JP2019528276A5 - - Google Patents
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- JP2019528276A5 JP2019528276A5 JP2019508889A JP2019508889A JP2019528276A5 JP 2019528276 A5 JP2019528276 A5 JP 2019528276A5 JP 2019508889 A JP2019508889 A JP 2019508889A JP 2019508889 A JP2019508889 A JP 2019508889A JP 2019528276 A5 JP2019528276 A5 JP 2019528276A5
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- 239000013078 crystal Substances 0.000 claims 20
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 9
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical group CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 8
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical group CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 8
- 239000003960 organic solvent Substances 0.000 claims 8
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 7
- 229940125904 compound 1 Drugs 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 6
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 6
- 210000003719 b-lymphocyte Anatomy 0.000 claims 6
- -1 phenylacetyl Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 238000000634 powder X-ray diffraction Methods 0.000 claims 5
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 4
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 235000019439 ethyl acetate Nutrition 0.000 claims 4
- 208000016025 Waldenstroem macroglobulinemia Diseases 0.000 claims 3
- 239000003054 catalyst Substances 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 125000006239 protecting group Chemical group 0.000 claims 3
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 2
- JWUJQDFVADABEY-UHFFFAOYSA-N 2-methyltetrahydrofuran Chemical compound CC1CCCO1 JWUJQDFVADABEY-UHFFFAOYSA-N 0.000 claims 2
- 125000004217 4-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])* 0.000 claims 2
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 claims 2
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 201000003444 follicular lymphoma Diseases 0.000 claims 2
- 201000009277 hairy cell leukemia Diseases 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 235000011090 malic acid Nutrition 0.000 claims 2
- 201000007924 marginal zone B-cell lymphoma Diseases 0.000 claims 2
- 208000021937 marginal zone lymphoma Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- BJEPYKJPYRNKOW-UWTATZPHSA-N (R)-malic acid Chemical compound OC(=O)[C@H](O)CC(O)=O BJEPYKJPYRNKOW-UWTATZPHSA-N 0.000 claims 1
- IWYDHOAUDWTVEP-SSDOTTSWSA-N (R)-mandelic acid Chemical compound OC(=O)[C@H](O)C1=CC=CC=C1 IWYDHOAUDWTVEP-SSDOTTSWSA-N 0.000 claims 1
- IWYDHOAUDWTVEP-ZETCQYMHSA-N (S)-mandelic acid Chemical compound OC(=O)[C@@H](O)C1=CC=CC=C1 IWYDHOAUDWTVEP-ZETCQYMHSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000011951 cationic catalyst Substances 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 229960001270 d- tartaric acid Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 229940116298 l- malic acid Drugs 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- FEWJPZIEWOKRBE-LWMBPPNESA-N levotartaric acid Chemical compound OC(=O)[C@@H](O)[C@H](O)C(O)=O FEWJPZIEWOKRBE-LWMBPPNESA-N 0.000 claims 1
- 230000036210 malignancy Effects 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
- 230000007935 neutral effect Effects 0.000 claims 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000005425 toluyl group Chemical group 0.000 claims 1
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022030942A JP7413419B2 (ja) | 2016-08-16 | 2022-03-01 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
| JP2023220256A JP7637459B2 (ja) | 2016-08-16 | 2023-12-27 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
| JP2025021657A JP2025081429A (ja) | 2016-08-16 | 2025-02-13 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2016/095510 | 2016-08-16 | ||
| CN2016095510 | 2016-08-16 | ||
| PCT/IB2017/054955 WO2018033853A2 (en) | 2016-08-16 | 2017-08-15 | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022030942A Division JP7413419B2 (ja) | 2016-08-16 | 2022-03-01 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019528276A JP2019528276A (ja) | 2019-10-10 |
| JP2019528276A5 true JP2019528276A5 (OSRAM) | 2020-09-24 |
| JP7402685B2 JP7402685B2 (ja) | 2023-12-21 |
Family
ID=61197220
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019508889A Active JP7402685B2 (ja) | 2016-08-16 | 2017-08-15 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
| JP2022030942A Active JP7413419B2 (ja) | 2016-08-16 | 2022-03-01 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
| JP2023220256A Active JP7637459B2 (ja) | 2016-08-16 | 2023-12-27 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
| JP2025021657A Pending JP2025081429A (ja) | 2016-08-16 | 2025-02-13 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022030942A Active JP7413419B2 (ja) | 2016-08-16 | 2022-03-01 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
| JP2023220256A Active JP7637459B2 (ja) | 2016-08-16 | 2023-12-27 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
| JP2025021657A Pending JP2025081429A (ja) | 2016-08-16 | 2025-02-13 | （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (12) | US10927117B2 (OSRAM) |
| EP (3) | EP4353322A3 (OSRAM) |
| JP (4) | JP7402685B2 (OSRAM) |
| KR (3) | KR102604975B1 (OSRAM) |
| CN (3) | CN116478165A (OSRAM) |
| AU (3) | AU2017314178B2 (OSRAM) |
| CA (1) | CA3033827A1 (OSRAM) |
| EA (1) | EA201990519A1 (OSRAM) |
| IL (2) | IL293319A (OSRAM) |
| MX (1) | MX384627B (OSRAM) |
| NZ (1) | NZ751418A (OSRAM) |
| SG (1) | SG11201901141WA (OSRAM) |
| TW (3) | TWI884890B (OSRAM) |
| WO (1) | WO2018033853A2 (OSRAM) |
| ZA (1) | ZA201900919B (OSRAM) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| SMT201700160T1 (it) | 2013-04-25 | 2017-05-08 | Beigene Ltd | Composti eterociclici fusi come inibitori di protein chinasi |
| ES2792183T3 (es) | 2013-09-13 | 2020-11-10 | Beigene Switzerland Gmbh | Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico |
| CN106604742B (zh) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| CN109475536B (zh) | 2016-07-05 | 2022-05-27 | 百济神州有限公司 | 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合 |
| WO2018033853A2 (en) | 2016-08-16 | 2018-02-22 | Beigene, Ltd. | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| PT3500299T (pt) | 2016-08-19 | 2024-02-21 | Beigene Switzerland Gmbh | Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro |
| CN110461847B (zh) | 2017-01-25 | 2022-06-07 | 百济神州有限公司 | (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途 |
| TW202515616A (zh) | 2017-06-26 | 2025-04-16 | 英屬開曼群島商百濟神州有限公司 | 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途 |
| CN110997677A (zh) | 2017-08-12 | 2020-04-10 | 百济神州有限公司 | 具有改进的双重选择性的Btk抑制剂 |
| WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors |
| AU2019245436B2 (en) * | 2018-03-29 | 2024-12-12 | Mati Therapeutics Inc. | Ophthalmic drug sustained release formulation and uses for dry eye syndrome treatment |
| CN111675711A (zh) * | 2019-03-11 | 2020-09-18 | 百济神州(苏州)生物科技有限公司 | Btk抑制剂化合物的单晶及其制备方法 |
| CN117820311A (zh) * | 2019-05-08 | 2024-04-05 | 百济神州(苏州)生物科技有限公司 | Btk抑制剂及其中间体的制备方法 |
| AU2020281410A1 (en) * | 2019-05-31 | 2021-10-07 | Haisco Pharmaceuticals Pte. Ltd. | BTK inhibitor ring derivative, preparation method therefor and pharmaceutical application thereof |
| WO2020249001A1 (zh) | 2019-06-10 | 2020-12-17 | 百济神州瑞士有限责任公司 | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 |
| CN112057432A (zh) * | 2019-06-10 | 2020-12-11 | 百济神州(苏州)生物科技有限公司 | 口服胶囊剂及其制备方法 |
| CN112057427B (zh) * | 2019-06-10 | 2024-09-03 | 百济神州(苏州)生物科技有限公司 | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 |
| TW202112369A (zh) * | 2019-06-10 | 2021-04-01 | 英屬開曼群島商百濟神州有限公司 | 口服膠囊劑及其製備方法 |
| CN110563733A (zh) * | 2019-09-12 | 2019-12-13 | 安帝康（无锡）生物科技有限公司 | 作为选择性btk抑制剂的咪唑并吡嗪类化合物 |
| US20220411430A1 (en) * | 2019-12-04 | 2022-12-29 | Henan Zhiwei Biomedicine Co., Ltd. | Substituted imidazolecarboxamide as bruton's tyrosine kinase inhibitors |
| CN110922409A (zh) * | 2019-12-19 | 2020-03-27 | 武汉九州钰民医药科技有限公司 | 制备btk抑制剂泽布替尼的方法 |
| CN110845504A (zh) * | 2019-12-19 | 2020-02-28 | 武汉九州钰民医药科技有限公司 | 合成赞布替尼的新方法 |
| CN110938077B (zh) * | 2019-12-25 | 2021-04-27 | 武汉九州钰民医药科技有限公司 | 合成Avapritinib的方法 |
| WO2021170045A1 (en) * | 2020-02-27 | 2021-09-02 | Beigene Switzerland Gmbh | Methods of treating dlbcl using btk inhibitors and combinations thereof |
| WO2021259732A1 (en) | 2020-06-24 | 2021-12-30 | Sandoz Ag | Multi-component compounds comprising zanubrutinib and a benzoic acid derivative |
| TW202216715A (zh) | 2020-07-07 | 2022-05-01 | 大陸商四川海思科製藥有限公司 | 降解btk激酶的化合物、製造方法及其應用 |
| WO2022101939A1 (en) * | 2020-11-13 | 2022-05-19 | Msn Laboratories Private Limited, R&D Center | Novel process for the preparation of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide or its salts thereof |
| WO2022105870A1 (en) * | 2020-11-20 | 2022-05-27 | Beigene, Ltd. | Methods of treating systemic lupus erythematosus using btk inhibitors |
| WO2022125862A1 (en) | 2020-12-11 | 2022-06-16 | Teva Pharmaceuticals International Gmbh | Processes for the preparation of zanubrutinib and intermediates thereof |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| WO2023014817A1 (en) | 2021-08-03 | 2023-02-09 | Syros Pharmaceuticals, Inc. | Compositions and methods for treating lymphomas with a cdk7 inhibitor in combination with a btk inhibitor |
| IT202100025997A1 (it) * | 2021-10-11 | 2023-04-11 | Olon Spa | Processo per la preparazione di zanubrutinib |
| IT202200009872A1 (it) * | 2022-05-12 | 2023-11-12 | Olon Spa | Processo di preparazione di Zanubrutinib in forma amorfa. |
| IT202200024192A1 (it) * | 2022-11-24 | 2024-05-24 | Olon Spa | Processo per la preparazione di Zanubrutinib. |
| CN118307541A (zh) * | 2023-01-09 | 2024-07-09 | 天津济坤医药科技有限公司 | 氘代吡唑并嘧啶衍生物及其制备方法和药物组合物、结合物及应用 |
| CN117430610A (zh) * | 2023-10-11 | 2024-01-23 | 宁夏医科大学 | 一种氘代稠合杂环化合物及其制备方法和应用 |
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