JP6890602B2 - ブルトン型チロシンキナーゼのイミダゾピラジン阻害剤 - Google Patents
ブルトン型チロシンキナーゼのイミダゾピラジン阻害剤 Download PDFInfo
- Publication number
- JP6890602B2 JP6890602B2 JP2018541596A JP2018541596A JP6890602B2 JP 6890602 B2 JP6890602 B2 JP 6890602B2 JP 2018541596 A JP2018541596 A JP 2018541596A JP 2018541596 A JP2018541596 A JP 2018541596A JP 6890602 B2 JP6890602 B2 JP 6890602B2
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- cancer
- disease
- tumor
- amino
- cells
- 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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- 0 BC(**=CC(C(NC1=NC=CCC1)=*)=C)OC Chemical compound BC(**=CC(C(NC1=NC=CCC1)=*)=C)OC 0.000 description 4
- LSRKRWBIOODTOZ-VIFPVBQESA-N Bc1c(c(N)ncc2)[n]2c([C@H](C)NOC(c2ccccc2)=O)n1 Chemical compound Bc1c(c(N)ncc2)[n]2c([C@H](C)NOC(c2ccccc2)=O)n1 LSRKRWBIOODTOZ-VIFPVBQESA-N 0.000 description 1
- UAMRYMXHBKMFAP-IHWYPQMZSA-N C=C(N)S/C=C\N Chemical compound C=C(N)S/C=C\N UAMRYMXHBKMFAP-IHWYPQMZSA-N 0.000 description 1
- YGEASXYKSOVGCW-UHFFFAOYSA-N CC(C)(C(C)(C)OBc1ccc(C(Nc2ncc[s]2)=O)c(OC)c1)O Chemical compound CC(C)(C(C)(C)OBc1ccc(C(Nc2ncc[s]2)=O)c(OC)c1)O YGEASXYKSOVGCW-UHFFFAOYSA-N 0.000 description 1
- AJKJLKSVNSWQRP-HJWRWDBZSA-N CC1(C)OB(c2ccc(C(NNS/C=C\N)=O)c(OC)c2)OC1(C)C Chemical compound CC1(C)OB(c2ccc(C(NNS/C=C\N)=O)c(OC)c2)OC1(C)C AJKJLKSVNSWQRP-HJWRWDBZSA-N 0.000 description 1
- CEZLPETXJOGAKX-UHFFFAOYSA-N COc(cc(cc1)Br)c1C(O)=O Chemical compound COc(cc(cc1)Br)c1C(O)=O CEZLPETXJOGAKX-UHFFFAOYSA-N 0.000 description 1
- LSZSWXSZYOEBIP-AWEZNQCLSA-N COc1cc(-c2c(c(N)ncc3)[n]3c([C@H]3NCCC3)n2)ccc1C(Nc1ncc[s]1)=O Chemical compound COc1cc(-c2c(c(N)ncc3)[n]3c([C@H]3NCCC3)n2)ccc1C(Nc1ncc[s]1)=O LSZSWXSZYOEBIP-AWEZNQCLSA-N 0.000 description 1
- XSQCXINHLRIGGD-DJNXLDHESA-N C[C@@H](c1nc(-c(cc2)ccc2C(NC2=NCC(C)C=C2)=O)c2[n]1ccnc2N)N(C)C(C#CC)=O Chemical compound C[C@@H](c1nc(-c(cc2)ccc2C(NC2=NCC(C)C=C2)=O)c2[n]1ccnc2N)N(C)C(C#CC)=O XSQCXINHLRIGGD-DJNXLDHESA-N 0.000 description 1
- XIDJFSRGLOUDGG-QWNKOJSDSA-N C[C@@H](c1nc(-c(cc2)ccc2C(Nc2ccc(C)cn2)=O)c2[n]1ccnc2N)N(C)C(/C=C/COC)=O Chemical compound C[C@@H](c1nc(-c(cc2)ccc2C(Nc2ccc(C)cn2)=O)c2[n]1ccnc2N)N(C)C(/C=C/COC)=O XIDJFSRGLOUDGG-QWNKOJSDSA-N 0.000 description 1
- WVJPORBPJXMQPQ-AWEZNQCLSA-N C[C@@H](c1nc(-c(cc2)ccc2C(Nc2ccc(C)cn2)=O)c2[n]1ccnc2N)NC Chemical compound C[C@@H](c1nc(-c(cc2)ccc2C(Nc2ccc(C)cn2)=O)c2[n]1ccnc2N)NC WVJPORBPJXMQPQ-AWEZNQCLSA-N 0.000 description 1
- DNYHAHOAJGPDBC-ZDUSSCGKSA-N C[C@@H](c1nc(-c(cc2)ccc2C(Nc2ccccn2)=O)c2[n]1ccnc2N)NC Chemical compound C[C@@H](c1nc(-c(cc2)ccc2C(Nc2ccccn2)=O)c2[n]1ccnc2N)NC DNYHAHOAJGPDBC-ZDUSSCGKSA-N 0.000 description 1
- CGVAWNLJFMPHFY-LBPRGKRZSA-N Nc1ncc[n](c([C@H](CCC2)N2OC(c2ccccc2)=O)n2)c1c2Br Chemical compound Nc1ncc[n](c([C@H](CCC2)N2OC(c2ccccc2)=O)n2)c1c2Br CGVAWNLJFMPHFY-LBPRGKRZSA-N 0.000 description 1
- ICSNLGPSRYBMBD-UHFFFAOYSA-N Nc1ncccc1 Chemical compound Nc1ncccc1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562252420P | 2015-11-06 | 2015-11-06 | |
| US62/252,420 | 2015-11-06 | ||
| US201562261228P | 2015-11-30 | 2015-11-30 | |
| US62/261,228 | 2015-11-30 | ||
| PCT/IB2016/056661 WO2017077507A1 (en) | 2015-11-06 | 2016-11-04 | Imidazopyrazine inhibitors of bruton's tyrosine kinase |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018536705A JP2018536705A (ja) | 2018-12-13 |
| JP2018536705A5 JP2018536705A5 (enExample) | 2019-11-21 |
| JP6890602B2 true JP6890602B2 (ja) | 2021-06-18 |
Family
ID=57286764
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018541596A Active JP6890602B2 (ja) | 2015-11-06 | 2016-11-04 | ブルトン型チロシンキナーゼのイミダゾピラジン阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US10736893B2 (enExample) |
| EP (2) | EP3371189A1 (enExample) |
| JP (1) | JP6890602B2 (enExample) |
| CN (1) | CN108602827B (enExample) |
| MA (1) | MA43162A (enExample) |
| WO (1) | WO2017077507A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6890602B2 (ja) * | 2015-11-06 | 2021-06-18 | アセルタ ファーマ ビー.ブイ. | ブルトン型チロシンキナーゼのイミダゾピラジン阻害剤 |
| ES2878973T3 (es) * | 2016-06-30 | 2021-11-19 | Hangzhou Bangshun Pharmaceutical Co Ltd | Derivado de fenilo de imidazopiridinamina y uso del mismo |
| CN108101905A (zh) * | 2016-11-24 | 2018-06-01 | 中国科学院上海药物研究所 | 嘧啶并[5,4-b]吲嗪或嘧啶并[5,4-b]吡呤化合物、其制备方法及用途 |
| CN110494433B (zh) | 2017-03-22 | 2023-03-17 | 廖细斌 | 布鲁顿酪氨酸激酶抑制剂 |
| US10800787B2 (en) | 2017-04-20 | 2020-10-13 | Apotex Inc. | Process for the preparation of acalabrutinib |
| WO2019013562A1 (ko) * | 2017-07-12 | 2019-01-17 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
| KR102384924B1 (ko) * | 2017-07-12 | 2022-04-08 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
| US11161851B2 (en) * | 2017-11-06 | 2021-11-02 | Suzhou Pengxu Pharmatech Co. Ltd. | Processes to produce acalabrutinib |
| CN109836416B (zh) * | 2017-11-27 | 2023-02-03 | 苏州鹏旭医药科技有限公司 | 一种化合物的制备方法 |
| CN108129483B (zh) * | 2018-01-26 | 2019-06-04 | 成都施贝康生物医药科技有限公司 | 一种btk抑制剂及其应用 |
| CN108250186B (zh) * | 2018-02-07 | 2020-01-14 | 杭州科巢生物科技有限公司 | Acalabrutinib及其中间体的合成方法 |
| KR102106821B1 (ko) | 2018-04-27 | 2020-05-06 | 재단법인대구경북과학기술원 | 이브루티닙을 유효성분으로 포함하는 퇴행성 뇌질환의 예방 또는 치료용 약학적 조성물 |
| CN109053780B (zh) * | 2018-07-05 | 2020-09-29 | 浙江合聚生物医药有限公司 | 一种抗肿瘤药物Acalabrutinib关键中间体的制备方法 |
| EA202190557A1 (ru) | 2018-08-29 | 2021-07-13 | Асерта Фарма Б.В. | СПОСОБЫ ПОЛУЧЕНИЯ 4-{8-АМИНО-3-[(2S)-1-(БУТ-2-ИНОЛ)ПИРРОЛИДИН-2-ИЛ]ИМИДАЗО[1,5-a]ПИРАЗИН-1-ИЛ}-N-(ПИРИДИН-2-ИЛ)БЕНЗАМИДА |
| KR102833011B1 (ko) * | 2018-09-14 | 2025-07-14 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 푸로[3,4-b]피롤-함유 BTK 억제제 |
| US12285182B2 (en) | 2018-10-10 | 2025-04-29 | Innova Vascular, Inc. | Devices and methods for removing an embolus |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| WO2020225831A1 (en) * | 2019-05-09 | 2020-11-12 | Msn Laboratories Private Limited, R&D Center | Improved process for the preparation of 4-{8-amino-3-[(2s)-1-(but-2-ynoyl)pyrrolidin-2-yl] imidazo[1,5-a]pyrazin-1-yl)}-n-(pyridine-2-yl)benzamide |
| CN113993871B (zh) * | 2019-07-12 | 2023-08-01 | 正大天晴药业集团股份有限公司 | 含有5-氮杂螺庚烷的btk抑制剂 |
| 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 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| KR20230027201A (ko) * | 2020-06-19 | 2023-02-27 | 아세르타 파마. 비.브이. | 아칼라브루티닙 말레산염 투약 형태 |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0565233A (ja) | 1991-03-08 | 1993-03-19 | Mitsui Toatsu Chem Inc | モノクローナル抗体含有凍結乾燥製剤 |
| US6267958B1 (en) | 1995-07-27 | 2001-07-31 | Genentech, Inc. | Protein formulation |
| US20030113316A1 (en) | 2001-07-25 | 2003-06-19 | Kaisheva Elizabet A. | Stable lyophilized pharmaceutical formulation of IgG antibodies |
| EP2029163A4 (en) | 2006-06-14 | 2010-08-11 | Imclone Llc | LYOPHILIZED FORMULATIONS OF ANTI-EGFR ANTIBODIES |
| US7894450B2 (en) | 2007-12-31 | 2011-02-22 | Nortel Network, Ltd. | Implementation of VPNs over a link state protocol controlled ethernet network |
| KR101653842B1 (ko) | 2008-01-04 | 2016-09-02 | 인텔리카인, 엘엘씨 | 특정 화학 물질, 조성물 및 방법 |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| LT2734522T (lt) * | 2011-07-19 | 2019-02-11 | Merck Sharp & Dohme B.V. | 4-imidazopiridazin-1-il-benzamidai ir 4-imidazotriazin-1-il-benzamidai kaip btk-inhibitoriai |
| EP2548877A1 (en) * | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
| WO2015057992A1 (en) * | 2013-10-16 | 2015-04-23 | Izumi Raquel | Btk inhibitors for hematopoietic mobilization |
| WO2015110923A2 (en) * | 2014-01-21 | 2015-07-30 | Acerta Pharma B.V. | Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia usng a btk inhibitor |
| US20170231995A1 (en) | 2014-08-11 | 2017-08-17 | Acerta Pharma B.V. | BTK Inhibitors to Treat Solid Tumors Through Modulation of the Tumor Microenvironment |
| JP6890602B2 (ja) * | 2015-11-06 | 2021-06-18 | アセルタ ファーマ ビー.ブイ. | ブルトン型チロシンキナーゼのイミダゾピラジン阻害剤 |
-
2016
- 2016-11-04 JP JP2018541596A patent/JP6890602B2/ja active Active
- 2016-11-04 WO PCT/IB2016/056661 patent/WO2017077507A1/en not_active Ceased
- 2016-11-04 MA MA043162A patent/MA43162A/fr unknown
- 2016-11-04 US US15/773,846 patent/US10736893B2/en active Active
- 2016-11-04 EP EP16794751.4A patent/EP3371189A1/en not_active Withdrawn
- 2016-11-04 EP EP21151227.2A patent/EP3865485A1/en not_active Withdrawn
- 2016-11-04 CN CN201680077913.0A patent/CN108602827B/zh active Active
-
2020
- 2020-06-30 US US16/917,222 patent/US11110088B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| MA43162A (fr) | 2018-09-12 |
| US20200330461A1 (en) | 2020-10-22 |
| US11110088B2 (en) | 2021-09-07 |
| WO2017077507A1 (en) | 2017-05-11 |
| CN108602827A (zh) | 2018-09-28 |
| CN108602827B (zh) | 2021-08-20 |
| EP3865485A1 (en) | 2021-08-18 |
| JP2018536705A (ja) | 2018-12-13 |
| US20180318297A1 (en) | 2018-11-08 |
| EP3371189A1 (en) | 2018-09-12 |
| US10736893B2 (en) | 2020-08-11 |
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