JPWO2021226440A5 - - Google Patents
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- JPWO2021226440A5 JPWO2021226440A5 JP2022566686A JP2022566686A JPWO2021226440A5 JP WO2021226440 A5 JPWO2021226440 A5 JP WO2021226440A5 JP 2022566686 A JP2022566686 A JP 2022566686A JP 2022566686 A JP2022566686 A JP 2022566686A JP WO2021226440 A5 JPWO2021226440 A5 JP WO2021226440A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyldiyl
- immunoconjugate
- espep
- alkyl
- och
- 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.)
- Pending
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 61
- 229940127121 immunoconjugate Drugs 0.000 claims 48
- -1 alkyldiyl Chemical group 0.000 claims 37
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 108090000765 processed proteins & peptides Proteins 0.000 claims 15
- 239000000758 substrate Substances 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000004452 carbocyclyl group Chemical group 0.000 claims 7
- 230000003308 immunostimulating effect Effects 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 6
- 125000006693 (C2-C9) heterocyclyl group Chemical group 0.000 claims 5
- 102000016387 Pancreatic elastase Human genes 0.000 claims 5
- 108010067372 Pancreatic elastase Proteins 0.000 claims 5
- 239000011230 binding agent Substances 0.000 claims 5
- 210000004027 cell Anatomy 0.000 claims 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 5
- 125000006519 CCH3 Chemical group 0.000 claims 4
- 125000000539 amino acid group Chemical group 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 4
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 claims 3
- 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 3
- 229940097043 glucuronic acid Drugs 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 2
- 230000021615 conjugation Effects 0.000 claims 2
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- GJMNLCSOIHOLQZ-FXQIFTODSA-N Ala-Ala-Val Chemical compound CC(C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)N)C(O)=O GJMNLCSOIHOLQZ-FXQIFTODSA-N 0.000 claims 1
- YHBDGLZYNIARKJ-GUBZILKMSA-N Ala-Pro-Val Chemical compound CC(C)[C@@H](C(O)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N YHBDGLZYNIARKJ-GUBZILKMSA-N 0.000 claims 1
- 102100037435 Antiviral innate immune response receptor RIG-I Human genes 0.000 claims 1
- 101710127675 Antiviral innate immune response receptor RIG-I Proteins 0.000 claims 1
- VHQSGALUSWIYOD-QXEWZRGKSA-N Asn-Pro-Val Chemical compound [H]N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(O)=O VHQSGALUSWIYOD-QXEWZRGKSA-N 0.000 claims 1
- 102000008096 B7-H1 Antigen Human genes 0.000 claims 1
- 108010074708 B7-H1 Antigen Proteins 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 101000914324 Homo sapiens Carcinoembryonic antigen-related cell adhesion molecule 5 Proteins 0.000 claims 1
- 101000914321 Homo sapiens Carcinoembryonic antigen-related cell adhesion molecule 7 Proteins 0.000 claims 1
- 101001125026 Homo sapiens Nucleotide-binding oligomerization domain-containing protein 2 Proteins 0.000 claims 1
- 101000617725 Homo sapiens Pregnancy-specific beta-1-glycoprotein 2 Proteins 0.000 claims 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- QEFRNWWLZKMPFJ-YGVKFDHGSA-N L-methionine S-oxide Chemical compound CS(=O)CC[C@H](N)C(O)=O QEFRNWWLZKMPFJ-YGVKFDHGSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 1
- 208000002030 Merkel cell carcinoma Diseases 0.000 claims 1
- 102100022691 NACHT, LRR and PYD domains-containing protein 3 Human genes 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010029266 Neuroendocrine carcinoma of the skin Diseases 0.000 claims 1
- 102100029441 Nucleotide-binding oligomerization domain-containing protein 2 Human genes 0.000 claims 1
- 102100022019 Pregnancy-specific beta-1-glycoprotein 2 Human genes 0.000 claims 1
- 108010001946 Pyrin Domain-Containing 3 Protein NLR Family Proteins 0.000 claims 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 1
- 229940044665 STING agonist Drugs 0.000 claims 1
- 101710196623 Stimulator of interferon genes protein Proteins 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 102000002689 Toll-like receptor Human genes 0.000 claims 1
- 108020000411 Toll-like receptor Proteins 0.000 claims 1
- 229940123384 Toll-like receptor (TLR) agonist Drugs 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006593 Urologic Neoplasms Diseases 0.000 claims 1
- 108010087049 alanyl-alanyl-prolyl-valine Proteins 0.000 claims 1
- 239000000427 antigen Substances 0.000 claims 1
- 102000036639 antigens Human genes 0.000 claims 1
- 108091007433 antigens Proteins 0.000 claims 1
- 229960003852 atezolizumab Drugs 0.000 claims 1
- 229950002916 avelumab Drugs 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000017763 cutaneous neuroendocrine carcinoma Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229950009791 durvalumab Drugs 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 229960001438 immunostimulant agent Drugs 0.000 claims 1
- 239000003022 immunostimulating agent Substances 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 229950000518 labetuzumab Drugs 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 102000007863 pattern recognition receptors Human genes 0.000 claims 1
- 108010089193 pattern recognition receptors Proteins 0.000 claims 1
- 229960002087 pertuzumab Drugs 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 229950001460 sacituzumab Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063022069P | 2020-05-08 | 2020-05-08 | |
| US63/022,069 | 2020-05-08 | ||
| PCT/US2021/031264 WO2021226440A1 (en) | 2020-05-08 | 2021-05-07 | Elastase-substrate, peptide linker immunoconjugates, and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023524271A JP2023524271A (ja) | 2023-06-09 |
| JPWO2021226440A5 true JPWO2021226440A5 (zh) | 2024-04-24 |
Family
ID=76181275
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022566686A Pending JP2023524271A (ja) | 2020-05-08 | 2021-05-07 | エラスターゼ－基質ペプチドリンカーイムノコンジュゲート、及びそれらの使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20230293716A1 (zh) |
| EP (1) | EP4146282A1 (zh) |
| JP (1) | JP2023524271A (zh) |
| CN (1) | CN115996756A (zh) |
| CA (1) | CA3176626A1 (zh) |
| WO (1) | WO2021226440A1 (zh) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20230149857A (ko) | 2016-07-07 | 2023-10-27 | 더 보드 어브 트러스티스 어브 더 리랜드 스탠포드 주니어 유니버시티 | 항체-애쥬번트 접합체 |
| WO2020190725A1 (en) | 2019-03-15 | 2020-09-24 | Bolt Biotherapeutics, Inc. | Immunoconjugates targeting her2 |
| CN116635084A (zh) * | 2020-12-11 | 2023-08-22 | 博尔特生物治疗药物有限公司 | 抗cea免疫缀合物和其用途 |
| WO2022125908A1 (en) * | 2020-12-11 | 2022-06-16 | Bolt Biotherapeutics, Inc. | Anti-pd-l1 immunoconjugates, and uses thereof |
| EP4259211A1 (en) * | 2020-12-11 | 2023-10-18 | Bolt Biotherapeutics, Inc. | Anti-her2 immunoconjugates, and uses thereof |
| CN116744978A (zh) * | 2020-12-11 | 2023-09-12 | 博尔特生物治疗药物有限公司 | 抗her2免疫缀合物及其用途 |
| WO2023076599A1 (en) * | 2021-10-29 | 2023-05-04 | Bolt Biotherapeutics, Inc. | Tlr agonist immunoconjugates with cysteine-mutant antibodies, and uses thereof |
| WO2023154318A1 (en) * | 2022-02-09 | 2023-08-17 | Bolt Biotherapeutics, Inc. | Anti-tr0p2, aminobenzazepine immunoconjugates, and uses thereof |
| TW202339806A (zh) * | 2022-02-09 | 2023-10-16 | 美商博特生物治療公司 | ８—磺醯基—苯并氮呯免疫結合物及其用途 |
| WO2023154302A1 (en) * | 2022-02-09 | 2023-08-17 | Bolt Biotherapeutics, Inc. | Macromolecule-supported 8-sulfonyl-benzazepine compounds and their uses |
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-
2021
- 2021-05-07 CN CN202180046241.8A patent/CN115996756A/zh active Pending
- 2021-05-07 JP JP2022566686A patent/JP2023524271A/ja active Pending
- 2021-05-07 US US17/923,541 patent/US20230293716A1/en active Pending
- 2021-05-07 WO PCT/US2021/031264 patent/WO2021226440A1/en unknown
- 2021-05-07 EP EP21728751.5A patent/EP4146282A1/en active Pending
- 2021-05-07 CA CA3176626A patent/CA3176626A1/en active Pending
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