JP2019516718A5 - - Google Patents
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- JP2019516718A5 JP2019516718A5 JP2018560589A JP2018560589A JP2019516718A5 JP 2019516718 A5 JP2019516718 A5 JP 2019516718A5 JP 2018560589 A JP2018560589 A JP 2018560589A JP 2018560589 A JP2018560589 A JP 2018560589A JP 2019516718 A5 JP2019516718 A5 JP 2019516718A5
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- compound according
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- tumor
- carcinoma
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 36
- -1 C 1 -C 3 alkyl Chemical group 0.000 claims 23
- 206010028980 Neoplasm Diseases 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 11
- 201000011510 cancer Diseases 0.000 claims 10
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 208000009956 adenocarcinoma Diseases 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 206010025323 Lymphomas Diseases 0.000 claims 7
- 206010039491 Sarcoma Diseases 0.000 claims 7
- 210000004027 cell Anatomy 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 201000009030 Carcinoma Diseases 0.000 claims 5
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 5
- 206010024612 Lipoma Diseases 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 206010016629 fibroma Diseases 0.000 claims 4
- 201000011066 hemangioma Diseases 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 102200006538 rs121913530 Human genes 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 3
- 201000008808 Fibrosarcoma Diseases 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 3
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 3
- 206010043276 Teratoma Diseases 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
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- 125000005962 1,4-oxazepanyl group Chemical group 0.000 claims 2
- 206010001233 Adenoma benign Diseases 0.000 claims 2
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- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims 2
- 201000004404 Neurofibroma Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 208000002458 carcinoid tumor Diseases 0.000 claims 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000001605 fetal effect Effects 0.000 claims 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 206010027191 meningioma Diseases 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010073106 Bone giant cell tumour malignant Diseases 0.000 claims 1
- 208000009458 Carcinoma in Situ Diseases 0.000 claims 1
- 201000005262 Chondroma Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 201000009047 Chordoma Diseases 0.000 claims 1
- 208000006332 Choriocarcinoma Diseases 0.000 claims 1
- 208000032170 Congenital Abnormalities Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 206010061619 Deformity Diseases 0.000 claims 1
- 208000000471 Dysplastic Nevus Syndrome Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
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- 206010014967 Ependymoma Diseases 0.000 claims 1
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- 208000007569 Giant Cell Tumors Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
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- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 201000010133 Oligodendroglioma Diseases 0.000 claims 1
- 201000009859 Osteochondrosis Diseases 0.000 claims 1
- 206010031299 Osteosis Diseases 0.000 claims 1
- 208000007641 Pinealoma Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 208000000097 Sertoli-Leydig cell tumor Diseases 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 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
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000005873 benzo[d]thiazolyl group Chemical group 0.000 claims 1
- 210000003445 biliary tract Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
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- 208000003362 bronchogenic carcinoma Diseases 0.000 claims 1
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- 229910052799 carbon Inorganic materials 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 210000000845 cartilage Anatomy 0.000 claims 1
- 201000005217 chondroblastoma Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000009060 clear cell adenocarcinoma Diseases 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 239000000835 fiber Substances 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
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- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 201000007487 gallbladder carcinoma Diseases 0.000 claims 1
- 208000015419 gastrin-producing neuroendocrine tumor Diseases 0.000 claims 1
- 201000000052 gastrinoma Diseases 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 208000006359 hepatoblastoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000000284 histiocytoma Diseases 0.000 claims 1
- 201000004933 in situ carcinoma Diseases 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 206010022498 insulinoma Diseases 0.000 claims 1
- 210000002570 interstitial cell Anatomy 0.000 claims 1
- 201000010985 invasive ductal carcinoma Diseases 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000002429 large intestine Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 201000004593 malignant giant cell tumor Diseases 0.000 claims 1
- 201000000289 malignant teratoma Diseases 0.000 claims 1
- 210000002418 meninge Anatomy 0.000 claims 1
- 208000010943 meningeal sarcoma Diseases 0.000 claims 1
- 201000003776 meninges sarcoma Diseases 0.000 claims 1
- 208000010492 mucinous cystadenocarcinoma Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 208000009091 myxoma Diseases 0.000 claims 1
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- 210000000653 nervous system Anatomy 0.000 claims 1
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- 208000004649 neutrophil actin dysfunction Diseases 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
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000004929 pyrrolidonyl group Chemical group N1(C(CCC1)=O)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 206010039667 schwannoma Diseases 0.000 claims 1
- 208000004548 serous cystadenocarcinoma Diseases 0.000 claims 1
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- 210000001550 testis Anatomy 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
- 210000001215 vagina Anatomy 0.000 claims 1
- 208000009540 villous adenoma Diseases 0.000 claims 1
- 210000003905 vulva Anatomy 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662338116P | 2016-05-18 | 2016-05-18 | |
| US62/338,116 | 2016-05-18 | ||
| US201762444614P | 2017-01-10 | 2017-01-10 | |
| US62/444,614 | 2017-01-10 | ||
| PCT/US2017/033099 WO2017201161A1 (en) | 2016-05-18 | 2017-05-17 | Kras g12c inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019516718A JP2019516718A (ja) | 2019-06-20 |
| JP2019516718A5 true JP2019516718A5 (enExample) | 2019-07-25 |
| JP7039489B2 JP7039489B2 (ja) | 2022-03-22 |
Family
ID=60326411
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018560589A Active JP7039489B2 (ja) | 2016-05-18 | 2017-05-17 | Ｋｒａｓ ｇ１２ｃ阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US11267812B2 (enExample) |
| EP (1) | EP3458445B1 (enExample) |
| JP (1) | JP7039489B2 (enExample) |
| KR (1) | KR102444509B1 (enExample) |
| CN (1) | CN109843856B (enExample) |
| AU (1) | AU2017266911B2 (enExample) |
| CA (1) | CA3024523A1 (enExample) |
| ES (1) | ES2863873T3 (enExample) |
| IL (1) | IL262867B (enExample) |
| MX (1) | MX382339B (enExample) |
| SG (1) | SG11201810171SA (enExample) |
| WO (1) | WO2017201161A1 (enExample) |
Families Citing this family (235)
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| ES2863873T3 (es) | 2016-05-18 | 2021-10-11 | Mirati Therapeutics Inc | Inhibidores de KRAS G12C |
| CR20190338A (es) | 2016-12-22 | 2019-09-09 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso |
| UA127968C2 (uk) | 2017-05-22 | 2024-02-28 | Емджен Інк. | Інгібітори g12c kras і способи їх застосування |
| US10640504B2 (en) | 2017-09-08 | 2020-05-05 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| CA3082579A1 (en) | 2017-11-15 | 2019-05-23 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| US10597405B2 (en) | 2017-12-08 | 2020-03-24 | Astrazeneca Ab | Chemical compounds |
| SG10202102462SA (en) * | 2018-01-19 | 2021-04-29 | Medshine Discovery Inc | Pyridone-pyrimidine derivative acting as krasg12c mutein inhibitor |
| TW201942115A (zh) | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物 |
| TW201942116A (zh) * | 2018-02-09 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌劑之四氫喹唑啉衍生物 |
| BR112020020307A2 (pt) * | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| EP3788053B1 (en) | 2018-05-04 | 2024-07-10 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
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| US12208099B2 (en) | 2018-09-10 | 2025-01-28 | Mirati Therapeutics, Inc. | Combination therapies |
| SMT202500028T1 (it) * | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Terapie combinate |
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| AU2019338207B2 (en) * | 2018-09-10 | 2025-01-02 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2020055755A1 (en) * | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| JP7337174B2 (ja) | 2018-09-18 | 2023-09-01 | ニカング セラピューティクス， インコーポレイテッド | Ｓｒｃホモロジー－２ホスファターゼ阻害剤としての三置換ヘテロアリール誘導体 |
| CN114042070A (zh) | 2018-09-30 | 2022-02-15 | 凯瑞康宁生物工程（武汉）有限公司 | 作为神经元组胺受体-3拮抗剂的化合物及其用途 |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
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| CN113874374B (zh) * | 2019-05-24 | 2024-12-27 | 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 |
| CN118745177A (zh) * | 2019-05-29 | 2024-10-08 | 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 |
| WO2021000885A1 (zh) * | 2019-07-01 | 2021-01-07 | 江苏恒瑞医药股份有限公司 | 喹唑啉酮类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| 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 |
| CN112390796B (zh) * | 2019-08-19 | 2023-06-27 | 贝达药业股份有限公司 | Kras g12c抑制剂及其在医药上的应用 |
| CN112430234B (zh) * | 2019-08-26 | 2023-04-28 | 信达生物制药(苏州)有限公司 | 一种新型kras g12c蛋白抑制剂及其制备方法和用途 |
| CN114615981B (zh) | 2019-08-29 | 2024-04-12 | 米拉蒂治疗股份有限公司 | Kras g12d抑制剂 |
| CN114616232B (zh) * | 2019-09-06 | 2026-05-05 | 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 |
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