JP2019502763A5 - - Google Patents
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- Publication number
- JP2019502763A5 JP2019502763A5 JP2018557284A JP2018557284A JP2019502763A5 JP 2019502763 A5 JP2019502763 A5 JP 2019502763A5 JP 2018557284 A JP2018557284 A JP 2018557284A JP 2018557284 A JP2018557284 A JP 2018557284A JP 2019502763 A5 JP2019502763 A5 JP 2019502763A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- optionally substituted
- group
- fluorines
- hydrogen
- 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
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 13
- 235000019000 fluorine Nutrition 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 2
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 229940122739 Calcineurin inhibitor Drugs 0.000 claims 1
- 102100024123 Calcineurin-binding protein cabin-1 Human genes 0.000 claims 1
- 101710192106 Calcineurin-binding protein cabin-1 Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 230000001387 anti-histamine Effects 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- VHOGYURTWQBHIL-UHFFFAOYSA-N leflunomide Chemical compound O1N=CC(C(=O)NC=2C=CC(=CC=2)C(F)(F)F)=C1C VHOGYURTWQBHIL-UHFFFAOYSA-N 0.000 claims 1
- 229960000681 leflunomide Drugs 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 0 CC1CN(*C(*)=C(*)*)CC1 Chemical compound CC1CN(*C(*)=C(*)*)CC1 0.000 description 1
- BIPHZZQRAKCOHL-UHFFFAOYSA-N CNC(CCC1)CN1C(C(O)=O)=O Chemical compound CNC(CCC1)CN1C(C(O)=O)=O BIPHZZQRAKCOHL-UHFFFAOYSA-N 0.000 description 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662281252P | 2016-01-21 | 2016-01-21 | |
| US62/281,252 | 2016-01-21 | ||
| PCT/US2017/013815 WO2017127371A1 (en) | 2016-01-21 | 2017-01-17 | Bruton's tyrosine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019502763A JP2019502763A (ja) | 2019-01-31 |
| JP2019502763A5 true JP2019502763A5 (https=) | 2020-02-27 |
| JP6950897B2 JP6950897B2 (ja) | 2021-10-13 |
Family
ID=59362831
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018557284A Active JP6950897B2 (ja) | 2016-01-21 | 2017-01-17 | ブルトン型チロシンキナーゼ阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10662187B2 (https=) |
| EP (1) | EP3405192B1 (https=) |
| JP (1) | JP6950897B2 (https=) |
| KR (1) | KR102699906B1 (https=) |
| CN (1) | CN109310671B (https=) |
| AU (1) | AU2017208998B2 (https=) |
| CA (1) | CA3009669C (https=) |
| EA (1) | EA201891626A1 (https=) |
| IL (1) | IL260691B (https=) |
| MX (1) | MX384833B (https=) |
| WO (1) | WO2017127371A1 (https=) |
| ZA (1) | ZA201805439B (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10793566B2 (en) * | 2016-01-21 | 2020-10-06 | Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. | Bruton's tyrosine kinase inhibitors |
| CN109071455B (zh) * | 2016-03-11 | 2022-08-02 | 嘉兴和剂药业有限公司 | 用于调节布鲁顿酪氨酸激酶的化合物及方法 |
| JOP20190113A1 (ar) * | 2016-11-18 | 2019-05-15 | Biocad Joint Stock Co | مثبطات بروتون تيروزين كيناز |
| CN107915584A (zh) * | 2017-12-16 | 2018-04-17 | 江苏长青农化股份有限公司 | 氟磺胺草醚中间体2‑氯‑4‑三氟甲基苯酚的合成方法 |
| CN108276254A (zh) * | 2018-03-26 | 2018-07-13 | 江苏长青农化南通有限公司 | 一种合成2-氯-4-三氟甲基苯酚的方法 |
| CN113365631B (zh) | 2019-01-18 | 2024-08-30 | 杭州邦顺制药有限公司 | 布鲁顿酪氨酸激酶抑制剂 |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| WO2021038540A1 (en) | 2019-08-31 | 2021-03-04 | Sun Pharma Advanced Research Company Limited | Cycloalkylidene carboxylic acids and derivatives as btk inhibitors |
| FI4036095T3 (fi) * | 2019-09-26 | 2024-02-14 | Jumbo Drug Bank Co Ltd | 4-Fluori-1H-pyratsolo[3,4-c]pyridiinijohdannaisia selektiivisinä Brutonin tyrosiinikinaasin (BTK) inhibiittoreina B-solulymfooman ja autoimmuunitautien hoitamiseksi |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN113493439B (zh) * | 2020-03-20 | 2022-10-14 | 深圳市塔吉瑞生物医药有限公司 | 取代的丙烯酰胺衍生物及其组合物及用途 |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| CN117377675A (zh) * | 2021-06-01 | 2024-01-09 | 正大天晴药业集团股份有限公司 | 含有并环或螺环的布鲁顿酪氨酸激酶降解剂 |
| WO2025113617A1 (zh) * | 2023-11-30 | 2025-06-05 | 武汉人福创新药物研发中心有限公司 | 含双环的tead抑制剂 |
| WO2025202889A1 (en) * | 2024-03-28 | 2025-10-02 | Array Biopharma Inc. | Her2 mutation inhibitors |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0615542B2 (ja) * | 1986-07-22 | 1994-03-02 | 吉富製薬株式会社 | ピラゾロピリジン化合物 |
| JP2701281B2 (ja) * | 1988-01-22 | 1998-01-21 | 吉富製薬株式会社 | ピラゾロピリジン化合物 |
| WO1993023036A1 (fr) * | 1992-05-21 | 1993-11-25 | Yoshitomi Pharmaceutical Industries, Ltd. | Compose de pyrazole condense optiquement actif, pour le traitement de la thrombocytopenie et de l'erythropenie |
| JPH0648941A (ja) * | 1992-06-02 | 1994-02-22 | Yoshitomi Pharmaceut Ind Ltd | 赤血球減少症治療剤 |
| US6921763B2 (en) * | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
| US8729107B2 (en) | 2002-12-06 | 2014-05-20 | Purdue Research Foundation | Pyridines for treating injured mammalian nerve tissue |
| SE0301906D0 (sv) * | 2003-06-26 | 2003-06-26 | Astrazeneca Ab | New compounds |
| DK2526933T3 (en) * | 2006-09-22 | 2015-05-18 | Pharmacyclics Inc | Inhibitors of Bruton's tyrosine kinase |
| US8633318B2 (en) * | 2008-09-16 | 2014-01-21 | Proximagen Ltd | Compounds for treatment or prevention of inflammation, an inflammatory disease, or an immune or an autoimmune disorder |
| US8846673B2 (en) * | 2009-08-11 | 2014-09-30 | Bristol-Myers Squibb Company | Azaindazoles as kinase inhibitors and use thereof |
| US7718662B1 (en) * | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| EP2487159A1 (en) * | 2011-02-11 | 2012-08-15 | MSD Oss B.V. | RorgammaT inhibitors |
| 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 |
| CN104080789B (zh) * | 2012-01-31 | 2016-05-11 | 南京奥昭生物科技有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
| WO2014022569A1 (en) | 2012-08-03 | 2014-02-06 | Principia Biopharma Inc. | Treatment of dry eye |
| WO2014026329A1 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof |
| WO2014026327A1 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof |
| US8957080B2 (en) * | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| US20160113893A1 (en) * | 2013-06-12 | 2016-04-28 | Proximagen Limited | New therapeutic uses of enzyme inhibitors |
| JP2016538270A (ja) * | 2013-10-25 | 2016-12-08 | ファーマサイクリックス エルエルシー | 移植片対宿主病を処置し予防する方法 |
| WO2015124570A1 (en) | 2014-02-18 | 2015-08-27 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical composition for the treatment of influenza a virus infection |
| GB201410430D0 (en) * | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
| US10351532B2 (en) * | 2014-12-29 | 2019-07-16 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Small molecule inhibitors of lactate dehydrogenase and methods of use thereof |
| WO2016170545A1 (en) * | 2015-04-22 | 2016-10-27 | Msn Laboratories Private Limited | Process for the preparation of 1-[(3r)-3-[4-amino-3-(4-phenoxyphenvl)-1h- pvrazolo[3,4-d]pyriniidin-1-y1]-1-piperidinvl]-2-propen-1-one and its polymorphs thereof |
-
2017
- 2017-01-17 KR KR1020187023916A patent/KR102699906B1/ko active Active
- 2017-01-17 WO PCT/US2017/013815 patent/WO2017127371A1/en not_active Ceased
- 2017-01-17 EP EP17741819.1A patent/EP3405192B1/en active Active
- 2017-01-17 IL IL260691A patent/IL260691B/en unknown
- 2017-01-17 MX MX2018008815A patent/MX384833B/es unknown
- 2017-01-17 JP JP2018557284A patent/JP6950897B2/ja active Active
- 2017-01-17 CA CA3009669A patent/CA3009669C/en active Active
- 2017-01-17 US US16/070,520 patent/US10662187B2/en active Active
- 2017-01-17 CN CN201780007631.8A patent/CN109310671B/zh active Active
- 2017-01-17 EA EA201891626A patent/EA201891626A1/ru unknown
- 2017-01-17 AU AU2017208998A patent/AU2017208998B2/en active Active
-
2018
- 2018-08-15 ZA ZA201805439A patent/ZA201805439B/en unknown