JP2021505553A5 - - Google Patents
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- Publication number
- JP2021505553A5 JP2021505553A5 JP2020529717A JP2020529717A JP2021505553A5 JP 2021505553 A5 JP2021505553 A5 JP 2021505553A5 JP 2020529717 A JP2020529717 A JP 2020529717A JP 2020529717 A JP2020529717 A JP 2020529717A JP 2021505553 A5 JP2021505553 A5 JP 2021505553A5
- Authority
- JP
- Japan
- Prior art keywords
- independently selected
- alkoxy
- alkyl
- optionally substituted
- pharmaceutically acceptable
- 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
- 125000003545 alkoxy group Chemical group 0.000 description 26
- 125000000217 alkyl group Chemical group 0.000 description 23
- 150000001875 compounds Chemical class 0.000 description 19
- 125000005843 halogen group Chemical group 0.000 description 16
- 150000003839 salts Chemical class 0.000 description 16
- 125000005842 heteroatom Chemical group 0.000 description 15
- 229910052760 oxygen Inorganic materials 0.000 description 15
- 229910052717 sulfur Inorganic materials 0.000 description 14
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 description 10
- 229910052799 carbon Inorganic materials 0.000 description 7
- 229910052739 hydrogen Inorganic materials 0.000 description 7
- 201000010099 disease Diseases 0.000 description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 description 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 4
- 125000001072 heteroaryl group Chemical group 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 210000000845 cartilage Anatomy 0.000 description 2
- 230000001771 impaired effect Effects 0.000 description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 2
- 125000004917 3-methyl-2-butyl group Chemical group CC(C(C)*)C 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 208000011594 Autoinflammatory disease Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010010356 Congenital anomaly Diseases 0.000 description 1
- 102000014150 Interferons Human genes 0.000 description 1
- 108010050904 Interferons Proteins 0.000 description 1
- 108010065805 Interleukin-12 Proteins 0.000 description 1
- 108090001005 Interleukin-6 Proteins 0.000 description 1
- 206010052779 Transplant rejections Diseases 0.000 description 1
- 108060008682 Tumor Necrosis Factor Proteins 0.000 description 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 230000008416 bone turnover Effects 0.000 description 1
- 125000004093 cyano group Chemical group *C#N 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 208000030172 endocrine system disease Diseases 0.000 description 1
- 125000004366 heterocycloalkenyl group Chemical group 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 229940079322 interferon Drugs 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
- 208000030159 metabolic disease Diseases 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 208000023504 respiratory system disease Diseases 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 230000007306 turnover Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1720101.3 | 2017-12-02 | ||
| GBGB1720101.3A GB201720101D0 (en) | 2017-12-02 | 2017-12-02 | Novel compounds and pharmaceutical compositions thereof for the treatment of diseases |
| GBGB1817343.5A GB201817343D0 (en) | 2018-10-25 | 2018-10-25 | Novel compounds and pharmaceutical compositions thereof for the treatment of diseases |
| GB1817343.5 | 2018-10-25 | ||
| PCT/EP2018/082537 WO2019105886A1 (en) | 2017-12-02 | 2018-11-26 | Novel compounds and pharmaceutical compositions thereof for the treatment of diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021505553A JP2021505553A (ja) | 2021-02-18 |
| JP2021505553A5 true JP2021505553A5 (https=) | 2022-01-06 |
| JP7326276B2 JP7326276B2 (ja) | 2023-08-15 |
Family
ID=64564856
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020529717A Active JP7326276B2 (ja) | 2017-12-02 | 2018-11-26 | 新規化合物及び疾患の治療のためのその医薬組成物 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US11339166B2 (https=) |
| EP (1) | EP3717471B1 (https=) |
| JP (1) | JP7326276B2 (https=) |
| KR (1) | KR102720958B1 (https=) |
| CN (1) | CN111433200B (https=) |
| AU (1) | AU2018374456B2 (https=) |
| BR (1) | BR112020010364A2 (https=) |
| CA (1) | CA3084090A1 (https=) |
| CO (1) | CO2020008066A2 (https=) |
| CY (1) | CY1125044T1 (https=) |
| DK (1) | DK3717471T3 (https=) |
| ES (1) | ES2908283T3 (https=) |
| HU (1) | HUE057581T2 (https=) |
| IL (1) | IL274938B2 (https=) |
| MA (1) | MA51200A (https=) |
| MX (1) | MX2020005423A (https=) |
| MY (1) | MY201849A (https=) |
| PH (1) | PH12020550725B1 (https=) |
| PL (1) | PL3717471T3 (https=) |
| PT (1) | PT3717471T (https=) |
| SG (1) | SG11202004925QA (https=) |
| TW (1) | TW201930301A (https=) |
| WO (1) | WO2019105886A1 (https=) |
| ZA (1) | ZA202004025B (https=) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS58514B1 (sr) | 2012-06-13 | 2019-04-30 | Incyte Holdings Corp | Supstituisana triciklična jedinjenja kao inhibitori fgfr |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| TWI712601B (zh) | 2015-02-20 | 2020-12-11 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
| US11241435B2 (en) | 2016-09-16 | 2022-02-08 | The General Hospital Corporation | Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| EP3717471B1 (en) * | 2017-12-02 | 2022-01-05 | Galapagos NV | Novel compounds and pharmaceutical compositions thereof for the treatment of diseases |
| AU2019262579B2 (en) | 2018-05-04 | 2024-09-12 | Incyte Corporation | Salts of an FGFR inhibitor |
| HRP20241288T1 (hr) | 2018-05-04 | 2024-12-06 | Incyte Corporation | Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| GB201907616D0 (en) * | 2019-05-29 | 2019-07-10 | Galapagos Nv | Novel compounds and pharmaceutical compositons thereof for the treatment of diseases |
| GB201907558D0 (en) | 2019-05-29 | 2019-07-10 | Galapagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of diseases |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3157361A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7832891B2 (ja) | 2019-12-04 | 2026-03-18 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤の誘導体 |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) * | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| JP2023520916A (ja) * | 2020-04-08 | 2023-05-22 | リミックス セラピューティクス インコーポレイテッド | スプライシングを調整するための化合物及び方法 |
| CN116234549B (zh) * | 2020-08-05 | 2025-11-25 | 总医院公司 | 盐诱导激酶抑制剂 |
| CN112010860B (zh) * | 2020-08-05 | 2023-03-10 | 南京纳丁菲医药科技有限公司 | 苄氧基吡唑并嘧啶化合物和药物组合物及其应用 |
| MX2023003677A (es) * | 2020-09-30 | 2023-06-22 | Fl2022 001 Inc | Inhibidores de hidroxiesteroide 17beta- deshidrogenasa 13 (hsd17b13) y usos de estos. |
| US12064421B2 (en) | 2020-11-02 | 2024-08-20 | Boehringer Ingelheim International Gmbh | Substituted 1H-pyrazolo[4,3-c]pyridines and derivatives as EGFR inhibitors |
| US20240174662A1 (en) * | 2021-02-01 | 2024-05-30 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
| WO2022165529A1 (en) * | 2021-02-01 | 2022-08-04 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| KR20230053049A (ko) * | 2021-10-13 | 2023-04-21 | 서울대학교산학협력단 | 류마티스 관절염 예방 또는 치료용 약학적 조성물 및 건강기능식품 |
| CN118119619A (zh) * | 2021-10-18 | 2024-05-31 | 上海美悦生物科技发展有限公司 | Sik抑制剂及其组合物、制备方法和用途 |
| AR128279A1 (es) * | 2022-01-19 | 2024-04-10 | Hoffmann La Roche | Nuevos derivados de bencimidazol piridina |
| AR128280A1 (es) * | 2022-01-19 | 2024-04-10 | Hoffmann La Roche | Derivados de bencimidazol piridina |
| US20250171437A1 (en) * | 2022-02-28 | 2025-05-29 | Agios Pharmaceuticals,Inc. | (4-benzo[d]oxazol-2-yl)-6,7-dihydro-1h-imidazo[4,5-c]pyridine-5(4h)-yl)methanone derivatives as mutant pah stabilizers for the treatment of phenylketonuria |
| CN119095854A (zh) * | 2022-02-28 | 2024-12-06 | 安吉奥斯医药品有限公司 | 用于稳定苯丙氨酸羟化酶突变的化合物和方法 |
| CN117843634A (zh) * | 2022-05-24 | 2024-04-09 | 上海美悦生物科技发展有限公司 | Sik抑制剂及其组合物、制备方法和用途 |
| JP2025523524A (ja) * | 2022-07-01 | 2025-07-23 | エフ． ホフマン－ラ ロシュ アーゲー | 関節リウマチの処置のためのＳＩＫモジュレーターとしてのイミダゾ［４，５－ｂ］ピリジンおよびピラゾロ［１，５－ａ］ピリミジン誘導体 |
| US20240124450A1 (en) * | 2022-09-21 | 2024-04-18 | Pfizer Inc. | Novel SIK Inhibitors |
| EP4642773A1 (en) * | 2022-12-27 | 2025-11-05 | F. Hoffmann-La Roche AG | New benzimidazole derivatives |
| EP4737443A1 (en) | 2023-05-24 | 2026-05-06 | Tanabe Pharma Corporation | Salt-inducible kinase inhibitory compound and pharmaceutical composition containing same |
| CN116813608B (zh) * | 2023-06-08 | 2024-03-22 | 英矽智能科技(上海)有限公司 | 噻唑类化合物及其应用 |
| CN121712757A (zh) * | 2023-07-19 | 2026-03-20 | 豪夫迈·罗氏有限公司 | 苯并咪唑作为sik活性调节剂 |
| AR133277A1 (es) | 2023-07-19 | 2025-09-10 | Hoffmann La Roche | Nuevos derivados de bencimidazol piridina |
| WO2025231117A1 (en) * | 2024-05-01 | 2025-11-06 | Nimbus Salacia, Inc. | Sik2 modulators and uses thereof |
| WO2025231112A1 (en) * | 2024-05-01 | 2025-11-06 | Nimbus Salacia, Inc. | Sik2 modulators and uses thereof |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2008279759A1 (en) * | 2007-07-20 | 2009-01-29 | Merck & Co., Inc. | Pyrazolo[1,5-a]pyrimidine derivatives |
| ATE522249T1 (de) * | 2007-07-26 | 2011-09-15 | Novartis Ag | Organische verbindungen |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| JP2011530511A (ja) * | 2008-08-05 | 2011-12-22 | メルク・シャープ・エンド・ドーム・コーポレイション | 治療用化合物 |
| GB201204384D0 (en) * | 2012-03-13 | 2012-04-25 | Univ Dundee | Anti-flammatory agents |
| US9260426B2 (en) | 2012-12-14 | 2016-02-16 | Arrien Pharmaceuticals Llc | Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors |
| US10730842B2 (en) * | 2015-09-03 | 2020-08-04 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of DYRK1A and uses thereof |
| EP3717471B1 (en) * | 2017-12-02 | 2022-01-05 | Galapagos NV | Novel compounds and pharmaceutical compositions thereof for the treatment of diseases |
| CN116234549B (zh) | 2020-08-05 | 2025-11-25 | 总医院公司 | 盐诱导激酶抑制剂 |
-
2018
- 2018-11-26 EP EP18811769.1A patent/EP3717471B1/en active Active
- 2018-11-26 BR BR112020010364-0A patent/BR112020010364A2/pt unknown
- 2018-11-26 SG SG11202004925QA patent/SG11202004925QA/en unknown
- 2018-11-26 MX MX2020005423A patent/MX2020005423A/es unknown
- 2018-11-26 WO PCT/EP2018/082537 patent/WO2019105886A1/en not_active Ceased
- 2018-11-26 ES ES18811769T patent/ES2908283T3/es active Active
- 2018-11-26 MY MYPI2020002758A patent/MY201849A/en unknown
- 2018-11-26 PH PH1/2020/550725A patent/PH12020550725B1/en unknown
- 2018-11-26 PT PT188117691T patent/PT3717471T/pt unknown
- 2018-11-26 IL IL274938A patent/IL274938B2/en unknown
- 2018-11-26 KR KR1020207019014A patent/KR102720958B1/ko active Active
- 2018-11-26 MA MA051200A patent/MA51200A/fr unknown
- 2018-11-26 CA CA3084090A patent/CA3084090A1/en active Pending
- 2018-11-26 HU HUE18811769A patent/HUE057581T2/hu unknown
- 2018-11-26 JP JP2020529717A patent/JP7326276B2/ja active Active
- 2018-11-26 AU AU2018374456A patent/AU2018374456B2/en active Active
- 2018-11-26 DK DK18811769.1T patent/DK3717471T3/da active
- 2018-11-26 PL PL18811769T patent/PL3717471T3/pl unknown
- 2018-11-26 CN CN201880077841.9A patent/CN111433200B/zh active Active
- 2018-11-26 US US16/768,825 patent/US11339166B2/en active Active
- 2018-11-30 TW TW107142872A patent/TW201930301A/zh unknown
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2020
- 2020-06-30 CO CONC2020/0008066A patent/CO2020008066A2/es unknown
- 2020-07-01 ZA ZA2020/04025A patent/ZA202004025B/en unknown
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2022
- 2022-03-02 CY CY20221100182T patent/CY1125044T1/el unknown
- 2022-04-13 US US17/719,653 patent/US12065443B2/en active Active