JP2020533280A5 - - Google Patents
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- JP2020533280A5 JP2020533280A5 JP2020510091A JP2020510091A JP2020533280A5 JP 2020533280 A5 JP2020533280 A5 JP 2020533280A5 JP 2020510091 A JP2020510091 A JP 2020510091A JP 2020510091 A JP2020510091 A JP 2020510091A JP 2020533280 A5 JP2020533280 A5 JP 2020533280A5
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- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- pharmaceutically acceptable
- acceptable salt
- compound according
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 27
- 150000003839 salts Chemical class 0.000 claims 25
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 8
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 6
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 230000003081 coactivator Effects 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 102000004169 proteins and genes Human genes 0.000 claims 4
- 108090000623 proteins and genes Proteins 0.000 claims 4
- 238000013518 transcription Methods 0.000 claims 4
- 230000035897 transcription Effects 0.000 claims 4
- 201000009030 Carcinoma Diseases 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 230000004655 Hippo pathway Effects 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 230000003211 malignant effect Effects 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 208000007538 neurilemmoma Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 201000003733 ovarian melanoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 230000002093 peripheral effect Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 206010039667 schwannoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 201000009906 Meningitis Diseases 0.000 claims 1
- 201000008395 adenosquamous carcinoma Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000000762 glandular Effects 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 206010027191 meningioma Diseases 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762548037P | 2017-08-21 | 2017-08-21 | |
| US62/548,037 | 2017-08-21 | ||
| PCT/US2018/047112 WO2019040380A1 (en) | 2017-08-21 | 2018-08-20 | BENZOSULFONYL COMPOUNDS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020533280A JP2020533280A (ja) | 2020-11-19 |
| JP2020533280A5 true JP2020533280A5 (enExample) | 2021-09-30 |
| JP7245229B2 JP7245229B2 (ja) | 2023-03-23 |
Family
ID=65439937
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020510091A Active JP7245229B2 (ja) | 2017-08-21 | 2018-08-20 | ベンゾスルホニル化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11192865B2 (enExample) |
| EP (1) | EP3691623B1 (enExample) |
| JP (1) | JP7245229B2 (enExample) |
| CN (1) | CN111542315B (enExample) |
| AU (1) | AU2018321291A1 (enExample) |
| CA (1) | CA3073543A1 (enExample) |
| WO (1) | WO2019040380A1 (enExample) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018204532A1 (en) | 2017-05-03 | 2018-11-08 | Vivace Therapeutics, Inc. | Non-fused tricyclic compounds |
| EP3691623B1 (en) | 2017-08-21 | 2022-10-05 | Vivace Therapeutics, Inc. | Benzosulfonyl compounds |
| EP3720430A4 (en) | 2017-12-06 | 2021-05-05 | Vivace Therapeutics, Inc. | BENZOCARBONYL COMPOUNDS |
| US11661403B2 (en) | 2018-05-16 | 2023-05-30 | Vivace Therapeutics, Inc. | Oxadiazole compounds |
| CN109912584B (zh) * | 2019-03-22 | 2021-08-13 | 中国药科大学 | 一种具有抗肿瘤活性的brd4蛋白抑制剂及其制备方法和应用 |
| MX2021014443A (es) * | 2019-05-31 | 2022-01-06 | Ikena Oncology Inc | Inhibidores del dominio asociado mejorador de la transcripcion (tead) y usos de los mismos. |
| US11458149B1 (en) * | 2019-05-31 | 2022-10-04 | Ikena Oncology, Inc. | TEAD inhibitors and uses thereof |
| EP4003983A1 (en) | 2019-07-29 | 2022-06-01 | Basilea Pharmaceutica International AG | 1,2,4-oxadiazol-5-one derivatives for the treatment of cancer |
| CN115279368B (zh) * | 2019-11-20 | 2024-05-24 | 维瓦斯治疗公司 | 杂芳基化合物 |
| US20230192607A1 (en) * | 2019-12-24 | 2023-06-22 | Dana-Farber Cancer Institute, Inc. | Transcriptional enhanced associate domain (tead) transcription factor inhibitors and uses thereof |
| CN115515959A (zh) * | 2020-05-08 | 2022-12-23 | 默克专利股份公司 | 用作tead结合剂的三环杂环 |
| CA3180846A1 (en) * | 2020-06-03 | 2021-12-09 | Dana-Farber Cancer Institute, Inc. | Inhibitors of transcriptional enhanced associate domain (tead) and uses thereof |
| US11787775B2 (en) | 2020-07-24 | 2023-10-17 | Genentech, Inc. | Therapeutic compounds and methods of use |
| PE20240017A1 (es) | 2020-09-30 | 2024-01-04 | Univ Leuven Kath | Derivados de 1,2,3,4-tetrahidroquinolina como inhibidores de la activacion de yap/taz-tead para el tratamiento del cancer |
| WO2022120355A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead degraders and uses thereof |
| WO2022120353A1 (en) * | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| AU2022210800A1 (en) | 2021-01-25 | 2023-08-10 | Ikena Oncology, Inc. | Combination of a 3-(imidazol-4-yl)-4-(amino)-benzenesulfonamide tead inhibitor with an egfr inhibitor and/or mek inhibitor for use in the treatment of lung cancer |
| US20240083903A1 (en) * | 2021-02-18 | 2024-03-14 | Merck Sharp & Dohme Llc | Aryl ether compounds as tead modulators |
| WO2022221866A1 (en) | 2021-04-16 | 2022-10-20 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| JP2024519845A (ja) * | 2021-05-19 | 2024-05-21 | ジェネンテック， インコーポレイテッド | 併用療法 |
| WO2022258040A1 (zh) * | 2021-06-11 | 2022-12-15 | 武汉人福创新药物研发中心有限公司 | 用于tead抑制剂的杂环化合物 |
| CN115594680A (zh) * | 2021-07-07 | 2023-01-13 | 武汉人福创新药物研发中心有限公司（Cn） | 一种tead抑制剂 |
| AU2022336415A1 (en) | 2021-09-01 | 2024-01-04 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| US20240279191A1 (en) * | 2021-09-24 | 2024-08-22 | The General Hospital Corporation | Small molecule inhibitors of tead-yap |
| WO2023057371A1 (en) | 2021-10-04 | 2023-04-13 | Basilea Pharmaceutica International Ag, Allschwil | 1,2,4-oxadiazol-5-one derivatives for the treatment of cancer |
| WO2023060227A1 (en) | 2021-10-07 | 2023-04-13 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| AU2022417524A1 (en) | 2021-12-23 | 2024-08-01 | Katholieke Universiteit Leuven | 2-pyrazole anilines and related analogs for inhibiting yap/taz-tead |
| WO2023116877A1 (zh) * | 2021-12-24 | 2023-06-29 | 武汉人福创新药物研发中心有限公司 | 作为tead抑制剂的杂环化合物 |
| CN118715221A (zh) * | 2022-01-30 | 2024-09-27 | 希格生科（深圳）有限公司 | 三环化合物及其应用 |
| WO2023173053A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| WO2023173057A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| WO2023204822A1 (en) * | 2022-04-22 | 2023-10-26 | Vivace Therapeutics, Inc. | Phenyl phosphine oxide compounds and methods of use thereof |
| CN119768393A (zh) | 2022-05-25 | 2025-04-04 | 医肯纳肿瘤学公司 | Mek抑制剂和其用途 |
| WO2024061366A1 (zh) * | 2022-09-23 | 2024-03-28 | 杭州天玑济世生物科技有限公司 | 具有磷酰化芳基结构的小分子化合物及其应用 |
| TW202423428A (zh) | 2022-09-29 | 2024-06-16 | 香港商英矽智能科技知識產權有限公司 | Tead抑制劑及其使用方法 |
| CN120019051A (zh) | 2022-10-13 | 2025-05-16 | 韩美药品株式会社 | 用于抑制yap-tead交互作用的新颖杂双环化合物及包含其的药学组成物 |
| TW202417429A (zh) * | 2022-10-13 | 2024-05-01 | 南韓商韓美藥品股份有限公司 | 用於抑制yap-tead交互作用的新穎雜雙環化合物及包含其之藥學組成物 |
| WO2024092116A1 (en) | 2022-10-26 | 2024-05-02 | Ikena Oncology, Inc. | Combination of tead inhibitors and egfr inhibitors and uses thereof |
| EP4596561A1 (en) | 2022-10-27 | 2025-08-06 | Suzhou Genhouse Bio Co., Ltd. | Phosphorus-containing compound, pharmaceutical composition and use thereof |
| WO2024099435A1 (zh) * | 2022-11-10 | 2024-05-16 | 武汉人福创新药物研发中心有限公司 | Tead抑制剂 |
| AU2023380159A1 (en) | 2022-11-18 | 2025-05-15 | Novartis Ag | Pharmaceutical combinations and uses thereof |
| WO2024173761A1 (en) | 2023-02-17 | 2024-08-22 | Ikena Oncology, Inc. | Combinations comprising mek inhibitors for use in the treatment of cancer |
| EP4669320A1 (en) | 2023-02-23 | 2025-12-31 | Novartis AG | COMBINATIONS OF TEAD AND KRAS G12D INHIBITORS FOR CANCER TREATMENT |
| CN120676942A (zh) | 2023-02-23 | 2025-09-19 | 诺华股份有限公司 | 用于治疗癌症的tead抑制剂和her2抑制剂组合 |
| KR20250097400A (ko) | 2023-12-21 | 2025-06-30 | 한미약품 주식회사 | Yap-tead 상호작용 억제를 위한 신규한 헤테로비시클릭 화합물 및 이를 포함하는 약학적 조성물 |
| WO2025215527A2 (en) | 2024-04-10 | 2025-10-16 | Novartis Ag | Pharmaceutical combinations and uses thereof |
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| US3895027A (en) | 1974-04-12 | 1975-07-15 | Lilly Co Eli | Process for preparing pyrazole-3-carboxylic acids |
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| DE2917997A1 (de) * | 1979-05-04 | 1980-11-20 | Hoechst Ag | Substituierte pyrrolidinyl-benzoesaeure- derivate und verfahren zu ihrer herstellung |
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| US8097650B2 (en) | 2005-07-27 | 2012-01-17 | The Trustees Of Columbia University In The City Of New York | Method of treating a condition associated with phosphorylation of TASK-1 |
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| EP2858635A1 (en) | 2012-06-11 | 2015-04-15 | The Regents of The University of California | Inhibitors of hippo-yap signaling pathway |
| JP6215315B2 (ja) * | 2012-06-12 | 2017-10-18 | アッヴィ・インコーポレイテッド | ピリジノンおよびピリダジノン誘導体 |
| EA201590549A1 (ru) * | 2012-09-13 | 2015-08-31 | Зе Боард Оф Трастиз Оф Зе Лилэнд Стенфорд Джуниор Юниверсити | Стимуляция развития овариального фолликула и созревания ооцита |
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| EP3156404A1 (en) * | 2015-10-15 | 2017-04-19 | Inventiva | New compounds inhibitors of the yap/taz-tead interaction and their use in the treatment of malignant mesothelioma |
| WO2018204532A1 (en) | 2017-05-03 | 2018-11-08 | Vivace Therapeutics, Inc. | Non-fused tricyclic compounds |
| EP3691623B1 (en) | 2017-08-21 | 2022-10-05 | Vivace Therapeutics, Inc. | Benzosulfonyl compounds |
| EP3720430A4 (en) | 2017-12-06 | 2021-05-05 | Vivace Therapeutics, Inc. | BENZOCARBONYL COMPOUNDS |
| US11661403B2 (en) | 2018-05-16 | 2023-05-30 | Vivace Therapeutics, Inc. | Oxadiazole compounds |
-
2018
- 2018-08-20 EP EP18848395.2A patent/EP3691623B1/en active Active
- 2018-08-20 CN CN201880068676.0A patent/CN111542315B/zh active Active
- 2018-08-20 CA CA3073543A patent/CA3073543A1/en not_active Abandoned
- 2018-08-20 JP JP2020510091A patent/JP7245229B2/ja active Active
- 2018-08-20 WO PCT/US2018/047112 patent/WO2019040380A1/en not_active Ceased
- 2018-08-20 AU AU2018321291A patent/AU2018321291A1/en not_active Abandoned
- 2018-08-20 US US16/640,557 patent/US11192865B2/en active Active
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