JP2015518825A5 - - Google Patents

Info

Publication number

JP2015518825A5

JP2015518825A5 JP2015512647A JP2015512647A JP2015518825A5 JP 2015518825 A5 JP2015518825 A5 JP 2015518825A5 JP 2015512647 A JP2015512647 A JP 2015512647A JP 2015512647 A JP2015512647 A JP 2015512647A JP 2015518825 A5 JP2015518825 A5 JP 2015518825A5

Authority

JP

Japan

Prior art keywords

group

drugs

pharmaceutical composition

scaffold

poly

Prior art date

2013-03-14

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
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• 150000001875 compounds Chemical class 0.000 claims description 17
• 229930003316 Vitamin D Natural products 0.000 claims description 11
• QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims description 11
• 108090000765 processed proteins & peptides Proteins 0.000 claims description 11
• 102000004169 proteins and genes Human genes 0.000 claims description 11
• 108090000623 proteins and genes Proteins 0.000 claims description 11
• 235000019166 vitamin D Nutrition 0.000 claims description 11
• 239000011710 vitamin D Substances 0.000 claims description 11
• 229940046008 vitamin d Drugs 0.000 claims description 11
• 150000003710 vitamin D derivatives Chemical class 0.000 claims description 10
• 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 claims description 3
• 239000000126 substance Substances 0.000 claims description 3
• 229940079593 drug Drugs 0.000 claims 40
• 239000003814 drug Substances 0.000 claims 40
• 239000008194 pharmaceutical composition Substances 0.000 claims 24
• 230000001225 therapeutic effect Effects 0.000 claims 22
• 238000000034 method Methods 0.000 claims 16
• 230000008685 targeting Effects 0.000 claims 15
• 108020004707 nucleic acids Proteins 0.000 claims 13
• 150000007523 nucleic acids Chemical class 0.000 claims 13
• 102000039446 nucleic acids Human genes 0.000 claims 13
• -1 glycans Polymers 0.000 claims 12
• 229910052799 carbon Inorganic materials 0.000 claims 7
• 229920001223 polyethylene glycol Polymers 0.000 claims 7
• 125000003275 alpha amino acid group Chemical group 0.000 claims 6
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
• 229920002873 Polyethylenimine Polymers 0.000 claims 5
• 108010039918 Polylysine Proteins 0.000 claims 5
• 150000001413 amino acids Chemical class 0.000 claims 5
• 230000000694 effects Effects 0.000 claims 5
• 125000005647 linker group Chemical group 0.000 claims 5
• 229920000656 polylysine Polymers 0.000 claims 5
• 229920001451 polypropylene glycol Polymers 0.000 claims 5
• 229920003169 water-soluble polymer Polymers 0.000 claims 5
• 108091093037 Peptide nucleic acid Proteins 0.000 claims 4
• 239000008280 blood Substances 0.000 claims 4
• 210000004369 blood Anatomy 0.000 claims 4
• 238000002825 functional assay Methods 0.000 claims 4
• 230000002503 metabolic effect Effects 0.000 claims 4
• JJAHTWIKCUJRDK-UHFFFAOYSA-N succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate Chemical group C1CC(CN2C(C=CC2=O)=O)CCC1C(=O)ON1C(=O)CCC1=O JJAHTWIKCUJRDK-UHFFFAOYSA-N 0.000 claims 4
• 125000003396 thiol group Chemical group [H]S* 0.000 claims 4
• 230000001268 conjugating effect Effects 0.000 claims 3
• 239000003937 drug carrier Substances 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
• 108091023037 Aptamer Proteins 0.000 claims 2
• 102000015081 Blood Coagulation Factors Human genes 0.000 claims 2
• 108010039209 Blood Coagulation Factors Proteins 0.000 claims 2
• 208000019399 Colonic disease Diseases 0.000 claims 2
• 239000004971 Cross linker Substances 0.000 claims 2
• 108090000695 Cytokines Proteins 0.000 claims 2
• 102000004127 Cytokines Human genes 0.000 claims 2
• 108090000790 Enzymes Proteins 0.000 claims 2
• 102000004190 Enzymes Human genes 0.000 claims 2
• 102000003973 Fibroblast growth factor 21 Human genes 0.000 claims 2
• 108090000376 Fibroblast growth factor 21 Proteins 0.000 claims 2
• 208000018522 Gastrointestinal disease Diseases 0.000 claims 2
• 101800001586 Ghrelin Proteins 0.000 claims 2
• 102000012004 Ghrelin Human genes 0.000 claims 2
• 108090000288 Glycoproteins Proteins 0.000 claims 2
• 102000003886 Glycoproteins Human genes 0.000 claims 2
• 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 2
• 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 2
• 102000014150 Interferons Human genes 0.000 claims 2
• 108010050904 Interferons Proteins 0.000 claims 2
• 208000018501 Lymphatic disease Diseases 0.000 claims 2
• 125000003172 aldehyde group Chemical group 0.000 claims 2
• 150000001412 amines Chemical group 0.000 claims 2
• 230000000202 analgesic effect Effects 0.000 claims 2
• 239000003242 anti bacterial agent Substances 0.000 claims 2
• 229940127003 anti-diabetic drug Drugs 0.000 claims 2
• 230000000843 anti-fungal effect Effects 0.000 claims 2
• 229940124599 anti-inflammatory drug Drugs 0.000 claims 2
• 230000001754 anti-pyretic effect Effects 0.000 claims 2
• 230000000692 anti-sense effect Effects 0.000 claims 2
• 229940124350 antibacterial drug Drugs 0.000 claims 2
• 229940088710 antibiotic agent Drugs 0.000 claims 2
• 239000003472 antidiabetic agent Substances 0.000 claims 2
• 229940121375 antifungal agent Drugs 0.000 claims 2
• 239000002246 antineoplastic agent Substances 0.000 claims 2
• 229940041181 antineoplastic drug Drugs 0.000 claims 2
• 239000002221 antipyretic Substances 0.000 claims 2
• 239000003443 antiviral agent Substances 0.000 claims 2
• 230000001588 bifunctional effect Effects 0.000 claims 2
• 239000003114 blood coagulation factor Substances 0.000 claims 2
• 229940019700 blood coagulation factors Drugs 0.000 claims 2
• VPKDCDLSJZCGKE-UHFFFAOYSA-N carbodiimide group Chemical group N=C=N VPKDCDLSJZCGKE-UHFFFAOYSA-N 0.000 claims 2
• 239000002327 cardiovascular agent Substances 0.000 claims 2
• 229940125692 cardiovascular agent Drugs 0.000 claims 2
• 208000010643 digestive system disease Diseases 0.000 claims 2
• 239000012636 effector Substances 0.000 claims 2
• 208000018685 gastrointestinal system disease Diseases 0.000 claims 2
• 230000009368 gene silencing by RNA Effects 0.000 claims 2
• GNKDKYIHGQKHHM-RJKLHVOGSA-N ghrelin Chemical compound C([C@H](NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)CN)COC(=O)CCCCCCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C1=CC=CC=C1 GNKDKYIHGQKHHM-RJKLHVOGSA-N 0.000 claims 2
• 239000003102 growth factor Substances 0.000 claims 2
• 125000005179 haloacetyl group Chemical group 0.000 claims 2
• 239000005556 hormone Substances 0.000 claims 2
• 229940088597 hormone Drugs 0.000 claims 2
• 229940079322 interferon Drugs 0.000 claims 2
• 210000003734 kidney Anatomy 0.000 claims 2
• 210000004185 liver Anatomy 0.000 claims 2
• 210000004072 lung Anatomy 0.000 claims 2
• 239000000203 mixture Substances 0.000 claims 2
• 208000017520 skin disease Diseases 0.000 claims 2
• 150000003384 small molecules Chemical class 0.000 claims 2
• 208000018556 stomach disease Diseases 0.000 claims 2
• 238000007920 subcutaneous administration Methods 0.000 claims 2
• 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 2
• 230000024033 toxin binding Effects 0.000 claims 2
• 238000002965 ELISA Methods 0.000 claims 1
• 238000006352 cycloaddition reaction Methods 0.000 claims 1
• 125000002228 disulfide group Chemical group 0.000 claims 1
• 238000009472 formulation Methods 0.000 claims 1
• 230000003054 hormonal effect Effects 0.000 claims 1
• 238000001802 infusion Methods 0.000 claims 1
• 238000002347 injection Methods 0.000 claims 1
• 239000007924 injection Substances 0.000 claims 1
• 238000007917 intracranial administration Methods 0.000 claims 1
• 238000007918 intramuscular administration Methods 0.000 claims 1
• 238000007913 intrathecal administration Methods 0.000 claims 1
• 238000001990 intravenous administration Methods 0.000 claims 1
• 229920000747 poly(lactic acid) Polymers 0.000 claims 1
• 239000004626 polylactic acid Substances 0.000 claims 1
• 230000000699 topical effect Effects 0.000 claims 1
• ASUGWWOMVNVWAW-UHFFFAOYSA-N 1-(2-methoxyethyl)pyrrole-2,5-dione Chemical compound COCCN1C(=O)C=CC1=O ASUGWWOMVNVWAW-UHFFFAOYSA-N 0.000 description 1
• XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
• PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 description 1
• 229940125904 compound 1 Drugs 0.000 description 1
• 235000018102 proteins Nutrition 0.000 description 1
• 239000007858 starting material Substances 0.000 description 1