CN102741255B - 作为双氢乳清酸脱氢酶抑制剂的抗疟剂 - Google Patents
作为双氢乳清酸脱氢酶抑制剂的抗疟剂 Download PDFInfo
- Publication number
- CN102741255B CN102741255B CN201080043385.XA CN201080043385A CN102741255B CN 102741255 B CN102741255 B CN 102741255B CN 201080043385 A CN201080043385 A CN 201080043385A CN 102741255 B CN102741255 B CN 102741255B
- Authority
- CN
- China
- Prior art keywords
- compound
- methyl
- mmol
- synthesis
- triazolo
- 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 Cc1nc2ncc[n]2c(Nc2ccc(*)cc2)c1 Chemical compound Cc1nc2ncc[n]2c(Nc2ccc(*)cc2)c1 0.000 description 3
- WCBJYRWGIUTUDN-UHFFFAOYSA-N CC(C)c1n[n]2c(O)cc(C)nc2n1 Chemical compound CC(C)c1n[n]2c(O)cc(C)nc2n1 WCBJYRWGIUTUDN-UHFFFAOYSA-N 0.000 description 1
- OIZSVTOIBNSVOS-UHFFFAOYSA-N CC(c1n[n]2c(Nc(cc3)ccc3S(F)(F)(F)(F)F)cc(C)nc2n1)(F)F Chemical compound CC(c1n[n]2c(Nc(cc3)ccc3S(F)(F)(F)(F)F)cc(C)nc2n1)(F)F OIZSVTOIBNSVOS-UHFFFAOYSA-N 0.000 description 1
- CUCVTDOXQYMYKL-UHFFFAOYSA-N CC(c1n[n]2c(Nc3ccc(C(F)(F)F)cc3)cc(C)nc2n1)(F)F Chemical compound CC(c1n[n]2c(Nc3ccc(C(F)(F)F)cc3)cc(C)nc2n1)(F)F CUCVTDOXQYMYKL-UHFFFAOYSA-N 0.000 description 1
- DJWKVIKEQRMJEF-UHFFFAOYSA-N CCC(c1n[n]2c(Nc3ccc(C(F)(F)F)cc3)cc(C)nc2n1)(F)F Chemical compound CCC(c1n[n]2c(Nc3ccc(C(F)(F)F)cc3)cc(C)nc2n1)(F)F DJWKVIKEQRMJEF-UHFFFAOYSA-N 0.000 description 1
- KLMAQENUZGRGRE-UHFFFAOYSA-N Cc1nc2nc(SC)n[n]2c(Nc2ccc(C(F)(F)F)cc2)c1 Chemical compound Cc1nc2nc(SC)n[n]2c(Nc2ccc(C(F)(F)F)cc2)c1 KLMAQENUZGRGRE-UHFFFAOYSA-N 0.000 description 1
- DDGIVYHVYWISJQ-UHFFFAOYSA-N Cc1nc2ncc[n]2c(Nc2cc(CCC3)c3cc2)c1 Chemical compound Cc1nc2ncc[n]2c(Nc2cc(CCC3)c3cc2)c1 DDGIVYHVYWISJQ-UHFFFAOYSA-N 0.000 description 1
- FZYCPSMDNJRNTQ-UHFFFAOYSA-N Cc1nc2ncc[n]2c(Nc2ccc(C(F)(F)F)c(F)c2)c1 Chemical compound Cc1nc2ncc[n]2c(Nc2ccc(C(F)(F)F)c(F)c2)c1 FZYCPSMDNJRNTQ-UHFFFAOYSA-N 0.000 description 1
- DKYDPWCBBMVYHM-UHFFFAOYSA-N Cc1nc2ncc[n]2c(Nc2ccc(CCCC3)c3c2)c1 Chemical compound Cc1nc2ncc[n]2c(Nc2ccc(CCCC3)c3c2)c1 DKYDPWCBBMVYHM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24686309P | 2009-09-29 | 2009-09-29 | |
| US61/246,863 | 2009-09-29 | ||
| PCT/US2010/050532 WO2011041304A2 (en) | 2009-09-29 | 2010-09-28 | Antimalarial agents that are inhibitors of dihydroorotate dehydrogenase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102741255A CN102741255A (zh) | 2012-10-17 |
| CN102741255B true CN102741255B (zh) | 2015-10-07 |
Family
ID=43826848
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080043385.XA Expired - Fee Related CN102741255B (zh) | 2009-09-29 | 2010-09-28 | 作为双氢乳清酸脱氢酶抑制剂的抗疟剂 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9238653B2 (https=) |
| EP (1) | EP2483274B1 (https=) |
| JP (1) | JP5818266B2 (https=) |
| CN (1) | CN102741255B (https=) |
| BR (1) | BR112012007179B8 (https=) |
| CA (1) | CA2775354C (https=) |
| DK (1) | DK2483274T3 (https=) |
| ES (1) | ES2527835T3 (https=) |
| HR (1) | HRP20150066T1 (https=) |
| ME (1) | ME02020B (https=) |
| PL (1) | PL2483274T3 (https=) |
| PT (1) | PT2483274E (https=) |
| SI (1) | SI2483274T1 (https=) |
| SM (1) | SMT201500071B (https=) |
| WO (1) | WO2011041304A2 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI674263B (zh) * | 2013-12-19 | 2019-10-11 | 瑞士商諾華公司 | 用於治療寄生蟲疾病之化合物及組合物 |
| EP3072894A1 (en) | 2015-03-26 | 2016-09-28 | Board Of Regents Of the University Of Texas System | New substituted triazolopyrimidines as anti-malarial agents |
| EP3254679A1 (de) | 2016-06-09 | 2017-12-13 | Christian-Albrechts-Universität zu Kiel | Wirkstoffe gegen protozoen und bakterien |
| US20200048259A1 (en) * | 2016-10-12 | 2020-02-13 | Merck Sharp & Dohme Corp. | Kdm5 inhibitors |
| JP7595413B2 (ja) | 2016-11-30 | 2024-12-06 | ケース ウエスタン リザーブ ユニバーシティ | 15-pgdh阻害剤とコルチコステロイドおよび/またはtnf阻害剤との組み合わせならびにその使用 |
| WO2018145080A1 (en) | 2017-02-06 | 2018-08-09 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase activity |
| CA3059255A1 (en) | 2017-04-07 | 2018-10-11 | Case Western Reserve University | Inhibitors of short-chain dehydrogenase activity for treating coronary disorders |
| CN120463721A (zh) | 2018-11-21 | 2025-08-12 | 卡斯西部储备大学 | 调节短链脱氢酶活性的组合物和方法 |
| EP3842100A1 (en) | 2019-12-24 | 2021-06-30 | The Board Of Regents Of The University Of Texas System | Anti-malarial agents |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5478825A (en) | 1991-02-22 | 1995-12-26 | Egis Gyogyszergyar | 5-(substituted amino)-1,2,4-triazolo (1,5-A) pyrimidine derivatives |
| HU208693B (en) | 1991-02-22 | 1993-12-28 | Egyt Gyogyszervegyeszeti Gyar | Process for producing 1,2,4-triazolo (1,5-a) pyrimidinis derivatives and their carbicycli-tetrahydro-thiofurane-tetrahydrothiopyrane-, or tetrahydropyridine- condensated derivatives or medical preparatives containing them |
| US8490825B2 (en) | 1999-12-08 | 2013-07-23 | Metal Container Corporation | Can lid closure and method of joining a can lid closure to a can body |
| CZ294535B6 (cs) * | 2001-08-02 | 2005-01-12 | Ústav Experimentální Botaniky Avčr | Heterocyklické sloučeniny na bázi N6-substituovaného adeninu, způsoby jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující |
| US20080027079A1 (en) | 2006-06-22 | 2008-01-31 | Board Of Regents, University Of Texas System | Dihydroorotate dehydrogenase inhibitors with selective anti-malarial activity |
| CN101622001A (zh) * | 2007-01-26 | 2010-01-06 | Irm责任有限公司 | 作为激酶抑制剂用于治疗疟原虫相关疾病的嘌呤化合物和组合物 |
| US9216983B2 (en) | 2007-12-21 | 2015-12-22 | Board Of Regents, University Of Texas System | Dihydroorotate dehydrogenase inhibitors with selective anti-malarial activity |
-
2010
- 2010-09-28 JP JP2012532236A patent/JP5818266B2/ja not_active Expired - Fee Related
- 2010-09-28 HR HRP20150066AT patent/HRP20150066T1/hr unknown
- 2010-09-28 BR BR112012007179A patent/BR112012007179B8/pt not_active IP Right Cessation
- 2010-09-28 ES ES10821105.3T patent/ES2527835T3/es active Active
- 2010-09-28 CA CA2775354A patent/CA2775354C/en not_active Expired - Fee Related
- 2010-09-28 PL PL10821105T patent/PL2483274T3/pl unknown
- 2010-09-28 WO PCT/US2010/050532 patent/WO2011041304A2/en not_active Ceased
- 2010-09-28 PT PT108211053T patent/PT2483274E/pt unknown
- 2010-09-28 US US13/499,031 patent/US9238653B2/en not_active Expired - Fee Related
- 2010-09-28 ME MEP-2015-8A patent/ME02020B/me unknown
- 2010-09-28 DK DK10821105.3T patent/DK2483274T3/en active
- 2010-09-28 EP EP10821105.3A patent/EP2483274B1/en active Active
- 2010-09-28 SI SI201030853T patent/SI2483274T1/sl unknown
- 2010-09-28 CN CN201080043385.XA patent/CN102741255B/zh not_active Expired - Fee Related
-
2015
- 2015-03-18 SM SM201500071T patent/SMT201500071B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2775354C (en) | 2019-01-15 |
| HRP20150066T1 (hr) | 2015-02-27 |
| HK1174639A1 (en) | 2013-06-14 |
| EP2483274B1 (en) | 2014-10-29 |
| EP2483274A2 (en) | 2012-08-08 |
| JP5818266B2 (ja) | 2015-11-18 |
| US9238653B2 (en) | 2016-01-19 |
| WO2011041304A2 (en) | 2011-04-07 |
| DK2483274T3 (en) | 2015-01-19 |
| BR112012007179A8 (pt) | 2018-01-23 |
| SMT201500071B (it) | 2015-05-05 |
| ES2527835T3 (es) | 2015-01-30 |
| PL2483274T3 (pl) | 2015-04-30 |
| BR112012007179B1 (pt) | 2020-12-01 |
| CA2775354A1 (en) | 2011-04-07 |
| CN102741255A (zh) | 2012-10-17 |
| JP2013506004A (ja) | 2013-02-21 |
| SI2483274T1 (sl) | 2015-02-27 |
| ME02020B (me) | 2015-05-20 |
| US20120302586A1 (en) | 2012-11-29 |
| WO2011041304A3 (en) | 2011-08-04 |
| BR112012007179B8 (pt) | 2021-05-25 |
| EP2483274A4 (en) | 2013-03-06 |
| BR112012007179A2 (pt) | 2017-07-25 |
| PT2483274E (pt) | 2015-02-04 |
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| REG | Reference to a national code |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
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Granted publication date: 20151007 Termination date: 20200928 |