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
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- compound
- carboxylic acid
- mmol
- expected compound
- pyridine
- 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.)
- Expired - Fee Related
Links
- 0 **1N=C(*)c(c(*)c2*)c1nc2O Chemical compound **1N=C(*)c(c(*)c2*)c1nc2O 0.000 description 18
- ACDXIFJYNXVULR-UHFFFAOYSA-N CC(C)c1cccc(-c(cc2)cnc2C(NO)=O)c1 Chemical compound CC(C)c1cccc(-c(cc2)cnc2C(NO)=O)c1 ACDXIFJYNXVULR-UHFFFAOYSA-N 0.000 description 2
- BSDGZUDFPKIYQG-UHFFFAOYSA-N Brc1ccncc1 Chemical compound Brc1ccncc1 BSDGZUDFPKIYQG-UHFFFAOYSA-N 0.000 description 1
- AOVMKJINVUYSBS-UHFFFAOYSA-N CC(C)C1=CCCC(c2cc(C[N-](C3=O)O)c3nc2)=C1 Chemical compound CC(C)C1=CCCC(c2cc(C[N-](C3=O)O)c3nc2)=C1 AOVMKJINVUYSBS-UHFFFAOYSA-N 0.000 description 1
- KUUWDWVXHOUGHC-UHFFFAOYSA-N CC1C(CNOCc2ccccc2)=CC=CC1 Chemical compound CC1C(CNOCc2ccccc2)=CC=CC1 KUUWDWVXHOUGHC-UHFFFAOYSA-N 0.000 description 1
- SAZSNDHPVFNVPZ-UHFFFAOYSA-N CN(CC1)CCN1c1ccnc(C(N(Cc2ccccc2)O)=O)c1 Chemical compound CN(CC1)CCN1c1ccnc(C(N(Cc2ccccc2)O)=O)c1 SAZSNDHPVFNVPZ-UHFFFAOYSA-N 0.000 description 1
- DSAIDOCXPGZVFP-UHFFFAOYSA-N COC(c(cc1)ncc1N1CCCCC1)=O Chemical compound COC(c(cc1)ncc1N1CCCCC1)=O DSAIDOCXPGZVFP-UHFFFAOYSA-N 0.000 description 1
- DSZRRVXOBFMTPY-UHFFFAOYSA-N Cc([s]c(N=C(N)N1)c2C1=O)c2-c(cc1)ccc1F Chemical compound Cc([s]c(N=C(N)N1)c2C1=O)c2-c(cc1)ccc1F DSZRRVXOBFMTPY-UHFFFAOYSA-N 0.000 description 1
- XYEOALKITRFCJJ-UHFFFAOYSA-N NOCc1ccccc1 Chemical compound NOCc1ccccc1 XYEOALKITRFCJJ-UHFFFAOYSA-N 0.000 description 1
- ZWYMVSUFMHBMGA-UHFFFAOYSA-N O=C(c(cc1)ncc1-c1ccccc1)NOCc1ccccc1 Chemical compound O=C(c(cc1)ncc1-c1ccccc1)NOCc1ccccc1 ZWYMVSUFMHBMGA-UHFFFAOYSA-N 0.000 description 1
- KVMMIDQDXZOPAB-UHFFFAOYSA-N OC(c1cc(cccc2)c2cn1)=O Chemical compound OC(c1cc(cccc2)c2cn1)=O KVMMIDQDXZOPAB-UHFFFAOYSA-N 0.000 description 1
- DJXDQXKCPCKIFS-UHFFFAOYSA-N ON(Cc1ccccc1)C(c(cc1)ncc1N1CCCC1)=O Chemical compound ON(Cc1ccccc1)C(c(cc1)ncc1N1CCCC1)=O DJXDQXKCPCKIFS-UHFFFAOYSA-N 0.000 description 1
- UXMUNRLTVOGMCA-UHFFFAOYSA-N ON(Cc1ccccc1)C(c1cc(-c(cc2)ccc2Cl)ccn1)=O Chemical compound ON(Cc1ccccc1)C(c1cc(-c(cc2)ccc2Cl)ccn1)=O UXMUNRLTVOGMCA-UHFFFAOYSA-N 0.000 description 1
- ZQKKQOFRVZHQKV-UHFFFAOYSA-N ONC(C1=NC=C2C=CC=CC2C1)=O Chemical compound ONC(C1=NC=C2C=CC=CC2C1)=O ZQKKQOFRVZHQKV-UHFFFAOYSA-N 0.000 description 1
- RJBSYHWLSDDXBW-UHFFFAOYSA-N ONC(c1cc([N+]([SH-](Cc(cc2Cl)ccc2Cl)=O)=O)ccn1)=O Chemical compound ONC(c1cc([N+]([SH-](Cc(cc2Cl)ccc2Cl)=O)=O)ccn1)=O RJBSYHWLSDDXBW-UHFFFAOYSA-N 0.000 description 1
- PDYHLDGWKQJXDD-UHFFFAOYSA-N ONC(c1cc(cccc2)c2cn1)=O Chemical compound ONC(c1cc(cccc2)c2cn1)=O PDYHLDGWKQJXDD-UHFFFAOYSA-N 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)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (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
ID=47189887
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 |
|---|---|---|---|---|
| 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 |
| AU2015306643B2 (en) * | 2014-08-28 | 2020-05-07 | 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 |
| CN107709321A (zh) | 2015-04-28 | 2018-02-16 | 盐野义制药株式会社 | 经取代的多环性吡啶酮衍生物及其前药 |
| 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 |
| HK1254961A1 (en) | 2015-12-15 | 2019-08-02 | Shionogi & Co., Ltd. | Medicine for treating influenza characterized by comprising combination of cap-dependent endonuclease inhibitor with anti-influenza drug |
| 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 |
| US10759814B2 (en) | 2016-08-10 | 2020-09-01 | Shionogi & Co., Ltd. | Pharmaceutical compositions containing substituted polycyclic pyridone derivatives and prodrug thereof |
| CN111032646B (zh) | 2017-08-01 | 2023-01-03 | 施万生物制药研发Ip有限责任公司 | 作为jak激酶抑制剂的吡唑并和三唑并双环化合物 |
| 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 |
| MX2022012677A (es) * | 2020-04-08 | 2023-01-11 | Remix Therapeutics Inc | Compuestos y metodos para modular el empalme. |
| 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 |
| KR100714519B1 (ko) * | 2002-03-07 | 2007-05-07 | 에프. 호프만-라 로슈 아게 | 이환 피리딘 및 피리미딘 ｐ38 키나아제 억제제 |
| 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 |
| SI2215094T1 (sl) * | 2007-11-15 | 2016-05-31 | Ym Biosciences Australia Pty Ltd | N vsebujoče heterociklične spojine |
| EP2923734B1 (en) | 2009-03-13 | 2018-01-10 | Katholieke Universiteit Leuven, K.U. Leuven R&D | Purine analogues and their use as immunosuppressive agents |
| US8835461B2 (en) | 2009-03-26 | 2014-09-16 | Shionogi & Co., Ltd. | 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 ES ES12787384.2T patent/ES2589459T3/es active Active
- 2012-10-19 EP EP12787384.2A patent/EP2794616B1/en not_active Not-in-force
- 2012-10-19 WO PCT/EP2012/070760 patent/WO2013057253A1/en not_active Ceased
- 2012-10-19 BR BR112014008412A patent/BR112014008412A2/pt not_active IP Right Cessation
- 2012-10-19 CN CN201280051684.7A patent/CN103958521B/zh not_active Expired - Fee Related
- 2012-10-19 KR KR1020147013721A patent/KR20140097197A/ko not_active Withdrawn
- 2012-10-19 MX MX2014003801A patent/MX342176B/es active IP Right Grant
- 2012-10-19 JP JP2014536253A patent/JP6033873B2/ja not_active Expired - Fee Related
- 2012-10-19 RU RU2014120477/04A patent/RU2014120477A/ru not_active Application Discontinuation
- 2012-10-19 CA CA2852843A patent/CA2852843A1/en not_active Abandoned
-
2016
- 2016-06-15 US US15/182,705 patent/US20160376286A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| MX2014003801A (es) | 2015-03-11 |
| MX342176B (es) | 2016-09-20 |
| HK1199881A1 (en) | 2015-07-24 |
| KR20140097197A (ko) | 2014-08-06 |
| ES2589459T3 (es) | 2016-11-14 |
| CN103958521B (zh) | 2016-10-19 |
| EP2794616A1 (en) | 2014-10-29 |
| US20160376286A1 (en) | 2016-12-29 |
| CN103958521A (zh) | 2014-07-30 |
| EP2794616B1 (en) | 2016-06-29 |
| WO2013057253A1 (en) | 2013-04-25 |
| US20130102601A1 (en) | 2013-04-25 |
| JP2014530838A (ja) | 2014-11-20 |
| CA2852843A1 (en) | 2013-04-25 |
| BR112014008412A2 (pt) | 2017-04-11 |
| RU2014120477A (ru) | 2015-11-27 |
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