JP2018535199A5 - - Google Patents
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- Publication number
- JP2018535199A5 JP2018535199A5 JP2018517807A JP2018517807A JP2018535199A5 JP 2018535199 A5 JP2018535199 A5 JP 2018535199A5 JP 2018517807 A JP2018517807 A JP 2018517807A JP 2018517807 A JP2018517807 A JP 2018517807A JP 2018535199 A5 JP2018535199 A5 JP 2018535199A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- substituted
- hydrogen
- het
- 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 154
- 229910052739 hydrogen Inorganic materials 0.000 claims 37
- 239000001257 hydrogen Substances 0.000 claims 37
- 125000001424 substituent group Chemical group 0.000 claims 24
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 23
- 150000002431 hydrogen Chemical group 0.000 claims 22
- 125000005843 halogen group Chemical group 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000004852 Lung Injury Diseases 0.000 claims 1
- 208000034486 Multi-organ failure Diseases 0.000 claims 1
- 208000010718 Multiple Organ Failure Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010069363 Traumatic lung injury Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 231100000515 lung injury Toxicity 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000029744 multiple organ dysfunction syndrome Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 230000019100 sperm motility Effects 0.000 claims 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
- -1 — (C═O) —OR 5h Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15189163 | 2015-10-09 | ||
| EP15189163.7 | 2015-10-09 | ||
| EP16174710.0 | 2016-06-16 | ||
| EP16174710 | 2016-06-16 | ||
| PCT/EP2016/073962 WO2017060406A1 (en) | 2015-10-09 | 2016-10-07 | Quinoxaline and pyridopyrazine derivatives as pi3kbeta inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018535199A JP2018535199A (ja) | 2018-11-29 |
| JP2018535199A5 true JP2018535199A5 (https=) | 2019-11-07 |
| JP6912460B2 JP6912460B2 (ja) | 2021-08-04 |
Family
ID=57104028
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018517807A Active JP6912460B2 (ja) | 2015-10-09 | 2016-10-07 | ＰＩ３Ｋβ阻害剤としてのキノキサリンおよびピリドピラジン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US10526316B2 (https=) |
| EP (1) | EP3359533B1 (https=) |
| JP (1) | JP6912460B2 (https=) |
| KR (1) | KR102630111B1 (https=) |
| CN (1) | CN108349946B (https=) |
| AU (1) | AU2016335086B2 (https=) |
| BR (1) | BR112018007068B1 (https=) |
| CA (1) | CA2999818C (https=) |
| EA (1) | EA037401B1 (https=) |
| ES (1) | ES2905673T3 (https=) |
| IL (1) | IL258513B (https=) |
| MA (1) | MA45896A (https=) |
| MX (1) | MX382601B (https=) |
| WO (1) | WO2017060406A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10526316B2 (en) | 2015-10-09 | 2020-01-07 | Janssen Pharmaceutica Nv | Quinoxaline and pyridopyrazine derivatives as PI3Kβ inhibitors |
| DK3472160T3 (da) | 2016-06-16 | 2021-05-10 | Janssen Pharmaceutica Nv | Bicykliske pyridin-, pyrazin- og pyrimidinderivater som pi3k-beta-inhibitorer |
| EP3601254B1 (en) * | 2017-03-29 | 2022-05-25 | Janssen Pharmaceutica NV | Quinoxaline and pyridopyrazine derivatives as pi3k-beta inhibitors |
| BR112020018094A2 (pt) | 2018-03-08 | 2020-12-22 | Incyte Corporation | Compostos de aminopirazina diol como inibidores de pi3k-¿ |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| CN111892597B (zh) * | 2020-09-01 | 2023-07-25 | 山西天宏达安医药科技有限公司 | 一种喹喔啉基吡啶并吡嗪类化合物及其制备方法与应用 |
| WO2024026419A1 (en) * | 2022-07-27 | 2024-02-01 | Black Diamond Therapeutics, Inc. | Quinoxaline derivatives as pik3 alpha modulators |
| AU2024272375A1 (en) * | 2023-05-12 | 2026-01-08 | Mirati Therapeutics, Inc. | Substituted quinoxalines |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1993537A4 (en) | 2006-03-02 | 2010-05-19 | Glaxosmithkline Llc | THIAZOLONES AS INHIBITORS OF P13-KINASES |
| WO2008014219A2 (en) | 2006-07-24 | 2008-01-31 | Smithkline Beecham Corporation | Thiozolidinedione derivatives as p13 kinase inhibitors |
| NZ578229A (en) * | 2007-02-22 | 2012-02-24 | Merck Serono Sa | Quinoxaline compounds and use thereof |
| WO2009021083A1 (en) | 2007-08-09 | 2009-02-12 | Smithkline Beecham Corporation | Quinoxaline derivatives as pi3 kinase inhibitors |
| EP3613743B1 (en) | 2008-01-04 | 2022-03-16 | Intellikine, LLC | Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives |
| PE20121148A1 (es) | 2009-08-17 | 2012-09-07 | Intellikine Llc | Compuestos heterociclicos y usos de los mismos |
| KR20120081164A (ko) | 2009-09-29 | 2012-07-18 | 엑스커버리 홀딩 컴퍼니 엘엘씨 | Ｐｉ3ｋ(델타) 선택적 억제제 |
| US8399460B2 (en) * | 2009-10-27 | 2013-03-19 | Astrazeneca Ab | Chromenone derivatives |
| UY33304A (es) | 2010-04-02 | 2011-10-31 | Amgen Inc | Compuestos heterocíclicos y sus usos |
| JP5719028B2 (ja) | 2010-10-06 | 2015-05-13 | グラクソスミスクライン エルエルシー | Ｐｉ３キナーゼ阻害剤としてのベンズイミダゾール誘導体 |
| WO2012116237A2 (en) | 2011-02-23 | 2012-08-30 | Intellikine, Llc | Heterocyclic compounds and uses thereof |
| UY34013A (es) * | 2011-04-13 | 2012-11-30 | Astrazeneca Ab | ?compuestos de cromenona con actividad anti-tumoral?. |
| WO2013028263A1 (en) | 2011-08-24 | 2013-02-28 | Glaxosmithkline Llc | Pyrazolopyrimidine derivatives as pi3 kinase inhibitors |
| WO2013095761A1 (en) | 2011-12-20 | 2013-06-27 | Glaxosmithkline Llc | Imidazopyridine derivatives as pi3 kinase inhibitors |
| US8778937B2 (en) | 2011-12-20 | 2014-07-15 | Glaxosmithkline Llc | Benzimidazole boronic acid derivatives as PI3 kinase inhibitors |
| GB201212513D0 (en) | 2012-07-13 | 2012-08-29 | Ucb Pharma Sa | Therapeutic agents |
| AU2015366202B2 (en) | 2014-12-19 | 2020-01-02 | Janssen Pharmaceutica Nv | Heterocyclyl linked imidazopyridazine derivatives as PI3Kbeta inhibitors |
| MA41174B1 (fr) | 2014-12-19 | 2019-09-30 | Janssen Pharmaceutica Nv | Dérivés d'imidazopyridazine utilisés en tant qu'inhibiteurs de pi3kbeta |
| US10526316B2 (en) | 2015-10-09 | 2020-01-07 | Janssen Pharmaceutica Nv | Quinoxaline and pyridopyrazine derivatives as PI3Kβ inhibitors |
-
2016
- 2016-10-07 US US15/766,887 patent/US10526316B2/en active Active
- 2016-10-07 CA CA2999818A patent/CA2999818C/en active Active
- 2016-10-07 MA MA045896A patent/MA45896A/fr unknown
- 2016-10-07 MX MX2018004304A patent/MX382601B/es unknown
- 2016-10-07 AU AU2016335086A patent/AU2016335086B2/en not_active Ceased
- 2016-10-07 ES ES16778024T patent/ES2905673T3/es active Active
- 2016-10-07 KR KR1020187011663A patent/KR102630111B1/ko active Active
- 2016-10-07 BR BR112018007068-8A patent/BR112018007068B1/pt active IP Right Grant
- 2016-10-07 EP EP16778024.6A patent/EP3359533B1/en active Active
- 2016-10-07 EA EA201890906A patent/EA037401B1/ru unknown
- 2016-10-07 WO PCT/EP2016/073962 patent/WO2017060406A1/en not_active Ceased
- 2016-10-07 JP JP2018517807A patent/JP6912460B2/ja active Active
- 2016-10-07 CN CN201680058332.2A patent/CN108349946B/zh active Active
-
2018
- 2018-04-05 IL IL258513A patent/IL258513B/en active IP Right Grant
-
2019
- 2019-11-12 US US16/680,605 patent/US11267804B2/en active Active
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