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
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- 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 (enExample) | 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 (enExample) |
| EP (1) | EP3442529B1 (enExample) |
| JP (2) | JP6911047B2 (enExample) |
| KR (1) | KR102418765B1 (enExample) |
| CN (1) | CN109310684B (enExample) |
| AU (1) | AU2017249078B2 (enExample) |
| CA (1) | CA3020875A1 (enExample) |
| ES (1) | ES2881801T3 (enExample) |
| MX (1) | MX380779B (enExample) |
| RU (1) | RU2747788C2 (enExample) |
| WO (1) | WO2017180389A1 (enExample) |
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 |
| US11564929B2 (en) | 2016-04-12 | 2023-01-31 | Eli Lilly And Company | Combination therapy with Notch and PI3K/mTOR inhibitors for use in treating cancer |
| KR102418765B1 (ko) | 2016-04-12 | 2022-07-08 | 일라이 릴리 앤드 캄파니 | 암 치료를 위한 Notch 및 CDK4/6 억제제의 조합 요법 |
| 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 |
| KR20190116420A (ko) | 2017-02-17 | 2019-10-14 | 프레드 헛친슨 켄서 리서치 센터 | Bcma 관련 암 및 자가면역 장애의 치료를 위한 조합 요법 |
| CN111886012A (zh) | 2017-11-06 | 2020-11-03 | 朱诺治疗学股份有限公司 | 细胞疗法与γ分泌酶抑制剂的组合 |
| IL257225A (en) * | 2018-01-29 | 2018-04-09 | Yeda Res & Dev | Treatment of sarcoma |
| BR112020022654A2 (pt) | 2018-05-06 | 2021-03-09 | Ayala Pharmaceuticals Inc. | Composições de combinação que compreendem compostos de bisfluoroalquil-1,4-benzodiazepinona e métodos de uso das mesmas |
| 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 |
|---|---|---|---|---|
| ZA9711537B (en) | 1996-12-23 | 1998-06-25 | Athena Neurosciences Inc Eli L | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-amyloid peptide release and/or its synthesis by use of such compounds. |
| JP2002526109A (ja) | 1998-10-02 | 2002-08-20 | ザ ガバメント オブ ザ ユナイテッドステイツ オブ アメリカ アズ リプレゼンテッド バイ ザ セクレタリー デパートメント オブ ヘルス アンド ヒューマン サービシーズ ザ ナショナル インステ | アポトーシス誘導物質と方法 |
| HRP20080053A2 (hr) | 2005-07-01 | 2009-08-31 | Medarex | Ljudska monoklonska protutijela na ligand 1 za programiranu smrt stanice (pd-l1) |
| 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 |
| BRPI0815135A2 (pt) | 2007-08-14 | 2015-02-03 | Lilly Co Eli | Derivados de azepina como inibidores de gama secretase. |
| JO2885B1 (en) | 2008-12-22 | 2015-03-15 | ايلي ليلي اند كومباني | Protein kinase inhibitors |
| 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 |
| JO3148B1 (ar) | 2011-07-27 | 2017-09-20 | Lilly Co Eli | مركب مثبط لإشارات مسار notch |
| US10010608B2 (en) | 2013-05-31 | 2018-07-03 | Merck Sharp & Dohme Corp. | Combination therapies for cancer |
| JP6586087B2 (ja) | 2013-08-20 | 2019-10-02 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | Ｐｄ−１アンタゴニストとジナシクリブとの組合せでの癌治療 |
| 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 |
| RU2718914C2 (ru) | 2014-09-13 | 2020-04-15 | Новартис Аг | Сочетанные способы лечения с использованием ингибиторов alk |
| EP3280795B1 (en) | 2015-04-07 | 2021-03-24 | Novartis AG | Combination of chimeric antigen receptor therapy and amino pyrimidine derivatives |
| 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 |
| KR102418765B1 (ko) | 2016-04-12 | 2022-07-08 | 일라이 릴리 앤드 캄파니 | 암 치료를 위한 Notch 및 CDK4/6 억제제의 조합 요법 |
| US11564929B2 (en) * | 2016-04-12 | 2023-01-31 | Eli Lilly And Company | Combination therapy with Notch and PI3K/mTOR inhibitors for use in treating cancer |
| KR102463617B1 (ko) | 2016-05-20 | 2022-11-03 | 일라이 릴리 앤드 캄파니 | Notch 및 PD-1 또는 PD-L1 억제제를 이용한 조합 요법 |
| CN116473978A (zh) | 2016-08-31 | 2023-07-25 | 伊莱利利公司 | 用于治疗实体瘤的给药方案 |
| EP3525796A1 (en) | 2016-10-12 | 2019-08-21 | Eli Lilly and Company | Targeted treatment of mature t-cell lymphoma |
| WO2018201056A1 (en) | 2017-04-28 | 2018-11-01 | Novartis Ag | Cells expressing a bcma-targeting chimeric antigen receptor, and combination therapy with a gamma secretase inhibitor |
| CN111886012A (zh) | 2017-11-06 | 2020-11-03 | 朱诺治疗学股份有限公司 | 细胞疗法与γ分泌酶抑制剂的组合 |
-
2017
- 2017-04-05 KR KR1020187032285A patent/KR102418765B1/ko 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 EP EP17717990.0A patent/EP3442529B1/en active Active
- 2017-04-05 RU RU2018138627A patent/RU2747788C2/ru 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 AU AU2017249078A patent/AU2017249078B2/en active Active
- 2017-04-05 ES ES17717990T patent/ES2881801T3/es active Active
-
2021
- 2021-07-07 JP JP2021112726A patent/JP7288482B2/ja active Active
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