JP2019524759A5 - - Google Patents
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- JP2019524759A5 JP2019524759A5 JP2019503986A JP2019503986A JP2019524759A5 JP 2019524759 A5 JP2019524759 A5 JP 2019524759A5 JP 2019503986 A JP2019503986 A JP 2019503986A JP 2019503986 A JP2019503986 A JP 2019503986A JP 2019524759 A5 JP2019524759 A5 JP 2019524759A5
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- JP
- Japan
- Prior art keywords
- alkyl
- subscript
- drug
- ligand
- needed
- Prior art date
- 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.)
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- 229940079593 drug Drugs 0.000 claims description 699
- 239000003814 drug Substances 0.000 claims description 699
- 150000001875 compounds Chemical class 0.000 claims description 468
- 229910052739 hydrogen Inorganic materials 0.000 claims description 355
- 239000000562 conjugate Substances 0.000 claims description 296
- 125000000217 alkyl group Chemical group 0.000 claims description 285
- -1 substituted Chemical class 0.000 claims description 271
- 150000003839 salts Chemical class 0.000 claims description 237
- 239000001257 hydrogen Substances 0.000 claims description 225
- 229910052799 carbon Inorganic materials 0.000 claims description 197
- 229910052757 nitrogen Inorganic materials 0.000 claims description 151
- 125000003118 aryl group Chemical group 0.000 claims description 145
- 239000003446 ligand Substances 0.000 claims description 142
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 108
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 105
- 101000629400 Homo sapiens Mesoderm-specific transcript homolog protein Proteins 0.000 claims description 96
- 102100026821 Mesoderm-specific transcript homolog protein Human genes 0.000 claims description 96
- 150000002431 hydrogen Chemical class 0.000 claims description 75
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 73
- 125000000623 heterocyclic group Chemical group 0.000 claims description 66
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 59
- 125000002947 alkylene group Chemical group 0.000 claims description 57
- 125000005842 heteroatom Chemical group 0.000 claims description 56
- 108010044540 auristatin Proteins 0.000 claims description 55
- 125000001072 heteroaryl group Chemical group 0.000 claims description 50
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 48
- 150000001412 amines Chemical class 0.000 claims description 47
- 235000008206 alpha-amino acids Nutrition 0.000 claims description 46
- 150000008134 glucuronides Chemical group 0.000 claims description 46
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims description 45
- 150000001576 beta-amino acids Chemical class 0.000 claims description 45
- 229910052717 sulfur Inorganic materials 0.000 claims description 44
- 229910052760 oxygen Inorganic materials 0.000 claims description 43
- 239000002253 acid Substances 0.000 claims description 42
- 125000004432 carbon atom Chemical group C* 0.000 claims description 42
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 42
- 150000001721 carbon Chemical group 0.000 claims description 41
- 238000007363 ring formation reaction Methods 0.000 claims description 41
- 102000005744 Glycoside Hydrolases Human genes 0.000 claims description 32
- 108010031186 Glycoside Hydrolases Proteins 0.000 claims description 32
- 125000006239 protecting group Chemical group 0.000 claims description 32
- 150000003335 secondary amines Chemical class 0.000 claims description 32
- 125000006850 spacer group Chemical group 0.000 claims description 32
- 108010016626 Dipeptides Proteins 0.000 claims description 29
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 27
- 238000003776 cleavage reaction Methods 0.000 claims description 27
- 230000007017 scission Effects 0.000 claims description 27
- 150000003512 tertiary amines Chemical group 0.000 claims description 24
- 108091005804 Peptidases Proteins 0.000 claims description 23
- 239000004365 Protease Substances 0.000 claims description 23
- 125000000524 functional group Chemical group 0.000 claims description 23
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 23
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 23
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims description 21
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 21
- 125000003342 alkenyl group Chemical group 0.000 claims description 20
- 125000004429 atom Chemical group 0.000 claims description 20
- 125000001424 substituent group Chemical group 0.000 claims description 20
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 19
- 210000004027 cell Anatomy 0.000 claims description 17
- 230000004913 activation Effects 0.000 claims description 16
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 16
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 16
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 14
- 238000006467 substitution reaction Methods 0.000 claims description 14
- 125000000304 alkynyl group Chemical group 0.000 claims description 13
- 239000002131 composite material Substances 0.000 claims description 13
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 12
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 12
- 150000001413 amino acids Chemical class 0.000 claims description 11
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 11
- 125000004434 sulfur atom Chemical group 0.000 claims description 11
- 230000002159 abnormal effect Effects 0.000 claims description 10
- 239000000611 antibody drug conjugate Substances 0.000 claims description 10
- 229940049595 antibody-drug conjugate Drugs 0.000 claims description 10
- 125000000837 carbohydrate group Chemical group 0.000 claims description 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 125000004122 cyclic group Chemical group 0.000 claims description 9
- 229910052736 halogen Inorganic materials 0.000 claims description 9
- 150000002367 halogens Chemical class 0.000 claims description 9
- MFRNYXJJRJQHNW-DEMKXPNLSA-N (2s)-2-[[(2r,3r)-3-methoxy-3-[(2s)-1-[(3r,4s,5s)-3-methoxy-5-methyl-4-[methyl-[(2s)-3-methyl-2-[[(2s)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid Chemical compound CN[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 MFRNYXJJRJQHNW-DEMKXPNLSA-N 0.000 claims description 8
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
- IEDXPSOJFSVCKU-HOKPPMCLSA-N [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrolidin-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate Chemical compound CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)CCC2=O)C(C)C)cc1)C(C)C IEDXPSOJFSVCKU-HOKPPMCLSA-N 0.000 claims description 8
- 125000005647 linker group Chemical group 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 108010093470 monomethyl auristatin E Proteins 0.000 claims description 8
- 108010059074 monomethylauristatin F Proteins 0.000 claims description 8
- 239000000427 antigen Substances 0.000 claims description 7
- 102000036639 antigens Human genes 0.000 claims description 7
- 108091007433 antigens Proteins 0.000 claims description 7
- 229930182480 glucuronide Natural products 0.000 claims description 7
- 239000007787 solid Substances 0.000 claims description 7
- 125000006539 C12 alkyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 6
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 230000002209 hydrophobic effect Effects 0.000 claims description 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 230000008685 targeting Effects 0.000 claims description 6
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 6
- 229920002554 vinyl polymer Polymers 0.000 claims description 6
- 235000001014 amino acid Nutrition 0.000 claims description 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 5
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 5
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 5
- 125000003107 substituted aryl group Chemical group 0.000 claims description 5
- 150000003573 thiols Chemical group 0.000 claims description 5
- WOWDZACBATWTAU-FEFUEGSOSA-N (2s)-2-[[(2s)-2-(dimethylamino)-3-methylbutanoyl]amino]-n-[(3r,4s,5s)-1-[(2s)-2-[(1r,2r)-3-[[(1s,2r)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-n,3-dimethylbutanamide Chemical compound CC(C)[C@H](N(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)C1=CC=CC=C1 WOWDZACBATWTAU-FEFUEGSOSA-N 0.000 claims description 4
- 101710160107 Outer membrane protein A Proteins 0.000 claims description 4
- 108010008739 auristatin PHE Proteins 0.000 claims description 4
- 108010009065 auristatin PYE Proteins 0.000 claims description 4
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims description 4
- 210000004899 c-terminal region Anatomy 0.000 claims description 4
- 150000001732 carboxylic acid derivatives Chemical group 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 210000002919 epithelial cell Anatomy 0.000 claims description 4
- 125000005549 heteroarylene group Chemical group 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 230000003834 intracellular effect Effects 0.000 claims description 4
- 108010047846 soblidotin Proteins 0.000 claims description 4
- DZMVCVHATYROOS-ZBFGKEHZSA-N soblidotin Chemical compound CC(C)[C@H](N(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)NCCC1=CC=CC=C1 DZMVCVHATYROOS-ZBFGKEHZSA-N 0.000 claims description 4
- 230000005945 translocation Effects 0.000 claims description 4
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims description 3
- 239000012634 fragment Substances 0.000 claims description 3
- 210000003712 lysosome Anatomy 0.000 claims description 3
- 230000001868 lysosomic effect Effects 0.000 claims description 3
- 230000001105 regulatory effect Effects 0.000 claims description 3
- JDVPQXZIJDEHAN-UHFFFAOYSA-N succinamic acid Chemical compound NC(=O)CCC(O)=O JDVPQXZIJDEHAN-UHFFFAOYSA-N 0.000 claims description 3
- 238000006845 Michael addition reaction Methods 0.000 claims description 2
- 102000035195 Peptidases Human genes 0.000 claims description 2
- 125000006244 carboxylic acid protecting group Chemical group 0.000 claims description 2
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 230000002792 vascular Effects 0.000 claims description 2
- 125000003003 spiro group Chemical group 0.000 claims 8
- 125000006575 electron-withdrawing group Chemical group 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000000732 arylene group Chemical group 0.000 claims 4
- 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 2
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 2
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 2
- 150000001720 carbohydrates Chemical class 0.000 claims 2
- 150000007513 acids Chemical class 0.000 claims 1
- 150000001371 alpha-amino acids Chemical class 0.000 claims 1
- 238000010504 bond cleavage reaction Methods 0.000 claims 1
- SNCZNSNPXMPCGN-UHFFFAOYSA-N butanediamide Chemical compound NC(=O)CCC(N)=O SNCZNSNPXMPCGN-UHFFFAOYSA-N 0.000 claims 1
- 230000002255 enzymatic effect Effects 0.000 claims 1
- 108010056119 protease So Proteins 0.000 claims 1
- 150000001768 cations Chemical class 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 125000005843 halogen group Chemical group 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 6
- OMRPLUKQNWNZAV-CONSDPRKSA-N (6as)-3-[3-[[(6as)-2-methoxy-8-(4-methoxyphenyl)-11-oxo-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-8-(4-aminophenyl)-2-methoxy-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-11-one Chemical compound C1=CC(OC)=CC=C1C1=CN2C(=O)C3=CC(OC)=C(OCCCOC=4C(=CC=5C(=O)N6C=C(C[C@H]6C=NC=5C=4)C=4C=CC(N)=CC=4)OC)C=C3N=C[C@@H]2C1 OMRPLUKQNWNZAV-CONSDPRKSA-N 0.000 description 5
- 125000002015 acyclic group Chemical group 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 3
- 201000011510 cancer Diseases 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 0 CCCC(CCC*)C(*)(C(*Nc(cc(C*)cc1*)c1O*)=O)NCCCC(O)=O Chemical compound CCCC(CCC*)C(*)(C(*Nc(cc(C*)cc1*)c1O*)=O)NCCCC(O)=O 0.000 description 2
- 125000003277 amino group Chemical group 0.000 description 2
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 description 2
- 125000004093 cyano group Chemical group *C#N 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 230000003463 hyperproliferative effect Effects 0.000 description 2
- 238000010253 intravenous injection Methods 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 150000001345 alkine derivatives Chemical class 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 230000005494 condensation Effects 0.000 description 1
- 238000009833 condensation Methods 0.000 description 1
- 229930182470 glycoside Natural products 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000002132 lysosomal effect Effects 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023060933A JP7573679B2 (ja) | 2016-08-09 | 2023-04-04 | 改善された生理化学的特性を有する自己安定性リンカーを用いる薬物コンジュゲート |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662372455P | 2016-08-09 | 2016-08-09 | |
| US62/372,455 | 2016-08-09 | ||
| PCT/US2017/046157 WO2018031690A1 (en) | 2016-08-09 | 2017-08-09 | Drug conjugates with self-stabilizing linkers having improved physiochemical properties |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023060933A Division JP7573679B2 (ja) | 2016-08-09 | 2023-04-04 | 改善された生理化学的特性を有する自己安定性リンカーを用いる薬物コンジュゲート |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019524759A JP2019524759A (ja) | 2019-09-05 |
| JP2019524759A5 true JP2019524759A5 (enExample) | 2020-09-24 |
| JP7257951B2 JP7257951B2 (ja) | 2023-04-14 |
Family
ID=61162990
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019503986A Active JP7257951B2 (ja) | 2016-08-09 | 2017-08-09 | 改善された生理化学的特性を有する自己安定性リンカーを用いる薬物コンジュゲート |
| JP2023060933A Active JP7573679B2 (ja) | 2016-08-09 | 2023-04-04 | 改善された生理化学的特性を有する自己安定性リンカーを用いる薬物コンジュゲート |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023060933A Active JP7573679B2 (ja) | 2016-08-09 | 2023-04-04 | 改善された生理化学的特性を有する自己安定性リンカーを用いる薬物コンジュゲート |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US11944689B2 (enExample) |
| EP (1) | EP3496747A4 (enExample) |
| JP (2) | JP7257951B2 (enExample) |
| KR (2) | KR20190038579A (enExample) |
| CN (1) | CN109562152B (enExample) |
| AU (2) | AU2017310436B2 (enExample) |
| BR (1) | BR112019001945A2 (enExample) |
| EA (1) | EA201990470A1 (enExample) |
| IL (1) | IL264453A (enExample) |
| MA (1) | MA45945A (enExample) |
| MX (2) | MX2019001302A (enExample) |
| SG (1) | SG11201900699QA (enExample) |
| TW (2) | TWI851531B (enExample) |
| WO (1) | WO2018031690A1 (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20240156969A1 (en) * | 2015-12-04 | 2024-05-16 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| CN109843919A (zh) | 2016-03-25 | 2019-06-04 | 西雅图基因公司 | 用于制备聚乙二醇化的药物-接头及其中间体的方法 |
| TWI851531B (zh) | 2016-08-09 | 2024-08-11 | 美商思進公司 | 具有改善之生理化學性質之具自我穩定連接子之藥物結合物 |
| KR102648564B1 (ko) | 2017-03-24 | 2024-03-19 | 씨젠 인크. | 글루쿠로니드 약물-링커의 제조 공정 및 그 중간물 |
| TWI851577B (zh) | 2018-06-07 | 2024-08-11 | 美商思進公司 | 喜樹鹼結合物 |
| GB201820864D0 (en) * | 2018-12-20 | 2019-02-06 | J A Kemp | Antibody-drug conjugates |
| JP7590328B2 (ja) | 2018-12-21 | 2024-11-26 | レゲネロン ファーマシューティカルス，インコーポレーテッド | ツブリシン及びタンパク質－ツブリシンコンジュゲート |
| KR102501394B1 (ko) * | 2019-05-02 | 2023-02-21 | 주식회사 레고켐 바이오사이언스 | 트리스 구조를 가지는 링커를 포함하는 리간드-약물 접합체 |
| JP2022530482A (ja) * | 2019-05-02 | 2022-06-29 | レゴケム バイオサイエンシズ， インク． | トリス構造を有するリンカーを含むリガンド―薬物複合体 |
| US20220304993A1 (en) * | 2019-06-21 | 2022-09-29 | Ascendis Pharma A/S | Conjugates of an electron-donating nitrogen or tertiary amine comprising compounds |
| CN115867283A (zh) * | 2020-12-23 | 2023-03-28 | 启德医药科技（苏州）有限公司 | 包含开环硫代琥珀酰亚胺基团、寡肽片段和手性部分的新型异构化合物 |
| US20240209080A1 (en) | 2021-04-10 | 2024-06-27 | Profoundbio Us Co. | Folr1 binding agents, conjugates thereof and methods of using the same |
| CA3216459A1 (en) | 2021-04-23 | 2022-10-27 | Profoundbio Us Co. | Anti-cd70 antibodies, conjugates thereof and methods of using the same |
| TW202320857A (zh) | 2021-07-06 | 2023-06-01 | 美商普方生物製藥美國公司 | 連接子、藥物連接子及其結合物及其使用方法 |
| CN118119409A (zh) | 2021-09-03 | 2024-05-31 | 东丽株式会社 | 癌的治疗和/或预防用药物组合物 |
| WO2023092099A1 (en) | 2021-11-19 | 2023-05-25 | Ardeagen Corporation | Gpc3 binding agents, conjugates thereof and methods of using the same |
| EP4548932A1 (en) | 2022-06-30 | 2025-05-07 | Toray Industries, Inc. | Pharmaceutical composition for treating and/or preventing cancer |
| WO2024193692A1 (zh) | 2023-03-22 | 2024-09-26 | 映恩生物制药（苏州）有限公司 | 连接子及其在配体药物偶联物中的应用 |
| KR20250169306A (ko) | 2023-04-18 | 2025-12-02 | 아스트라제네카 아베 | 절단가능한 링커를 포함하는 접합체 |
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-
2017
- 2017-08-09 TW TW106126961A patent/TWI851531B/zh active
- 2017-08-09 US US16/324,198 patent/US11944689B2/en active Active
- 2017-08-09 CN CN201780047894.1A patent/CN109562152B/zh active Active
- 2017-08-09 MA MA045945A patent/MA45945A/fr unknown
- 2017-08-09 BR BR112019001945-6A patent/BR112019001945A2/pt unknown
- 2017-08-09 KR KR1020197005530A patent/KR20190038579A/ko not_active Ceased
- 2017-08-09 WO PCT/US2017/046157 patent/WO2018031690A1/en not_active Ceased
- 2017-08-09 EA EA201990470A patent/EA201990470A1/ru unknown
- 2017-08-09 JP JP2019503986A patent/JP7257951B2/ja active Active
- 2017-08-09 AU AU2017310436A patent/AU2017310436B2/en not_active Ceased
- 2017-08-09 MX MX2019001302A patent/MX2019001302A/es unknown
- 2017-08-09 EP EP17840229.3A patent/EP3496747A4/en active Pending
- 2017-08-09 KR KR1020247000631A patent/KR20240010534A/ko not_active Withdrawn
- 2017-08-09 TW TW113107936A patent/TW202500191A/zh unknown
- 2017-08-09 SG SG11201900699QA patent/SG11201900699QA/en unknown
-
2019
- 2019-01-24 IL IL264453A patent/IL264453A/en unknown
-
2022
- 2022-11-24 AU AU2022275478A patent/AU2022275478B2/en not_active Expired - Fee Related
-
2023
- 2023-04-04 JP JP2023060933A patent/JP7573679B2/ja active Active
- 2023-12-13 MX MX2023013592A patent/MX2023013592A/es unknown
-
2024
- 2024-01-11 US US18/410,296 patent/US20240226320A1/en not_active Abandoned
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