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公开(公告)号：EP1137666B9
公开(公告)日：2009-04-01
申请号：EP99960657.7
申请日：1999-12-07
发明人： DONG, Zheng, Xin , COY, David, H.
IPC分类号： C07K14/605 , A61K38/26 , A61P3/08
CPC分类号： C07K14/605 , A61K38/00 , Y02P20/55
摘要： The present invention is directed to peptide analogues of glucagon-like peptide-1, the pharmaceutically-acceptable salts thereof, to methods of using such analogues to treat mammals and to pharmaceutical compositions useful therefor comprising said analogues.
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公开(公告)号：EP0438519B1
公开(公告)日：1998-05-06
申请号：EP89912292.3
申请日：1989-10-13
IPC分类号： C07K7/02 , C07K14/595 , A61K38/16
CPC分类号： C07K14/57572 , A61K38/00 , C07K7/02 , C07K7/086
摘要： In general, the invention features a linear (i.e., non-cyclic) bombesin analog of biologically active mammalian gastrin-releasing peptide (GRP) and amphibian bombesin, having an active site and a binding site responsable for the binding of the peptide to a receptor on a target cell; cleavage of a peptide bond in the active site of naturally occuring bombesin or GRP is unnecessary for in vivo bilogical activity. The analog has one of the following modifications: (a) a deletion of a residue within the active site and a modification of a residue outside of the active site, or (b) a remplacement of one or two residues within the active site with a synthetic amino acid. The analog is capable of binding to the receptor and acting as a competitive inhibitor of the naturally occurring peptide by binding to the receptor and, by virtue of one of the modifications, failing to exhibit the in vivo biological activity of the naturally occurring peptide.
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公开(公告)号：EP0344297A1
公开(公告)日：1989-12-06
申请号：EP89901170.0
申请日：1988-11-18
CPC分类号： C07K14/6555 , A61K38/00
摘要： A method of treating a mammal suffering from cancer by administering to the mammal somatostatin or an analog thereof, the analog being a hexapeptide analog or higher, in a dosage of at least 25 µg/kg/day.
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4.发明公开ANALOGS OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND METHODS FOR THEIR USE 审中-公开ANALOGA DESPITUITÄRENADENYLATCYCLASE-AKTIVIERENDEN POLYPEPTIDS（PACAP）UND VERFAHREN ZU DEREN VERWENDUNG
公开(公告)号：EP3019184A1
公开(公告)日：2016-05-18
申请号：EP14806816.6
申请日：2014-06-09
CPC分类号： C07K14/4705 , A61K38/13 , A61K38/14 , A61K38/1816 , A61K45/06 , A61K47/64 , A61K49/0004 , A61K51/08 , C07K14/57563 , A61K2300/00
摘要： This invention relates to analogs of pituitary adenylate cyclase-activating polypeptide (PACAP), which are agonists for the PACAP/vasoactive intestinal peptide (VIP) receptors: PAC
1 , VPAC
1 and VPAC
2 receptors. These PACAP analogs can be used as prophylactic/therapeutic agents for a wide range of medical disorders. These PACAP analogs coupled to suitable radionuclides can be used in the localization, diagnosis and treatment of disseminated cancers and metastatic tumors, and coupled to small molecule therapeutics can be used as vectors for targeted drug delivery. This invention also provides pharmaceutical compositions of one or more PACAP analogs of the invention either alone or in combination with one or more other prophylactic/therapeutic agent.摘要翻译： 本发明涉及垂体腺苷酸环化酶活化多肽（PACAP）的类似物，其是PACAP /血管活性肠肽（VIP）受体的激动剂：PAC1，VPAC1和VPAC2受体。 这些PACAP类似物可用作广泛的医学疾病的预防/治疗剂。 耦合到合适的放射性核素的这些PACAP类似物可用于弥散性癌症和转移性肿瘤的定位，诊断和治疗，并且与小分子治疗剂相结合可用作靶向药物递送的载体。 本发明还提供本发明的一种或多种PACAP类似物的药物组合物，其单独或与一种或多种其它预防/治疗剂组合。
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公开(公告)号：EP1011716B9
公开(公告)日：2004-03-03
申请号：EP95943375.6
申请日：1995-12-07
申请人： THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND , SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES S.A.S.
发明人： COY, David, H. , TAYLOR, John, E.
IPC分类号： A61K38/31 , C07K7/00 , C07K14/655
CPC分类号： A61K38/31 , C07K14/6555
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公开(公告)号：EP0956296A2
公开(公告)日：1999-11-17
申请号：EP97949758.0
申请日：1997-12-04
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.) , The Administrators of The Tulane Educational Fund
发明人： MORGAN, Barry , MURPHY, William , COY, David, H.
CPC分类号： C07K14/6555
摘要： The invention features somatostatin antagonists having a D-amino acid at the second residue.
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公开(公告)号：EP0833646A1
公开(公告)日：1998-04-08
申请号：EP96917939.0
申请日：1996-06-03
申请人： The Administrators of The Tulane Educational Fund , THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , The Louisiana State University Medical Center Foundation , CHILDREN'S HOSPITAL, INC.
发明人： COY, David, H. , WOLTERING, Eugene, A. , O'DORISIO, M., Sue , O'DORISIO, Thomas, M. , MURPHY, William, A.
CPC分类号： C07K14/655 , A61K38/00
摘要： Disclosed are methods and compositions for the diagnosis and treatment of diseases associated with aberrant expression of a somatostatin receptor (e.g., cancer) or with increased production of a factor regulatable by somatostatin (e.g., acromegaly). The compounds of the invention are of the general formulae: a) (Y)n+1P, b) (Y)n-Ala-Y-P, or c) (I), wherein P is a somatostatin peptide analog which binds to a somatostatin receptor, Y is D-tyrosine, L-tyrosine, or desamino-tyrosine, n is an integer from 1 to 32, inclusive, each q, independently, is an integer from 1 to 32, inclusive, and each s, independently, is an integer from 1 to 32, inclusive, where q and s can be the same or different, and X is of the formula D-NH2-CH(CH2)mNH2-CO2H or L-NH2-CH(CH2)mNH2-CO2H, wherein m is an integer from 1 to 10, inclusive.
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公开(公告)号：EP0489089A1
公开(公告)日：1992-06-10
申请号：EP90913117.0
申请日：1990-08-17
CPC分类号： C07K14/57572 , A61K38/00 , C07K7/02 , C07K7/086 , C07K7/18
摘要： Un analogue linéaire (c'est-à-dire non cyclique) de bombésine amphibienne biologiquement active ou d'un peptide de libération de gastrine mammifère (GRP) possède un site actif et un site de liaison responsable de la liaison du peptide sur un récepteur d'une cellule cible. Le clivage d'une liaison peptide dans le site actif de la bombésine se produisant naturellement ou du GRP n'est pas nécessaire pour une activité biologique in vivo. L'analogue possède l'une des modifications suivantes: (a) une délétion d'un reste d'acide aminé dans le site actif et une modification d'un acide aminé à l'extérieur du site actif, (b) un remplacement de deux restes d'acides aminés dans le site actif par un acide aminé synthétique, un reste beta-amino acide, ou un reste gamma-amino acide, ou (c) une liaison non peptide au lieu d'une liaison peptide entre un reste d'amino acide du site actif et un reste amino acide adjacent.
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公开(公告)号：EP0438566A1
公开(公告)日：1991-07-31
申请号：EP90912128.0
申请日：1990-08-16
摘要： Un peptide linéaire qui est un analogue d'une substance biologiquement active se produisant naturellement P possède un site actif et un site de liaison responsable de la liaison de ce peptide sur un récepteur d'une cellule cible. L'analogue possède une liaison non peptide au lieu d'une liaison peptide entre un reste d'amino acide du site actif et un reste d'amino acide adjacent ou un reste synthétique de beta-amino acide ou de gamma-amino acide remplaçant deux restes d'amino acide du site actif.
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10.发明公开THE USE OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND PACAP ANALOGS AS ADJUNCTIVE TREATMENTS WITH INHIBITORS OF CALCINEURIN OR INHIBITORS OF THE MAMMALIAN TARGET OF RAPAMYCIN (mTOR) COMPLEXES 审中-公开使用本垂体腺苷酸环化酶激活多肽（PACAP）和PACAP ANALOG作为支持治疗钙调磷酸酶抑制剂或抑制剂MTOR-配合物的
公开(公告)号：EP2533795A2
公开(公告)日：2012-12-19
申请号：EP11740499.6
申请日：2011-02-07
CPC分类号： A61K38/2235 , A61K38/13 , A61K45/06 , A61K2300/00
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