JP2020517598A5 - - Google Patents
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- Publication number
- JP2020517598A5 JP2020517598A5 JP2019555918A JP2019555918A JP2020517598A5 JP 2020517598 A5 JP2020517598 A5 JP 2020517598A5 JP 2019555918 A JP2019555918 A JP 2019555918A JP 2019555918 A JP2019555918 A JP 2019555918A JP 2020517598 A5 JP2020517598 A5 JP 2020517598A5
- Authority
- JP
- Japan
- Prior art keywords
- isoindole
- methoxyphenyl
- dihydro
- oxo
- fluoro
- 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
Links
- -1 oxan-4-yl Chemical group 0.000 claims 34
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 22
- 230000002265 prevention Effects 0.000 claims 16
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 15
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 13
- 206010028980 Neoplasm Diseases 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 206010009944 Colon cancer Diseases 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 5
- 238000000634 powder X-ray diffraction Methods 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide Chemical compound CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims 4
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 4
- 206010025323 Lymphomas Diseases 0.000 claims 4
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical group CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 4
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 4
- 239000007900 aqueous suspension Substances 0.000 claims 4
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 4
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 4
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 4
- 230000003211 malignant effect Effects 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 208000019838 Blood disease Diseases 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- 208000014951 hematologic disease Diseases 0.000 claims 3
- 208000018706 hematopoietic system disease Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 2
- 101150073096 NRAS gene Proteins 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 150000004668 long chain fatty acids Chemical class 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000002071 myeloproliferative effect Effects 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 239000002245 particle Substances 0.000 claims 2
- 150000003512 tertiary amines Chemical class 0.000 claims 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 2
- QKRMFCXDTFLKKT-UHFFFAOYSA-N 2-hydroxyethanesulfonic acid Chemical compound OCCS(O)(=O)=O.OCCS(O)(=O)=O QKRMFCXDTFLKKT-UHFFFAOYSA-N 0.000 claims 1
- 229940080296 2-naphthalenesulfonate Drugs 0.000 claims 1
- GIZKBEAJKWOWLS-UHFFFAOYSA-N 6-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]-2,3-dihydroisoindol-1-one Chemical compound ClC=1C(=NC(=NC=1)NC1CCOCC1)C1=CC=C2CNC(C2=C1)=O GIZKBEAJKWOWLS-UHFFFAOYSA-N 0.000 claims 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims 1
- 206010014950 Eosinophilia Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 239000007821 HATU Substances 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 102000019149 MAP kinase activity proteins Human genes 0.000 claims 1
- 108040008097 MAP kinase activity proteins Proteins 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- LKJPYSCBVHEWIU-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide Chemical compound C=1C=C(C#N)C(C(F)(F)F)=CC=1NC(=O)C(O)(C)CS(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-UHFFFAOYSA-N 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 239000004721 Polyphenylene oxide Substances 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000389 T-cell leukemia Diseases 0.000 claims 1
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 239000000010 aprotic solvent Substances 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 1
- 229940077388 benzenesulfonate Drugs 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 1
- 229950004221 besilate Drugs 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 210000002798 bone marrow cell Anatomy 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 238000007323 disproportionation reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 210000002308 embryonic cell Anatomy 0.000 claims 1
- 201000011523 endocrine gland cancer Diseases 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- AFAXGSQYZLGZPG-UHFFFAOYSA-L ethane-1,2-disulfonate Chemical compound [O-]S(=O)(=O)CCS([O-])(=O)=O AFAXGSQYZLGZPG-UHFFFAOYSA-L 0.000 claims 1
- 230000001605 fetal effect Effects 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 230000000527 lymphocytic effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 claims 1
- KVBGVZZKJNLNJU-UHFFFAOYSA-M naphthalene-2-sulfonate Chemical compound C1=CC=CC2=CC(S(=O)(=O)[O-])=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-M 0.000 claims 1
- 229950006327 napsilate Drugs 0.000 claims 1
- 239000002736 nonionic surfactant Substances 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 201000005528 peripheral nervous system neoplasm Diseases 0.000 claims 1
- 229920000570 polyether Polymers 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 208000012201 sexual and gender identity disease Diseases 0.000 claims 1
- 208000015891 sexual disease Diseases 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000002411 thermogravimetry Methods 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 125000005500 uronium group Chemical group 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
- NAZAQFAQNOECEK-SECBINFHSA-N COc1cc(F)cc([C@@H](CO)N)c1 Chemical compound COc1cc(F)cc([C@@H](CO)N)c1 NAZAQFAQNOECEK-SECBINFHSA-N 0.000 description 2
- QAPPIHUULOISOQ-LLVKDONJSA-N C[C@H](C(O)=O)N(Cc(cc1)c2cc1-c(nc(NC1CCOCC1)nc1)c1Cl)C2=O Chemical compound C[C@H](C(O)=O)N(Cc(cc1)c2cc1-c(nc(NC1CCOCC1)nc1)c1Cl)C2=O QAPPIHUULOISOQ-LLVKDONJSA-N 0.000 description 1
- DEXRGKNMLMWKQQ-SSDOTTSWSA-N C[C@H](C(O)=O)N(Cc(cc1)c2cc1-c(nc(nc1)Cl)c1Cl)C2=O Chemical compound C[C@H](C(O)=O)N(Cc(cc1)c2cc1-c(nc(nc1)Cl)c1Cl)C2=O DEXRGKNMLMWKQQ-SSDOTTSWSA-N 0.000 description 1
- 0 C[C@](*(O)=O)N(Cc(cc1)c2cc1-c(nc(NC1CCOCC1)nc1)c1Cl)C2=O Chemical compound C[C@](*(O)=O)N(Cc(cc1)c2cc1-c(nc(NC1CCOCC1)nc1)c1Cl)C2=O 0.000 description 1
- AHVQYHFYQWKUKB-UHFFFAOYSA-N NC1CCOCC1 Chemical compound NC1CCOCC1 AHVQYHFYQWKUKB-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1706327.2A GB201706327D0 (en) | 2017-04-20 | 2017-04-20 | A pharmaceutical compound |
| GB1706327.2 | 2017-04-20 | ||
| PCT/IB2018/052745 WO2018193410A1 (en) | 2017-04-20 | 2018-04-20 | 6-pyrimidin-isoindole derivative as erk1/2 inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020517598A JP2020517598A (ja) | 2020-06-18 |
| JP2020517598A5 true JP2020517598A5 (https=) | 2021-05-27 |
| JP7113846B2 JP7113846B2 (ja) | 2022-08-05 |
Family
ID=58795788
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019555918A Active JP7113846B2 (ja) | 2017-04-20 | 2018-04-20 | Ｅｒｋ１／２阻害剤としての６－ピリミジン－イソインドール誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US11142518B2 (https=) |
| EP (1) | EP3612524B1 (https=) |
| JP (1) | JP7113846B2 (https=) |
| KR (1) | KR102652193B1 (https=) |
| CN (1) | CN110831939B (https=) |
| AU (1) | AU2018255935B2 (https=) |
| CA (1) | CA3059674A1 (https=) |
| DK (1) | DK3612524T3 (https=) |
| ES (1) | ES2994283T3 (https=) |
| FI (1) | FI3612524T3 (https=) |
| GB (1) | GB201706327D0 (https=) |
| IL (1) | IL269803B (https=) |
| MA (1) | MA52123A (https=) |
| MX (1) | MX2019012471A (https=) |
| MY (1) | MY203722A (https=) |
| PH (1) | PH12019502154A1 (https=) |
| SA (1) | SA519410253B1 (https=) |
| SG (1) | SG11201909189QA (https=) |
| TW (1) | TWI813566B (https=) |
| WO (1) | WO2018193410A1 (https=) |
| ZA (1) | ZA201907484B (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3365334B1 (en) | 2015-10-21 | 2024-07-17 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| NZ766835A (en) | 2018-03-02 | 2023-09-29 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| JP7174143B2 (ja) | 2018-07-24 | 2022-11-17 | 大鵬薬品工業株式会社 | Ｓｈｐ２活性を阻害するヘテロ二環性化合物 |
| CN109608444B (zh) * | 2018-11-27 | 2022-02-11 | 中国药科大学 | 含异吲哚啉酮的erk抑制剂及其制备方法与用途 |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| EP4093406A4 (en) * | 2020-01-24 | 2024-02-28 | Taiho Pharmaceutical Co., Ltd. | IMPROVEMENT OF THE ANTI-TUMORAL ACTIVITY OF SHP2 INHIBITOR PYRIMIDINONE IN COMBINATION WITH NEW ANTI-CANCER DRUGS AGAINST CANCER |
| WO2021218912A1 (zh) * | 2020-04-30 | 2021-11-04 | 南京明德新药研发有限公司 | 含苯基并内磺酰胺的化合物 |
| CN113967198A (zh) * | 2020-07-24 | 2022-01-25 | 鲁南制药集团股份有限公司 | 一种甾体cyp17抑制剂胶囊及其制备方法 |
| CA3190001A1 (en) * | 2020-08-21 | 2022-02-24 | Shanghai Ringene Biopharma Co., Ltd. | Aromatic ring-lactam compound, preparation method therefor and use thereof |
| US20240287051A1 (en) * | 2021-06-11 | 2024-08-29 | Otsuka Pharmaceutical Co., Ltd. | Process for preparing an erk inhibitor |
| WO2023059885A1 (en) * | 2021-10-08 | 2023-04-13 | Slayback Pharma Llc, | Stable pharmaceutical compositions of cyclophosphamide |
| US20240415835A1 (en) * | 2021-10-26 | 2024-12-19 | Otsuka Pharmaceutical Co., Ltd. | Compositions comprising an erk inhibitor |
| CN114085213B (zh) * | 2022-01-20 | 2022-03-25 | 苏州国匡医药科技有限公司 | 一种arv-471的制备方法 |
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