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ANTIANGIOGENIC COMPOUNDS
专利权人:
КОВКС ТЕКНОЛОДЖИЗ АЙЭЛЭНД ЛИМИТЕД (IE)
发明人:
ДОППАЛППУДИ Венката Рамана (US),ЛАЙ Цзин-Юй (US),ЛЮ Бинь (US),ЛЮ Динго (US),ДЕШАРНАЙС Джоэл (US),БХАТ Абхиджит Суреш (US),ФУ Яньвэнь (US),ОУТС Брайан Дуглас (US),ЧЕНЬ Ган (US),БРЭДШОУ Курт Уилльям (US
申请号:
RU2010149608/10
公开号:
RU2010149608A
申请日:
2009.05.04
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. The compound of formula R1- [VEGF-Peptide] -R2, where [VEGF-Peptide] is a peptide having the sequence:! V1-E2-P3-N4-C5-D6-I7-H8-V9-M10-W11-V12-W13-X14-C15-F16-E17-R18-X 19-X 20-X 21-X 22-X 23 (SEQ ID NO: 126), where R1 is absent or represents CH3, C (O) CH3, C (O) CH2CH3, C (O) CH2CH2CH3, C (O) CH (CH3) CH3, C (O) CH2CH2CH2CH3, C (O) CH (CH3) CH2CH3, C (O) C6H5, C (O) CH2CH2 (CH2CH2O) 1-5Me, amido-2-PEG, N-acyl and N-alkyl, amino-protecting group, lipid fatty acid group or hydrocarbon; and R2 is absent or represents OH, NH2, NH (CH3), NHCH2CH3, NHCH2CH2CH3, NHCH (CH3) CH3, NHCH2CH2CH2CH3, NHCH (CH3) CH2CH3, NHC6H5, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxylic acid protecting group, a fatty acid group and X14 is E or V, X19 may be any residue of a hydrophobic amino acid or its D isomer, X20 may be absent, or may be any neutral, hydrophobic or aromatic amino acid or its D isomer, X21 may be absent, or may be any positively charged the residue or any aliphatic non-polar residue or its D-iso form, X22 may be absent or may be selected from the group consisting of G, V, L, I, P, S, T, W, F, E, Kac or their D-isomers, X23 may be absent or selected from the group consisting from G, A, I, L, Q, E, F, T, S, Y, and Kac and their D isomers, and where one is from the group consisting of V1, E2, P3, N4, V9, M10, V12 , X14, E17, and the C-terminal residue may be substituted by a binding residue containing a nucleophilic side chain of an amino group of the N-terminus or a carboxyl group of the C-terminus covalently linked to the antibody binding site directly or via an intermediate linker, the connecting residue selected from the group consisting of K, R, Y, C, T, S, homologues of lysine, homocysteine, homoserine, Dap, Dab, N-terminal residue and C-terminal residue, or a pharmaceutically acceptable salt thereof. ! 2. Connected1. Соединению формулы R1-[VEGF-Пептид]-R2, где [VEGF-Пептид] представляет пептид, имеющий последовательность: ! V1-E2-P3-N4-C5-D6-I7-H8-V9-M10-W11-V12-W1
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