JP6033873B2 - ピリミジン−４−オン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その使用 - Google Patents
ピリミジン−４−オン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その使用 Download PDFInfo
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- JP6033873B2 JP6033873B2 JP2014536253A JP2014536253A JP6033873B2 JP 6033873 B2 JP6033873 B2 JP 6033873B2 JP 2014536253 A JP2014536253 A JP 2014536253A JP 2014536253 A JP2014536253 A JP 2014536253A JP 6033873 B2 JP6033873 B2 JP 6033873B2
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- compound
- carboxylic acid
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- pyridine
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- YBBRCQOCSYXUOC-UHFFFAOYSA-N sulfuryl dichloride Chemical compound ClS(Cl)(=O)=O YBBRCQOCSYXUOC-UHFFFAOYSA-N 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 229950009390 symclosene Drugs 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229940061367 tamiflu Drugs 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- YQNLCZUFCGAPEV-UHFFFAOYSA-N tert-butyl 3-[2-[benzyl(hydroxy)carbamoyl]pyridin-4-yl]-8-azabicyclo[3.2.1]oct-3-ene-8-carboxylate Chemical compound CC(C)(C)OC(=O)N1C(C2)CCC1C=C2C(C=1)=CC=NC=1C(=O)N(O)CC1=CC=CC=C1 YQNLCZUFCGAPEV-UHFFFAOYSA-N 0.000 description 1
- RIFXIGDBUBXKEI-UHFFFAOYSA-N tert-butyl 3-oxopiperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCCC(=O)C1 RIFXIGDBUBXKEI-UHFFFAOYSA-N 0.000 description 1
- ZHXRGALVSBYWLF-UHFFFAOYSA-N tert-butyl 4-[2-[benzyl(oxan-2-yloxy)carbamoyl]pyridin-4-yl]piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1C1=CC=NC(C(=O)N(CC=2C=CC=CC=2)OC2OCCCC2)=C1 ZHXRGALVSBYWLF-UHFFFAOYSA-N 0.000 description 1
- JWIOZKDQPDVJNT-UHFFFAOYSA-N tert-butyl 5-(trifluoromethylsulfonyloxy)-3,6-dihydro-2h-pyridine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC=C(OS(=O)(=O)C(F)(F)F)C1 JWIOZKDQPDVJNT-UHFFFAOYSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- CKXZPVPIDOJLLM-UHFFFAOYSA-N tert-butyl n-piperidin-4-ylcarbamate Chemical compound CC(C)(C)OC(=O)NC1CCNCC1 CKXZPVPIDOJLLM-UHFFFAOYSA-N 0.000 description 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
- VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 description 1
- RBNBDIMXFJYDLQ-UHFFFAOYSA-N thieno[3,2-d]pyrimidine Chemical compound C1=NC=C2SC=CC2=N1 RBNBDIMXFJYDLQ-UHFFFAOYSA-N 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 description 1
- 239000003734 thymidylate synthase inhibitor Substances 0.000 description 1
- 229960005196 titanium dioxide Drugs 0.000 description 1
- XJDNKRIXUMDJCW-UHFFFAOYSA-J titanium tetrachloride Chemical compound Cl[Ti](Cl)(Cl)Cl XJDNKRIXUMDJCW-UHFFFAOYSA-J 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 239000001226 triphosphate Substances 0.000 description 1
- 235000011178 triphosphate Nutrition 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 230000035899 viability Effects 0.000 description 1
- 230000029812 viral genome replication Effects 0.000 description 1
- 210000002845 virion Anatomy 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Pulmonology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161550057P | 2011-10-21 | 2011-10-21 | |
| US61/550,057 | 2011-10-21 | ||
| PCT/EP2012/070760 WO2013057253A1 (en) | 2011-10-21 | 2012-10-19 | Pyrimidin-4-one derivatives and their use in the treatment, amelioration or prevention of a viral disease |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014530838A JP2014530838A (ja) | 2014-11-20 |
| JP2014530838A5 JP2014530838A5 (enExample) | 2015-12-03 |
| JP6033873B2 true JP6033873B2 (ja) | 2016-11-30 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014536253A Expired - Fee Related JP6033873B2 (ja) | 2011-10-21 | 2012-10-19 | ピリミジン−４−オン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その使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20130102601A1 (enExample) |
| EP (1) | EP2794616B1 (enExample) |
| JP (1) | JP6033873B2 (enExample) |
| KR (1) | KR20140097197A (enExample) |
| CN (1) | CN103958521B (enExample) |
| BR (1) | BR112014008412A2 (enExample) |
| CA (1) | CA2852843A1 (enExample) |
| ES (1) | ES2589459T3 (enExample) |
| MX (1) | MX342176B (enExample) |
| RU (1) | RU2014120477A (enExample) |
| WO (1) | WO2013057253A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017521424A (ja) | 2014-07-07 | 2017-08-03 | ザヴィラ ファーマシューティカルズ ゲーエムベーハー | ウイルス疾患の治療、改善又は予防におけるジヒドロピリドピラジン−１，８−ジオン及びそれらの使用 |
| MA40538A (fr) * | 2014-08-28 | 2021-04-07 | X Chem Inc | Inhibiteurs de l'époxyde hydrolase soluble et utilisations de ceux-ci |
| WO2016133888A1 (en) * | 2015-02-16 | 2016-08-25 | Biota Pharmaceuticals, Inc. | Compounds for treating respiratory syncytial virus infections |
| DK4219508T3 (da) | 2015-04-28 | 2024-08-05 | Shionogi & Co | Substitueret polycyklisk pyridonderivat og prodrug deraf |
| 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 |
| JP6323860B2 (ja) * | 2015-12-15 | 2018-05-16 | 塩野義製薬株式会社 | キャップ依存的エンドヌクレアーゼ阻害剤及び抗インフルエンザ薬を組み合わせることを特徴とするインフルエンザ治療用医薬 |
| CN109415345B (zh) | 2016-06-29 | 2022-01-11 | 豪夫迈·罗氏有限公司 | 基于哒嗪酮的广谱抗流感抑制剂 |
| AU2017310774B2 (en) | 2016-08-10 | 2023-01-19 | Shionogi & Co., Ltd. | Substituted polycyclic pyridone derivative and pharmaceutical composition containing prodrug thereof |
| EP3652169A1 (en) | 2017-08-01 | 2020-05-20 | Theravance Biopharma R&D IP, LLC | Pyrazolo and triazolo bicyclic compounds as jak kinase inhibitors |
| JP2022518741A (ja) | 2019-01-23 | 2022-03-16 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | ＪＡＫキナーゼ阻害剤としてのイミダゾ［１，５－ａ］ピリジン、１，２，４－トリアゾロ［４，３－ａ］ピリジンおよびイミダゾ［１，５－ａ］ピラジン |
| KR20230004575A (ko) * | 2020-04-08 | 2023-01-06 | 레믹스 테라퓨틱스 인크. | 스플라이싱을 조절하기 위한 화합물 및 방법 |
| EP4308572B1 (en) * | 2021-03-17 | 2025-04-23 | F. Hoffmann-La Roche AG | New thienopyrimidinone derivatives |
| US11932656B1 (en) | 2023-10-06 | 2024-03-19 | King Faisal University | Thieno[2,3-d]pyrimidines as COX-2 inhibitors |
Family Cites Families (8)
| 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 |
| RU2301233C2 (ru) * | 2002-03-07 | 2007-06-20 | Ф.Хоффманн-Ля Рош Аг | Бициклические пиридины и пиримидины в качестве ингибиторов киназы р38 |
| CN101014572B (zh) | 2004-09-15 | 2011-07-06 | 盐野义制药株式会社 | 具有hiv整合酶抑制活性的氨基甲酰基吡啶酮衍生物 |
| AU2008323628B2 (en) * | 2007-11-15 | 2013-10-17 | Ym Biosciences Australia Pty Ltd | N-containing heterocyclic compounds |
| ES2665277T3 (es) | 2009-03-13 | 2018-04-25 | Katholieke Universiteit Leuven K.U. Leuven R&D | Análogos de purina y su uso como agentes inmunosupresores |
| WO2010110231A1 (ja) | 2009-03-26 | 2010-09-30 | 塩野義製薬株式会社 | 置換された３－ヒドロキシ－４－ピリドン誘導体 |
| 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 |
| WO2011000566A2 (en) * | 2009-06-30 | 2011-01-06 | Savira Pharmaceuticals Gmbh | Compounds and pharmaceutical compositions for the treatment of negative-sense ssrna virus infections |
-
2012
- 2012-10-18 US US13/655,418 patent/US20130102601A1/en not_active Abandoned
- 2012-10-19 ES ES12787384.2T patent/ES2589459T3/es active Active
- 2012-10-19 JP JP2014536253A patent/JP6033873B2/ja not_active Expired - Fee Related
- 2012-10-19 CA CA2852843A patent/CA2852843A1/en not_active Abandoned
- 2012-10-19 CN CN201280051684.7A patent/CN103958521B/zh not_active Expired - Fee Related
- 2012-10-19 MX MX2014003801A patent/MX342176B/es active IP Right Grant
- 2012-10-19 WO PCT/EP2012/070760 patent/WO2013057253A1/en not_active Ceased
- 2012-10-19 KR KR1020147013721A patent/KR20140097197A/ko not_active Withdrawn
- 2012-10-19 RU RU2014120477/04A patent/RU2014120477A/ru not_active Application Discontinuation
- 2012-10-19 BR BR112014008412A patent/BR112014008412A2/pt not_active IP Right Cessation
- 2012-10-19 EP EP12787384.2A patent/EP2794616B1/en not_active Not-in-force
-
2016
- 2016-06-15 US US15/182,705 patent/US20160376286A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP2794616B1 (en) | 2016-06-29 |
| MX2014003801A (es) | 2015-03-11 |
| US20130102601A1 (en) | 2013-04-25 |
| ES2589459T3 (es) | 2016-11-14 |
| JP2014530838A (ja) | 2014-11-20 |
| WO2013057253A1 (en) | 2013-04-25 |
| EP2794616A1 (en) | 2014-10-29 |
| BR112014008412A2 (pt) | 2017-04-11 |
| MX342176B (es) | 2016-09-20 |
| CA2852843A1 (en) | 2013-04-25 |
| KR20140097197A (ko) | 2014-08-06 |
| CN103958521B (zh) | 2016-10-19 |
| HK1199881A1 (en) | 2015-07-24 |
| CN103958521A (zh) | 2014-07-30 |
| US20160376286A1 (en) | 2016-12-29 |
| RU2014120477A (ru) | 2015-11-27 |
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