JP2021502993A5 - - Google Patents
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- JP2021502993A5 JP2021502993A5 JP2020526612A JP2020526612A JP2021502993A5 JP 2021502993 A5 JP2021502993 A5 JP 2021502993A5 JP 2020526612 A JP2020526612 A JP 2020526612A JP 2020526612 A JP2020526612 A JP 2020526612A JP 2021502993 A5 JP2021502993 A5 JP 2021502993A5
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- Prior art keywords
- alkyl
- compound
- compound according
- pharmaceutically acceptable
- carcinoma
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- 150000001875 compounds Chemical class 0.000 claims 44
- -1 dialkylamynylalkyl Chemical group 0.000 claims 31
- 206010028980 Neoplasm Diseases 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 19
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 16
- 201000009030 Carcinoma Diseases 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 15
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 12
- 208000009956 adenocarcinoma Diseases 0.000 claims 11
- 125000004404 heteroalkyl group Chemical group 0.000 claims 11
- 125000001188 haloalkyl group Chemical group 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 206010025323 Lymphomas Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 210000004027 cell Anatomy 0.000 claims 7
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 6
- 229910052805 deuterium Inorganic materials 0.000 claims 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims 6
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- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 239000003085 diluting agent Substances 0.000 claims 5
- 239000003937 drug carrier Substances 0.000 claims 5
- 206010016629 fibroma Diseases 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
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- 125000004043 oxo group Chemical group O=* 0.000 claims 4
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- 201000008808 Fibrosarcoma Diseases 0.000 claims 3
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 210000004379 membrane Anatomy 0.000 claims 3
- 239000012528 membrane Substances 0.000 claims 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 102200006538 rs121913530 Human genes 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 2
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000007054 Medullary Carcinoma Diseases 0.000 claims 2
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- 125000002252 acyl group Chemical group 0.000 claims 2
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
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- 229910052760 oxygen Inorganic materials 0.000 claims 2
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- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000010485 smooth muscle tumor Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- QNRATNLHPGXHMA-XZHTYLCXSA-N (r)-(6-ethoxyquinolin-4-yl)-[(2s,4s,5r)-5-ethyl-1-azabicyclo[2.2.2]octan-2-yl]methanol;hydrochloride Chemical compound Cl.C([C@H]([C@H](C1)CC)C2)CN1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OCC)C=C21 QNRATNLHPGXHMA-XZHTYLCXSA-N 0.000 claims 1
- 125000005962 1,4-oxazepanyl 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
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- 206010073106 Bone giant cell tumour malignant Diseases 0.000 claims 1
- 206010006417 Bronchial carcinoma Diseases 0.000 claims 1
- 235000002566 Capsicum Nutrition 0.000 claims 1
- 240000008574 Capsicum frutescens Species 0.000 claims 1
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- 241000483002 Euproctis similis Species 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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- 235000008331 Pinus X rigitaeda Nutrition 0.000 claims 1
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- 241000018646 Pinus brutia Species 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 235000019892 Stellar Nutrition 0.000 claims 1
- 208000015778 Undifferentiated pleomorphic sarcoma Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 210000000013 bile duct Anatomy 0.000 claims 1
- 201000000053 blastoma Diseases 0.000 claims 1
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- 201000002143 bronchus adenoma Diseases 0.000 claims 1
- 239000001390 capsicum minimum Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 201000005217 chondroblastoma Diseases 0.000 claims 1
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- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims 1
- 235000013399 edible fruits Nutrition 0.000 claims 1
- 201000008184 embryoma Diseases 0.000 claims 1
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000003325 follicular Effects 0.000 claims 1
- 208000015419 gastrin-producing neuroendocrine tumor Diseases 0.000 claims 1
- 201000000052 gastrinoma Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003494 hepatocyte Anatomy 0.000 claims 1
- 230000001096 hypoplastic effect Effects 0.000 claims 1
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- 230000002401 inhibitory effect Effects 0.000 claims 1
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- 206010022498 insulinoma Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
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- 235000013372 meat Nutrition 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000004929 pyrrolidonyl group Chemical group N1(C(CCC1)=O)* 0.000 claims 1
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- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
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- 0 CN1C*CCC1 Chemical compound CN1C*CCC1 0.000 description 4
- AVFZOVWCLRSYKC-UHFFFAOYSA-N CN1CCCC1 Chemical compound CN1CCCC1 AVFZOVWCLRSYKC-UHFFFAOYSA-N 0.000 description 2
- DMTBYMLDOZTFNH-UHFFFAOYSA-N C(C1=CCCC=C1)N1CCCC1 Chemical compound C(C1=CCCC=C1)N1CCCC1 DMTBYMLDOZTFNH-UHFFFAOYSA-N 0.000 description 1
- ZPUPZCHSZPHARG-UHFFFAOYSA-N COc1nc(CN(CC2)c3c4c(Br)cccc4ccn3)c2c(N(CC2)CCN2C(C(F)=C)=O)n1 Chemical compound COc1nc(CN(CC2)c3c4c(Br)cccc4ccn3)c2c(N(CC2)CCN2C(C(F)=C)=O)n1 ZPUPZCHSZPHARG-UHFFFAOYSA-N 0.000 description 1
- ALXGHTGDCLDMSE-SFHVURJKSA-N COc1nc(CN(CC2)c3cccc4ccnc(Cl)c34)c2c(N(CC2)C[C@H](CC#N)N2C(C(F)=C)=O)n1 Chemical compound COc1nc(CN(CC2)c3cccc4ccnc(Cl)c34)c2c(N(CC2)C[C@H](CC#N)N2C(C(F)=C)=O)n1 ALXGHTGDCLDMSE-SFHVURJKSA-N 0.000 description 1
- CDDGNGVFPQRJJM-UHFFFAOYSA-N FC1CNCC1 Chemical compound FC1CNCC1 CDDGNGVFPQRJJM-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762586775P | 2017-11-15 | 2017-11-15 | |
| US62/586,775 | 2017-11-15 | ||
| PCT/US2018/061060 WO2019099524A1 (en) | 2017-11-15 | 2018-11-14 | Kras g12c inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021502993A JP2021502993A (ja) | 2021-02-04 |
| JP2021502993A5 true JP2021502993A5 (enExample) | 2021-12-23 |
| JP7322019B2 JP7322019B2 (ja) | 2023-08-07 |
Family
ID=66431793
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020526612A Active JP7322019B2 (ja) | 2017-11-15 | 2018-11-14 | Ｋｒａｓ ｇ１２ｃ阻害剤 |
| JP2021526287A Active JP7346565B2 (ja) | 2017-11-15 | 2019-05-14 | Ｋｒａｓ ｇ１２ｃ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021526287A Active JP7346565B2 (ja) | 2017-11-15 | 2019-05-14 | Ｋｒａｓ ｇ１２ｃ阻害剤 |
Country Status (34)
Families Citing this family (194)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2017266911B2 (en) * | 2016-05-18 | 2021-09-02 | Array Biopharma, Inc. | KRas G12C inhibitors |
| SI3710439T1 (sl) * | 2017-11-15 | 2023-06-30 | Mirati Therapeutics, Inc., | Zaviralci mutacije kras g12c |
| CA3098574A1 (en) * | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| TW202012415A (zh) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| ES2961253T3 (es) * | 2018-08-31 | 2024-03-11 | Mirati Therapeutics Inc | Inhibidores de KRas G12C |
| CA3111980A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3849538A4 (en) * | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3849536A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| HRP20250059T1 (hr) * | 2018-09-10 | 2025-03-28 | Mirati Therapeutics, Inc. | Kombinirane terapije |
| HRP20250480T1 (hr) | 2018-09-10 | 2025-06-20 | Mirati Therapeutics, Inc | Kombinacija dasatiniba i adagrasiba za primjenu u liječenju nesitnostaničnog raka pluća |
| EP3871673B1 (en) | 2018-10-26 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | Novel indazole compound or salt thereof |
| SI3735299T1 (sl) | 2018-11-09 | 2025-02-28 | F. Hoffmann-La Roche Ag | Kondenzirane obročne spojine |
| EA202190630A1 (ru) * | 2018-12-05 | 2021-10-11 | Мирати Терапьютикс, Инк. | Способы комбинированной терапии |
| WO2020146613A1 (en) | 2019-01-10 | 2020-07-16 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| CN113382774A (zh) * | 2019-02-12 | 2021-09-10 | 诺华股份有限公司 | 包含tno155和krasg12c抑制剂的药物组合 |
| CN113508118B (zh) | 2019-03-05 | 2024-07-19 | 阿斯利康(瑞典)有限公司 | 用作抗癌剂的稠合三环化合物 |
| WO2020238791A1 (zh) * | 2019-05-24 | 2020-12-03 | 江苏恒瑞医药股份有限公司 | 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| WO2020239077A1 (zh) * | 2019-05-29 | 2020-12-03 | 上海翰森生物医药科技有限公司 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN112047939B (zh) * | 2019-06-06 | 2023-05-02 | 江苏先声药业有限公司 | 一种具有抗肿瘤活性的四氢吡啶并嘧啶类化合物 |
| CN112300153B (zh) * | 2019-07-26 | 2023-06-13 | 博瑞生物医药（苏州）股份有限公司 | 一种杂环化合物、药物组合物和用途 |
| JP7756069B6 (ja) * | 2019-08-02 | 2025-11-27 | 上海済▲ユウ▼医薬科技股▲フン▼有限公司 | 四環式化合物、その調製と使用の方法 |
| TWI752580B (zh) * | 2019-08-07 | 2022-01-11 | 大陸商北京加科思新藥研發有限公司 | Kras突變蛋白抑制劑 |
| CN112390788A (zh) * | 2019-08-13 | 2021-02-23 | 苏州闻天医药科技有限公司 | 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途 |
| CN112390797A (zh) * | 2019-08-15 | 2021-02-23 | 微境生物医药科技(上海)有限公司 | 新型螺环类K-Ras G12C抑制剂 |
| WO2021043322A1 (zh) * | 2019-09-06 | 2021-03-11 | 正大天晴药业集团南京顺欣制药有限公司 | 氮杂环庚烷并嘧啶类衍生物及其医药用途 |
| US20220402916A1 (en) | 2019-09-18 | 2022-12-22 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CA3152025A1 (en) * | 2019-09-24 | 2021-04-01 | David BRIERE | Combination therapies |
| TW202115062A (zh) * | 2019-09-25 | 2021-04-16 | 大陸商北京加科思新藥研發有限公司 | Kras突變蛋白抑制劑 |
| JP7395723B2 (ja) | 2019-10-02 | 2023-12-11 | トルレモ・セラピューティクス・アクチェンゲゼルシャフト | 複素環式誘導体、医薬組成物および癌の処置または寛解におけるそれらの使用 |
| US20230257374A1 (en) * | 2019-10-10 | 2023-08-17 | Innovent Biologics (Suzhou) Co., Ltd. | Novel kras g12c protein inhibitor, preparation method therefor, and use thereof |
| CN112694475B (zh) | 2019-10-23 | 2025-09-23 | 苏州泽璟生物制药股份有限公司 | 环烷基类和杂环烷基类抑制剂及其制备方法和应用 |
| US11697657B2 (en) | 2019-10-28 | 2023-07-11 | Merck Sharp & Dohme Llc | Small molecule inhibitors of KRAS G12C mutant |
| KR102894761B1 (ko) * | 2019-10-30 | 2025-12-02 | 젠플리트 테라퓨틱스 (상하이) 아이엔씨. | 치환된 헤테로환형 융합된 환형 화합물, 이의 제조 방법 및 이의 약학적 용도 |
| US11566007B2 (en) | 2019-11-04 | 2023-01-31 | Revolution Medicines, Inc. | Ras inhibitors |
| EP4054720A1 (en) | 2019-11-04 | 2022-09-14 | Revolution Medicines, Inc. | Ras inhibitors |
| CN113286794B (zh) * | 2019-11-04 | 2024-03-12 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| US11608346B2 (en) | 2019-11-04 | 2023-03-21 | Revolution Medicines, Inc. | Ras inhibitors |
| CN112778301A (zh) * | 2019-11-07 | 2021-05-11 | 苏州泽璟生物制药股份有限公司 | 四氢吡啶并嘧啶类抑制剂及其制备方法和应用 |
| CN112824410A (zh) * | 2019-11-21 | 2021-05-21 | 苏州泽璟生物制药股份有限公司 | 氮杂七元环类抑制剂及其制备方法和应用 |
| TW202133855A (zh) | 2019-11-27 | 2021-09-16 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| JP2023505100A (ja) | 2019-11-27 | 2023-02-08 | レボリューション メディシンズ インコーポレイテッド | 共有ｒａｓ阻害剤及びその使用 |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
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