JP2019511526A5 - - Google Patents
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- JP2019511526A5 JP2019511526A5 JP2018553357A JP2018553357A JP2019511526A5 JP 2019511526 A5 JP2019511526 A5 JP 2019511526A5 JP 2018553357 A JP2018553357 A JP 2018553357A JP 2018553357 A JP2018553357 A JP 2018553357A JP 2019511526 A5 JP2019511526 A5 JP 2019511526A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- oxo
- fluoro
- methyl
- ethyl
- 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
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- 150000003839 salts Chemical class 0.000 claims description 48
- 206010028980 Neoplasm Diseases 0.000 claims description 17
- DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims description 17
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 17
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 16
- 201000011510 cancer Diseases 0.000 claims description 16
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 15
- 239000003814 drug Substances 0.000 claims description 15
- 201000005202 lung cancer Diseases 0.000 claims description 15
- 208000020816 lung neoplasm Diseases 0.000 claims description 15
- UZWDCWONPYILKI-UHFFFAOYSA-N n-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine Chemical compound C1CN(CC)CCN1CC(C=N1)=CC=C1NC1=NC=C(F)C(C=2C=C3N(C(C)C)C(C)=NC3=C(F)C=2)=N1 UZWDCWONPYILKI-UHFFFAOYSA-N 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 10
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 9
- 206010006187 Breast cancer Diseases 0.000 claims description 9
- 208000026310 Breast neoplasm Diseases 0.000 claims description 9
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 9
- 206010033128 Ovarian cancer Diseases 0.000 claims description 9
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 9
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 9
- 206010060862 Prostate cancer Diseases 0.000 claims description 9
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 9
- 206010039491 Sarcoma Diseases 0.000 claims description 9
- 208000005017 glioblastoma Diseases 0.000 claims description 9
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 9
- 201000001441 melanoma Diseases 0.000 claims description 9
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 9
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 8
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 8
- 206010009944 Colon cancer Diseases 0.000 claims description 8
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 8
- 206010059352 Desmoid tumour Diseases 0.000 claims description 8
- 208000000172 Medulloblastoma Diseases 0.000 claims description 8
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 8
- 208000002517 adenoid cystic carcinoma Diseases 0.000 claims description 8
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims description 8
- 201000006827 desmoid tumor Diseases 0.000 claims description 8
- 201000007416 salivary gland adenoid cystic carcinoma Diseases 0.000 claims description 8
- 201000002528 pancreatic cancer Diseases 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims 17
- -1 N- [5- (4-ethyl- Piperazin-1-ylmethyl) -pyridin-2-yl]-[5-fluoro-4- (7-fluoro-3-isopropyl-2-methyl-3H-benzimidazol-5-yl) -pyrimidin-2-yl] Chemical class 0.000 claims 13
- YCBAQKQAINQRFW-UGSOOPFHSA-N 4,4,4-trifluoro-n-[(2s)-1-[[(7s)-5-(2-hydroxyethyl)-6-oxo-7h-pyrido[2,3-d][3]benzazepin-7-yl]amino]-1-oxopropan-2-yl]butanamide Chemical compound OCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)CCC(F)(F)F)C)C2=CC=CC=C2C2=CC=CN=C21 YCBAQKQAINQRFW-UGSOOPFHSA-N 0.000 claims 6
- 150000001412 amines Chemical class 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 1
- 241000321096 Adenoides Species 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- 206010011732 Cyst Diseases 0.000 description 1
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 description 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 1
- 210000002534 adenoid Anatomy 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000031513 cyst Diseases 0.000 description 1
- FATAVLOOLIRUNA-UHFFFAOYSA-N formylmethyl Chemical group [CH2]C=O FATAVLOOLIRUNA-UHFFFAOYSA-N 0.000 description 1
- 201000002313 intestinal cancer Diseases 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 230000036210 malignancy Effects 0.000 description 1
- 208000037821 progressive disease Diseases 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021112726A JP7288482B2 (ja) | 2016-04-12 | 2021-07-07 | がんの処置のための、Ｎｏｔｃｈ阻害剤およびＣＤＫ４／６阻害剤の併用療法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662321311P | 2016-04-12 | 2016-04-12 | |
| US62/321,311 | 2016-04-12 | ||
| PCT/US2017/026134 WO2017180389A1 (en) | 2016-04-12 | 2017-04-05 | Combination therapy with notch and cdk4/6 inhibitors for the treatment of cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021112726A Division JP7288482B2 (ja) | 2016-04-12 | 2021-07-07 | がんの処置のための、Ｎｏｔｃｈ阻害剤およびＣＤＫ４／６阻害剤の併用療法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019511526A JP2019511526A (ja) | 2019-04-25 |
| JP2019511526A5 true JP2019511526A5 (OSRAM) | 2020-05-14 |
| JP6911047B2 JP6911047B2 (ja) | 2021-07-28 |
Family
ID=58548919
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018553357A Active JP6911047B2 (ja) | 2016-04-12 | 2017-04-05 | がんの処置のための、Ｎｏｔｃｈ阻害剤およびＣＤＫ４／６阻害剤の併用療法 |
| JP2021112726A Active JP7288482B2 (ja) | 2016-04-12 | 2021-07-07 | がんの処置のための、Ｎｏｔｃｈ阻害剤およびＣＤＫ４／６阻害剤の併用療法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021112726A Active JP7288482B2 (ja) | 2016-04-12 | 2021-07-07 | がんの処置のための、Ｎｏｔｃｈ阻害剤およびＣＤＫ４／６阻害剤の併用療法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US11298362B2 (OSRAM) |
| EP (1) | EP3442529B1 (OSRAM) |
| JP (2) | JP6911047B2 (OSRAM) |
| KR (1) | KR102418765B1 (OSRAM) |
| CN (1) | CN109310684B (OSRAM) |
| AU (1) | AU2017249078B2 (OSRAM) |
| CA (1) | CA3020875A1 (OSRAM) |
| ES (1) | ES2881801T3 (OSRAM) |
| MX (1) | MX380779B (OSRAM) |
| RU (1) | RU2747788C2 (OSRAM) |
| WO (1) | WO2017180389A1 (OSRAM) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI609687B (zh) | 2015-04-14 | 2018-01-01 | 美國禮來大藥廠 | 平滑肌肉瘤之標靶性治療 |
| RU2754452C2 (ru) * | 2016-04-12 | 2021-09-02 | Эли Лилли Энд Компани | Комбинированная терапия ингибиторами notch и pi3k/mtor для применения в лечении рака |
| ES2881801T3 (es) | 2016-04-12 | 2021-11-30 | Lilly Co Eli | Terapia de combinación con inhibidores de Notch y CDK4/6 para su uso en el tratamiento de cáncer de pulmón |
| KR102463617B1 (ko) | 2016-05-20 | 2022-11-03 | 일라이 릴리 앤드 캄파니 | Notch 및 PD-1 또는 PD-L1 억제제를 이용한 조합 요법 |
| EP3525796A1 (en) | 2016-10-12 | 2019-08-21 | Eli Lilly and Company | Targeted treatment of mature t-cell lymphoma |
| SG11201907580SA (en) | 2017-02-17 | 2019-09-27 | Hutchinson Fred Cancer Res | Combination therapies for treatment of bcma-related cancers and autoimmune disorders |
| AU2018359907A1 (en) | 2017-11-06 | 2020-05-07 | Fred Hutchinson Cancer Center | Combination of a cell therapy and a gamma secretase inhibitor |
| IL257225A (en) * | 2018-01-29 | 2018-04-09 | Yeda Res & Dev | Treatment of sarcoma |
| JP7522661B2 (ja) * | 2018-05-06 | 2024-07-25 | アヤラ ファーマシューティカルズ インコーポレイテッド | ビスフルオロアルキル－１，４－ベンゾジアゼピノン化合物を含む組み合わせ組成物およびその使用方法 |
| WO2019226667A1 (en) * | 2018-05-25 | 2019-11-28 | Nantomics, Llc | Comprehensive molecular profiling with proteomic and genomic analyses |
| CN112535686B (zh) * | 2019-09-20 | 2022-06-14 | 山东轩竹医药科技有限公司 | 激酶抑制剂的新用途 |
| CN113880809B (zh) * | 2020-07-03 | 2022-10-18 | 盛世泰科生物医药技术(苏州)有限公司 | 一种嘧啶类衍生物及其制备方法和应用 |
| WO2023109875A1 (en) * | 2021-12-16 | 2023-06-22 | Edigene Therapeutics (Beijing) Inc. | Biomarkers for colorectal cancer treatment |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2272305A1 (en) | 1996-12-23 | 1998-07-02 | Elan Pharmaceuticals, Inc. | Cycloalkyl, lactam, lactone and related compounds as .beta.-amyloid peptide release inhibitors |
| EP1117778A2 (en) | 1998-10-02 | 2001-07-25 | THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES | Methods and compositions for inducing differentiation and apoptosis in cells that overexpress the notch protein |
| KR101411165B1 (ko) | 2005-07-01 | 2014-06-25 | 메다렉스, 엘.엘.시. | 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날항체 |
| WO2008112249A1 (en) | 2007-03-13 | 2008-09-18 | Trustees Of Columbia University In The City Of New York | Synergistic interaction of notch-1 inhibitors with glucocorticoids |
| CA2694209C (en) | 2007-08-14 | 2013-09-17 | Eli Lilly And Company | Azepine derivatives as gamma-secretase inhibitors |
| PA8852901A1 (es) | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| US8637493B2 (en) | 2009-11-12 | 2014-01-28 | University Of Massachusetts | Methods for treating glioblastoma |
| CN102085372A (zh) | 2009-12-04 | 2011-06-08 | 中国医学科学院基础医学研究所 | Notch通路抑制剂用于治疗mTOR活化导致的肿瘤的用途 |
| JO3003B1 (ar) * | 2011-01-14 | 2016-09-05 | Lilly Co Eli | مركب أيميدازو [4، 5 -c ] كينولين-2- واحد واستخدامه كمثبط كيناز PI3/mtor |
| AR087107A1 (es) | 2011-07-27 | 2014-02-12 | Lilly Co Eli | Compuesto inhibidor de la señalizacion de la trayectoria notch |
| ES2822665T3 (es) | 2013-05-31 | 2021-05-04 | Merck Sharp & Dohme | Terapias de combinación para el cáncer |
| KR102232153B1 (ko) | 2013-08-20 | 2021-03-24 | 머크 샤프 앤드 돔 코포레이션 | Pd-1 길항제와 디나시클립의 조합을 사용한 암의 치료 |
| US10092645B2 (en) | 2014-06-17 | 2018-10-09 | Medimmune Limited | Methods of treatment with antagonists against PD-1 and PD-L1 in combination with radiation therapy |
| KR20170060042A (ko) | 2014-09-13 | 2017-05-31 | 노파르티스 아게 | Alk 억제제의 조합 요법 |
| ES2876974T3 (es) | 2015-04-07 | 2021-11-15 | Novartis Ag | Combinación de terapia con receptor de antígeno quimérico y derivados de amino pirimidina |
| TWI609687B (zh) | 2015-04-14 | 2018-01-01 | 美國禮來大藥廠 | 平滑肌肉瘤之標靶性治療 |
| RU2754452C2 (ru) | 2016-04-12 | 2021-09-02 | Эли Лилли Энд Компани | Комбинированная терапия ингибиторами notch и pi3k/mtor для применения в лечении рака |
| ES2881801T3 (es) | 2016-04-12 | 2021-11-30 | Lilly Co Eli | Terapia de combinación con inhibidores de Notch y CDK4/6 para su uso en el tratamiento de cáncer de pulmón |
| KR102463617B1 (ko) | 2016-05-20 | 2022-11-03 | 일라이 릴리 앤드 캄파니 | Notch 및 PD-1 또는 PD-L1 억제제를 이용한 조합 요법 |
| SG10202107832UA (en) | 2016-08-31 | 2021-09-29 | Lilly Co Eli | Dosage regimen for treatment of solid tumors |
| EP3525796A1 (en) | 2016-10-12 | 2019-08-21 | Eli Lilly and Company | Targeted treatment of mature t-cell lymphoma |
| EP3615055A1 (en) | 2017-04-28 | 2020-03-04 | Novartis AG | Cells expressing a bcma-targeting chimeric antigen receptor, and combination therapy with a gamma secretase inhibitor |
| AU2018359907A1 (en) | 2017-11-06 | 2020-05-07 | Fred Hutchinson Cancer Center | Combination of a cell therapy and a gamma secretase inhibitor |
-
2017
- 2017-04-05 ES ES17717990T patent/ES2881801T3/es active Active
- 2017-04-05 CN CN201780036170.7A patent/CN109310684B/zh active Active
- 2017-04-05 US US16/093,123 patent/US11298362B2/en active Active
- 2017-04-05 JP JP2018553357A patent/JP6911047B2/ja active Active
- 2017-04-05 MX MX2018012457A patent/MX380779B/es unknown
- 2017-04-05 CA CA3020875A patent/CA3020875A1/en active Pending
- 2017-04-05 WO PCT/US2017/026134 patent/WO2017180389A1/en not_active Ceased
- 2017-04-05 RU RU2018138627A patent/RU2747788C2/ru active
- 2017-04-05 EP EP17717990.0A patent/EP3442529B1/en active Active
- 2017-04-05 KR KR1020187032285A patent/KR102418765B1/ko active Active
- 2017-04-05 AU AU2017249078A patent/AU2017249078B2/en active Active
-
2021
- 2021-07-07 JP JP2021112726A patent/JP7288482B2/ja active Active
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