JP2022043059A5 - - Google Patents
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- Publication number
- JP2022043059A5 JP2022043059A5 JP2021191658A JP2021191658A JP2022043059A5 JP 2022043059 A5 JP2022043059 A5 JP 2022043059A5 JP 2021191658 A JP2021191658 A JP 2021191658A JP 2021191658 A JP2021191658 A JP 2021191658A JP 2022043059 A5 JP2022043059 A5 JP 2022043059A5
- Authority
- JP
- Japan
- Prior art keywords
- fluoro
- indole
- methylsulfonyl
- phenyl
- amino
- 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
- -1 3- (2-((2-Fluoro-3- (methylsulfonyl) phenyl) amino) -5-methylpyrimidine-4-yl) -1H-indole-7-yl Chemical group 0.000 claims 74
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 22
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 15
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims 11
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 229910052731 fluorine Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 239000000460 chlorine Chemical group 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 239000011737 fluorine Chemical group 0.000 claims 3
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- SOVJEVPWSAQNKB-KHCICDEESA-N (2R)-2-[(3R,5R)-3,5-dimethylpiperazin-1-yl]-N-[3-[2-(2-fluoro-3-methylsulfonylanilino)-5-methylpyrimidin-4-yl]-1H-indol-7-yl]-3-methoxypropanamide Chemical compound C[C@@H]1CN(C[C@H](N1)C)[C@@H](C(=O)NC=1C=CC=C2C(=CNC=12)C1=NC(=NC=C1C)NC1=C(C(=CC=C1)S(=O)(=O)C)F)COC SOVJEVPWSAQNKB-KHCICDEESA-N 0.000 claims 1
- SOVJEVPWSAQNKB-IECBHUPTSA-N (2S)-2-[(3R,5R)-3,5-dimethylpiperazin-1-yl]-N-[3-[2-(2-fluoro-3-methylsulfonylanilino)-5-methylpyrimidin-4-yl]-1H-indol-7-yl]-3-methoxypropanamide Chemical compound COC[C@H](N1C[C@@H](C)N[C@H](C)C1)C(=O)Nc1cccc2c(c[nH]c12)-c1nc(Nc2cccc(c2F)S(C)(=O)=O)ncc1C SOVJEVPWSAQNKB-IECBHUPTSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- WPNLVUFQGUADSS-UHFFFAOYSA-N N-(4-methyl-1,4-diazepan-1-yl)propanamide Chemical compound CCC(=O)NN1CCCN(C)CC1 WPNLVUFQGUADSS-UHFFFAOYSA-N 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023180744A JP7626819B2 (ja) | 2017-01-17 | 2023-10-20 | Ｊａｋ１選択的阻害剤 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762447057P | 2017-01-17 | 2017-01-17 | |
| US62/447,057 | 2017-01-17 | ||
| JP2019537377A JP6986086B2 (ja) | 2017-01-17 | 2018-01-16 | Ｊａｋ１選択的阻害剤 |
| PCT/EP2018/051038 WO2018134213A1 (en) | 2017-01-17 | 2018-01-16 | Jak1 selective inhibitors |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019537377A Division JP6986086B2 (ja) | 2017-01-17 | 2018-01-16 | Ｊａｋ１選択的阻害剤 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023180744A Division JP7626819B2 (ja) | 2017-01-17 | 2023-10-20 | Ｊａｋ１選択的阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022043059A JP2022043059A (ja) | 2022-03-15 |
| JP2022043059A5 true JP2022043059A5 (https=) | 2022-07-13 |
| JP7394820B2 JP7394820B2 (ja) | 2023-12-08 |
Family
ID=61024756
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019537377A Active JP6986086B2 (ja) | 2017-01-17 | 2018-01-16 | Ｊａｋ１選択的阻害剤 |
| JP2021191658A Active JP7394820B2 (ja) | 2017-01-17 | 2021-11-26 | Ｊａｋ１選択的阻害剤 |
| JP2023180744A Active JP7626819B2 (ja) | 2017-01-17 | 2023-10-20 | Ｊａｋ１選択的阻害剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019537377A Active JP6986086B2 (ja) | 2017-01-17 | 2018-01-16 | Ｊａｋ１選択的阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023180744A Active JP7626819B2 (ja) | 2017-01-17 | 2023-10-20 | Ｊａｋ１選択的阻害剤 |
Country Status (38)
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2938648T3 (es) | 2017-01-17 | 2023-04-13 | Astrazeneca Ab | Inhibidores selectivos de JAK1 |
| EP3789386A1 (en) | 2017-01-26 | 2021-03-10 | Hanmi Pharm. Co., Ltd. | Pyrimidine compound and pharmaceutical use thereof |
| EP3823964A1 (en) * | 2018-07-18 | 2021-05-26 | Astrazeneca AB | A xinafoate salt of a jak inhibiting compound |
| KR101954370B1 (ko) | 2018-07-25 | 2019-03-05 | 한미약품 주식회사 | 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물 |
| CA3113732C (en) * | 2018-09-21 | 2023-07-11 | Shanghai Ennovabio Pharmaceuticals Co., Ltd. | Aromatic heterocyclic compound with kinase inhibitory activity |
| BR112021016522A2 (pt) | 2019-02-22 | 2021-10-26 | Hanmi Pharm. Co., Ltd. | Composição farmacêutica para o tratamento da leucemia mieloide aguda |
| MX2021012749A (es) * | 2019-04-19 | 2021-11-18 | Dizal Jiangsu Pharmaceutical Co Ltd | Inhibidor selectivo de la jak1 cinasa. |
| EA202290154A1 (ru) | 2019-06-27 | 2022-03-29 | Ханми Фарм. Ко., Лтд. | Фармацевтическая композиция для лечения острого миелоидного лейкоза, содержащая ингибитор flt3 и химиотерапевтические агенты |
| US12435084B2 (en) | 2020-04-09 | 2025-10-07 | Eli Lilly And Company | Indazole derivatives as inhibitors of SARM1 |
| WO2022111499A1 (zh) * | 2020-11-26 | 2022-06-02 | 深圳铂立健医药有限公司 | 一种酰胺化合物、药物组合物及其应用 |
| TW202246243A (zh) * | 2021-02-26 | 2022-12-01 | 美商泰拉生物科學公司 | 胺基嘧啶化合物及其使用方法 |
| US12240836B2 (en) * | 2022-07-05 | 2025-03-04 | Dong-A St Co., Ltd. | Compounds as GCN2 inhibitors, pharmaceutical compositions and uses thereof |
| CN115260128B (zh) * | 2022-09-21 | 2022-12-09 | 苏州凯瑞医药科技有限公司 | 一种新型jak抑制剂关键中间体的制备方法 |
| EP4648776A1 (en) * | 2023-01-11 | 2025-11-19 | Pfizer Inc. | Compositions and methods for the treatment and/or prevention of type 1 diabetes |
| CN115974845B (zh) * | 2023-01-19 | 2024-09-20 | 奥锐特药业股份有限公司 | 奥希替尼中间体的制备方法 |
| US20240307353A1 (en) * | 2023-03-16 | 2024-09-19 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of asthma |
| GB202316063D0 (en) | 2023-10-20 | 2023-12-06 | Astrazeneca Ab | Dosing regime |
| GB202403369D0 (en) | 2024-03-08 | 2024-04-24 | Astrazeneca Ab | Process and intermediates for the production of a jak1 inhibitor |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008515986A (ja) * | 2004-10-13 | 2008-05-15 | ワイス | Ｎ−ベンゼンスルホニル置換アニリノ−ピリミジン類似物 |
| GB2431927B (en) | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
| CN101421250A (zh) * | 2006-01-30 | 2009-04-29 | 埃克塞里艾克西斯公司 | 作为jak-2调节剂的4-芳基-2-氨基-嘧啶或4-芳基-2-氨基烷基-嘧啶及包含它们的药物组合物 |
| WO2008097930A1 (en) | 2007-02-05 | 2008-08-14 | Amira Pharmaceuticals, Inc. | Reverse indoles as 5-lipoxygenase-activating protein (flap) inhibitors |
| US20100298343A1 (en) | 2007-10-05 | 2010-11-25 | John Howard Hutchinson | 5-lipoxygenase-activating protein (flap) inhibitors |
| WO2009046416A1 (en) * | 2007-10-05 | 2009-04-09 | Targegen Inc. | Anilinopyrimidines as jak kinase inhibitors |
| GB0805477D0 (en) * | 2008-03-26 | 2008-04-30 | Univ Nottingham | Pyrimidines triazines and their use as pharmaceutical agents |
| UA110324C2 (en) * | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| EP3354652B1 (en) | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| TW201217387A (en) * | 2010-09-15 | 2012-05-01 | Hoffmann La Roche | Azabenzothiazole compounds, compositions and methods of use |
| AU2014339897A1 (en) | 2013-10-24 | 2016-04-21 | Abbvie Inc. | JAK1 selective inhibitor and uses thereof |
| JP6767491B2 (ja) * | 2015-09-25 | 2020-10-14 | ディザル（ジァンスー）ファーマシューティカル・カンパニー・リミテッド | Ｊａｋを阻害するための化合物及び方法 |
| ES2938648T3 (es) | 2017-01-17 | 2023-04-13 | Astrazeneca Ab | Inhibidores selectivos de JAK1 |
-
2018
- 2018-01-16 ES ES18701296T patent/ES2938648T3/es active Active
- 2018-01-16 CA CA3049175A patent/CA3049175A1/en active Pending
- 2018-01-16 MA MA47301A patent/MA47301B1/fr unknown
- 2018-01-16 UA UAA201909176A patent/UA124246C2/uk unknown
- 2018-01-16 MX MX2022002976A patent/MX418519B/es unknown
- 2018-01-16 CN CN202211243959.9A patent/CN115925693B/zh active Active
- 2018-01-16 CR CR20190332A patent/CR20190332A/es unknown
- 2018-01-16 PL PL18701296.8T patent/PL3571192T3/pl unknown
- 2018-01-16 MX MX2019008435A patent/MX390625B/es unknown
- 2018-01-16 KR KR1020197023855A patent/KR102585048B1/ko active Active
- 2018-01-16 CN CN201880018044.3A patent/CN110461830B/zh active Active
- 2018-01-16 EP EP18701296.8A patent/EP3571192B1/en active Active
- 2018-01-16 HR HRP20230069TT patent/HRP20230069T1/hr unknown
- 2018-01-16 DK DK18701296.8T patent/DK3571192T3/da active
- 2018-01-16 PT PT187012968T patent/PT3571192T/pt unknown
- 2018-01-16 MY MYPI2019004083A patent/MY199735A/en unknown
- 2018-01-16 US US16/478,168 patent/US10961228B2/en active Active
- 2018-01-16 JO JOP/2019/0174A patent/JOP20190174B1/ar active
- 2018-01-16 AU AU2018209667A patent/AU2018209667B2/en active Active
- 2018-01-16 EA EA201991700A patent/EA037067B1/ru unknown
- 2018-01-16 JP JP2019537377A patent/JP6986086B2/ja active Active
- 2018-01-16 HU HUE18701296A patent/HUE061064T2/hu unknown
- 2018-01-16 PE PE2019001401A patent/PE20191108A1/es unknown
- 2018-01-16 SI SI201830849T patent/SI3571192T1/sl unknown
- 2018-01-16 RS RS20230130A patent/RS63981B1/sr unknown
- 2018-01-16 FI FIEP18701296.8T patent/FI3571192T3/fi active
- 2018-01-16 PH PH1/2019/501639A patent/PH12019501639B1/en unknown
- 2018-01-16 WO PCT/EP2018/051038 patent/WO2018134213A1/en not_active Ceased
- 2018-01-16 EP EP22209765.1A patent/EP4219470A1/en active Pending
- 2018-01-16 LT LTEPPCT/EP2018/051038T patent/LT3571192T/lt unknown
- 2018-01-16 SG SG11201906222WA patent/SG11201906222WA/en unknown
- 2018-01-16 SM SM20230051T patent/SMT202300051T1/it unknown
- 2018-01-16 KR KR1020237032917A patent/KR102659213B1/ko active Active
- 2018-01-17 TW TW107101685A patent/TWI753089B/zh active
- 2018-01-17 AR ARP180100104A patent/AR110753A1/es unknown
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2019
- 2019-07-04 IL IL267851A patent/IL267851B/en unknown
- 2019-07-15 CL CL2019001993A patent/CL2019001993A1/es unknown
- 2019-07-17 DO DO2019000184A patent/DOP2019000184A/es unknown
- 2019-07-17 NI NI201900077A patent/NI201900077A/es unknown
- 2019-07-17 EC ECSENADI201951352A patent/ECSP19051352A/es unknown
- 2019-07-23 CO CONC2019/0007888A patent/CO2019007888A2/es unknown
- 2019-10-18 ZA ZA2019/06875A patent/ZA201906875B/en unknown
-
2021
- 2021-03-01 US US17/188,097 patent/US11897869B2/en active Active
- 2021-11-26 JP JP2021191658A patent/JP7394820B2/ja active Active
-
2023
- 2023-10-20 JP JP2023180744A patent/JP7626819B2/ja active Active
- 2023-12-13 US US18/538,067 patent/US12473272B2/en active Active
-
2025
- 2025-09-30 US US19/345,428 patent/US20260028329A1/en active Pending
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