JP2018505166A5 - - Google Patents
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- JP2018505166A5 JP2018505166A5 JP2017539435A JP2017539435A JP2018505166A5 JP 2018505166 A5 JP2018505166 A5 JP 2018505166A5 JP 2017539435 A JP2017539435 A JP 2017539435A JP 2017539435 A JP2017539435 A JP 2017539435A JP 2018505166 A5 JP2018505166 A5 JP 2018505166A5
- Authority
- JP
- Japan
- Prior art keywords
- crr
- nrc
- compound according
- nrso
- sulfur
- 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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- 150000001875 compounds Chemical class 0.000 claims 21
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 9
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 239000001301 oxygen Chemical group 0.000 claims 9
- 229910052717 sulfur Chemical group 0.000 claims 9
- 239000011593 sulfur Chemical group 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- -1 2H-pyrrolyl Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 102100036342 Interleukin-1 receptor-associated kinase 1 Human genes 0.000 claims 3
- 101710199015 Interleukin-1 receptor-associated kinase 1 Proteins 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000000160 oxazolidinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004502 1,2,3-oxadiazolyl group Chemical group 0.000 claims 1
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims 1
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 claims 1
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 claims 1
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 claims 1
- VXNZUUAINFGPBY-UHFFFAOYSA-N 1-Butene Chemical group CCC=C VXNZUUAINFGPBY-UHFFFAOYSA-N 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
- 206010002556 Ankylosing Spondylitis 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
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease 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
- 102100022691 NACHT, LRR and PYD domains-containing protein 3 Human genes 0.000 claims 1
- 101710126825 NACHT, LRR and PYD domains-containing protein 3 Proteins 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
- 201000004854 SAPHO syndrome Diseases 0.000 claims 1
- 201000010848 Schnitzler Syndrome Diseases 0.000 claims 1
- 206010040047 Sepsis 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
- 208000002849 chondrocalcinosis Diseases 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 125000003838 furazanyl group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 1
- 125000002636 imidazolinyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 206010072221 mevalonate kinase deficiency Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 230000000737 periodic effect Effects 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 1
- 125000002755 pyrazolinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562112793P | 2015-02-06 | 2015-02-06 | |
| US62/112,793 | 2015-02-06 | ||
| PCT/US2016/016708 WO2016127024A1 (en) | 2015-02-06 | 2016-02-05 | Pyridazinone macrocycles as irak inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018505166A JP2018505166A (ja) | 2018-02-22 |
| JP2018505166A5 true JP2018505166A5 (enExample) | 2019-03-14 |
| JP6920202B2 JP6920202B2 (ja) | 2021-08-18 |
Family
ID=55436166
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017539435A Expired - Fee Related JP6920202B2 (ja) | 2015-02-06 | 2016-02-05 | Ｉｒａｋ阻害剤としてのピリダジノン大環状化合物及びその使用 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9624246B2 (enExample) |
| EP (1) | EP3253763B1 (enExample) |
| JP (1) | JP6920202B2 (enExample) |
| KR (1) | KR102551597B1 (enExample) |
| CN (1) | CN107428765B (enExample) |
| AU (1) | AU2016215184B2 (enExample) |
| BR (1) | BR112017014970B1 (enExample) |
| CA (1) | CA2970550C (enExample) |
| ES (1) | ES2841452T3 (enExample) |
| IL (1) | IL253519B (enExample) |
| MX (1) | MX380929B (enExample) |
| RU (1) | RU2708066C2 (enExample) |
| SG (1) | SG11201704651UA (enExample) |
| WO (1) | WO2016127024A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2708066C2 (ru) * | 2015-02-06 | 2019-12-04 | Мерк Патент Гмбх | Макроциклы пиридазинона в качестве ингибиторов irak-киназы и их применения |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| JOP20180011A1 (ar) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | مشتقات بيرولو [1، 2-b]بيريدازين |
| WO2019111218A1 (en) | 2017-12-08 | 2019-06-13 | Cadila Healthcare Limited | Novel heterocyclic compounds as irak4 inhibitors |
| CN109956957B (zh) * | 2017-12-22 | 2021-11-09 | 广州白云山医药集团股份有限公司白云山制药总厂 | 一种咪唑并[1,2-b]哒嗪大环类激酶抑制剂 |
| IL277408B2 (en) * | 2018-04-05 | 2024-08-01 | Merck Patent Gmbh | Heteroaryl compounds as type ii irak inhibitors and uses thereof |
| TWI842978B (zh) | 2018-07-13 | 2024-05-21 | 美商基利科學股份有限公司 | 衍生物 |
| TWI727392B (zh) | 2018-08-13 | 2021-05-11 | 美商基利科學股份有限公司 | 噻二唑irak4抑制劑 |
| JP7169429B2 (ja) | 2018-08-13 | 2022-11-10 | ギリアード サイエンシーズ， インコーポレイテッド | ＩＲＡＫ４阻害剤としてのピロロ［１，２－ｂ］ピリダジン誘導体 |
| WO2020036830A1 (en) | 2018-08-13 | 2020-02-20 | Gilead Sciences, Inc. | Pyrrolo[1,2-b]pyridazine derivatives as irak4 inhibitors |
| US11998534B2 (en) * | 2020-02-12 | 2024-06-04 | Eubulus Biotherapeutics Inc. | GPX4 inhibitor in combination with anticancer agent for treating proliferative disease |
| CN111603471B (zh) * | 2020-06-24 | 2021-07-09 | 山东省科学院生物研究所 | 一种邻二氮杂环化合物在制备抑制tlr4受体的药物中的用途 |
| KR102871840B1 (ko) * | 2020-09-30 | 2025-10-15 | 아사히 가세이 파마 가부시키가이샤 | 거대고리 화합물 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000247959A (ja) * | 1999-02-26 | 2000-09-12 | Kowa Co | ピリダジン−３−オン誘導体及びこれを含有する医薬 |
| JP2010138073A (ja) * | 2007-03-30 | 2010-06-24 | Taisho Pharmaceutical Co Ltd | ピコリン酸アミド化合物 |
| US8703768B2 (en) * | 2010-06-09 | 2014-04-22 | Hoffmann-La Roche Inc. | Nitrogen containing heteroaryl compounds |
| US9586948B2 (en) * | 2012-10-08 | 2017-03-07 | Merck Sharp & Dohme Corp. | Inhibitors of IRAK4 activity |
| US9567320B2 (en) * | 2013-02-07 | 2017-02-14 | Merck Patent Gmbh | Pyridazinone-amides derivatives |
| RS56269B1 (sr) * | 2013-02-07 | 2017-11-30 | Merck Patent Gmbh | Makrociklični piridazinon derivati |
| RU2708066C2 (ru) * | 2015-02-06 | 2019-12-04 | Мерк Патент Гмбх | Макроциклы пиридазинона в качестве ингибиторов irak-киназы и их применения |
-
2016
- 2016-02-05 RU RU2017130761A patent/RU2708066C2/ru active
- 2016-02-05 AU AU2016215184A patent/AU2016215184B2/en not_active Ceased
- 2016-02-05 ES ES16706471T patent/ES2841452T3/es active Active
- 2016-02-05 EP EP16706471.6A patent/EP3253763B1/en active Active
- 2016-02-05 BR BR112017014970-2A patent/BR112017014970B1/pt not_active IP Right Cessation
- 2016-02-05 MX MX2017009624A patent/MX380929B/es unknown
- 2016-02-05 KR KR1020177020262A patent/KR102551597B1/ko active Active
- 2016-02-05 SG SG11201704651UA patent/SG11201704651UA/en unknown
- 2016-02-05 CA CA2970550A patent/CA2970550C/en active Active
- 2016-02-05 WO PCT/US2016/016708 patent/WO2016127024A1/en not_active Ceased
- 2016-02-05 US US15/016,584 patent/US9624246B2/en not_active Expired - Fee Related
- 2016-02-05 JP JP2017539435A patent/JP6920202B2/ja not_active Expired - Fee Related
- 2016-02-05 CN CN201680018681.1A patent/CN107428765B/zh not_active Expired - Fee Related
-
2017
- 2017-03-06 US US15/450,463 patent/US10517872B2/en active Active
- 2017-07-17 IL IL253519A patent/IL253519B/en active IP Right Grant
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