CN110248937B - 4,5-环状1,2,4-三唑酮 - Google Patents
4,5-环状1,2,4-三唑酮 Download PDFInfo
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- CN110248937B CN110248937B CN201780067556.4A CN201780067556A CN110248937B CN 110248937 B CN110248937 B CN 110248937B CN 201780067556 A CN201780067556 A CN 201780067556A CN 110248937 B CN110248937 B CN 110248937B
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- fluoro
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- benzamide
- triazolo
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/63—Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
- C12N15/70—Vectors or expression systems specially adapted for E. coli
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
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- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- C12N1/00—Microorganisms, e.g. protozoa; Compositions thereof; Processes of propagating, maintaining or preserving microorganisms or compositions thereof; Processes of preparing or isolating a composition containing a microorganism; Culture media therefor
- C12N1/20—Bacteria; Culture media therefor
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- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/0004—Oxidoreductases (1.)
- C12N9/0012—Oxidoreductases (1.) acting on nitrogen containing compounds as donors (1.4, 1.5, 1.6, 1.7)
- C12N9/0036—Oxidoreductases (1.) acting on nitrogen containing compounds as donors (1.4, 1.5, 1.6, 1.7) acting on NADH or NADPH (1.6)
- C12N9/0038—Oxidoreductases (1.) acting on nitrogen containing compounds as donors (1.4, 1.5, 1.6, 1.7) acting on NADH or NADPH (1.6) with a heme protein as acceptor (1.6.2)
- C12N9/0042—NADPH-cytochrome P450 reductase (1.6.2.4)
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- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/0004—Oxidoreductases (1.)
- C12N9/0071—Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14)
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- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/10—Nitrogen as only ring hetero atom
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- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
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- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
- C12P17/182—Heterocyclic compounds containing nitrogen atoms as the only ring heteroatoms in the condensed system
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- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
- C12P17/188—Heterocyclic compound containing in the condensed system at least one hetero ring having nitrogen atoms and oxygen atoms as the only ring heteroatoms
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- C12Y—ENZYMES
- C12Y106/00—Oxidoreductases acting on NADH or NADPH (1.6)
- C12Y106/02—Oxidoreductases acting on NADH or NADPH (1.6) with a heme protein as acceptor (1.6.2)
- C12Y106/02004—NADPH-hemoprotein reductase (1.6.2.4), i.e. NADP-cytochrome P450-reductase
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- C12Y—ENZYMES
- C12Y114/00—Oxidoreductases acting on paired donors, with incorporation or reduction of molecular oxygen (1.14)
- C12Y114/14—Oxidoreductases acting on paired donors, with incorporation or reduction of molecular oxygen (1.14) with reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen (1.14.14)
- C12Y114/14001—Unspecific monooxygenase (1.14.14.1)
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- 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
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- Bioinformatics & Cheminformatics (AREA)
- General Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Physics & Mathematics (AREA)
- Plant Pathology (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Biophysics (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210298141.0A CN114921391B (zh) | 2016-10-27 | 2017-10-25 | 4,5-环状1,2,4-三唑酮 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2016/103642 | 2016-10-27 | ||
| CNPCT/CN2016/103642 | 2016-10-27 | ||
| PCT/EP2017/077301 WO2018077944A2 (en) | 2016-10-27 | 2017-10-25 | 4,5-annulated 1,2,4-triazolones |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202210298141.0A Division CN114921391B (zh) | 2016-10-27 | 2017-10-25 | 4,5-环状1,2,4-三唑酮 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN110248937A CN110248937A (zh) | 2019-09-17 |
| CN110248937B true CN110248937B (zh) | 2022-03-29 |
Family
ID=60293935
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780067556.4A Active CN110248937B (zh) | 2016-10-27 | 2017-10-25 | 4,5-环状1,2,4-三唑酮 |
| CN202210298141.0A Active CN114921391B (zh) | 2016-10-27 | 2017-10-25 | 4,5-环状1,2,4-三唑酮 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202210298141.0A Active CN114921391B (zh) | 2016-10-27 | 2017-10-25 | 4,5-环状1,2,4-三唑酮 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US10968216B2 (enExample) |
| EP (1) | EP3532474B1 (enExample) |
| JP (3) | JP7680184B2 (enExample) |
| CN (2) | CN110248937B (enExample) |
| CA (1) | CA3041650A1 (enExample) |
| TW (1) | TW201827430A (enExample) |
| UY (1) | UY37460A (enExample) |
| WO (1) | WO2018077944A2 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10968216B2 (en) | 2016-10-27 | 2021-04-06 | Bayer Aktiengesellschaft | 4,5-annulated 1,2,4-triazolones |
| JOP20190094A1 (ar) | 2016-10-27 | 2019-04-25 | Broad Inst Inc | مركبات 1، 2، 4-تريازولون تحمل ثلاثة بدائل عند المواقع 2، 4، 5 مفيدة كمثبطات لديهيدروجيناز ثنائي هيدرو أوروتات (dhodh) |
| TW201945346A (zh) | 2018-04-10 | 2019-12-01 | 德商拜耳廠股份有限公司 | 2,4,5-三取代的1,2,4-三唑酮之製備方法 |
| EP3553052A1 (en) * | 2018-04-10 | 2019-10-16 | Bayer AG | 5-oxo-4,5-dihydro-1h-1,2,4-triazol derivatives for the treatment of cancer |
| WO2019197269A1 (en) * | 2018-04-11 | 2019-10-17 | Bayer Aktiengesellschaft | Combinations of copanlisib with triazolone derivatives and their use in the treatment of cancer |
| TW202043208A (zh) * | 2019-01-11 | 2020-12-01 | 美商健生生物科技公司 | 二氫乳清酸脫氫酶抑制劑 |
| TW202104207A (zh) | 2019-04-17 | 2021-02-01 | 美商健生生物科技公司 | 二氫乳清酸脫氫酶抑制劑 |
| JP2022546208A (ja) * | 2019-08-29 | 2022-11-04 | ヤンセン バイオテツク,インコーポレーテツド | 置換尿素ジヒドロオロト酸デヒドロゲナーゼ阻害剤 |
| BR112022006846A2 (pt) * | 2019-10-10 | 2022-07-05 | Janssen Biotech Inc | Inibidores da biaril di-hidro-orotato desidrogenase |
| WO2021238881A1 (zh) * | 2020-05-29 | 2021-12-02 | 南京明德新药研发有限公司 | 三氮唑酮类化合物 |
| WO2022012548A1 (en) * | 2020-07-14 | 2022-01-20 | Nanjing Zhengxiang Pharmaceuticals Co., Ltd. | Compounds as dhodh inhibitors |
| CN111773214B (zh) * | 2020-07-17 | 2021-04-20 | 中国人民解放军军事科学院军事医学研究院 | 2,4,5-三取代的1,2,4-三唑酮在制备抗病毒药物中的用途 |
| WO2022070069A1 (en) * | 2020-09-30 | 2022-04-07 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| AU2022256514A1 (en) * | 2021-04-16 | 2023-10-19 | Hotspot Therapeutics, Inc. | Compounds, compositions and methods of treating cancer |
| CN117616026A (zh) * | 2021-07-05 | 2024-02-27 | 微境生物医药科技(上海)有限公司 | 用作dhodh抑制剂的1,2,4-三唑酮衍生物及其制备方法和用途 |
| CN118284603A (zh) * | 2021-11-26 | 2024-07-02 | 南京明德新药研发有限公司 | 三氮唑酮类化合物的晶型及其应用 |
| WO2024015863A1 (en) * | 2022-07-12 | 2024-01-18 | Hotspot Therapeutics, Inc. | Cbl-b inhibitor, compositions comprising a cbl-b inhibitor in a method of treating a disease associated with cell proliferation |
| WO2024015864A1 (en) * | 2022-07-12 | 2024-01-18 | Hotspot Therapeutics, Inc. | Cbl-b inhibitors and anti-pd1/anti-pd-l1 for use in the treatment of cancer |
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| WO2013087579A1 (en) * | 2011-12-12 | 2013-06-20 | Bayer Intellectual Property Gmbh | Substituted triazolopyridines and their use as ttk inhibitors |
| WO2013186692A1 (en) * | 2012-06-15 | 2013-12-19 | Glenmark Pharmaceuticals S.A. | TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS |
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| DE19627901A1 (de) | 1996-07-11 | 1998-01-15 | Bayer Ag | Substituierte aromatische Carbonylverbindungen und ihre Derivate |
| DE19901846A1 (de) | 1999-01-19 | 2000-07-20 | Bayer Ag | Substituierte Arylheterocyclen |
| US6444613B1 (en) | 1999-03-12 | 2002-09-03 | Hoechst Schering Agrevo Gmbh | Defoliant |
| CA2427615A1 (en) * | 2000-10-30 | 2002-06-13 | Pharmacia Corporation | Aspergillus ochraceus 11 alpha hydroxylase and oxidoreductase |
| WO2003006424A1 (en) | 2001-07-10 | 2003-01-23 | 4Sc Ag | Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents |
| BRPI0922180A2 (pt) | 2008-12-08 | 2015-12-29 | Sirtris Pharmaceuticals Inc | insoindolinona e análogos correlatos como moduladores de sirtuína |
| NZ595819A (en) | 2009-04-02 | 2013-02-22 | Merck Serono Sa | DIHYDROOROTATE DEHYDROGENASE INHIBITORS; benzimidazole-4-carboxylic acid |
| US8686048B2 (en) | 2010-05-06 | 2014-04-01 | Rhizen Pharmaceuticals Sa | Immunomodulator and anti-inflammatory compounds |
| WO2012080504A1 (de) * | 2010-12-16 | 2012-06-21 | Pharmazell Gmbh | NEUARTIGE 7ß-HYDROXYSTEROID DEHYDROGENASE-MUTANTEN UND VERFAHREN ZUR HERSTELLUNG VON URSODESOXYCHOLSÄURE |
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| CN104561093A (zh) * | 2014-12-25 | 2015-04-29 | 华东师范大学 | 一种重组人源CYP3A4/CPR/cyt b5蛋白共转染共表达的方法 |
| US20160251341A1 (en) | 2015-02-27 | 2016-09-01 | Verseon Corporation | Substituted triazole compounds as serine protease inhibitors |
| CN106543139B (zh) | 2015-09-17 | 2020-03-17 | 沈阳中化农药化工研发有限公司 | 一种三唑酮类化合物及其用途 |
| JOP20190094A1 (ar) * | 2016-10-27 | 2019-04-25 | Broad Inst Inc | مركبات 1، 2، 4-تريازولون تحمل ثلاثة بدائل عند المواقع 2، 4، 5 مفيدة كمثبطات لديهيدروجيناز ثنائي هيدرو أوروتات (dhodh) |
| US10968216B2 (en) | 2016-10-27 | 2021-04-06 | Bayer Aktiengesellschaft | 4,5-annulated 1,2,4-triazolones |
| EP3553052A1 (en) * | 2018-04-10 | 2019-10-16 | Bayer AG | 5-oxo-4,5-dihydro-1h-1,2,4-triazol derivatives for the treatment of cancer |
| US20190307728A1 (en) * | 2018-04-10 | 2019-10-10 | Bayer Pharma Aktiengesellschaft | Methods of treatment with a 2,4,5-trisubstituted 1,2,4-triazolone |
| TW201945346A (zh) * | 2018-04-10 | 2019-12-01 | 德商拜耳廠股份有限公司 | 2,4,5-三取代的1,2,4-三唑酮之製備方法 |
| WO2019197269A1 (en) * | 2018-04-11 | 2019-10-17 | Bayer Aktiengesellschaft | Combinations of copanlisib with triazolone derivatives and their use in the treatment of cancer |
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2017
- 2017-10-25 US US16/345,178 patent/US10968216B2/en active Active
- 2017-10-25 CN CN201780067556.4A patent/CN110248937B/zh active Active
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013087579A1 (en) * | 2011-12-12 | 2013-06-20 | Bayer Intellectual Property Gmbh | Substituted triazolopyridines and their use as ttk inhibitors |
| WO2013186692A1 (en) * | 2012-06-15 | 2013-12-19 | Glenmark Pharmaceuticals S.A. | TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS |
Non-Patent Citations (1)
| Title |
|---|
| Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitors with Potent and Selective Activity against the Malaria Parasite Plasmodium falciparum;Margaret A. Phillips等;《J. Med. Chem.》;20080604;第51卷(第12期);第3649-3653页 * |
Also Published As
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| JP7747799B2 (ja) | 2025-10-01 |
| US20190375747A1 (en) | 2019-12-12 |
| EP3532474A2 (en) | 2019-09-04 |
| WO2018077944A3 (en) | 2018-06-14 |
| CA3041650A1 (en) | 2018-05-03 |
| JP2024063131A (ja) | 2024-05-10 |
| CN110248937A (zh) | 2019-09-17 |
| JP2019535689A (ja) | 2019-12-12 |
| WO2018077944A2 (en) | 2018-05-03 |
| US20210188846A1 (en) | 2021-06-24 |
| JP2022130571A (ja) | 2022-09-06 |
| UY37460A (es) | 2018-05-31 |
| JP7680184B2 (ja) | 2025-05-20 |
| CN114921391A (zh) | 2022-08-19 |
| US10968216B2 (en) | 2021-04-06 |
| EP3532474B1 (en) | 2024-03-27 |
| TW201827430A (zh) | 2018-08-01 |
| CN114921391B (zh) | 2024-01-02 |
| US11787797B2 (en) | 2023-10-17 |
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