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    • 3. 发明授权
    • Irreversible peptide ligands for bombesin receptors, their use, and
process for making the same
    • BOMBESIN受体的不可逆肽配体,其使用及其制备方法
    • US5100873A
    • 1992-03-31
    • US380539
    • 1989-07-17
    • Roberto de CastiglioneMauro GalantinoFabio CorradiLuigia GozziniMarina CiomeiIsabella Molinari
    • Roberto de CastiglioneMauro GalantinoFabio CorradiLuigia GozziniMarina CiomeiIsabella Molinari
    • A61K38/00A61P35/00C07K1/02C07K7/06C07K7/08
    • C07K7/086A61K38/00
    • A peptide of formula (I):A-B-C-D-Gln-Trp-Ala-Val-X-Y-T-W (I)wherein either:(i) A represents a hydrogen atom, a Boc group or an acetyl group, one of B and C represents a pMel or mMel residue, and the other of B and C represents a sigma bond or a Gly, Leu-Gly, E-Leu-Gly or Gln-E-Leu-Gly, E, or E-Gly residue with E=Arg(A), arg(A), Lys(A), lys(A), Orn(A) and orn(A); or(ii) A represents a hydrogen atom;B represents a Glp-Arg-Leu-Gly residue;C represents a pMel or mMel residue;D represents a sigma bond or an Asn or Thr residue;X represents a Gly or ala residue;Y represents a sigma bond or a His(R.sub.1);his(R.sub.1), Phe, phe, Ser, ser, Ala or ala residue,T represents a sigma bond or a Leu, leu, Phe or phe residue;W represents an OH, amino, pentylamino or phenethyl-amino group or a Met-R.sub.2, Leu-R.sub.2, Ile-R.sub.2 or Nle-R.sub.2 residue;R.sub.1 represents a hydrogen atom or a Tos, Dnp or Bzl group; andR.sub.2 represents an amino, hydroxy, methoxy or hydrazino group;and its pharmaceutically acceptable salts are disclosed.
    • 式(I)的肽:ABCD-Gln-Trp-Ala-Val-XYTW(I)其中:(i)A表示氢原子,Boc基或乙酰基,B和C之一表示pMel 或mMel残基,B和C中的另一个表示σ键或具有E = Arg(Gly)的Gly,Leu-Gly,E-Leu-Gly或Gln-E-Leu-Gly,E或E-Gly残基 ),arg(A),Lys(A),lys(A),Orn(A)和orn(A); 或(ii)A表示氢原子; B表示Glp-Arg-Leu-Gly残基; C表示pMel或mMel残基; D表示σ键或Asn或Thr残基; X表示Gly或ala残基; Y表示σ键或His(R1); 他的(R1),Phe,phe,Ser,ser,Ala或ala残基,T表示σ键或Leu,leu,Phe或phe残基; W表示OH,氨基,戊基氨基或苯乙基 - 氨基或Met-R2,Leu-R2,Ile-R2或Nle-R2残基; R1表示氢原子或Tos,Dnp或Bzl基团; 并且R 2表示氨基,羟基,甲氧基或肼基; 及其药学上可接受的盐。
    • 9. 发明授权
    • Peptides
    • 多肽
    • US4491541A
    • 1985-01-01
    • US542974
    • 1983-10-18
    • Roberto de CastiglioneLuigia GozziniPier C. MontecucchiGiuseppe Perseo
    • Roberto de CastiglioneLuigia GozziniPier C. MontecucchiGiuseppe Perseo
    • A61K38/00C07K5/078C07K5/097C07K5/107C07K5/117C07K7/06C07C103/52
    • C07K7/06C07K5/06173C07K5/0823C07K5/1016C07K5/1024A61K38/00Y02P20/55
    • A peptide of formula (I):X-A-B-C-Trp-D-YwhereinX represents hydrogen, or a terminal nitrogn protecting group selecting from the group consisting of the acyl, aromatic oxycarbonyl, alkyl, aralkyl and aliphatic oxycarbonyl;A represent a valence bond or a L-.alpha.-amino acid residue;B represent a L-.alpha.-imino acid residue or a L-.alpha.-amino acid;C represent a L-.alpha.-imino acid residue or a neutral L-.alpha.-amino acid residue;D represents a valence bond or a L-.alpha.-amino acid residue; andY represents hydroxy, an amino group or a group of the formula OR, NHR, NR.sub.2 or NH--NH--R', wherein R represents a straight chain, branched chain or cyclic (including fused or bridged ring) alkyl group having up to 11 carbon atoms, optionally being substituted; a phenyl group or an aralkyl group having from 7 to 9 carbon atoms; and R' represents hydrogen, any of the groups which R may represent; a straight chain, branched chain or cyclic aliphatic acyl group having from 1 to 11 carbon atoms, optionally substituted by hydroxy, an amino group or a halogen atom; an aromatic acyl group, optionally substituted by hydroxy, amino, or a halogen atom; a straight chain, branched chain or cyclic aliphatic oxycarbonyl group having from 3 to 11 carbon atoms, or an aromatic oxycarbonyl group.
    • 式(I)的肽:X-A-B-C-Trp-D-Y,其中X表示氢,或末端硝基保护基选自酰基,芳族氧羰基,烷基,芳烷基和脂族氧基羰基; A代表价键或L-α-氨基酸残基; B代表L-α-亚氨基酸残基或L-α-氨基酸; C代表L-α-亚氨基酸残基或中性L-α-氨基酸残基; D表示价键或L-α-氨基酸残基; 并且Y表示羟基,氨基或式OR的基团,NHR,NR2或NH-NH-R',其中R表示直链,支链或环状(包括稠合或桥接的环)烷基,其具有至多 11个碳原子,任选被取代; 具有7至9个碳原子的苯基或芳烷基; 并且R'表示氢,R可以表示的任何基团; 具有1至11个碳原子的直链,支链或环状脂族酰基,任选被羟基,氨基或卤素原子取代; 任选被羟基,氨基或卤素原子取代的芳族酰基; 具有3至11个碳原子的直链,支链或环状脂族氧基羰基或芳族氧羰基。