JP2018516851A5 - - Google Patents
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- JP2018516851A5 JP2018516851A5 JP2017550548A JP2017550548A JP2018516851A5 JP 2018516851 A5 JP2018516851 A5 JP 2018516851A5 JP 2017550548 A JP2017550548 A JP 2017550548A JP 2017550548 A JP2017550548 A JP 2017550548A JP 2018516851 A5 JP2018516851 A5 JP 2018516851A5
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- 150000001875 compounds Chemical class 0.000 claims description 247
- 238000000034 method Methods 0.000 claims description 82
- 125000003545 alkoxy group Chemical group 0.000 claims description 52
- 125000000217 alkyl group Chemical group 0.000 claims description 50
- 125000005843 halogen group Chemical group 0.000 claims description 48
- 238000009739 binding Methods 0.000 claims description 43
- 230000027455 binding Effects 0.000 claims description 42
- 125000001188 haloalkyl group Chemical group 0.000 claims description 40
- 125000000732 arylene group Chemical group 0.000 claims description 22
- 125000005549 heteroarylene group Chemical group 0.000 claims description 22
- 229960001230 asparagine Drugs 0.000 claims description 21
- 125000005647 linker group Chemical group 0.000 claims description 20
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 19
- 150000001413 amino acids Chemical group 0.000 claims description 18
- 125000003342 alkenyl group Chemical group 0.000 claims description 17
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 17
- 125000000304 alkynyl group Chemical group 0.000 claims description 17
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 17
- 125000003118 aryl group Chemical group 0.000 claims description 17
- 150000001540 azides Chemical class 0.000 claims description 17
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 17
- 125000001072 heteroaryl group Chemical group 0.000 claims description 17
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 17
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 17
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 15
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 13
- 125000000404 glutamine group Chemical group N[C@@H](CCC(N)=O)C(=O)* 0.000 claims description 12
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 12
- 125000006850 spacer group Chemical group 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 239000000562 conjugate Substances 0.000 claims description 10
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical group [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 239000003638 chemical reducing agent Substances 0.000 claims description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 8
- 150000001408 amides Chemical class 0.000 claims description 6
- 230000015572 biosynthetic process Effects 0.000 claims description 6
- 229960002173 citrulline Drugs 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 238000003786 synthesis reaction Methods 0.000 claims description 6
- 239000004474 valine Substances 0.000 claims description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 6
- 239000000611 antibody drug conjugate Substances 0.000 claims description 5
- 229940049595 antibody-drug conjugate Drugs 0.000 claims description 5
- 235000018417 cysteine Nutrition 0.000 claims description 5
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 229920001481 poly(stearyl methacrylate) Polymers 0.000 claims description 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 4
- 108060008539 Transglutaminase Proteins 0.000 claims description 4
- 239000002253 acid Substances 0.000 claims description 4
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 4
- 102000003601 transglutaminase Human genes 0.000 claims description 4
- 239000011701 zinc Substances 0.000 claims description 4
- 229910052725 zinc Inorganic materials 0.000 claims description 4
- NDDSIUHFLJACFT-VWURTLBMSA-N (2s)-2-amino-3-phenylpropanoic acid;(2s)-2,4-diamino-4-oxobutanoic acid Chemical compound OC(=O)[C@@H](N)CC(N)=O.OC(=O)[C@@H](N)CC1=CC=CC=C1 NDDSIUHFLJACFT-VWURTLBMSA-N 0.000 claims description 3
- ALBODLTZUXKBGZ-JUUVMNCLSA-N (2s)-2-amino-3-phenylpropanoic acid;(2s)-2,6-diaminohexanoic acid Chemical compound NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CC1=CC=CC=C1 ALBODLTZUXKBGZ-JUUVMNCLSA-N 0.000 claims description 3
- UGCWVVMCHYLGBO-DQZFIDPSSA-N (2s,3s)-2-amino-3-methylpentanoic acid;(2s)-2,4-diamino-4-oxobutanoic acid Chemical compound CC[C@H](C)[C@H](N)C(O)=O.OC(=O)[C@@H](N)CC(N)=O UGCWVVMCHYLGBO-DQZFIDPSSA-N 0.000 claims description 3
- FZUBHJJEYNHYFU-DKWTVANSSA-N 2-aminoacetic acid;(2s)-2,4-diamino-4-oxobutanoic acid Chemical compound NCC(O)=O.OC(=O)[C@@H](N)CC(N)=O FZUBHJJEYNHYFU-DKWTVANSSA-N 0.000 claims description 3
- 239000004471 Glycine Substances 0.000 claims description 3
- 239000004473 Threonine Substances 0.000 claims description 3
- 230000021615 conjugation Effects 0.000 claims description 3
- 229960000310 isoleucine Drugs 0.000 claims description 3
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 claims description 2
- DVLFYONBTKHTER-UHFFFAOYSA-N 3-(N-morpholino)propanesulfonic acid Chemical compound OS(=O)(=O)CCCN1CCOCC1 DVLFYONBTKHTER-UHFFFAOYSA-N 0.000 claims description 2
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims description 2
- 239000007995 HEPES buffer Substances 0.000 claims description 2
- 239000007993 MOPS buffer Substances 0.000 claims description 2
- 108010090665 Mannosyl-Glycoprotein Endo-beta-N-Acetylglucosaminidase Proteins 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- 102000000447 Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase Human genes 0.000 claims description 2
- 108010055817 Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase Proteins 0.000 claims description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 239000007975 buffered saline Substances 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 235000019253 formic acid Nutrition 0.000 claims description 2
- -1 linker compound Chemical class 0.000 claims description 2
- 150000002894 organic compounds Chemical class 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 239000010452 phosphate Substances 0.000 claims description 2
- 239000011780 sodium chloride Substances 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims description 2
- 239000000427 antigen Substances 0.000 claims 30
- 108091007433 antigens Proteins 0.000 claims 30
- 102000036639 antigens Human genes 0.000 claims 30
- 239000012634 fragment Substances 0.000 claims 30
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 4
- 206010017758 gastric cancer Diseases 0.000 claims 4
- 201000011549 stomach cancer Diseases 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 230000003321 amplification Effects 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 208000029824 high grade glioma Diseases 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 2
- 201000010893 malignant breast melanoma Diseases 0.000 claims 2
- 201000011614 malignant glioma Diseases 0.000 claims 2
- 208000006178 malignant mesothelioma Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 238000003199 nucleic acid amplification method Methods 0.000 claims 2
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- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 206010042863 synovial sarcoma Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 108090000695 Cytokines Proteins 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 claims 1
- 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 claims 1
- 101000623901 Homo sapiens Mucin-16 Proteins 0.000 claims 1
- 101001123448 Homo sapiens Prolactin receptor Proteins 0.000 claims 1
- 101000638154 Homo sapiens Transmembrane protease serine 2 Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 108010002352 Interleukin-1 Proteins 0.000 claims 1
- 108090000177 Interleukin-11 Proteins 0.000 claims 1
- 108010065805 Interleukin-12 Proteins 0.000 claims 1
- 108090000176 Interleukin-13 Proteins 0.000 claims 1
- 108050003558 Interleukin-17 Proteins 0.000 claims 1
- 108010002350 Interleukin-2 Proteins 0.000 claims 1
- 108010002386 Interleukin-3 Proteins 0.000 claims 1
- 108090000978 Interleukin-4 Proteins 0.000 claims 1
- 108010002616 Interleukin-5 Proteins 0.000 claims 1
- 108090001005 Interleukin-6 Proteins 0.000 claims 1
- 108090001007 Interleukin-8 Proteins 0.000 claims 1
- 108010002335 Interleukin-9 Proteins 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
- 102100023123 Mucin-16 Human genes 0.000 claims 1
- 102100029000 Prolactin receptor Human genes 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 102100031989 Transmembrane protease serine 2 Human genes 0.000 claims 1
- 108010087914 epidermal growth factor receptor VIII Proteins 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 239000000203 mixture Substances 0.000 description 25
- 239000011230 binding agent Substances 0.000 description 20
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 12
- 229940024606 amino acid Drugs 0.000 description 4
- 235000001014 amino acid Nutrition 0.000 description 4
- 0 CC(C)[C@@](C(N[C@@](CCCNC(N)=O)C(C)=O)=O)NC(*(C)(C)N(C(CC1C)=O)C1=O)=O Chemical compound CC(C)[C@@](C(N[C@@](CCCNC(N)=O)C(C)=O)=O)NC(*(C)(C)N(C(CC1C)=O)C1=O)=O 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- OVSKIKFHRZPJSS-UHFFFAOYSA-N 2,4-D Chemical compound OC(=O)COC1=CC=C(Cl)C=C1Cl OVSKIKFHRZPJSS-UHFFFAOYSA-N 0.000 description 1
- ROEXBULBZKICBC-KRQJBFIFSA-N C[C@@H](C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]([C@@](C[C@H](C)[C@@H](C)[C@@H]1C)(NC(O)=O)O)OC)cc2OC)c2Cl)=O)[C@]1(C)O)=O)N(C)C(c(cc1)cc(S(C)(=O)=O)c1NNC)=O Chemical compound C[C@@H](C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]([C@@](C[C@H](C)[C@@H](C)[C@@H]1C)(NC(O)=O)O)OC)cc2OC)c2Cl)=O)[C@]1(C)O)=O)N(C)C(c(cc1)cc(S(C)(=O)=O)c1NNC)=O ROEXBULBZKICBC-KRQJBFIFSA-N 0.000 description 1
- LHKUAZUPONJFED-BJWVSRTKSA-N C[C@@H](C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]1OC)cc2OC)c2Cl)=O)[C@@H](C)[C@@H](C)[C@H](C)[C@@H](C)C[C@]1(NC(O)=O)O)=O)NC Chemical compound C[C@@H](C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]1OC)cc2OC)c2Cl)=O)[C@@H](C)[C@@H](C)[C@H](C)[C@@H](C)C[C@]1(NC(O)=O)O)=O)NC LHKUAZUPONJFED-BJWVSRTKSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021044152A JP2021113191A (ja) | 2015-03-27 | 2021-03-17 | メイタンシノイド誘導体、そのコンジュゲート、及び使用方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562139044P | 2015-03-27 | 2015-03-27 | |
| US62/139,044 | 2015-03-27 | ||
| US201562252239P | 2015-11-06 | 2015-11-06 | |
| US62/252,239 | 2015-11-06 | ||
| PCT/US2016/024343 WO2016160615A1 (en) | 2015-03-27 | 2016-03-25 | Maytansinoid derivatives, conjugates thereof, and methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021044152A Division JP2021113191A (ja) | 2015-03-27 | 2021-03-17 | メイタンシノイド誘導体、そのコンジュゲート、及び使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018516851A JP2018516851A (ja) | 2018-06-28 |
| JP2018516851A5 true JP2018516851A5 (enExample) | 2019-05-23 |
| JP6948950B2 JP6948950B2 (ja) | 2021-10-13 |
Family
ID=55650789
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017550548A Active JP6948950B2 (ja) | 2015-03-27 | 2016-03-25 | メイタンシノイド誘導体、そのコンジュゲート、及び使用方法 |
| JP2021044152A Withdrawn JP2021113191A (ja) | 2015-03-27 | 2021-03-17 | メイタンシノイド誘導体、そのコンジュゲート、及び使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021044152A Withdrawn JP2021113191A (ja) | 2015-03-27 | 2021-03-17 | メイタンシノイド誘導体、そのコンジュゲート、及び使用方法 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US20160375147A1 (enExample) |
| EP (1) | EP3273998B1 (enExample) |
| JP (2) | JP6948950B2 (enExample) |
| KR (2) | KR20240142591A (enExample) |
| CN (2) | CN107995912A (enExample) |
| AU (1) | AU2016243527B2 (enExample) |
| BR (1) | BR112017020149A8 (enExample) |
| CA (1) | CA2978340C (enExample) |
| CL (1) | CL2017002422A1 (enExample) |
| CO (1) | CO2017010890A2 (enExample) |
| EA (1) | EA034950B1 (enExample) |
| IL (1) | IL254267B (enExample) |
| MX (2) | MX386328B (enExample) |
| PH (1) | PH12017501780A1 (enExample) |
| SG (1) | SG11201707148PA (enExample) |
| WO (1) | WO2016160615A1 (enExample) |
| ZA (1) | ZA201706040B (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015022585B1 (pt) | 2013-03-15 | 2023-04-04 | Regeneron Pharmaceuticals, Inc | Composto, composição farmacêutica, conjugado droga-anticorpo, e, uso dos mesmos |
| JP6608823B2 (ja) | 2013-08-26 | 2019-11-20 | 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 | マクロライドジアステレオマーを含む医薬組成物、その合成方法、及び治療上の使用 |
| KR20240142591A (ko) | 2015-03-27 | 2024-09-30 | 리제너론 파아마슈티컬스, 인크. | 메이탄시노이드 유도체, 이의 컨주게이트, 및 사용 방법 |
| EP3310800B1 (en) | 2015-06-19 | 2021-11-17 | Centurion BioPharma Corporation | Delivery systems for controlled drug release |
| JP6993958B2 (ja) | 2015-07-06 | 2022-02-04 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | 多重特異性抗原結合分子およびその使用 |
| AU2017211120C1 (en) | 2016-01-25 | 2021-10-07 | Regeneron Pharmaceuticals, Inc. | Maytansinoid derivatives, conjugates thereof, and methods of use |
| EP3448891A1 (en) | 2016-04-28 | 2019-03-06 | Regeneron Pharmaceuticals, Inc. | Methods of making multispecific antigen-binding molecules |
| MY199468A (en) | 2016-09-23 | 2023-10-31 | Regeneron Pharma | Anti-steap2 antibodies, antibody-drug conjugates, and bispecific antigen-binding molecules that bind steap2 and cd3, and uses thereof |
| PT3515946T (pt) | 2016-09-23 | 2022-08-04 | Regeneron Pharma | Anticorpos anti-muc16 (mucin 16) |
| TWI782930B (zh) | 2016-11-16 | 2022-11-11 | 美商再生元醫藥公司 | 抗met抗體,結合met之雙特異性抗原結合分子及其使用方法 |
| MX2019006131A (es) | 2016-11-29 | 2019-08-21 | Regeneron Pharma | Metodos para tratar cancer de mama positivo para prlr. |
| CN110944718A (zh) | 2017-05-18 | 2020-03-31 | 里珍纳龙药品有限公司 | 环糊精蛋白质药物偶联物 |
| MA50546A (fr) | 2017-06-07 | 2020-09-16 | Regeneron Pharma | Compositions et méthodes pour l'internalisation d'enzymes |
| CA3080857A1 (en) | 2017-11-07 | 2019-05-16 | Regeneron Pharmaceuticals, Inc. | Hydrophilic linkers for antibody drug conjugates |
| US11572373B2 (en) * | 2017-11-30 | 2023-02-07 | Ladrx Corporation | Maytansinoid-based drug delivery systems |
| KR102871690B1 (ko) | 2018-04-30 | 2025-10-16 | 리제너론 파마슈티칼스 인코포레이티드 | Her2 및/또는 aplp2에 결합하는 항체 및 이중특이적 항원-결합 분자 및 접합체 그리고 이들의 용도 |
| AU2019269685B2 (en) | 2018-05-17 | 2025-12-04 | Regeneron Pharmaceuticals, Inc. | Anti-CD63 antibodies, conjugates, and uses thereof |
| WO2020057543A1 (zh) * | 2018-09-21 | 2020-03-26 | 中国人民解放军军事科学院军事医学研究院 | 基于芳硝基的连接子、含连接子的抗体偶联药物及连接子的用途 |
| JP2022523360A (ja) | 2019-02-21 | 2022-04-22 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | Metに結合する抗met抗体および二特異性抗原結合分子を使用した眼癌の治療方法 |
| KR20220063185A (ko) | 2019-09-16 | 2022-05-17 | 리제너론 파마슈티칼스 인코포레이티드 | 면역-pet 영상화를 위한 방사성 표지된 met 결합 단백질 |
| US11814428B2 (en) * | 2019-09-19 | 2023-11-14 | Regeneron Pharmaceuticals, Inc. | Anti-PTCRA antibody-drug conjugates and uses thereof |
| WO2021097220A1 (en) | 2019-11-15 | 2021-05-20 | Seagen Inc. | Methods of treating her2 positive breast cancer with tucatinib in combination with an anti-her2 antibody-drug conjugate |
| CN113292574B (zh) * | 2020-02-21 | 2022-05-03 | 四川大学 | 一类手性多环的托品烷化合物及其制备方法和用途 |
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