JPWO2020201991A5 - - Google Patents
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- JPWO2020201991A5 JPWO2020201991A5 JP2021558566A JP2021558566A JPWO2020201991A5 JP WO2020201991 A5 JPWO2020201991 A5 JP WO2020201991A5 JP 2021558566 A JP2021558566 A JP 2021558566A JP 2021558566 A JP2021558566 A JP 2021558566A JP WO2020201991 A5 JPWO2020201991 A5 JP WO2020201991A5
- Authority
- JP
- Japan
- Prior art keywords
- pyridin
- pharmaceutical composition
- group
- tautomer
- halogen
- 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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- -1 2 -amino-3-chloropyridin-4-yl Chemical group 0.000 claims 30
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 230000003463 hyperproliferative effect Effects 0.000 claims 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 11
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 239000001301 oxygen Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 8
- 239000002246 antineoplastic agent Substances 0.000 claims 8
- 229940127089 cytotoxic agent Drugs 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 8
- 229910052717 sulfur Chemical group 0.000 claims 8
- 239000011593 sulfur Chemical group 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 229950003054 binimetinib Drugs 0.000 claims 2
- ACWZRVQXLIRSDF-UHFFFAOYSA-N binimetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1F ACWZRVQXLIRSDF-UHFFFAOYSA-N 0.000 claims 2
- 229950001969 encorafenib Drugs 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- CMJCXYNUCSMDBY-ZDUSSCGKSA-N lgx818 Chemical compound COC(=O)N[C@@H](C)CNC1=NC=CC(C=2C(=NN(C=2)C(C)C)C=2C(=C(NS(C)(=O)=O)C=C(Cl)C=2)F)=N1 CMJCXYNUCSMDBY-ZDUSSCGKSA-N 0.000 claims 2
- 229950001290 lorlatinib Drugs 0.000 claims 2
- IIXWYSCJSQVBQM-LLVKDONJSA-N lorlatinib Chemical compound N=1N(C)C(C#N)=C2C=1CN(C)C(=O)C1=CC=C(F)C=C1[C@@H](C)OC1=CC2=CN=C1N IIXWYSCJSQVBQM-LLVKDONJSA-N 0.000 claims 2
- 210000004214 philadelphia chromosome Anatomy 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- AILRADAXUVEEIR-UHFFFAOYSA-N 5-chloro-4-n-(2-dimethylphosphorylphenyl)-2-n-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidine-2,4-diamine Chemical compound COC1=CC(N2CCC(CC2)N2CCN(C)CC2)=CC=C1NC(N=1)=NC=C(Cl)C=1NC1=CC=CC=C1P(C)(C)=O AILRADAXUVEEIR-UHFFFAOYSA-N 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000001446 Anaplastic Thyroid Carcinoma Diseases 0.000 claims 1
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 1
- 239000002146 L01XE16 - Crizotinib Substances 0.000 claims 1
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000009905 Neurofibromatoses Diseases 0.000 claims 1
- 206010029748 Noonan syndrome Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 1
- 229960001611 alectinib Drugs 0.000 claims 1
- KDGFLJKFZUIJMX-UHFFFAOYSA-N alectinib Chemical compound CCC1=CC=2C(=O)C(C3=CC=C(C=C3N3)C#N)=C3C(C)(C)C=2C=C1N(CC1)CCC1N1CCOCC1 KDGFLJKFZUIJMX-UHFFFAOYSA-N 0.000 claims 1
- 229950004272 brigatinib Drugs 0.000 claims 1
- 208000035269 cancer or benign tumor Diseases 0.000 claims 1
- 229960001602 ceritinib Drugs 0.000 claims 1
- VERWOWGGCGHDQE-UHFFFAOYSA-N ceritinib Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1C1CCNCC1 VERWOWGGCGHDQE-UHFFFAOYSA-N 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 229960002271 cobimetinib Drugs 0.000 claims 1
- RESIMIUSNACMNW-BXRWSSRYSA-N cobimetinib fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F RESIMIUSNACMNW-BXRWSSRYSA-N 0.000 claims 1
- 229960005061 crizotinib Drugs 0.000 claims 1
- KTEIFNKAUNYNJU-GFCCVEGCSA-N crizotinib Chemical compound O([C@H](C)C=1C(=C(F)C=CC=1Cl)Cl)C(C(=NC=1)N)=CC=1C(=C1)C=NN1C1CCNCC1 KTEIFNKAUNYNJU-GFCCVEGCSA-N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 229960002465 dabrafenib Drugs 0.000 claims 1
- BFSMGDJOXZAERB-UHFFFAOYSA-N dabrafenib Chemical compound S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 BFSMGDJOXZAERB-UHFFFAOYSA-N 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 210000002165 glioblast Anatomy 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 1
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 201000004931 neurofibromatosis Diseases 0.000 claims 1
- 208000037244 polycythemia vera Diseases 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 229950010746 selumetinib Drugs 0.000 claims 1
- CYOHGALHFOKKQC-UHFFFAOYSA-N selumetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1Cl CYOHGALHFOKKQC-UHFFFAOYSA-N 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 201000008440 thyroid gland anaplastic carcinoma Diseases 0.000 claims 1
- 208000019179 thyroid gland undifferentiated (anaplastic) carcinoma Diseases 0.000 claims 1
- 229960004066 trametinib Drugs 0.000 claims 1
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical compound CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 claims 1
- 229960003862 vemurafenib Drugs 0.000 claims 1
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023049681A JP2023078421A (ja) | 2019-04-02 | 2023-03-27 | タンパク質チロシンホスファターゼ阻害剤 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962828356P | 2019-04-02 | 2019-04-02 | |
| US62/828,356 | 2019-04-02 | ||
| US202062992558P | 2020-03-20 | 2020-03-20 | |
| US62/992,558 | 2020-03-20 | ||
| PCT/IB2020/053019 WO2020201991A1 (en) | 2019-04-02 | 2020-03-30 | Protein tyrosine phosphatase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023049681A Division JP2023078421A (ja) | 2019-04-02 | 2023-03-27 | タンパク質チロシンホスファターゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022527796A JP2022527796A (ja) | 2022-06-06 |
| JPWO2020201991A5 true JPWO2020201991A5 (enExample) | 2022-09-02 |
| JP7284830B2 JP7284830B2 (ja) | 2023-05-31 |
Family
ID=70277430
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021558566A Active JP7284830B2 (ja) | 2019-04-02 | 2020-03-30 | タンパク質チロシンホスファターゼ阻害剤 |
| JP2023049681A Pending JP2023078421A (ja) | 2019-04-02 | 2023-03-27 | タンパク質チロシンホスファターゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023049681A Pending JP2023078421A (ja) | 2019-04-02 | 2023-03-27 | タンパク質チロシンホスファターゼ阻害剤 |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US11634417B2 (enExample) |
| EP (1) | EP3947367A1 (enExample) |
| JP (2) | JP7284830B2 (enExample) |
| KR (1) | KR102698608B1 (enExample) |
| CN (1) | CN113874363B (enExample) |
| AU (1) | AU2020251841B2 (enExample) |
| BR (1) | BR112021018664A2 (enExample) |
| CA (1) | CA3135555C (enExample) |
| CL (2) | CL2021002542A1 (enExample) |
| CO (1) | CO2021013030A2 (enExample) |
| CR (1) | CR20210501A (enExample) |
| CU (1) | CU20210080A7 (enExample) |
| DO (1) | DOP2021000206A (enExample) |
| EC (1) | ECSP21072994A (enExample) |
| GE (2) | GEP20237561B (enExample) |
| IL (2) | IL320682A (enExample) |
| MA (1) | MA55511A (enExample) |
| MX (1) | MX2021012122A (enExample) |
| PE (1) | PE20220141A1 (enExample) |
| PH (1) | PH12021552227A1 (enExample) |
| PY (1) | PY2018672A (enExample) |
| SG (1) | SG11202110502PA (enExample) |
| TW (1) | TWI766261B (enExample) |
| UY (1) | UY38628A (enExample) |
| WO (1) | WO2020201991A1 (enExample) |
| ZA (1) | ZA202108443B (enExample) |
Families Citing this family (42)
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| US11179397B2 (en) | 2018-10-03 | 2021-11-23 | Gilead Sciences, Inc. | Imidazopyrimidine derivatives |
| MA53921A (fr) | 2018-10-17 | 2022-01-26 | Array Biopharma Inc | Inhibiteurs de protéine tyrosine phosphatase |
| BR112021018664A2 (pt) * | 2019-04-02 | 2021-11-23 | Array Biopharma Inc | Inibidores de proteína tirosina fosfatase |
| CA3183032A1 (en) | 2020-06-18 | 2021-12-23 | Mallika Singh | Methods for delaying, preventing, and treating acquired resistance to ras inhibitors |
| MX2023002248A (es) | 2020-09-03 | 2023-05-16 | Revolution Medicines Inc | Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2. |
| CR20230165A (es) | 2020-09-15 | 2023-06-02 | Revolution Medicines Inc | Derivados indólicos como inhibidores de ras en el tratamiento del cáncer |
| KR20230147159A (ko) * | 2021-03-23 | 2023-10-20 | 상하이 하이옌 파마슈티컬 테크놀로지 컴퍼니, 리미티드 | 헤테로고리로 치환된 메탄온계 유도체, 이의 조성물 및 의약적 용도 |
| CN117083285A (zh) * | 2021-03-31 | 2023-11-17 | 南京明德新药研发有限公司 | 一系列含Se的吡嗪类化合物及其应用 |
| TWI825637B (zh) | 2021-03-31 | 2023-12-11 | 美商輝瑞股份有限公司 | 啶－１，６（２ｈ，７ｈ）－二酮 |
| KR20230165309A (ko) * | 2021-04-01 | 2023-12-05 | 어레이 바이오파마 인크. | Shp2 억제제의 결정질 형태 |
| CN117460725A (zh) * | 2021-04-01 | 2024-01-26 | 阵列生物制药公司 | Shp2抑制剂的晶型 |
| IL308193A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| CR20230558A (es) | 2021-05-05 | 2024-01-24 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cáncer |
| TW202244049A (zh) * | 2021-05-12 | 2022-11-16 | 大陸商藥雅科技（上海）有限公司 | Shp2磷酸酶抑制劑的製備及其應用 |
| CN115960109B (zh) * | 2021-05-31 | 2024-06-25 | 药雅科技(上海)有限公司 | 稠环类shp2磷酸酶抑制剂的制备及其应用 |
| IL309984A (en) | 2021-07-09 | 2024-03-01 | Kanaph Therapeutics Inc | Shp2 inhibitor and use thereof |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| WO2023061263A1 (zh) * | 2021-10-14 | 2023-04-20 | 北京泰德制药股份有限公司 | Shp2抑制剂、包含其的药物组合物及其用途 |
| CN119136806A (zh) | 2022-03-08 | 2024-12-13 | 锐新医药公司 | 用于治疗免疫难治性肺癌的方法 |
| CA3256136A1 (en) * | 2022-03-23 | 2023-09-28 | Array Biopharma Inc. | CRYSTALLINE SALT FORM OF AN SHP2 INHIBITOR |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CN115177622B (zh) * | 2022-07-19 | 2024-09-17 | 中南大学湘雅二医院 | 多个化合物在制备治疗骨髓增殖性肿瘤的药物中的应用 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| PE20260039A1 (es) | 2023-04-07 | 2026-01-09 | Revolution Medicines Inc | Inhibidores macrociclicos de ras |
| TW202448897A (zh) | 2023-04-14 | 2024-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑之結晶形式、含有其之組合物及其使用方法 |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| WO2024218632A1 (en) | 2023-04-17 | 2024-10-24 | Array Biopharma Inc. | Erk protein kinase inhibitors |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025006753A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
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