JP2020537671A5 - - Google Patents
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- Publication number
- JP2020537671A5 JP2020537671A5 JP2020521968A JP2020521968A JP2020537671A5 JP 2020537671 A5 JP2020537671 A5 JP 2020537671A5 JP 2020521968 A JP2020521968 A JP 2020521968A JP 2020521968 A JP2020521968 A JP 2020521968A JP 2020537671 A5 JP2020537671 A5 JP 2020537671A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- independently
- nrc
- ring
- halogen
- 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
- 150000001875 compounds Chemical class 0.000 claims 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 239000011593 sulfur Substances 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000003627 8 membered carbocyclic group Chemical group 0.000 claims 2
- 102000001284 I-kappa-B kinase Human genes 0.000 claims 2
- 108060006678 I-kappa-B kinase Proteins 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 230000009885 systemic effect Effects 0.000 claims 2
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 208000007815 Acquired Hyperostosis Syndrome Diseases 0.000 claims 1
- 208000026326 Adult-onset Still disease Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 206010008690 Chondrocalcinosis pyrophosphate Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 102100026018 Interleukin-1 receptor antagonist protein Human genes 0.000 claims 1
- 101710144554 Interleukin-1 receptor antagonist protein Proteins 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 201000004854 SAPHO syndrome Diseases 0.000 claims 1
- 201000010848 Schnitzler Syndrome Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 201000002661 Spondylitis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000002849 chondrocalcinosis Diseases 0.000 claims 1
- 208000022993 cryopyrin-associated periodic syndrome Diseases 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000028774 intestinal disease Diseases 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000025487 periodic fever syndrome Diseases 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 201000003068 rheumatic fever Diseases 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 230000001256 tonic effect Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 0 C**(/C=C/C(/c1c(*)cnc(NC2=C(*)CC=C(*C)C=C2)n1)=C/C1(C)*C)/C=C1/C#N Chemical compound C**(/C=C/C(/c1c(*)cnc(NC2=C(*)CC=C(*C)C=C2)n1)=C/C1(C)*C)/C=C1/C#N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762573251P | 2017-10-17 | 2017-10-17 | |
| US62/573,251 | 2017-10-17 | ||
| PCT/US2018/056190 WO2019079373A1 (en) | 2017-10-17 | 2018-10-17 | PYRIMIDINE TBK / IKKε INHIBITORY COMPOUNDS AND USES THEREOF |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020537671A JP2020537671A (ja) | 2020-12-24 |
| JP2020537671A5 true JP2020537671A5 (enExample) | 2021-11-25 |
| JP7266592B2 JP7266592B2 (ja) | 2023-04-28 |
Family
ID=64110185
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020521968A Active JP7266592B2 (ja) | 2017-10-17 | 2018-10-17 | ピリミジンＴＢＫ／ＩＫＫεインヒビター化合物およびそれらの使用 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20230019491A1 (enExample) |
| EP (1) | EP3697772A1 (enExample) |
| JP (1) | JP7266592B2 (enExample) |
| KR (1) | KR20200072519A (enExample) |
| CN (1) | CN111247135A (enExample) |
| AU (1) | AU2018352699A1 (enExample) |
| BR (1) | BR112020007466A2 (enExample) |
| CA (1) | CA3078579A1 (enExample) |
| IL (1) | IL273891A (enExample) |
| MX (1) | MX2020003507A (enExample) |
| RU (1) | RU2020115596A (enExample) |
| SG (1) | SG11202003407VA (enExample) |
| TW (1) | TWI802604B (enExample) |
| WO (1) | WO2019079373A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3078583A1 (en) * | 2017-10-17 | 2019-04-25 | Merck Patent Gmbh | Pyrimidine tbk/ikk.epsilon. inhibitor compounds and uses thereof |
| JP7359783B2 (ja) | 2018-06-05 | 2023-10-11 | クリネティックス ファーマシューティカルズ，インク． | メラノコルチンサブタイプ－２受容体（ｍｃ２ｒ）アンタゴニストおよびその使用 |
| CN112552280A (zh) * | 2019-09-25 | 2021-03-26 | 常州强力先端电子材料有限公司 | 一种高产酸的磺酰亚胺类光产酸剂 |
| JP7657792B2 (ja) * | 2019-11-07 | 2025-04-07 | クリネティックス ファーマシューティカルズ，インク． | メラノコルチンサブタイプ－２受容体（ｍｃ２ｒ）アンタゴニストおよびその使用 |
| PT4077307T (pt) | 2019-12-18 | 2025-06-03 | Crinetics Pharmaceuticals Inc | Antagonistas do recetor de subtipo 2 da melanocortina (mc2r) à base de piperidina gem-dissubstituída e suas utilizações |
| JP7651574B2 (ja) | 2019-12-23 | 2025-03-26 | クリネティックス ファーマシューティカルズ，インク． | スピロ環式ピペリジンメラノコルチンサブタイプ－２受容体（ｍｃ２ｒ）アンタゴニストおよびその使用 |
| IL305952A (en) | 2021-03-19 | 2023-11-01 | Crinetics Pharmaceuticals Inc | Melanocortin subtype 2 receptor (MC2R) antagonist for disease treatment |
| CN117447407B (zh) * | 2023-12-19 | 2024-06-11 | 潍坊医学院 | 一种JAK2抑制剂Pacritinib及其中间体的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2911139A1 (fr) * | 2007-01-05 | 2008-07-11 | Sanofi Aventis Sa | Nouveaux derives de phenyl-(4-phenyl-pyrimidin-2-yl)amines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk |
| ES2535166T3 (es) * | 2007-09-04 | 2015-05-06 | The Scripps Research Institute | Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas |
| CN102791697A (zh) * | 2009-10-12 | 2012-11-21 | 瑞科西有限公司 | 作为TBKL和/或IKKε抑制剂的氨基-嘧啶化合物 |
| GB201012105D0 (en) | 2010-07-19 | 2010-09-01 | Domainex Ltd | Novel pyrimidine compounds |
| BR112013026202A2 (pt) * | 2011-04-12 | 2017-07-25 | Myrexis Inc | composições e usos terapêuticos de inibidores quinase epsilon relacionado a ikk e quinase i de ligação a tank |
| DE102011112978A1 (de) | 2011-09-09 | 2013-03-14 | Merck Patent Gmbh | Benzonitrilderivate |
| JP2018524350A (ja) * | 2015-06-29 | 2018-08-30 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ＴＢＫ／ＩＫＫε阻害剤化合物及びその用途 |
-
2018
- 2018-10-17 RU RU2020115596A patent/RU2020115596A/ru unknown
- 2018-10-17 BR BR112020007466-7A patent/BR112020007466A2/pt not_active IP Right Cessation
- 2018-10-17 KR KR1020207014078A patent/KR20200072519A/ko not_active Withdrawn
- 2018-10-17 US US16/756,769 patent/US20230019491A1/en not_active Abandoned
- 2018-10-17 AU AU2018352699A patent/AU2018352699A1/en not_active Abandoned
- 2018-10-17 TW TW107136567A patent/TWI802604B/zh not_active IP Right Cessation
- 2018-10-17 EP EP18797386.2A patent/EP3697772A1/en not_active Withdrawn
- 2018-10-17 CA CA3078579A patent/CA3078579A1/en active Pending
- 2018-10-17 MX MX2020003507A patent/MX2020003507A/es unknown
- 2018-10-17 WO PCT/US2018/056190 patent/WO2019079373A1/en not_active Ceased
- 2018-10-17 JP JP2020521968A patent/JP7266592B2/ja active Active
- 2018-10-17 CN CN201880067979.0A patent/CN111247135A/zh active Pending
- 2018-10-17 SG SG11202003407VA patent/SG11202003407VA/en unknown
-
2020
- 2020-04-07 IL IL273891A patent/IL273891A/en unknown
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