BR112019008458A2 - 1,2,4-triazolonas 2,4,5-trisubstituídas. - Google Patents
1,2,4-triazolonas 2,4,5-trisubstituídas.Info
- Publication number
- BR112019008458A2 BR112019008458A2 BR112019008458A BR112019008458A BR112019008458A2 BR 112019008458 A2 BR112019008458 A2 BR 112019008458A2 BR 112019008458 A BR112019008458 A BR 112019008458A BR 112019008458 A BR112019008458 A BR 112019008458A BR 112019008458 A2 BR112019008458 A2 BR 112019008458A2
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- triazolones
- trisubstituted
- pharmaceutical compositions
- prophylaxis
- Prior art date
Links
- MDTUWBLTRPRXBX-UHFFFAOYSA-N 1,2,4-triazol-3-one Chemical class O=C1N=CN=N1 MDTUWBLTRPRXBX-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- FFSJPOPLSWBGQY-UHFFFAOYSA-N triazol-4-one Chemical class O=C1C=NN=N1 FFSJPOPLSWBGQY-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
Abstract
1,2,4-triazolonas 2,4,5-trisubstituídas. a presente invenção provê compostos de triazolona da fórmula geral (i): (i), em que r1, r2, r3, r4 e r5 são conforme aqui definidos, métodos de preparação dos ditos compostos, compostos intermediários úteis na preparação dos ditos compostos, composições e combinações farmacêuticas compreendendo os ditos compostos e o uso dos ditos compostos na produção de composições farmacêuticas para o tratamento ou profilaxia de doenças, em particular de distúrbios hiperproliferativos, como um agente único ou em combinação com outros princípios ativos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2016/103643 | 2016-10-27 | ||
| US201762569296P | 2017-10-06 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| BR112019008458A2 true BR112019008458A2 (pt) | 2019-07-09 |
Family
ID=60164720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112019008458A BR112019008458A2 (pt) | 2016-10-27 | 2017-10-25 | 1,2,4-triazolonas 2,4,5-trisubstituídas. |
Country Status (26)
| Country | Link |
|---|---|
| US (4) | US10815215B2 (pt) |
| EP (1) | EP3532468B1 (pt) |
| JP (1) | JP7084389B2 (pt) |
| KR (1) | KR20190084954A (pt) |
| CN (2) | CN115557907A (pt) |
| AU (1) | AU2017351688B2 (pt) |
| BR (1) | BR112019008458A2 (pt) |
| CA (1) | CA3041643A1 (pt) |
| CL (1) | CL2019001160A1 (pt) |
| CO (1) | CO2019004137A2 (pt) |
| CR (1) | CR20190212A (pt) |
| CU (1) | CU24572B1 (pt) |
| DO (1) | DOP2019000110A (pt) |
| EC (1) | ECSP19030002A (pt) |
| GE (1) | GEP20217248B (pt) |
| IL (1) | IL266214B (pt) |
| JO (1) | JOP20190094A1 (pt) |
| MX (1) | MX2019005009A (pt) |
| NI (1) | NI201900041A (pt) |
| PE (1) | PE20191005A1 (pt) |
| PH (1) | PH12019500932A1 (pt) |
| TN (1) | TN2019000136A1 (pt) |
| TW (1) | TW201827414A (pt) |
| UA (1) | UA123688C2 (pt) |
| UY (1) | UY37461A (pt) |
| WO (1) | WO2018077923A1 (pt) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3041650A1 (en) | 2016-10-27 | 2018-05-03 | 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 |
| WO2020067412A1 (ja) | 2018-09-28 | 2020-04-02 | 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 |
| 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 |
| MX2021009521A (es) * | 2019-02-07 | 2021-09-08 | Janssen Biotech Inc | Inhibidores de dihidroorotato deshidrogenasa. |
| 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 |
| CN114286813A (zh) * | 2019-08-29 | 2022-04-05 | 詹森生物科技公司 | 取代的脲二氢乳清酸脱氢酶抑制剂 |
| BR112022006846A2 (pt) * | 2019-10-10 | 2022-07-05 | Janssen Biotech Inc | Inibidores da biaril di-hidro-orotato desidrogenase |
| 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 |
| EP4100124A1 (en) * | 2020-02-04 | 2022-12-14 | 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 |
| EP4166551A1 (en) * | 2020-05-29 | 2023-04-19 | Medshine Discovery Inc. | Triazolone compound |
| 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 |
| KR20230039678A (ko) * | 2020-07-14 | 2023-03-21 | 난징 젠샤인 파마슈티컬스 컴퍼니, 리미티드 | Dhodh 억제제로서의 화합물 |
| 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 |
| 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 |
| 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 |
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| US4098896A (en) | 1975-09-29 | 1978-07-04 | Chevron Research Company | 1-Halohydrocarbylthio-3-hydrocarbylthio-4-substituted-1,2,4-delta2 -triazolidin-5-ones |
| DE3936622A1 (de) | 1989-11-03 | 1991-05-08 | Bayer Ag | Halogenierte sulfonylaminocarbonyltriazolinone |
| DE3709574A1 (de) | 1987-03-24 | 1988-10-06 | Bayer Ag | Substituierte triazolinone |
| DE3934081A1 (de) | 1989-10-12 | 1991-04-18 | Bayer Ag | Sulfonylaminocarbonyltriazolinone |
| DE3936623A1 (de) | 1989-11-03 | 1991-05-08 | Bayer Ag | Sulfonylaminocarbonyltriazolinone mit ueber schwefel gebundenen substituenten |
| DE4110795A1 (de) | 1991-04-04 | 1992-10-08 | Bayer Ag | Sulfonylaminocarbonyltriazolinone mit ueber sauerstoff gebundenen substituenten |
| DE3916208A1 (de) | 1989-05-18 | 1990-11-22 | Bayer Ag | Substituierte triazolone |
| DE4342190A1 (de) | 1993-12-10 | 1995-06-14 | Bayer Ag | Verfahren und neue Zwischenprodukte zur Herstellung von Triazolinonen |
| DE4433968A1 (de) | 1994-09-23 | 1996-03-28 | Bayer Ag | Verfahren zur Herstellung von Alkoxytriazolinonen |
| DE19627901A1 (de) | 1996-07-11 | 1998-01-15 | Bayer Ag | Substituierte aromatische Carbonylverbindungen und ihre Derivate |
| AR022889A1 (es) | 1999-03-12 | 2002-09-04 | Bayer Cropscience Ag | Agente desfoliante |
| AU2009333543A1 (en) | 2008-12-08 | 2011-07-07 | Sirtris Pharmaceuticals, Inc. | Isoindolinone and related analogs as sirtuin modulators |
| WO2010071813A1 (en) | 2008-12-19 | 2010-06-24 | Aryx Therapeutics, Inc. | AGONISTS OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR-α |
| KR101796483B1 (ko) | 2010-09-01 | 2017-11-10 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | Ｎ-(테트라졸-5-일)- 및 ｎ-(트리아졸-5-일)아릴카복사미드 및 제초제로서의 그의 용도 |
| EP2675440B1 (en) | 2011-02-14 | 2020-03-25 | Merck Sharp & Dohme Corp. | Cathepsin cysteine protease inhibitors |
| 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 |
| TWI568722B (zh) * | 2012-06-15 | 2017-02-01 | 葛蘭馬克製藥公司 | 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物 |
| 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) |
-
2017
- 2017-06-16 JO JOP/2019/0094A patent/JOP20190094A1/ar unknown
- 2017-10-25 CA CA3041643A patent/CA3041643A1/en active Pending
- 2017-10-25 CU CU2019000045A patent/CU24572B1/es unknown
- 2017-10-25 WO PCT/EP2017/077252 patent/WO2018077923A1/en unknown
- 2017-10-25 GE GEAP201715096A patent/GEP20217248B/en unknown
- 2017-10-25 JP JP2019522859A patent/JP7084389B2/ja active Active
- 2017-10-25 AU AU2017351688A patent/AU2017351688B2/en not_active Expired - Fee Related
- 2017-10-25 CN CN202210811374.6A patent/CN115557907A/zh active Pending
- 2017-10-25 PE PE2019000896A patent/PE20191005A1/es unknown
- 2017-10-25 UA UAA201905676A patent/UA123688C2/uk unknown
- 2017-10-25 CN CN201780066589.7A patent/CN110023302B/zh active Active
- 2017-10-25 TN TNP/2019/000136A patent/TN2019000136A1/en unknown
- 2017-10-25 BR BR112019008458A patent/BR112019008458A2/pt not_active IP Right Cessation
- 2017-10-25 EP EP17788234.7A patent/EP3532468B1/en active Active
- 2017-10-25 US US16/345,168 patent/US10815215B2/en active Active
- 2017-10-25 CR CR20190212A patent/CR20190212A/es unknown
- 2017-10-25 KR KR1020197011905A patent/KR20190084954A/ko not_active Application Discontinuation
- 2017-10-25 MX MX2019005009A patent/MX2019005009A/es 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 CO CONC2019/0004137A patent/CO2019004137A2/es unknown
- 2019-04-26 DO DO2019000110A patent/DOP2019000110A/es unknown
- 2019-04-26 CL CL2019001160A patent/CL2019001160A1/es unknown
- 2019-04-26 EC ECSENADI201930002A patent/ECSP19030002A/es unknown
- 2019-04-26 NI NI201900041A patent/NI201900041A/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/US20230365524A1/en active Pending
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