JP6226889B2 - 新規抗マラリア薬 - Google Patents
新規抗マラリア薬 Download PDFInfo
- Publication number
- JP6226889B2 JP6226889B2 JP2014557157A JP2014557157A JP6226889B2 JP 6226889 B2 JP6226889 B2 JP 6226889B2 JP 2014557157 A JP2014557157 A JP 2014557157A JP 2014557157 A JP2014557157 A JP 2014557157A JP 6226889 B2 JP6226889 B2 JP 6226889B2
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- pyrazin
- trifluoromethyl
- amino
- alkyl
- 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 *c1c(N)ncc(Br)n1 Chemical compound *c1c(N)ncc(Br)n1 0.000 description 3
- PVOAHINGSUIXLS-UHFFFAOYSA-N CN1CCNCC1 Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 description 2
- BRWHELOBNYKNCQ-UHFFFAOYSA-N CC(/N=C(\C=N)/N)OCN1CCN(C)CC1 Chemical compound CC(/N=C(\C=N)/N)OCN1CCN(C)CC1 BRWHELOBNYKNCQ-UHFFFAOYSA-N 0.000 description 1
- NZMLBKQYAICUTC-PREYCYJLSA-N CC/C=C\[C@](C)(C(C)OCN1CCN(C)CC1)/N=C(\C(Br)=N)/N Chemical compound CC/C=C\[C@](C)(C(C)OCN1CCN(C)CC1)/N=C(\C(Br)=N)/N NZMLBKQYAICUTC-PREYCYJLSA-N 0.000 description 1
- URTAFSMSZSSRGQ-UHFFFAOYSA-N CCC(C)/N=C(\C=N)/N Chemical compound CCC(C)/N=C(\C=N)/N URTAFSMSZSSRGQ-UHFFFAOYSA-N 0.000 description 1
- GJQCXICOYCNNKH-UHFFFAOYSA-N CN(CC1)CCN1C(c(cc1)ccc1-c1nc(-c2ccc(C(F)(F)F)nc2)c(N)nc1)=O Chemical compound CN(CC1)CCN1C(c(cc1)ccc1-c1nc(-c2ccc(C(F)(F)F)nc2)c(N)nc1)=O GJQCXICOYCNNKH-UHFFFAOYSA-N 0.000 description 1
- KTOXEDIFORKAKJ-UHFFFAOYSA-N Nc(nc1)c(-c2ccc(C(F)(F)F)nc2)nc1-c(cc1)ccc1C(N1CCNCC1)=O Chemical compound Nc(nc1)c(-c2ccc(C(F)(F)F)nc2)nc1-c(cc1)ccc1C(N1CCNCC1)=O KTOXEDIFORKAKJ-UHFFFAOYSA-N 0.000 description 1
- KRRTXVSBTPCDOS-UHFFFAOYSA-N Nc(nc1)cnc1Br Chemical compound Nc(nc1)cnc1Br KRRTXVSBTPCDOS-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/4965—Non-condensed pyrazines
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further 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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- 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
- A61P33/06—Antimalarials
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261600324P | 2012-02-17 | 2012-02-17 | |
| US61/600,324 | 2012-02-17 | ||
| PCT/IB2013/051235 WO2013121387A1 (en) | 2012-02-17 | 2013-02-15 | Anti -malarial agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015507004A JP2015507004A (ja) | 2015-03-05 |
| JP2015507004A5 JP2015507004A5 (enExample) | 2016-02-12 |
| JP6226889B2 true JP6226889B2 (ja) | 2017-11-08 |
Family
ID=48014134
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014557157A Expired - Fee Related JP6226889B2 (ja) | 2012-02-17 | 2013-02-15 | 新規抗マラリア薬 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US9266842B2 (enExample) |
| EP (1) | EP2814820B1 (enExample) |
| JP (1) | JP6226889B2 (enExample) |
| CN (1) | CN104136426B (enExample) |
| BR (1) | BR112014020212B1 (enExample) |
| CA (1) | CA2864483A1 (enExample) |
| CY (1) | CY1118074T1 (enExample) |
| DK (1) | DK2814820T3 (enExample) |
| ES (1) | ES2589283T3 (enExample) |
| HR (1) | HRP20161237T1 (enExample) |
| HU (1) | HUE029876T2 (enExample) |
| IN (1) | IN2014MN01622A (enExample) |
| LT (1) | LT2814820T (enExample) |
| ME (1) | ME02535B (enExample) |
| PL (1) | PL2814820T3 (enExample) |
| PT (1) | PT2814820T (enExample) |
| RS (1) | RS55201B1 (enExample) |
| SI (1) | SI2814820T1 (enExample) |
| SM (1) | SMT201600441B (enExample) |
| WO (1) | WO2013121387A1 (enExample) |
| ZA (1) | ZA201406786B (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT2814820T (lt) * | 2012-02-17 | 2016-10-25 | University Of Cape Town | Antimaliariniai agentai |
| EP3118198A1 (en) | 2015-07-13 | 2017-01-18 | MMV Medicines for Malaria Venture | Anti-malarial agents |
| WO2017067881A1 (en) | 2015-10-19 | 2017-04-27 | Glaxosmithkline Intellectual Property Development Limited | Pyrazine compounds for use in the treatment of parasitic protozoal infections |
| ES2928240T3 (es) * | 2018-01-24 | 2022-11-16 | Glaxosmithkline Ip Dev Ltd | Compuestos novedosos para el tratamiento de infecciones parasitarias |
| CN112142715A (zh) * | 2020-10-10 | 2020-12-29 | 鲁南制药集团股份有限公司 | 一种2-氨基-5-杂环基取代的吡嗪衍生物及其用途 |
| US20250122167A1 (en) * | 2021-11-23 | 2025-04-17 | Glaxosmithkline Intellectual Property Development Limited | Pyrazine Compounds Useful in the Treatment of Parasitic Protozoal Infection |
| JP2025531008A (ja) | 2022-08-09 | 2025-09-19 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | フロピリミジン誘導体 |
| WO2024033280A1 (en) | 2022-08-09 | 2024-02-15 | Merck Patent Gmbh | Furopyridin and furopyrimidin, inhibitors of pi4k, for use in the treatment of parasite infection and malaria |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2545422C (en) * | 2003-12-03 | 2015-06-02 | Cytopia Research Pty Ltd | Tubulin inhibitors |
| US20080039450A1 (en) * | 2006-06-22 | 2008-02-14 | Jensen Annika J | Compounds |
| EP1900727A1 (en) * | 2006-08-30 | 2008-03-19 | Cellzome Ag | Aminopyridine derivatives as kinase inhibitors |
| GB0625659D0 (en) * | 2006-12-21 | 2007-01-31 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| JP5735986B2 (ja) * | 2010-01-18 | 2015-06-17 | エムエムヴィ メディシンズ フォア マラリア ヴェンチャーＭｍｖ Ｍｅｄｉｃｉｎｅｓ Ｆｏｒ Ｍａｌａｒｉａ Ｖｅｎｔｕｒｅ | 新規抗マラリア剤 |
| US9062008B2 (en) * | 2010-05-12 | 2015-06-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| CA2828578A1 (en) * | 2011-03-04 | 2012-09-13 | Lexicon Pharmaceuticals, Inc. | Mst1 kinase inhibitors and methods of their use |
| LT2814820T (lt) * | 2012-02-17 | 2016-10-25 | University Of Cape Town | Antimaliariniai agentai |
-
2013
- 2013-02-15 LT LTEP13712926.8T patent/LT2814820T/lt unknown
- 2013-02-15 EP EP13712926.8A patent/EP2814820B1/en active Active
- 2013-02-15 HU HUE13712926A patent/HUE029876T2/en unknown
- 2013-02-15 PT PT137129268T patent/PT2814820T/pt unknown
- 2013-02-15 SI SI201330290A patent/SI2814820T1/sl unknown
- 2013-02-15 CN CN201380009373.9A patent/CN104136426B/zh not_active Expired - Fee Related
- 2013-02-15 CA CA2864483A patent/CA2864483A1/en not_active Abandoned
- 2013-02-15 DK DK13712926.8T patent/DK2814820T3/en active
- 2013-02-15 PL PL13712926T patent/PL2814820T3/pl unknown
- 2013-02-15 WO PCT/IB2013/051235 patent/WO2013121387A1/en not_active Ceased
- 2013-02-15 ME MEP-2016-214A patent/ME02535B/me unknown
- 2013-02-15 ES ES13712926.8T patent/ES2589283T3/es active Active
- 2013-02-15 IN IN1622MUN2014 patent/IN2014MN01622A/en unknown
- 2013-02-15 BR BR112014020212-5A patent/BR112014020212B1/pt not_active IP Right Cessation
- 2013-02-15 RS RS20160814A patent/RS55201B1/sr unknown
- 2013-02-15 JP JP2014557157A patent/JP6226889B2/ja not_active Expired - Fee Related
- 2013-02-15 HR HRP20161237TT patent/HRP20161237T1/hr unknown
- 2013-02-15 US US14/379,332 patent/US9266842B2/en not_active Expired - Fee Related
-
2014
- 2014-09-16 ZA ZA2014/06786A patent/ZA201406786B/en unknown
-
2016
- 2016-10-10 CY CY20161100998T patent/CY1118074T1/el unknown
- 2016-12-02 SM SM201600441T patent/SMT201600441B/it unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR112014020212A8 (pt) | 2018-01-23 |
| JP2015507004A (ja) | 2015-03-05 |
| EP2814820A1 (en) | 2014-12-24 |
| PT2814820T (pt) | 2016-10-25 |
| US9266842B2 (en) | 2016-02-23 |
| IN2014MN01622A (enExample) | 2015-05-15 |
| CY1118074T1 (el) | 2017-06-28 |
| DK2814820T3 (en) | 2016-10-03 |
| WO2013121387A1 (en) | 2013-08-22 |
| CN104136426B (zh) | 2017-10-03 |
| SMT201600441B (it) | 2017-01-10 |
| SI2814820T1 (sl) | 2016-10-28 |
| CN104136426A (zh) | 2014-11-05 |
| ES2589283T3 (es) | 2016-11-11 |
| ZA201406786B (en) | 2015-06-24 |
| RS55201B1 (sr) | 2017-01-31 |
| US20150031682A1 (en) | 2015-01-29 |
| CA2864483A1 (en) | 2013-08-22 |
| LT2814820T (lt) | 2016-10-25 |
| HRP20161237T1 (hr) | 2016-11-04 |
| BR112014020212B1 (pt) | 2021-11-23 |
| ME02535B (me) | 2017-02-20 |
| PL2814820T3 (pl) | 2017-01-31 |
| HUE029876T2 (en) | 2017-04-28 |
| EP2814820B1 (en) | 2016-07-20 |
| HK1202859A1 (en) | 2015-10-09 |
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