JP2017500018A5 - - Google Patents

Info

Publication number

JP2017500018A5

JP2017500018A5 JP2016532590A JP2016532590A JP2017500018A5 JP 2017500018 A5 JP2017500018 A5 JP 2017500018A5 JP 2016532590 A JP2016532590 A JP 2016532590A JP 2016532590 A JP2016532590 A JP 2016532590A JP 2017500018 A5 JP2017500018 A5 JP 2017500018A5

Authority

JP

Japan

Prior art keywords

apelin

seq

antigen

binding fragment

aplnr

Prior art date

2014-11-20

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 230000027455 binding Effects 0.000 claims 34
• 239000000427 antigen Substances 0.000 claims 31
• 102000036639 antigens Human genes 0.000 claims 31
• 108091007433 antigens Proteins 0.000 claims 31
• 239000012634 fragment Substances 0.000 claims 31
• 108010052412 Apelin Proteins 0.000 claims 27
• 108091008803 APLNR Proteins 0.000 claims 24
• 102000016555 Apelin receptors Human genes 0.000 claims 24
• 102000018746 Apelin Human genes 0.000 claims 22
• BWVPHIKGXQBZPV-QKFDDRBGSA-N apelin Chemical compound NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N1[C@H](C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=2NC=NC=2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=2NC=NC=2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CCSC)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(O)=O)CCC1 BWVPHIKGXQBZPV-QKFDDRBGSA-N 0.000 claims 20
• 125000003275 alpha amino acid group Chemical group 0.000 claims 19
• 102000004169 proteins and genes Human genes 0.000 claims 13
• 108090000623 proteins and genes Proteins 0.000 claims 13
• 230000001404 mediated effect Effects 0.000 claims 12
• 238000003556 assay Methods 0.000 claims 9
• 238000000338 in vitro Methods 0.000 claims 9
• 230000005764 inhibitory process Effects 0.000 claims 7
• 230000001593 cAMP accumulation Effects 0.000 claims 6
• 108010047041 Complementarity Determining Regions Proteins 0.000 claims 4
• 239000008194 pharmaceutical composition Substances 0.000 claims 4
• 108090000765 processed proteins & peptides Proteins 0.000 claims 4
• 101000793362 Homo sapiens Apelin receptor Proteins 0.000 claims 3
• 102000047215 human APLNR Human genes 0.000 claims 3
• 229920001184 polypeptide Polymers 0.000 claims 3
• 102000004196 processed proteins & peptides Human genes 0.000 claims 3
• 208000017442 Retinal disease Diseases 0.000 claims 2
• 206010038923 Retinopathy Diseases 0.000 claims 2
• 108010040480 apelin-13 peptide Proteins 0.000 claims 2
• 239000003085 diluting agent Substances 0.000 claims 2
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
• 239000003937 drug carrier Substances 0.000 claims 2
• 230000003993 interaction Effects 0.000 claims 2
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
• 102400000252 Apelin-13 Human genes 0.000 claims 1
• 102400000253 Apelin-31 Human genes 0.000 claims 1
• 101800001805 Apelin-31 Proteins 0.000 claims 1
• 102400000251 Apelin-36 Human genes 0.000 claims 1
• 101800001808 Apelin-36 Proteins 0.000 claims 1
• 101100246550 Caenorhabditis elegans pyr-1 gene Proteins 0.000 claims 1
• 108060003951 Immunoglobulin Proteins 0.000 claims 1
• 206010028980 Neoplasm Diseases 0.000 claims 1
• 208000034038 Pathologic Neovascularization Diseases 0.000 claims 1
• 125000000539 amino acid group Chemical group 0.000 claims 1
• QZNKGTRFBWGADN-SLUWFFAESA-N apelin-12 Chemical compound CC(C)C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N2CCC[C@H]2C(=O)N[C@@H](CCSC)C(=O)N3CCC[C@H]3C(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]4CCCN4C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCC(=O)N)N QZNKGTRFBWGADN-SLUWFFAESA-N 0.000 claims 1
• 108010006026 apelin-12 peptide Proteins 0.000 claims 1
• XXCCRHIAIBQDPX-PEWBXTNBSA-N apelin-13 Chemical compound C([C@@H](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCSC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](N)CCC(N)=O)C1=CN=CN1 XXCCRHIAIBQDPX-PEWBXTNBSA-N 0.000 claims 1
• 108010062131 apelin-14 Proteins 0.000 claims 1
• SVWSKJCJNAIKNH-MJZUAXFLSA-N apelin-17 Chemical compound C([C@@H](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCSC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](N)CCCCN)C1=CN=CN1 SVWSKJCJNAIKNH-MJZUAXFLSA-N 0.000 claims 1
• BVTLGARMSLXAHI-VDEROMQGSA-N apelin-36 Chemical compound C([C@@H](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCSC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)CNC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(C)C)C(C)C)C1=CN=CN1 BVTLGARMSLXAHI-VDEROMQGSA-N 0.000 claims 1
• 201000011510 cancer Diseases 0.000 claims 1
• 238000012875 competitive assay Methods 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000035475 disorder Diseases 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 230000000694 effects Effects 0.000 claims 1
• 102000018358 immunoglobulin Human genes 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 206010061289 metastatic neoplasm Diseases 0.000 claims 1
• BPGBAEXPBQHBSV-UHFFFAOYSA-N pyr1 Chemical compound C1=C2C3=C(C)C(C(NC=C4)=O)=C4C(C)=C3NC2=CC=C1OC(=O)C1=CC=CC=C1 BPGBAEXPBQHBSV-UHFFFAOYSA-N 0.000 claims 1