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1. 发明申请

WO02095395A8 BENZOPHENONE-LINKED CRF AND CRF-LIKE PEPTIDES FOR COVALENT LABELING OF CORTICOTROPIN-RELEASING FACTOR (CRF) BINDING PROTEIN 审中-公开
标题翻译：苯并呋喃连接的CRF和CRF样蛋白用于CORTICOTROPIN-释放因子（CRF）结合蛋白的共价标签
公开(公告)号：WO02095395A8
公开(公告)日：2004-04-29
申请号：PCT/EP0205798
申请日：2002-05-27
申请人： MAX PLANCK GESELLSCHAFT , ECKART KLAUS , SPIESS JOACHIM , JAHN OLAF
发明人： ECKART KLAUS , SPIESS JOACHIM , JAHN OLAF
IPC分类号： C07K14/47 , C07K14/575 , G01N33/74
CPC分类号： G01N33/743 , C07K14/47 , C07K14/57509
摘要： The present invention relates to a ligand of the Corticotropin-Releasing Factor (CRF)-binding protein (CRFBP) selected from the group consisting of CRF, Urocortin (Ucn), and Urotensin, said ligand comprising a covalently linked benzophenone moiety. Further, the present invention relates to a process for the purification of a CRFBP which comprises reacting said CRFBP with the ligand of the invention, performing photoaffinity labeling, and purifying the resultant photoreaction products by HPLC. The present invention also relates to the use of the ligand of the invention for detecting CRFBP and for identifying the binding site within CRFBP. The present invention also relates to a method for identifying an inhibitor of the binding of ARF to CRFBP.
摘要翻译：本发明涉及选自由CRF，Urocortin（Ucn）和促胃素素组成的组的促肾上腺皮质激素释放因子（CRF）结合蛋白（CRFBP）的配体，所述配体包含共价连接的二苯甲酮部分。此外，本发明涉及一种纯化CRFBP的方法，其包括使所述CRFBP与本发明的配体反应，进行光亲和标记，并通过HPLC纯化所得光反应产物。本发明还涉及本发明的配体用于检测CRFBP和鉴定CRFBP内的结合位点的用途。本发明还涉及鉴定ARF与CRFBP结合的抑制剂的方法。

2. 发明申请

WO0224732A3 METHODS FOR IMPROVING THE ANTAGONISTIC/AGONISTIC PROPERTIES OF PEPTIDIC ANTAGONISTS/AGONISTS OF THE CORTICOTROPIN-RELEASING FACTOR RECEPTOR (CRFR) 审中-公开
标题翻译：用于改善角质形成蛋白激酶因子受体（CRFR）的拮抗剂拮抗剂/激动剂的拮抗/促炎性质的方法
公开(公告)号：WO0224732A3
公开(公告)日：2003-01-23
申请号：PCT/EP0111031
申请日：2001-09-24
申请人： MAX PLANCK GESELLSCHAFT , ECKART KLAUS , SPIESS JOACHIM , JAHN OLAF
发明人： ECKART KLAUS , SPIESS JOACHIM , JAHN OLAF
IPC分类号： A61K38/00 , A61K38/22 , C07K14/575 , G01N33/68
CPC分类号： C07K14/57509 , A61K38/00
摘要： The present invention relates to a method for improving the antagonistic/agonistic properties of peptidic antagonists/agonists of the corticotropin-releasing factor receptor (CRFR). Further, the present invention relates to an antagonist of the ligand of the corticotropin-releasing factor receptor (CRFR) comprising or alternatively consisting of the amino acid sequence of astressin wherein at least Ala at position 11 is replaced by another amino acid. Further, the present invention relates to an antibody directed against the agonist or antagonist of the present invention. Also described is an anti-idiotypic antibody which is directed against the antibody(ies) of the invention. The present invention also relates to a pharmaceutical or diagnostic composition comprising the antagonist, the agonist, the antibody(ies) and/or the anti-idiotypic antibody of the invention. Furthermore, the present invention relates to a kit comprising the agonist, the antagonist, the antibody(ies) and/or the anti-idiotypic antibody of the present invention. Also described is the use of the agonist, the antagonists, the antibody(ies) and/or the anti-idiotypic antibody of the invention for the preparation of a pharmaceutical composition for the treatment, diagnosis and/or prevention of corticotropin-releasing factor receptor-associated diseases. The present invention also relates to a method of refining the agonist and/or the antagonists of the present invention by means of peptidomimetics and synthesizing the refined compound. Furthermore, the present invention relates to a method of formulating the agonist/antagonist of the invention into a pharmaceutical composition.
摘要翻译：本发明涉及改善促肾上腺皮质激素释放因子受体（CRFR）的肽拮抗剂/激动剂的拮抗/激动性质的方法。此外，本发明涉及促肾上腺皮质激素释放因子受体（CRFR）的配体的拮抗剂，其包含或者由阿斯匹林的氨基酸序列组成，其中至少11位的Ala被另一个氨基酸替代。此外，本发明涉及针对本发明的激动剂或拮抗剂的抗体。还描述了针对本发明的抗体的抗独特型抗体。本发明还涉及包含本发明的拮抗剂，激动剂，抗体和/或抗独特型抗体的药物或诊断组合物。此外，本发明涉及包含本发明的激动剂，拮抗剂，抗体和/或抗独特型抗体的试剂盒。还描述了本发明的激动剂，拮抗剂，抗体和/或抗独特型抗体用于制备用于治疗，诊断和/或预防促肾上腺皮质激素释放因子受体的药物组合物的用途相关疾病本发明还涉及通过肽模拟物精制本发明的激动剂和/或拮抗剂并合成精制化合物的方法。此外，本发明涉及将本发明的激动剂/拮抗剂配制成药物组合物的方法。

3. 发明申请

WO0005253A9 ANTAGONISTS SPECIFIC FOR THE CORTICOTROPIN-RELEASING FACTOR RECEPTOR TYPE 2 (CRFR2) 审中-公开
标题翻译： CORTICOTROPIN-REXTOR因子受体2型（CRFR2）特异性拮抗剂
公开(公告)号：WO0005253A9
公开(公告)日：2000-07-27
申请号：PCT/EP9905297
申请日：1999-07-23
申请人： MAX PLANCK GESELLSCHAFT , SPIESS JOACHIM , RUEHMANN ANDREAS
发明人： SPIESS JOACHIM , RUEHMANN ANDREAS
IPC分类号： A61K38/00 , A61K38/16 , A61K39/395 , C07K14/435 , C07K14/575 , C07K16/18 , C12N15/12 , C12N15/63 , G01N33/53 , G01N33/68
CPC分类号： C07K14/57509 , A61K38/00
摘要： The present invention relates to an antagonist of the ligand of the Corticotropin-Releasing Factor Receptor, type 2 (CRFR2) lacking the 8 to 10 N-terminal amino acids of native sauvagine. The present invention also relates to an antagonist of the ligand of the Corticotropin-Releasing Factor Receptor, type 2 (CRFR2) lacking the 11 N-terminal amino acids of native sauvagine, wherein the N-terminal amino acid of said antagonist is a charged amino acid. Furthermore, the present invention relates to a polynucleotide encoding the antagonist of the present invention, a vector comprising the polynucleotide of the present invention, and a host comprising the polynucleotide or the vector of the present invention. Also described are a method for producing the antagonist of the present invention, antibodies directed the antagonist of the present invention, as well as anti-idiotypic antibodies directed against the antibody of the present invention. The present invention also relates to pharmaceutical and diagnostic compositions comprising the antagonist, the polynucleotide, the vector, the antibody, and/or the anti-idiotypic antibody of the present invention. Furthermore, the present invention relates to a kit comprising one or more of the above mentioned compounds of the present invention and to the use of one or more of these compounds for the preparation of a pharmaceutical composition for preventing and/or treating a Corticotropin-Releasing Factor Receptor, type 2 (CRFR2)-associated disease.
摘要翻译：本发明涉及不含天然sauvagine的8至10个N-末端氨基酸的促性激素释放因子受体2型（CRFR2）的配体的拮抗剂。本发明还涉及缺乏天然sauvagine的11个N-末端氨基酸的促肾上腺皮质激素释放因子受体2型（CRFR2）的配体的拮抗剂，其中所述拮抗剂的N-末端氨基酸是带电氨基酸。此外，本发明涉及编码本发明拮抗剂的多核苷酸，包含本发明多核苷酸的载体和包含本发明的多核苷酸或载体的宿主。还描述了制备本发明拮抗剂的方法，针对本发明拮抗剂的抗体以及针对本发明抗体的抗独特型抗体。本发明还涉及包含本发明的拮抗剂，多核苷酸，载体，抗体和/或抗独特型抗体的药物和诊断组合物。此外，本发明涉及一种试剂盒，其包含一种或多种上述本发明化合物，以及这些化合物中的一种或多种用于制备用于预防和/或治疗促肾上腺皮质激素释放的药物组合物因子受体2型（CRFR2）相关疾病。

4. 发明申请

WO0005253A2 ANTAGONISTS SPECIFIC FOR THE CORTICOTROPIN-RELEASING FACTOR RECEPTOR TYPE 2 (CRFR2) 审中-公开
标题翻译： 2型促分裂素释放因子受体特异性拮抗剂（CRFR2）
公开(公告)号：WO0005253A2
公开(公告)日：2000-02-03
申请号：PCT/EP9905297
申请日：1999-07-23
申请人： MAX PLANCK GESELLSCHAFT , SPIESS JOACHIM , RUEHMANN ANDREAS
发明人： SPIESS JOACHIM , RUEHMANN ANDREAS
IPC分类号： A61K38/00 , A61K38/16 , A61K39/395 , C07K14/435 , C07K14/575 , C07K16/18 , C12N15/12 , C12N15/63 , G01N33/53 , G01N33/68
CPC分类号： C07K14/57509 , A61K38/00
摘要： The present invention relates to an antagonist of the ligand of the Corticotropin-Releasing Factor Receptor, type 2 (CRFR2) lacking the 8 to 10 N-terminal amino acids of native sauvagine. The present invention also relates to an antagonist of the ligand of the Corticotropin-Releasing Factor Receptor, type 2 (CRFR2) lacking the 11 N-terminal amino acids of native sauvagine, wherein the N-terminal amino acid of said antagonist is a charged amino acid. Furthermore, the present invention relates to a polynucleotide encoding the antagonist of the present invention, a vector comprising the polynucleotide of the present invention, and a host comprising the polynucleotide or the vector of the present invention. Also described are a method for producing the antagonist of the present invention, antibodies directed the antagonist of the present invention, as well as anti-idiotypic antibodies directed against the antibody of the present invention. The present invention also relates to pharmaceutical and diagnostic compositions comprising the antagonist, the polynucleotide, the vector, the antibody, and/or the anti-idiotypic antibody of the present invention. Furthermore, the present invention relates to a kit comprising one or more of the above mentioned compounds of the present invention and to the use of one or more of these compounds for the preparation of a pharmaceutical composition for preventing and/or treating a Corticotropin-Releasing Factor Receptor, type 2 (CRFR2)-associated disease.
摘要翻译：本发明涉及缺乏天然苏维A的8至10个N端氨基酸的2型促肾上腺皮质激素释放因子受体（CRFR2）配体的拮抗剂。本发明还涉及缺乏天然苏维A的11个N-末端氨基酸的2型促肾上腺皮质激素释放因子受体（CRFR2）的配体的拮抗剂，其中所述拮抗剂的N-末端氨基酸是带电荷的氨基酸酸。此外，本发明涉及编码本发明拮抗剂的多核苷酸，包含本发明多核苷酸的载体和包含本发明多核苷酸或载体的宿主。还描述了生产本发明拮抗剂的方法，针对本发明拮抗剂的抗体以及针对本发明抗体的抗独特型抗体。本发明还涉及包含本发明的拮抗剂，多核苷酸，载体，抗体和/或抗独特型抗体的药物和诊断组合物。此外，本发明涉及包含一种或多种上述本发明化合物的试剂盒以及这些化合物中的一种或多种在制备用于预防和/或治疗促肾上腺皮质激素释放的药物组合物中的用途因子受体，2型（CRFR2）相关疾病。

5. 发明申请

WO9718238A2 CRF ANALOGS 审中-公开
标题翻译： CRF模拟
公开(公告)号：WO9718238A2
公开(公告)日：1997-05-22
申请号：PCT/EP9605010
申请日：1996-11-14
申请人： MAX PLANCK GESELLSCHAFT , SPIESS JOACHIM , RUEHMANN ANDREAS
发明人： SPIESS JOACHIM , RUEHMANN ANDREAS
IPC分类号： A61K38/00 , C07K14/575 , A61K38/22 , G01N33/74
CPC分类号： C07K14/57509 , A61K38/00
摘要： The present invention relates to lipophilic CRF analogs which are useful as active ingredients in pharmaceutical or diagnostic compositions.
摘要翻译：本发明涉及用作药物或诊断组合物中的活性成分的亲脂性CRF类似物。

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