JP2019518770A5 - - Google Patents
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- JP2019518770A5 JP2019518770A5 JP2018567108A JP2018567108A JP2019518770A5 JP 2019518770 A5 JP2019518770 A5 JP 2019518770A5 JP 2018567108 A JP2018567108 A JP 2018567108A JP 2018567108 A JP2018567108 A JP 2018567108A JP 2019518770 A5 JP2019518770 A5 JP 2019518770A5
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- JP
- Japan
- Prior art keywords
- compound
- salt
- atropisomer
- formula
- pharmaceutical composition
- 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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- 150000001875 compounds Chemical class 0.000 claims 27
- 150000003839 salts Chemical class 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 5
- 230000035772 mutation Effects 0.000 claims 4
- 101001042041 Bos taurus Isocitrate dehydrogenase [NAD] subunit beta, mitochondrial Proteins 0.000 claims 3
- 101000960234 Homo sapiens Isocitrate dehydrogenase [NADP] cytoplasmic Proteins 0.000 claims 3
- 102100039905 Isocitrate dehydrogenase [NADP] cytoplasmic Human genes 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- -1 and independently Inorganic materials 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
- KPGXRSRHYNQIFN-UHFFFAOYSA-N 2-oxoglutaric acid Chemical compound OC(=O)CCC(=O)C(O)=O KPGXRSRHYNQIFN-UHFFFAOYSA-N 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000088 Enchondromatosis Diseases 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 208000026616 Ollier disease Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- XJLXINKUBYWONI-DQQFMEOOSA-N [[(2r,3r,4r,5r)-5-(6-aminopurin-9-yl)-3-hydroxy-4-phosphonooxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [(2s,3r,4s,5s)-5-(3-carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate Chemical compound NC(=O)C1=CC=C[N+]([C@@H]2[C@H]([C@@H](O)[C@H](COP([O-])(=O)OP(O)(=O)OC[C@@H]3[C@H]([C@@H](OP(O)(O)=O)[C@@H](O3)N3C4=NC=NC(N)=C4N=C3)O)O2)O)=C1 XJLXINKUBYWONI-DQQFMEOOSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000006462 myelodysplastic/myeloproliferative neoplasm Diseases 0.000 claims 1
- 229930027945 nicotinamide-adenine dinucleotide Natural products 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
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical compound OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 claims 1
- 102200069708 rs121913499 Human genes 0.000 claims 1
- 102200069690 rs121913500 Human genes 0.000 claims 1
- 208000011580 syndromic disease Diseases 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
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 0 CC(C)=CC(N(C(C(c1nc(C2=CCC(*)=C*=C2)c[s]1)=C1)=O)C2=CC=C*(*)C=C2)=C1C(*)=O Chemical compound CC(C)=CC(N(C(C(c1nc(C2=CCC(*)=C*=C2)c[s]1)=C1)=O)C2=CC=C*(*)C=C2)=C1C(*)=O 0.000 description 1
- MYZVYKPBACOLTA-UHFFFAOYSA-N CCOc(c(N(C(C=C(C)C)=C(C=C1c2nc(-c(cc3)ccc3C#N)c[s]2)C(N2CC(CC3)NC3C2)=O)C1=O)c1)ccc1Cl Chemical compound CCOc(c(N(C(C=C(C)C)=C(C=C1c2nc(-c(cc3)ccc3C#N)c[s]2)C(N2CC(CC3)NC3C2)=O)C1=O)c1)ccc1Cl MYZVYKPBACOLTA-UHFFFAOYSA-N 0.000 description 1
- DVEMFVYDDZQXDK-UHFFFAOYSA-N CCOc(cc1N(C(C=C(C)C)=C(C(N2CC(CC3)NC3C2)O)C=C2c3nc(-c(cc4)ccc4Cl)c[s]3)C2=O)ccc1Cl Chemical compound CCOc(cc1N(C(C=C(C)C)=C(C(N2CC(CC3)NC3C2)O)C=C2c3nc(-c(cc4)ccc4Cl)c[s]3)C2=O)ccc1Cl DVEMFVYDDZQXDK-UHFFFAOYSA-N 0.000 description 1
- ZADFWCZFXVOCTO-UHFFFAOYSA-N CCc(c(N(C(CC(C)C)=C(C=C1c2nc(-c3ccc(C(F)(F)F)nc3)c[s]2)C(N2CCNCC2)=O)C1=O)c1)ccc1Cl Chemical compound CCc(c(N(C(CC(C)C)=C(C=C1c2nc(-c3ccc(C(F)(F)F)nc3)c[s]2)C(N2CCNCC2)=O)C1=O)c1)ccc1Cl ZADFWCZFXVOCTO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662353298P | 2016-06-22 | 2016-06-22 | |
| US62/353,298 | 2016-06-22 | ||
| PCT/US2017/038549 WO2017223202A1 (en) | 2016-06-22 | 2017-06-21 | Thiazole derivatives useful as mutant idh1 inhibitors for treating cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019518770A JP2019518770A (ja) | 2019-07-04 |
| JP2019518770A5 true JP2019518770A5 (enExample) | 2020-07-30 |
| JP6987798B2 JP6987798B2 (ja) | 2022-01-05 |
Family
ID=59276859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018567108A Active JP6987798B2 (ja) | 2016-06-22 | 2017-06-21 | 癌の治療に変異体ｉｄｈ１阻害剤として有用なチアゾール誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10836759B2 (enExample) |
| EP (1) | EP3475276B1 (enExample) |
| JP (1) | JP6987798B2 (enExample) |
| CN (1) | CN109641887B (enExample) |
| AU (1) | AU2017281088B2 (enExample) |
| CA (1) | CA3028999A1 (enExample) |
| ES (1) | ES2880347T3 (enExample) |
| WO (1) | WO2017223202A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2961807A1 (en) | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| EP3201185B1 (en) | 2014-09-19 | 2018-11-21 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| CN111909130B (zh) | 2014-09-19 | 2023-10-31 | 福马治疗股份有限公司 | 作为突变型异柠檬酸脱氢酶抑制剂的吡啶-2(1h)-酮喹啉酮衍生物 |
| AU2015317321B2 (en) | 2014-09-19 | 2020-03-12 | Forma Therapeutics, Inc. | Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors |
| US9624216B2 (en) | 2015-04-21 | 2017-04-18 | Forma Therapeutics, Inc. | Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors |
| WO2016171755A1 (en) | 2015-04-21 | 2016-10-27 | Forma Therapeutics, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| WO2019222551A1 (en) | 2018-05-16 | 2019-11-21 | Forma Therapeutics, Inc. | Solid forms of ((s)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile |
| US11311527B2 (en) | 2018-05-16 | 2022-04-26 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1) |
| US11013733B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1) |
| US11013734B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation |
| WO2019222553A1 (en) | 2018-05-16 | 2019-11-21 | Forma Therapeutics, Inc. | Inhibiting mutant idh-1 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2406389B1 (en) * | 2009-03-13 | 2019-05-08 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| CN102439012A (zh) | 2009-03-24 | 2012-05-02 | 吉里德卡利斯托加公司 | 2-嘌呤基-3-甲苯基-喹唑啉酮衍生物的阻转异构体和使用方法 |
| ES2651132T3 (es) * | 2013-03-14 | 2018-01-24 | Novartis Ag | 3-Pirimidin-4-il-oxazolidin-2-onas como inhibidores de IDH mutante |
| EP3237385B1 (en) * | 2014-12-22 | 2021-11-24 | The United States of America, as represented by The Secretary, Department of Health and Human Services | Mutant idh1 inhibitors useful for treating cancer |
-
2017
- 2017-06-21 JP JP2018567108A patent/JP6987798B2/ja active Active
- 2017-06-21 ES ES17735296T patent/ES2880347T3/es active Active
- 2017-06-21 WO PCT/US2017/038549 patent/WO2017223202A1/en not_active Ceased
- 2017-06-21 US US16/312,206 patent/US10836759B2/en active Active
- 2017-06-21 CA CA3028999A patent/CA3028999A1/en active Pending
- 2017-06-21 CN CN201780051410.0A patent/CN109641887B/zh active Active
- 2017-06-21 EP EP17735296.0A patent/EP3475276B1/en active Active
- 2017-06-21 AU AU2017281088A patent/AU2017281088B2/en active Active