AU2019360428B2 - Pyrazole derivatives as H4 antagonist compounds - Google Patents

Pyrazole derivatives as H4 antagonist compounds Download PDF

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Publication number
AU2019360428B2
AU2019360428B2 AU2019360428A AU2019360428A AU2019360428B2 AU 2019360428 B2 AU2019360428 B2 AU 2019360428B2 AU 2019360428 A AU2019360428 A AU 2019360428A AU 2019360428 A AU2019360428 A AU 2019360428A AU 2019360428 B2 AU2019360428 B2 AU 2019360428B2
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Australia
Prior art keywords
methyl
mmol
pyrazole
compound according
cas
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AU2019360428A
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AU2019360428A1 (en
Inventor
Giovanni BOTTEGONI
Giles Albert Brown
Miles Stuart Congreve
Charlotte Fieldhouse
Mark PICKWORTH
Nigel Alan Swain
Barry John Teobald
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Nxera Pharma UK Ltd
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Nxera Pharma UK Ltd
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Assigned to NXERA PHARMA UK LIMITED reassignment NXERA PHARMA UK LIMITED Amend patent request/document other than specification (104) Assignors: HEPTARES THERAPEUTICS LIMITED
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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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2019360428A 2018-10-19 2019-10-21 Pyrazole derivatives as H4 antagonist compounds Active AU2019360428B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1817047.2A GB201817047D0 (en) 2018-10-19 2018-10-19 H4 antagonist compounds
GB1817047.2 2018-10-19
PCT/GB2019/052997 WO2020079457A1 (en) 2018-10-19 2019-10-21 Pyrazole derivatives as h4 antagonist compounds

Publications (2)

Publication Number Publication Date
AU2019360428A1 AU2019360428A1 (en) 2021-04-29
AU2019360428B2 true AU2019360428B2 (en) 2024-05-09

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2019360428A Active AU2019360428B2 (en) 2018-10-19 2019-10-21 Pyrazole derivatives as H4 antagonist compounds

Country Status (13)

Country Link
US (2) US12234227B2 (https=)
EP (1) EP3867248B1 (https=)
JP (1) JP7532353B2 (https=)
KR (1) KR102873380B1 (https=)
CN (1) CN113272297B (https=)
AU (1) AU2019360428B2 (https=)
BR (1) BR112021007372A2 (https=)
CA (1) CA3116628A1 (https=)
ES (1) ES3058587T3 (https=)
GB (1) GB201817047D0 (https=)
MX (1) MX2021004280A (https=)
SG (1) SG11202103133QA (https=)
WO (1) WO2020079457A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB202005858D0 (en) * 2020-04-22 2020-06-03 Heptares Therapeutics Ltd H4 Antagonist compounds
GB202019667D0 (en) * 2020-12-14 2021-01-27 Heptares Therapeutics Ltd H4 antagonist comnpounds
WO2022203399A1 (ko) * 2021-03-26 2022-09-29 주식회사 스탠다임 아데노신 a2a 수용체 길항제 및 이의 용도
WO2022232259A1 (en) * 2021-04-28 2022-11-03 Cornell University Soluble adenylyl cyclase (sac) inhibitors and uses thereof
EP4421067A4 (en) * 2021-10-19 2026-01-14 Unimatec Co Ltd PYRAZOLE COMPOUND CONTAINING FLUORIDE AND ITS PRODUCTION PROCESS
KR102621694B1 (ko) * 2022-09-15 2024-01-08 주식회사 스탠다임 아데노신 a2a 수용체 길항제 및 이의 용도

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1103551A1 (en) * 1998-07-24 2001-05-30 Daiichi Pharmaceutical Co., Ltd. Pyrazole derivatives and salts thereof
WO2005054239A1 (en) * 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
WO2007072163A2 (en) * 2005-12-20 2007-06-28 Pfizer Limited Pyrimidine derivatives
WO2008060766A2 (en) * 2006-10-02 2008-05-22 Abbott Laboratories Histamine h4 receptor ligands for use in pain treatment
WO2010059658A1 (en) * 2008-11-20 2010-05-27 Glaxosmithkline Llc Chemical compounds

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000169475A (ja) 1998-07-24 2000-06-20 Dai Ichi Seiyaku Co Ltd ピラゾ―ル誘導体およびその塩
US20100035863A1 (en) 2006-09-12 2010-02-11 Ucb Pharma, S.A. 2 Amino-Pyrimidine Derivatives As H4 Receptor Antagonists, Processes For Preparing Them And Their Use In Pharmaceutical Compositions
CL2008000467A1 (es) 2007-02-14 2008-08-22 Janssen Pharmaceutica Nv Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma
WO2009068512A1 (en) 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
PE20091524A1 (es) 2007-12-19 2009-09-25 Palau Pharma Sa Derivados de 2-aminopirimidina
CN101903385B (zh) 2007-12-21 2013-11-06 帕劳制药股份有限公司 作为组胺h4受体拮抗剂的4-氨基嘧啶衍生物
TW201035078A (en) 2009-03-20 2010-10-01 Incyte Corp Substituted heterocyclic compounds
MX2012004995A (es) 2009-10-29 2012-10-03 Sirtris Pharmaceuticals Inc Piridinas biciclicas y analogos como moduladores de sirtuina.
WO2011076878A1 (en) 2009-12-23 2011-06-30 Palau Pharma, S.A. Aminoalkylpyrimidine derivatives as histamine h4 receptor antagonists
US9580443B2 (en) 2012-11-16 2017-02-28 Merck Patent Gmbh Heterocyclic derivatives as modulators of kinase activity
US11401255B2 (en) 2016-07-28 2022-08-02 Mayo Foundation For Medical Education And Research Small molecule activators of Parkin enzyme function

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1103551A1 (en) * 1998-07-24 2001-05-30 Daiichi Pharmaceutical Co., Ltd. Pyrazole derivatives and salts thereof
WO2005054239A1 (en) * 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
WO2007072163A2 (en) * 2005-12-20 2007-06-28 Pfizer Limited Pyrimidine derivatives
WO2008060766A2 (en) * 2006-10-02 2008-05-22 Abbott Laboratories Histamine h4 receptor ligands for use in pain treatment
WO2010059658A1 (en) * 2008-11-20 2010-05-27 Glaxosmithkline Llc Chemical compounds

Also Published As

Publication number Publication date
EP3867248B1 (en) 2025-12-10
KR102873380B1 (ko) 2025-10-23
CA3116628A1 (en) 2020-04-23
EP3867248A1 (en) 2021-08-25
CN113272297B (zh) 2024-03-19
US20250115587A1 (en) 2025-04-10
WO2020079457A1 (en) 2020-04-23
US20210300906A1 (en) 2021-09-30
GB201817047D0 (en) 2018-12-05
US12234227B2 (en) 2025-02-25
SG11202103133QA (en) 2021-05-28
CN113272297A (zh) 2021-08-17
ES3058587T3 (en) 2026-03-11
KR20210079318A (ko) 2021-06-29
JP7532353B2 (ja) 2024-08-13
MX2021004280A (es) 2021-05-31
EP3867248C0 (en) 2025-12-10
JP2022507013A (ja) 2022-01-18
BR112021007372A2 (pt) 2021-07-20
AU2019360428A1 (en) 2021-04-29

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