JPWO2020247475A5 - - Google Patents
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- JPWO2020247475A5 JPWO2020247475A5 JP2021572409A JP2021572409A JPWO2020247475A5 JP WO2020247475 A5 JPWO2020247475 A5 JP WO2020247475A5 JP 2021572409 A JP2021572409 A JP 2021572409A JP 2021572409 A JP2021572409 A JP 2021572409A JP WO2020247475 A5 JPWO2020247475 A5 JP WO2020247475A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- heterocyclyl
- alkyl
- pharmaceutically acceptable
- acceptable salt
- 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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- 150000003839 salts Chemical class 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 15
- 206010028980 Neoplasm Diseases 0.000 claims 13
- 125000001188 haloalkyl group Chemical group 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 150000002431 hydrogen Chemical group 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 9
- 208000009956 adenocarcinoma Diseases 0.000 claims 9
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 9
- 201000009030 Carcinoma Diseases 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 8
- -1 cyano, hydroxyl Chemical group 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000004404 heteroalkyl group Chemical group 0.000 claims 8
- 206010025323 Lymphomas Diseases 0.000 claims 7
- 206010039491 Sarcoma Diseases 0.000 claims 7
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 206010024612 Lipoma Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 206010016629 fibroma Diseases 0.000 claims 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 201000008808 Fibrosarcoma Diseases 0.000 claims 3
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- 125000003118 aryl group Chemical group 0.000 claims 3
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
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- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
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- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
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- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000004605 1,2,3,4-tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
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- 206010014967 Ependymoma Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
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- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 102000051325 Glucagon Human genes 0.000 claims 1
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- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims 1
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- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 201000004458 Myoma Diseases 0.000 claims 1
- 201000004404 Neurofibroma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 201000010133 Oligodendroglioma Diseases 0.000 claims 1
- 206010031149 Osteitis Diseases 0.000 claims 1
- 208000007641 Pinealoma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 208000005678 Rhabdomyoma Diseases 0.000 claims 1
- 101100465401 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) SCL1 gene Proteins 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 208000000097 Sertoli-Leydig cell tumor Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000015778 Undifferentiated pleomorphic sarcoma Diseases 0.000 claims 1
- 206010046431 Urethral cancer Diseases 0.000 claims 1
- 206010046458 Urethral neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000009311 VIPoma Diseases 0.000 claims 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 206010048214 Xanthoma Diseases 0.000 claims 1
- 206010048215 Xanthomatosis Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 210000002534 adenoid Anatomy 0.000 claims 1
- 201000005179 adrenal carcinoma Diseases 0.000 claims 1
- 201000005188 adrenal gland cancer Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 201000007434 ampulla of Vater carcinoma Diseases 0.000 claims 1
- 208000001119 benign fibrous histiocytoma Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
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- 208000003362 bronchogenic carcinoma Diseases 0.000 claims 1
- 201000002143 bronchus adenoma Diseases 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 208000011825 carcinoma of the ampulla of vater Diseases 0.000 claims 1
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- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 1
- 229960004666 glucagon Drugs 0.000 claims 1
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- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
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- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 1
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- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962857515P | 2019-06-05 | 2019-06-05 | |
| US62/857,515 | 2019-06-05 | ||
| PCT/US2020/035891 WO2020247475A1 (en) | 2019-06-05 | 2020-06-03 | Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022535577A JP2022535577A (ja) | 2022-08-09 |
| JPWO2020247475A5 true JPWO2020247475A5 (https=) | 2023-05-08 |
| JP2022535577A5 JP2022535577A5 (https=) | 2023-05-08 |
| JP7541538B2 JP7541538B2 (ja) | 2024-08-28 |
Family
ID=71842807
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021572409A Active JP7541538B2 (ja) | 2019-06-05 | 2020-06-03 | 癌を処置するためのprc2阻害剤としてのイミダゾ[1,2-c]ピリミジン誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US12252493B2 (https=) |
| EP (1) | EP3980422A1 (https=) |
| JP (1) | JP7541538B2 (https=) |
| KR (1) | KR20220027933A (https=) |
| CN (1) | CN114269748A (https=) |
| AU (1) | AU2020288563A1 (https=) |
| CA (1) | CA3142711A1 (https=) |
| IL (1) | IL288529A (https=) |
| WO (1) | WO2020247475A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3746446T3 (da) | 2018-01-31 | 2022-06-27 | Mirati Therapeutics Inc | PRC2-inhibitorer |
| US12421228B2 (en) | 2019-04-22 | 2025-09-23 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as PRC2 inhibitors |
| US12252493B2 (en) | 2019-06-05 | 2025-03-18 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as PRC2 inhibitors for treating cancer |
| CN114907385A (zh) * | 2021-02-10 | 2022-08-16 | 上海青煜医药科技有限公司 | 氮杂芳基化合物、其制备方法及应用 |
| WO2023016511A1 (zh) * | 2021-08-11 | 2023-02-16 | 上海青煜医药科技有限公司 | 氮杂芳基化合物、其制备方法及应用 |
| WO2023049723A1 (en) * | 2021-09-24 | 2023-03-30 | Oric Pharmaceuticals, Inc. | Prc2 inhibitors for use in treating blood disorders |
| EP4404932A4 (en) * | 2021-09-24 | 2025-07-23 | Oric Pharmaceuticals Inc | PRC2 INHIBITORS FOR USE IN THE TREATMENT OF BLOOD DISORDERS |
| EP4630004A1 (en) * | 2022-12-05 | 2025-10-15 | Oric Pharmaceuticals, Inc. | Treatment of prostate cancer having androgen receptor variants |
| WO2024215699A1 (en) * | 2023-04-11 | 2024-10-17 | Oric Pharmaceuticals, Inc. | Treatment of t-cell lymphoma |
| IL326327A (en) * | 2023-08-04 | 2026-04-01 | Oric Pharmaceuticals Inc | Prostate cancer treatment |
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| WO2010021381A1 (ja) | 2008-08-22 | 2010-02-25 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
| UA110112C2 (uk) | 2010-05-07 | 2015-11-25 | Глаксосмітклайн Ллс | Індоли |
| US8846935B2 (en) | 2010-05-07 | 2014-09-30 | Glaxosmithkline Llc | Indazoles |
| US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| US20130310379A1 (en) | 2010-11-19 | 2013-11-21 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CA2819620A1 (en) | 2010-12-03 | 2012-06-21 | Epizyme, Inc. | Modulators of histone methyltransferase, and methods of use thereof |
| ES2951688T3 (es) | 2011-02-28 | 2023-10-24 | Epizyme Inc | Compuestos de heteroarilo biciclico fusionados en 6,5 sustituidos |
| JO3363B1 (ar) | 2011-04-13 | 2019-03-13 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| TWI598336B (zh) | 2011-04-13 | 2017-09-11 | 雅酶股份有限公司 | 經取代之苯化合物 |
| CA2834164A1 (en) | 2011-05-10 | 2012-11-15 | Gilead Sciences, Inc. | Fused benzoxazinones as ion channel modulators |
| CA2850570A1 (en) | 2011-09-30 | 2013-04-04 | Glaxosmithkline Llc | Methods of treating cancer |
| WO2013063417A1 (en) | 2011-10-27 | 2013-05-02 | Memorial Sloan-Kettering Cancer Center | Methyltransferase inhibitors for treating cancer |
| EP2780014A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| EP2780013A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| NZ628762A (en) | 2012-02-10 | 2016-07-29 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
| SG10201912111TA (en) | 2012-04-13 | 2020-02-27 | Epizyme Inc | Combination therapy for treating cancer |
| WO2013173441A2 (en) | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
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-
2020
- 2020-06-03 US US17/615,778 patent/US12252493B2/en active Active
- 2020-06-03 CN CN202080055867.0A patent/CN114269748A/zh active Pending
- 2020-06-03 JP JP2021572409A patent/JP7541538B2/ja active Active
- 2020-06-03 CA CA3142711A patent/CA3142711A1/en not_active Abandoned
- 2020-06-03 WO PCT/US2020/035891 patent/WO2020247475A1/en not_active Ceased
- 2020-06-03 KR KR1020227000118A patent/KR20220027933A/ko not_active Withdrawn
- 2020-06-03 EP EP20747226.7A patent/EP3980422A1/en active Pending
- 2020-06-03 AU AU2020288563A patent/AU2020288563A1/en not_active Abandoned
-
2021
- 2021-11-29 IL IL288529A patent/IL288529A/en unknown
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2025
- 2025-02-05 US US19/045,764 patent/US20250179082A1/en active Pending
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