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MX2019009571A - 2-heteroaril-3-oxo-2,3-dihidropiridazin-4-carboxamidas. - Google Patents

2-heteroaril-3-oxo-2,3-dihidropiridazin-4-carboxamidas.

Info

Publication number
MX2019009571A
MX2019009571A MX2019009571A MX2019009571A MX2019009571A MX 2019009571 A MX2019009571 A MX 2019009571A MX 2019009571 A MX2019009571 A MX 2019009571A MX 2019009571 A MX2019009571 A MX 2019009571A MX 2019009571 A MX2019009571 A MX 2019009571A
Authority
MX
Mexico
Prior art keywords
compounds
dihydropyridazine
heteroaryl
oxo
cancer
Prior art date
Application number
MX2019009571A
Other languages
English (en)
Inventor
Schmees Norbert
Zorn Ludwig
Stöckigt Detlef
Platten Michael
Röhn Ulrike
Röse Lars
Bader Benjamin
Irlbacher Horst
GUTCHER Ilona
Kober Christina
Carretero Rafael
Original Assignee
Bayer Ag
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 Bayer Ag filed Critical Bayer Ag
Publication of MX2019009571A publication Critical patent/MX2019009571A/es

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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • 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
    • 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
    • C07D237/04—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
    • 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
    • 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La presente invención comprende compuestos de 2-heteroaril-3-oxo-2,3-dihidropiridazin-4-carboxamida de la fórmula general (I): (ver Fórmula) en donde X, R1, R2, R3, R4 y R5 son como se definen en la presente, procedimientos para preparar tales compuestos, compuestos intermedios útiles para preparar dichos compuestos, composiciones y combinaciones farmacéuticas que comprenden tales compuestos y el uso de dichos compuestos para la elaboración de composiciones farmacéuticas para el tratamiento o la profilaxis de enfermedades, en particular cáncer o afecciones con respuestas inmunes desreguladas u otros trastornos asociados con la señalización anormal de AHR, como único agente o en combinación con otros ingredientes activos.
MX2019009571A 2017-02-09 2018-02-02 2-heteroaril-3-oxo-2,3-dihidropiridazin-4-carboxamidas. MX2019009571A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17155406 2017-02-09
EP17202882 2017-11-21
PCT/EP2018/052627 WO2018146010A1 (en) 2017-02-09 2018-02-02 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer

Publications (1)

Publication Number Publication Date
MX2019009571A true MX2019009571A (es) 2020-01-20

Family

ID=61188789

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2019009571A MX2019009571A (es) 2017-02-09 2018-02-02 2-heteroaril-3-oxo-2,3-dihidropiridazin-4-carboxamidas.

Country Status (38)

Country Link
US (2) US20240294505A1 (es)
EP (1) EP3580211B1 (es)
JP (1) JP7128826B2 (es)
KR (1) KR102627266B1 (es)
CN (3) CN116531380A (es)
AU (1) AU2018217860B2 (es)
BR (1) BR112019016497A2 (es)
CA (1) CA3052718A1 (es)
CL (1) CL2019002255A1 (es)
CO (1) CO2019008684A2 (es)
CR (1) CR20190364A (es)
CU (1) CU24564B1 (es)
CY (1) CY1124484T1 (es)
DK (1) DK3580211T3 (es)
DO (1) DOP2019000206A (es)
EC (1) ECSP19057713A (es)
ES (1) ES2847162T3 (es)
GE (1) GEP20217281B (es)
HR (1) HRP20210143T1 (es)
HU (1) HUE053191T2 (es)
IL (1) IL268469B (es)
JO (1) JOP20190193A1 (es)
LT (1) LT3580211T (es)
MA (1) MA47447B1 (es)
MX (1) MX2019009571A (es)
NI (1) NI201900085A (es)
PE (1) PE20191496A1 (es)
PH (1) PH12019501846A1 (es)
PL (1) PL3580211T3 (es)
RS (1) RS61401B1 (es)
SA (1) SA519402422B1 (es)
SG (1) SG11201907232XA (es)
SI (1) SI3580211T1 (es)
TW (1) TWI770113B (es)
UA (1) UA124507C2 (es)
UY (1) UY37606A (es)
WO (1) WO2018146010A1 (es)
ZA (1) ZA201905902B (es)

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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
CN109813913B (zh) * 2019-01-31 2021-11-09 中国医学科学院肿瘤医院 芳烃受体(AhR)在预测免疫治疗效果中的应用
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
CN112724256B (zh) * 2019-10-28 2022-09-16 中国农业大学 一种高稳定性的磺胺类药物抗体hAb 4D11及其应用
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
US20230084899A1 (en) * 2019-12-16 2023-03-16 Bayer Aktiengesellschaft Combination of an ahr-inhibitor and an pd1-inhibitor antibody and its use in the treatment of cancer
CN115244048A (zh) 2020-02-26 2022-10-25 捷豹治疗有限公司 可用于调节AhR信号传导的吡啶并嘧啶衍生物
WO2021194326A1 (en) * 2020-03-27 2021-09-30 Dong-A St Co., Ltd. Aminopyrimidine derivatives and their use as aryl hydrocarbon receptor modulators
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
CN114369097B (zh) * 2020-10-15 2023-07-14 山东轩竹医药科技有限公司 杂芳环类AhR抑制剂
CN114539221A (zh) * 2020-11-27 2022-05-27 苏州泽璟生物制药股份有限公司 氘代2-芳杂环-3-氧-2,3-二氢哒嗪-4-甲酰胺类抑制剂及其制备方法和应用
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
CN114835687B (zh) * 2021-04-02 2023-09-05 北京华森英诺生物科技有限公司 AhR抑制剂
WO2023043753A1 (en) * 2021-09-14 2023-03-23 Allianthera (Suzhou) Biopharmaceutical Co., Ltd. 2-aryl or heteroaryl-3-oxo-4-carbamide-6-cyclic-dihydropyrazine aryl hydrocarbon receptor modulators and their use in the treatment of diseases and disorders
AU2022369984A1 (en) 2021-10-20 2024-03-28 University Of Rochester Methods and compositions for rejuvenating cns glial populations by suppression of transcription factors
CN119948035A (zh) 2022-10-03 2025-05-06 捷豹治疗有限公司 可用于调节AhR信号传导的化合物

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KR102627266B1 (ko) 2024-01-24
EP3580211A1 (en) 2019-12-18
UA124507C2 (uk) 2021-09-29
CN110678459B (zh) 2023-04-04
DK3580211T3 (da) 2021-01-25
CA3052718A1 (en) 2018-08-16
UY37606A (es) 2018-09-28
IL268469A (en) 2019-09-26
SI3580211T1 (sl) 2021-06-30
HRP20210143T1 (hr) 2021-03-19
US20240294505A1 (en) 2024-09-05
CY1124484T1 (el) 2022-07-22
CU24564B1 (es) 2022-01-13
CL2019002255A1 (es) 2020-01-03
NI201900085A (es) 2019-11-15
MA47447A (fr) 2019-12-18
ZA201905902B (en) 2021-05-26
IL268469B (en) 2022-04-01
ECSP19057713A (es) 2019-08-30
JOP20190193A1 (ar) 2019-08-08
RS61401B1 (sr) 2021-02-26
PH12019501846A1 (en) 2020-03-09
MA47447B1 (fr) 2021-02-26
AU2018217860B2 (en) 2021-07-08
TWI770113B (zh) 2022-07-11
BR112019016497A2 (pt) 2022-05-10
TW201840549A (zh) 2018-11-16
HUE053191T2 (hu) 2021-06-28
EP3580211B1 (en) 2020-12-02
AU2018217860A1 (en) 2019-08-22
SA519402422B1 (ar) 2021-11-14
US20230121195A1 (en) 2023-04-20
LT3580211T (lt) 2021-02-25
GEP20217281B (en) 2021-08-10
ES2847162T3 (es) 2021-08-02
JP2020506946A (ja) 2020-03-05
CU20190073A7 (es) 2020-03-04
CO2019008684A2 (es) 2019-08-20
KR20190115460A (ko) 2019-10-11
CN116531380A (zh) 2023-08-04
DOP2019000206A (es) 2019-09-30
CR20190364A (es) 2019-09-27
CN116554152A (zh) 2023-08-08
WO2018146010A1 (en) 2018-08-16
JP7128826B2 (ja) 2022-08-31
CN110678459A (zh) 2020-01-10
PE20191496A1 (es) 2019-10-21
US11795164B2 (en) 2023-10-24
PL3580211T3 (pl) 2021-04-19
SG11201907232XA (en) 2019-09-27

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