公开(公告)号：WO2010039851A9

公开(公告)日：2010-06-24

申请号：PCT/US2009059058

申请日：2009-09-30

Applicant: WYETH LLC ,  BAZHINA NATALIYA ,  DONATO GEORGE JOSEPH ,  FABIAN STEVEN R ,  LOKHNAUTH JOHN ,  MEGATI SREENIVASULU ,  MELUCCI CHARLES ,  OFSLAGER CHRISTIAN ,  PATEL NIKETA ,  RADEBAUGH GALEN ,  SHAH SYED M ,  SZELIGA JAN ,  ZHANG HUYI ,  ZHU TIANMIN

Inventor： BAZHINA NATALIYA ,  DONATO GEORGE JOSEPH ,  FABIAN STEVEN R ,  LOKHNAUTH JOHN ,  MEGATI SREENIVASULU ,  MELUCCI CHARLES ,  OFSLAGER CHRISTIAN ,  PATEL NIKETA ,  RADEBAUGH GALEN ,  SHAH SYED M ,  SZELIGA JAN ,  ZHANG HUYI ,  ZHU TIANMIN

IPC: C07D471/08 ,  A61K31/485 ,  A61P1/10 ,  C07D489/08

CPC classification number: A61K31/485 ,  A61J1/05 ,  A61K9/0019 ,  A61K9/0053 ,  A61K9/08 ,  A61K9/20 ,  A61M5/178 ,  C07D471/08 ,  C07D489/08 ,  Y10T436/145555

Abstract: The present invention provides a compound of formula I wherein X", R1, and R2 are as defined herein, and compositions thereof. The compounds include and are based on an impurity of methylnaltrexone, a peripheral opioid antagonist.

Abstract translation: 本发明提供了其中X“，R 1和R 2如本文所定义的式I化合物及其组合物。该化合物包括并基于甲基纳曲酮，外周阿片样物质拮抗剂的杂质。

公开(公告)号：WO2006105199A2

公开(公告)日：2006-10-05

申请号：PCT/US2006011470

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: C07K1/02

CPC classification number: C07K14/005 ,  A61K47/542 ,  C12N2740/16122

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.

Abstract translation: 提供了可用于制备合成肽的方法的肽片段或由可操作地连接到脂肪酸的合成肽组成的缀合物，其中所述方法包括在组装过程中将2个或更多个肽片段化学偶联在一起，以产生 合成肽或缀合物。

公开(公告)号：WO2009042194A3

公开(公告)日：2009-05-14

申请号：PCT/US2008011147

申请日：2008-09-25

Applicant: TRIMERIS INC ,  BRAY BRIAN L ,  JOHNSTON BARBARA E ,  SCHNEIDER STEPHEN E ,  TVERMOES NICOLAI A ,  ZHANG HUYI ,  FRIEDRICH PAUL E

Inventor： BRAY BRIAN L ,  JOHNSTON BARBARA E ,  SCHNEIDER STEPHEN E ,  TVERMOES NICOLAI A ,  ZHANG HUYI ,  FRIEDRICH PAUL E

IPC: C07K14/16

CPC classification number: C07K14/005 ,  A61K38/00 ,  C07K2319/00 ,  C12N2740/16122

Abstract: Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.

Abstract translation: 本文提供了合成肽的方法。 特别地，本文提供了治疗性抗病毒肽的合成方法。

公开(公告)号：WO2005089796A1

公开(公告)日：2005-09-29

申请号：PCT/US2005/007486

申请日：2005-03-08

Applicant: TRIMERIS, INC. ,  BRAY, Brian ,  ZHANG, Huyi

Inventor： BRAY, Brian ,  ZHANG, Huyi

IPC: A61K39/21

CPC classification number: A61K47/60

Abstract: Provided is a method for site-specific chemical modification of an HIV gp41 -derived peptide, wherein during synthesis one or more amine groups of the HIV gp41 -derived peptide are chosen to blocked by a chemical protecting agent, and one or more amine groups are selected to be unprotected, and remain free to be reacted with an amine reactive functionality. The resultant HIV gp41-derived peptide may be used to produce a substantially homogeneous conjugate comprised of HIV gp41-derived peptide and polymer by covalently coupling the polymer to the one or more free (unprotected) amine groups of the HIV gp41-derived peptide.

Abstract translation: 提供了一种用于HIV gp41衍生肽的位点特异性化学修饰的方法，其中在合成期间，HIV gp41衍生的肽的一个或多个胺基选择为被化学保护剂阻断，并且一个或多个胺基为 选择为未保护的，并保持与胺反应性官能度反应。 所得到的HIV gp41衍生肽可用于通过共价偶联聚合物与HIV gp41衍生肽的一个或多个游离（未受保护）的胺基团来产生由HIV gp41衍生的肽和聚合物组成的基本均匀的缀合物。

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：WO2010039851A1

公开(公告)日：2010-04-08

申请号：PCT/US2009/059058

申请日：2009-09-30

Applicant: WYETH LLC ,  BAZHINA, Nataliya ,  DONATO, George, Joseph ,  FABIAN, Steven, R. ,  LOKHNAUTH, John ,  MEGATI, Sreenivasulu ,  MELUCCI, Charles ,  OFSLAGER, Christian ,  PATEL, Niketa ,  RADEBAUGH, Galen ,  SHAH, Syed, M. ,  SZELIGA, Jan ,  ZHANG, Huyi ,  ZHU, Tianmin

Inventor： BAZHINA, Nataliya ,  DONATO, George, Joseph ,  FABIAN, Steven, R. ,  LOKHNAUTH, John ,  MEGATI, Sreenivasulu ,  MELUCCI, Charles ,  OFSLAGER, Christian ,  PATEL, Niketa ,  RADEBAUGH, Galen ,  SHAH, Syed, M. ,  SZELIGA, Jan ,  ZHANG, Huyi ,  ZHU, Tianmin

IPC: C07D471/08 ,  C07D489/08 ,  A61K31/485 ,  A61P1/10

CPC classification number: A61K31/485 ,  A61J1/05 ,  A61K9/0019 ,  A61K9/0053 ,  A61K9/08 ,  A61K9/20 ,  A61M5/178 ,  C07D471/08 ,  C07D489/08 ,  Y10T436/145555

Abstract: The present invention provides a compound of formula I: wherein X - , R 1 , and R 2 are as defined herein, and compositions thereof. The compounds are peripheral opioid receptors.

Abstract translation: 本发明提供式I化合物：其中X，R 1和R 2如本文所定义，及其组合物。 化合物是周围的阿片受体。

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：WO2009042194A2

公开(公告)日：2009-04-02

申请号：PCT/US2008/011147

申请日：2008-09-25

Applicant: TRIMERIS, INC. ,  BRAY, Brian, L. ,  JOHNSTON, Barbara, E. ,  SCHNEIDER, Stephen, E. ,  TVERMOES, Nicolai, A. ,  ZHANG, Huyi ,  FRIEDRICH, Paul, E.

Inventor： BRAY, Brian, L. ,  JOHNSTON, Barbara, E. ,  SCHNEIDER, Stephen, E. ,  TVERMOES, Nicolai, A. ,  ZHANG, Huyi ,  FRIEDRICH, Paul, E.

IPC: C07K14/16

CPC classification number: C07K14/005 ,  A61K38/00 ,  C07K2319/00 ,  C12N2740/16122

Abstract: Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.

Abstract translation: 本文提供了合成肽的方法。 特别地，本文提供了治疗性抗病毒肽的合成方法。

公开(公告)号：WO2007097903A3

公开(公告)日：2007-08-30

申请号：PCT/US2007/002990

申请日：2007-02-02

Applicant: TRIMERIS, INC. ,  DWYER, John ,  BRAY, Brian, L. ,  SCHNEIDER, Stephen, E. ,  ZHANG, Huyi ,  TVERMOES, Nicolai, A. ,  JOHNSTON, Barbara, E. ,  FRIEDRICH, Paul, E.

Inventor： DWYER, John ,  BRAY, Brian, L. ,  SCHNEIDER, Stephen, E. ,  ZHANG, Huyi ,  TVERMOES, Nicolai, A. ,  JOHNSTON, Barbara, E. ,  FRIEDRICH, Paul, E.

IPC: C07K5/00

Abstract: Provided is an HIV fusion inhibitor peptide having an amino acid sequence of any one of SEQ ID NO:9. SEQ ID NO:10, SEQ ID NO:11, SEQ ID NO:12, SEQ ID NO:13, SEQ ID NO:14, or SEQ ID NO: 15; and provided is a pharmaceutical composition comprising a HIV fusion inhibitor peptide and one or more of a pharmaceutically acceptable carrier and macromolecular carrier, and uses and methods of treatment provided by these compositions.