AU2017351688B2 - 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH - Google Patents
2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH Download PDFInfo
- Publication number
- AU2017351688B2 AU2017351688B2 AU2017351688A AU2017351688A AU2017351688B2 AU 2017351688 B2 AU2017351688 B2 AU 2017351688B2 AU 2017351688 A AU2017351688 A AU 2017351688A AU 2017351688 A AU2017351688 A AU 2017351688A AU 2017351688 B2 AU2017351688 B2 AU 2017351688B2
- Authority
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- Australia
- Prior art keywords
- group
- alkyl
- fluoro
- oxo
- dihydro
- Prior art date
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- Expired - Fee Related
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Classifications
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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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
- C07D249/12—Oxygen or sulfur 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2016/103643 | 2016-10-27 | ||
| CNPCT/CN2016/103643 | 2016-10-27 | ||
| US201762569296P | 2017-10-06 | 2017-10-06 | |
| US62569296 | 2017-10-06 | ||
| PCT/EP2017/077252 WO2018077923A1 (en) | 2016-10-27 | 2017-10-25 | 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2017351688A1 AU2017351688A1 (en) | 2019-04-11 |
| AU2017351688B2 true AU2017351688B2 (en) | 2022-02-03 |
Family
ID=60164720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017351688A Expired - Fee Related AU2017351688B2 (en) | 2016-10-27 | 2017-10-25 | 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH |
Country Status (26)
| Country | Link |
|---|---|
| US (4) | US10815215B2 (enExample) |
| EP (1) | EP3532468B1 (enExample) |
| JP (1) | JP7084389B2 (enExample) |
| KR (1) | KR20190084954A (enExample) |
| CN (2) | CN110023302B (enExample) |
| AU (1) | AU2017351688B2 (enExample) |
| BR (1) | BR112019008458A2 (enExample) |
| CA (1) | CA3041643A1 (enExample) |
| CL (1) | CL2019001160A1 (enExample) |
| CO (1) | CO2019004137A2 (enExample) |
| CR (1) | CR20190212A (enExample) |
| CU (1) | CU24572B1 (enExample) |
| DO (1) | DOP2019000110A (enExample) |
| EC (1) | ECSP19030002A (enExample) |
| GE (1) | GEP20217248B (enExample) |
| IL (1) | IL266214B (enExample) |
| JO (1) | JOP20190094A1 (enExample) |
| MX (1) | MX382665B (enExample) |
| NI (1) | NI201900041A (enExample) |
| PE (1) | PE20191005A1 (enExample) |
| PH (1) | PH12019500932A1 (enExample) |
| TN (1) | TN2019000136A1 (enExample) |
| TW (1) | TW201827414A (enExample) |
| UA (1) | UA123688C2 (enExample) |
| UY (1) | UY37461A (enExample) |
| WO (1) | WO2018077923A1 (enExample) |
Families Citing this family (34)
| 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) |
| SMT202100553T1 (it) | 2017-04-24 | 2021-11-12 | Aurigene Discovery Tech Ltd | Metodi d'uso per derivati benzotriazolici trisostituiti come inibitori di diidroorotato ossigenasi |
| US11717512B2 (en) | 2018-02-20 | 2023-08-08 | Servier Pharmaceuticals Llc | Methods of use for trisubstituted benzotriazole derivatives |
| 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 |
| JP7126556B2 (ja) | 2018-09-28 | 2022-08-26 | 富士フイルム株式会社 | シタラビンを含む抗腫瘍剤、シタラビンと併用される抗腫瘍効果増強剤、抗腫瘍用キット、およびシタラビンと併用される抗腫瘍剤 |
| EP3898597A1 (en) | 2018-12-21 | 2021-10-27 | Les Laboratoires Servier SAS | Crystalline and salt forms of an organic compound and pharmaceutical compositions thereof |
| 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 |
| JP2022519383A (ja) * | 2019-02-07 | 2022-03-23 | ヤンセン バイオテツク，インコーポレーテツド | ジヒドロオロト酸デヒドロゲナーゼ阻害剤 |
| 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 |
| EP3750892A1 (en) | 2019-06-14 | 2020-12-16 | Yerevan State University | Novel 5-cyclopropyl-furo[3,4-c]pyridine-3,4(1h,5h)-dione 1,1' substituted derivatives and their uses |
| CA3152836A1 (en) * | 2019-08-29 | 2021-03-04 | Janssen Biotech, Inc. | Substituted urea dihydroorotate dehydrogenase inhibitors |
| JP2022552496A (ja) * | 2019-10-10 | 2022-12-16 | ヤンセン バイオテツク，インコーポレーテツド | ビアリールジヒドロオロト酸デヒドロゲナーゼ阻害剤 |
| CN114222732B (zh) * | 2019-10-28 | 2023-04-04 | 南京明德新药研发有限公司 | 一种尿酸促排剂及其合成方法和其在医药上的应用 |
| JP2023513496A (ja) * | 2020-02-04 | 2023-03-31 | ヤンセン バイオテツク，インコーポレーテツド | ジヒドロオロト酸デヒドロゲナーゼ阻害剤としての複素環式化合物 |
| EP3912627B1 (en) | 2020-05-20 | 2022-09-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of coronavirus infections |
| WO2021240429A1 (en) | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Benzofuran and benzopyran dihydroorotate dehydrogenase inhibitors |
| JP7653456B2 (ja) * | 2020-05-29 | 2025-03-28 | メッドシャイン ディスカバリー インコーポレイテッド | トリアゾロン系化合物 |
| WO2021240424A1 (en) | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Indazole and benzoisoxazole dihydroorotate dehydrogenase inhibitors |
| WO2021240423A1 (en) * | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| JP2023535346A (ja) * | 2020-07-14 | 2023-08-17 | ナンジン ゼンシャイン ファーマシューティカルズ カンパニー リミテッド | Ｄｈｏｄｈ阻害剤としての化合物 |
| 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 |
| EP3960170A1 (en) | 2020-08-25 | 2022-03-02 | Bayer AG | Dosing schedule for a method of treatment with dhodh inhibitors |
| GB2598624A (en) * | 2020-09-07 | 2022-03-09 | Lorico Aurelio | Use of triazole analogues for inhibition of a tripartite VOR protein complex in multicellular organisms |
| WO2022063299A1 (zh) * | 2020-09-28 | 2022-03-31 | 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 |
| WO2022070069A1 (en) * | 2020-09-30 | 2022-04-07 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| WO2022070071A1 (en) * | 2020-09-30 | 2022-04-07 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| WO2022167402A1 (en) | 2021-02-02 | 2022-08-11 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of therapy comprising administering a therapeutically effective combination comprising a dhodh inhibitor and an idh inhibitor |
| WO2023280181A1 (zh) * | 2021-07-05 | 2023-01-12 | 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 |
| WO2023093812A1 (zh) * | 2021-11-26 | 2023-06-01 | 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 |
| KR102686544B1 (ko) * | 2023-12-04 | 2024-07-19 | 대한민국 | Bay-2402234을 유효성분으로 포함하는 중증열성혈소판감소증후군 예방 또는 치료용 약학 조성물 |
| WO2025202415A1 (en) | 2024-03-28 | 2025-10-02 | Institut National de la Santé et de la Recherche Médicale | Dhodh inhibitors for use in the chronopharmacoligical treatment and prevention of obesity and obesity-related metabolic disorders |
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| CN103006645A (zh) * | 2011-09-27 | 2013-04-03 | 华东理工大学 | 2-氨基苯并噻唑衍生物作为dhodh抑制剂的应用 |
| WO2013186692A1 (en) * | 2012-06-15 | 2013-12-19 | Glenmark Pharmaceuticals S.A. | TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS |
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| US4237140A (en) * | 1979-05-18 | 1980-12-02 | E. I. Du Pont De Nemours And Company | Analgesic mixture of nalbuphine and acetaminophen |
| DE3936622A1 (de) | 1989-11-03 | 1991-05-08 | Bayer Ag | Halogenierte sulfonylaminocarbonyltriazolinone |
| DE3936623A1 (de) | 1989-11-03 | 1991-05-08 | Bayer Ag | Sulfonylaminocarbonyltriazolinone mit ueber schwefel gebundenen substituenten |
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| DE4433968A1 (de) | 1994-09-23 | 1996-03-28 | Bayer Ag | Verfahren zur Herstellung von Alkoxytriazolinonen |
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| 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 |
| 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 |
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2017
- 2017-06-16 JO JOP/2019/0094A patent/JOP20190094A1/ar unknown
- 2017-10-25 KR KR1020197011905A patent/KR20190084954A/ko not_active Ceased
- 2017-10-25 CR CR20190212A patent/CR20190212A/es unknown
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- 2017-10-25 US US16/345,168 patent/US10815215B2/en active Active
- 2017-10-25 BR BR112019008458A patent/BR112019008458A2/pt not_active IP Right Cessation
- 2017-10-25 TN TNP/2019/000136A patent/TN2019000136A1/en unknown
- 2017-10-25 MX MX2019005009A patent/MX382665B/es unknown
- 2017-10-25 CN CN201780066589.7A patent/CN110023302B/zh active Active
- 2017-10-25 GE GEAP201715096A patent/GEP20217248B/en unknown
- 2017-10-25 JP JP2019522859A patent/JP7084389B2/ja active Active
- 2017-10-25 EP EP17788234.7A patent/EP3532468B1/en active Active
- 2017-10-25 CA CA3041643A patent/CA3041643A1/en active Pending
- 2017-10-25 CN CN202210811374.6A patent/CN115557907B/zh active Active
- 2017-10-25 CU CU2019000045A patent/CU24572B1/es unknown
- 2017-10-25 AU AU2017351688A patent/AU2017351688B2/en not_active Expired - Fee Related
- 2017-10-25 WO PCT/EP2017/077252 patent/WO2018077923A1/en not_active Ceased
- 2017-10-25 UA UAA201905676A patent/UA123688C2/uk unknown
- 2017-10-27 UY UY0001037461A patent/UY37461A/es not_active Application Discontinuation
- 2017-10-27 TW TW106137255A patent/TW201827414A/zh unknown
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2019
- 2019-04-23 IL IL266214A patent/IL266214B/en unknown
- 2019-04-25 PH PH12019500932A patent/PH12019500932A1/en unknown
- 2019-04-26 CL CL2019001160A patent/CL2019001160A1/es unknown
- 2019-04-26 CO CONC2019/0004137A patent/CO2019004137A2/es unknown
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- 2019-04-26 DO DO2019000110A patent/DOP2019000110A/es unknown
- 2019-04-26 EC ECSENADI201930002A patent/ECSP19030002A/es unknown
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2020
- 2020-08-18 US US16/996,721 patent/US11130745B2/en active Active
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2021
- 2021-08-20 US US17/407,951 patent/US11713304B2/en active Active
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2023
- 2023-04-20 US US18/137,281 patent/US12486248B2/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103006645A (zh) * | 2011-09-27 | 2013-04-03 | 华东理工大学 | 2-氨基苯并噻唑衍生物作为dhodh抑制剂的应用 |
| WO2013186692A1 (en) * | 2012-06-15 | 2013-12-19 | Glenmark Pharmaceuticals S.A. | TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS |
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| HÉLÈNE MUNIER-LEHMANN ET AL, "On Dihydroorotate Dehydrogenases and Their Inhibitors and Uses", JOURNAL OF MEDICINAL CHEMISTRY, 2013, vol. 56, no. 8, pages 3148 - 3167 * |
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