SG11201907232XA - 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer - Google Patents

2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer

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Publication number
SG11201907232XA
SG11201907232XA SG11201907232XA SG11201907232XA SG11201907232XA SG 11201907232X A SG11201907232X A SG 11201907232XA SG 11201907232X A SG11201907232X A SG 11201907232XA SG 11201907232X A SG11201907232X A SG 11201907232XA SG 11201907232X A SG11201907232X A SG 11201907232XA
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SG
Singapore
Prior art keywords
berlin
international
compounds
str
dihydropyridazine
Prior art date
Application number
SG11201907232XA
Inventor
Ilona Gutcher
Ulrike Röhn
Norbert Schmees
Ludwig Zorn
Lars Röse
Benjamin Bader
Christina Kober
Rafael Carretero
Detlef Stöckigt
Horst Irlbacher
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 SG11201907232XA publication Critical patent/SG11201907232XA/en

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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

Filing Language: (26) Publication Language: (30) Priority Data: 17155406.6 17202882.1 02 February 2018 (02.02.2018) English English 09 February 2017 (09.02.2017) EP 21 November 2017 (21.11.2017) EP R 5 W N 0 I .0\" 0 © R . 0 0 2 H N 'IR O O 1-1 O 71- 1-1 3 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 16 August 2018 (16.08.2018) WIPO I PCT omit VIII °nolo olomiloollm Hollow° oimIE (10) International Publication Number WO 2018/146010 Al (51) International Patent Classification: C07D 401/14 (2006.01) C07D 409/04 (2006.01) C07D 405/14 (2006.01) C07D 413/04 (2006.01) C07D 401/04 (2006.01) CO7D 417/04 (2006.01) C07D 403/04 (2006.01) CO7D 417/14 (2006.01) C07D 237/04 (2006.01) A61K 31/501 (2006.01) C07D 237/24 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/EP2018/052627 (22) International Filing Date: (71) Applicants: BAYER AKTIENGESELLSCHAFT [DE/DE]; Kaiser-Wilhelm-Allee 1, 51373 Lev- erkusen (DE). BAYER PHARMA AKTIENGESEL- LSCHAFT [DE/DE]; Miillerstr. 178, 13353 Berlin (DE). DEUTSCHES KREBSFORSCHUNGSZEN- TRUM [DE/DE]; Im Neuenheimer Feld 280, 69120 Hei- delberg (DE). (72) Inventors: GUTCHER, Ilona; Paul-Robeson-Str. 28, 10439 Berlin (DE). ROHN, Ulrike; Boyenstr. 42, 10115 Berlin (DE). SCHMEES, Norbert; Bondickstr. 61, 13469 Berlin (DE). ZORN, Ludwig; Osianderweg 45A, 13509 Berlin (DE). ROSE, Lars; Fuchsring 82, 13465 Berlin (DE). BADER, Benjamin; Hillmannstr. 14, 13467 Berlin (DE). KOBER, Christina; Heidelberger Str. 18, 76646 Bruchsal (DE). CARRETERO, Rafael; Milhlingstr. 6, 69121 Heidelberg (DE). STOCKIGT, Detlef; Clara- Zetkin-Str. 27, 14471 Potsdam (DE). IRLBACHER, Horst; Winsstr. 47, 10405 Berlin (DE). PLATTEN, Michael; Cambridgestr. 7, 69115 Heidelberg (DE). (74) Agent: BIP PATENTS; Alfred-Nobel-Str. 10, 40789 Mon- heim am Rhein (DE). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) Published: with international search report (Art. 21(3)) with sequence listing part of description (Rule 5.2(a)) 1-1 (54) Title: 2-HETEROARYL-3-OXO-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES FOR THE TREATMENT OF CANCER (57) : The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carbox- amide compounds of general formula (I), in which X, R1, R 2 , R 3 , R4 and - lc 5 are as defined here- in, methods of preparing said compounds, intermediate compounds useful for preparing said com- pounds, pharmaceutical compositions and combinations comprising said compounds and the use of (I) said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other dis- orders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
SG11201907232XA 2017-02-09 2018-02-02 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer SG11201907232XA (en)

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)

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SG11201907232XA true SG11201907232XA (en) 2019-09-27

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US (1) US11795164B2 (en)
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JP (1) JP7128826B2 (en)
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JOP20190193A1 (en) 2017-02-09 2019-08-08 Bayer Pharma AG 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer
CN109813913B (en) * 2019-01-31 2021-11-09 中国医学科学院肿瘤医院 Use of aromatic hydrocarbon receptor (AhR) for predicting immunotherapy effect
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 (en) * 2019-10-28 2022-09-16 中国农业大学 High-stability sulfonamide antibody hAb4D11 and application thereof
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
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AU2021226411A1 (en) 2020-02-26 2022-09-22 Jaguahr Therapeutics Pte Ltd Pyridopyrimidine derivatives useful in modulation of AhR signalling
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CN114539221A (en) * 2020-11-27 2022-05-27 苏州泽璟生物制药股份有限公司 Deuterated 2-heteroaromatic-3-oxo-2, 3-dihydropyridazine-4-formamide inhibitor as well as preparation method and application thereof
CN114685426A (en) * 2020-12-28 2022-07-01 苏州泽璟生物制药股份有限公司 Sulfonamide inhibitor and preparation method and application thereof
CN114835687B (en) * 2021-04-02 2023-09-05 北京华森英诺生物科技有限公司 AhR inhibitors
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
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CR20190364A (en) 2019-09-27
HRP20210143T1 (en) 2021-03-19
DK3580211T3 (en) 2021-01-25
TW201840549A (en) 2018-11-16
TWI770113B (en) 2022-07-11
RS61401B1 (en) 2021-02-26
CU24564B1 (en) 2022-01-13
DOP2019000206A (en) 2019-09-30
CU20190073A7 (en) 2020-03-04
CL2019002255A1 (en) 2020-01-03
CA3052718A1 (en) 2018-08-16
SI3580211T1 (en) 2021-06-30
HUE053191T2 (en) 2021-06-28
JP7128826B2 (en) 2022-08-31
AU2018217860A1 (en) 2019-08-22
CN116531380A (en) 2023-08-04
GEP20217281B (en) 2021-08-10
PH12019501846A1 (en) 2020-03-09
SA519402422B1 (en) 2021-11-14
JOP20190193A1 (en) 2019-08-08
KR20190115460A (en) 2019-10-11
ES2847162T3 (en) 2021-08-02
MA47447B1 (en) 2021-02-26
AU2018217860B2 (en) 2021-07-08
LT3580211T (en) 2021-02-25
US11795164B2 (en) 2023-10-24
US20230121195A1 (en) 2023-04-20
WO2018146010A1 (en) 2018-08-16
EP3580211B1 (en) 2020-12-02
MA47447A (en) 2019-12-18
CN110678459A (en) 2020-01-10
BR112019016497A2 (en) 2022-05-10
CO2019008684A2 (en) 2019-08-20
KR102627266B1 (en) 2024-01-24
UY37606A (en) 2018-09-28
CY1124484T1 (en) 2022-07-22
JP2020506946A (en) 2020-03-05
NI201900085A (en) 2019-11-15
CN116554152A (en) 2023-08-08
PL3580211T3 (en) 2021-04-19
EP3580211A1 (en) 2019-12-18
UA124507C2 (en) 2021-09-29
PE20191496A1 (en) 2019-10-21
IL268469B (en) 2022-04-01
ZA201905902B (en) 2021-05-26
CN110678459B (en) 2023-04-04
ECSP19057713A (en) 2019-08-30
IL268469A (en) 2019-09-26

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