RU2016151190A - Соединения, включающие саморасщепляющуюся группу - Google Patents
Соединения, включающие саморасщепляющуюся группу Download PDFInfo
- Publication number
- RU2016151190A RU2016151190A RU2016151190A RU2016151190A RU2016151190A RU 2016151190 A RU2016151190 A RU 2016151190A RU 2016151190 A RU2016151190 A RU 2016151190A RU 2016151190 A RU2016151190 A RU 2016151190A RU 2016151190 A RU2016151190 A RU 2016151190A
- Authority
- RU
- Russia
- Prior art keywords
- compound
- integer
- alkyl
- protein
- chemical formula
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 30
- 235000018102 proteins Nutrition 0.000 claims 12
- 102000004169 proteins and genes Human genes 0.000 claims 12
- 108090000623 proteins and genes Proteins 0.000 claims 12
- 239000000126 substance Substances 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000002947 alkylene group Chemical group 0.000 claims 9
- 125000005647 linker group Chemical group 0.000 claims 8
- 125000003275 alpha amino acid group Chemical group 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 108090000992 Transferases Proteins 0.000 claims 5
- 102000004357 Transferases Human genes 0.000 claims 5
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 4
- 238000006243 chemical reaction Methods 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 3
- 235000001014 amino acid Nutrition 0.000 claims 3
- 239000012620 biological material Chemical group 0.000 claims 3
- -1 isoprenyl Chemical class 0.000 claims 3
- 229920001184 polypeptide Polymers 0.000 claims 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 3
- 102000004196 processed proteins & peptides Human genes 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- ZJNLYGOUHDJHMG-UHFFFAOYSA-N 1-n,4-n-bis(5-methylhexan-2-yl)benzene-1,4-diamine Chemical compound CC(C)CCC(C)NC1=CC=C(NC(C)CCC(C)C)C=C1 ZJNLYGOUHDJHMG-UHFFFAOYSA-N 0.000 claims 2
- HSJKGGMUJITCBW-UHFFFAOYSA-N 3-hydroxybutanal Chemical compound CC(O)CC=O HSJKGGMUJITCBW-UHFFFAOYSA-N 0.000 claims 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 2
- 108010038807 Oligopeptides Proteins 0.000 claims 2
- 102000015636 Oligopeptides Human genes 0.000 claims 2
- 108010081667 aflibercept Proteins 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229960003989 tocilizumab Drugs 0.000 claims 2
- 125000006659 (C1-C20) hydrocarbyl group Chemical group 0.000 claims 1
- 125000006736 (C6-C20) aryl group Chemical group 0.000 claims 1
- MJZJYWCQPMNPRM-UHFFFAOYSA-N 6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine Chemical compound CC1(C)N=C(N)N=C(N)N1OCCCOC1=CC(Cl)=C(Cl)C=C1Cl MJZJYWCQPMNPRM-UHFFFAOYSA-N 0.000 claims 1
- 101100208110 Arabidopsis thaliana TRX4 gene Proteins 0.000 claims 1
- 102100022005 B-lymphocyte antigen CD20 Human genes 0.000 claims 1
- 101100425276 Dictyostelium discoideum trxD gene Proteins 0.000 claims 1
- 238000005698 Diels-Alder reaction Methods 0.000 claims 1
- 108010008165 Etanercept Proteins 0.000 claims 1
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 claims 1
- 102000013404 Geranyltranstransferase Human genes 0.000 claims 1
- 108010026318 Geranyltranstransferase Proteins 0.000 claims 1
- 101000897405 Homo sapiens B-lymphocyte antigen CD20 Proteins 0.000 claims 1
- 238000006736 Huisgen cycloaddition reaction Methods 0.000 claims 1
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical compound ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 1
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 1
- 101100154863 Mus musculus Txndc2 gene Proteins 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 229960000446 abciximab Drugs 0.000 claims 1
- 229960002833 aflibercept Drugs 0.000 claims 1
- 150000001299 aldehydes Chemical class 0.000 claims 1
- IAJILQKETJEXLJ-QTBDOELSSA-N aldehydo-D-glucuronic acid Chemical compound O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C(O)=O IAJILQKETJEXLJ-QTBDOELSSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940121375 antifungal agent Drugs 0.000 claims 1
- 239000003429 antifungal agent Substances 0.000 claims 1
- 239000000427 antigen Substances 0.000 claims 1
- 230000000890 antigenic effect Effects 0.000 claims 1
- 102000036639 antigens Human genes 0.000 claims 1
- 108091007433 antigens Proteins 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003096 antiparasitic agent Substances 0.000 claims 1
- 229940125687 antiparasitic agent Drugs 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- 229960004669 basiliximab Drugs 0.000 claims 1
- 229960000397 bevacizumab Drugs 0.000 claims 1
- 229960001838 canakinumab Drugs 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 1
- 150000001728 carbonyl compounds Chemical class 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 229960003115 certolizumab pegol Drugs 0.000 claims 1
- 229960005395 cetuximab Drugs 0.000 claims 1
- 238000012650 click reaction Methods 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
- 229960002806 daclizumab Drugs 0.000 claims 1
- 229960001251 denosumab Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 229960002224 eculizumab Drugs 0.000 claims 1
- 229960000284 efalizumab Drugs 0.000 claims 1
- 125000006575 electron-withdrawing group Chemical group 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 229960000403 etanercept Drugs 0.000 claims 1
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 claims 1
- 125000004030 farnesyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])C([H])([H])C([H])=C(C([H])([H])[H])C([H])([H])C([H])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 229960003297 gemtuzumab ozogamicin Drugs 0.000 claims 1
- 125000002686 geranylgeranyl group Chemical group [H]C([*])([H])/C([H])=C(C([H])([H])[H])/C([H])([H])C([H])([H])/C([H])=C(C([H])([H])[H])/C([H])([H])C([H])([H])/C([H])=C(C([H])([H])[H])/C([H])([H])C([H])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 229940097043 glucuronic acid Drugs 0.000 claims 1
- 229960001743 golimumab Drugs 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002519 immonomodulatory effect Effects 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 229960000598 infliximab Drugs 0.000 claims 1
- 229950004101 inotuzumab ozogamicin Drugs 0.000 claims 1
- 229960005386 ipilimumab Drugs 0.000 claims 1
- 125000000468 ketone group Chemical group 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 229960005108 mepolizumab Drugs 0.000 claims 1
- 229960003816 muromonab-cd3 Drugs 0.000 claims 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
- 229960005027 natalizumab Drugs 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 238000010534 nucleophilic substitution reaction Methods 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 229960000402 palivizumab Drugs 0.000 claims 1
- 229960001972 panitumumab Drugs 0.000 claims 1
- 229960002087 pertuzumab Drugs 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 229960003876 ranibizumab Drugs 0.000 claims 1
- 229960001886 rilonacept Drugs 0.000 claims 1
- 108010046141 rilonacept Proteins 0.000 claims 1
- 229960004641 rituximab Drugs 0.000 claims 1
- 108010017584 romiplostim Proteins 0.000 claims 1
- 229960004262 romiplostim Drugs 0.000 claims 1
- 239000000523 sample Substances 0.000 claims 1
- WUWDLXZGHZSWQZ-WQLSENKSSA-N semaxanib Chemical compound N1C(C)=CC(C)=C1\C=C/1C2=CC=CC=C2NC\1=O WUWDLXZGHZSWQZ-WQLSENKSSA-N 0.000 claims 1
- 239000000758 substrate Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- 229960003824 ustekinumab Drugs 0.000 claims 1
- 229950000815 veltuzumab Drugs 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
- A61K47/6813—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin the drug being a peptidic cytokine, e.g. an interleukin or interferon
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
- A61K47/6855—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6871—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting an enzyme
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D309/10—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K19/00—Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
- C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- C07K2317/94—Stability, e.g. half-life, pH, temperature or enzyme-resistance
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Cell Biology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (92)
1. Соединение, включающее саморасщепляющуюся группу, представленную следующей химической формулой 1:
[Химическая формула 1]
G представляет собой группу глюкуроновой кислоты или ее производное;
A представляет собой (C1-C20)гидрокарбил, биоматериал или модифицированный биоматериал;
B представляет собой (C1-C100)гидрокарбил;
W представляет собой электроноакцепторную группу;
Z представляет собой водород, (C1-C8)алкил, галоген, циано или нитро;
n представляет собой целое число от 1 до 3, и, когда n представляет собой целое число 2 или более, каждый из заместителей Z являются одинаковыми или отличными друг от друга;
L представляет собой линкер, связывающий A и W саморасщепляющейся группы при помощи ковалентных связей; и
R1 и R2, каждый независимо, представляют собой водород, (C1-C8)алкил или (C3-C8)циклоалкил.
2. Соединение по п. 1, где G представляет собой
R3 представляет собой водород или защитную группу карбоксила, и R4(s), каждый независимо, представляют собой водород или защитную группу гидроксила.
3. Соединение по п. 1, где W представляет собой -C(O)-, -C(O)NRʹ-, -C(O)O-, -SO2NRʹ-, -P(O)RʹʹNRʹ-, -SONRʹ- или -PO2NRʹ-, и Rʹ и Rʺ, каждый независимо, представляют собой водород, (C1-C8)алкил, (C3-C8)циклоалкил, (C1-C8)алкокси, (C1-C8)алкилтио, моно- или ди-(C1-C8)алкиламино, (C3-C20)гетероарил или (C6-C20)арил.
4. Соединение по п. 1, где линкер L представляет собой алкилен, содержащий от 1 до 50 атомов углерода, и удовлетворяет по меньшей мере одному из следующих условий (i) - (iv):
(i) алкилен включает по меньшей мере одну ненасыщенную связь,
(ii) алкилен включает по меньшей мере один гетероарилен,
(iii) атом углерода алкилена замещен одним или несколькими гетероатомами, выбранными из азота (N), кислорода (О) и серы (S), и
(iv) алкилен дополнительно замещен одним или несколькими алкилами, содержащими от 1 до 20 атомов углерода.
5. Соединение по п. 1, где линкер L включает по меньшей мере одно звено, представляющее собой изопрениловое производное, представленное следующей химической формулой A, которое распознается изопреноид-трансферазой.
[Химическая формула A]
6. Соединение по п. 5, где линкер L дополнительно включает связывающее звено, образованное в результате реакций 1,3-диполярного циклоприсоединения, гетеро-реакций Дильса-Альдера, реакций нуклеофильного замещения, реакций карбонильных соединений не-альдольного типа, присоединений по месту кратных связей углерод-углерод, реакций окисления или клик-реакций.
7. Соединение по п. 6, где связывающее звено образовано путем реакции между ацетиленом и азидом или реакции между группой альдегида или кетона и гидразином или гидроксиламином.
8. Соединение по п. 7, где связывающее звено представлено следующей химической формулой B, C, D или E:
[Химическая формула B]
[Химическая формула C]
[Химическая формула D]
[Химическая формула E]
L1 представляет собой простую связь или алкилен, содержащий от 1 до 30 атомов углерода;
R11 представляет собой водород или алкил, содержащий от 1 до 10 атомов углерода; и
L2 представляет собой алкилен, содержащий от 1 до 30 атомов углерода.
9. Соединение по п. 6, где линкер L дополнительно включает соединительное звено, представленное следующей химической формулой F или G:
[Химическая формула F]
-(CH2)r(V(CH2)p)q-
[Химическая формула G]
-(CH2CH2X)w-
V представляет собой простую связь, -O-, -S-, -NR21-, -C(O)NR22-, -NR23C(O)-, -NR24SO2- или -SO2NR25-;
X представляет собой -O-, (C1-C8)алкилен или -NR21-;
R21 - R25, каждый независимо, представляют собой водород, (C1-C6)алкил, (C1-C6)алкил(C6-C20)арил или (C1-C6)алкил(C3-C20)гетероарил;
r представляет собой целое число от 1 до 10;
p представляет собой целое число от 0 до 10;
q представляет собой целое число от 1 до 10; и
w представляет собой целое число от 1 до 10.
10. Соединение по п. 1, где, когда A представляет собой гидрокарбил, содержащий от 1 до 20 атомов углерода, L представляет собой , или , V представляет собой простую связь, -O-, -S-, -NR21-, -C(O)NR22-, -NR23C(O)-, -NR24SO2- или -SO2NR25-, R21 - R25, каждый независимо, представляют собой водород, (C1-C6)алкил, (C1-C6)алкил(C6-C20)арил или (C1-C6)алкил(C3-C20)гетероарил, r представляет собой целое число от 1 до 10, p представляет собой целое число от 0 до 10, q представляет собой целое число от 1 до 10, и L1 представляет собой простую связь.
11. Соединение по п. 1, где биоматериал представляет собой белок.
12. Соединение по п. 11, где белок представляет собой олигопептид, полипептид, антитело, фрагмент антигенного полипептида или repebody.
13. Соединение по п. 12, где белок содержит аминокислотный мотив, который должен распознаваться изопреноид-трансферазой.
14. Соединение по п. 13, где белок дополнительно включает спейсерное звено, состоящее из аминокислоты, олигопептида или полипептида, между белком и аминокислотным мотивом.
15. Соединение по п. 13 или 14, где белок ковалентно связан с линкером L через аминокислотный мотив.
16. Соединение по п. 15, где аминокислотный мотив ковалентно связан с C-концом белка или ковалентно связан с по меньшей мере одним спейсерным звеном, ковалентно связанным с C-концом белка.
17. Соединение по п. 16, где C-конец белка представляет собой C-конец легкой цепи или тяжелой цепи антитела.
18. Соединение по п. 13, где изопреноид-трансфераза представляет собой фарнезилпротеинтрансферазу (FTаза) или геранилгеранилтрансферазу (GGTаза).
19. Соединение по п. 12, где антитело выбрано из группы, состоящей из интактных поликлональных антител, интактных моноклональных антител, фрагментов антител, одноцепочечных Fv-мутантов (scFv), мультиспецифичных антител, биспецифичных антител, химерных антител, гуманизированных антител, человеческих антител, гибридных белков, включающих антиген-определяющую часть антитела, и других модифицированных молекул иммуноглобулинов, включающих сайт распознавания антигена.
20. Соединение по п. 19, где антитело выбрано из группы, состоящей из муромонаба-CD3, абциксимаба, ритуксимаба, даклизумаба, паливизумаба, инфликсимаба, трастузумаба, этанерцепта, базиликсимаба, гемтузумаба озогамицина, алемтузумаба, ибритутомаба тиуксетана, адалимумаба, алефацепта, омализумаба, эфализумаба, тозитумомаба-I131, цетуксимаба, бевацизумаба, натализумаба, ранибизумаба, панитумумаба, экулизумаба, рилонацепта, цертолизумаба пегола, ромиплостима, AMG-531, CNTO-148, CNTO-1275, ABT-874, LEA-29Y, белимумаба, TACI-Ig, анти-CD20 второго поколения, ACZ-885, тоцилизумаба, атлизумаба, меполизумаба, пертузумаба, HuMax CD20, тремелимумаба (CP-675 206), тицилимумаба, MDX-010, IDEC-114, инотузумаба озогамицина, HuMax EGFR, афлиберцепта, VEGF Trap-Eye, HuMax-CD4, Ala-Ala, ChAglyCD3, TRX4, катумаксомаба, IGN101, MT-201, преговомаба, CH-14,18, WX-G250, AMG-162, AAB-001, мотавизумаба, MEDI-524, эфунгумаба, Aurograb®, раксибацумаба, анти-CD20 третьего поколения, LY2469298 и велтузумаба.
21. Соединение по п. 19, где белок представляет собой моноклональное антитело.
22. Соединение по п. 13 или 14, где аминокислотный мотив представляет собой CYYX, XXCC, XCXC или CXX, где C представляет собой цистеин, Y представляет собой алифатическую аминокислоту, и X представляет собой аминокислоту, которая определяет субстрат-специфичность изопреноид-трансферазы.
23. Соединение по п. 1, где B представляет собой активное вещество.
24. Соединение по п. 23, где активное вещество представляет собой лекарственное средство, токсин, аффинный лиганд, детекторный зонд или их комбинацию.
25. Соединение по п. 23, где активное вещество представляет собой иммуномодулирующее соединение, противораковое средство, противовирусное средство, антибактериальное средство, противогрибковое средство, противопаразитарное средство или их комбинацию.
26. Соединение по п. 22, где белок, содержащий аминокислотный мотив, выбран из группы, состоящей из A-HC-(G)zCVIM, A-HC-(G)zCVLL, A-LC-(G)zCVIM и A-LC-(G)zCVLL, где A представляет собой антитело, HC представляет собой тяжелую цепь, LC представляет собой легкую цепь, G представляет собой глициновое звено, и z представляет собой целое число от 0 до 20.
27. Соединение по п. 26, где оно выбрано из соединений, имеющих следующие структуры:
где
Z представляет собой водород, (C1-C8)алкил, галоген, циано или нитро;
X представляет собой -O-, (C1-C8)алкилен или -NR21-;
R21 представляет собой водород, (C1-C6)алкил, (C1-C6)алкил(C6-C20)арил или (C1-C6)алкил(C3-C20)гетероарил;
n представляет собой целое число от 1 до 3, и, когда n представляет собой целое число 2 или более, каждый из заместителей Z являются одинаковыми или отличными друг от друга;
r представляет собой целое число от 1 до 10;
q представляет собой целое число от 1 до 10;
w представляет собой целое число от 1 до 10;
x представляет собой целое число от 0 до 10;
g представляет собой целое число от 1 до 10;
-S-mAb представляет собой A-HC-(G)zCVIM-, A-HC-(G)zCVLL-, A-LC-(G)zCVIM- или A-LC-(G)zCVLL-, где A представляет собой антитело, HC представляет собой тяжелую цепь, LC представляет собой легкую цепь, G представляет собой глициновое звено, и z представляет собой целое число от 0 до 20;
B представляет собой лекарственное средство, имеющее структуру, выбранную из следующих структур; и
y представляет собой целое число от 1 до 10.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR20140064360 | 2014-05-28 | ||
KR10-2014-0064360 | 2014-05-28 | ||
KR1020150073161A KR101628872B1 (ko) | 2014-05-28 | 2015-05-26 | 자가-희생 기를 포함하는 화합물 |
KR10-2015-0073161 | 2015-05-26 | ||
PCT/KR2015/005299 WO2015182984A1 (ko) | 2014-05-28 | 2015-05-27 | 자가-희생 기를 포함하는 화합물 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2020101906A Division RU2020101906A (ru) | 2014-05-28 | 2015-05-27 | Соединения, включающие саморасщепляющуюся группу |
Publications (3)
Publication Number | Publication Date |
---|---|
RU2016151190A true RU2016151190A (ru) | 2018-07-02 |
RU2016151190A3 RU2016151190A3 (ru) | 2019-01-25 |
RU2712744C2 RU2712744C2 (ru) | 2020-01-30 |
Family
ID=54872920
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2020101906A RU2020101906A (ru) | 2014-05-28 | 2015-05-27 | Соединения, включающие саморасщепляющуюся группу |
RU2016151190A RU2712744C2 (ru) | 2014-05-28 | 2015-05-27 | Соединения, включающие саморасщепляющуюся группу |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2020101906A RU2020101906A (ru) | 2014-05-28 | 2015-05-27 | Соединения, включающие саморасщепляющуюся группу |
Country Status (14)
Country | Link |
---|---|
US (4) | US9993568B2 (ru) |
EP (1) | EP3156424A4 (ru) |
JP (2) | JP6815201B2 (ru) |
KR (1) | KR101628872B1 (ru) |
CN (2) | CN105358579B (ru) |
AU (2) | AU2015268300B2 (ru) |
BR (1) | BR112016027722A8 (ru) |
CA (1) | CA2949943A1 (ru) |
HK (1) | HK1216180A1 (ru) |
IL (1) | IL249181B2 (ru) |
MX (1) | MX2016015511A (ru) |
NZ (1) | NZ727007A (ru) |
RU (2) | RU2020101906A (ru) |
WO (1) | WO2015182984A1 (ru) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20120308584A1 (en) * | 2011-05-08 | 2012-12-06 | Legochem Biosciences, Inc. | Protein-active agent conjugates and method for preparing the same |
KR101628872B1 (ko) | 2014-05-28 | 2016-06-09 | 주식회사 레고켐 바이오사이언스 | 자가-희생 기를 포함하는 화합물 |
WO2017051249A1 (en) | 2015-09-25 | 2017-03-30 | Legochem Biosciences, Inc. | Compositions and methods related to anti-cd19 antibody drug conjugates |
WO2017051254A1 (en) | 2015-09-25 | 2017-03-30 | Legochem Biosciences, Inc. | Compositions and methods related to anti-egfr antibody drug conjugates |
RS65660B1 (sr) * | 2015-11-25 | 2024-07-31 | Ligachem Biosciences Inc | Konјugati koji sadrže samozapaljive grupe i postupci povezani sa njima |
KR20180077300A (ko) * | 2015-11-25 | 2018-07-06 | 주식회사 레고켐 바이오사이언스 | 펩타이드 그룹을 포함하는 접합체 및 이와 관련된 제조방법 |
CA3006249A1 (en) | 2015-11-25 | 2017-06-01 | Legochem Biosciences, Inc. | Antibody-drug conjugates comprising branched linkers and methods related thereto |
KR102085798B1 (ko) | 2016-12-28 | 2020-03-06 | 주식회사 인투셀 | 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물 |
WO2018124758A2 (ko) * | 2016-12-28 | 2018-07-05 | 주식회사 인투셀 | 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물 |
WO2018174544A2 (ko) | 2017-03-21 | 2018-09-27 | 주식회사 펩트론 | Muc1에 특이적으로 결합하는 항체 및 그의 용도 |
RU2746413C1 (ru) | 2017-03-21 | 2021-04-13 | Пептрон, Инк. | Антитело, специфически связывающееся с muc1, и его применение |
KR101938800B1 (ko) | 2017-03-29 | 2019-04-10 | 주식회사 레고켐 바이오사이언스 | 피롤로벤조디아제핀 이량체 전구체 및 이의 리간드-링커 접합체 화합물 |
WO2018182341A1 (ko) * | 2017-03-29 | 2018-10-04 | 주식회사 레고켐 바이오사이언스 | 피롤로벤조디아제핀 이량체 전구체 및 이의 리간드-링커 접합체 화합물 |
BR112019028295A2 (pt) | 2017-07-04 | 2020-07-21 | Intocell, Inc. | compostos que compreendem ligante clivável e usos dos mesmos |
WO2019035649A1 (ko) * | 2017-08-14 | 2019-02-21 | 주식회사 레고켐 바이오사이언스 | EGFRvIII에 대한 항체를 포함하는 항체 약물 접합체 |
KR102275930B1 (ko) | 2018-03-14 | 2021-07-12 | (주)알테오젠 | Folr1에 특이적으로 결합하는 항체 및 그의 용도 |
WO2019212253A1 (ko) | 2018-05-02 | 2019-11-07 | 사회복지법인 삼성생명공익재단 | C-met에 특이적으로 결합하는 항체 및 그의 용도 |
US11827703B2 (en) * | 2018-05-09 | 2023-11-28 | Legochem Biosciences, Inc. | Compositions and methods related to anti-CD19 antibody drug conjugates |
AU2019277094A1 (en) | 2018-05-29 | 2021-01-21 | Bristol-Myers Squibb Company | Modified self-immolating moieties for use in prodrugs and conjugates and methods of using and making |
WO2020141460A2 (en) * | 2019-01-03 | 2020-07-09 | Intocell, Inc. | Compounds comprising cleavable linker and uses thereof |
US20220096641A1 (en) | 2019-01-03 | 2022-03-31 | Legochem Biosciences, Inc. | Pyrrolobenzodiazepine dimer compound with improved safety and use thereof |
EP3906064A4 (en) * | 2019-01-03 | 2023-03-08 | Intocell, Inc. | CLEAVABLE LINKER COMPOUNDS AND USES THEREOF |
BR112021017303A2 (pt) | 2019-03-06 | 2021-11-16 | Legochem Biosciences Inc | Conjugado de anticorpo ou um sal ou solvato farmaceuticamente aceitável deste, anticorpo que se liga com especificidade ao dlk1 ou um fragmento de ligação ao antígeno deste, composição farmacêutica para prevenção ou tratamento de doença proliferativa, câncer ou angiogênica, métodos para prevenção e para tratamento de doença proliferativa, câncer ou angiogênica, e, uso do conjugado |
US11434291B2 (en) | 2019-05-14 | 2022-09-06 | Provention Bio, Inc. | Methods and compositions for preventing type 1 diabetes |
KR20210028544A (ko) | 2019-09-04 | 2021-03-12 | 주식회사 레고켐 바이오사이언스 | 인간 ror1에 대한 항체를 포함하는 항체 약물 접합체 및 이의 용도 |
JP6704083B1 (ja) | 2019-11-22 | 2020-06-03 | 東邦チタニウム株式会社 | 銅粉体とその製造方法 |
CA3182445A1 (en) | 2020-06-11 | 2021-12-16 | Francisco Leon | Methods and compositions for preventing type 1 diabetes |
CN116782937A (zh) | 2020-12-10 | 2023-09-19 | 优特力克斯有限公司 | 抗pd-1抗体及其用途 |
CN114716548A (zh) | 2021-01-05 | 2022-07-08 | (株)爱恩德生物 | 抗-fgfr3抗体及其用途 |
JP2024512324A (ja) | 2021-03-05 | 2024-03-19 | ジーオー セラピューティクス,インコーポレイテッド | 抗グリコcd44抗体およびその使用 |
WO2022211508A1 (ko) | 2021-03-30 | 2022-10-06 | 주식회사 레고켐바이오사이언스 | 인간 cldn18.2에 대한 항체를 포함하는 항체 약물 접합체 및 이의 용도 |
AU2022324456A1 (en) | 2021-08-05 | 2024-02-15 | Go Therapeutics, Inc. | Anti-glyco-muc4 antibodies and their uses |
KR20230066257A (ko) | 2021-11-05 | 2023-05-15 | 서울대학교병원 | 리지스틴 특이적 항체 및 이의 용도 |
GB202203070D0 (en) | 2022-03-04 | 2022-04-20 | Iksuda Therapeutics Ltd | Anti-canag antibody conjugate |
Family Cites Families (40)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US1011896A (en) | 1911-05-10 | 1911-12-19 | Western Electric Co | Fuse. |
US5112739A (en) | 1988-08-02 | 1992-05-12 | Polaroid Corporation | Enzyme controlled release system |
DK0795334T3 (da) * | 1996-03-12 | 2006-06-06 | Sanofi Aventis Deutschland | Nye prodrugs til behandling af tumorer og betændelsessygdomme |
KR100192328B1 (ko) | 1996-04-03 | 1999-06-15 | 구본준 | 양방향 수평전하 전송소자 |
US6218519B1 (en) | 1996-04-12 | 2001-04-17 | Pro-Neuron, Inc. | Compounds and methods for the selective treatment of cancer and bacterial infections |
WO1998019705A1 (en) | 1996-11-05 | 1998-05-14 | Bristol-Myers Squibb Company | Branched peptide linkers |
US6759509B1 (en) | 1996-11-05 | 2004-07-06 | Bristol-Myers Squibb Company | Branched peptide linkers |
AU2003294796A1 (en) | 2002-12-05 | 2004-06-23 | Schering Ag | Epothilone analogs for site specific delivery in the treatment of proliferative diseases |
US7498298B2 (en) * | 2003-11-06 | 2009-03-03 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
PA8645301A1 (es) | 2004-09-10 | 2006-07-03 | Wyeth Corp | Anticuerpo anti-5t4 humanizados y conjugados anticuerpo anti-5t4/calicheamicina |
EP4026840A1 (en) * | 2005-07-18 | 2022-07-13 | Seagen Inc. | Beta-glucuronide-linker drug conjugates |
MX2009002857A (es) | 2006-09-15 | 2009-03-30 | Enzon Pharmaceuticals Inc | Enlazadores polimericos basados en lisina. |
CL2007003622A1 (es) | 2006-12-13 | 2009-08-07 | Medarex Inc | Anticuerpo monoclonal humano anti-cd19; composicion que lo comprende; y metodo de inhibicion del crecimiento de celulas tumorales. |
US9353140B2 (en) * | 2009-11-25 | 2016-05-31 | Academia Sinica | BQC-G, a tumor-selective anti-cancer prodrug |
FR2960153B1 (fr) | 2010-05-20 | 2012-08-17 | Centre Nat Rech Scient | Nouveaux bras autoreactifs et prodrogues les comprenant |
US9591882B2 (en) * | 2010-08-05 | 2017-03-14 | Robert LaGrand Duffin | Absorbent sleeve |
EP2702522A4 (en) | 2011-04-29 | 2015-03-25 | Hewlett Packard Development Co | SYSTEMS AND METHOD FOR IN-STORAGE PROCESSING OF EVENTS |
US20120308584A1 (en) | 2011-05-08 | 2012-12-06 | Legochem Biosciences, Inc. | Protein-active agent conjugates and method for preparing the same |
CN103987384A (zh) * | 2011-10-14 | 2014-08-13 | 西雅图基因公司 | 吡咯并苯并二氮杂卓和靶向结合物 |
JP6228551B2 (ja) | 2012-01-03 | 2017-11-08 | インビクタス オンコロジー プライベート リミテッド | リガンド−標的指向分子およびその方法 |
KR102305226B1 (ko) | 2013-03-15 | 2021-09-29 | 아비에 도이치란트 게엠베하 운트 콤파니 카게 | 항-egfr 항체 약물 접합체 제형 |
WO2014194030A2 (en) | 2013-05-31 | 2014-12-04 | Immunogen, Inc. | Conjugates comprising cell-binding agents and cytotoxic agents |
KR102645430B1 (ko) | 2013-10-15 | 2024-03-11 | 씨젠 인크. | 개선된 리간드-약물 컨쥬게이트 약물동력학을 위한 peg화된 약물-링커 |
MX2016007364A (es) | 2013-12-19 | 2016-09-08 | Seattle Genetics Inc | Enlazadores de carbamato de metileno para su uso en conjugados de farmacos dirigidos. |
EP2913064A1 (en) | 2014-02-26 | 2015-09-02 | celares GmbH | Branched drug-linker conjugates for the coupling to biological targeting molecules |
KR101628872B1 (ko) | 2014-05-28 | 2016-06-09 | 주식회사 레고켐 바이오사이언스 | 자가-희생 기를 포함하는 화합물 |
TWI805109B (zh) | 2014-08-28 | 2023-06-11 | 美商奇諾治療有限公司 | 對cd19具專一性之抗體及嵌合抗原受體 |
NZ730552A (en) | 2014-09-11 | 2024-03-22 | Seagen Inc | Targeted delivery of tertiary amine-containing drug substances |
CN111620862A (zh) | 2014-12-09 | 2020-09-04 | 艾伯维公司 | Bcl-xl抑制性化合物和包括其的抗体药物缀合物 |
KR20160080832A (ko) | 2014-12-29 | 2016-07-08 | 주식회사 레고켐 바이오사이언스 | 리피바디 유도체-약물 복합체, 그 제조방법 및 용도 |
EP3892305A1 (en) | 2015-01-30 | 2021-10-13 | Sutro Biopharma, Inc. | Hemiasterlin derivatives for conjugation and therapy |
WO2017051249A1 (en) * | 2015-09-25 | 2017-03-30 | Legochem Biosciences, Inc. | Compositions and methods related to anti-cd19 antibody drug conjugates |
WO2017051254A1 (en) * | 2015-09-25 | 2017-03-30 | Legochem Biosciences, Inc. | Compositions and methods related to anti-egfr antibody drug conjugates |
CN107531793B (zh) | 2015-10-13 | 2022-01-11 | 优瑞科生物技术公司 | 对人类cd19具有专一性的抗体药剂和其用途 |
KR20180077300A (ko) * | 2015-11-25 | 2018-07-06 | 주식회사 레고켐 바이오사이언스 | 펩타이드 그룹을 포함하는 접합체 및 이와 관련된 제조방법 |
RS65660B1 (sr) * | 2015-11-25 | 2024-07-31 | Ligachem Biosciences Inc | Konјugati koji sadrže samozapaljive grupe i postupci povezani sa njima |
CA3006249A1 (en) * | 2015-11-25 | 2017-06-01 | Legochem Biosciences, Inc. | Antibody-drug conjugates comprising branched linkers and methods related thereto |
AU2017353936A1 (en) | 2016-11-04 | 2019-05-02 | Novimmune Sa | Anti-CD19 antibodies and methods of use thereof |
US11827703B2 (en) | 2018-05-09 | 2023-11-28 | Legochem Biosciences, Inc. | Compositions and methods related to anti-CD19 antibody drug conjugates |
BR112021017303A2 (pt) * | 2019-03-06 | 2021-11-16 | Legochem Biosciences Inc | Conjugado de anticorpo ou um sal ou solvato farmaceuticamente aceitável deste, anticorpo que se liga com especificidade ao dlk1 ou um fragmento de ligação ao antígeno deste, composição farmacêutica para prevenção ou tratamento de doença proliferativa, câncer ou angiogênica, métodos para prevenção e para tratamento de doença proliferativa, câncer ou angiogênica, e, uso do conjugado |
-
2015
- 2015-05-26 KR KR1020150073161A patent/KR101628872B1/ko active IP Right Grant
- 2015-05-27 BR BR112016027722A patent/BR112016027722A8/pt active Search and Examination
- 2015-05-27 JP JP2016569844A patent/JP6815201B2/ja active Active
- 2015-05-27 RU RU2020101906A patent/RU2020101906A/ru unknown
- 2015-05-27 CN CN201580000364.2A patent/CN105358579B/zh active Active
- 2015-05-27 NZ NZ727007A patent/NZ727007A/en unknown
- 2015-05-27 EP EP15799360.1A patent/EP3156424A4/en active Pending
- 2015-05-27 CA CA2949943A patent/CA2949943A1/en active Pending
- 2015-05-27 AU AU2015268300A patent/AU2015268300B2/en active Active
- 2015-05-27 RU RU2016151190A patent/RU2712744C2/ru active
- 2015-05-27 IL IL249181A patent/IL249181B2/en unknown
- 2015-05-27 MX MX2016015511A patent/MX2016015511A/es unknown
- 2015-05-27 WO PCT/KR2015/005299 patent/WO2015182984A1/ko active Application Filing
- 2015-05-27 US US14/898,932 patent/US9993568B2/en active Active
- 2015-05-27 CN CN201710524324.9A patent/CN107648613B/zh active Active
- 2015-09-25 US US14/865,778 patent/US9919057B2/en active Active
-
2016
- 2016-04-13 HK HK16104200.0A patent/HK1216180A1/zh unknown
-
2018
- 2018-06-11 US US16/005,245 patent/US10383949B2/en active Active
-
2019
- 2019-08-20 US US16/545,869 patent/US10980890B2/en active Active
-
2020
- 2020-05-07 JP JP2020082104A patent/JP2020143098A/ja active Pending
-
2021
- 2021-06-21 AU AU2021204136A patent/AU2021204136B2/en active Active
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
RU2016151190A (ru) | Соединения, включающие саморасщепляющуюся группу | |
JP2017519741A5 (ru) | ||
JP2020143098A5 (ru) | ||
US20230212283A1 (en) | Matrix metalloprotease-cleavable and serine protease-cleavable substrates and methods of use thereof | |
JP6826055B2 (ja) | 抗pdl1抗体、活性化可能抗pdl1抗体、およびその使用方法 | |
CN107849133B (zh) | 抗cd166抗体、可活化抗cd166抗体及其使用方法 | |
AU2018241141B2 (en) | Pertuzumab variants and evaluation thereof | |
EP3655779A1 (en) | Methods of qualitatively and/or quantitatively analyzing properties of activatable antibodies and uses thereof | |
JP2022064924A (ja) | 抗pd-1抗体、活性化可能抗pd-1抗体、およびその使用方法 | |
JP5226926B2 (ja) | Her3活性の阻害剤 | |
EP3592775A1 (en) | Cd147 antibodies, activatable cd147 antibodies, and methods of making and use thereof | |
EP3890764A2 (en) | Matrix metalloprotease-cleavable and serine or cysteine protease-cleavable substrates and methods of use thereof | |
WO2016179335A1 (en) | Anti-itga3 antibodies, activatable anti-itga3 antibodies, and methods of use thereof | |
IL255416B2 (en) | Anti-CD71 antibodies, activatable anti-CD71 antibodies, preparations containing them and their uses | |
KR20200058406A (ko) | 활성화 가능한 항-cd166 항체 및 이의 사용 방법 | |
CA2913732A1 (en) | Compositions and methods for conjugating activatable antibodies | |
EP3762420A1 (en) | Activatable cd147 antibodies and methods of making and use thereof | |
AU2015266664B2 (en) | Anti-epidermal growth factor receptor (EGFR) antibodies | |
JP7039577B2 (ja) | 抗edb抗体および抗体-薬物コンジュゲート | |
JP2023073965A (ja) | 癌関連免疫抑制阻害剤 | |
IL265762B2 (en) | Dosing regimen of avolumab for cancer treatment | |
Adair et al. | Therapeutic antibodies | |
WO2019131769A1 (ja) | 新規抗pad4抗体 | |
US20110305630A1 (en) | Misfolded proteins in cancer treatment and diagnosis | |
JP7447255B2 (ja) | ヒト化抗ca ix抗体、およびその使用方法 |