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    Novel Corticotropin-Releasing Factor Receptor 1 (Crfr1) Agonist
    81.
    发明申请
    Novel Corticotropin-Releasing Factor Receptor 1 (Crfr1) Agonist 审中-公开
    新型促肾上腺皮质激素释放因子受体1（Crfr1）激动剂

    公开(公告)号：US20080221021A1

    公开(公告)日：2008-09-11

    申请号：US10586469

    申请日：2005-01-14

    Applicant: Joachim Spiess ,  Olaf Jahn ,  Hossein Tezval

    Inventor： Joachim Spiess ,  Olaf Jahn ,  Hossein Tezval

    IPC: A61K38/16 ,  C07K14/00 ,  C07H21/04 ,  C12N15/64 ,  A61K31/7088 ,  A61P25/24 ,  A61P5/06 ,  A61P25/00

    CPC classification number: C07K14/705 ,  A61K38/00 ,  C07K14/57509

    Abstract: The present invention relates to a compound which is highly selective for CRFR1 without having any significant cross-reactivity for corticotropin-releasing-factor-receptor-2 (CRFR2) and/or corticotropin-releasing-factor-binding protein (CRFBP), said compound comprising or alternatively consisting of the amino acid sequence as depicted in SEQ ID No: 1. In another aspect, the present invention relates to a pharmaceutical and/or diagnostic composition comprising the novel CRFR1 agonist of the present invention. The present invention also provides a kit comprising the novel CRFR1 agonist of the present invention and optionally instructions to use. Furthermore, the present invention provides the use of the compound of the present invention for the preparation of a pharmaceutical composition for the treatment of depression and, additionally, the use of the compound of the present invention for the preparation of a diagnostic composition for the determination of pituitary corticotroph responsiveness and/or for differentiating pituitary and ectopic production of ACTH in patients with ACTH-dependent Cushing's syndrome.

    Abstract translation: 本发明涉及对CRFR1具有高度选择性的化合物，对促肾上腺皮质激素释放因子受体-2（CRFR2）和/或促肾上腺皮质激素释放因子结合蛋白（CRFBP）没有任何显着的交叉反应性，所述化合物 包括或者由SEQ ID No：1所示的氨基酸序列组成。另一方面，本发明涉及包含本发明的新型CRFR1激动剂的药物和/或诊断组合物。 本发明还提供了一种试剂盒，其包含本发明的新型CRFR1激动剂和任选的使用说明书。 此外，本发明提供了本发明化合物在制备用于治疗抑郁症的药物组合物中的用途，另外还提供了本发明化合物在制备用于测定的诊断组合物中的用途 垂体促肾上腺皮质反应性和/或用于区分ACTH依赖性库兴综合征患者ACTH的垂体和异位产生。

    Urotensin-II agonists and antagonists
    82.
    发明授权
    Urotensin-II agonists and antagonists 失效
    促肾上腺素Ⅱ激动剂和拮抗剂

    公开(公告)号：US07241737B2

    公开(公告)日：2007-07-10

    申请号：US10399542

    申请日：2001-10-19

    Applicant: David H. Coy ,  Wojciech J. Rossowski ,  John E. Taylor

    Inventor： David H. Coy ,  Wojciech J. Rossowski ,  John E. Taylor

    IPC: A61K38/08 ,  C07K7/06

    CPC classification number: C07K7/52 ,  A61K38/00 ,  C07K14/57509

    Abstract: The present invention is directed to a novel class of cyclic polypeptides of the formula: (R1)a-AA1-cyclo[AA2-AA3-AA4-AA5-AA6-Cys]-AA7-R2, pharmaceutically acceptable salts thereof, wherein the variables are as defined in the specification, which inhibit the effects of urotensin-II and are useful for treating a variety of diseases and/or conditions characterized by an excess of urotensin-II including ischaemic heart disease, congestive heart failure, portal hypertension, variceal bleeding, hypotension, angina pectoris, myocardial infarction, ulcers, anxiety, schizophrenia, manic depression, delirium, dementia, mental retardation and/or dyskinesias.

    Abstract translation: 本发明涉及一类新型的下式的环状多肽：（R 1）a-A 1 - 环[AA] SUP→2→A→3→A→4→A→5→A→6→Cys〕 其中所述变量如本说明书中所定义，其抑制泌尿生长素-2的作用，并且可用于治疗 多种疾病和/或病症，其特征在于过量的泌尿生长素II，包括缺血性心脏病，充血性心力衰竭，门静脉高压，静脉曲张出血，低血压，心绞痛，心肌梗死，溃疡，焦虑，精神分裂症，躁狂抑郁，del妄，痴呆 ，精神发育迟滞和/或运动障碍。

    Promoter sequences for urocortin II and the use thereof
    85.
    发明申请
    Promoter sequences for urocortin II and the use thereof 失效
    urocortin II的启动子序列及其用途

    公开(公告)号：US20040002107A1

    公开(公告)日：2004-01-01

    申请号：US10438803

    申请日：2003-05-15

    Inventor： Ned H. Kalin ,  Patrick Henry Roseboom ,  Steven Anil Nanda

    IPC: C12Q001/68 ,  C07H021/04 ,  C12N009/64 ,  C12P021/02 ,  C12N005/06

    CPC classification number: C07K14/57509

    Abstract: Various human urocortin II promoter sequences are disclosed. Nucleic acids and host cells that contain the promoter sequences are also disclosed. Further disclosed are various methods involving the use of these sequences. Also disclosed are methods of modulating the activity of a human urocortin II promoter sequence and methods of modulating urocortin II expression in a cell.

    Abstract translation: 公开了各种人urocortin II启动子序列。 还公开了含有启动子序列的核酸和宿主细胞。 进一步公开的是涉及使用这些序列的各种方法。 还公开了调节人类尿皮质素II启动子序列的活性的方法以及调节细胞中尿皮质素II表达的方法。

    Cyclic CRF agonists
    89.
    发明授权
    Cyclic CRF agonists 有权
    循环CRF激动剂

    公开(公告)号：US06326463B1

    公开(公告)日：2001-12-04

    申请号：US09424889

    申请日：1999-11-29

    Applicant: Jean E. F. Rivier

    Inventor： Jean E. F. Rivier

    IPC: A61K3828

    CPC classification number: C07K14/57509 ,  A61K38/00 ,  G01N33/566 ,  G01N33/68 ,  G01N33/74 ,  G01N2333/5751 ,  Y10S930/26

    Abstract: Novel cyclic CRF agonist peptides have the amino acid sequence: (cyclo 30-33)Ac-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-R32-R33-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2 wherein R32 is His, D-His or an equivalent &agr;-amino acid; R33 is Lys or Orn. The N-terminus may be extended by Tyr, D-Tyr or Ile. Lys may be substituted for Arg23, and its side chain connected by a lactam bridge to Glu20 to form a bicyclic peptide. Certain disclosed CRF agonists include: (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Glu30, Lys33]r/hCRF(7-41); (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Glu30, D-His32, Lys33]r/hCRF(7-41); (bicyclo 20-23, 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Lys23,33, Glu30, D-His32]-r/hCRF(7-41); (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle18,21, Glu30, D-Ala32, Lys33]&agr;-helicale CRF(7-41); and (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, CML27,40, Glu30, Lys33]r/hCRF(7-41). Labelled agonist such as (cyclo 30-33)[Ac-I125Tyr6, D-Phe12, Nle21,38, Glu30, Lys33]r/hCRF(6-41) and (cyclo 30-33)[Ac-I125D-Tyr6, D-Phe12, Nle21,38, Glu30, D-His32, Lys33]r/hCRF(6-41) are useful in screening for more potent CRF agonists.

    Abstract translation: 新型循环CRF激动剂肽具有氨基酸序列：（环30-33）Ac-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle -Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-R32-R33-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2，其中R32是His，D-His 或等效的α-氨基酸; R33是Lys或Orn。 N末端可以被Tyr，D-Tyr或Ile延伸。 Lys可以代替Arg23，其侧链通过内酰胺桥连接至Glu20以形成双环肽。 某些公开的CRF激动剂包括：（环30-33）[Ac-Ser7，D-Phe12，Nle21,38，Glu30，Lys33] r / hCRF（7-41）; （环30-33）[Ac-Ser7，D-Phe12，Nle21,38，Glu30，D-His32，Lys33] r / hCRF（7-41）; （双环20-23,30-33）[Ac-Ser7，D-Phe12，Nle21,38，Lys23,33，Glu30，D-His32] -r / hCRF（7-41）; （环30-33）[Ac-Ser7，D-Phe12，Nle18,21，Glu30，D-Ala32，Lys33]α-螺旋CRF（7-41）; 和（环30-33）[Ac-Ser7，D-Phe12，Nle21,38，CML27,40，Glu30，Lys33] r / hCRF（7-41）。 标记的激动剂如（环30-33）[Ac-I125Tyr6，D-Phe12，Nle21,38，Glu30，Lys33] r / hCRF（6-41）和（环30-33）[Ac-I125D-Tyr6，D -Phe12，Nle21,38，Glu30，D-His32，Lys33] r / hCRF（6-41）可用于筛选更有效的CRF激动剂。

    Cyclic CRF antagonist peptides
    90.
    发明授权
    Cyclic CRF antagonist peptides 有权
    循环CRF拮抗肽

    公开(公告)号：US06323312B1

    公开(公告)日：2001-11-27

    申请号：US09424127

    申请日：1999-11-17

    Applicant: Jean E. F. Rivier

    Inventor： Jean E. F. Rivier

    IPC: A61K3812

    CPC classification number: G01N33/74 ,  A61K38/00 ,  C07K14/57509 ,  G01N33/566 ,  G01N2333/5751

    Abstract: Novel cyclic CRF antagonist peptides are created by shortening the N-terminus of a CRF family peptide by 8 residues and adding an acyl group. CML is present in what would be the 27-position of the native CRF sequence, and a cyclizing bond is created between the side chains of the residues in positions 30 and 33. The side chain of Lys, preferably, in position 33 is linked to the side chain of Glu in position 30 by a lactam bridce. Disclosed CRF antagonists include: (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,40, Glu30, Lys33]r/hCRF(9-4); (cyclo 30-33)[Ac-Asp9, D-Phe12, CML18,27, Nle21,38, Glu30, Lys33]r-hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,37, Glu30, Lys33]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, CML14,27, Nle21,38, Glu30, Lys33]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27, Glu30, Lys33]r/hCRF(9-41); and (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,40, Glu30, Aib32, Lys33]r/hCRF(9-41).

    Abstract translation: 通过将CRF家族肽的N末端缩短8个残基并加入酰基来产生新的循环CRF拮抗剂肽。 CML存在于天然CRF序列的27位上，并且在位置30和33的残基的侧链之间产生环化键。Lys的侧链优选位于33位与 位置30处的Glu的侧链通过内酰胺桥接。 公开的CRF拮抗剂包括：（环30-33）[Ac-Asp9，D-Phe12，Nle21,38，CML27,40，Glu30，Lys33] r / hCRF（9-4）; （环30-33）[Ac-Asp9，D-Phe12，CML18,27，Nle21,38，Glu30，Lys33] r-hCRF（9-41）; （环30-33）[Ac-Asp9，D-Phe12，Nle21,38，CML27,37，Glu30，Lys33] r / hCRF（9-41）; （环30-33）[Ac-Asp9，D-Phe12，CML14,27，Nle21,38，Glu30，Lys33] r / hCRF（9-41）; （环30-33）[Ac-Asp9，D-Phe12，Nle21,38，CML27，Glu30，Lys33] r / hCRF（9-41）; 和（环30-33）[Ac-Asp9，D-Phe12，Nle21,38，CML27,40，Glu30，Aib32，Lys33] r / hCRF（9-41）。

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