBERT DENNIS M

Inventor： BARNEY SHAWN ,  GUTHRIE KELLY I ,  MERUTKA GENE ,  ANWER MOHMED K ,  LAMBERT DENNIS M

IPC: A61K38/00 ,  A61K38/21 ,  A61K38/27 ,  A61K47/48 ,  A61P31/14 ,  A61P31/16 ,  A61P31/18 ,  A61P31/20 ,  C07K5/113 ,  C07K5/117 ,  C07K14/135 ,  C07K14/15 ,  C07K14/16 ,  C07K14/59 ,  C07K19/00 ,  A61K38/02 ,  A61K38/08 ,  A61K38/10 ,  A61K38/16 ,  A61K38/18 ,  A61K38/19 ,  A61K38/22 ,  C07K7/06 ,  C07K7/08 ,  C07K14/00

CPC classification number: C07K14/005 ,  A61K38/00 ,  A61K47/62 ,  C07K5/1021 ,  C07K5/1024 ,  C07K14/59 ,  C07K2319/00 ,  C12N2740/16122 ,  C12N2760/18522

Abstract: The present invention relates to enhancer peptide sequences originally derived from various retroviral envelope (gp41) protein sequences that enhance the pharmacokinetic properties of any core polypeptide to which they are linked. The invention is based on the discovery that hybrid polypeptides comprising the enhancer peptide sequences linked to a core polypeptide possess enhanced pharmacokinetic properties such as increased half life. The invention further relates to methods for enhancing the pharmacokinetic properties of any core polypeptide through linkage of the enhancer peptide sequences to the core polypeptide. The core polypeptides to be used in the practice of the invention can include any pharmacologically useful peptide that can be used, for example, as a therapeutic or prophylactic reagent.

Abstract translation: 本发明涉及最初衍生自增强其所连接的核心多肽的药代动力学性质的各种逆转录病毒包膜（gp41）蛋白质序列的增强子肽序列。 本发明基于以下发现：包含与核心多肽连接的增强子肽序列的杂合多肽具有增强的药代动力学性质，例如增加的半衰期。 本发明还涉及通过将增强子肽序列与核心多肽连接来增强任何核心多肽的药代动力学性质的方法。 用于本发明实践的核心多肽可包括可用于例如治疗或预防试剂的任何药理学上有用的肽。

公开(公告)号：WO0151673A8

公开(公告)日：2002-04-11

申请号：PCT/US0035727

申请日：2000-07-05

Applicant: TRIMERIS INC

Inventor： JEFFS PETER ,  LACKEY JOHN WILLIAM ,  ERICKSON JOEL BURTON ,  LAWLESS MARY K ,  MERUTKA GENE

IPC: G01N33/50 ,  A61K38/16 ,  A61K45/00 ,  A61P31/18 ,  C07K14/02 ,  C07K14/055 ,  C07K14/11 ,  C07K14/115 ,  C07K14/12 ,  C07K14/125 ,  C07K14/13 ,  C07K14/135 ,  C07K14/155 ,  C07K14/16 ,  G01N33/15 ,  G01N33/566 ,  G01N33/569 ,  G01N33/68 ,  C12Q1/70 ,  A61K38/00 ,  A61K39/21 ,  G01N33/53

CPC classification number: C07K14/005 ,  A61K38/162 ,  C12N2710/16322 ,  C12N2730/10122 ,  C12N2740/15022 ,  C12N2740/16222 ,  C12N2760/16122 ,  C12N2760/18122 ,  C12N2760/18422 ,  C12N2760/18522 ,  C12N2760/18722 ,  G01N33/68 ,  G01N2500/00

Abstract: The present invention relates to peptides which exhibit potent anti-retroviral activity. The peptides of the invention comprise DP178 (SEQ ID:1) peptide corresponding to amino acids 638 to 673 of the HIV-1LAI gp41 protein, and fragments, analogs and homologs of DP178. The invention further relates to the uses of such peptides as inhibitory of human and non-human retroviral, especially HIV, transmission to uninfected cells.

Abstract translation: 本发明涉及显示出有力的抗​​逆转录病毒活性的肽。 本发明的肽包含对应于HIV-1LAI gp41蛋白的氨基酸638至673的DP178（SEQ ID：1）肽，以及DP178的片段，类似物和同系物。 本发明还涉及这样的肽的用途，例如抑制人和非人类逆转录病毒，特别是HIV，向未感染细胞的传播。

公开(公告)号：WO2010047826A3

公开(公告)日：2011-06-09

申请号：PCT/US2009005781

申请日：2009-10-23

Applicant: TRIMERIS INC ,  BRAY BRIAN L ,  DI JIE ,  GREENBERG MICHAEL ,  HEILMAN DAVID ,  OHMSTEDE CAROL ,  SILINSKI PETER ,  WEBB SCOTT

Inventor： BRAY BRIAN L ,  DI JIE ,  GREENBERG MICHAEL ,  HEILMAN DAVID ,  OHMSTEDE CAROL ,  SILINSKI PETER ,  WEBB SCOTT

IPC: A61K9/00

CPC classification number: A61K38/162

Abstract: Provided herein are dosage formulations and dosing regimens of an antiviral peptide therapeutic, including methods of using the same.

Abstract translation: 本文提供了抗病毒肽治疗剂的剂型和给药方案，包括使用它们的方法。

公开(公告)号：WO2007103456A3

公开(公告)日：2008-02-21

申请号：PCT/US2007005858

申请日：2007-03-06

Applicant: TRIMERIS INC ,  LU RONG JIAN ,  PICKENS JASON C ,  TUCKER JOHN ALAN ,  ZINEVITCH TANYA ,  SVIRIDOV SERGEY ,  KONOPLEV VITALI

Inventor： LU RONG JIAN ,  PICKENS JASON C ,  TUCKER JOHN ALAN ,  ZINEVITCH TANYA ,  SVIRIDOV SERGEY ,  KONOPLEV VITALI

IPC: C07D213/61 ,  C07D231/12 ,  C07D239/26 ,  C07D239/46 ,  C07D249/06 ,  C07D257/04 ,  C07D263/32 ,  C07D277/28 ,  C07D285/06 ,  C07D295/22 ,  C07D307/52 ,  C07D333/22 ,  C07D333/28 ,  C07D333/34 ,  C07D401/04

CPC classification number: C07D263/32 ,  C07D213/61 ,  C07D231/12 ,  C07D239/26 ,  C07D239/47 ,  C07D249/06 ,  C07D257/04 ,  C07D277/28 ,  C07D285/06 ,  C07D295/26 ,  C07D307/52 ,  C07D333/22 ,  C07D333/28 ,  C07D333/34 ,  C07D401/04 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/14 ,  C07D495/04

Abstract: This invention relates to piperazine and piperidine biaryl compounds of Formula (I) or a pharmaceutically acceptable prodrug, salt, polymorph, solvate, enantiomer, diastereomer, racemate, mixture of stereoisomers thereof, or derivative thereof; and to processes for preparing the compounds or pharmaceutical compositions containing the same. The compounds and pharmaceutical compositions of the present invention are provided for use in the treatment of HIV infection and/or AIDS.

Abstract translation: 本发明涉及式（I）的哌嗪和哌啶联芳基化合物或其药学上可接受的前药，盐，多晶型物，溶剂合物，对映异构体，非对映体，外消旋体，其立体异构体或其衍生物的混合物; 以及制备含有其的化合物或药物组合物的方法。 提供本发明的化合物和药物组合物用于治疗HIV感染和/或AIDS。

公开(公告)号：WO2006105201A3

公开(公告)日：2006-10-05

申请号：PCT/US2006/011474

申请日：2006-03-28

Applicant: TRIMERIS, INC. ,  WRING, Stephen ,  FRICK, Lloyd ,  SCHNEIDER, Stephen ,  ZHANG, Huyi ,  DI, Jie ,  HEILMAN, David

Inventor： WRING, Stephen ,  FRICK, Lloyd ,  SCHNEIDER, Stephen ,  ZHANG, Huyi ,  DI, Jie ,  HEILMAN, David

IPC: C07K5/00

Abstract: Provided is a conjugate comprised of HIV gp41 -derived peptide operatively linked to fatty acid, and pharmaceutical compositions and medicaments containing the conjugate. Also provided are methods for producing a conjugate according to the present invention which include, but are not limited to, covalently coupling a linker to the HIV gp41 -derived peptide, wherein the linker is covalently coupled to fatty acid.

公开(公告)号：WO2006105199A3

公开(公告)日：2006-10-05

申请号：PCT/US2006/011470

申请日：2006-03-28

Applicant: TRIMERIS, INC. ,  SCHNEIDER, Stephen ,  MADER, Catherine, J. ,  BRAY, Brian ,  TVERMOES, Nicolai ,  ZHANG, Huyi

Inventor： SCHNEIDER, Stephen ,  MADER, Catherine, J. ,  BRAY, Brian ,  TVERMOES, Nicolai ,  ZHANG, Huyi

IPC: A61K38/00

Abstract: Provided are peptide fragments which may be used in a method of producing a synthetic peptide, or a conjugate comprised of the synthetic peptide operatively linked to fatty acid, wherein the method comprises chemically coupling 2 or more peptide fragments together in a process of assembly to produce the synthetic peptide or conjugate.

公开(公告)号：WO9959615A9

公开(公告)日：2000-06-22

申请号：PCT/US9911219

申请日：1999-05-20

Applicant: TRIMERIS INC

Inventor： BARNEY SHAWN ,  GUTHRIE KELLY I ,  MERUTKA GENE ,  ANWER MOHMED K ,  LAMBERT DENNIS M

IPC: A61K38/00 ,  A61K38/02 ,  A61K38/08 ,  A61K38/10 ,  A61K38/16 ,  A61K38/18 ,  A61K38/19 ,  A61K38/22 ,  A61K47/48 ,  A61P31/04 ,  A61P31/12 ,  A61P31/16 ,  A61P31/18 ,  A61P37/02 ,  A61P43/00 ,  C07K5/113 ,  C07K5/117 ,  C07K7/06 ,  C07K7/08 ,  C07K14/00 ,  C07K14/135 ,  C07K14/16 ,  C07K14/59 ,  C07K19/00

CPC classification number: C07K14/005 ,  A61K38/00 ,  A61K47/62 ,  C07K5/1021 ,  C07K5/1024 ,  C07K14/59 ,  C07K2319/00 ,  C12N2740/16122 ,  C12N2760/18522

Abstract: The present invention relates to enhancer peptide sequences originally derived from various retroviral envelope (gp41) protein sequences that enhance the pharmacokinetic properties of any core polypeptide to which they are linked. The invention is based on the discovery that hybrid polypeptides comprising the enhancer peptide sequences linked to a core polypeptide possess enhanced pharmacokinetic properties such as increased half life. The invention further relates to methods for enhancing the pharmacokinetic properties of any core polypeptide through linkage of the enhancer peptide sequences to the core polypeptide. The core polypeptides to be used in the practice of the invention can include any pharmacologically useful peptide that can be used, for example, as a therapeutic or prophylactic reagent.

Abstract translation: 本发明涉及最初衍生自增强其所连接的核心多肽的药代动力学性质的各种逆转录病毒包膜（gp41）蛋白质序列的增强子肽序列。 本发明基于以下发现：包含与核心多肽连接的增强子肽序列的杂合多肽具有增强的药代动力学性质，例如增加的半衰期。 本发明还涉及通过将增强子肽序列与核心多肽连接来增强任何核心多肽的药代动力学性质的方法。 用于本发明实践的核心多肽可包括可用于例如治疗或预防试剂的任何药理学上有用的肽。