JPWO2021138512A5 - - Google Patents
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- JPWO2021138512A5 JPWO2021138512A5 JP2022540992A JP2022540992A JPWO2021138512A5 JP WO2021138512 A5 JPWO2021138512 A5 JP WO2021138512A5 JP 2022540992 A JP2022540992 A JP 2022540992A JP 2022540992 A JP2022540992 A JP 2022540992A JP WO2021138512 A5 JPWO2021138512 A5 JP WO2021138512A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- alkyl
- inhibitor
- amino
- pharmaceutically acceptable
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 81
- 150000003839 salts Chemical class 0.000 claims description 53
- 239000003112 inhibitor Substances 0.000 claims description 50
- 150000001413 amino acids Chemical group 0.000 claims description 36
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 28
- 125000001424 substituent group Chemical group 0.000 claims description 28
- 125000001475 halogen functional group Chemical group 0.000 claims description 26
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 24
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 17
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 201000011510 cancer Diseases 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 12
- 239000012269 PD-1/PD-L1 inhibitor Substances 0.000 claims description 11
- 229940121653 pd-1/pd-l1 inhibitor Drugs 0.000 claims description 11
- 206010009944 Colon cancer Diseases 0.000 claims description 10
- -1 amino-8-(pyrimidin-4-yl)-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl Chemical group 0.000 claims description 10
- 208000029742 colonic neoplasm Diseases 0.000 claims description 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 10
- 201000001441 melanoma Diseases 0.000 claims description 10
- 206010005003 Bladder cancer Diseases 0.000 claims description 8
- 206010006187 Breast cancer Diseases 0.000 claims description 8
- 208000026310 Breast neoplasm Diseases 0.000 claims description 8
- 206010014733 Endometrial cancer Diseases 0.000 claims description 8
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 8
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 8
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 8
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 8
- 206010038389 Renal cancer Diseases 0.000 claims description 8
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 8
- 150000001875 compounds Chemical class 0.000 claims description 8
- 201000010982 kidney cancer Diseases 0.000 claims description 8
- 201000005202 lung cancer Diseases 0.000 claims description 8
- 208000020816 lung neoplasm Diseases 0.000 claims description 8
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 8
- 201000002528 pancreatic cancer Diseases 0.000 claims description 8
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 8
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 8
- 206010061424 Anal cancer Diseases 0.000 claims description 6
- 208000007860 Anus Neoplasms Diseases 0.000 claims description 6
- 102000008096 B7-H1 Antigen Human genes 0.000 claims description 6
- 108010074708 B7-H1 Antigen Proteins 0.000 claims description 6
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 6
- 208000002030 Merkel cell carcinoma Diseases 0.000 claims description 6
- 206010027406 Mesothelioma Diseases 0.000 claims description 6
- 206010033128 Ovarian cancer Diseases 0.000 claims description 6
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 6
- 206010060862 Prostate cancer Diseases 0.000 claims description 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 6
- 206010039491 Sarcoma Diseases 0.000 claims description 6
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 6
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 6
- 201000011165 anus cancer Diseases 0.000 claims description 6
- 201000010881 cervical cancer Diseases 0.000 claims description 6
- 208000017763 cutaneous neuroendocrine carcinoma Diseases 0.000 claims description 6
- 239000012458 free base Substances 0.000 claims description 6
- 201000010536 head and neck cancer Diseases 0.000 claims description 6
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 6
- 201000007270 liver cancer Diseases 0.000 claims description 6
- 208000014018 liver neoplasm Diseases 0.000 claims description 6
- 201000005443 oral cavity cancer Diseases 0.000 claims description 6
- 206010038038 rectal cancer Diseases 0.000 claims description 6
- 201000001275 rectum cancer Diseases 0.000 claims description 6
- 201000008261 skin carcinoma Diseases 0.000 claims description 6
- 201000002510 thyroid cancer Diseases 0.000 claims description 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 4
- AQOSXEZNVWHOHG-UHFFFAOYSA-N NC1=NC(=C(C=2N1N=C(N=2)CN1N=C(N=N1)C1=NC=CC=C1)C1=NC=NC=C1)C=1C=C(C#N)C=CC=1 Chemical compound NC1=NC(=C(C=2N1N=C(N=2)CN1N=C(N=N1)C1=NC=CC=C1)C1=NC=NC=C1)C=1C=C(C#N)C=CC=1 AQOSXEZNVWHOHG-UHFFFAOYSA-N 0.000 claims description 4
- 206010029266 Neuroendocrine carcinoma of the skin Diseases 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000002947 alkylene group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 230000001413 cellular effect Effects 0.000 claims description 4
- 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 description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- VAZQLKLWNFTTFT-UHFFFAOYSA-N 3-[8-amino-5-(1-methyl-6-oxopyridazin-3-yl)-2-(pyridin-2-ylmethyl)-[1,2,4]triazolo[1,5-a]pyrazin-6-yl]benzonitrile Chemical group N1=C(C=2N(N=C(N=2)CC2=CC=CC=N2)C(=C1C1=CC(C#N)=CC=C1)C=1C=CC(=O)N(N=1)C)N VAZQLKLWNFTTFT-UHFFFAOYSA-N 0.000 claims description 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- QARLNMDDSQMINK-BVRKHOPBSA-N (3R)-1-[[7-cyano-2-[3-[3-[[3-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]-1,7-naphthyridin-8-yl]amino]-2-methylphenyl]-2-methylphenyl]-1,3-benzoxazol-5-yl]methyl]pyrrolidine-3-carboxylic acid Chemical group C(#N)C1=CC(=CC=2N=C(OC=21)C=1C(=C(C=CC=1)C1=C(C(=CC=C1)NC=1N=CC=C2C=C(C=NC=12)CN1C[C@@H](CC1)O)C)C)CN1C[C@@H](CC1)C(=O)O QARLNMDDSQMINK-BVRKHOPBSA-N 0.000 claims description 2
- UWNQHIDMVGEEFD-UHFFFAOYSA-N 3-[4-amino-2-(pyridin-2-ylmethyl)-7-pyrimidin-4-yltriazolo[4,5-c]pyridin-6-yl]benzonitrile Chemical group N1=C(C=2C(C(C1=C1C=C(C#N)C=C[CH]1)=C1C=CN=C[N]1)=NN(N=2)CC1=CC=CC=N1)N UWNQHIDMVGEEFD-UHFFFAOYSA-N 0.000 claims description 2
- UDTYMQWVZMEAGS-UHFFFAOYSA-N 3-[4-amino-2-[(3-fluoropyridin-2-yl)methyl]-7-pyridin-4-yltriazolo[4,5-c]pyridin-6-yl]benzonitrile Chemical compound N1=C(C=2C(C(C1=C1C=C(C#N)C=C[CH]1)=C1C=CN=C[CH]1)=NN(N=2)CC1=C(F)C=CC=N1)N UDTYMQWVZMEAGS-UHFFFAOYSA-N 0.000 claims description 2
- MSXIFXOIITVIOS-UHFFFAOYSA-N 3-[4-amino-2-[(3-fluoropyridin-2-yl)methyl]-7-pyrimidin-4-yltriazolo[4,5-c]pyridin-6-yl]benzonitrile Chemical compound NC1=NC(=C(C=2C1=NN(N=2)CC1=NC=CC=C1F)C1=NC=NC=C1)C=1C=C(C#N)C=CC=1 MSXIFXOIITVIOS-UHFFFAOYSA-N 0.000 claims description 2
- WDIMPXNTABEEDG-UHFFFAOYSA-N 3-[4-amino-7-(2-methylpyrazol-3-yl)-2-(pyridin-2-ylmethyl)triazolo[4,5-c]pyridin-6-yl]-2-fluorobenzonitrile Chemical compound N1=C(C=2C(C(=C1C1=C(F)C(C#N)=CC=C1)C1=CC=NN1C)=NN(N=2)CC1=CC=CC=N1)N WDIMPXNTABEEDG-UHFFFAOYSA-N 0.000 claims description 2
- MNUAACPKOCGMKO-UHFFFAOYSA-N 3-[5-amino-2-(pyridin-2-ylmethyl)-8-pyrimidin-4-yl-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]benzonitrile Chemical group NC1=NC(=C(C=2N1N=C(N=2)CC1=NC=CC=C1)C1=NC=NC=C1)C=1C=C(C#N)C=CC=1 MNUAACPKOCGMKO-UHFFFAOYSA-N 0.000 claims description 2
- USUJGMZEOPRMRJ-UHFFFAOYSA-N 3-[5-amino-2-[(2,6-difluorophenyl)-hydroxymethyl]-8-pyrimidin-4-yl-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]benzonitrile Chemical compound NC1=NC(C2=CC=CC(=C2)C#N)=C(C2=NC(=NN12)C(O)C1=C(F)C=CC=C1F)C1=CC=NC=N1 USUJGMZEOPRMRJ-UHFFFAOYSA-N 0.000 claims description 2
- PSIZASRGFVKTTQ-UHFFFAOYSA-N 3-[5-amino-2-[(2,6-difluorophenyl)-hydroxymethyl]-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]-2-fluorobenzonitrile Chemical compound NC1=NC(=CC=2N1N=C(N=2)C(O)C1=C(C=CC=C1F)F)C=1C(=C(C#N)C=CC=1)F PSIZASRGFVKTTQ-UHFFFAOYSA-N 0.000 claims description 2
- MWOOCFNLLDAOEV-UHFFFAOYSA-N 3-[5-amino-2-[(3-methylpyridin-2-yl)methoxy]-8-pyrimidin-4-yl-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]benzonitrile Chemical compound NC1=NC(=C(C=2N1N=C(N=2)OCC1=NC=CC=C1C)C1=NC=NC=C1)C=1C=C(C#N)C=CC=1 MWOOCFNLLDAOEV-UHFFFAOYSA-N 0.000 claims description 2
- FBUFJQGAFJKAJJ-UHFFFAOYSA-N 3-[5-amino-2-[(5-pyridin-2-yltetrazol-1-yl)methyl]-8-pyrimidin-4-yl-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]benzonitrile Chemical compound NC1=NC(=C(C=2N1N=C(N=2)CN1N=NN=C1C1=NC=CC=C1)C1=NC=NC=C1)C=1C=C(C#N)C=CC=1 FBUFJQGAFJKAJJ-UHFFFAOYSA-N 0.000 claims description 2
- XAVOVGDLJRYSDJ-UHFFFAOYSA-N 3-[5-amino-2-[hydroxy(phenyl)methyl]-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]benzonitrile Chemical group NC1=NC(=CC=2N1N=C(N=2)C(C1=CC=CC=C1)O)C=1C=C(C#N)C=CC=1 XAVOVGDLJRYSDJ-UHFFFAOYSA-N 0.000 claims description 2
- PLZPCHXKFQBBGL-UHFFFAOYSA-N 3-[8-amino-2-[(2,6-difluorophenyl)-hydroxymethyl]-5-(2,6-dimethylpyridin-4-yl)-[1,2,4]triazolo[1,5-a]pyrazin-6-yl]benzonitrile Chemical compound FC1=C(C(C=2N=C3C(=NC(C4=CC(C#N)=CC=C4)=C(N3N=2)C2=CC(C)=NC(=C2)C)N)O)C(F)=CC=C1 PLZPCHXKFQBBGL-UHFFFAOYSA-N 0.000 claims description 2
- UDHRZPXDBKETGI-UHFFFAOYSA-N 3-[8-amino-2-[(2,6-difluorophenyl)-hydroxymethyl]-5-pyrimidin-4-yl-[1,2,4]triazolo[1,5-a]pyrazin-6-yl]benzonitrile Chemical compound FC1=C(C(C=2N=C3C(=NC(C4=CC(C#N)=CC=C4)=C(N3N=2)C2=CC=NC=N2)N)O)C(F)=CC=C1 UDHRZPXDBKETGI-UHFFFAOYSA-N 0.000 claims description 2
- KZAQSNJJLYBWHO-UHFFFAOYSA-N 3-[8-amino-2-[amino-(2,6-difluorophenyl)methyl]-5-(4-methyl-1,3-oxazol-5-yl)-[1,2,4]triazolo[1,5-a]pyrazin-6-yl]benzonitrile Chemical compound NC=1C=2N(C(=C(N=1)C=1C=C(C#N)C=CC=1)C1=C(N=CO1)C)N=C(N=2)C(C1=C(C=CC=C1F)F)N KZAQSNJJLYBWHO-UHFFFAOYSA-N 0.000 claims description 2
- VLLMDXWWQMNKSI-UHFFFAOYSA-N 5-amino-7-(3-cyano-2-fluorophenyl)-2-[(2,6-difluorophenyl)-hydroxymethyl]-[1,2,4]triazolo[1,5-c]pyrimidine-8-carbonitrile Chemical compound NC1=NC(=C(C=2N1N=C(N=2)C(O)C1=C(C=CC=C1F)F)C#N)C1=C(C(=CC=C1)C#N)F VLLMDXWWQMNKSI-UHFFFAOYSA-N 0.000 claims description 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 229960003852 atezolizumab Drugs 0.000 claims description 2
- 229960002621 pembrolizumab Drugs 0.000 claims description 2
- 208000000649 small cell carcinoma Diseases 0.000 claims description 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 2
- 108010047041 Complementarity Determining Regions Proteins 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 239000000427 antigen Substances 0.000 claims 3
- 102000036639 antigens Human genes 0.000 claims 3
- 108091007433 antigens Proteins 0.000 claims 3
- 239000012634 fragment Substances 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 238000000034 method Methods 0.000 description 29
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- VZHDVSBCDXQCHY-UHFFFAOYSA-N 3-[5-amino-2-[(5-pyrazol-1-yltetrazol-2-yl)methyl]-8-pyrimidin-4-yl-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]benzonitrile Chemical compound N1(N=CC=C1)C=1N=NN(N=1)CC1=NN2C(=NC(=C(C2=N1)C1=NC=NC=C1)C=1C=C(C#N)C=CC=1)N VZHDVSBCDXQCHY-UHFFFAOYSA-N 0.000 description 1
- FYICDFUJPPPZCX-UHFFFAOYSA-N 3-[5-amino-2-[[2-fluoro-6-[[(1-methyl-2-oxopyrrolidin-3-yl)amino]methyl]phenyl]-hydroxymethyl]-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]-2-fluorobenzonitrile Chemical compound NC1=NC(=CC=2N1N=C(N=2)C(O)C1=C(C=CC=C1CNC1C(N(CC1)C)=O)F)C=1C(=C(C#N)C=CC=1)F FYICDFUJPPPZCX-UHFFFAOYSA-N 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062956960P | 2020-01-03 | 2020-01-03 | |
| US62/956,960 | 2020-01-03 | ||
| PCT/US2020/067593 WO2021138512A1 (en) | 2020-01-03 | 2020-12-30 | Combination therapy comprising a2a/a2b and pd-1/pd-l1 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023509456A JP2023509456A (ja) | 2023-03-08 |
| JPWO2021138512A5 true JPWO2021138512A5 (ru) | 2023-12-22 |
Family
ID=74285585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022540992A Pending JP2023509456A (ja) | 2020-01-03 | 2020-12-30 | Ａ２ａ／ａ２ｂ及びｐｄ－１／ｐｄ－ｌ１阻害剤を含む併用療法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20210205311A1 (ru) |
| EP (1) | EP4085060A1 (ru) |
| JP (1) | JP2023509456A (ru) |
| KR (1) | KR20220150281A (ru) |
| CN (1) | CN115279766A (ru) |
| AU (1) | AU2020417813A1 (ru) |
| CA (1) | CA3166549A1 (ru) |
| CL (1) | CL2022001794A1 (ru) |
| IL (1) | IL294438A (ru) |
| MX (1) | MX2022008208A (ru) |
| TW (1) | TW202135824A (ru) |
| WO (1) | WO2021138512A1 (ru) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7474709B2 (ja) | 2018-02-27 | 2024-04-25 | インサイト・コーポレイション | Ａ２ａ／ａ２ｂ阻害剤としてのイミダゾピリミジン及びトリアゾロピリミジン |
| MA52940A (fr) | 2018-05-18 | 2021-04-28 | Incyte Corp | Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b |
| AU2019297361B2 (en) | 2018-07-05 | 2024-06-27 | Incyte Corporation | Fused pyrazine derivatives as A2A / A2B inhibitors |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| WO2024025986A1 (en) * | 2022-07-28 | 2024-02-01 | Merck Sharp & Dohme Llc | Pharmaceutical compositions of programmed death receptor 1 (pd-1) antibodies and ph20 variants or fragments thereof |
| WO2024025989A1 (en) * | 2022-07-28 | 2024-02-01 | Merck Sharp & Dohme Llc | Pharmaceutical compositions of programmed death receptor 1 (pd-1) antibodies and rhuph20 or variants or fragments thereof |
| CN118384164A (zh) * | 2023-01-25 | 2024-07-26 | 因派蒂斯生物科学有限公司 | 用腺苷a2a抑制剂治疗癌症的方法 |
| WO2024214088A1 (en) * | 2023-04-14 | 2024-10-17 | Aurigene Oncology Limited | Heterocyclic compounds as dual inhibitors of pd-l1 and adenosine receptors |
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2020
- 2020-12-30 CA CA3166549A patent/CA3166549A1/en active Pending
- 2020-12-30 TW TW109146917A patent/TW202135824A/zh unknown
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- 2020-12-30 JP JP2022540992A patent/JP2023509456A/ja active Pending
- 2020-12-30 US US17/138,485 patent/US20210205311A1/en active Pending
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- 2020-12-30 MX MX2022008208A patent/MX2022008208A/es unknown
- 2020-12-30 CN CN202080097070.7A patent/CN115279766A/zh active Pending
- 2020-12-30 KR KR1020227026581A patent/KR20220150281A/ko unknown
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