JPWO2021156178A5 - - Google Patents
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- Publication number
- JPWO2021156178A5 JPWO2021156178A5 JP2022542951A JP2022542951A JPWO2021156178A5 JP WO2021156178 A5 JPWO2021156178 A5 JP WO2021156178A5 JP 2022542951 A JP2022542951 A JP 2022542951A JP 2022542951 A JP2022542951 A JP 2022542951A JP WO2021156178 A5 JPWO2021156178 A5 JP WO2021156178A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- salt
- cancer
- hydrogen
- pharmaceutically acceptable
- 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
- 150000003839 salts Chemical class 0.000 claims description 37
- 150000001875 compounds Chemical class 0.000 claims description 34
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 239000001257 hydrogen Substances 0.000 claims description 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 15
- 150000002367 halogens Chemical class 0.000 claims description 11
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 6
- 229910052801 chlorine Inorganic materials 0.000 claims description 6
- 239000000460 chlorine Substances 0.000 claims description 6
- 229910052731 fluorine Inorganic materials 0.000 claims description 6
- 239000011737 fluorine Substances 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 5
- 239000013543 active substance Substances 0.000 claims description 5
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 4
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 4
- 229910052794 bromium Inorganic materials 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 201000009036 biliary tract cancer Diseases 0.000 claims description 2
- 208000020790 biliary tract neoplasm Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000025402 neoplasm of esophagus Diseases 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000000203 mixture Substances 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20155157.9 | 2020-02-03 | ||
| EP20155157 | 2020-02-03 | ||
| PCT/EP2021/052261 WO2021156178A1 (en) | 2020-02-03 | 2021-02-01 | [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2023512174A JP2023512174A (ja) | 2023-03-24 |
| JPWO2021156178A5 true JPWO2021156178A5 (https=) | 2024-02-08 |
| JP2023512174A5 JP2023512174A5 (https=) | 2024-02-08 |
| JP7626773B2 JP7626773B2 (ja) | 2025-02-04 |
Family
ID=69467424
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022542951A Active JP7626773B2 (ja) | 2020-02-03 | 2021-02-01 | ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230126204A1 (https=) |
| EP (1) | EP4100409B1 (https=) |
| JP (1) | JP7626773B2 (https=) |
| CN (1) | CN115052878B (https=) |
| WO (1) | WO2021156178A1 (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11608343B2 (en) * | 2020-04-24 | 2023-03-21 | Boehringer Ingelheim International Gmbh | Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors |
| TW202214641A (zh) | 2020-06-30 | 2022-04-16 | 美商艾瑞生藥股份有限公司 | Ｈｅｒ２突變抑制劑 |
| EP4323356A1 (en) | 2021-04-13 | 2024-02-21 | Nuvalent, Inc. | Amino-substituted heterocycles for treating cancers with egfr mutations |
| PE20250118A1 (es) | 2021-06-26 | 2025-01-16 | Array Biopharma Inc | Inhibidores de mutacion de her2 |
| WO2023081637A1 (en) | 2021-11-02 | 2023-05-11 | Enliven Therapeutics, Inc. | Fused tetracyclic quinazoline derivatives as inhibitors of erbb2 |
| JP2025509995A (ja) | 2022-03-28 | 2025-04-11 | 江蘇恒瑞医薬股▲ふん▼有限公司 | 含窒素複素環系化合物、その調製方法及びその医薬的使用 |
| WO2023195773A1 (ko) * | 2022-04-05 | 2023-10-12 | 보로노이 주식회사 | 헤테로아릴 유도체 및 이의 용도 |
| CN117384162A (zh) * | 2022-05-17 | 2024-01-12 | 浙江文达医药科技有限公司 | 选择性her2抑制剂 |
| US20240132521A1 (en) | 2022-08-22 | 2024-04-25 | Iambic Therapeutics, Inc. | Compounds and methods for modulating her2 |
| EP4637773A1 (en) | 2022-12-22 | 2025-10-29 | Boehringer Ingelheim International GmbH | Crystalline forms of a her2 inhibitor |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024215809A2 (en) * | 2023-04-11 | 2024-10-17 | Cogent Biosciences, Inc. | Erbb2 inhibitors |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326016A (en) | 2023-07-28 | 2026-03-01 | Boehringer Ingelheim Int | Process for manufacturing a HER2 inhibitor |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| WO2025034912A2 (en) | 2023-08-07 | 2025-02-13 | Cogent Biosciences, Inc. | Compounds for fgfr inhibition |
| CN119320383A (zh) * | 2023-09-05 | 2025-01-17 | 北京鞍石生物科技股份有限公司 | 含氮杂芳基化合物及其制备方法和应用 |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (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 |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (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 |
| WO2026015801A1 (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 |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19608588A1 (de) | 1996-03-06 | 1997-09-11 | Thomae Gmbh Dr K | Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| PL373848A1 (en) | 2001-12-12 | 2005-09-19 | Pfizer Products Inc. | Quinazoline derivatives for the treatment of abnormal cell growth |
| MXPA06005024A (es) | 2003-11-06 | 2006-07-06 | Pfizer Prod Inc | Combinaciones de inhibidor de erbb2 selectivo/anticuerpos anti-erbb en el tratamiento del cancer. |
| ES2364901T3 (es) | 2005-11-15 | 2011-09-16 | Array Biopharma, Inc. | Procesos e intermedios para la preparación de derivados de n4-fenil-quinazolin-4-amina. |
| MX368464B (es) * | 2013-12-05 | 2019-10-02 | Pfizer | Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinil o y pirrolo[2,3-d]piridinilo. |
| EP3143015B1 (en) | 2014-05-13 | 2019-02-20 | ARIAD Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| CN110526912B (zh) | 2014-06-19 | 2023-02-14 | 武田药品工业株式会社 | 用于激酶抑制的杂芳基化合物 |
| JP6863901B2 (ja) | 2015-05-13 | 2021-04-28 | アリアド ファーマシューティカルズ， インコーポレイテッド | キナーゼ阻害のためのヘテロアリール化合物 |
| JP6791979B2 (ja) | 2016-03-01 | 2020-11-25 | シャンハイ ファーマシューティカルズ ホールディング カンパニー，リミティド | 含窒素ヘテロ環化合物、製造方法、中間体、組成物及び応用 |
| CN111032655B (zh) | 2017-08-31 | 2022-09-02 | 达纳-法伯癌症研究所股份有限公司 | Egfr和/或her2抑制剂和使用方法 |
| EP3677583A4 (en) | 2017-09-01 | 2021-07-21 | Shanghai Pharmaceuticals Holding Co., Ltd. | NITROGENOUS HETEROCYCLIC COMPOUND, METHOD OF PREPARATION, INTERMEDIATE, COMPOSITION AND APPLICATION |
| US11608343B2 (en) * | 2020-04-24 | 2023-03-21 | Boehringer Ingelheim International Gmbh | Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors |
| EP4637773A1 (en) * | 2022-12-22 | 2025-10-29 | Boehringer Ingelheim International GmbH | Crystalline forms of a her2 inhibitor |
| AU2023410266A1 (en) * | 2022-12-22 | 2025-06-12 | Boehringer Ingelheim International Gmbh | Solid dispersion of a her2 inhibitor |
-
2021
- 2021-02-01 JP JP2022542951A patent/JP7626773B2/ja active Active
- 2021-02-01 EP EP21702989.1A patent/EP4100409B1/en active Active
- 2021-02-01 WO PCT/EP2021/052261 patent/WO2021156178A1/en not_active Ceased
- 2021-02-01 US US17/759,880 patent/US20230126204A1/en active Pending
- 2021-02-01 CN CN202180012671.8A patent/CN115052878B/zh active Active
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