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
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- 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 (65)
| 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 |
| CN108715615B (zh) | 2013-09-13 | 2020-11-27 | 百济神州(广州)生物科技有限公司 | 抗pd1抗体及其作为治疗剂与诊断剂的用途 |
| CN104341388B (zh) | 2013-10-16 | 2017-03-22 | 北京诺诚健华医药科技有限公司 | 芳香族酰胺类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| WO2015181633A2 (en) | 2014-04-11 | 2015-12-03 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bruton's tyrosine kinase |
| CN110156892B (zh) | 2014-07-03 | 2023-05-16 | 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 |
| WO2016020901A1 (en) | 2014-08-07 | 2016-02-11 | Acerta Pharma B.V. | Methods of treating cancers, immune and autoimmune diseases, and inflammatory diseases based on btk occupancy and btk resynthesis rate |
| PL3179992T3 (pl) | 2014-08-11 | 2022-08-16 | Acerta Pharma B.V. | Kombinacje terapeutyczne inhibitora BTK, inhibitora PD-1 i/lub inhibitora PD-L1 |
| 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 |
| HRP20211813T1 (hr) | 2014-08-11 | 2022-03-04 | Acerta Pharma B.V. | Terapeutske kombinacije inhibitora btk i inhibitora bcl-2 |
| TW201618773A (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、及／或ｃｄｋ４／６抑制劑的治療組合物 |
| CA2966259A1 (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 |
| 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 |
| MA44909A (fr) | 2015-09-15 | 2018-07-25 | Acerta Pharma Bv | Association thérapeutique d'un inhibiteur du cd19 et d'un inhibiteur de la btk |
| 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 |
| KR102684436B1 (ko) | 2015-10-16 | 2024-07-15 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | Ep4 길항제 |
| ES2839408T3 (es) | 2016-01-13 | 2021-07-05 | Acerta Pharma Bv | Combinaciones terapéuticas de un antifolato y un inhibidor de BTK |
| 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 |
| JP6993056B2 (ja) | 2016-07-05 | 2022-02-15 | ベイジーン リミテッド | 癌治療のためのｐｄ－１アンタゴニスト及びｒａｆ阻害剤の組合せ |
| CN116478166A (zh) | 2016-08-16 | 2023-07-25 | 百济神州(苏州)生物科技有限公司 | 一种化合物的晶型、其制备和用途 |
| DK3500299T3 (da) * | 2016-08-19 | 2024-01-29 | Beigene Switzerland Gmbh | Kombination af zanubrutinib med et anti-CD20- eller et anti-PD-1-antistof til anvendelse i behandling af cancer |
| MX390121B (es) | 2016-09-19 | 2025-03-20 | Mei Pharma Inc | Combinaciones de un inhibidor de btk y un inhibidor de pi3k para tratar neoplasias malignas hematológicas. |
| 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 |
| CN110799543A (zh) | 2017-06-26 | 2020-02-14 | 百济神州有限公司 | 肝细胞癌的免疫治疗 |
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| EP3689877A4 (en) * | 2017-11-03 | 2020-08-19 | South China Agricultural University | MERGED TRICYCLIC COMPOUND CONTAINING NITROGEN AND ITS USE AS AN AGROFORESTRY INSECTICIDE |
| CN111801334B (zh) * | 2017-11-29 | 2023-06-09 | 百济神州瑞士有限责任公司 | 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤 |
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| 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 |
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| 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 |
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| US20220362357A1 (en) | 2018-08-31 | 2022-11-17 | Stichting Radboud Universitair Medisch Centrum | Synergistic Combinations of Amino Acid Depletion Agent Sensitizers (AADAS) and Amino Acid Depletion Agents (AADA), and Therapeutic Methods of Use Thereof |
| 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 |
| EP3966204B1 (en) * | 2019-05-10 | 2024-11-27 | 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 |
| EP3981400A4 (en) * | 2019-06-10 | 2023-07-12 | BeiGene Switzerland GmbH | Oral capsule and preparation method therefor |
| EP3981399A4 (en) * | 2019-06-10 | 2023-05-31 | BeiGene Switzerland GmbH | ORAL SOLID TABLET WITH A TYROSINE KINAS INHIBITOR AND METHOD OF MANUFACTURE THEREOF |
| 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 |
| EP4051680B1 (en) | 2019-10-30 | 2025-09-03 | Biogen MA Inc. | Condensed bi-heterocycles as inhibiting agents for bruton's tyrosine kinase |
| WO2021110142A1 (en) * | 2019-12-04 | 2021-06-10 | Henan Normal University | Substituted imidazolecarboxamide as bruton's tyrosine kinase inhibitors |
| 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 |
| 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 |
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| KR20230051227A (ko) | 2020-08-14 | 2023-04-17 | 노파르티스 아게 | 헤테로아릴 치환된 스피로피페리디닐 유도체 및 이의 제약 용도 |
| US20250073238A1 (en) * | 2020-11-20 | 2025-03-06 | Beigene Switzerland Gmbh | Methods of treating systemic lupus erythematosus using btk inhibitors |
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| EP4284434A4 (en) * | 2021-01-30 | 2024-12-25 | BeiGene Switzerland GmbH | METHODS FOR 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 |
| TW202317558A (zh) * | 2021-06-21 | 2023-05-01 | 英屬開曼群島商百濟神州有限公司 | （ｒ）－戊二醯亞胺ｃｒｂｎ配位體及使用方法 |
| 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 |
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