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    CRFR1 selective ligands
    1.
    发明授权
    CRFR1 selective ligands 有权
    CRFR1选择性配体

    公开(公告)号：US07851588B2

    公开(公告)日：2010-12-14

    申请号：US12366816

    申请日：2009-02-06

    申请人： Jean E. F. Rivier ,  Wylie W. Vale, Jr. ,  Marilyn H. Perrin ,  Jozsef Gulyas

    发明人： Jean E. F. Rivier ,  Wylie W. Vale, Jr. ,  Marilyn H. Perrin ,  Jozsef Gulyas

    IPC分类号： A61K38/12

    CPC分类号： C07K14/47 ,  A61K38/00 ,  C07K14/57509

    摘要： CRF peptide analogs that bind to CRFR1 with an affinity far greater than they bind to CRFR2. Some of these analogs exhibit CRF agonist activity. One exemplary analog that may be made by solid-phase synthesis is:(cyclo 31-34)[Ac-Pro4,D-Phe12,Nle18,21,Glu31,Lys34]-sucker urotensin(4-41).

    摘要翻译： 结合CRFR1的CRF肽类似物的亲和力远远大于它们与CRFR2结合的亲和力。 这些类似物中的一些表现出CRF激动剂活性。 可以通过固相合成制备的一个示例性类似物是：（环31-34）[Ac-Pro4，D-Phe12，Nle18,21，Glu31，Lys34]刺激性尿素转运蛋白（4-41）。

    Urocortin peptides, nucleic acid encoding same methods for using same
    3.
    发明授权
    Urocortin peptides, nucleic acid encoding same methods for using same 失效
    尿细胞肽，核酸编码方法相同

    公开(公告)号：US06214797B1

    公开(公告)日：2001-04-10

    申请号：US08981189

    申请日：1997-12-10

    申请人： Wylie W. Vale, Jr. ,  Joan Vaughan ,  Cynthia J. Donaldson ,  Kathy A. Lewis ,  Paul Sawchenko ,  Jean E. F. Rivier ,  Marilyn H. Perrin

    发明人： Wylie W. Vale, Jr. ,  Joan Vaughan ,  Cynthia J. Donaldson ,  Kathy A. Lewis ,  Paul Sawchenko ,  Jean E. F. Rivier ,  Marilyn H. Perrin

    IPC分类号： A61K3817

    CPC分类号： C07K14/57509 ,  A61K38/00

    摘要： Urocortin (Ucn) is a native mammalian peptide generally related to Urotensin I and Corticotropin Releasing Factor (CRF). Human Ucn has the formula: Asp-Asn-Pro-Ser-Leu-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Thr-Leu-Leu-Glu-Leu-Ala-Arg-Thr-Gln-Ser-Gln-Arg-Glu-Arg-Ala-Glu-Gln-Asn-Arg-Ile-Ile-Phe-Asp-Ser-Val-NH2 (SEQ ID NO:15). Rat-derived Ucn is identical but for 2 substitutions, Asp2 for Asn2 and Pro4 for Ser4. Ucn or analogs thereof or pharmaceutically acceptable salts can be administered to humans and other mammals to achieve substantial elevation of ACTH, &bgr;-endorphin, &bgr;-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone. They can also be used to lower blood pressure over an extended period of time, as stimulants to elevate mood and to improve memory and learning performance, as well as diagnostically. Shortened fragments may be administered to release endogenous CRF and/or Ucn in the brain and peripherally. Ucn antagonists can be used to block the action of Ucn and/or CRF, as can antibodies to Ucn. Labelled Ucn agonists and antagonists can be used in drug screening assays along with CRF receptors; they may also be used diagnostically along with Ucn antibodies.

    摘要翻译： Urocortin（Ucn）是通常与促进素I和促皮质素释放因子（CRF）相关的天然哺乳动物肽。 人Ucn具有下式：Asp-Asn-Pro-Ser-Leu-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Thr-Leu-Leu-Glu-Leu-Ala-Arg- Thr-Gln-Ser-Gln-Arg-Glu-Arg-Ala-Glu-Gln-Asn-Arg-Ile-Ile-Phe-Asp-Ser-Val-NH2（SEQ ID NO：15）。 大鼠衍生的Ucn是相同的，但是对于2个取代，As 2的Asp 2和Ser 4的Pro 4。 可以将Ucn或其类似物或药学上可接受的盐施用于人和其它哺乳动物，以实现ACTH，β-内啡肽，β-促脂解素，前 - 肌内注射皮质酮基因和皮质酮的其它产物的显着升高。 它们也可用于在较长时间内降低血压，作为兴奋剂提高心情，提高记忆力和学习表现以及诊断。 可以施用缩短的片段以释放脑中和外周的内源性CRF和/或Ucn。 Ucn拮抗剂可用于阻断Ucn和/或CRF的作用，以及Ucn的抗体。 标记的Uc激动剂和拮抗剂可与CRF受体一起用于药物筛选测定; 它们也可以与Ucn抗体一起在诊断上使用。

    Melanin-concentrating hormones
    6.
    发明授权
    Melanin-concentrating hormones 失效
    黑色素浓缩激素

    公开(公告)号：US5049655A

    公开(公告)日：1991-09-17

    申请号：US326984

    申请日：1989-03-22

    申请人： Joan Vaughan ,  Wolfgang H. Fischer ,  Jean E. F. Rivier ,  Jean-Louis M. Nahon ,  Francoise G. Presse ,  Wylie W. Vale, Jr.

    发明人： Joan Vaughan ,  Wolfgang H. Fischer ,  Jean E. F. Rivier ,  Jean-Louis M. Nahon ,  Francoise G. Presse ,  Wylie W. Vale, Jr.

    IPC分类号： C12N15/09 ,  A61K38/00 ,  A61K38/04 ,  A61P35/00 ,  C07K7/06 ,  C07K7/08 ,  C07K7/64 ,  C07K14/00 ,  C07K14/575 ,  C12N15/12 ,  C12N15/16

    CPC分类号： C07K7/08 ,  C07K7/64 ,  A61K38/00 ,  Y10S530/827 ,  Y10S530/854

    摘要： Mammalian melanin-concentrating hormone (MCH) is isolated from rat tissue, purified and characterized. These MCH peptides are useful for treating skin disorders, for suppressing the proliferation of skin tumor cells, such as melanomas in mammals, and for modulating the secretion of ACTH. Generally, peptides are provided which have the following formula: ##STR1## or which are naturally occurring homologs of the peptide with said formula. The peptides which are the naturally occurring MCH homologs of mammalian species other than rat can also be obtained using the materials disclosed, as demonstrated specifically with human MCH, which is found to have the same structure as rat MCH. Also disclosed are the amino acid sequences of, and the nucleotide sequences of the cDNAs which encode, the putative precursors of rat MCH and human MCH. These precursors may also include one or more biologically active peptides N-terminally of the mature MCH's. Among these peptides, which are thought to be formed from the MCH precursors, are the peptide with the sequence H-Glu-Ile-Gly-Asp-Glu-Glu-Asn-Ser-Ala-Lys-Phe-Pro-Ile-NH.sub.2, which is cross-reactive with antibodies against alpha-MSH and CRF, and the peptide with the sequence H-Gly-X.sub.NGE -Phe-Pro-Ala-Glu-Asn-Gly-Val-Gln-Asn-Thr-Glu-Ser-Thr-Gln-Glu-OH, wherein X.sub.NGE is Pro-Ala-Val or Ser-Val-Ala, which is cross-reactive with antibodies against GRF.

    摘要翻译： 从大鼠组织中分离哺乳动物黑色素浓缩激素（MCH），进行纯化和表征。 这些MCH肽可用于治疗皮肤病症，抑制皮肤肿瘤细胞增殖，如哺乳动物的黑素瘤，以及调节ACTH的分泌。 通常，提供具有下式的肽：＆lt; IMAGE＆gt;或具有所述式的肽的天然存在同系物。 作为除大鼠之外的哺乳动物物种的天然存在的MCH同源物的肽也可以使用公开的材料获得，如用人MCH特异性证实的，其被发现具有与大鼠MCH相同的结构。 还公开了编码大鼠MCH和人MCH的推定前体的cDNA的氨基酸序列和cDNA的核苷酸序列。 这些前体还可以包括成熟MCH的N-末端的一种或多种生物活性肽。 在这些被认为由MCH前体形成的肽中，具有序列H-Glu-Ile-Gly-Asp-Glu-Glu-Asn-Ser-Ala-Lys-Phe-Pro-Ile-NH 2的肽 ，其与抗α-MSH和CRF的抗体具有交叉反应性，并且具有序列H-Gly-XNGE-Phe-Pro-Ala-Glu-Asn-Gly-Val-Gln-Asn-Thr-Glu-Ser -Thr-Gln-Glu -OH，其中XNGE是Pro-Ala-Val或Ser-Val-Ala，其与抗GRF的抗体交叉反应。

    Human inhibin
    7.
    发明授权
    Human inhibin 失效
    人抑制素

    公开(公告)号：US4737578A

    公开(公告)日：1988-04-12

    申请号：US848924

    申请日：1986-04-07

    申请人： Ronald M. Evans ,  Michael G. Rosenfeld ,  Gail Cerelli ,  Kelly E. Mayo ,  Joachim Spiess ,  Jean E. F. Rivier ,  Wylie W. Vale, Jr.

    发明人： Ronald M. Evans ,  Michael G. Rosenfeld ,  Gail Cerelli ,  Kelly E. Mayo ,  Joachim Spiess ,  Jean E. F. Rivier ,  Wylie W. Vale, Jr.

    IPC分类号： A61K38/00 ,  C07K14/575 ,  C07K7/10 ,  C07K13/00

    CPC分类号： C07K14/575 ,  A61K38/00 ,  Y10S930/26

    摘要： Proteins with inhibin activity having a weight of about 32,000 daltons. The molecule is composed of two chains having molecular weights of about 18,000 and about 14,000 daltons, respectively, which are bound together by disulfide bonding. The 18K chain is obtained from the human inhibin gene and has the formula: H-Ser-Thr-Pro-Leu-Met-Ser-Trp-Pro-Trp-Ser-Pro-Ser-Ala-Leu-Arg-Leu-Leu-Gln-Arg-Pro-Pro-Glu-Glu-Pro-Ala-Ala-His-Ala-Asn-Cys-His-Arg-Val-Ala-Leu-Asn-Ile-Ser-Phe-Gln-Glu-Leu-Gly-Trp-Glu-Arg-Trp-Ile-Val-Tyr-Pro-Pro-Ser-Phe-R.sub.65 -Phe-His-Tyr-Cys-His-Gly-Gly-Cys-Gly-Leu-His-Ile-Pro-Pro-Asn-Leu-Ser-Leu-Pro-Val-Pro-Gly-Ala-Pro-Pro-Thr-Pro-Ala-Gln-Pro-Tyr-Ser-Leu-Leu-Pro-Gly-Ala-Gln-Pro-Cys-Cys-Ala-Ala-Leu-Pro-Gly-Thr-Met-Arg-Pro-Leu-His-Val-Arg-Thr-Thr-Ser-Asp-Gly-Gly-Tyr-Ser-P e-Lys-Tyr-Glu-Thr-Val-Pro-Asn-Leu-Leu-Thr-Gln-His-Cys-Ala-Cys-Ile-OH, wherein R.sub.65 is Ile or Arg. The 18K chain is connected by disulfide bonding to the 14K chain.

    摘要翻译： 具有约32,000道尔顿重量的具有抑制素活性的蛋白质。 该分子由分子量分别为约18,000和约14,000道尔顿的两条链组成，它们通过二硫键结合在一起。 18K链由人抑制素基因得到，具有下式：H-Ser-Thr-Pro-Leu-Met-Ser-Trp-Pro-Trp-Ser-Pro-Ser-Ala-Leu-Arg-Leu-Leu Gln-Arg-Pro-Pro-Glu-Glu-Pro-Ala-Ala-His-Ala-Asn-Cys-His-Arg-Val-Ala-Le-Asn-Ile-Ser-Phe-Gln-Glu- Leu-Gly-Trp-Glu-Arg-Trp-Ile-Val-Tyr-Pro-Pro-Ser-Phe-R65-Phe-His-Tyr-Cys-His-Gly-Gly-Cys-Gly-Leu-His- Ile-Pro-Pro-As n-Leu-Ser-Leu-Pro-Val-Pro-Gly-Ala-Pro-Pro-Thr-Pro-Ala-Gln-Pro-Tyr-Ser-Leu-Leu-Pro-Gly -Ala-Gln-Pro-Cys-Cys-Ala-Ala-Leu-Pro-Gly-Thr-Met-Arg-Pr-Leu-His-Val-Arg-Thr-Thr-Ser-Asp-Gly-Gly- Tyr-Ser-P e-Lys-Tyr-Glu-Thr-Val-Pro-Asn-Leu-Leu-Thr-Gln-His-Cys-Ala-Cys-Ile-OH，其中R65是Ile或Arg。 18K链通过二硫键与14K链连接。

    Peptides containing an aliphatic-aromatic ketone side chain
    8.
    发明授权
    Peptides containing an aliphatic-aromatic ketone side chain 失效
    含有脂肪族 - 芳香族酮侧链的肽

    公开(公告)号：US4677193A

    公开(公告)日：1987-06-30

    申请号：US704299

    申请日：1985-02-22

    申请人： Jean E. F. Rivier ,  Harry A. Anderson ,  Wylie W. Vale, Jr.

    发明人： Jean E. F. Rivier ,  Harry A. Anderson ,  Wylie W. Vale, Jr.

    IPC分类号： A61K38/04 ,  A61K38/00 ,  A61K38/22 ,  A61P5/00 ,  C07K1/113 ,  C07K7/06 ,  C07K7/23 ,  C07K14/00 ,  C07K14/575 ,  C07K7/20

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

    摘要： GnRH peptide analogs which regulate the secretion of gonadotropins by the pituitary gland and either promote or inhibit the release of steroids by the gonads. Administration of an effective amount of a GnRH antagonist prevents ovulation of female mammalian eggs and/or the release of gonadotropins. Administration of GnRH agonists can be used to regulate fertility in male and female mammals.These and other peptide hormones exhibit improved binding efficiency and biological potency as a result having a residue in a critical, generally central location in the chain which residue contains a mixed alkyl ketone side-chain terminating in an aromatic group. Methods for efficiently synthesizing these peptides from readily available compounds are disclosed.

    摘要翻译： GnRH肽类似物，其调节垂体分泌促性腺激素并促进或抑制性腺释放类固醇。 施用有效量的GnRH拮抗剂可防止雌性哺乳动物卵的排卵和/或释放促性腺激素。 GnRH激动剂的施用可用于调节雄性和雌性哺乳动物的生育力。 这些和其它肽激素表现出改善的结合效率和生物效力，因此在链中的关键的，通常中心的位置具有残基，残基含有终止于芳族基团的混合烷基酮侧链。 公开了从容易获得的化合物有效地合成这些肽的方法。

    CRF analogs
    9.
    发明授权
    CRF analogs 失效
    CRF类似物

    公开(公告)号：US4594329A

    公开(公告)日：1986-06-10

    申请号：US610110

    申请日：1984-05-14

    申请人： Wylie W. Vale, Jr. ,  Jean E. F. Rivier

    发明人： Wylie W. Vale, Jr. ,  Jean E. F. Rivier

    IPC分类号： A61K38/00 ,  C07K14/575 ,  C07K7/00 ,  A61K37/02

    CPC分类号： C07K14/57509 ,  A61K38/00 ,  Y10S436/817

    摘要： Analogs of rCRF and oCRF are disclosed that can be administered to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or a lowering of blood pressure over an extended period of time. One analog which has been found to be particularly potent is: H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Met-Leu-Glu-Met-Ala-Lys-Ala-Glu-Gln-Glu-Ala-Glu-Gln-Ala-Ala-Leu-Asn-Arg-Leu-Leu-Leu-Glu-Glu-Ala-NH.sub.2. In the analogs, one or more of the first five N-terminal residues may be deleted or may be substituted by a peptide up to 10 amino acids long and/or by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. These analogs or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier, can be administered to mammals, including humans. These analogs may also be used as stimulants to elevate mood and improve memory and learning, as well as diagnostically.

    摘要翻译： 公开了rCRF和oCRF的类似物，其可被施用以实现ACTH，β-内啡肽，β-促肌动蛋白，前 - 肌动蛋白皮质素基因的其他产物和皮​​质酮水平的显着升高和/或延长期间的血压降低 的时间。 已经发现特别有效的一种类似物是：H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu- Leu-Glu-Met-Ala-Lys-Ala-Glu-Gln-Glu-Ala-Glu-Gln-Ala-Ala-Leu-Asn -Arg-Leu-Leu-Leu-Glu-Glu-Ala-NH2。 在类似物中，前五个N-末端残基中的一个或多个可以被缺失或可被长达10个氨基酸的肽和/或被含有至多7个碳原子的酰化剂所取代。 还可以在整个链中进行许多其它取代。 分散在药学上或兽医学上可接受的液体或固体载体中的这些类似物或其药学或兽医学上可接受的盐可以施用于哺乳动物，包括人。 这些类似物也可以用作兴奋剂以提高心情，改善记忆和学习以及诊断。