JP2013528570A5 - - Google Patents

Info

Publication number

JP2013528570A5

JP2013528570A5 JP2013502023A JP2013502023A JP2013528570A5 JP 2013528570 A5 JP2013528570 A5 JP 2013528570A5 JP 2013502023 A JP2013502023 A JP 2013502023A JP 2013502023 A JP2013502023 A JP 2013502023A JP 2013528570 A5 JP2013528570 A5 JP 2013528570A5

Authority

JP

Japan

Prior art keywords

group

region

groups

moiety

intact antibody

Prior art date

2011-03-31

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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• 238000009472 formulation Methods 0.000 claims 12
• 239000000203 mixture Substances 0.000 claims 12
• 150000001875 compounds Chemical class 0.000 claims 8
• 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 8
• 238000000034 method Methods 0.000 claims 6
• -1 optionally Chemical group 0.000 claims 6
• 150000003839 salts Chemical class 0.000 claims 6
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
• 125000002723 alicyclic group Chemical group 0.000 claims 4
• 125000003275 alpha amino acid group Chemical group 0.000 claims 4
• 125000003118 aryl group Chemical group 0.000 claims 4
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
• 125000001072 heteroaryl group Chemical group 0.000 claims 4
• 125000005842 heteroatom Chemical group 0.000 claims 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
• 239000007788 liquid Substances 0.000 claims 4
• 229910052760 oxygen Inorganic materials 0.000 claims 4
• 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
• 125000005843 halogen group Chemical group 0.000 claims 3
• 125000000468 ketone group Chemical group 0.000 claims 3
• 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 2
• RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
• 229910019142 PO4 Inorganic materials 0.000 claims 2
• 241000725643 Respiratory syncytial virus Species 0.000 claims 2
• 206010052779 Transplant rejections Diseases 0.000 claims 2
• DVKFVGVMPLXLKC-PUGXJXRHSA-N [(2s,3r,4s,5s,6r)-2-[(2s,3s,4s,5r)-3,4-dihydroxy-2,5-bis(hydroxymethyl)oxolan-2-yl]-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] dihydrogen phosphate Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@]1(CO)[C@@]1(OP(O)(O)=O)[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 DVKFVGVMPLXLKC-PUGXJXRHSA-N 0.000 claims 2
• 206010064930 age-related macular degeneration Diseases 0.000 claims 2
• 239000010452 phosphate Substances 0.000 claims 2
• 230000001105 regulatory effect Effects 0.000 claims 2
• 230000000087 stabilizing effect Effects 0.000 claims 2
• 208000023275 Autoimmune disease Diseases 0.000 claims 1
• KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical compound NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims 1
• 208000024172 Cardiovascular disease Diseases 0.000 claims 1
• 208000011231 Crohn disease Diseases 0.000 claims 1
• 229930194542 Keto Natural products 0.000 claims 1
• 201000006165 Kuhnt-Junius degeneration Diseases 0.000 claims 1
• 241000124008 Mammalia Species 0.000 claims 1
• 206010028980 Neoplasm Diseases 0.000 claims 1
• 208000000733 Paroxysmal Hemoglobinuria Diseases 0.000 claims 1
• 102100036050 Phosphatidylinositol N-acetylglucosaminyltransferase subunit A Human genes 0.000 claims 1
• ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical group OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 1
• 201000004681 Psoriasis Diseases 0.000 claims 1
• RYYWUUFWQRZTIU-UHFFFAOYSA-N Thiophosphoric acid Chemical group OP(O)(S)=O RYYWUUFWQRZTIU-UHFFFAOYSA-N 0.000 claims 1
• 208000000208 Wet Macular Degeneration Diseases 0.000 claims 1
• VRKQBSISJQUWFI-PIRXJBDWSA-N [(2R,3R,4R,5S,6R)-3,4-dihydroxy-6-(hydroxymethyl)-5-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl] dihydrogen phosphate Chemical compound P(=O)(O)(O)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO VRKQBSISJQUWFI-PIRXJBDWSA-N 0.000 claims 1
• 125000003172 aldehyde group Chemical group 0.000 claims 1
• 150000001299 aldehydes Chemical class 0.000 claims 1
• HXXFSFRBOHSIMQ-FPRJBGLDSA-N alpha-D-galactose 1-phosphate Chemical compound OC[C@H]1O[C@H](OP(O)(O)=O)[C@H](O)[C@@H](O)[C@H]1O HXXFSFRBOHSIMQ-FPRJBGLDSA-N 0.000 claims 1
• 125000003277 amino group Chemical group 0.000 claims 1
• 238000004873 anchoring Methods 0.000 claims 1
• 208000006673 asthma Diseases 0.000 claims 1
• 229960000397 bevacizumab Drugs 0.000 claims 1
• 230000023555 blood coagulation Effects 0.000 claims 1
• 201000011510 cancer Diseases 0.000 claims 1
• XPPKVPWEQAFLFU-UHFFFAOYSA-N diphosphoric acid Chemical group OP(O)(=O)OP(O)(O)=O XPPKVPWEQAFLFU-UHFFFAOYSA-N 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000035475 disorder Diseases 0.000 claims 1
• 239000002552 dosage form Substances 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 125000001475 halogen functional group Chemical group 0.000 claims 1
• 208000015181 infectious disease Diseases 0.000 claims 1
• 238000001990 intravenous administration Methods 0.000 claims 1
• 150000002576 ketones Chemical class 0.000 claims 1
• VRKQBSISJQUWFI-QUYVBRFLSA-N maltose 1-phosphate Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)O[C@H](OP(O)(O)=O)[C@H](O)[C@H]1O VRKQBSISJQUWFI-QUYVBRFLSA-N 0.000 claims 1
• 230000000873 masking effect Effects 0.000 claims 1
• 150000004712 monophosphates Chemical group 0.000 claims 1
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
• 125000004430 oxygen atom Chemical group O* 0.000 claims 1
• 201000003045 paroxysmal nocturnal hemoglobinuria Diseases 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 1
• ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical group [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 claims 1
• 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
• 125000003003 spiro group Chemical group 0.000 claims 1
• QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
• 125000001273 sulfonato group Chemical group [O-]S(*)(=O)=O 0.000 claims 1
• 125000002264 triphosphate group Chemical group [H]OP(=O)(O[H])OP(=O)(O[H])OP(=O)(O[H])O* 0.000 claims 1