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公开(公告)号：EP1067950A1
公开(公告)日：2001-01-17
申请号：EP99916562.4
申请日：1999-04-09
发明人： RICHELSON, Elliott , CUSACK, Bernadette, Marie , PANG, Yuan-Ping , McCORMICK, Daniel, J. , FAUQ, Abdul , TYLER, Beth, Marie , BOULES, Mona
CPC分类号： C07K7/083 , A61K38/00 , C07D209/08 , C07K7/14 , C07K7/18 , C07K14/70 , C07K14/702
摘要： The invention provides a novel amino acid, neo-tryptophan as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.
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公开(公告)号：EP0759934B1
公开(公告)日：1999-04-14
申请号：EP95920949.5
申请日：1995-05-17
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公开(公告)号：EP0759934A1
公开(公告)日：1997-03-05
申请号：EP95920949.0
申请日：1995-05-17
发明人： CLERC, François-Frédéric , DUBROEUCQ, Marie-Christine , HELYNCK, Gérard , LEBOUL, Jean , MARTIN, Jean-Paul
IPC分类号： C12P21 , A61K38 , A61P1 , A61P9 , A61P11 , A61P25 , A61P35 , A61P37 , C07C27 , C07K5 , C07K7 , C07K14 , C12R1
摘要： Compounds of formula (I) in which R is a hydroxy, alkoxy, phenylalkyloxy radical or -NH-CH2-COOH, R1 is a hydrogen atom, an adamantylacetyl, adamantylcarbonyl, norbornylacetyl, norbornylphenoxycarbonyl, benzoyl, nicotinoyl, 4-phenylbenzoyl, 4-tert-butylbenzoyl, 2-pyrrolidinecarbonyl radical or a protective group of an amine function, R2 is an Arg or Lys residue, R3 is an Arg or Lys residue, R4 is a Pro, m, n and p residue, which are the same or different and are a number equal to 0 or 1, given that when R1 is a hydrogen atom, the sum m+n+p is at least equal to 1, R5 and R6 are the same and are a hydroxy or methoxy radical and R7 is a hydrogen, chlorine, bromine or iodine atom or a nitro radical, the equivalents of the compounds of formula (I) in which one or more peptide bonds (CO-NH) between two amino acid residues are replaced by -CH2-NH bonds and/or the peptide bond (CO-NH) between the amino acid residues R2 and R3 is replaced by a CH=CH bond. The invention also concerns the salts of said compounds, the preparation thereof and drugs containing same.
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公开(公告)号：EP0752873A1
公开(公告)日：1997-01-15
申请号：EP95911829.0
申请日：1995-02-21
发明人： MERTENS, John , TOURWE, Dirk , CEUSTERS, Marc
CPC分类号： A61K51/08 , A61K38/00 , A61K51/085 , A61K51/088 , A61K2121/00 , A61K2123/00 , C07K7/083
摘要： The invention relates to a labelled peptide compound, wherein the peptide has a selective neurotensin receptor affinity and is represented by the general formula (I): R1 - (1Pro)n - ?2Xaa - 3Xbb -4Xcc - 5Xdd - 6Xee - 7¿Leu - OH, wherein R¿1? is a (C1-C3)alkanoyl group, an arylcarbonyl group, an aryl-(C1-C3)alkanoyl group, or a chelating group attached by an amide bond or through a spacing group to the peptide molecule; Xaa and Xbb are each individually Arg or Lys; Xcc is an unsubstituted or substituted cyclic amino acid, preferably selected from Pro and Hyp; Xdd is Tyr, Trp or Phe; Xee is Leu, Ile or t.-butylalanine; and n is 0 or 1; and wherein said peptide is labelled with (a) a metal isotope, or (b) with a radioactive halogen isotope; on the understanding that: (i) if the label is a metal isotope, R1 represents a chelating group for chelating said isotope; and (ii) if the label is a radioactive halogen isotope, said halogen isotope is attached to ?4¿Tyr in the 2-position of the phenyl ring, to 4Trp, or to the aryl group of substituent R¿1?. The invention further relates to a pharmaceutical composition comprising said labelled peptide compound, to the use of said composition for diagnosis and therapy, and to a kit for preparing a radiopharmaceutical composition.
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35.发明公开Polypeptides, methods for their preparation, pharmaceutical compositions comprising them and use 失效多肽，其制备方法，包含其使用的药物组合物
公开(公告)号：EP0333071A3
公开(公告)日：1990-09-26
申请号：EP89104302.8
申请日：1989-03-10
申请人： Eisai Co., Ltd.
发明人： Tsuchiya, Yutaka , Sasaki, Atsushi , Yoshino, Hiroshi , Karibe, Norio , Sugimoto, Hachiro , Kubota, Atsuhiko , Kosasa, Michiko , Araki, Shin , Ikeda, Masuhiro , Yamanishi, Yoshiharu , Machida, Ryoichi , Yamatsu, Kiyomi
摘要： A polypeptide is shown with the following formula:
wherein A, B, C, D, E, F and R 1 are as defined in claim 1. The invention includes pharmaceutical compositions comprising the above polypeptide and the use of this polypeptide. Finally, preparation methods for the new polypeptide are disclosed.-
36.发明公开Polypeptides, methods for their preparation, pharmaceutical compositions comprising them and use 失效多肽，其制备方法，含有它们的药物组合物。
公开(公告)号：EP0333071A2
公开(公告)日：1989-09-20
申请号：EP89104302.8
申请日：1989-03-10
申请人： Eisai Co., Ltd.
发明人： Tsuchiya, Yutaka , Sasaki, Atsushi , Yoshino, Hiroshi , Karibe, Norio , Sugimoto, Hachiro , Kubota, Atsuhiko , Kosasa, Michiko , Araki, Shin , Ikeda, Masuhiro , Yamanishi, Yoshiharu , Machida, Ryoichi , Yamatsu, Kiyomi
摘要： A polypeptide is shown with the following formula:
wherein A, B, C, D, E, F and R 1 are as defined in claim 1.
The invention includes pharmaceutical compositions comprising the above polypeptide and the use of this polypeptide. Finally, preparation methods for the new polypeptide are disclosed.摘要翻译： 多肽被示为具有下式：ABCDEFR <1> worin A，B，C，D，E，F和R <1>是如在claimsoft 1.本发明包括药物组合物，包含上述多肽和使用的定义 这种多肽。 最后，对于新的多肽制备方法游离缺失盘。
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公开(公告)号：EP2673001B1
公开(公告)日：2016-12-21
申请号：EP12737597.0
申请日：2012-02-10
CPC分类号： C07K7/083 , A61K38/10 , A61K47/62 , A61K47/645 , A61K47/6929 , A61K48/00 , A61K48/0025 , A61K48/0091 , C07K2319/035 , C12N9/1211 , C12N15/87 , C12Y207/01021
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38.发明公开ACTIVATED NEUROTENSIN MOLECULES AND THE USES THEREOF 审中-公开AktivierteNeurotensinmoleküleund Verwendungendafür
公开(公告)号：EP2896402A1
公开(公告)日：2015-07-22
申请号：EP14305074.8
申请日：2014-01-20
摘要： The present invention relates to activated neurotensin, pharmaceutical compositions comprising the same, and the uses thereof. The compounds and compositions of the invention may be used e.g., to reduce body temperature or pain.
摘要翻译： 本发明涉及活化的神经丝氨酸，包含其的药物组合物及其用途。 本发明的化合物和组合物可用于例如降低体温或疼痛。
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公开(公告)号：EP1991561B1
公开(公告)日：2015-06-17
申请号：EP07722808.8
申请日：2007-02-13
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40.发明公开
公开(公告)号：EP2729184A1
公开(公告)日：2014-05-14
申请号：EP12779758.7
申请日：2012-05-03
CPC分类号： C07K5/10 , A61K38/2228 , A61K51/08 , A61K51/088 , C07K7/02 , C07K7/083 , C07K14/57509 , G01N33/5061 , G01N33/5088 , G01N2333/5751
摘要： Novel urotensin II receptor (UT) agonists and antagonists are described herein. More specifically, novel derivatives of urotensin ll-related peptide (URP) are described herein.
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