JP2018536650A5 - - Google Patents

Info

Publication number

JP2018536650A5

JP2018536650A5 JP2018522067A JP2018522067A JP2018536650A5 JP 2018536650 A5 JP2018536650 A5 JP 2018536650A5 JP 2018522067 A JP2018522067 A JP 2018522067A JP 2018522067 A JP2018522067 A JP 2018522067A JP 2018536650 A5 JP2018536650 A5 JP 2018536650A5

Authority

JP

Japan

Prior art keywords

conjugate

antibody

seq

factor

sequence

Prior art date

2016-10-27

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.)

Pending

Links

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• 125000003275 alpha amino acid group Chemical group 0.000 claims 39
• 229920005862 polyol Polymers 0.000 claims 32
• 150000003077 polyols Chemical class 0.000 claims 32
• 239000003814 drug Substances 0.000 claims 21
• 230000000295 complement effect Effects 0.000 claims 18
• 238000006467 substitution reaction Methods 0.000 claims 14
• 206010064930 age-related macular degeneration Diseases 0.000 claims 12
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
• 239000002202 Polyethylene glycol Substances 0.000 claims 11
• 208000035475 disorder Diseases 0.000 claims 11
• 229920001223 polyethylene glycol Polymers 0.000 claims 11
• 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 7
• 125000005647 linker group Chemical group 0.000 claims 7
• 239000008194 pharmaceutical composition Substances 0.000 claims 7
• 208000005590 Choroidal Neovascularization Diseases 0.000 claims 6
• 206010060823 Choroidal neovascularisation Diseases 0.000 claims 6
• 208000008069 Geographic Atrophy Diseases 0.000 claims 6
• 108091007491 NSP3 Papain-like protease domains Proteins 0.000 claims 6
• 235000001014 amino acid Nutrition 0.000 claims 6
• 229940024606 amino acid Drugs 0.000 claims 6
• 239000005557 antagonist Substances 0.000 claims 6
• 201000005667 central retinal vein occlusion Diseases 0.000 claims 6
• 208000002780 macular degeneration Diseases 0.000 claims 6
• 208000004644 retinal vein occlusion Diseases 0.000 claims 6
• 229940124597 therapeutic agent Drugs 0.000 claims 6
• 125000003396 thiol group Chemical group [H]S* 0.000 claims 5
• 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 4
• 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 4
• 206010055665 Corneal neovascularisation Diseases 0.000 claims 3
• 206010012688 Diabetic retinal oedema Diseases 0.000 claims 3
• 206010012689 Diabetic retinopathy Diseases 0.000 claims 3
• 201000002563 Histoplasmosis Diseases 0.000 claims 3
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
• CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 3
• 208000007135 Retinal Neovascularization Diseases 0.000 claims 3
• 208000017442 Retinal disease Diseases 0.000 claims 3
• 206010038923 Retinopathy Diseases 0.000 claims 3
• 206010046851 Uveitis Diseases 0.000 claims 3
• 201000000159 corneal neovascularization Diseases 0.000 claims 3
• 208000001309 degenerative myopia Diseases 0.000 claims 3
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• 239000001257 hydrogen Substances 0.000 claims 3
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• 235000004400 serine Nutrition 0.000 claims 3
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• WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 2
• -1 His Chemical compound 0.000 claims 2
• 101000666856 Homo sapiens Vasoactive intestinal polypeptide receptor 1 Proteins 0.000 claims 2
• PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 2
• 208000022873 Ocular disease Diseases 0.000 claims 2
• MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 2
• 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 2
• 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 2
• 102100038388 Vasoactive intestinal polypeptide receptor 1 Human genes 0.000 claims 2
• 125000000539 amino acid group Chemical group 0.000 claims 2
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• 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 2
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• 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
• 102100022014 Angiopoietin-1 receptor Human genes 0.000 claims 1
• 102100034608 Angiopoietin-2 Human genes 0.000 claims 1
• FRYULLIZUDQONW-IMJSIDKUSA-N Asp-Asp Chemical group OC(=O)C[C@H](N)C(=O)N[C@@H](CC(O)=O)C(O)=O FRYULLIZUDQONW-IMJSIDKUSA-N 0.000 claims 1
• DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 1
• NOWKCMXCCJGMRR-UHFFFAOYSA-N Aziridine Chemical compound C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 claims 1
• 101000753291 Homo sapiens Angiopoietin-1 receptor Proteins 0.000 claims 1
• 101000924533 Homo sapiens Angiopoietin-2 Proteins 0.000 claims 1
• 101000955962 Homo sapiens Vacuolar protein sorting-associated protein 51 homolog Proteins 0.000 claims 1
• DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 1
• HAXFWIACAGNFHA-UHFFFAOYSA-N aldrithiol Chemical compound C=1C=CC=NC=1SSC1=CC=CC=N1 HAXFWIACAGNFHA-UHFFFAOYSA-N 0.000 claims 1
• 125000003277 amino group Chemical group 0.000 claims 1
• 235000009582 asparagine Nutrition 0.000 claims 1
• 229960001230 asparagine Drugs 0.000 claims 1
• 235000003704 aspartic acid Nutrition 0.000 claims 1
• OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 1
• 235000018417 cysteine Nutrition 0.000 claims 1
• XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
• 230000006240 deamidation Effects 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 230000000694 effects Effects 0.000 claims 1
• 150000002118 epoxides Chemical class 0.000 claims 1
• 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
• 235000013922 glutamic acid Nutrition 0.000 claims 1
• 239000004220 glutamic acid Substances 0.000 claims 1
• 208000028867 ischemia Diseases 0.000 claims 1
• 238000006317 isomerization reaction Methods 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• ZHCAAFJSYLFLPX-UHFFFAOYSA-N nitrocyclohexatriene Chemical group [O-][N+](=O)C1=CC=C=C[CH]1 ZHCAAFJSYLFLPX-UHFFFAOYSA-N 0.000 claims 1
• 150000003355 serines Chemical class 0.000 claims 1
• 238000002560 therapeutic procedure Methods 0.000 claims 1
• JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
• ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 claims 1