EA201892666A1 - 3-оксо-2,6-дифенил-2,3-дигидропиридазин-4-карбоксамиды - Google Patents

3-оксо-2,6-дифенил-2,3-дигидропиридазин-4-карбоксамиды

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Publication number
EA201892666A1
EA201892666A1 EA201892666A EA201892666A EA201892666A1 EA 201892666 A1 EA201892666 A1 EA 201892666A1 EA 201892666 A EA201892666 A EA 201892666A EA 201892666 A EA201892666 A EA 201892666A EA 201892666 A1 EA201892666 A1 EA 201892666A1
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EA
Eurasian Patent Office
Prior art keywords
compounds
diphenyl
oxo
carboxamides
pyridazine
Prior art date
Application number
EA201892666A
Other languages
English (en)
Inventor
Норберт Шмеес
Илона Гутхер
Хорст Ирльбахер
Беньямин Бадер
На Чжао
Михаэль Платтен
Ульрике Рён
Ларс Рёзе
Детлеф Штёккигт
Людвиг Цорн
Original Assignee
Байер Фарма Акциенгезельшафт
Дойчес Кребсфоршунгсцентрум (Дкфц)
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.)
Filing date
Publication date
Application filed by Байер Фарма Акциенгезельшафт, Дойчес Кребсфоршунгсцентрум (Дкфц) filed Critical Байер Фарма Акциенгезельшафт
Publication of EA201892666A1 publication Critical patent/EA201892666A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/14—Oxygen atoms
    • C07D237/16—Two oxygen atoms
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Настоящее изобретение охватывает 3-оксо-2,6-дифенил-2,3-дигидропиридазин-4-карбоксамидные соединения общей формулы (I)в которой R, R, R, R, Rи Rявляются такими, как определено в описании изобретения, способы получения указанных соединений, промежуточные соединения, пригодные для получения указанных соединений, фармацевтические композиции и комбинации, содержащие указанные соединения, и применение указанных соединений для производства фармацевтических композиций для лечения или профилактики заболеваний, в частности злокачественного новообразования или состояний с разрегулированными иммунными ответами, или других нарушений, связанных с аберрантной сигнализацией AHR, в виде единственного средства или в комбинации с другими активными компонентами.
EA201892666A 2016-05-25 2017-05-23 3-оксо-2,6-дифенил-2,3-дигидропиридазин-4-карбоксамиды EA201892666A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2016083308 2016-05-25
CN2017074408 2017-02-22
PCT/EP2017/062355 WO2017202816A1 (en) 2016-05-25 2017-05-23 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides

Publications (1)

Publication Number Publication Date
EA201892666A1 true EA201892666A1 (ru) 2019-08-30

Family

ID=58745251

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201892666A EA201892666A1 (ru) 2016-05-25 2017-05-23 3-оксо-2,6-дифенил-2,3-дигидропиридазин-4-карбоксамиды

Country Status (27)

Country Link
US (1) US11040035B2 (ru)
EP (1) EP3464248B1 (ru)
JP (1) JP6964096B2 (ru)
KR (1) KR20190009369A (ru)
CN (1) CN109863140B (ru)
AU (1) AU2017269870A1 (ru)
BR (1) BR112018074185A2 (ru)
CA (1) CA3025227A1 (ru)
CL (1) CL2018003345A1 (ru)
CO (1) CO2018012654A2 (ru)
CR (1) CR20180556A (ru)
CU (1) CU20180143A7 (ru)
DO (1) DOP2018000256A (ru)
EA (1) EA201892666A1 (ru)
EC (1) ECSP18087725A (ru)
IL (1) IL263046A (ru)
MA (1) MA45087A (ru)
MX (1) MX2018014443A (ru)
NI (1) NI201800124A (ru)
PE (1) PE20190509A1 (ru)
PH (1) PH12018502472A1 (ru)
SG (1) SG11201810366WA (ru)
SV (1) SV2018005787A (ru)
TN (1) TN2018000392A1 (ru)
TW (1) TW201742859A (ru)
UY (1) UY37256A (ru)
WO (1) WO2017202816A1 (ru)

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TWI759301B (zh) 2016-05-24 2022-04-01 美商安美基公司 聚乙二醇化卡非佐米化合物
JOP20190193A1 (ar) * 2017-02-09 2019-08-08 Bayer Pharma AG ممركبات 2-أريل غير متجانس-3-أكسو-2، 3-ثنائي هيدرو بيريدازين-4-كربوكساميد لمعالجة السرطان
EP3713922A1 (en) * 2017-11-21 2020-09-30 Bayer Aktiengesellschaft Sulphur substituted 3-oxo-2,3-dihydropyridazine-4-carboxamides
EP3713923B1 (en) 2017-11-21 2021-12-01 Bayer Aktiengesellschaft 2-phenylpyrimidine-4-carboxamides as ahr inhibitors
EA037978B1 (ru) * 2017-11-21 2021-06-18 Байер Акциенгезельшафт 2-гетероарил-3-оксо-2,3-дигидропиридазин-4-карбоксамиды для лечения злокачественного новообразования
EP3713931A1 (en) 2017-11-21 2020-09-30 Bayer Aktiengesellschaft 3-oxo-6-heteroaryl-2-phenyl-2,3-dihydropyridazine-4-carboxamides
SG11202101441SA (en) 2018-08-24 2021-03-30 Jaguahr Therapeutics Pte Ltd Tetrahydropyridopyrimidine derivatives as ahr modulators
WO2020043880A1 (en) 2018-08-31 2020-03-05 Jaguahr Therapeutics Pte Ltd Heterocyclic compounds as ahr modulators
CN109771437B (zh) * 2019-03-28 2023-03-17 西安交通大学医学院第一附属医院 三氟胸苷在制备治疗三阴性乳腺癌药物中的应用
EP3715471A1 (en) * 2019-03-29 2020-09-30 Deutsches Krebsforschungszentrum, Stiftung des öffentlichen Rechts Ahr signature marker set
EP3721894A1 (en) 2019-04-10 2020-10-14 Deutsches Krebsforschungszentrum, Stiftung des öffentlichen Rechts Interleukin-4-induced gene 1 (il4i1) as a biomarker and uses thereof
JPWO2021020362A1 (ru) * 2019-07-29 2021-02-04
EP3835432A1 (en) 2019-12-10 2021-06-16 Deutsches Krebsforschungszentrum, Stiftung des öffentlichen Rechts Interleukin-4-induced gene 1 (il4i1) and respective metabolites as biomarkers for cancer
CA3164474A1 (en) * 2019-12-16 2021-06-24 Bayer Aktiengesellschaft Combination of an ahr-inhibitor and an pd1-inhibitor antibody and its use in the treatment of cancer
IL294647A (en) 2020-01-10 2022-09-01 Ikena Oncology Inc AHR inhibitors and their uses
KR20220153595A (ko) 2020-02-26 2022-11-18 재규어 테라퓨틱스 피티이 리미티드 AhR 신호전달의 조절에 유용한 피리도피리미딘 유도체
MX2022011826A (es) * 2020-03-27 2022-10-18 Dong A St Co Ltd Derivados de aminopirimidina y su uso como moduladores del receptor de hidrocarburos de arilo.
US11911376B2 (en) 2020-03-30 2024-02-27 The Regents Of The University Of Colorado Methods for preventing and treating retinal damage
CN114181212B (zh) * 2020-09-15 2023-06-06 山东轩竹医药科技有限公司 哒嗪酮类AhR抑制剂
WO2022078356A1 (zh) * 2020-10-15 2022-04-21 山东轩竹医药科技有限公司 杂芳环类AhR抑制剂
CN114685426A (zh) * 2020-12-28 2022-07-01 苏州泽璟生物制药股份有限公司 磺酰胺类抑制剂及其制备方法和应用
CN118234710A (zh) * 2021-09-14 2024-06-21 元启(苏州)生物制药有限公司 2-芳基或杂芳基-3-氧代-4-甲酰胺-6-环-二氢吡嗪芳基烃受体调节剂和其在治疗疾病和病症中的用途
WO2024076300A1 (en) 2022-10-03 2024-04-11 Jaguahr Therapeutics Pte Ltd Compounds useful in modulation of ahr signalling

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Also Published As

Publication number Publication date
ECSP18087725A (es) 2018-11-30
PE20190509A1 (es) 2019-04-10
US20200237757A1 (en) 2020-07-30
MX2018014443A (es) 2019-04-15
PH12018502472A1 (en) 2019-09-23
SV2018005787A (es) 2019-02-07
EP3464248B1 (en) 2021-09-08
AU2017269870A1 (en) 2018-12-06
CN109863140A (zh) 2019-06-07
TN2018000392A1 (en) 2020-06-15
TW201742859A (zh) 2017-12-16
CN109863140B (zh) 2023-02-21
IL263046A (en) 2018-12-31
MA45087A (fr) 2021-05-26
UY37256A (es) 2018-01-02
CL2018003345A1 (es) 2019-03-15
NI201800124A (es) 2019-04-29
CU20180143A7 (es) 2019-07-04
WO2017202816A1 (en) 2017-11-30
JP6964096B2 (ja) 2021-11-10
SG11201810366WA (en) 2018-12-28
CA3025227A1 (en) 2017-11-30
CR20180556A (es) 2019-04-23
US11040035B2 (en) 2021-06-22
EP3464248A1 (en) 2019-04-10
KR20190009369A (ko) 2019-01-28
CO2018012654A2 (es) 2018-12-14
JP2019516744A (ja) 2019-06-20
BR112018074185A2 (pt) 2019-03-06
DOP2018000256A (es) 2019-02-15

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