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    ANTIVIRAL PEPTIDES
    2.
    发明申请
    ANTIVIRAL PEPTIDES 审中-公开
    抗病毒肽

    公开(公告)号：WO1995015766A1

    公开(公告)日：1995-06-15

    申请号：PCT/US1994013950

    申请日：1994-12-06

    Applicant: HOUGHTEN PHARMACEUTICALS, INC.

    Inventor： HOUGHTEN PHARMACEUTICALS, INC. ,  HOUGHTEN, Richard, A. ,  WEBER, Patricia, A.

    IPC: A61K38/08

    CPC classification number: C07K7/06 ,  A61K38/00 ,  A61L2/0082 ,  A61L2/16 ,  C12N7/04

    Abstract: The present invention provides antiviral peptides having the general structure, Arg - Arg - Trp - Trp - Cys - Arg - X, where X is an amino acid or an amino acid analog, the stereochemistry of the amino acids or amino acid analogs can be (D)- or (L)-amino acids and the amino and carboxy termini of the peptide can be modified. The invention also provides a pharmaceutical composition comprising an antiviral peptide and methods of using an antiviral peptide in vitro or in vivo to reduce or inhibit a viral infection.

    Abstract translation: 本发明提供具有通式结构的抗病毒肽Arg-Arg-Trp-Trp-Cys-Arg-X，其中X是氨基酸或氨基酸类似物，氨基酸或氨基酸类似物的立体化学可以是 D） - 或（L） - 氨基酸，并且肽的氨基和羧基末端可以被修饰。 本发明还提供了包含抗病毒肽的药物组合物和在体外或体内使用抗病毒肽来减少或抑制病毒感染的方法。

    CYTOKINE REGULATORY AGENTS AND METHODS OF USE IN PATHOLOGIES AND CONDITIONS ASSOCIATED WITH ALTERED CYTOKINE LEVELS
    3.
    发明申请
    CYTOKINE REGULATORY AGENTS AND METHODS OF USE IN PATHOLOGIES AND CONDITIONS ASSOCIATED WITH ALTERED CYTOKINE LEVELS 审中-公开
    细胞因子调节剂和与改变的细胞因子水平相关的病理学和条件的使用方法

    公开(公告)号：WO1996027386A1

    公开(公告)日：1996-09-12

    申请号：PCT/US1996003112

    申请日：1996-03-05

    Applicant: HOUGHTEN PHARMACEUTICALS, INC.

    Inventor： HOUGHTEN PHARMACEUTICALS, INC. ,  GIRTEN, Beverly, E. ,  ANDABLIBI, Ali ,  BASU, Amaresh ,  FAGAN, Patrick ,  HOUGHTEN, Richard, A. ,  LOULLIS, Costas, C. ,  OMHOLT, Paul ,  SUTO, Mark, J. ,  WEBER, Patricia, A. ,  TUTTLE, Ronald, R.

    IPC: A61K38/00

    CPC classification number: C07K14/695 ,  A61K38/00 ,  C07K5/0812 ,  C07K5/1024 ,  C07K14/68

    Abstract: The present invention relates to novel peptides that are potent cytokine regulatory agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a cytokine regulatory agent. Administration of such a cytokine regulatory agent to a subject can enhance or restrain cytokine activity. Thus, the present invention provides a method of regulating cytokine activity in a subject having a condition characterized by aberrant or altered cytokine activity. The invention also provides methods of treating such conditions, including, for example, disuse deconditioning, diseases mediated by nitric oxide and cytokines, adverse drug reactions, obesity, septic shock, and adverse side effects due to cancer chemotherapy or occurring as in response to organ transplantation.

    Abstract translation: 本发明涉及有效的细胞因子调节剂的新型肽。 此外，本发明涉及包含药学上可接受的载体和细胞因子调节剂的药物组合物。 向受试者施用这样的细胞因子调节剂可以增强或抑制细胞因子活性。 因此，本发明提供一种调节受试者中细胞因子活性的方法，其特征在于异常或改变的细胞因子活性。 本发明还提供了治疗这些病症的方法，包括例如废除解毒，由一氧化氮和细胞因子介导的疾病，药物不良反应，肥胖症，败血性休克以及由于癌症化学疗法或作为对器官的反应而发生的不良副作用 移植。

    PERALKYLATED OLIGOPEPTIDE MIXTURES
    4.
    发明申请
    PERALKYLATED OLIGOPEPTIDE MIXTURES 审中-公开
    PERALKYLATED OLIGEPEPTIDE MIXTURES

    公开(公告)号：WO1995000539A1

    公开(公告)日：1995-01-05

    申请号：PCT/US1994006554

    申请日：1994-06-10

    Applicant: HOUGHTEN PHARMACEUTICALS, INC.

    Inventor： HOUGHTEN PHARMACEUTICALS, INC. ,  HOUGHTEN, Richard A. ,  OSTRESH, John, M. ,  BLONDELLE, Sylvie

    IPC: C07K07/00

    CPC classification number: C07K1/04 ,  C07K1/12 ,  C12Q1/18

    Abstract: Linear C1-C7-alkyl peralkylated oligopeptide sets of molecules are disclosed, as are their methods of synthesis and use in acceptor binding assays. Each molecule or chain of a set contains the same number of two to about ten substituted C1-C7-alkyl peralkylated amino acid residues, and the member chains of a set are present in equimolar amounts. The chains of a set contain one or more predetermined peralkylated amino acid residues at one or more predetermined positions of the peralkylated oligopeptide chain. The set contains equimolar amounts of at least six different peralkylated amino acid residues at one or more of the same predetermined positions of the peralkylated oligopeptide chain. Libraries of such sets, processes for their use and solid support-linked peralkylated sets are also contemplated, as are specific permethylated oligopeptides.

    Abstract translation: 公开了线性C 1 -C 7烷基全烷基化寡肽组分子，以及其在受体结合测定中的合成和使用方法。 一组的每个分子或链含有相同数量的两个至约十个取代的C 1 -C 7烷基全烷基化氨基酸残基，并且一组的成员链以等摩尔量存在。 一组的链在全烷基化寡肽链的一个或多个预定位置含有一个或多个预定的全烷基化氨基酸残基。 该组在全烷基化寡肽链的一个或多个相同的预定位置含有等摩尔量的至少六个不同的烷基化氨基酸残基。 这些组的文库，它们的使用方法和固体支持物连接的烷基化组也被考虑，特定的甲基化寡肽也是如此。

    PROTECTED BIOPOLYMERS FOR ORAL ADMINISTRATION AND METHODS OF USING SAME
    6.
    发明申请
    PROTECTED BIOPOLYMERS FOR ORAL ADMINISTRATION AND METHODS OF USING SAME 审中-公开
    用于口腔管理的保护性生物降解剂及其使用方法

    公开(公告)号：WO1997022356A1

    公开(公告)日：1997-06-26

    申请号：PCT/US1996020378

    申请日：1996-12-18

    Applicant: HOUGHTEN PHARMACEUTICALS, INC.

    Inventor： HOUGHTEN PHARMACEUTICALS, INC. ,  MANIAR, Manoj ,  MAUCH, Steven

    IPC: A61K38/00

    CPC classification number: A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/585

    Abstract: The present invention provides a composition comprising an ion exchange resin and a therapeutically active biopolymer in a form for oral administration. The present invention also provides a composition comprising Amberlite3 IRP-64 and a cytokine regulatory agent having the amino acid sequence Ac-Nle-Gln-His-(D)Phe-Arg-(D)Trp-Gly-NH2, in a form for oral administration. The present invention further provides a method of protecting a therapeutically active biopolymer from degradation by forming a complex of the biopolymer and an ion exchange resin. In addition, the present invention provides a method of reducing or inhibiting the severity of a pathological condition by orally administering a therapeutically effective dose of the composition.

    Abstract translation: 本发明提供包含离子交换树脂和用于口服给药形式的治疗活性生物聚合物的组合物。 本发明还提供了包含Amberlite3 IRP-64和具有氨基酸序列Ac-Nle-Gln-His-（D）Phe-Arg-（D）Trp-Gly-NH 2）的细胞因子调节剂的组合物，其形式为 口服。 本发明还提供了通过形成生物聚合物和离子交换树脂的复合物来保护治疗活性生物聚合物免于降解的方法。 此外，本发明提供通过口服施用治疗有效剂量的组合物来减少或抑制病理状况的严重性的方法。

    DIMERIC OLIGOPEPTIDE MIXTURE SETS
    7.
    发明申请
    DIMERIC OLIGOPEPTIDE MIXTURE SETS 审中-公开
    二聚体寡聚体混合物

    公开(公告)号：WO1995014929A1

    公开(公告)日：1995-06-01

    申请号：PCT/US1994013513

    申请日：1994-11-21

    Applicant: HOUGHTEN PHARMACEUTICALS, INC.

    Inventor： HOUGHTEN PHARMACEUTICALS, INC. ,  HOUGHTEN, Richard, A. ,  PINILLA, Clemencia

    IPC: G01N33/53

    CPC classification number: C40B30/04 ,  C07K1/047 ,  G01N33/54306 ,  G01N33/6845

    Abstract: Dimeric oligopeptide mixture sets, their synthesis and use in determining the sequence of an oligopeptide dimer ligand that optimally binds to a receptor are disclosed. A dimeric oligopeptide mixture set has two oligopeptide portions bonded together by a disulfide bond. Each oligopeptide of a first oligopeptide portion has the same number of 3 to about 10 residues including an oxidized mercaptan-containing residue that forms part of the disulfide bond and an amino acid residue sequence that includes at least one of at least six residues in addition to the oxidized mercaptan-containing residue at the same one or more predetermined positions of the oligopeptide chain. The second portion has an oligopeptide chain having a length of 4 to about 10 residues, including an oxidized mercaptan-containing residue that forms part of the disulfide bond. The second portion is a mixture whose chains have equimolar amounts of those at least six amino acid residues at the same one or more other positions of the oligopeptide chain.

    Abstract translation: 公开了二聚寡肽混合物组合及其在确定最佳结合受体的寡肽二聚体配体序列中的用途。 二聚寡肽混合物组具有通过二硫键结合在一起的两个寡肽部分。 第一寡肽部分的每个寡肽具有相同数量的3至约10个残基，包括形成二硫键的一部分的含氧化的含硫醇的残基和包含至少6个残基中的至少一个的氨基酸残基序列， 在寡肽链的相同一个或多个预定位置上含氧化的含硫醇的残基。 第二部分具有长度为4至约10个残基的寡肽链，包括形成二硫键的一部分的含氧化的含硫醇的残基。 第二部分是其链在寡肽链的相同一个或多个其它位置具有等摩尔量的那些至少6个氨基酸残基的混合物。

    LINEAR SUBSTITUTED OLIGOALKYLENEIMINE LIBRARIES
    9.
    发明申请
    LINEAR SUBSTITUTED OLIGOALKYLENEIMINE LIBRARIES 审中-公开
    线性取代的寡聚二乙烯基化合物

    公开(公告)号：WO1994026775A1

    公开(公告)日：1994-11-24

    申请号：PCT/US1994005335

    申请日：1994-05-13

    Applicant: HOUGHTEN PHARMACEUTICALS, INC.

    Inventor： HOUGHTEN PHARMACEUTICALS, INC. ,  HOUGHTEN, Richard, A. ,  CUERVO, Julio, Hernan ,  WEITL, Fred, F.

    IPC: C07K07/02

    CPC classification number: C07K1/047 ,  B01J19/0046 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  B01J2219/00596 ,  B01J2219/00725 ,  C40B40/10

    Abstract: Linear substituted oligoalkyleneimine molecules and libraries of molecules are disclosed, as are their methods of synthesis and use in acceptor binding assays. Each molecule or chain of a library contains the same number of 2 to about 10 substituted alkyleneimine repeating units, whose substituents are reduced amino acid side chains bonded to the repeating units at a position alpha to the nitrogen atom, and the member chains of a library are present in equimolar amounts. The chains of a library contain one or more predetermined reduced amino acid side chain-substituted repeating units at one or more predetermined positions of the substituted oligoalkyleneimine chain. The library contains equimolar amounts of at least six different reduced amino acid side chain-substituted repeating units at one or more of the same predetermined positions of the substituted oligoalkyleneimine chain. Particularly preferred linear substituted oligoalkyleneimine molecules and libraries are linear substituted oligoethyleneimines.

    Abstract translation: 公开了线性取代的低聚亚烷基亚胺分子和分子文库，以及其在受体结合测定中的合成和使用方法。 文库的每个分子或链包含相同数量的2至约10个取代的亚烷基亚胺重复单元，其取代基是与氮原子的α位置的重复单元键合的氨基酸侧链，并且文库的成员链 以等摩尔量存在。 文库的链在取代的低聚亚烷基亚胺链的一个或多个预定位置含有一个或多个预定的还原氨基酸侧链取代的重复单元。 该文库在取代的低聚亚烷基亚胺链的一个或多个相同的预定位置包含等摩尔量的至少六个不同的还原氨基酸侧链取代的重复单元。 特别优选的线性取代的低聚亚烷基亚胺分子和文库是线性取代的低聚亚乙基亚胺。

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