JPWO2022036101A5 - - Google Patents
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- JPWO2022036101A5 JPWO2022036101A5 JP2023509443A JP2023509443A JPWO2022036101A5 JP WO2022036101 A5 JPWO2022036101 A5 JP WO2022036101A5 JP 2023509443 A JP2023509443 A JP 2023509443A JP 2023509443 A JP2023509443 A JP 2023509443A JP WO2022036101 A5 JPWO2022036101 A5 JP WO2022036101A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyldiyl
- peg
- pep
- alkyl
- amino
- 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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- 229940127121 immunoconjugate Drugs 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- -1 alkyldiyl Chemical group 0.000 claims 13
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 8
- 125000004452 carbocyclyl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 208000002030 Merkel cell carcinoma Diseases 0.000 claims 3
- HBHMYSGFYOWCSU-UHFFFAOYSA-N NC1=NC2=CN=NC2=CC=C1 Chemical group NC1=NC2=CN=NC2=CC=C1 HBHMYSGFYOWCSU-UHFFFAOYSA-N 0.000 claims 3
- 206010029266 Neuroendocrine carcinoma of the skin Diseases 0.000 claims 3
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 3
- 208000017763 cutaneous neuroendocrine carcinoma Diseases 0.000 claims 3
- 206010017758 gastric cancer Diseases 0.000 claims 3
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 201000011549 stomach cancer Diseases 0.000 claims 3
- 125000006693 (C2-C9) heterocyclyl group Chemical group 0.000 claims 2
- 108010074708 B7-H1 Antigen Proteins 0.000 claims 2
- 102000008096 B7-H1 Antigen Human genes 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 125000006519 CCH3 Chemical group 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 claims 2
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 2
- 101150117918 Tacstd2 gene Proteins 0.000 claims 2
- 102100027212 Tumor-associated calcium signal transducer 2 Human genes 0.000 claims 2
- 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 2
- 150000001413 amino acids Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 229940097043 glucuronic acid Drugs 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
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 2
- 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 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- DJQYYYCQOZMCRC-UHFFFAOYSA-N 2-aminopropane-1,3-dithiol Chemical compound SCC(N)CS DJQYYYCQOZMCRC-UHFFFAOYSA-N 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
- 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
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 108010016626 Dipeptides Proteins 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm 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
- 101000617725 Homo sapiens Pregnancy-specific beta-1-glycoprotein 2 Proteins 0.000 claims 1
- 101000669402 Homo sapiens Toll-like receptor 7 Proteins 0.000 claims 1
- 101000800483 Homo sapiens Toll-like receptor 8 Proteins 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-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 group O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 1
- OVRNDRQMDRJTHS-UHFFFAOYSA-N N-acelyl-D-glucosamine Natural products CC(=O)NC1C(O)OC(CO)C(O)C1O OVRNDRQMDRJTHS-UHFFFAOYSA-N 0.000 claims 1
- OVRNDRQMDRJTHS-RTRLPJTCSA-N N-acetyl-D-glucosamine Chemical compound CC(=O)N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-RTRLPJTCSA-N 0.000 claims 1
- MBLBDJOUHNCFQT-LXGUWJNJSA-N N-acetylglucosamine Natural products CC(=O)N[C@@H](C=O)[C@@H](O)[C@H](O)[C@H](O)CO MBLBDJOUHNCFQT-LXGUWJNJSA-N 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 102100022019 Pregnancy-specific beta-1-glycoprotein 2 Human genes 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102100039390 Toll-like receptor 7 Human genes 0.000 claims 1
- 102100033110 Toll-like receptor 8 Human genes 0.000 claims 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006593 Urologic Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 230000008484 agonism Effects 0.000 claims 1
- 108010084094 alanyl-alanyl-alanyl-alanine Proteins 0.000 claims 1
- 108010087049 alanyl-alanyl-prolyl-valine Proteins 0.000 claims 1
- 235000001014 amino acid Nutrition 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
- 235000003704 aspartic acid Nutrition 0.000 claims 1
- 229960003852 atezolizumab Drugs 0.000 claims 1
- 229950002916 avelumab Drugs 0.000 claims 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000001268 conjugating effect Effects 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
- 201000007492 gastroesophageal junction adenocarcinoma Diseases 0.000 claims 1
- 229950000518 labetuzumab Drugs 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001394 metastastic effect Effects 0.000 claims 1
- 206010061289 metastatic neoplasm Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 229960002087 pertuzumab Drugs 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000007112 pro inflammatory response Effects 0.000 claims 1
- 229950001460 sacituzumab Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 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 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- 208000022679 triple-negative breast carcinoma Diseases 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 |
|---|---|---|---|
| US202063065219P | 2020-08-13 | 2020-08-13 | |
| US63/065,219 | 2020-08-13 | ||
| PCT/US2021/045752 WO2022036101A1 (en) | 2020-08-13 | 2021-08-12 | Pyrazoloazepine immunoconjugates, and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023537940A JP2023537940A (ja) | 2023-09-06 |
| JPWO2022036101A5 true JPWO2022036101A5 (https=) | 2024-08-14 |
| JP2023537940A5 JP2023537940A5 (https=) | 2024-08-14 |
Family
ID=77627548
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023509443A Pending JP2023537940A (ja) | 2020-08-13 | 2021-08-12 | ピラゾロアゼピンイムノコンジュゲート、及びその使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230263903A1 (https=) |
| EP (1) | EP4196168A1 (https=) |
| JP (1) | JP2023537940A (https=) |
| KR (1) | KR20230051189A (https=) |
| CN (1) | CN116234586A (https=) |
| AU (1) | AU2021326516A1 (https=) |
| CA (1) | CA3186059A1 (https=) |
| IL (1) | IL300316A (https=) |
| MX (1) | MX2023001679A (https=) |
| WO (1) | WO2022036101A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN118475372A (zh) * | 2021-10-29 | 2024-08-09 | 博尔特生物治疗药物有限公司 | 具有半胱氨酸突变抗体的tlr激动剂免疫缀合物及其用途 |
| WO2026050213A1 (en) * | 2024-08-27 | 2026-03-05 | Usbolt Biotherapeutics, Inc. | Tlr agonist immunoconjugates and uses thereof |
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2021
- 2021-08-12 CN CN202180056589.5A patent/CN116234586A/zh active Pending
- 2021-08-12 US US18/017,541 patent/US20230263903A1/en active Pending
- 2021-08-12 EP EP21765793.1A patent/EP4196168A1/en active Pending
- 2021-08-12 AU AU2021326516A patent/AU2021326516A1/en not_active Abandoned
- 2021-08-12 KR KR1020237004880A patent/KR20230051189A/ko not_active Withdrawn
- 2021-08-12 WO PCT/US2021/045752 patent/WO2022036101A1/en not_active Ceased
- 2021-08-12 MX MX2023001679A patent/MX2023001679A/es unknown
- 2021-08-12 JP JP2023509443A patent/JP2023537940A/ja active Pending
- 2021-08-12 CA CA3186059A patent/CA3186059A1/en active Pending
- 2021-08-12 IL IL300316A patent/IL300316A/en unknown
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