JPWO2022140456A5 - - Google Patents
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- Publication number
- JPWO2022140456A5 JPWO2022140456A5 JP2023539379A JP2023539379A JPWO2022140456A5 JP WO2022140456 A5 JPWO2022140456 A5 JP WO2022140456A5 JP 2023539379 A JP2023539379 A JP 2023539379A JP 2023539379 A JP2023539379 A JP 2023539379A JP WO2022140456 A5 JPWO2022140456 A5 JP WO2022140456A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- cancer
- salt
- halo
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 17
- 125000001475 halogen functional group Chemical group 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- -1 hetercycloalkyl Chemical group 0.000 claims 5
- 201000010536 head and neck cancer Diseases 0.000 claims 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 108091007960 PI3Ks Proteins 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 230000000155 isotopic effect Effects 0.000 claims 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 241000282412 Homo Species 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 201000003911 head and neck carcinoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000002349 hydroxyamino group Chemical group [H]ON([H])[*] 0.000 claims 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000005412 pyrazyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063129368P | 2020-12-22 | 2020-12-22 | |
| US63/129,368 | 2020-12-22 | ||
| PCT/US2021/064709 WO2022140456A1 (en) | 2020-12-22 | 2021-12-21 | Substituted aminobenzyl heteroaryl compounds as egfr and/or pi3k inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2024501995A JP2024501995A (ja) | 2024-01-17 |
| JP2024501995A5 JP2024501995A5 (https=) | 2024-12-27 |
| JPWO2022140456A5 true JPWO2022140456A5 (https=) | 2024-12-27 |
Family
ID=79730547
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023539379A Pending JP2024501995A (ja) | 2020-12-22 | 2021-12-21 | Ｅｇｆｒ及び／又はｐｉ３ｋ阻害剤としての置換アミノベンジルヘテロアリール化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US20240239764A1 (https=) |
| EP (1) | EP4267554A1 (https=) |
| JP (1) | JP2024501995A (https=) |
| KR (1) | KR20230155422A (https=) |
| CN (1) | CN117295716A (https=) |
| AU (1) | AU2021410726A1 (https=) |
| CA (1) | CA3206168A1 (https=) |
| IL (1) | IL303965A (https=) |
| MX (1) | MX2023007550A (https=) |
| WO (1) | WO2022140456A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023078401A1 (en) * | 2021-11-05 | 2023-05-11 | Fochon Biosciences, Ltd. | Compounds as protein kinase inhibitors |
| CN117024404A (zh) * | 2022-05-10 | 2023-11-10 | 四川汇宇制药股份有限公司 | 苯并吡啶衍生物及其用途 |
| WO2025101914A1 (en) * | 2023-11-10 | 2025-05-15 | Mekanistic Therapeutics Llc | Substituted aminobenzyl heteroaryl compounds as egfr and/or pi3k inhibitors having improved therapeutic index against solid tumors |
Family Cites Families (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3989816A (en) | 1975-06-19 | 1976-11-02 | Nelson Research & Development Company | Vehicle composition containing 1-substituted azacycloheptan-2-ones |
| JPS567710A (en) | 1979-06-28 | 1981-01-27 | Sansho Seiyaku Kk | Whitening cosmetic |
| US4444762A (en) | 1980-04-04 | 1984-04-24 | Nelson Research & Development Company | Vehicle composition containing 1-substituted azacyclopentan-2-ones |
| DE3583799D1 (de) | 1985-01-11 | 1991-09-19 | Abbott Lab Ltd | Feste zubereitung mit langsamer freisetzung. |
| JP2773959B2 (ja) | 1990-07-10 | 1998-07-09 | 信越化学工業株式会社 | 大腸内放出性固形製剤 |
| US6605712B1 (en) | 1990-12-20 | 2003-08-12 | Arch Development Corporation | Gene transcription and ionizing radiation: methods and compositions |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| ID19609A (id) | 1996-07-13 | 1998-07-23 | Glaxo Group Ltd | Senyawa-senyawa heterosiklik |
| US6225318B1 (en) | 1996-10-17 | 2001-05-01 | Pfizer Inc | 4-aminoquinazolone derivatives |
| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| UA73092C2 (uk) | 1998-07-17 | 2005-06-15 | Брістол-Майерс Сквібб Компані | Таблетка з ентеросолюбільним покриттям і спосіб її приготування |
| DE69924735T2 (de) | 1998-07-28 | 2006-01-19 | Tanabe Seiyaku Co., Ltd. | Zur wirkstoffabgabe an zielorten im darm fähige zubereitung |
| JP3270834B2 (ja) | 1999-01-27 | 2002-04-02 | ファイザー・プロダクツ・インク | 抗がん剤として有用なヘテロ芳香族二環式誘導体 |
| AR035851A1 (es) | 2000-03-28 | 2004-07-21 | Wyeth Corp | 3-cianoquinolinas, 3-ciano-1,6-naftiridinas y 3-ciano-1,7-naftiridinas como inhibidoras de proteina quinasas |
| US6521618B2 (en) | 2000-03-28 | 2003-02-18 | Wyeth | 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors |
| ES2201899B1 (es) | 2002-04-01 | 2005-06-01 | Almirall Prodesfarma, S.A. | Derivados de la azaindolilpiperidina como agentes antihistaminicos y antialergicos. |
| KR100735639B1 (ko) | 2004-12-29 | 2007-07-04 | 한미약품 주식회사 | 암세포 성장 억제 효과를 갖는 퀴나졸린 유도체 및 이의제조방법 |
| PE20070207A1 (es) | 2005-07-22 | 2007-03-09 | Genentech Inc | Tratamiento combinado de los tumores que expresan el her |
| 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. |
| CN101003514A (zh) | 2006-01-20 | 2007-07-25 | 上海艾力斯医药科技有限公司 | 喹唑啉衍生物、其制备方法及用途 |
| DE102006012251A1 (de) * | 2006-03-15 | 2007-11-08 | Grünenthal GmbH | Substituierte 4-Amino-chinazolin-Derivate und ihre Verwendung zur Herstellung von Arzneimitteln |
| WO2007114926A2 (en) | 2006-04-04 | 2007-10-11 | The Regents Of The University Of California | Kinase antagonists |
| EP2049502B1 (en) | 2006-07-28 | 2012-01-04 | Novartis AG | 2,4-substituted quinazolines as lipid kinase inhibitors |
| UY31137A1 (es) | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
| WO2009012647A1 (fr) | 2007-07-20 | 2009-01-29 | Shanghai Hengrui Pharmaceutical Co., Ltd. | Procédés de préparation de dérivés de quinazoline et leurs utilisations pharmaceutiques |
| EP2060565A1 (en) | 2007-11-16 | 2009-05-20 | 4Sc Ag | Novel bifunctional compounds which inhibit protein kinases and histone deacetylases |
| EP2303890A4 (en) | 2008-06-19 | 2012-04-11 | Progenics Pharm Inc | INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE |
| EP2323659A4 (en) | 2008-08-05 | 2012-03-14 | Abbott Lab | COMPOUNDS USEFUL AS INHIBITORS OF PROTEIN KINASES |
| AR079814A1 (es) | 2009-12-31 | 2012-02-22 | Otsuka Pharma Co Ltd | Compuestos heterociclicos, composiciones farmaceuticas que los contienen y sus usos |
| ES2565627T3 (es) | 2010-07-30 | 2016-04-06 | Oncotherapy Science, Inc. | Derivados de quinolina e inhibidores de MELK que contienen los mismos |
| DE102010049595A1 (de) | 2010-10-26 | 2012-04-26 | Merck Patent Gmbh | Chinazolinderivate |
| US8664230B2 (en) | 2011-03-17 | 2014-03-04 | The Asan Foundation | Pyridopyrimidine derivatives and use thereof |
| ITMI20110480A1 (it) | 2011-03-25 | 2012-09-26 | F I S Fabbrica Italiana Sint P A | Procedimento per la preparazione di lapatinib e suoi sali |
| KR20140048216A (ko) | 2011-06-29 | 2014-04-23 | 오츠카 세이야쿠 가부시키가이샤 | 치료 화합물로서의 퀴나졸린 및 관련된 사용 방법 |
| US9499530B2 (en) | 2011-08-01 | 2016-11-22 | Hangzhou Minsheng Institutes For Pharma Research | Quinazoline derivative, composition having the derivative, and use of the derivative in preparing medicament |
| US8785459B2 (en) | 2011-12-27 | 2014-07-22 | Development Center For Biotechnology | Quinazoline compounds as kinase inhibitors |
| US20130331405A1 (en) | 2012-06-12 | 2013-12-12 | The Regents Of The University Of California | PIK3CA Mutation Status and SASH1 Expression Predicts Synergy Between Lapatinib and an AKT Inhibitor in HER2 Positive Breast Cancer |
| CA2969974C (en) | 2014-12-15 | 2020-08-04 | The Regents Of The University Of Michigan | Small molecule inhibitors of egfr and pi3k |
| PE20181366A1 (es) * | 2015-08-03 | 2018-08-27 | Bristol Myers Squibb Co | Compuestos heterociclicos utiles como moduladores de factor de necrosis tumoral (tnf) alfa |
| CN110022878A (zh) * | 2016-11-03 | 2019-07-16 | 密执安大学评议会 | Egfr/pi3k的小分子双重抑制剂及其用途 |
| US20190002460A1 (en) | 2017-06-28 | 2019-01-03 | The Regents Of The University Of Michigan | Small molecule inhibitors of egfr and pi3k |
| EP3955923A1 (en) * | 2019-04-18 | 2022-02-23 | The Regents Of The University Of Michigan | Combination with checkpoint inhibitors to treat cancer |
| BR112021022099A2 (pt) * | 2019-05-31 | 2021-12-28 | Chiesi Farm Spa | Derivados de amino quinazolina como inibidores de p2x3 |
-
2021
- 2021-12-21 WO PCT/US2021/064709 patent/WO2022140456A1/en not_active Ceased
- 2021-12-21 MX MX2023007550A patent/MX2023007550A/es unknown
- 2021-12-21 US US18/258,746 patent/US20240239764A1/en active Pending
- 2021-12-21 US US17/558,399 patent/US11673876B2/en active Active
- 2021-12-21 JP JP2023539379A patent/JP2024501995A/ja active Pending
- 2021-12-21 EP EP21844900.7A patent/EP4267554A1/en active Pending
- 2021-12-21 CN CN202180093055.XA patent/CN117295716A/zh active Pending
- 2021-12-21 KR KR1020237025037A patent/KR20230155422A/ko active Pending
- 2021-12-21 CA CA3206168A patent/CA3206168A1/en active Pending
- 2021-12-21 IL IL303965A patent/IL303965A/en unknown
- 2021-12-21 AU AU2021410726A patent/AU2021410726A1/en active Pending
-
2023
- 2023-04-26 US US18/307,576 patent/US20240083868A1/en active Pending
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