JP2015535277A5 - - Google Patents
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- JP2015535277A5 JP2015535277A5 JP2015540256A JP2015540256A JP2015535277A5 JP 2015535277 A5 JP2015535277 A5 JP 2015535277A5 JP 2015540256 A JP2015540256 A JP 2015540256A JP 2015540256 A JP2015540256 A JP 2015540256A JP 2015535277 A5 JP2015535277 A5 JP 2015535277A5
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- JP
- Japan
- Prior art keywords
- halo
- alkyl
- alkoxy
- independently selected
- group
- 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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- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 239000001257 hydrogen Substances 0.000 claims description 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 20
- 150000001875 compounds Chemical class 0.000 claims description 19
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 16
- -1 hydroxy, hydroxy Chemical group 0.000 claims description 15
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 10
- 150000002431 hydrogen Chemical class 0.000 claims description 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 4
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims description 4
- 125000004414 alkyl thio group Chemical group 0.000 claims description 4
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
- 125000004076 pyridyl group Chemical group 0.000 claims description 3
- 125000001475 halogen functional group Chemical group 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 21
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 210000003719 b-lymphocyte Anatomy 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000005549 heteroarylene group Chemical group 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 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
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 125000000732 arylene group Chemical group 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
- 201000010099 disease Diseases 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 description 20
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261721920P | 2012-11-02 | 2012-11-02 | |
| US61/721,920 | 2012-11-02 | ||
| US201361772028P | 2013-03-04 | 2013-03-04 | |
| US61/772,028 | 2013-03-04 | ||
| PCT/IB2013/059846 WO2014068527A1 (en) | 2012-11-02 | 2013-11-01 | Bruton's tyrosine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015535277A JP2015535277A (ja) | 2015-12-10 |
| JP2015535277A5 true JP2015535277A5 (cg-RX-API-DMAC10.html) | 2016-09-08 |
| JP6178861B2 JP6178861B2 (ja) | 2017-08-09 |
Family
ID=49596360
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015540256A Expired - Fee Related JP6178861B2 (ja) | 2012-11-02 | 2013-11-01 | ブルトン型チロシンキナーゼ阻害剤 |
Country Status (27)
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AP2015008203A0 (en) | 2012-08-10 | 2015-01-31 | Boehringer Ingelheim Int | Heteroaromatic compounds as bruton's tyrosine kinase (BTK) inhibitors |
| CN104822681B (zh) | 2012-09-10 | 2018-01-30 | 普林斯匹亚生物制药公司 | 作为激酶抑制剂的吡唑并嘧啶化合物 |
| CN103848810A (zh) * | 2012-11-30 | 2014-06-11 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
| US8895750B2 (en) | 2013-03-14 | 2014-11-25 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds as BTK inhibitors |
| US9156847B2 (en) * | 2013-03-15 | 2015-10-13 | Janssen Pharmaceutica Nv | Processes and intermediates for preparing a medicament |
| CN105026400A (zh) * | 2013-03-15 | 2015-11-04 | 詹森药业有限公司 | 用于制备药物的方法和中间体 |
| EP2970300B1 (en) | 2013-03-15 | 2018-05-16 | Boehringer Ingelheim International GmbH | Heteroaromatic compounds as btk inhibitors |
| LT3035991T (lt) | 2013-08-19 | 2020-11-10 | Taris Biomedical Llc | Daugiablokiai vaistų vartojimo įtaisai |
| SI3052476T1 (sl) | 2013-09-30 | 2020-12-31 | Guangzhou Innocare Pharma Tech Co., Ltd. | Substituirani nikotinimidni inhibitorji BTK in njihova priprava in uporaba pri zdravljenju raka, vnetja in avtoimunske bolezni |
| EP3099674B1 (en) * | 2014-01-29 | 2018-10-24 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as btk inhibitors |
| EP3107544B1 (en) | 2014-02-21 | 2020-10-07 | Principia Biopharma Inc. | Salts and solid form of a btk inhibitor |
| 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 |
| CN105085474B (zh) | 2014-05-07 | 2018-05-18 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
| GB201410430D0 (en) | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
| WO2016008411A1 (en) * | 2014-07-18 | 2016-01-21 | Beigene, Ltd. | 5-amino-4-carbamoyl-pyrazole compounds as selective and irreversible t790m over wt-egfr kinase inhibitors and use thereof |
| WO2016019237A2 (en) * | 2014-07-31 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| CN105884747B (zh) * | 2014-08-28 | 2021-01-05 | 首药控股(北京)有限公司 | 一种制备布鲁顿酪氨酸激酶(btk)激酶抑制剂的制备方法 |
| CA2970723C (en) | 2014-12-18 | 2023-09-05 | Principia Biopharma Inc. | Treatment of pemphigus |
| WO2016192074A1 (en) * | 2015-06-04 | 2016-12-08 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| EP3313839A1 (en) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| US10611766B2 (en) | 2015-09-16 | 2020-04-07 | Loxo Oncology Inc. | Pyrazolopyrimidine derivatives as BTK inhibitors for the treatment of cancer |
| ES2964946T3 (es) * | 2015-11-17 | 2024-04-10 | Merck Patent Gmbh | Métodos para tratar esclerosis múltiple usando compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton |
| EA034561B1 (ru) | 2015-12-16 | 2020-02-20 | Бёрингер Ингельхайм Интернациональ Гмбх | Бипиразолильные производные, пригодные для лечения аутоиммунных заболеваний |
| CN114573510B (zh) * | 2015-12-16 | 2025-02-25 | 洛克索肿瘤学股份有限公司 | 可用作激酶抑制剂的化合物 |
| JP6916185B2 (ja) | 2016-01-13 | 2021-08-11 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｂｔｋ阻害剤としてのイソキノロン類 |
| 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 |
| US11352339B2 (en) | 2016-03-24 | 2022-06-07 | Mission Therapeutics Limited | 1-cyano-pyrrolidine derivatives as DUB inhibitors |
| US10882843B2 (en) | 2016-05-16 | 2021-01-05 | Suzhou Sinovent Pharmaceuticals Co., Ltd. | 5-aminopyrazole carboxamide derivative as BTK inhibitor and preparation method and pharmaceutical composition thereof |
| IL293621B2 (en) | 2016-06-29 | 2023-09-01 | Principia Biopharma Inc | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[4,3-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4 -Methyl-4-[4-(oxane-3-yl)piperazine-1-yl)penta-2-ananitrile |
| GB201616511D0 (en) | 2016-09-29 | 2016-11-16 | Mission Therapeutics Limited | Novel compounds |
| GB201616627D0 (en) | 2016-09-30 | 2016-11-16 | Mission Therapeutics Limited | Novel compounds |
| TWI771327B (zh) * | 2016-10-05 | 2022-07-21 | 英商使命醫療公司 | 新穎化合物 |
| MX2019006288A (es) | 2016-12-03 | 2020-10-01 | Juno Therapeutics Inc | Metodos y composiciones para el uso de celulas t terapeuticas en combinacion con inhibidores de quinasa. |
| EP3558363A1 (en) | 2016-12-21 | 2019-10-30 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| US11247987B2 (en) | 2017-10-06 | 2022-02-15 | Forma Therapeutics, Inc. | Inhibiting ubiquitin specific peptidase 30 |
| CN111212644B (zh) * | 2017-11-10 | 2021-01-15 | 苏州信诺维医药科技有限公司 | 作为btk抑制剂的5-氨基吡唑甲酰胺化合物的无定型固体分散体 |
| WO2019091440A1 (zh) * | 2017-11-10 | 2019-05-16 | 苏州信诺维医药科技有限公司 | 作为btk抑制剂的5-氨基吡唑甲酰胺化合物的晶型i |
| CN111225912B (zh) * | 2017-11-10 | 2020-11-10 | 苏州信诺维医药科技有限公司 | 作为btk抑制剂的5-氨基吡唑甲酰胺化合物及其制备方法 |
| CN108530436B (zh) * | 2018-05-17 | 2020-12-29 | 黄传满 | 一种吡唑类化合物及其制备方法和应用 |
| EP3793997B1 (en) | 2018-05-17 | 2024-03-13 | Forma Therapeutics, Inc. | Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors |
| LT3860989T (lt) | 2018-10-05 | 2023-06-12 | Forma Therapeutics, Inc. | Sulieti pirolinai, kurie veikia kaip ubikvitinui specifinės proteazės 30 (ups30) inhibitoriai |
| AU2020234712B2 (en) * | 2019-03-14 | 2025-12-04 | Abbvie Inc. | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| CN114364798A (zh) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | 用于治疗癌症的Dbait分子与激酶抑制剂的组合 |
| CN120136774A (zh) | 2019-05-21 | 2025-06-13 | 詹森药业有限公司 | 用于制备btk抑制剂的方法和中间体 |
| IL291994A (en) | 2019-10-14 | 2022-06-01 | Principia Biopharma Inc | Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine- 1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN115461341A (zh) | 2020-01-22 | 2022-12-09 | 普林斯匹亚生物制药公司 | 2-[3-[4-氨基-3-(2-氟-4-苯氧基-苯基)-1h-吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧杂环丁烷-3-基)哌嗪-1-基]戊-2-烯腈的晶型 |
| TW202317099A (zh) * | 2020-09-10 | 2023-05-01 | 美商絡速藥業公司 | 用於製備(s)-5-胺基-3-(4-((5-氟-2-甲氧基苯甲醯胺基)甲基)苯基)-1-(1,1,1-三氟丙烷-2-基)-1h-吡唑-4-甲醯胺之方法及中間體 |
| CN116829555A (zh) * | 2020-09-11 | 2023-09-29 | 卡里科生命科学有限责任公司 | 蛋白酪氨酸磷酸酶抑制剂及其使用方法 |
| WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| WO2023284765A1 (zh) * | 2021-07-16 | 2023-01-19 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡唑类化合物及包含该化合物的组合物及其用途 |
| CN116554102B (zh) * | 2022-01-28 | 2025-10-03 | 深圳海博为药业有限公司 | 一种作为btk抑制剂的化合物及其制备方法和应用 |
| AU2023216263A1 (en) * | 2022-02-04 | 2024-08-22 | Retune Pharma Inc. | Certain chemical entities, compositions, and methods |
| WO2024153237A1 (zh) * | 2023-01-19 | 2024-07-25 | 北京普祺医药科技股份有限公司 | 一种igf-1r酪氨酸激酶抑制剂、药物组合物及其用途 |
| WO2024153226A1 (zh) * | 2023-01-19 | 2024-07-25 | 北京普祺医药科技股份有限公司 | 一种吡唑并环类化合物、药物组合物及其用途 |
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-
2013
- 2013-11-01 US US14/439,478 patent/US20150291554A1/en not_active Abandoned
- 2013-11-01 CN CN201380065731.8A patent/CN105008344B/zh not_active Expired - Fee Related
- 2013-11-01 EP EP13792494.0A patent/EP2914586B1/en active Active
- 2013-11-01 GE GEAP201313816A patent/GEP201606597B/en unknown
- 2013-11-01 AU AU2013340345A patent/AU2013340345B2/en not_active Ceased
- 2013-11-01 MX MX2015005422A patent/MX2015005422A/es unknown
- 2013-11-01 MD MDA20150035A patent/MD20150035A2/ro not_active Application Discontinuation
- 2013-11-01 JP JP2015540256A patent/JP6178861B2/ja not_active Expired - Fee Related
- 2013-11-01 CA CA2888960A patent/CA2888960C/en not_active Expired - Fee Related
- 2013-11-01 KR KR1020157014092A patent/KR101668574B1/ko not_active Expired - Fee Related
- 2013-11-01 EA EA201500393A patent/EA201500393A1/ru unknown
- 2013-11-01 HK HK15112141.6A patent/HK1211293A1/xx unknown
- 2013-11-01 WO PCT/IB2013/059846 patent/WO2014068527A1/en not_active Ceased
- 2013-11-01 SG SG11201502893WA patent/SG11201502893WA/en unknown
- 2013-11-01 ES ES13792494.0T patent/ES2625944T3/es active Active
- 2013-11-01 AP AP2015008381A patent/AP2015008381A0/xx unknown
- 2013-11-01 BR BR112015009624A patent/BR112015009624A2/pt active Search and Examination
- 2013-11-01 PE PE2015000569A patent/PE20151070A1/es not_active Application Discontinuation
- 2013-11-04 TW TW102139984A patent/TWI518080B/zh not_active IP Right Cessation
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2015
- 2015-04-27 PH PH12015500940A patent/PH12015500940A1/en unknown
- 2015-04-29 CO CO15098489A patent/CO7350624A2/es unknown
- 2015-04-30 IL IL238571A patent/IL238571A0/en unknown
- 2015-04-30 CR CR20150228A patent/CR20150228A/es unknown
- 2015-04-30 TN TNP2015000168A patent/TN2015000168A1/fr unknown
- 2015-04-30 NI NI201500059A patent/NI201500059A/es unknown
- 2015-05-01 DO DO2015000100A patent/DOP2015000100A/es unknown
- 2015-05-04 CL CL2015001168A patent/CL2015001168A1/es unknown
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2017
- 2017-06-16 US US15/624,969 patent/US10266513B2/en active Active
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2019
- 2019-03-08 US US16/296,319 patent/US10815213B2/en active Active
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2020
- 2020-09-18 US US17/025,026 patent/US20210002251A1/en not_active Abandoned