JP2020525429A5 - - Google Patents
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- Publication number
- JP2020525429A5 JP2020525429A5 JP2019570808A JP2019570808A JP2020525429A5 JP 2020525429 A5 JP2020525429 A5 JP 2020525429A5 JP 2019570808 A JP2019570808 A JP 2019570808A JP 2019570808 A JP2019570808 A JP 2019570808A JP 2020525429 A5 JP2020525429 A5 JP 2020525429A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- nhc
- halo
- methyl
- 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.)
- Granted
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- 125000005843 halogen group Chemical group 0.000 claims 25
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 16
- -1 amino, hydroxy Chemical group 0.000 claims 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000004429 atom Chemical group 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 10
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000003831 tetrazolyl group Chemical group 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 6
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 6
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- MVXVYAKCVDQRLW-UHFFFAOYSA-N azain Natural products C1=CN=C2NC=CC2=C1 MVXVYAKCVDQRLW-UHFFFAOYSA-N 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
- 208000035473 Communicable disease Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 229960002685 biotin Drugs 0.000 claims 2
- 235000020958 biotin Nutrition 0.000 claims 2
- 239000011616 biotin Substances 0.000 claims 2
- 230000002708 enhancing effect Effects 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 229940046009 vitamin E Drugs 0.000 claims 2
- 239000011709 vitamin E Substances 0.000 claims 2
- MTAODLNXWYIKSO-UHFFFAOYSA-N 2-fluoropyridine Chemical compound FC1=CC=CC=N1 MTAODLNXWYIKSO-UHFFFAOYSA-N 0.000 claims 1
- 102000008096 B7-H1 Antigen Human genes 0.000 claims 1
- 108010074708 B7-H1 Antigen Proteins 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 101000914484 Homo sapiens T-lymphocyte activation antigen CD80 Proteins 0.000 claims 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical group C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 102100027222 T-lymphocyte activation antigen CD80 Human genes 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003275 alpha amino acid group Chemical group 0.000 claims 1
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 230000012010 growth Effects 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 210000004798 organs belonging to the digestive system Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 230000004936 stimulating effect Effects 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762523903P | 2017-06-23 | 2017-06-23 | |
| US62/523,903 | 2017-06-23 | ||
| PCT/US2018/038768 WO2018237153A1 (en) | 2017-06-23 | 2018-06-21 | Immunomodulators acting as antagonists of pd-1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020525429A JP2020525429A (ja) | 2020-08-27 |
| JP2020525429A5 true JP2020525429A5 (enExample) | 2021-07-29 |
| JP7206222B2 JP7206222B2 (ja) | 2023-01-17 |
Family
ID=62909620
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019570808A Active JP7206222B2 (ja) | 2017-06-23 | 2018-06-21 | Ｐｄ－１のアンタゴニストとして作用する免疫調節剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11066445B2 (enExample) |
| EP (1) | EP3642220A1 (enExample) |
| JP (1) | JP7206222B2 (enExample) |
| KR (1) | KR102735038B1 (enExample) |
| CN (1) | CN110997698B (enExample) |
| WO (1) | WO2018237153A1 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9856292B2 (en) | 2014-11-14 | 2018-01-02 | Bristol-Myers Squibb Company | Immunomodulators |
| SI3458111T1 (sl) | 2016-05-19 | 2021-07-30 | Bristol-Myers Squibb Company | Imunomodulatorji prikazani s pet |
| EP3535280B1 (en) | 2016-11-07 | 2022-03-16 | Bristol-Myers Squibb Company | Immunomodulators |
| WO2018200571A1 (en) | 2017-04-25 | 2018-11-01 | Arbutus Biopharma Corporation | Substituted 2,3-dihydro-1h-indene analogs and methods using same |
| WO2019070643A1 (en) | 2017-10-03 | 2019-04-11 | Bristol-Myers Squibb Company | IMMUNOMODULATORS |
| WO2019191624A1 (en) | 2018-03-29 | 2019-10-03 | Arbutus Biopharma, Inc. | Substituted 1,1'-biphenyl compounds, analogues thereof, and methods using same |
| SG11202104455XA (en) * | 2018-12-11 | 2021-05-28 | Heidelberg Pharma Res Gmbh | Synthesis of (s)-6-hydroxytryptophan and derivatives thereof |
| CN113677402A (zh) | 2019-03-28 | 2021-11-19 | 百时美施贵宝公司 | 治疗肿瘤的方法 |
| CN113891748A (zh) | 2019-03-28 | 2022-01-04 | 百时美施贵宝公司 | 治疗肿瘤的方法 |
| EP3972694A1 (en) * | 2019-05-21 | 2022-03-30 | Bristol-Myers Squibb Company | Immunomodulators |
| CN114174537A (zh) | 2019-05-30 | 2022-03-11 | 百时美施贵宝公司 | 细胞定位特征和组合疗法 |
| WO2020243568A1 (en) | 2019-05-30 | 2020-12-03 | Bristol-Myers Squibb Company | Methods of identifying a subject suitable for an immuno-oncology (i-o) therapy |
| WO2020243563A1 (en) | 2019-05-30 | 2020-12-03 | Bristol-Myers Squibb Company | Multi-tumor gene signatures for suitability to immuno-oncology therapy |
| WO2021055994A1 (en) | 2019-09-22 | 2021-03-25 | Bristol-Myers Squibb Company | Quantitative spatial profiling for lag-3 antagonist therapy |
| CN115942973A (zh) | 2019-11-08 | 2023-04-07 | 百时美施贵宝公司 | 用于黑色素瘤的lag-3拮抗剂疗法 |
| EP4087857B1 (en) * | 2020-01-06 | 2023-11-01 | Bristol-Myers Squibb Company | Immunomodulators |
| ES2970547T3 (es) | 2020-03-30 | 2024-05-29 | Bristol Myers Squibb Co | Inmunomoduladores |
| KR20230008790A (ko) * | 2020-05-08 | 2023-01-16 | 브리스톨-마이어스 스큅 컴퍼니 | 면역조정제 |
| CN111961117B (zh) * | 2020-08-19 | 2022-03-11 | 中山大学 | 一种环肽化合物及其应用 |
| EP4204095A1 (en) | 2020-08-28 | 2023-07-05 | Bristol-Myers Squibb Company | Lag-3 antagonist therapy for hepatocellular carcinoma |
| IL300916A (en) | 2020-08-31 | 2023-04-01 | Bristol Myers Squibb Co | Cell localization signature and immunotherapy |
| AU2021364837A1 (en) | 2020-10-23 | 2023-05-25 | Bristol-Myers Squibb Company | Lag-3 antagonist therapy for lung cancer |
| WO2022120179A1 (en) | 2020-12-03 | 2022-06-09 | Bristol-Myers Squibb Company | Multi-tumor gene signatures and uses thereof |
| US20240199701A1 (en) * | 2021-03-24 | 2024-06-20 | Bristol-Myers Squibb Company | Immunomodulators |
| US20240181052A1 (en) | 2021-03-29 | 2024-06-06 | Juno Therapeutics, Inc. | Methods for dosing and treatment with a combination of a checkpoint inhibitor therapy and a car t cell therapy |
| EP4323380A2 (en) * | 2021-04-12 | 2024-02-21 | Bristol-Myers Squibb Company | Cyclic peptide immunomodulators |
| EP4419540A1 (en) * | 2021-10-20 | 2024-08-28 | Bristol-Myers Squibb Company | Immunomodulators |
| CN118176214A (zh) | 2021-10-29 | 2024-06-11 | 百时美施贵宝公司 | 血液癌症的lag-3拮抗剂疗法 |
| MX2024008831A (es) | 2022-01-26 | 2024-07-25 | Bristol Myers Squibb Co | Terapia combinada para carcinoma hepatocelular. |
| IL315992A (en) | 2022-04-08 | 2024-11-01 | Bristol Myers Squibb Co | Identification, classification and quantification of tertiary lymphoid structures using machine learning |
| IL321575A (en) | 2022-12-21 | 2025-08-01 | Bristol Myers Squibb Co | Combination therapy for lung cancer |
| WO2024196952A1 (en) | 2023-03-20 | 2024-09-26 | Bristol-Myers Squibb Company | Tumor subtype assessment for cancer therapy |
| WO2025061971A1 (en) | 2023-09-20 | 2025-03-27 | Trimt Gmbh | Functionalized peptides for in-vivo addressing of pd-l1 expression |
| WO2025245489A1 (en) | 2024-05-24 | 2025-11-27 | Bristol-Myers Squibb Company | Treatment of tumors in subjects having fgl-1 positive samples |
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| CA2960778C (en) | 2014-09-11 | 2023-03-07 | Bristol-Myers Squibb Company | Macrocyclic inhibitors of the pd-1/pd-l1 and cd80(b7-1)/pd-l1 protein/protein interactions |
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| EA034516B1 (ru) | 2014-11-25 | 2020-02-14 | Бристол-Маерс Сквибб Компани | Способы и композиции для мечения радиоактивным изотопомf биологических препаратов |
| US9861680B2 (en) * | 2014-12-18 | 2018-01-09 | Bristol-Myers Squibb Company | Immunomodulators |
| US9944678B2 (en) * | 2014-12-19 | 2018-04-17 | Bristol-Myers Squibb Company | Immunomodulators |
| US20160222060A1 (en) * | 2015-02-04 | 2016-08-04 | Bristol-Myers Squibb Company | Immunomodulators |
| US9809625B2 (en) * | 2015-03-18 | 2017-11-07 | Bristol-Myers Squibb Company | Immunomodulators |
| US10143746B2 (en) | 2016-03-04 | 2018-12-04 | Bristol-Myers Squibb Company | Immunomodulators |
| US10358463B2 (en) * | 2016-04-05 | 2019-07-23 | Bristol-Myers Squibb Company | Immunomodulators |
| SI3458111T1 (sl) | 2016-05-19 | 2021-07-30 | Bristol-Myers Squibb Company | Imunomodulatorji prikazani s pet |
| EP3535280B1 (en) | 2016-11-07 | 2022-03-16 | Bristol-Myers Squibb Company | Immunomodulators |
| WO2019070643A1 (en) | 2017-10-03 | 2019-04-11 | Bristol-Myers Squibb Company | IMMUNOMODULATORS |
-
2018
- 2018-06-21 EP EP18740706.9A patent/EP3642220A1/en active Pending
- 2018-06-21 WO PCT/US2018/038768 patent/WO2018237153A1/en not_active Ceased
- 2018-06-21 KR KR1020207001815A patent/KR102735038B1/ko active Active
- 2018-06-21 US US16/624,989 patent/US11066445B2/en active Active
- 2018-06-21 JP JP2019570808A patent/JP7206222B2/ja active Active
- 2018-06-21 CN CN201880052406.0A patent/CN110997698B/zh active Active
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