发明名称 CONJUGATE VACCINE USING TRIMMING FUNCTION OF ERAP1
摘要 The present invention provides a compound represented by the formula (1):;;wherein Xa and Ya are each a single bond or the like, cancer antigen peptide A is an MHC class I-restricted cancer antigen peptide, and R1 is a hydrogen atom; a group represented by the formula (2): ;;wherein Xb and Yb are each a single bond or the like, and cancer antigen peptide B is different from the cancer antigen peptide A and is an MHC class I or II-restricted cancer antigen peptide; a group represented by the formula (3):;;wherein Xc and Yc are each a single bond or the like, and cancer antigen peptide C is an MHC class II-restricted cancer antigen peptide; or cancer antigen peptide D, wherein the cancer antigen peptide D is an MHC class I or II-restricted cancer antigen peptide containing one cysteine residue, or a salt thereof, for example.
申请公布号 US2016045582(A1) 申请公布日期 2016.02.18
申请号 US201414780241 申请日期 2014.03.28
申请人 SUMITOMO DAINIPPON PHARMA CO., LTD. 发明人 BAN Hitoshi;NISHIO Yukihiro;GOTO Masashi;TAKANASHI Yosuke
分类号 A61K39/00;C12N9/12;A61K47/48 主分类号 A61K39/00
代理机构 代理人
主权项 1. A compound represented by formula (1):or a pharmaceutically acceptable salt thereof, wherein Xa and Ya are each independently a single bond or a divalent peptide group consisting of 1-4 amino acid residues, and a total of the amino acid residue number for Xa and the amino acid residue number for Ya is an integer of 0-4, cancer antigen peptide A is an MHC class I-restricted cancer antigen peptide consisting of 7-30 amino acid residues, an amino group of an N-terminal amino acid of the cancer antigen peptide A binds to Ya in the formula (1), and a carbonyl group of a C-terminal amino acid of the cancer antigen peptide A binds to a hydroxyl group in the formula (1), and R1 is a hydrogen atom; a group represented by formula (2):wherein Xb and Yb are each independently a single bond or a divalent peptide group consisting of 1-4 amino acid residues, and a total of the amino acid residue number for Xb and the amino acid residue number for Yb is an integer of 0-4, cancer antigen peptide B is different from the cancer antigen peptide A, and is an MHC class I-restricted cancer antigen peptide consisting of 7-30 amino acid residues or an MHC class II-restricted cancer antigen peptide consisting of 7-30 amino acid residues, an amino group of an N-terminal amino acid of the cancer antigen peptide B binds to Yb in the formula (2), and a carbonyl group of a C-terminal amino acid of the cancer antigen peptide B binds to a hydroxyl group in the formula (2), and a thioether group in the formula (2) binds to a thioether group in the formula (1); a group represented by formula (3):wherein Xc and Yc are each independently a single bond or a divalent peptide group consisting of 1-4 amino acid residues, and a total of the amino acid residue number for Xc and the amino acid residue number for Yc is an integer of 0-4, cancer antigen peptide C is an MHC class II-restricted cancer antigen peptide consisting of 7-30 amino acid residues, a carbonyl group of a C-terminal amino acid of the cancer antigen peptide C binds to Xc in the formula (3), and an amino group of an N-terminal amino acid of the cancer antigen peptide C binds to a hydrogen atom in the formula (3), and a thioether group in the formula (3) binds to a thioether group in the formula (1); or cancer antigen peptide D,wherein the cancer antigen peptide D is an MHC class I-restricted cancer antigen peptide consisting of 7-30 amino acid residues containing one cysteine residue or an MHC class II-restricted cancer antigen peptide consisting of 7-30 amino acid residues containing one cysteine residue, and a thioether group of the cysteine residue of the cancer antigen peptide D binds to a thioether group in the formula (1), provided when R1 is a hydrogen atom, the sequence of the formula (1) is not identical to the partial sequence of a cancer antigen protein.
地址 Osaka-shi, Osaka JP