JP2019532974A5 - - Google Patents
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- Publication number
- JP2019532974A5 JP2019532974A5 JP2019522663A JP2019522663A JP2019532974A5 JP 2019532974 A5 JP2019532974 A5 JP 2019532974A5 JP 2019522663 A JP2019522663 A JP 2019522663A JP 2019522663 A JP2019522663 A JP 2019522663A JP 2019532974 A5 JP2019532974 A5 JP 2019532974A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- cycloalkyl
- oxo
- alkoxy
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 67
- 125000005843 halogen group Chemical group 0.000 claims 47
- 125000003545 alkoxy group Chemical group 0.000 claims 27
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- 125000004438 haloalkoxy group Chemical group 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 18
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 17
- 150000002431 hydrogen Chemical class 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 13
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 229920006395 saturated elastomer Polymers 0.000 claims 8
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 4
- 208000027866 inflammatory disease Diseases 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 101000977771 Homo sapiens Interleukin-1 receptor-associated kinase 4 Proteins 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 102100023533 Interleukin-1 receptor-associated kinase 4 Human genes 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 201000005569 Gout Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000001589 carboacyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010018634 Gouty Arthritis Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease 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
- 208000002193 Pain Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 230000000735 allogeneic effect Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 208000020408 systemic-onset juvenile idiopathic arthritis Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662416550P | 2016-11-02 | 2016-11-02 | |
| US62/416,550 | 2016-11-02 | ||
| US201662417893P | 2016-11-04 | 2016-11-04 | |
| US62/417,893 | 2016-11-04 | ||
| PCT/EP2017/077886 WO2018083085A1 (en) | 2016-11-02 | 2017-10-31 | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019532974A JP2019532974A (ja) | 2019-11-14 |
| JP2019532974A5 true JP2019532974A5 (OSRAM) | 2020-12-03 |
| JP7059268B2 JP7059268B2 (ja) | 2022-04-25 |
Family
ID=60201582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019522663A Active JP7059268B2 (ja) | 2016-11-02 | 2017-10-31 | ＩＲＡＫ４モデュレーターとしてのピラゾロ［１，５ａ］ピリミジン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US11434250B2 (OSRAM) |
| EP (1) | EP3535273A1 (OSRAM) |
| JP (1) | JP7059268B2 (OSRAM) |
| CN (1) | CN109890829B (OSRAM) |
| WO (1) | WO2018083085A1 (OSRAM) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| TWI842978B (zh) | 2018-07-13 | 2024-05-21 | 美商基利科學股份有限公司 | 衍生物 |
| KR102659550B1 (ko) * | 2018-08-13 | 2024-04-23 | 길리애드 사이언시즈, 인코포레이티드 | Irak4 억제제로서의 피롤로[1,2-b]피리다진 유도체 |
| GB201904373D0 (en) * | 2019-03-29 | 2019-05-15 | Galapagos Nv | Novel compounds and pharamaceutical compositions thereof for the treatment of inflammatory disorders |
| CN113402499B (zh) | 2021-06-21 | 2022-05-13 | 上海勋和医药科技有限公司 | 一种亚磺酰亚胺取代的吲唑类irak4激酶抑制剂、制备方法及用途 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0329214D0 (en) | 2003-12-17 | 2004-01-21 | Glaxo Group Ltd | Novel compounds |
| AU2008345225A1 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| CA2727036C (en) | 2008-06-20 | 2017-03-21 | Genentech, Inc. | Triazolopyridine jak inhibitor compounds and methods |
| MX358682B (es) * | 2010-07-13 | 2018-08-31 | Hoffmann La Roche | Derivados de pirazolo [1,5a]pirimidina y de tieno[3,2b] pirimidina como moduladores de la cinasa asociada al receptor de la interleucina 4 (irak4). |
| US9307932B2 (en) | 2010-07-14 | 2016-04-12 | Ecole Polytechnique Federale De Lausanne (Epfl) | System and method for 3D gait assessment |
| RS63320B1 (sr) * | 2010-12-08 | 2022-07-29 | The U S A As Represented By The Secretary Department Of Health And Human Services | Supstituisani pirazolopirimidini kao aktivatori glukocerebrozidaze |
| BR112015012454B1 (pt) * | 2012-12-07 | 2022-07-05 | Vertex Pharmaceuticals Incorporated | Compostos inibidores de atr quinase, seu uso e composição farmacêutica compreendendo os mesmos |
| JP6437452B2 (ja) * | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| CN106456609A (zh) | 2014-06-20 | 2017-02-22 | 奥瑞基尼探索技术有限公司 | 作为irak4抑制剂的取代的吲唑化合物 |
| DK3215511T3 (da) | 2014-11-06 | 2024-05-13 | Bial R&D Invest S A | Substituerede pyrazolo(1,5-a)pyrimidiner og deres anvendelse i behandlingen af medicinske lidelser |
| WO2016144848A1 (en) | 2015-03-12 | 2016-09-15 | Merck Sharp & Dohme Corp. | Pyrrolotriazine inhibitors of irak4 activity |
| EP3268367B8 (en) * | 2015-03-12 | 2022-11-16 | Merck Sharp & Dohme LLC | Carboxamide inhibitors of irak4 activity |
| US10040802B2 (en) | 2015-03-12 | 2018-08-07 | Merck Sharp & Dohme Corp. | Thienopyrazine inhibitors of IRAK4 activity |
| EP3267996B1 (en) | 2015-03-12 | 2020-11-11 | Merck Sharp & Dohme Corp. | Pyrazolopyrimidine inhibitors of irak4 activity |
| HK1249435A1 (zh) | 2015-07-15 | 2018-11-02 | Aurigene Discovery Technologies Limited | 作为irak-4抑制剂的取代的氮杂化合物 |
| CU20180006A7 (es) | 2015-07-15 | 2018-06-05 | Aurigene Discovery Tech Ltd | Compuestos de indazaol y azaindazol como inhibidores de irak-4 |
| JP6895439B2 (ja) | 2015-12-22 | 2021-06-30 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ＩＲＡＫ４調節因子としてのピラゾロ［１，５ａ］ピリミジン誘導体 |
-
2017
- 2017-10-31 WO PCT/EP2017/077886 patent/WO2018083085A1/en not_active Ceased
- 2017-10-31 EP EP17792062.6A patent/EP3535273A1/en not_active Ceased
- 2017-10-31 JP JP2019522663A patent/JP7059268B2/ja active Active
- 2017-10-31 CN CN201780065283.XA patent/CN109890829B/zh not_active Expired - Fee Related
-
2020
- 2020-04-30 US US16/863,741 patent/US11434250B2/en active Active
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