JP2016521273A5 - - Google Patents
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- JP2016521273A5 JP2016521273A5 JP2016509281A JP2016509281A JP2016521273A5 JP 2016521273 A5 JP2016521273 A5 JP 2016521273A5 JP 2016509281 A JP2016509281 A JP 2016509281A JP 2016509281 A JP2016509281 A JP 2016509281A JP 2016521273 A5 JP2016521273 A5 JP 2016521273A5
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- JP
- Japan
- Prior art keywords
- substituted
- aryl
- cycloalkyl
- alkyl
- saturated
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 28
- 125000003118 aryl group Chemical group 0.000 claims 25
- 125000001072 heteroaryl group Chemical group 0.000 claims 23
- 125000000623 heterocyclic group Chemical group 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000000753 cycloalkyl group Chemical group 0.000 claims 22
- 229920006395 saturated elastomer Polymers 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 125000003342 alkenyl group Chemical group 0.000 claims 15
- 125000003545 alkoxy group Chemical group 0.000 claims 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 15
- 125000001424 substituent group Chemical group 0.000 claims 13
- 125000000304 alkynyl group Chemical group 0.000 claims 10
- 125000004429 atom Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 8
- 125000004404 heteroalkyl group Chemical group 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- -1 propioyl Chemical group 0.000 claims 4
- TVTJUIAKQFIXCE-HUKYDQBMSA-N 2-amino-9-[(2R,3S,4S,5R)-4-fluoro-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-prop-2-ynyl-1H-purine-6,8-dione Chemical compound NC=1NC(C=2N(C(N(C=2N=1)[C@@H]1O[C@@H]([C@H]([C@H]1O)F)CO)=O)CC#C)=O TVTJUIAKQFIXCE-HUKYDQBMSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 229940125851 compound 27 Drugs 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 125000003647 acryloyl group Chemical group O=C([*])C([H])=C([H])[H] 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 206010052178 Lymphocytic lymphoma Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 238000000021 kinase assay Methods 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2013/074728 | 2013-04-25 | ||
| CNPCT/CN2013/074728 | 2013-04-25 | ||
| PCT/CN2014/075943 WO2014173289A1 (en) | 2013-04-25 | 2014-04-22 | Fused heterocyclic compounds as protein kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016521273A JP2016521273A (ja) | 2016-07-21 |
| JP2016521273A5 true JP2016521273A5 (enExample) | 2017-04-06 |
| JP6204568B2 JP6204568B2 (ja) | 2017-09-27 |
Family
ID=51791057
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016509281A Active JP6204568B2 (ja) | 2013-04-25 | 2014-04-22 | タンパク質キナーゼ阻害剤としての縮合複素環化合物 |
Country Status (29)
| Country | Link |
|---|---|
| US (8) | US9447106B2 (enExample) |
| EP (1) | EP2989106B1 (enExample) |
| JP (1) | JP6204568B2 (enExample) |
| KR (1) | KR101793807B1 (enExample) |
| CN (1) | CN104884458B (enExample) |
| AU (1) | AU2014256633B2 (enExample) |
| BR (1) | BR112015025260B1 (enExample) |
| CA (1) | CA2902686C (enExample) |
| CY (2) | CY1118834T1 (enExample) |
| DK (1) | DK2989106T3 (enExample) |
| EA (1) | EA028756B1 (enExample) |
| ES (1) | ES2619125T3 (enExample) |
| FR (1) | FR22C1010I2 (enExample) |
| HR (1) | HRP20170217T1 (enExample) |
| HU (2) | HUE031980T2 (enExample) |
| LT (2) | LT2989106T (enExample) |
| LU (1) | LUC00250I2 (enExample) |
| MX (1) | MX367918B (enExample) |
| NL (1) | NL301161I2 (enExample) |
| NO (1) | NO2022005I1 (enExample) |
| NZ (1) | NZ711540A (enExample) |
| PL (1) | PL2989106T3 (enExample) |
| PT (1) | PT2989106T (enExample) |
| RS (1) | RS55770B1 (enExample) |
| SG (1) | SG11201506764WA (enExample) |
| SI (1) | SI2989106T1 (enExample) |
| SM (1) | SMT201700160T1 (enExample) |
| WO (1) | WO2014173289A1 (enExample) |
| ZA (1) | ZA201508504B (enExample) |
Families Citing this family (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2902686C (en) * | 2013-04-25 | 2017-01-24 | Beigene, Ltd. | Fused heterocyclic compounds as protein kinase inhibitors |
| CN112552401B (zh) | 2013-09-13 | 2023-08-25 | 广州百济神州生物制药有限公司 | 抗pd1抗体及其作为治疗剂与诊断剂的用途 |
| KR102272792B1 (ko) | 2013-09-30 | 2021-07-05 | 광저우 이노케어 파마 테크 씨오., 엘티디. | Ｂｔｋ의 치환된 니코틴이미드 저해제 및 그의 제조 방법 및 암, 염증 및 자가면역 질환에의 용도 |
| US9937171B2 (en) | 2014-04-11 | 2018-04-10 | Acerta Pharma B.V. | Methods of blocking the CXCR-4/SDF-1 signaling pathway with inhibitors of bruton's tyrosine kinase |
| WO2015185998A2 (en) | 2014-04-11 | 2015-12-10 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase |
| MX388871B (es) | 2014-06-27 | 2025-03-20 | Nogra Pharma Ltd | Moduladores del receptor arilo y metodos para elaborar y usar los mismos. |
| 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 |
| TW201618783A (zh) | 2014-08-07 | 2016-06-01 | 艾森塔製藥公司 | 以布魯頓(Bruton)氏酪胺酸激酶(BTK)佔據和BTK再合成速率為基礎之治療癌症、免疫和自體免疫疾病及發炎性疾病之方法 |
| PL3179991T3 (pl) | 2014-08-11 | 2022-02-14 | Acerta Pharma B.V. | Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2 |
| TW201618774A (zh) | 2014-08-11 | 2016-06-01 | 艾森塔製藥公司 | 使用ｂｔｋ抑制劑透過調變腫瘤微環境來治療實體腫瘤及其他疾病之方法 |
| TW201618775A (zh) | 2014-08-11 | 2016-06-01 | 艾森塔製藥公司 | Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、ｐｄ－１抑制劑及／或ｐｄ－ｌ１抑制劑之治療組合物 |
| AR101504A1 (es) | 2014-08-11 | 2016-12-21 | Acerta Pharma Bv | Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6 |
| WO2016071216A1 (en) * | 2014-11-03 | 2016-05-12 | Bayer Pharma Aktiengesellschaft | Piperidinylpyrazolopyrimidinones and their use |
| WO2016087994A1 (en) | 2014-12-05 | 2016-06-09 | Acerta Pharma B.V. | Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment |
| WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| EP3747472B1 (en) | 2015-09-15 | 2024-04-03 | Acerta Pharma B.V. | Therapeutic combinations of a cd19 inhibitor and a btk inhibitor |
| WO2017046746A1 (en) | 2015-09-15 | 2017-03-23 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor and a gitr binding molecule, a 4-1bb agonist, or an ox40 agonist |
| BR112018007664B1 (pt) | 2015-10-16 | 2023-12-19 | Eisai R&D Management Co., Ltd | Compostos antagonistas de ep4, composição compreendendo o composto e uso dos mesmos para tratar câncer |
| CN106588913B (zh) * | 2015-10-16 | 2018-11-02 | 陈剑 | 具有咪唑并吡啶类衍生物，其制备及其在医药上的应用 |
| DK3402503T3 (da) | 2016-01-13 | 2020-12-21 | Acerta Pharma Bv | Terapeutiske kombinationer af et antifolat og en btk-hæmmer |
| CN105732638B (zh) * | 2016-01-22 | 2018-01-30 | 成都倍特药业有限公司 | 一种具有螺环或桥环结构的布鲁顿酪氨酸激酶抑制剂及其制备方法 |
| CN107021963A (zh) | 2016-01-29 | 2017-08-08 | 北京诺诚健华医药科技有限公司 | 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用 |
| US10864203B2 (en) | 2016-07-05 | 2020-12-15 | Beigene, Ltd. | Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer |
| 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 |
| WO2018033135A1 (en) | 2016-08-19 | 2018-02-22 | Beigene, Ltd. | Use of a combination comprising a btk inhibitor for treating cancers |
| IL292938A (en) | 2016-09-19 | 2022-07-01 | Mei Pharma Inc | Combined treatment |
| US11555038B2 (en) | 2017-01-25 | 2023-01-17 | Beigene, Ltd. | Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| EP3645569A4 (en) | 2017-06-26 | 2021-03-24 | BeiGene, Ltd. | IMMUNOTHERAPY FOR LIVER CELL CARCINOMA |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| WO2019086009A1 (zh) * | 2017-11-03 | 2019-05-09 | 华南农业大学 | 含氮稠合三环化合物及其作为农林业杀虫剂的应用 |
| 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 |
| WO2019208805A1 (ja) | 2018-04-27 | 2019-10-31 | 小野薬品工業株式会社 | Ｂｔｋ阻害活性を有する化合物を有効成分として含む自己免疫疾患の予防および／または治療剤 |
| EP3883649A1 (en) | 2018-05-17 | 2021-09-29 | Avidin KFT | Imidazo-pyrazole carboxamide derivatives as anticancer agents and the synthesis thereof |
| CN108484615A (zh) * | 2018-05-25 | 2018-09-04 | 陈海鹏 | 一种化合物、合成方法及其在制备抗肿瘤药物中的用途 |
| CN108558886A (zh) * | 2018-05-25 | 2018-09-21 | 陈海鹏 | 一种含有氰基的三环类化合物及其在制备抗肿瘤药物中的用途 |
| CN108467397A (zh) * | 2018-05-25 | 2018-08-31 | 陈海鹏 | 一种含有氰基的三环类化合物及其在抗肿瘤药物中的用途 |
| KR20210038877A (ko) | 2018-07-25 | 2021-04-08 | 노파르티스 아게 | Nlrp3 인플라마좀 억제제 |
| CA3111126A1 (en) | 2018-08-31 | 2020-03-05 | Stichting Katholieke Universiteit | Synergistic combinations of amino acid depletion agent sensitizers (aadas) and amino acid depletion agents (aada), and therapeutic methods of use thereof |
| 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 |
| AU2020276334B2 (en) | 2019-05-10 | 2022-12-22 | Henan Zhiwei Biomedicine Co., Ltd. | Substituted 1-amino-1H-imidazole-5-carboxamide as Bruton's Tyrosine Kinase inhibitors |
| AR119731A1 (es) | 2019-05-17 | 2022-01-05 | Novartis Ag | Inhibidores del inflamasoma nlrp3 |
| US20220249491A1 (en) * | 2019-06-10 | 2022-08-11 | Beigene Switzerland Gmbh | Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor |
| 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 |
| CN114174299B (zh) * | 2019-07-26 | 2024-10-25 | 百济神州有限公司 | 通过btk抑制剂与e3连接酶配体缀合对布鲁顿氏酪氨酸激酶(btk)的降解以及使用方法 |
| WO2021083135A1 (en) | 2019-10-28 | 2021-05-06 | Beigene, Ltd. | Bcl-2 INHIBITORS |
| ES3060629T3 (en) * | 2019-10-30 | 2026-03-27 | Biogen Ma Inc | Condensed bi-heterocycles as inhibiting agents for bruton's tyrosine kinase |
| 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 |
| US20230089557A1 (en) * | 2020-02-27 | 2023-03-23 | Beigene Switzerland Gmbh | Methods of treating dlbcl using btk inhibitors and combinations thereof |
| IL296582A (en) | 2020-04-15 | 2022-11-01 | Beigene Ltd | bcl-2 inhibitor |
| WO2021259732A1 (en) | 2020-06-24 | 2021-12-30 | Sandoz Ag | Multi-component compounds comprising zanubrutinib and a benzoic acid derivative |
| CN116018138B (zh) * | 2020-07-13 | 2025-08-15 | 河南知微生物医药有限公司 | 作为布鲁诺酪氨酸激酶抑制剂的取代的1H-咪唑并[1,2-b]吡唑-3-甲酰胺 |
| CN113943293A (zh) * | 2020-07-16 | 2022-01-18 | 百济神州(北京)生物科技有限公司 | 用于制备作为protac btk降解剂的双官能化合物的方法 |
| JP7545570B2 (ja) | 2020-08-14 | 2024-09-04 | ノバルティス アーゲー | ヘテロアリール置換スピロピペリジニル誘導体及びその薬学的使用 |
| 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 |
| KR20230107866A (ko) | 2020-11-20 | 2023-07-18 | 베이진 스위찰랜드 게엠베하 | Btk 억제제를 사용한 전신성 홍반성 루푸스의 치료 방법 |
| CN114573586B (zh) * | 2020-11-28 | 2023-11-03 | 杭州和正医药有限公司 | 一种抑制布鲁顿酪氨酸激酶活性的多环化合物、药物组合物及其应用 |
| EP4259633A1 (en) | 2020-12-11 | 2023-10-18 | 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 |
| CN116981675A (zh) * | 2020-12-31 | 2023-10-31 | 百济神州有限公司 | 通过布鲁顿氏酪氨酸激酶（btk）抑制剂与e3连接酶配体的缀合降解btk和使用方法 |
| WO2022161484A1 (en) * | 2021-01-30 | 2022-08-04 | Beigene, Ltd. | Methods of treating chronic active antibody-mediated rejection using btk inhibitors |
| CN116348453B (zh) * | 2021-04-25 | 2025-07-04 | 烨辉医药科技(上海)有限公司 | 杂芳族甲酰胺化合物及其用途 |
| JP2024525181A (ja) * | 2021-06-21 | 2024-07-10 | ベイジーン スウィッツァーランド ゲーエムベーハー | （ｒ）－グルタルイミドｃｒｂｎリガンド及び使用方法 |
| 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 |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
| UY40374A (es) | 2022-08-03 | 2024-02-15 | Novartis Ag | Inhibidores de inflamasoma nlrp3 |
| CN117886822A (zh) * | 2023-12-24 | 2024-04-16 | 神隆医药（常熟）有限公司 | 一种高收率且适于工业化推广的泽布替尼中间体的制备方法 |
Family Cites Families (99)
| 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 |
| JP2003508401A (ja) | 1999-08-27 | 2003-03-04 | アボット・ラボラトリーズ | Ｃｏｘ−２阻害薬として有用なスルホニルフェニルピラゾール化合物 |
| JP2003509428A (ja) | 1999-09-17 | 2003-03-11 | アボツト・ゲー・エム・ベー・ハー・ウント・コンパニー・カーゲー | 治療薬としてのピラゾロピリミジン |
| WO2002050071A1 (en) | 2000-12-21 | 2002-06-27 | Bristol-Myers Squibb Company | Thiazolyl inhibitors of tec family tyrosine kinases |
| AP2002002460A0 (en) | 2001-03-09 | 2002-06-30 | Pfizer Prod Inc | Novel benzimidazole anti-inflammatory compounds. |
| WO2003004497A1 (en) * | 2001-07-05 | 2003-01-16 | Sumitomo Pharmaceuticals Company, Limited | Novel heterocyclic compound |
| EP1572113B1 (en) * | 2002-08-26 | 2017-05-17 | 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 |
| 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 |
| US7405295B2 (en) | 2003-06-04 | 2008-07-29 | Cgi Pharmaceuticals, Inc. | 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 |
| WO2005011597A2 (en) | 2003-07-29 | 2005-02-10 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| WO2005047290A2 (en) | 2003-11-11 | 2005-05-26 | Cellular Genomics Inc. | Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors |
| AU2005304473A1 (en) | 2004-11-10 | 2006-05-18 | Cgi Pharmaceuticals, Inc. | Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity |
| US8101770B2 (en) | 2004-12-16 | 2012-01-24 | Vertex Pharmaceuticals Incorporated | Pyridones useful as inhibitors of kinases |
| MX2007011041A (es) | 2005-03-10 | 2008-02-22 | Cgi Pharmaceuticals Inc | Ciertas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas. |
| 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 |
| ATE548363T1 (de) | 2005-08-29 | 2012-03-15 | Vertex Pharma | 3,5-disubstituierte pyrid-2-one, die sich als inhibitoren der tec-familie von nicht-rezeptor- tyrosinkinasen eignen |
| WO2007026720A1 (ja) * | 2005-08-31 | 2007-03-08 | Taisho Pharmaceutical Co., Ltd. | 縮環ピラゾール誘導体 |
| WO2007026950A1 (en) | 2005-09-01 | 2007-03-08 | Astellas Pharma Inc. | Pyridazinone derivatives used for the treatment of pain |
| KR20080098490A (ko) | 2006-01-13 | 2008-11-10 | 파마시클릭스, 인코포레이티드 | 티로신 키나제 억제제 및 이의 용도 |
| WO2007136790A2 (en) | 2006-05-18 | 2007-11-29 | Mannkind Corporation | Intracellular kinase inhibitors |
| TWI398252B (zh) | 2006-05-26 | 2013-06-11 | 諾華公司 | 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. |
| WO2008033858A2 (en) | 2006-09-11 | 2008-03-20 | Cgi Pharmaceuticals, Inc. | Kinase inhibitors, and methods of using and identifying kinase inhibitors |
| PE20081370A1 (es) | 2006-09-11 | 2008-11-28 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas |
| 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. |
| DK2526933T3 (en) | 2006-09-22 | 2015-05-18 | Pharmacyclics Inc | Inhibitors of Bruton's tyrosine kinase |
| JP2010505859A (ja) | 2006-10-06 | 2010-02-25 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤およびそれを使用するための方法 |
| CA2668286C (en) | 2006-11-03 | 2014-09-16 | Pharmacyclics, Inc. | Bruton's tyrosine kinase activity probe and method of using |
| CN101730699A (zh) | 2007-03-21 | 2010-06-09 | 百时美施贵宝公司 | 可用于治疗增殖性、变应性、自身免疫性和炎症性疾病的稠合杂环化合物 |
| 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 |
| TWI552752B (zh) | 2007-10-19 | 2016-10-11 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
| CN101835755B (zh) | 2007-10-23 | 2013-12-11 | 霍夫曼-拉罗奇有限公司 | 激酶抑制剂 |
| JP5643105B2 (ja) | 2007-12-14 | 2014-12-17 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 新規イミダゾ［１，２−ａ］ピリジン及びイミダゾ［１，２−ｂ］ピリダジン誘導体 |
| PL2242749T3 (pl) | 2008-02-05 | 2013-09-30 | Hoffmann La Roche | Nowe pirydynony i pirydazynony |
| CA2723237A1 (en) | 2008-05-06 | 2009-11-12 | Peter A. Blomgren | Substituted amides, method of making, and use as btk inhibitors |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| PE20110164A1 (es) | 2008-07-02 | 2011-03-28 | Hoffmann La Roche | Nuevas fenilpirazinonas como inhibidores de quinasa |
| WO2010006947A1 (en) | 2008-07-15 | 2010-01-21 | F. Hoffmann-La Roche Ag | Novel phenyl-imidazopyridines and pyridazines |
| CA2730930C (en) | 2008-07-16 | 2015-01-13 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| ES2461494T3 (es) | 2008-07-18 | 2014-05-20 | F. Hoffmann-La Roche Ag | Nuevas fenilimidazopirazinas |
| US8476430B2 (en) | 2008-07-24 | 2013-07-02 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| JP2012501654A (ja) | 2008-09-05 | 2012-01-26 | アビラ セラピューティクス， インコーポレイテッド | 不可逆的インヒビターの設計のためのアルゴリズム |
| 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 |
| US8598174B2 (en) | 2008-11-12 | 2013-12-03 | Genetech, Inc. | Pyridazinones, method of making, and method of use thereof |
| US8426428B2 (en) | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
| 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 |
| WO2010068810A2 (en) | 2008-12-10 | 2010-06-17 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
| US8084620B2 (en) | 2008-12-19 | 2011-12-27 | Bristol-Myers Squibb Company | Carbazole carboxamide compounds useful as kinase inhibitors |
| EP3828185B1 (en) | 2009-01-06 | 2024-11-20 | 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 |
| WO2010122038A1 (en) | 2009-04-24 | 2010-10-28 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| US8765754B2 (en) | 2009-04-29 | 2014-07-01 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
| EP2440204B1 (en) | 2009-06-12 | 2013-12-18 | Bristol-Myers Squibb Company | Nicotinamide compounds useful as kinase modulators |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| US8846673B2 (en) | 2009-08-11 | 2014-09-30 | Bristol-Myers Squibb Company | Azaindazoles as kinase inhibitors and use thereof |
| NZ598985A (en) | 2009-09-04 | 2013-07-26 | Biogen Idec Inc | Bruton's tyrosine kinase inhibitors |
| EP2485589A4 (en) | 2009-09-04 | 2013-02-06 | Biogen Idec Inc | HETEROARYL-BTK INHIBITORS |
| US7718662B1 (en) | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| EP2566869B1 (en) | 2010-05-07 | 2016-03-02 | Gilead Connecticut, Inc. | Pyridone and aza-pyridone compounds and methods of use |
| TWI500617B (zh) | 2010-05-31 | 2015-09-21 | Ono Pharmaceutical Co | Purine ketone derivatives |
| CA3007787C (en) | 2010-06-03 | 2020-03-10 | Pharmacyclics Llc | The use of inhibitors of bruton's tyrosine kinase (btk) |
| WO2011159857A1 (en) | 2010-06-16 | 2011-12-22 | Bristol-Myers Squibb Company | Carboline carboxamide compounds useful as kinase inhibitors |
| MX342164B (es) | 2010-06-23 | 2016-09-19 | Hanmi Science Co Ltd | Derivados de pirimidina fusionados novedosos para la inhibicion de la actividad de tirosina cinasa. |
| US20120053189A1 (en) | 2010-06-28 | 2012-03-01 | Pharmacyclics, Inc. | Btk inhibitors for the treatment of immune mediated conditions |
| MX336875B (es) | 2010-08-10 | 2016-02-04 | Celgene Avilomics Res Inc | Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk). |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
| CA2809836C (en) | 2010-09-01 | 2019-01-15 | Gilead Connecticut, Inc. | Pyridinones/pyrazinones, method of making, and method of use thereof for the treatment of disorders mediated by bruton's tyrosine kinase |
| US8975260B2 (en) | 2010-09-01 | 2015-03-10 | Genetech, Inc | Pyridazinones, method of making, and method of use thereof |
| JP6147727B2 (ja) | 2011-04-01 | 2017-06-14 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼｂｔｋ阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| CA2760174A1 (en) | 2011-12-01 | 2013-06-01 | Pharmascience Inc. | Protein kinase inhibitors and uses thereof |
| CN103596958A (zh) * | 2011-04-20 | 2014-02-19 | 葛兰素集团有限公司 | 用作抗结核病化合物的四氢吡唑并[1,5-a]嘧啶 |
| PL2710005T3 (pl) | 2011-05-17 | 2017-07-31 | Principia Biopharma Inc. | Inhibitory kinazy tyrozynowej |
| AU2012257802A1 (en) | 2011-05-17 | 2013-10-31 | F. Hoffmann-La Roche Ag | Inhibitors of Bruton's tyrosine kinase |
| WO2012158795A1 (en) * | 2011-05-17 | 2012-11-22 | Principia Biopharma Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| US20140107151A1 (en) | 2011-05-17 | 2014-04-17 | Principia Biophama Inc. | Tyrosine kinase inhibitors |
| MX354412B (es) | 2011-06-10 | 2018-03-05 | Merck Patent Gmbh | Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton. |
| ES2548414T3 (es) | 2011-07-08 | 2015-10-16 | Novartis Ag | Novedosos derivados de pirrolo pirimidina |
| CA2902686C (en) | 2013-04-25 | 2017-01-24 | Beigene, Ltd. | Fused heterocyclic compounds as protein kinase inhibitors |
| CN112552401B (zh) | 2013-09-13 | 2023-08-25 | 广州百济神州生物制药有限公司 | 抗pd1抗体及其作为治疗剂与诊断剂的用途 |
| EA201690746A1 (ru) | 2013-10-25 | 2016-12-30 | Фармасайкликс Элэлси | Лечение с применением ингибиторов тирозинкиназы брутона и иммунотерапии |
| WO2016087994A1 (en) | 2014-12-05 | 2016-06-09 | Acerta Pharma B.V. | Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment |
| SG11201704808VA (en) | 2014-12-18 | 2017-07-28 | Principia Biopharma Inc | Treatment of pemphigus |
| US20180193274A1 (en) | 2014-12-24 | 2018-07-12 | Principia Biopharma Inc. | Compositions for ileo-jejunal drug delivery |
| WO2017046746A1 (en) | 2015-09-15 | 2017-03-23 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor and a gitr binding molecule, a 4-1bb agonist, or an ox40 agonist |
| US20190054090A1 (en) | 2015-10-01 | 2019-02-21 | Gilead Sciences, Inc. | Combination of a btk inhibitor and a checkpoint inhibitor for treating cancers |
| 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 |
| WO2018033135A1 (en) | 2016-08-19 | 2018-02-22 | Beigene, Ltd. | Use of a combination comprising a btk inhibitor for treating cancers |
| US11555038B2 (en) | 2017-01-25 | 2023-01-17 | Beigene, Ltd. | Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| EP3612839A1 (en) | 2017-04-20 | 2020-02-26 | ADC Therapeutics SA | Combination therapy |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| 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 |
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