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    Cytokine restraining agents and methods of use in pathologies and conditions associated with altered cytokine levels
    4.
    发明授权
    Cytokine restraining agents and methods of use in pathologies and conditions associated with altered cytokine levels 失效
    细胞因子抑制剂和与改变的细胞因子水平相关的病理学和病症中使用的方法

    公开(公告)号：US5760001A

    公开(公告)日：1998-06-02

    申请号：US447143

    申请日：1995-05-22

    申请人： Beverly E. Girten ,  Richard A. Houghten ,  Costas C. Loullis ,  Mark J. Suto ,  Ronald R. Tuttle

    发明人： Beverly E. Girten ,  Richard A. Houghten ,  Costas C. Loullis ,  Mark J. Suto ,  Ronald R. Tuttle

    IPC分类号： A61K38/00 ,  C07K5/087 ,  C07K5/117 ,  C07K7/06 ,  C07K14/68 ,  C07K14/695

    CPC分类号： C07K7/06 ,  C07K14/68 ,  C07K14/695 ,  C07K5/0812 ,  C07K5/1024 ,  A61K38/00

    摘要： The present invention relates to novel peptides that are potent cytokine restraining agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a cytokine restraining agent. Administration of such a cytokine restraining agent to a subject restrains, but does not necessarily suppress, cytokine activity completely. Thus, the present invention provides a method of restraining pathologically elevated cytokine activity in a subject. The invention also provides methods of treating disuse deconditioning and diseases mediated by nitric oxide and cytokines, such as diabetes and glomerulonephritis, a method of organ protection, a method of organ protection, and a method of reducing the negative side effects of cancer chemotherapy, such as nephrotoxicity.

    摘要翻译： 本发明涉及有效的细胞因子抑制剂的新型肽。 此外，本发明涉及包含药学上可接受的载体和细胞因子抑制剂的药物组合物。 对受试者施用这种细胞因子抑制剂抑制，但不一定抑制细胞因子活性。 因此，本发明提供抑制受试者中病理升高的细胞因子活性的方法。 本发明还提供了治疗废用脱毒和由一氧化氮和细胞因子如糖尿病和肾小球肾炎介导的疾病，器官保护方法，器官保护方法和降低癌症化学疗法的负面副作用的方法， 作为肾毒性。

    Melanocortin receptor ligands and methods of using same
    6.
    发明授权
    Melanocortin receptor ligands and methods of using same 失效
    黑皮质素受体配体及其使用方法

    公开(公告)号：US06350430B1

    公开(公告)日：2002-02-26

    申请号：US09027108

    申请日：1998-02-20

    申请人： Colette T. Dooley ,  Beverly E. Girten ,  Richard A. Houghten

    发明人： Colette T. Dooley ,  Beverly E. Girten ,  Richard A. Houghten

    IPC分类号： A61K5100

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/1019 ,  C07K5/1024 ,  C07K5/1027 ,  C07K14/68

    摘要： The invention provides ligands for melanocortin receptors. For example, the invention provides the melanocortin receptor peptide ligand Ac-Nlc-Gln-His-(p(I)-D-Phe)-Arg-(D-Trp)-Cly-NH2, (SEQ ID NO: 1), where the iodo group is unlabeled or radioactively labeled. The invention additionally provides methods of assaying for melanocortin receptors in a cell or tissue such as brain. The invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a melanocortin receptor ligand and to methods of administering the pharmaceutical composition to a subject. The invention further provides tetrapeptide ligands for melanocortin receptors and methods of altering melanocortin receptor activity.

    摘要翻译： 本发明提供黑皮质素受体的配体。 例如，本发明提供黑皮质素受体肽配体Ac-Nlc-Gln-His-（p（I）-D-Phe）-Arg-（D-Trp）-Cly-NH 2，（SEQ ID NO：1） 其中碘基团未标记或放射性标记。 本发明另外提供了测定细胞或组织如脑中黑皮质素受体的方法。 本发明还涉及包含药学上可接受的载体和黑皮质素受体配体的药物组合物以及向受试者施用该药物组合物的方法。 本发明还提供了黑皮质素受体的四肽配体和改变黑皮质素受体活性的方法。

    MU opioid receptor ligands: agonists and antagonists
    10.
    发明授权
    MU opioid receptor ligands: agonists and antagonists 失效
    MU阿片受体配体：激动剂和拮抗剂

    公开(公告)号：US5919897A

    公开(公告)日：1999-07-06

    申请号：US488659

    申请日：1995-06-07

    申请人： Colette T. Dooley ,  Richard A. Houghten

    发明人： Colette T. Dooley ,  Richard A. Houghten

    IPC分类号： A61K38/00 ,  C07K14/665 ,  C07K5/00

    CPC分类号： C07K14/665 ,  A61K38/00

    摘要： The present invention provides novel opioid peptides. Disclosed are opioid peptides having the general structures Ac-Phe-Arg-Trp-Trp-Tyr-Xaa-NH.sub.2 (SEQ ID NO. 1); Ac-Arg-Trp-Ile-Gly-Trp-Xaa-NH.sub.2 (SEQ ID NO. 2); Trp-Trp-Pro-Lys-His-Xaa-NH.sub.2 (SEQ ID NO. 3); and shorter versions of the latter, namely, Trp-Trp-Pro-Xaa-NH.sub.2 (SEQ ID NO. 4); Tyr-Pro-Phe-Gly-Phe-Xaa-NH.sub.2 (SEQ ID NO. 5); (D)Ile-(D)Met-(D)Ser-(D)Trp-(D)Trp-Gly.sub.n -Xaa-NH.sub.2 (SEQ ID NO. 6); and (D)Ile-(D)Met-(D)Thr-(D)Trp-Gly-Xaa-NH.sub.2 (SEQ ID NO. 7). Within each genus, Xaa is substituted by a specific amino acid. The invention also relates to an opioid peptide having the general structure Tyr-A1-B2-C3-NH.sub.2 (SEQ ID NO. 214), wherein A is D-Nve or D-Nle, B is Gly, Phe, or Trp, and C is Trp or Nap. Also included within the invention are opioid peptides of the general structure Me.sub.x H.sub.y N-Tyr-Tyr-Phe.sub.m -Pro.sub.n -NH.sub.2 (SEQ ID NO. 221) which are peptides modified by permethylation, perallylation, perethylation, perbenzylation and/or pernaphthylation and which can be further modified by reduction.

    摘要翻译： 本发明提供新的阿片样肽。 公开了具有通式结构Ac-Phe-Arg-Trp-Trp-Tyr-Xaa-NH 2（SEQ ID NO.1）的阿片样肽。 Ac-Arg-Trp-Ile-Gly-Trp-Xaa-NH 2（SEQ ID NO.2）; Trp-Trp-Pro-Lys-His-Xaa-NH 2（SEQ ID NO.3）; 和较短版本的后者，即Trp-Trp-Pro-Xaa-NH2（SEQ ID NO.4）; Tyr-Pro-Phe-Gly-Phe-Xaa-NH2（SEQ ID NO.5）; （D）Ile-（D）Met-（D）Ser-（D）Trp-（D）Trp-Glyn-Xaa-NH2（SEQ ID NO.6）; 和（D）Ile-（D）Met-（D）Thr-（D）Trp-Gly-Xaa-NH 2（SEQ ID NO.7）。 在每个属中，Xaa被特定的氨基酸取代。 本发明还涉及具有通式结构Tyr-A1-B2-C3-NH2（SEQ ID NO.214）的阿片肽，其中A是D-Nve或D-Nle，B是Gly，Phe或Trp，以及 C是Trp或Nap。 本发明还包括通用结构MexHyN-Tyr-Tyr-Phem-Pron-NH2（SEQ ID NO：221）的阿片肽，其是通过甲基化，过氧化，对乙酰化，过苄化和/或全萘基改性修饰的肽，其可以是 进一步通过减少修改。