EA201991016A1 - 2,4,5-трехзамещенные 1,2,4-триазолоны, применяемые в качестве ингибиторов дгодг - Google Patents

2,4,5-трехзамещенные 1,2,4-триазолоны, применяемые в качестве ингибиторов дгодг

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Publication number
EA201991016A1
EA201991016A1 EA201991016A EA201991016A EA201991016A1 EA 201991016 A1 EA201991016 A1 EA 201991016A1 EA 201991016 A EA201991016 A EA 201991016A EA 201991016 A EA201991016 A EA 201991016A EA 201991016 A1 EA201991016 A1 EA 201991016A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
dgodg
triazolones
tri
inhibitors
Prior art date
Application number
EA201991016A
Other languages
English (en)
Other versions
EA039707B1 (ru
Inventor
Штефан Николаус Градль
Дуй Нгуен
Кнут Айс
Юдит Гюнтер
Тимо Штелльфельд
Андреас Янцер
Свен Кристиан
Томас Мюллер
Шериф Эль Шэйх
Хан Джи Жу
Чангджийа Жао
Дэвид Брайен Сайкс
Стивен Джеймс Феррара
Кери Лиу
Михаель Крёбер
Клаудиа Мерц
Михаель Нихюс
Мартина Шэфер
Катья Циммерманн
Карл Фридрих Низинг
Original Assignee
Байер Акциенгезельшафт
Байер Фарма Акциенгезельшафт
Зе Броуд Инститьют, Инк.
Президент Энд Феллоус Оф Харвард Колледж
Зе Дженерэл Хоспитэл Корпорейшн
Priority date (The priority date 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 date listed.)
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Publication date
Application filed by Байер Акциенгезельшафт, Байер Фарма Акциенгезельшафт, Зе Броуд Инститьют, Инк., Президент Энд Феллоус Оф Харвард Колледж, Зе Дженерэл Хоспитэл Корпорейшн filed Critical Байер Акциенгезельшафт
Priority claimed from PCT/EP2017/077252 external-priority patent/WO2018077923A1/en
Publication of EA201991016A1 publication Critical patent/EA201991016A1/ru
Publication of EA039707B1 publication Critical patent/EA039707B1/ru

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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Настоящее изобретение касается триазолоновых соединений общей формулы (I)в которой R, R, R, Rи Rимеют значения, как определено в настоящем документе, способов получения указанных соединений, промежуточных соединений, пригодных для получения указанных соединений, фармацевтических композиций и комбинаций, содержащих указанные соединения, и применения указанных соединений для производства фармацевтических композиций для лечения или профилактики заболеваний, в частности гиперпролиферативных заболеваний, в виде отдельного вещества или в комбинации с другими активными ингредиентами.
EA201991016A 2017-10-06 2017-10-25 2,4,5-трехзамещенные 1,2,4-триазолоны, способы их получения, промежуточные соединения, фармацевтическая композиция и применение соединений для лечения гиперпролиферативного заболевания EA039707B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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 (2)

Publication Number Publication Date
EA201991016A1 true EA201991016A1 (ru) 2019-09-30
EA039707B1 EA039707B1 (ru) 2022-03-02

Family

ID=81077496

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201991016A EA039707B1 (ru) 2017-10-06 2017-10-25 2,4,5-трехзамещенные 1,2,4-триазолоны, способы их получения, промежуточные соединения, фармацевтическая композиция и применение соединений для лечения гиперпролиферативного заболевания

Country Status (1)

Country Link
EA (1) EA039707B1 (ru)

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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***酮化合物

Also Published As

Publication number Publication date
EA039707B1 (ru) 2022-03-02

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