PE20191496A1 - 2-heteroaril-3-oxo-2,3-dihidropiridazin-4-carboxamidas - Google Patents

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

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Publication number
PE20191496A1
PE20191496A1 PE2019001570A PE2019001570A PE20191496A1 PE 20191496 A1 PE20191496 A1 PE 20191496A1 PE 2019001570 A PE2019001570 A PE 2019001570A PE 2019001570 A PE2019001570 A PE 2019001570A PE 20191496 A1 PE20191496 A1 PE 20191496A1
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PE
Peru
Prior art keywords
dihydropyridazine
oxo
heteroaryl
optionally substituted
compounds
Prior art date
Application number
PE2019001570A
Other languages
English (en)
Inventor
Norbert Schmees
Ilona Gutcher
Horst Irlbacher
Benjamin Bader
Detlef Stockigt
Lars Rose
Ludwig Zorn
Ulrike Rohn
Christina Kober
Rafael Carretero
Michael Platten
Original Assignee
Bayer Ag
Bayer Pharma 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.)
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Publication date
Application filed by Bayer Ag, Bayer Pharma AG filed Critical Bayer Ag
Publication of PE20191496A1 publication Critical patent/PE20191496A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic 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
    • C07D237/10Heterocyclic 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
    • C07D237/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

Referido a compuestos de 2-heteroaril-3-oxo-2,3- dihidropiridazin-4-carboxamida de la formula (I), en donde R1 es hidroxialquilo-C2-C6 opcionalmente sustituidos; cicloalquilo-C3-C6 opcionalmente sustituido, entre otros; R2 es Cl, Ciano, entre otros; R3 es H, F, Cl o metilo; R4 es H o F; R5 es heteroarilo monociclico opcionalmente sustituido, entre otros; X es CH o N. Un compuesto seleccionado es N-(1-hidroxi-3-metilbutan-2-il)-6-(4-metilfenil)-2-(1-metil-1H-pirazol-4-il)-3-oxo- 2,3-dihidropiridazin-4-carboxamida. Tambien se refiere a un procedimiento para preparar dichos compuestos, compuestos intermedios, una composicion y combinacion farmaceutica que los comprende y el uso de dichos compuestos para el tratamiento o la profilaxis del cancer, afecciones con respuestas inmunes desreguladas u otros trastornos asociados con la senalizacion anormal de AHR, como unico agente o en combinacion con otros ingredientes activos.
PE2019001570A 2017-02-09 2018-02-02 2-heteroaril-3-oxo-2,3-dihidropiridazin-4-carboxamidas PE20191496A1 (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
PE20191496A1 true PE20191496A1 (es) 2019-10-21

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PE2019001570A PE20191496A1 (es) 2017-02-09 2018-02-02 2-heteroaril-3-oxo-2,3-dihidropiridazin-4-carboxamidas

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US (1) US11795164B2 (es)
EP (1) EP3580211B1 (es)
JP (1) JP7128826B2 (es)
KR (1) KR102627266B1 (es)
CN (3) CN110678459B (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
KR20220128622A (ko) * 2019-12-16 2022-09-21 바이엘 악티엔게젤샤프트 Ahr-억제제 및 pd1-억제제 항체의 조합물 및 암 치료에서의 그의 용도
EP4110778A1 (en) 2020-02-26 2023-01-04 Jaguahr Therapeutics Pte Ltd Pyridopyrimidine derivatives useful in modulation of ahr signalling
EP4126839A4 (en) * 2020-03-27 2024-04-17 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
AU2022345008A1 (en) * 2021-09-14 2024-04-04 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
US20230190961A1 (en) 2021-10-20 2023-06-22 University Of Rochester Compositions and methods for treating myelin deficiency by rejuvenating glial progenitor cells
WO2024076300A1 (en) 2022-10-03 2024-04-11 Jaguahr Therapeutics Pte Ltd Compounds useful in modulation of ahr signalling

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SI3580211T1 (sl) 2021-06-30
HRP20210143T1 (hr) 2021-03-19
CN116531380A (zh) 2023-08-04
CN110678459A (zh) 2020-01-10
CO2019008684A2 (es) 2019-08-20
TWI770113B (zh) 2022-07-11
CY1124484T1 (el) 2022-07-22
CR20190364A (es) 2019-09-27
CN116554152A (zh) 2023-08-08
SG11201907232XA (en) 2019-09-27
CU20190073A7 (es) 2020-03-04
UY37606A (es) 2018-09-28
CN110678459B (zh) 2023-04-04
GEP20217281B (en) 2021-08-10
JP7128826B2 (ja) 2022-08-31
MA47447A (fr) 2019-12-18
NI201900085A (es) 2019-11-15
US20230121195A1 (en) 2023-04-20
US11795164B2 (en) 2023-10-24
CU24564B1 (es) 2022-01-13
LT3580211T (lt) 2021-02-25
ZA201905902B (en) 2021-05-26
AU2018217860B2 (en) 2021-07-08
AU2018217860A1 (en) 2019-08-22
PL3580211T3 (pl) 2021-04-19
KR102627266B1 (ko) 2024-01-24
DK3580211T3 (da) 2021-01-25
EP3580211A1 (en) 2019-12-18
TW201840549A (zh) 2018-11-16
HUE053191T2 (hu) 2021-06-28
PH12019501846A1 (en) 2020-03-09
CA3052718A1 (en) 2018-08-16
ES2847162T3 (es) 2021-08-02
KR20190115460A (ko) 2019-10-11
MA47447B1 (fr) 2021-02-26
JP2020506946A (ja) 2020-03-05
WO2018146010A1 (en) 2018-08-16
ECSP19057713A (es) 2019-08-30
CL2019002255A1 (es) 2020-01-03
BR112019016497A2 (pt) 2022-05-10
IL268469A (en) 2019-09-26
RS61401B1 (sr) 2021-02-26
IL268469B (en) 2022-04-01
EP3580211B1 (en) 2020-12-02
MX2019009571A (es) 2020-01-20
DOP2019000206A (es) 2019-09-30
JOP20190193A1 (ar) 2019-08-08
UA124507C2 (uk) 2021-09-29
SA519402422B1 (ar) 2021-11-14

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