JP2015509927A5 - - Google Patents
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- Publication number
- JP2015509927A5 JP2015509927A5 JP2014555678A JP2014555678A JP2015509927A5 JP 2015509927 A5 JP2015509927 A5 JP 2015509927A5 JP 2014555678 A JP2014555678 A JP 2014555678A JP 2014555678 A JP2014555678 A JP 2014555678A JP 2015509927 A5 JP2015509927 A5 JP 2015509927A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- cycloalkyl
- alkyl
- heterocycloalkyl
- 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
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000001072 heteroaryl group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 14
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 125000002993 cycloalkylene group Chemical group 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 6
- 125000000732 arylene group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000005549 heteroarylene group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000004474 heteroalkylene group Chemical group 0.000 claims 4
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261593146P | 2012-01-31 | 2012-01-31 | |
| US61/593,146 | 2012-01-31 | ||
| US201261637765P | 2012-04-24 | 2012-04-24 | |
| US61/637,765 | 2012-04-24 | ||
| US13/460,524 US8501724B1 (en) | 2012-01-31 | 2012-04-30 | Purinone compounds as kinase inhibitors |
| US13/460,524 | 2012-04-30 | ||
| PCT/US2013/023918 WO2013116382A1 (en) | 2012-01-31 | 2013-01-30 | Purinone compounds as kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017020756A Division JP6501209B2 (ja) | 2012-01-31 | 2017-02-07 | キナーゼ阻害剤としてのプリノン化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015509927A JP2015509927A (ja) | 2015-04-02 |
| JP2015509927A5 true JP2015509927A5 (enExample) | 2016-03-03 |
| JP6095075B2 JP6095075B2 (ja) | 2017-03-15 |
Family
ID=48870746
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014555678A Expired - Fee Related JP6095075B2 (ja) | 2012-01-31 | 2013-01-30 | キナーゼ阻害剤としてのプリノン化合物 |
| JP2017020756A Expired - Fee Related JP6501209B2 (ja) | 2012-01-31 | 2017-02-07 | キナーゼ阻害剤としてのプリノン化合物 |
| JP2018228582A Pending JP2019059758A (ja) | 2012-01-31 | 2018-12-05 | キナーゼ阻害剤としてのプリノン化合物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017020756A Expired - Fee Related JP6501209B2 (ja) | 2012-01-31 | 2017-02-07 | キナーゼ阻害剤としてのプリノン化合物 |
| JP2018228582A Pending JP2019059758A (ja) | 2012-01-31 | 2018-12-05 | キナーゼ阻害剤としてのプリノン化合物 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US8501724B1 (enExample) |
| EP (2) | EP2809672A4 (enExample) |
| JP (3) | JP6095075B2 (enExample) |
| KR (2) | KR20180030730A (enExample) |
| CN (2) | CN104640861B (enExample) |
| AU (3) | AU2013215166B2 (enExample) |
| BR (1) | BR112014018728A8 (enExample) |
| CA (2) | CA2863140C (enExample) |
| HK (1) | HK1203489A1 (enExample) |
| IL (1) | IL261282A (enExample) |
| MX (1) | MX2014009219A (enExample) |
| PH (1) | PH12014501815A1 (enExample) |
| RU (2) | RU2655388C2 (enExample) |
| WO (1) | WO2013116382A1 (enExample) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2529621B1 (en) | 2006-09-22 | 2016-10-05 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| US20120101114A1 (en) | 2007-03-28 | 2012-04-26 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| EP3311818A3 (en) | 2008-07-16 | 2018-07-18 | Pharmacyclics, LLC | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| EA031737B1 (ru) | 2010-06-03 | 2019-02-28 | Фармасайкликс, Инк. | Применение ингибиторов тирозинкиназы брутона (btk) для лечения лейкоза и лимфомы |
| US9376438B2 (en) | 2011-05-17 | 2016-06-28 | Principia Biopharma, Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| SI2710005T1 (sl) | 2011-05-17 | 2017-03-31 | Principia Biopharma Inc. | Zaviralci tirozinske kinaze |
| EP2731612A4 (en) | 2011-07-13 | 2015-04-08 | Pharmacyclics Inc | BRUTON TYROSINE KINASE HEMMER |
| ES2671748T3 (es) | 2011-07-21 | 2018-06-08 | Tolero Pharmaceuticals, Inc. | Inhibidores heterocíclicos de proteína quinasas |
| US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
| US8501724B1 (en) * | 2012-01-31 | 2013-08-06 | Pharmacyclics, Inc. | Purinone compounds as kinase inhibitors |
| US9296753B2 (en) | 2012-06-04 | 2016-03-29 | Pharmacyclics Llc | Crystalline forms of a Bruton's tyrosine kinase inhibitor |
| EP3550031A1 (en) | 2012-07-24 | 2019-10-09 | Pharmacyclics, LLC | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| HK1211942A1 (en) | 2012-09-10 | 2016-06-03 | Principia Biopharma Inc. | Pyrazolopyrimidine compounds as kinase inhibitors |
| BR112015011171A2 (pt) | 2012-11-15 | 2017-07-11 | Pharmacyclics Inc | compostos de pirrolopirimidina como inibidores da quinase |
| US20140142099A1 (en) * | 2012-11-20 | 2014-05-22 | Principia Biopharma Inc. | Purinone Derivatives as Tyrosine Kinase Inhibitors |
| JP6433974B2 (ja) | 2013-03-14 | 2018-12-05 | トレロ ファーマシューティカルズ， インコーポレイテッド | Ｊａｋ２およびａｌｋ２阻害剤およびその使用方法 |
| AU2014251038A1 (en) | 2013-04-08 | 2015-11-26 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
| US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| JP6458018B2 (ja) * | 2013-07-02 | 2019-01-23 | ファーマサイクリックス エルエルシー | キナーゼ阻害剤としてのプリノン化合物 |
| EP3027192A4 (en) | 2013-08-02 | 2017-03-22 | Pharmacyclics, LLC | Methods for the treatment of solid tumors |
| US9415050B2 (en) | 2013-08-12 | 2016-08-16 | Pharmacyclics Llc | Methods for the treatment of HER2 amplified cancer |
| CA2925124A1 (en) | 2013-09-30 | 2015-04-02 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| MX372673B (es) | 2014-02-21 | 2020-03-25 | Principia Biopharma Inc | Un inhibidor de btk para usarse en el tratamiento de penfigo y sales y formas sólidas del mismo. |
| EP3119910A4 (en) | 2014-03-20 | 2018-02-21 | Pharmacyclics LLC | Phospholipase c gamma 2 and resistance associated mutations |
| WO2015151006A1 (en) * | 2014-03-29 | 2015-10-08 | Lupin Limited | Substituted purine compounds as btk inhibitors |
| EP3174539A4 (en) | 2014-08-01 | 2017-12-13 | Pharmacyclics, LLC | Inhibitors of bruton's tyrosine kinase |
| AU2015300798A1 (en) | 2014-08-07 | 2017-02-02 | Pharmacyclics Llc | Novel formulations of a Bruton's tyrosine kinase inhibitor |
| PT3233103T (pt) | 2014-12-18 | 2021-01-18 | Principia Biopharma Inc | Tratamento de pênfigo |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibitor |
| SI3303334T1 (sl) | 2015-06-03 | 2021-09-30 | Principia Biopharma Inc. | Zaviralci tirozin kinaz |
| MA42242A (fr) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc | Inhibiteurs de la tyrosine kinase |
| CN105753863B (zh) * | 2015-09-11 | 2018-07-31 | 东莞市真兴贝特医药技术有限公司 | 氧代二氢咪唑并吡啶类化合物及其应用 |
| CN108349940B (zh) * | 2015-10-14 | 2021-08-13 | 淄博百极常生制药有限公司 | 布鲁顿酪氨酸激酶抑制剂 |
| KR102708936B1 (ko) | 2015-11-20 | 2024-09-25 | 포르마 세라퓨틱스 인크. | 유비퀴틴-특이적 프로테아제 1 억제제로서의 퓨리논 |
| CN115650985B (zh) | 2016-04-15 | 2024-08-02 | 癌症研究科技有限公司 | 作为ret激酶抑制剂的杂环化合物 |
| WO2017178845A1 (en) | 2016-04-15 | 2017-10-19 | Cancer Research Technology Limited | Heterocyclic compounds as ret kinase inhibitors |
| EA201892836A1 (ru) | 2016-06-29 | 2019-07-31 | Принсипиа Биофарма Инк. | Составы 2-[3-[4-амино-3-(2-фтор-4-феноксифенил)пиразол[3,4-d]пиримидин-1-ил]пиперидин-1-карбонил]-4-метил-4-[4-(оксетан-3-ил)пиперазин-1-ил]пент-2-еннитрила с модифицированным высвобождением |
| IL284255B (en) * | 2016-08-29 | 2022-07-01 | Hoffmann La Roche | 7-substituted sulfonimidoylpurinone compounds for the treatment and prophylaxis of virus infection |
| CN106588937B (zh) | 2017-01-16 | 2018-09-21 | 东莞市真兴贝特医药技术有限公司 | 咪唑并吡嗪类化合物及其制备方法和应用 |
| KR102362646B1 (ko) | 2017-02-24 | 2022-02-11 | 길리애드 사이언시즈, 인코포레이티드 | 브루톤의 티로신 키나제의 억제제 |
| WO2018156901A1 (en) | 2017-02-24 | 2018-08-30 | Gilead Sciences, Inc. | Inhibitors of bruton's tyrosine kinase |
| GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
| CN109111446B (zh) * | 2017-06-22 | 2021-11-30 | 上海度德医药科技有限公司 | 一种具有药物活性的杂芳基化合物 |
| AU2019247498A1 (en) | 2018-04-05 | 2020-11-26 | Sumitomo Pharma Oncology, Inc. | AXL kinase inhibitors and use of the same |
| WO2019200254A1 (en) | 2018-04-13 | 2019-10-17 | Tolero Pharmaceuticals, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
| AU2019310590A1 (en) | 2018-07-26 | 2021-01-14 | Sumitomo Pharma Oncology, Inc. | Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same |
| CN110964016B (zh) * | 2018-09-29 | 2021-05-28 | 南京药捷安康生物科技有限公司 | 氨基降茨烷衍生物及其制备方法与应用 |
| CA3127502A1 (en) | 2019-02-12 | 2020-08-20 | Sumitomo Dainippon Pharma Oncology, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子 |
| MX2022004427A (es) | 2019-10-14 | 2022-07-12 | Principia Biopharma Inc | Metodos para el tratamiento de la trombocitopenia inmunitaria mediante la administracion de (r)-2-[3-[4-amino-3-(2-fluoro-4-feno xi-fenil)pirazolo[3,4-d]pirimidin-1-il]piperidino-1-carbonil]-4-m etil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enonitrilo. |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| CN115348862A (zh) | 2020-01-20 | 2022-11-15 | 建新公司 | 用于复发型多发性硬化症(rms)的治疗性酪氨酸激酶抑制剂 |
| MX2022009009A (es) | 2020-01-22 | 2022-08-15 | Principia Biopharma Inc | Formas cristalinas de 2-[3-[4-amino-3-(2-fluoro-4-fenoxi-fenil)-1h -pirazolo[3,4-d]pirimidin-1-il]piperidin-1-carbonil]-4-metil-4-[4 -(oxetan-3-il)piperazin-1-il]pent-2-enonitrilo. |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| KR102577689B1 (ko) | 2020-05-22 | 2023-09-12 | 코오롱인더스트리 주식회사 | 가스켓 조립체 및 이를 포함하는 연료전지 가습기 |
| CN113527300B (zh) * | 2020-06-04 | 2023-02-03 | 广州百霆医药科技有限公司 | 布鲁顿酪氨酸蛋白激酶抑制剂 |
| AU2021398051A1 (en) | 2020-12-10 | 2023-07-27 | Principia Biopharma Inc. | Crystal form of tolebrutinib, preparation method therefor and use thereof |
| EP4342468A4 (en) * | 2021-05-21 | 2025-06-04 | Hangzhou Solipharma Co., Ltd. | Tolbrutinib salt and crystal form thereof, manufacturing process therefor, pharmaceutical composition therefrom and use thereof |
| US20250154149A1 (en) * | 2022-02-16 | 2025-05-15 | Betta Pharmaceuticals Co., Ltd. | Pharmaceutical composition and method for preparing active ingredient compound thereof |
| CN120302975A (zh) | 2022-10-31 | 2025-07-11 | 住友制药美国公司 | 治疗骨髓增生性肿瘤的pim1抑制剂 |
| CN117777134B (zh) * | 2022-12-19 | 2025-02-25 | 艾立康药业股份有限公司 | 作为mat2a抑制剂的多环类化合物 |
| WO2025218778A1 (zh) * | 2024-04-19 | 2025-10-23 | 赛诺哈勃药业（成都）有限公司 | 杂环化合物及其作为ret抑制剂的用途 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged pharmaceutical product |
| US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
| US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
| US6326469B1 (en) | 1994-04-22 | 2001-12-04 | Sugen, Inc. | Megakaryocytic protein tyrosine kinases |
| HUP0303363A2 (hu) * | 1999-09-17 | 2004-07-28 | Abbott Gmbh & Co., Kg | Kináz-inhibitor hatású heterociklusos vegyületek alkalmazása gyógyszerkészítmények előállítására |
| US7071199B1 (en) * | 1999-09-17 | 2006-07-04 | Abbott Gmbh & Cco. Kg | Kinase inhibitors as therapeutic agents |
| JP4279784B2 (ja) * | 2002-12-04 | 2009-06-17 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | １，３−ジヒドロ−イミダゾール縮合環化合物 |
| WO2007035873A1 (en) * | 2005-09-21 | 2007-03-29 | Pharmacopeia, Inc. | Purinone derivatives for treating neurodegenerative diseases |
| EP2529621B1 (en) * | 2006-09-22 | 2016-10-05 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| US20080119496A1 (en) | 2006-11-16 | 2008-05-22 | Pharmacopeia Drug Discovery, Inc. | 7-Substituted Purine Derivatives for Immunosuppression |
| CA2669686A1 (en) * | 2006-11-16 | 2008-05-22 | Pharmacopeia, Llc | 7-substituted purine derivatives for immunosuppression |
| CA3001152A1 (en) | 2007-03-28 | 2008-10-09 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| TWI500617B (zh) * | 2010-05-31 | 2015-09-21 | Ono Pharmaceutical Co | Purine ketone derivatives |
| US8501724B1 (en) * | 2012-01-31 | 2013-08-06 | Pharmacyclics, Inc. | Purinone compounds as kinase inhibitors |
| JP6458018B2 (ja) * | 2013-07-02 | 2019-01-23 | ファーマサイクリックス エルエルシー | キナーゼ阻害剤としてのプリノン化合物 |
-
2012
- 2012-04-30 US US13/460,524 patent/US8501724B1/en not_active Expired - Fee Related
-
2013
- 2013-01-30 US US14/375,765 patent/US9469642B2/en not_active Expired - Fee Related
- 2013-01-30 BR BR112014018728A patent/BR112014018728A8/pt not_active Application Discontinuation
- 2013-01-30 RU RU2014134141A patent/RU2655388C2/ru not_active IP Right Cessation
- 2013-01-30 CA CA2863140A patent/CA2863140C/en not_active Expired - Fee Related
- 2013-01-30 KR KR1020187007316A patent/KR20180030730A/ko not_active Ceased
- 2013-01-30 HK HK15103865.9A patent/HK1203489A1/xx unknown
- 2013-01-30 WO PCT/US2013/023918 patent/WO2013116382A1/en not_active Ceased
- 2013-01-30 CN CN201380018581.5A patent/CN104640861B/zh not_active Expired - Fee Related
- 2013-01-30 CA CA2940039A patent/CA2940039A1/en not_active Abandoned
- 2013-01-30 CN CN201610685231.XA patent/CN106279172A/zh active Pending
- 2013-01-30 EP EP13743025.2A patent/EP2809672A4/en not_active Withdrawn
- 2013-01-30 MX MX2014009219A patent/MX2014009219A/es unknown
- 2013-01-30 AU AU2013215166A patent/AU2013215166B2/en not_active Ceased
- 2013-01-30 JP JP2014555678A patent/JP6095075B2/ja not_active Expired - Fee Related
- 2013-01-30 KR KR1020147024260A patent/KR101841325B1/ko not_active Expired - Fee Related
- 2013-01-30 RU RU2018118216A patent/RU2018118216A/ru not_active Application Discontinuation
- 2013-01-30 EP EP16170469.7A patent/EP3147285A3/en not_active Withdrawn
-
2014
- 2014-07-31 PH PH12014501815A patent/PH12014501815A1/en unknown
-
2016
- 2016-07-01 US US15/200,834 patent/US20160368924A1/en not_active Abandoned
- 2016-07-20 AU AU2016206309A patent/AU2016206309A1/en not_active Abandoned
-
2017
- 2017-02-07 JP JP2017020756A patent/JP6501209B2/ja not_active Expired - Fee Related
-
2018
- 2018-02-20 AU AU2018201203A patent/AU2018201203A1/en not_active Abandoned
- 2018-08-21 IL IL261282A patent/IL261282A/en unknown
- 2018-12-05 JP JP2018228582A patent/JP2019059758A/ja active Pending
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