PE20191005A1 - 1,2,4-triazolonas 2,4,5-trisustituidas - Google Patents
1,2,4-triazolonas 2,4,5-trisustituidasInfo
- Publication number
- PE20191005A1 PE20191005A1 PE2019000896A PE2019000896A PE20191005A1 PE 20191005 A1 PE20191005 A1 PE 20191005A1 PE 2019000896 A PE2019000896 A PE 2019000896A PE 2019000896 A PE2019000896 A PE 2019000896A PE 20191005 A1 PE20191005 A1 PE 20191005A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- alkyl
- cycloalkyl
- haloalkyl
- halogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- 108010052167 Dihydroorotate Dehydrogenase Proteins 0.000 abstract 2
- 102100032823 Dihydroorotate dehydrogenase (quinone), mitochondrial Human genes 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000006313 (C5-C8) alkyl group Chemical group 0.000 abstract 1
- MDTUWBLTRPRXBX-UHFFFAOYSA-N 1,2,4-triazol-3-one Chemical compound O=C1N=CN=N1 MDTUWBLTRPRXBX-UHFFFAOYSA-N 0.000 abstract 1
- IFYSNBXAAHMRJF-AWEZNQCLSA-N 5-fluoro-4-(3-methyl-5-oxo-4-propan-2-yl-1,2,4-triazol-1-yl)-N-(2-methylphenyl)-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxybenzamide Chemical compound FC=1C(=CC(=C(C(=O)NC2=C(C=CC=C2)C)C=1)O[C@H](C(F)(F)F)C)N1N=C(N(C1=O)C(C)C)C IFYSNBXAAHMRJF-AWEZNQCLSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
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- 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
-
- 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
- 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
- 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
-
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (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)
Abstract
Referido a un compuesto de formula (I), caracterizado porque R1 es alquiloC5-C8, haloalquiloC2-C8, cicloalquilo C4-C8, entre otros; R2 H, o halogeno; R3 es alquilo C1-C6; cicloalquiloC3-C8, haloalquilo C1-C6, entre otros; R4 alquilo C1-C6 opcionalmente sustituido, cicloalquilo C3-C8 o fenilo; R5 es halogeno, alquilo C1-C6, ente otros. Son compuestos 1,2,4-TRIAZOLONAS 2,4,5-trisustituidas que inhiben la dihidroorotato deshidrogenasa (DHODH); un compuesto seleccionado es 5-fluoro-4-[3-metil-5-oxo-4-(propan-2-il)-4,5-dihidro-1H-1,2,4-triazol-1-il]-N-(2-metilfenil)-2-{[(2S)-1,1,1-trifluoropropan-2-il]oxi}benzamida. Tambien se refiere a metodos de preparacion de dichos compuestos, compuestos intermedios utiles para preparar dichos compuestos, composiciones farmaceuticas y combinaciones que comprenden dichos compuestos y el uso de dichos compuestos para preparar composiciones farmaceuticas como un unico agente o en combinacion con otros ingredientes activos, para el tratamiento o la profilaxis de enfermedades, en particular de trastornos hiperproliferativos como el cancer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2016/103643 | 2016-10-27 | ||
| US201762569296P | 2017-10-06 | 2017-10-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20191005A1 true PE20191005A1 (es) | 2019-07-15 |
Family
ID=60164720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019000896A PE20191005A1 (es) | 2016-10-27 | 2017-10-25 | 1,2,4-triazolonas 2,4,5-trisustituidas |
Country Status (26)
| Country | Link |
|---|---|
| US (4) | US10815215B2 (es) |
| EP (1) | EP3532468B1 (es) |
| JP (1) | JP7084389B2 (es) |
| KR (1) | KR20190084954A (es) |
| CN (2) | CN115557907B (es) |
| AU (1) | AU2017351688B2 (es) |
| BR (1) | BR112019008458A2 (es) |
| CA (1) | CA3041643A1 (es) |
| CL (1) | CL2019001160A1 (es) |
| CO (1) | CO2019004137A2 (es) |
| CR (1) | CR20190212A (es) |
| CU (1) | CU24572B1 (es) |
| DO (1) | DOP2019000110A (es) |
| EC (1) | ECSP19030002A (es) |
| GE (1) | GEP20217248B (es) |
| IL (1) | IL266214B (es) |
| JO (1) | JOP20190094A1 (es) |
| MX (1) | MX382665B (es) |
| NI (1) | NI201900041A (es) |
| PE (1) | PE20191005A1 (es) |
| PH (1) | PH12019500932A1 (es) |
| TN (1) | TN2019000136A1 (es) |
| TW (1) | TW201827414A (es) |
| UA (1) | UA123688C2 (es) |
| UY (1) | UY37461A (es) |
| WO (1) | WO2018077923A1 (es) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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) |
| CN110248937B (zh) * | 2016-10-27 | 2022-03-29 | 拜耳股份有限公司 | 4,5-环状1,2,4-三唑酮 |
| HRP20211462T1 (hr) | 2017-04-24 | 2021-12-24 | Aurigene Discovery Technologies Limited | Postupci uporabe za trisupstituirane derivate benzotriazola kao inhibitora dihidroorotatne oksigenaze |
| ES3038736T3 (en) | 2018-02-20 | 2025-10-14 | Servier Lab | Benzotriazole derivative for use in treating double and triple hit diffuse large b cell lymphoma |
| 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 |
| EP3858361B1 (en) | 2018-09-28 | 2025-10-08 | FUJIFILM Corporation | Antitumor agent containing cytarabine, antitumor effect enhancer used in combination with cytarabine, antitumor kit, and antitumor agent used in combination with cytarabine |
| MX2021007536A (es) | 2018-12-21 | 2021-09-23 | Les Laboratoires Servier Sas | Formas de sal y cristalinas de un compuesto organico y composiciones farmaceuticas del mismo. |
| 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 |
| CN113453680A (zh) * | 2019-02-07 | 2021-09-28 | 詹森生物科技公司 | 二氢乳清酸脱氢酶抑制剂 |
| 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 |
| 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 |
| KR20220083735A (ko) * | 2019-10-10 | 2022-06-20 | 얀센 바이오테크 인코포레이티드 | 바이-아릴 다이하이드로오로테이트 탈수소효소 억제제 |
| 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 |
| WO2021156787A1 (en) * | 2020-02-04 | 2021-08-12 | Janssen Biotech, Inc. | Heterocyclic compounds as dihydroorotate dehydrogenase inhibitors |
| ES2929379T3 (es) | 2020-05-20 | 2022-11-28 | Inst Nat Sante Rech Med | Métodos para el tratamiento de infecciones por coronavirus |
| WO2021240423A1 (en) * | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| WO2021240429A1 (en) | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Benzofuran and benzopyran dihydroorotate dehydrogenase inhibitors |
| WO2021240424A1 (en) | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Indazole and benzoisoxazole dihydroorotate dehydrogenase inhibitors |
| CN115667245B (zh) * | 2020-05-29 | 2024-05-17 | 南京明德新药研发有限公司 | 三氮唑酮类化合物 |
| US20230271943A1 (en) * | 2020-07-14 | 2023-08-31 | Nanjing Zenshine 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 |
| 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 |
| WO2022070071A1 (en) * | 2020-09-30 | 2022-04-07 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| WO2022070069A1 (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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| 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) |
| CN110248937B (zh) | 2016-10-27 | 2022-03-29 | 拜耳股份有限公司 | 4,5-环状1,2,4-三唑酮 |
| 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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