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1. 发明授权

US5840682A Peptide antagonists of neurotensin 失效
标题翻译：神经降压肽的肽拮抗剂
公开(公告)号：US5840682A
公开(公告)日：1998-11-24
申请号：US737695
申请日：1996-11-19
申请人： Francois-Frederic Clerc , Marie-Christine Dubroeucq , Gerard Helynck , Jean Leboul , Jean-Paul Martin
发明人： Francois-Frederic Clerc , Marie-Christine Dubroeucq , Gerard Helynck , Jean Leboul , Jean-Paul Martin
IPC分类号： C12P21/02 , A61K38/00 , A61P1/00 , A61P1/04 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/18 , A61P25/28 , A61P35/00 , A61P37/08 , C07C27/22 , C07K5/10 , C07K7/02 , C07K7/06 , C07K7/08 , C07K7/18 , C07K14/655 , C12R1/04 , A61K38/12
CPC分类号： C07K14/6555 , C07C27/22 , C07K7/02 , C07K7/083 , C07K7/18 , A61K38/00 , Y02P20/55
摘要： The invention is directed to a compound of formula ##STR1## in which R represents a hydroxyl, alkyloxy, phenylalkyloxy or --NH--CH.sub.2 --COOH radical, R.sub.1 represents a hydrogen atom, an adamantylacetyl, adamantylcarbonyl, norbornylacetyl, norbornylphenoxycarbonyl, benzoyl, nicotinoyl, 4-phenylbenzoyl, 4-tert-butylbenzoyl or 2-pyrrolidinecarbonyl radical or a protective group for an amine functional group, R.sub.2 represents an Arg or Lys residue, R.sub.3 represents an Arg or Lys residue, R.sub.4 represents a Pro residue, m, n and p, which are the identical or different, represent a number equal to 0 or 1, R.sub.5 and R.sub.6 are identical and represent a hydroxyl or methoxy radical and R.sub.7 represents a hydrogen, chlorine, bromine or iodine atom or a nitro radical, or the compound wherein one or a number of peptide bonds between two amino acid residues are replaced by --CH.sub.2 --NH bonds or the peptide bond between the R.sub.2 and R.sub.3 amino acid residues is replaced by a CH.dbd.CH bond, provided that when R.sub.1 is a hydrogen atom, then the sum of m+n+p is at least equal to 1. The invention is also directed to a pharmaceutical composition comprising the compound of formula I and the preparation of the compound.
摘要翻译： PCT No.PCT / FR95 / 00643 Sec。 371日期1996年11月19日 102（e）日期1996年11月19日PCT提交1995年5月17日PCT公布。 WO95 / 32218 PCT公开号日期：1995年11月30日本发明涉及式（I）的化合物，其中R表示羟基，烷氧基，苯基烷氧基或-NH-CH2-COOH基，R1表示氢原子，金刚烷基乙酰基，金刚烷基羰基，降冰片基乙酰基，降冰片基苯氧基羰基，苯甲酰基，烟酰基，4-苯基苯甲酰基，4-叔丁基苯甲酰基或2-吡咯烷羰基或胺官能团的保护基，R2表示Arg或Lys残基，R3表示Arg或Lys残基，R4表示相同或不同的Pro残基，m，n和p表示等于0或1的数，R5和R6相同，表示羟基或甲氧基，R7表示氢，氯，溴或碘原子或硝基，或其中两个氨基酸残基之间的一个或多个肽键被-CH 2 -NH键取代或R2和R3氨基酸残基之间的肽键被CH = CH键取代的化合物，只要R1是啊然后m + n + p的总和至少等于1.本发明还涉及包含式I化合物和化合物的制备的药物组合物。

2. 发明授权

US5856439A Farnesyl transferase inhibitors, preparation thereof, and pharmaceutical compositions containing same 失效
公开(公告)号：US5856439A
公开(公告)日：1999-01-05
申请号：US875752
申请日：1997-08-01
申请人： Francois-Frederic Clerc
发明人： Francois-Frederic Clerc
IPC分类号： A61K38/00 , A61P35/00 , A61P43/00 , C07K5/103 , A61K38/07
CPC分类号： C07K5/1013 , A61K38/00
摘要： Novel farnesyl transferase inhibitors of general formula (I) ##STR1## preparation thereof and pharmaceutical compositions containing same. In general formula (I), R.sub.1 is Y--S--A.sub.1 -- (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl or alkoxycarbonyl radical, or a radical R.sub.4 --S--, where R.sub.4 is a C.sub.1-6 alkyl radical optionally substituted by a phenyl radical, or a radical of general formula (II), ##STR2## wherein A.sub.1, X.sub.1, Y.sub.1, R'.sub.2, R'.sub.2, X.sub.2, Y.sub.2, R.sub.3, R'.sub.3 and R are as defined below, and A.sub.1 is a C.sub.1-4 alkylene radical optionally .alpha.-substituted in the >C(X.sub.1) (Y.sub.1) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical); X.sub.1 and Y.sub.1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, a >C.dbd.O grouping; R.sub.2 is a straight or branched C.sub.1-4 alkyl radical optionally substituted by a cyclohexyl radical; R'.sub.2 is hydrogen or alkyl; X.sub.2 and Y.sub.2 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, a >C.dbd.O grouping; R.sub.3 is a C.sub.1-4 alkyl radical optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that, when R.sub.3 is an alkyl radical substituted by a hyroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that, when R.sub.3 is an alkyl radical substituted by a hydroxy radical, R.sub.3 may form a lactone with the .alpha.-carboxy radical; R'.sub.3 is hydrogen or alkyl; X is an oxygen or sulphur atom; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted phenyl radical. These novel products have anticancer properties.

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