JP2015524457A5 - - Google Patents
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- JP2015524457A5 JP2015524457A5 JP2015525852A JP2015525852A JP2015524457A5 JP 2015524457 A5 JP2015524457 A5 JP 2015524457A5 JP 2015525852 A JP2015525852 A JP 2015525852A JP 2015525852 A JP2015525852 A JP 2015525852A JP 2015524457 A5 JP2015524457 A5 JP 2015524457A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- optionally
- cycloalkyl
- group
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 36
- 125000003107 substituted aryl group Chemical group 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 21
- 229910052760 oxygen Inorganic materials 0.000 claims 20
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 19
- 229910052717 sulfur Inorganic materials 0.000 claims 17
- 239000003814 drug Substances 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 239000000654 additive Substances 0.000 claims 7
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 239000000969 carrier Substances 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 5
- 125000003367 polycyclic group Chemical group 0.000 claims 5
- 239000003446 ligand Substances 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 125000002877 alkyl aryl group Chemical group 0.000 claims 3
- 239000013078 crystal Substances 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- -1 —CF 3 Chemical group 0.000 claims 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- 229940123066 Polymerase inhibitor Drugs 0.000 claims 2
- 238000003556 assay Methods 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 229940126523 co-drug Drugs 0.000 claims 2
- 206010022000 influenza Diseases 0.000 claims 2
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- 101800004538 Bradykinin Proteins 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- 102100031780 Endonuclease Human genes 0.000 claims 1
- 108010042407 Endonucleases Proteins 0.000 claims 1
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 claims 1
- 102100035792 Kininogen-1 Human genes 0.000 claims 1
- 239000000867 Lipoxygenase Inhibitor Substances 0.000 claims 1
- 229940123424 Neuraminidase inhibitor Drugs 0.000 claims 1
- OFHCOWSQAMBJIW-AVJTYSNKSA-N alfacalcidol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C OFHCOWSQAMBJIW-AVJTYSNKSA-N 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 claims 1
- 229930003827 cannabinoid Natural products 0.000 claims 1
- 239000003557 cannabinoid Substances 0.000 claims 1
- 229940125400 channel inhibitor Drugs 0.000 claims 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 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 238000002866 fluorescence resonance energy transfer Methods 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical group 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000002911 sialidase inhibitor Substances 0.000 claims 1
- 230000008685 targeting Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261679968P | 2012-08-06 | 2012-08-06 | |
| US61/679,968 | 2012-08-06 | ||
| PCT/EP2013/066388 WO2014023691A1 (en) | 2012-08-06 | 2013-08-05 | Dihydroxypyrimidine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015524457A JP2015524457A (ja) | 2015-08-24 |
| JP2015524457A5 true JP2015524457A5 (enExample) | 2016-09-23 |
Family
ID=49118489
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015525852A Pending JP2015524457A (ja) | 2012-08-06 | 2013-08-05 | ジヒドロキシピリミジン炭酸誘導体及びウイルス性疾患の治療、改善又は予防における使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8921388B2 (enExample) |
| EP (1) | EP2885289A1 (enExample) |
| JP (1) | JP2015524457A (enExample) |
| KR (1) | KR20150039832A (enExample) |
| CN (1) | CN104619699A (enExample) |
| BR (1) | BR112015002516A2 (enExample) |
| CA (1) | CA2879245A1 (enExample) |
| HK (2) | HK1210177A1 (enExample) |
| MX (1) | MX2015001478A (enExample) |
| RU (1) | RU2015107803A (enExample) |
| WO (1) | WO2014023691A1 (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| PL3808749T3 (pl) | 2012-12-07 | 2023-07-10 | Vertex Pharmaceuticals Incorporated | Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych |
| EP2970288A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| JP2016512239A (ja) | 2013-03-15 | 2016-04-25 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な化合物 |
| PL3077397T3 (pl) | 2013-12-06 | 2020-04-30 | Vertex Pharmaceuticals Inc. | Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne |
| SG10201902206QA (en) | 2014-06-05 | 2019-04-29 | Vertex Pharma | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
| PT3157566T (pt) | 2014-06-17 | 2019-07-11 | Vertex Pharma | Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr |
| CA2953862A1 (en) | 2014-07-07 | 2016-01-14 | F. Hoffmann-La Roche Ag | Dihydropyridopyrazine-1,8-diones and their use in the treatment, amelioration or prevention of viral diseases |
| US10774051B2 (en) * | 2015-04-24 | 2020-09-15 | Shionogi & Co., Ltd. | 6-membered heterocyclic derivatives and pharmaceutical composition comprising the same |
| EP4219508B1 (en) | 2015-04-28 | 2024-06-05 | Shionogi & Co., Ltd | Substituted polycyclic pyridone derivative and prodrug thereof |
| ES2938877T3 (es) | 2015-04-28 | 2023-04-17 | Shionogi & Co | Derivados de piridona policíclicos sustituidos y profármacos de los mismos |
| US20170081331A1 (en) | 2015-09-18 | 2017-03-23 | F. Hoffmann-La Roche Ag | Pyrazolopyrazines and their use in the treatment, amelioration or prevention of a viral disease |
| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| EP3374350B1 (en) | 2015-11-09 | 2022-01-05 | Forge Therapeutics, Inc. | Hydroxypyridinone and hydroxypyrimidinone based compounds for treating bacterial infections |
| WO2017083434A1 (en) | 2015-11-09 | 2017-05-18 | Forge Therapeutics, Inc. | Pyrone based compounds for treating bacterial infections |
| CR20180356A (es) | 2015-12-15 | 2018-08-22 | Shionogi & Co | Un medicamento caracterizado por combinar un inhibidor de la endonucleasa cap-dependiente del virus de la influenza y un fármaco anti-influenza |
| JP6957535B2 (ja) | 2016-06-29 | 2021-11-02 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ピリダジノンベースの広域スペクトル抗インフルエンザ阻害剤 |
| NZ791086A (en) | 2016-08-10 | 2025-08-29 | Shionogi & Co | Substituted polycyclic pyridone derivative and pharmaceutical composition containing prodrug thereof |
| JP6692113B2 (ja) * | 2016-10-21 | 2020-05-13 | 塩野義製薬株式会社 | ６員複素環誘導体を含有する医薬組成物 |
| WO2018208985A2 (en) | 2017-05-10 | 2018-11-15 | Forge Therapeutics, Inc. | Antibacterial compounds |
| JP2020533376A (ja) | 2017-09-15 | 2020-11-19 | アドゥロ バイオテック，インク． | ピラゾロピリミジノン化合物およびその使用 |
| CN109503528B (zh) * | 2018-05-15 | 2022-06-14 | 天津国际生物医药联合研究院 | 一种化合物及其在抗沙粒病毒感染中的应用 |
| JP7495395B2 (ja) * | 2018-09-20 | 2024-06-04 | ブラックスミス メディシンズ，インク． | 抗菌性化合物 |
| CA3122093A1 (en) | 2018-12-06 | 2020-06-11 | Constellation Pharmaceuticals, Inc. | Modulators of trex1 |
| CN109897007A (zh) * | 2019-02-25 | 2019-06-18 | 天津国际生物医药联合研究院 | 二羟基嘧啶化合物及其应用 |
| WO2021195260A1 (en) | 2020-03-25 | 2021-09-30 | Forge Therapeutics, Inc. | Lpxc inhibitor and methods of making |
| US20210315902A1 (en) * | 2020-03-25 | 2021-10-14 | Forge Therapeutics, Inc. | Lpxc inhibitor, formulations, and uses thereof |
| CA3191084A1 (en) | 2020-09-09 | 2022-03-17 | Gerald Burke | Formulations of a somatostatin modulator |
| BR112023022917A2 (pt) * | 2021-05-05 | 2024-01-23 | Constellation Pharmaceuticals Inc | Moduladores de trex1 |
| MX2024003859A (es) | 2021-09-28 | 2024-05-21 | Blacksmith Medicines Inc | Inhibidores de lpxc y usos de estos. |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5475109A (en) | 1994-10-17 | 1995-12-12 | Merck & Co., Inc. | Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease |
| AU2002334205B2 (en) * | 2001-10-26 | 2007-07-05 | Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa | Dihydroxypyrimidine carboxamide inhibitors of HIV integrase |
| US7169780B2 (en) * | 2001-10-26 | 2007-01-30 | Istitute Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase |
| US20040176366A1 (en) | 2002-08-30 | 2004-09-09 | Wathen Michael W | Method of preventing or treating atherosclerosis or restenosis |
| TW200526635A (en) * | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
| JP2007517900A (ja) * | 2004-01-12 | 2007-07-05 | ギリアード サイエンシーズ， インコーポレイテッド | ピリミジンホスホネート抗ウイルス化合物および使用方法 |
| JP4953297B2 (ja) | 2004-09-15 | 2012-06-13 | 塩野義製薬株式会社 | Ｈｉｖインテグラーゼ阻害活性を有するカルバモイルピリドン誘導体 |
| TW200716632A (en) | 2005-05-16 | 2007-05-01 | Gilead Sciences Inc | Integrase inhibitor compounds |
| TWI518084B (zh) | 2009-03-26 | 2016-01-21 | 鹽野義製藥股份有限公司 | 哌喃酮與吡啶酮衍生物之製造方法 |
| EP2412708A4 (en) | 2009-03-26 | 2014-07-23 | Shionogi & Co | SUBSTITUTED 3-HYDROXY-4-PYRIDONE DERIVATIVE |
| WO2011000566A2 (en) | 2009-06-30 | 2011-01-06 | Savira Pharmaceuticals Gmbh | Compounds and pharmaceutical compositions for the treatment of negative-sense ssrna virus infections |
| US20130065857A1 (en) | 2009-10-12 | 2013-03-14 | Baylor College Of Medicine | Novel dxr inhibitors for antimicrobial therapy |
| WO2012088283A1 (en) | 2010-12-23 | 2012-06-28 | Baylor College Of Medicine | Small molecule compounds as broad-spectrum inhibitors of metallo-beta-lactamases |
| WO2012151567A1 (en) * | 2011-05-05 | 2012-11-08 | St. Jude Children's Research Hospital | Pyrimidinone compounds and methods for preventing and treating influenza |
| CN102617487B (zh) * | 2012-03-02 | 2014-04-02 | 北京工业大学 | 多取代嘧啶酮类化合物及其制备方法和应用 |
| CN102911124B (zh) * | 2012-10-25 | 2015-11-25 | 山东大学 | 羟基嘧啶酮类化合物及其制备方法与应用 |
-
2013
- 2013-08-05 JP JP2015525852A patent/JP2015524457A/ja active Pending
- 2013-08-05 CA CA2879245A patent/CA2879245A1/en not_active Abandoned
- 2013-08-05 US US13/958,913 patent/US8921388B2/en not_active Expired - Fee Related
- 2013-08-05 CN CN201380041462.1A patent/CN104619699A/zh active Pending
- 2013-08-05 WO PCT/EP2013/066388 patent/WO2014023691A1/en not_active Ceased
- 2013-08-05 MX MX2015001478A patent/MX2015001478A/es unknown
- 2013-08-05 RU RU2015107803A patent/RU2015107803A/ru not_active Application Discontinuation
- 2013-08-05 HK HK15111131.0A patent/HK1210177A1/xx unknown
- 2013-08-05 HK HK15112102.3A patent/HK1211289A1/xx unknown
- 2013-08-05 BR BR112015002516A patent/BR112015002516A2/pt not_active IP Right Cessation
- 2013-08-05 EP EP13759141.8A patent/EP2885289A1/en not_active Withdrawn
- 2013-08-05 KR KR20157005600A patent/KR20150039832A/ko not_active Withdrawn
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