JP2022071072A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2022071072A5 JP2022071072A5 JP2022030942A JP2022030942A JP2022071072A5 JP 2022071072 A5 JP2022071072 A5 JP 2022071072A5 JP 2022030942 A JP2022030942 A JP 2022030942A JP 2022030942 A JP2022030942 A JP 2022030942A JP 2022071072 A5 JP2022071072 A5 JP 2022071072A5
- Authority
- JP
- Japan
- Prior art keywords
- crystal
- compound
- crystals
- pharmaceutical composition
- amorphous form
- 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
- 239000013078 crystal Substances 0.000 claims 57
- 229940125904 compound 1 Drugs 0.000 claims 19
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 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
- 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
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 210000003719 b-lymphocyte Anatomy 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 4
- 235000019439 ethyl acetate Nutrition 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 230000009477 glass transition Effects 0.000 claims 3
- 238000002844 melting Methods 0.000 claims 3
- 230000008018 melting Effects 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- JWUJQDFVADABEY-UHFFFAOYSA-N 2-methyltetrahydrofuran Chemical compound CC1CCCO1 JWUJQDFVADABEY-UHFFFAOYSA-N 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 238000001704 evaporation Methods 0.000 claims 2
- 201000003444 follicular lymphoma Diseases 0.000 claims 2
- 201000009277 hairy cell leukemia Diseases 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 201000007924 marginal zone B-cell lymphoma Diseases 0.000 claims 2
- 208000021937 marginal zone lymphoma Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 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
- BYWBCSRCPLBDFU-CYBMUJFWSA-N [3-[4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yl]oxyphenyl]-[(3R)-3-aminopyrrolidin-1-yl]methanone Chemical compound NCC1=CC(=NC(=C1)C(F)(F)F)OC=1C=C(C=CC=1)C(=O)N1C[C@@H](CC1)N BYWBCSRCPLBDFU-CYBMUJFWSA-N 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2016095510 | 2016-08-16 | ||
| CNPCT/CN2016/095510 | 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 |
| JP2019508889A 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 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019508889A Division 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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023220256A Division 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022071072A JP2022071072A (ja) | 2022-05-13 |
| JP2022071072A5 true JP2022071072A5 (enExample) | 2022-12-13 |
| JP7413419B2 JP7413419B2 (ja) | 2024-01-15 |
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 Before (1)
| 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 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 (enExample) |
| EP (3) | EP4509183A3 (enExample) |
| JP (4) | JP7402685B2 (enExample) |
| KR (3) | KR102604975B1 (enExample) |
| CN (3) | CN116478166A (enExample) |
| AU (3) | AU2017314178B2 (enExample) |
| CA (1) | CA3033827A1 (enExample) |
| EA (1) | EA201990519A1 (enExample) |
| IL (2) | IL293319A (enExample) |
| MX (1) | MX384627B (enExample) |
| NZ (1) | NZ751418A (enExample) |
| SG (1) | SG11201901141WA (enExample) |
| TW (3) | TWI760356B (enExample) |
| WO (1) | WO2018033853A2 (enExample) |
| ZA (1) | ZA201900919B (enExample) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015025260B1 (pt) | 2013-04-25 | 2021-11-03 | Beigene, Ltd | Compostos heterocíclicos fundidos como inibidores da proteína quinase, sua composição, combinação e uso |
| RS63571B9 (sr) | 2013-09-13 | 2023-02-28 | Beigene Switzerland Gmbh | Anti-pd1 antitela i njihova primena kao terapeutska i dijagnostička sredstva |
| US10544225B2 (en) | 2014-07-03 | 2020-01-28 | Beigene, Ltd. | Anti-PD-L1 antibodies and their use as therapeutics and diagnostics |
| WO2018007885A1 (en) | 2016-07-05 | 2018-01-11 | Beigene, Ltd. | COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER |
| JP7402685B2 (ja) | 2016-08-16 | 2023-12-21 | ベイジーン スウィッツァーランド ゲーエムベーハー | （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 |
| AU2017313085B2 (en) | 2016-08-19 | 2024-06-20 | Beone Medicines I Gmbh | Use of a combination comprising a Btk inhibitor for treating cancers |
| 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 |
| WO2019001417A1 (en) | 2017-06-26 | 2019-01-03 | Beigene, Ltd. | IMMUNOTHERAPY FOR HEPATOCELLULAR CARCINOMA |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
| KR20210100005A (ko) * | 2018-03-29 | 2021-08-13 | 마티 테라퓨틱스 인코포레이티드 | 안과 약제의 서방성 제형 및 건성 증후군 치료 용도 |
| 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 |
| CN111909152B (zh) * | 2019-05-08 | 2023-12-15 | 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 |
| BR112021024131A2 (pt) * | 2019-05-31 | 2022-01-11 | Haisco Pharmaceuticals Pte Ltd | Derivado de anel inibidor de btk, método de preparação para o mesmo e aplicação farmacêutica do mesmo |
| 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 |
| 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 |
| CN113950327A (zh) * | 2019-06-10 | 2022-01-18 | 百济神州瑞士有限责任公司 | 口服胶囊剂及其制备方法 |
| 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 |
| 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 |
| KR102801205B1 (ko) * | 2019-12-04 | 2025-04-29 | 허난 즈웨이 바이오메디슨 씨오., 엘티디. | 브루톤 티로신 키나제 억제제인 이미다졸 카복사마이드 유도체 |
| 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 |
| 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 |
| 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 |
| CN115175678B (zh) * | 2020-02-27 | 2024-12-27 | 百济神州瑞士有限责任公司 | 使用btk抑制剂及其组合治疗dlbcl的方法 |
| WO2021259732A1 (en) | 2020-06-24 | 2021-12-30 | Sandoz Ag | Multi-component compounds comprising zanubrutinib and a benzoic acid derivative |
| US20230248833A1 (en) | 2020-07-07 | 2023-08-10 | Sichuan Haisco Pharmaceutical Co., Ltd. | Compound having btk kinase degrading activity, and preparation method and pharmaceutical use therefor |
| 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 |
| JP2023550416A (ja) * | 2020-11-20 | 2023-12-01 | ベイジーン スウィッツァーランド ゲーエムベーハー | Ｂｔｋ阻害剤を用いて全身性エリテマトーデスを治療する方法 |
| US20240124461A1 (en) | 2020-12-11 | 2024-04-18 | 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 |
Family Cites Families (118)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE792533A (fr) | 1971-12-09 | 1973-06-08 | Int Chem & Nuclear Corp | Nouvelles pyrazolo (1,5a) pyrimidines et leur procede de preparation |
| JP2778921B2 (ja) | 1994-11-18 | 1998-07-23 | 三共株式会社 | イミダゾピラゾール誘導体 |
| ES2222919T3 (es) | 1999-08-27 | 2005-02-16 | Abbott Laboratories | Compuestos sulfonilfenilpirazoles utiles como inhibidores de cox-2. |
| DE60004685T2 (de) * | 1999-09-17 | 2004-07-29 | Abbott Gmbh & Co. Kg | Pyrazolopyrimidine als arzneimittel |
| EP1322750A4 (en) | 2000-09-08 | 2004-09-29 | California Inst Of Techn | PROTEOLYSIS TARGET DRUG TARGET MEDICINE |
| US20020094989A1 (en) * | 2000-10-11 | 2002-07-18 | Hale Jeffrey J. | Pyrrolidine modulators of CCR5 chemokine receptor activity |
| DK1347971T3 (da) | 2000-12-21 | 2006-05-15 | Bristol Myers Squibb Co | Thiazolylinhibitorer af tyrosinkinaser fra Tec-familien |
| US6642256B2 (en) * | 2000-12-21 | 2003-11-04 | Warner-Lambert Company Llc | Piperidine derivatives as subtype selective N-Methyl-D-Aspartate antagonists |
| WO2002072576A1 (en) | 2001-03-09 | 2002-09-19 | Pfizer Products Inc. | Benzimidazole anti-inflammatory compounds |
| JPWO2003004497A1 (ja) | 2001-07-05 | 2004-10-28 | 住友製薬株式会社 | 新規複素環化合物 |
| US20040132101A1 (en) | 2002-09-27 | 2004-07-08 | Xencor | Optimized Fc variants and methods for their generation |
| AU2003265585B2 (en) | 2002-08-26 | 2008-07-03 | Takeda Pharmaceutical Company Limited | Calcium receptor modulating compound and use thereof |
| CN1771231B (zh) | 2002-08-26 | 2011-05-25 | 武田药品工业株式会社 | 钙受体调节性化合物及其用途 |
| WO2005014599A1 (en) | 2003-06-04 | 2005-02-17 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds |
| US20060183746A1 (en) | 2003-06-04 | 2006-08-17 | Currie Kevin S | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds |
| WO2005005429A1 (en) | 2003-06-30 | 2005-01-20 | Cellular Genomics, Inc. | Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds |
| MXPA06001098A (es) | 2003-07-29 | 2006-04-24 | Irm Llc | Compuestos y composiciones utiles como inhibidores de proteina cinasa. |
| WO2005047290A2 (en) | 2003-11-11 | 2005-05-26 | Cellular Genomics Inc. | Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors |
| SG159549A1 (en) | 2004-11-10 | 2010-03-30 | Cgi Pharmaceuticals Inc | Imidazo[1,2-a] pyrazin-8-ylamines useful as modulators of kinase activity |
| RU2423351C2 (ru) | 2004-12-16 | 2011-07-10 | Вертекс Фармасьютикалз Инкорпорейтед | Пирид-2-оны, применимые как ингибиторы протеинкиназ семейства тес для лечения воспалительных, пролиферативных и иммунологически-опосредованных заболеваний |
| BRPI0608252A2 (pt) | 2005-03-10 | 2010-04-06 | Cgi Pharmaceuticals Inc | entidades quìmicas, composições farmacêuticas compreendendo as mesmas, métodos utilizando as referidas entidades quìmicas e uso das referidas entidades quìmicas |
| EP1919906B1 (en) | 2005-08-29 | 2011-10-12 | Vertex Pharmaceuticals Incorporated | 3, 5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases |
| JP2009507792A (ja) | 2005-08-29 | 2009-02-26 | バーテックス ファーマシューティカルズ インコーポレイテッド | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| WO2007026720A1 (ja) * | 2005-08-31 | 2007-03-08 | Taisho Pharmaceutical Co., Ltd. | 縮環ピラゾール誘導体 |
| BRPI0617100A2 (pt) | 2005-09-01 | 2011-07-12 | Astellas Pharma Inc | composto derivado de piridazinona, composição farmacêutica, método para previnir ou tratar uma doença e uso de um composto derivado de piridazinona |
| CN101421269A (zh) | 2006-01-13 | 2009-04-29 | 环状药物公司 | 酪氨酸激酶抑制剂及其用途 |
| US8604031B2 (en) | 2006-05-18 | 2013-12-10 | Mannkind Corporation | Intracellular kinase inhibitors |
| TWI398252B (zh) | 2006-05-26 | 2013-06-11 | Novartis Ag | 吡咯并嘧啶化合物及其用途 |
| AR063946A1 (es) | 2006-09-11 | 2009-03-04 | Cgi Pharmaceuticals Inc | Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. |
| JP2010502751A (ja) | 2006-09-11 | 2010-01-28 | シージーアイ ファーマシューティカルズ，インコーポレイティド | キナーゼ阻害物質、およびキナーゼ阻害物質の使用および同定方法 |
| AR063706A1 (es) | 2006-09-11 | 2009-02-11 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. |
| PE20081370A1 (es) | 2006-09-11 | 2008-11-28 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas |
| PT2201840E (pt) | 2006-09-22 | 2012-02-14 | Pharmacyclics Inc | Inibidores da tirosina quinase de bruton |
| AU2007308045A1 (en) | 2006-10-06 | 2008-04-17 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| EP2089391B1 (en) | 2006-11-03 | 2013-01-16 | Pharmacyclics, Inc. | Bruton's tyrosine kinase activity probe and method of using |
| EP2125819B1 (en) | 2007-03-21 | 2014-10-22 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful for the treatment of proliferative, allergic, autoimmune or inflammatory diseases |
| WO2008144253A1 (en) | 2007-05-14 | 2008-11-27 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| CL2008002793A1 (es) | 2007-09-20 | 2009-09-04 | Cgi Pharmaceuticals Inc | Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| CA2702674C (en) | 2007-10-19 | 2016-05-03 | Avila Therapeutics, Inc. | Heteroaryl compounds and uses thereof |
| CA2701275C (en) | 2007-10-23 | 2016-06-21 | F. Hoffmann-La Roche Ag | Kinase inhibitors |
| ES2462642T3 (es) | 2007-12-14 | 2014-05-26 | F. Hoffmann-La Roche Ag | Nuevos derivados de imidazo[1,2-a]piridina e imidazo[1,2-b]piridazina |
| CA2710462C (en) | 2008-02-05 | 2015-11-24 | F. Hoffmann-La Roche Ag | Pyridinones and pyridazinones |
| AU2009244291B2 (en) | 2008-05-06 | 2014-02-13 | Genentech, Inc. | Substituted amides, method of making, and use as Btk inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| TWI458721B (zh) | 2008-06-27 | 2014-11-01 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| JP5490789B2 (ja) | 2008-07-02 | 2014-05-14 | エフ．ホフマン−ラ ロシュ アーゲー | キナーゼ阻害剤としての新規なフェニルピラジノン |
| ES2552681T3 (es) | 2008-07-15 | 2015-12-01 | F. Hoffmann-La Roche Ag | Nuevas fenil-imidazopiridinas y piridazinas |
| AU2009270856B2 (en) | 2008-07-16 | 2013-07-25 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors |
| EP2307418B1 (en) | 2008-07-18 | 2014-03-12 | F.Hoffmann-La Roche Ag | Novel phenylimidazopyrazines |
| JP2011529073A (ja) | 2008-07-24 | 2011-12-01 | ブリストル−マイヤーズ スクイブ カンパニー | キナーゼ調節因子として有用な縮合ヘテロ環化合物 |
| CN102405284B (zh) | 2008-09-05 | 2016-01-20 | 新基阿维罗米克斯研究公司 | 设计不可逆抑制剂的算法 |
| EP2348860B1 (en) | 2008-10-31 | 2015-05-27 | Genentech, Inc. | Pyrazolopyrimidine jak inhibitor compounds and methods |
| US20120028981A1 (en) | 2008-11-05 | 2012-02-02 | Principia Biopharma Inc. | Kinase Knockdown Via Electrophilically Enhanced Inhibitors |
| WO2010056875A1 (en) | 2008-11-12 | 2010-05-20 | Cgi Pharmaceuticals, Inc. | Pyridazinones and their use as btk inhibitors |
| US8426428B2 (en) | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
| WO2010068810A2 (en) | 2008-12-10 | 2010-06-17 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
| WO2010068806A1 (en) | 2008-12-10 | 2010-06-17 | Cgi Pharmaceuticals, Inc. | Amide derivatives as btk inhibitors in the treatment of allergic, autoimmune and inflammatory disorders as well as cancer |
| WO2010068788A1 (en) | 2008-12-10 | 2010-06-17 | Cgi Pharmaceuticals, Inc. | Heterocyclic amides as btk inhibitors |
| SG171815A1 (en) | 2008-12-19 | 2011-07-28 | Bristol Myers Squibb Co | Carbazole carboxamide compounds useful as kinase inhibitors |
| EP2379559B1 (en) | 2009-01-06 | 2017-10-25 | Dana-Farber Cancer Institute, Inc. | Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders |
| US8299077B2 (en) | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| ES2513915T3 (es) | 2009-04-24 | 2014-10-27 | F. Hoffmann-La Roche Ag | Inhibidores de la tirosina quinasa de Bruton |
| EP2424368B1 (en) | 2009-04-29 | 2014-12-31 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
| ES2444777T3 (es) | 2009-06-12 | 2014-02-26 | Bristol-Myers Squibb Company | Compuestos de nicotinamida útiles como moduladores de quinasas |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| EP2789615B1 (en) | 2009-08-11 | 2017-05-03 | Bristol-Myers Squibb Company | Azaindazoles as Btk kinase modulators and use thereof |
| US9029359B2 (en) | 2009-09-04 | 2015-05-12 | Biogen Idec Ma, Inc. | Heteroaryl Btk inhibitors |
| PL2473049T3 (pl) | 2009-09-04 | 2019-07-31 | Biogen Ma Inc. | Inhibitory kinazy tyrozynowej brutona |
| US7741330B1 (en) * | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
| ES2573716T3 (es) | 2010-05-07 | 2016-06-09 | Gilead Connecticut, Inc. | Compuestos de piridona y aza-piridona y métodos de utilización |
| MY169745A (en) | 2010-05-31 | 2019-05-14 | Ono Pharmaceutical Co | Purinone derivative |
| EA201890869A3 (ru) | 2010-06-03 | 2019-03-29 | Фармасайкликс, Инк. | Применение ингибиторов тирозинкиназы брутона (btk) |
| EP2582668B1 (en) | 2010-06-16 | 2016-01-13 | Bristol-Myers Squibb Company | Carboline carboxamide compounds useful as kinase inhibitors |
| LT2585470T (lt) | 2010-06-23 | 2017-04-10 | Hanmi Science Co., Ltd. | Nauji kondensuoti pirimidino dariniai tirozino kinazės aktyvumo slopinimui |
| US20120053189A1 (en) | 2010-06-28 | 2012-03-01 | Pharmacyclics, Inc. | Btk inhibitors for the treatment of immune mediated conditions |
| RU2013109393A (ru) | 2010-08-10 | 2014-09-20 | Сэлджин Авиаломикс Ресеарч, Инк. | Безилатная соль ингибитора втк |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
| EP2611798B1 (en) | 2010-09-01 | 2015-04-08 | Gilead Connecticut, Inc. | Pyridazinones, method of making, and method of use thereof |
| CN103189369B (zh) | 2010-09-01 | 2016-08-24 | 吉利德康涅狄格有限公司 | 吡啶酮/吡嗪酮、其制备方法及使用方法 |
| WO2012135801A1 (en) | 2011-04-01 | 2012-10-04 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| CA2760174A1 (en) | 2011-12-01 | 2013-06-01 | Pharmascience Inc. | Protein kinase inhibitors and uses thereof |
| US20140038989A1 (en) | 2011-04-20 | 2014-02-06 | Glaxo Group Limited | Tetrahydropyrazolo [1,5-a] pyrimidine as anti-tuberculosis compounds |
| PL2710005T3 (pl) | 2011-05-17 | 2017-07-31 | Principia Biopharma Inc. | Inhibitory kinazy tyrozynowej |
| US9376438B2 (en) | 2011-05-17 | 2016-06-28 | Principia Biopharma, Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| BR112013029620A2 (pt) | 2011-05-17 | 2016-09-06 | Hoffmann La Roche | inibidores de tirosina quinase de bruton |
| US20140107151A1 (en) | 2011-05-17 | 2014-04-17 | Principia Biophama Inc. | Tyrosine kinase inhibitors |
| SG10201604682VA (en) | 2011-06-10 | 2016-07-28 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
| ES2548414T3 (es) | 2011-07-08 | 2015-10-16 | Novartis Ag | Novedosos derivados de pirrolo pirimidina |
| BR112015025260B1 (pt) | 2013-04-25 | 2021-11-03 | Beigene, Ltd | Compostos heterocíclicos fundidos como inibidores da proteína quinase, sua composição, combinação e uso |
| RS63571B9 (sr) | 2013-09-13 | 2023-02-28 | Beigene Switzerland Gmbh | Anti-pd1 antitela i njihova primena kao terapeutska i dijagnostička sredstva |
| TWI660739B (zh) | 2013-10-25 | 2019-06-01 | 製藥公司 | 使用布魯頓氏酪胺酸激酶抑制劑之治療及免疫療法 |
| US10544225B2 (en) | 2014-07-03 | 2020-01-28 | Beigene, Ltd. | Anti-PD-L1 antibodies and their use as therapeutics and diagnostics |
| TW201607930A (zh) * | 2014-07-18 | 2016-03-01 | 百濟神州有限公司 | 作為ｔ７９０ｍ／ｗｔ－ｅｇｆｒ的選擇性和不可逆的激酶抑制劑的５－氨基－４－氨甲醯基－吡唑化合物及其用途 |
| US20170239351A1 (en) | 2014-08-11 | 2017-08-24 | Acerta Pharma B.V. | Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, a PD-1 Inhibitor, and/or a PD-L1 Inhibitor |
| CA2958139A1 (en) | 2014-08-14 | 2016-02-18 | Assia Chemical Industries Ltd. | Solid state forms of ibrutinib |
| WO2016087994A1 (en) | 2014-12-05 | 2016-06-09 | Acerta Pharma B.V. | Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment |
| CA2970723C (en) * | 2014-12-18 | 2023-09-05 | Principia Biopharma Inc. | Treatment of pemphigus |
| HUE061809T2 (hu) * | 2014-12-24 | 2023-08-28 | Principia Biopharma Inc | Készítmények csípõbél-éhbél szakaszba történõ hatóanyag beadáshoz |
| US9717745B2 (en) | 2015-03-19 | 2017-08-01 | Zhejiang DTRM Biopharma Co. Ltd. | Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases |
| US20190022092A1 (en) | 2015-09-15 | 2019-01-24 | Acerta Pharma B.V. | Therapeutic Combinations of a BTK Inhibitor and a GITR Binding Molecule, a 4-1BB Agonist, or an OX40 Agonist |
| JP2018530550A (ja) | 2015-10-01 | 2018-10-18 | ギリアド サイエンシズ， インコーポレイテッド | 癌を治療するためのｂｔｋ阻害剤とチェックポイント阻害剤との組合せ |
| CN107530348B (zh) | 2016-02-19 | 2020-10-20 | 江苏恒瑞医药股份有限公司 | 一种含有jak激酶抑制剂或其可药用盐的药物组合物 |
| JP7402685B2 (ja) | 2016-08-16 | 2023-12-21 | ベイジーン スウィッツァーランド ゲーエムベーハー | （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 |
| AU2017313085B2 (en) | 2016-08-19 | 2024-06-20 | Beone Medicines I Gmbh | Use of a combination comprising a Btk inhibitor for treating cancers |
| TW201818936A (zh) | 2016-11-25 | 2018-06-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種吡啶酮類衍生物醫藥組成物及其製備方法 |
| 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 |
| KR20190137151A (ko) | 2017-04-20 | 2019-12-10 | 에이디씨 테라퓨틱스 에스에이 | 병용 요법 |
| WO2019001417A1 (en) | 2017-06-26 | 2019-01-03 | Beigene, Ltd. | IMMUNOTHERAPY FOR HEPATOCELLULAR CARCINOMA |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
| SG11202009137PA (en) | 2018-03-21 | 2020-10-29 | Mei Pharma Inc | Combination therapy |
| CN113950327A (zh) | 2019-06-10 | 2022-01-18 | 百济神州瑞士有限责任公司 | 口服胶囊剂及其制备方法 |
| 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 |
| US20220281876A1 (en) | 2019-07-26 | 2022-09-08 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| US20220387404A1 (en) | 2019-09-11 | 2022-12-08 | Beigene, Ltd. | Treatment of cancer using a combination comprising multi-tyrosine kinase inhibitor and immune checkpoint inhibitor |
| CN114729050A (zh) | 2019-11-21 | 2022-07-08 | 百济神州有限公司 | 使用抗OX40抗体与PI3激酶δ抑制剂组合治疗癌症的方法 |
| CN115175678B (zh) | 2020-02-27 | 2024-12-27 | 百济神州瑞士有限责任公司 | 使用btk抑制剂及其组合治疗dlbcl的方法 |
-
2017
- 2017-08-15 JP JP2019508889A patent/JP7402685B2/ja active Active
- 2017-08-15 EP EP24217178.3A patent/EP4509183A3/en active Pending
- 2017-08-15 IL IL293319A patent/IL293319A/en unknown
- 2017-08-15 EP EP17841172.4A patent/EP3500575B1/en active Active
- 2017-08-15 KR KR1020197007529A patent/KR102604975B1/ko active Active
- 2017-08-15 EP EP24160079.0A patent/EP4353322A3/en active Pending
- 2017-08-15 TW TW106127682A patent/TWI760356B/zh active
- 2017-08-15 NZ NZ751418A patent/NZ751418A/en unknown
- 2017-08-15 TW TW111117667A patent/TWI865873B/zh active
- 2017-08-15 SG SG11201901141WA patent/SG11201901141WA/en unknown
- 2017-08-15 EA EA201990519A patent/EA201990519A1/ru unknown
- 2017-08-15 CN CN202310119012.5A patent/CN116478166A/zh active Pending
- 2017-08-15 AU AU2017314178A patent/AU2017314178B2/en active Active
- 2017-08-15 CN CN201780049930.8A patent/CN109563099B/zh active Active
- 2017-08-15 CA CA3033827A patent/CA3033827A1/en active Pending
- 2017-08-15 US US16/325,447 patent/US10927117B2/en active Active
- 2017-08-15 TW TW113147712A patent/TWI884890B/zh active
- 2017-08-15 CN CN202310094009.2A patent/CN116478165A/zh active Pending
- 2017-08-15 WO PCT/IB2017/054955 patent/WO2018033853A2/en not_active Ceased
- 2017-08-15 MX MX2019001900A patent/MX384627B/es unknown
- 2017-08-15 IL IL264784A patent/IL264784B/en unknown
- 2017-08-15 KR KR1020237039678A patent/KR102793825B1/ko active Active
- 2017-08-15 KR KR1020257011064A patent/KR20250052473A/ko not_active Ceased
-
2019
- 2019-02-13 ZA ZA2019/00919A patent/ZA201900919B/en unknown
-
2021
- 2021-01-12 US US17/146,855 patent/US20210130363A1/en not_active Abandoned
-
2022
- 2022-01-17 AU AU2022200278A patent/AU2022200278B2/en active Active
- 2022-03-01 JP JP2022030942A patent/JP7413419B2/ja active Active
- 2022-05-10 US US17/740,877 patent/US20220274994A1/en not_active Abandoned
- 2022-05-10 US US17/740,882 patent/US11591340B2/en active Active
- 2022-07-06 US US17/858,826 patent/US11884674B2/en active Active
- 2022-07-06 US US17/858,827 patent/US11814389B2/en active Active
- 2022-09-02 US US17/901,951 patent/US11851437B2/en active Active
-
2023
- 2023-03-07 US US18/118,555 patent/US20230242542A1/en not_active Abandoned
- 2023-10-19 US US18/381,767 patent/US11999743B2/en active Active
- 2023-11-03 US US18/386,777 patent/US12103931B2/en active Active
- 2023-12-01 US US18/526,535 patent/US11970500B1/en active Active
- 2023-12-27 JP JP2023220256A patent/JP7637459B2/ja active Active
-
2024
- 2024-01-03 AU AU2024200030A patent/AU2024200030A1/en active Pending
- 2024-08-21 US US18/810,987 patent/US20240409546A1/en active Pending
-
2025
- 2025-02-13 JP JP2025021657A patent/JP2025081429A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2022071072A5 (enExample) | ||
| JP2024026550A5 (enExample) | ||
| JP2019528276A5 (enExample) | ||
| JP2022121594A5 (enExample) | ||
| CN105646584B (zh) | 替诺福韦艾拉酚胺富马酸盐晶型及其制备方法和用途 | |
| AU2023200013B2 (en) | Methods for making and using endoxifen | |
| CN102351857B (zh) | 盐酸托烷司琼化合物 | |
| CN107249591A (zh) | 治疗癌症的方法 | |
| JP2015512942A5 (enExample) | ||
| CN1970547B (zh) | 非布司他的晶型及其制备方法 | |
| FI3856341T3 (fi) | (s)-1-(4-fluorifenyyli)-1-(2-(4-(6-(1-metyyli-1h-pyratsol-4-yyli)pyrrolo[2,1-f][1,2,4]triatsin-4-yyli)piperatsinyyli)pyrimidin-5-yyli)etaani-1-amiinin kidemuotoja ja valmistusmenetelmiä | |
| TW202200594A (zh) | 一種glp-1受體激動劑的晶型a及其製備方法 | |
| CN102367252A (zh) | 一种盐酸托烷司琼化合物 | |
| JP2014144916A (ja) | ２−アシルアミノチアゾール化合物の結晶 | |
| TW202340135A (zh) | （ｚ）—因多昔芬之組合物及其富集方法 | |
| US10556863B1 (en) | Crystalline form of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, preparation method therefor and use thereof | |
| JP2013526491A (ja) | メチソシルデナフィル・クエン酸塩結晶型ｏ及びその調製方法並びに応用 | |
| US20210171536A1 (en) | Compound of eoc315 mod.i crystal form and preparation method thereof | |
| WO2017017301A1 (es) | Formas cristalinas de bilastina y procedimientos para su preparación | |
| JPWO2020051538A5 (enExample) | ||
| WO2014056396A1 (zh) | 甲磺酸氟马替尼晶型及其制备方法和用途 | |
| CN102241608A (zh) | 瑞替加滨化合物及其组合物 | |
| CN116710102A (zh) | 一种五环三萜类化合物结晶及其制备方法 | |
| CN101993417A (zh) | 磷酸二甲啡烷的稳定新晶型 | |
| JP2020524707A (ja) | 塩酸メフパリブの多形体およびその製造方法と使用 |