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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- 150000008163 sugars Chemical class 0.000 description 1
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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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pulmonology (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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Family Applications (1)
| 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 |
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| CN107074880A (zh) | 2014-07-07 | 2017-08-18 | 萨维拉制药有限公司 | 二氢吡啶并吡嗪‑1,8‑二酮和它们在治疗、改善或预防病毒疾病中的用途 |
| US10081616B2 (en) * | 2014-08-28 | 2018-09-25 | X-Chem, Inc. | Soluble epoxide hydrolase inhibitors and uses thereof |
| WO2016133888A1 (en) * | 2015-02-16 | 2016-08-25 | Biota Pharmaceuticals, Inc. | Compounds for treating respiratory syncytial virus infections |
| ES2857906T3 (es) | 2015-04-28 | 2021-09-29 | Shionogi & Co | Derivado de piridona policíclica contra la influenza y profármaco del mismo |
| 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 |
| SG10201911957QA (en) | 2015-12-15 | 2020-02-27 | Shionogi & Co | Medicine for treating influenza characterized by comprising combination of cap-dependent endonuclease inhibitor with anti-influenza drug |
| 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 |
| EP4458348A3 (en) | 2016-08-10 | 2025-01-29 | Shionogi & Co., Ltd | Pharmaceutical compositions containing substituted polycyclic pyridone derivatives and prodrug thereof |
| CA3069990A1 (en) | 2017-08-01 | 2019-02-07 | Theravance Biopharma R&D Ip, Llc | Pyrazolo and triazolo bicyclic compounds as jak kinase inhibitors |
| CN113498352A (zh) | 2019-01-23 | 2021-10-12 | 施万生物制药研发Ip有限责任公司 | 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪 |
| CN116096725A (zh) * | 2020-04-08 | 2023-05-09 | 雷密克斯医疗公司 | 用于调节剪接的化合物和方法 |
| CN116997555A (zh) * | 2021-03-17 | 2023-11-03 | 豪夫迈·罗氏有限公司 | 新颖噻吩并嘧啶酮衍生物 |
| US11932656B1 (en) | 2023-10-06 | 2024-03-19 | King Faisal University | Thieno[2,3-d]pyrimidines as COX-2 inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US5475109A (en) | 1994-10-17 | 1995-12-12 | Merck & Co., Inc. | Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease |
| KR100714519B1 (ko) * | 2002-03-07 | 2007-05-07 | 에프. 호프만-라 로슈 아게 | 이환 피리딘 및 피리미딘 ｐ38 키나아제 억제제 |
| EP1790638B1 (en) | 2004-09-15 | 2013-04-03 | Shionogi Co., Ltd. | Carbamoylpyridone derivative having hiv integrase inhibitory activity |
| ES2564422T3 (es) * | 2007-11-15 | 2016-03-22 | Ym Biosciences Australia Pty Ltd | Compuestos heterocíclicos que contienen N |
| 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 |
| EP2412708A4 (en) | 2009-03-26 | 2014-07-23 | Shionogi & Co | SUBSTITUTED 3-HYDROXY-4-PYRIDONE DERIVATIVE |
| 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 WO PCT/EP2012/070760 patent/WO2013057253A1/en not_active Ceased
- 2012-10-19 JP JP2014536253A patent/JP6033873B2/ja not_active Expired - Fee Related
- 2012-10-19 EP EP12787384.2A patent/EP2794616B1/en not_active Not-in-force
- 2012-10-19 ES ES12787384.2T patent/ES2589459T3/es active Active
- 2012-10-19 KR KR1020147013721A patent/KR20140097197A/ko not_active Withdrawn
- 2012-10-19 CN CN201280051684.7A patent/CN103958521B/zh not_active Expired - Fee Related
- 2012-10-19 CA CA2852843A patent/CA2852843A1/en not_active Abandoned
- 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 MX MX2014003801A patent/MX342176B/es active IP Right Grant
-
2016
- 2016-06-15 US US15/182,705 patent/US20160376286A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20130102601A1 (en) | 2013-04-25 |
| ES2589459T3 (es) | 2016-11-14 |
| MX342176B (es) | 2016-09-20 |
| BR112014008412A2 (pt) | 2017-04-11 |
| CN103958521A (zh) | 2014-07-30 |
| KR20140097197A (ko) | 2014-08-06 |
| CN103958521B (zh) | 2016-10-19 |
| HK1199881A1 (en) | 2015-07-24 |
| EP2794616A1 (en) | 2014-10-29 |
| WO2013057253A1 (en) | 2013-04-25 |
| JP2014530838A (ja) | 2014-11-20 |
| MX2014003801A (es) | 2015-03-11 |
| US20160376286A1 (en) | 2016-12-29 |
| EP2794616B1 (en) | 2016-06-29 |
| CA2852843A1 (en) | 2013-04-25 |
| RU2014120477A (ru) | 2015-11-27 |
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