JP6586098B2 - キナーゼ阻害剤としてのピラゾリル尿素 - Google Patents

キナーゼ阻害剤としてのピラゾリル尿素 Download PDF

Info

Publication number
JP6586098B2
JP6586098B2 JP2016551294A JP2016551294A JP6586098B2 JP 6586098 B2 JP6586098 B2 JP 6586098B2 JP 2016551294 A JP2016551294 A JP 2016551294A JP 2016551294 A JP2016551294 A JP 2016551294A JP 6586098 B2 JP6586098 B2 JP 6586098B2
Authority
JP
Japan
Prior art keywords
tert
butyl
pyrazol
naphthalen
pyridin
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2016551294A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017505794A5 (enExample
JP2017505794A (ja
Inventor
ロングシヨー，アリステア・イアン
フオーダイス，ユアン・アレクサンダー・フレイザー
オニオンズ，スチユアート・トーマス
キング−アンダーウツド，ジヨン
ベナブル，ジエニフアー・ダイアン
ウオルターズ，イアイン
Original Assignee
レスピバート・リミテツド
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 レスピバート・リミテツド filed Critical レスピバート・リミテツド
Publication of JP2017505794A publication Critical patent/JP2017505794A/ja
Publication of JP2017505794A5 publication Critical patent/JP2017505794A5/ja
Priority to JP2019162164A priority Critical patent/JP6952085B2/ja
Application granted granted Critical
Publication of JP6586098B2 publication Critical patent/JP6586098B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D403/14—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 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
    • C07D409/14—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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016551294A 2014-02-14 2015-02-13 キナーゼ阻害剤としてのピラゾリル尿素 Active JP6586098B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2019162164A JP6952085B2 (ja) 2014-02-14 2019-09-05 キナーゼ阻害剤としてのピラゾリル尿素

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461940282P 2014-02-14 2014-02-14
US61/940,282 2014-02-14
US201461941064P 2014-02-18 2014-02-18
US61/941,064 2014-02-18
PCT/GB2015/050401 WO2015121660A1 (en) 2014-02-14 2015-02-13 Pyrazolyl-ureas as kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2019162164A Division JP6952085B2 (ja) 2014-02-14 2019-09-05 キナーゼ阻害剤としてのピラゾリル尿素

Publications (3)

Publication Number Publication Date
JP2017505794A JP2017505794A (ja) 2017-02-23
JP2017505794A5 JP2017505794A5 (enExample) 2019-04-04
JP6586098B2 true JP6586098B2 (ja) 2019-10-02

Family

ID=52573661

Family Applications (4)

Application Number Title Priority Date Filing Date
JP2016551294A Active JP6586098B2 (ja) 2014-02-14 2015-02-13 キナーゼ阻害剤としてのピラゾリル尿素
JP2016550815A Active JP6630280B2 (ja) 2014-02-14 2015-02-13 抗炎症化合物としての芳香族複素環化合物
JP2019162164A Active JP6952085B2 (ja) 2014-02-14 2019-09-05 キナーゼ阻害剤としてのピラゾリル尿素
JP2019220267A Active JP6841891B2 (ja) 2014-02-14 2019-12-05 抗炎症化合物としての芳香族複素環化合物

Family Applications After (3)

Application Number Title Priority Date Filing Date
JP2016550815A Active JP6630280B2 (ja) 2014-02-14 2015-02-13 抗炎症化合物としての芳香族複素環化合物
JP2019162164A Active JP6952085B2 (ja) 2014-02-14 2019-09-05 キナーゼ阻害剤としてのピラゾリル尿素
JP2019220267A Active JP6841891B2 (ja) 2014-02-14 2019-12-05 抗炎症化合物としての芳香族複素環化合物

Country Status (20)

Country Link
US (8) US9447076B2 (enExample)
EP (4) EP3418279B1 (enExample)
JP (4) JP6586098B2 (enExample)
KR (1) KR102413704B1 (enExample)
CN (4) CN110522731B (enExample)
AU (3) AU2015216705B2 (enExample)
BR (1) BR112016015838B1 (enExample)
CA (1) CA2938924C (enExample)
DK (2) DK3105222T3 (enExample)
EA (1) EA034927B1 (enExample)
ES (2) ES2677595T3 (enExample)
JO (1) JO3392B1 (enExample)
MX (2) MX371353B (enExample)
PL (2) PL3357919T3 (enExample)
PT (2) PT3357919T (enExample)
SG (1) SG11201607058PA (enExample)
TR (1) TR201809072T4 (enExample)
TW (2) TWI751099B (enExample)
UY (1) UY35998A (enExample)
WO (2) WO2015121660A1 (enExample)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA105763C2 (uk) 2007-12-19 2014-06-25 Кансер Рісерч Текнолоджі Лімітед 8-ЗАМІЩЕНІ ПІРИДО[2,3-b]ПІРАЗИНИ ТА ЇХ ЗАСТОСУВАННЯ
WO2011092469A1 (en) 2010-02-01 2011-08-04 Cancer Research Technology Limited 1-(5-tert-butyl-2-phenyl-2h-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy
SG11201400226UA (en) 2011-10-03 2014-09-26 Respivert Ltd 1-pyrazolyl-3- (4- ( (2 -anilinopyrimidin- 4 - yl) oxy) napththalen- 1 - yl) ureas as p38 map kinase inhibitors
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
EP2890701B1 (en) 2012-08-29 2017-03-29 Respivert Limited Kinase inhibitors
EP2890460B1 (en) 2012-08-29 2017-02-22 Respivert Limited Kinase inhibitors
EP2890695A2 (en) 2012-08-29 2015-07-08 Respivert Limited Kinase inhibitors
US9732063B2 (en) 2012-11-16 2017-08-15 Respivert Limited Kinase inhibitors
EP2970190A1 (en) 2013-03-14 2016-01-20 Respivert Limited Kinase inhibitors
KR102283876B1 (ko) 2013-04-02 2021-07-29 옥슬러 액퀴지션즈 리미티드 키나제 저해제로서 유용한 우레아 유도체
WO2014162121A1 (en) 2013-04-02 2014-10-09 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
GB201320732D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Methods of chemical synthesis
EP3083604A1 (en) 2013-12-20 2016-10-26 Respivert Limited Urea derivatives useful as kinase inhibitors
CN110522731B (zh) * 2014-02-14 2022-08-02 瑞斯比维特有限公司 作为抗炎化合物的芳族杂环化合物
MA40775A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivé d'acide 4-(4-(4-phényluréido-naphtalén -1-yl) oxy-pyridin-2-yl) amino-benzoïque utilisé en tant qu'inhibiteur de la kinase p38
CN105801486A (zh) * 2016-03-31 2016-07-27 常州大学 一种1-（2,4二溴苯基）-3-吡唑醇的合成方法
AU2017245888B2 (en) 2016-04-06 2021-05-13 Oxular Acquisitions Limited Kinase inhibitors
US20190151324A1 (en) 2016-06-23 2019-05-23 University Of Maryland, Baltimore NON-CATALYTIC SUBSTRATE-SELECTIVE P38alpha-SPECIFIC MAPK INHIBITORS WITH ENDOTHELIAL-STABILIZING AND ANTI-INFLAMMATORY ACTIVITY, AND METHODS OF USE THEREOF
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
UY37918A (es) 2017-10-05 2019-04-30 Fulcrum Therapeutics Inc Inhibidores de la quinasa p38 que reducen la expresión de dux4 y de los genes corriente abajo para el tratamiento de fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
WO2020118194A1 (en) 2018-12-07 2020-06-11 University Of Maryland, Baltimore NON-ATP/CATALYTIC SITE p38 MITOGEN ACTIVATED PROTEIN KINASE INHIBITORS
US10851102B2 (en) * 2019-01-23 2020-12-01 Theravance Biopharma R&D Ip, Llc Imidazole and triazole containing bicyclic compounds as JAK inhibitors
US11286260B2 (en) * 2020-05-18 2022-03-29 Gen1E Lifesciences Inc. P38α mitogen-activated protein kinase inhibitors
CN111889025B (zh) * 2020-09-01 2022-01-11 山东大学 一种耐酸碱耐盐超两亲分子乳化剂及其制备方法和乳液
NZ798990A (en) 2020-10-29 2025-09-26 Gen1E Lifesciences Inc Crystalline 5-(dimethylamino)-n-(4-(morpholinomethyl)phenyl) naphthalene-1-sulfonamide di-hydrochloride di-hydrate
KR20230142752A (ko) * 2021-02-03 2023-10-11 비피 애셋 브이, 인크. 흡입을 위한 퓨린 억제제의 제제
CN117120422A (zh) 2021-03-23 2023-11-24 Gen1E生命科学公司 取代的萘基P38α丝裂原活化的蛋白激酶抑制剂
CN116655608B (zh) * 2023-05-30 2025-08-19 成都瑞芬思德丹生物科技有限公司 一种具有抗炎活性的吡咯烷酮类化合物及其制备方法和应用

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
US20080300281A1 (en) 1997-12-22 2008-12-04 Jacques Dumas Inhibition of p38 Kinase Activity Using Aryl and Heteroaryl Substituted Heterocyclic Ureas
IL136768A0 (en) 1997-12-22 2001-06-14 Bayer Ag INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
DK1056725T3 (da) 1997-12-22 2006-10-02 Bayer Pharmaceuticals Corp Inhibering af raf-kinase ved hjælp af aryl- og heteroaryl-substituerede heterocykliske urinstoffer
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
DE60024830T2 (de) 1999-07-09 2006-06-14 Boehringer Ingelheim Pharma Verfahren zur herstellung heteroarylsubstituierter ureaverbindungen
CA2389360C (en) 1999-11-16 2008-06-03 Steffen Breitfelder Urea derivatives as anti-inflammatory agents
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
US6492529B1 (en) 2000-01-18 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Bis pyrazole-1H-pyrazole intermediates and their synthesis
WO2001064642A2 (en) 2000-02-29 2001-09-07 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
EP1392661A1 (en) 2001-05-16 2004-03-03 Boehringer Ingelheim Pharmaceuticals Inc. Diarylurea derivatives useful as anti-inflammatory agents
ES2284887T3 (es) 2001-07-11 2007-11-16 Boehringer Ingelheim Pharmaceuticals Inc. Metodos para tratar enfermedades transmitidas por citocinas.
AU2003209119A1 (en) 2002-02-11 2003-09-04 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
ES2425739T3 (es) 2002-02-11 2013-10-17 Bayer Healthcare Llc Sorafenib-tosilato para el tratamiento de enfermedades caracterizadas por angiogénesis anormal
ES2299689T3 (es) * 2002-02-25 2008-06-01 Boehringer Ingelheim Pharmaceuticals Inc. Compuestos de cicloalquil-uera fusionada con benzo 1,4-disustituido, utiles para el tratamiento de enfermedades por citoquinas.
EP2471533A1 (en) 2002-06-27 2012-07-04 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
WO2004007472A1 (ja) 2002-07-10 2004-01-22 Ono Pharmaceutical Co., Ltd. Ｃｃｒ４アンタゴニストおよびその医薬用途
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
CN1839126A (zh) 2003-02-28 2006-09-27 拜耳制药公司 用于治疗癌症和其它病症的新的氰基吡啶衍生物
EP2295427A1 (en) 2004-04-30 2011-03-16 Bayer HealthCare, LLC Substituted pyrazolyl urea derivatives useful in the treatment of cancer
GB0500435D0 (en) 2005-01-10 2005-02-16 Novartis Ag Organic compounds
WO2007002635A2 (en) 2005-06-27 2007-01-04 Bristol-Myers Squibb Company C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
AU2007325576B2 (en) 2006-10-20 2013-01-10 Icos Corporation Compositions of Chk1 inhibitors
WO2009117080A1 (en) 2008-03-17 2009-09-24 Ambit Biosciences Corporaton Quinazoline derivatives as raf kinase modulators and methods of use thereof
GB0818033D0 (en) 2008-10-02 2008-11-05 Respivert Ltd Novel compound
JP2012504591A (ja) 2008-10-02 2012-02-23 レスピバート・リミテツド ｐ３８ＭＡＰキナーゼ阻害剤
JP2012511563A (ja) 2008-12-11 2012-05-24 レスピバート・リミテツド ｐ３８ＭＡＰキナーゼ阻害剤
GB0905955D0 (en) 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
GB0921731D0 (en) 2009-12-11 2010-01-27 Respivert Ltd Theraputic uses
GB0921730D0 (en) 2009-12-11 2010-01-27 Respivert Ltd Method of treatment
ES2676918T3 (es) 2010-03-15 2018-07-26 Ube Industries, Ltd. Método para producir un compuesto de amida
GB201005589D0 (en) 2010-04-01 2010-05-19 Respivert Ltd Novel compounds
JP5787977B2 (ja) 2010-04-08 2015-09-30 レスピバート・リミテツド Ｐ３８ｍａｐキナーゼ阻害剤
JP5787976B2 (ja) * 2010-04-08 2015-09-30 レスピバート・リミテツド Ｐ３８ｍａｐキナーゼ阻害剤としてのピラゾリルウレア
WO2011158044A2 (en) 2010-06-17 2011-12-22 Respivert Limited Respiratory formulations and compounds for use therein
GB201010193D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Medicinal use
GB201010196D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Methods
SG11201400226UA (en) * 2011-10-03 2014-09-26 Respivert Ltd 1-pyrazolyl-3- (4- ( (2 -anilinopyrimidin- 4 - yl) oxy) napththalen- 1 - yl) ureas as p38 map kinase inhibitors
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
HRP20161714T1 (hr) 2011-12-09 2017-02-10 Chiesi Farmaceutici S.P.A. Inhibitori kinaze
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
GB201215357D0 (en) * 2012-08-29 2012-10-10 Respivert Ltd Compounds
EP2890695A2 (en) 2012-08-29 2015-07-08 Respivert Limited Kinase inhibitors
EP2890460B1 (en) 2012-08-29 2017-02-22 Respivert Limited Kinase inhibitors
EP2890701B1 (en) 2012-08-29 2017-03-29 Respivert Limited Kinase inhibitors
US9732063B2 (en) 2012-11-16 2017-08-15 Respivert Limited Kinase inhibitors
EP2970190A1 (en) 2013-03-14 2016-01-20 Respivert Limited Kinase inhibitors
WO2014162121A1 (en) 2013-04-02 2014-10-09 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
KR102283876B1 (ko) 2013-04-02 2021-07-29 옥슬러 액퀴지션즈 리미티드 키나제 저해제로서 유용한 우레아 유도체
EP3083604A1 (en) 2013-12-20 2016-10-26 Respivert Limited Urea derivatives useful as kinase inhibitors
CN110522731B (zh) 2014-02-14 2022-08-02 瑞斯比维特有限公司 作为抗炎化合物的芳族杂环化合物
WO2016051186A1 (en) 2014-10-01 2016-04-07 Respivert Limited N-phenyl-3-quinazolin-6-yl-benzamide derivatives as p38 kinase inhibitors
MA40775A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivé d'acide 4-(4-(4-phényluréido-naphtalén -1-yl) oxy-pyridin-2-yl) amino-benzoïque utilisé en tant qu'inhibiteur de la kinase p38

Also Published As

Publication number Publication date
US20160368896A1 (en) 2016-12-22
US20150232450A1 (en) 2015-08-20
US20190092752A1 (en) 2019-03-28
AU2015216705B2 (en) 2019-03-28
PL3357919T3 (pl) 2020-06-01
KR20160115949A (ko) 2016-10-06
JO3392B1 (ar) 2019-10-20
EP3418279A1 (en) 2018-12-26
BR112016015838A8 (pt) 2021-07-06
EP3105223B1 (en) 2018-09-12
DK3105222T3 (en) 2018-07-23
CN106573914A (zh) 2017-04-19
PT3105222T (pt) 2018-07-18
US10815217B2 (en) 2020-10-27
JP6630280B2 (ja) 2020-01-15
US20180118719A1 (en) 2018-05-03
CA2939355A1 (en) 2015-08-20
UY35998A (es) 2015-08-31
US20170057945A1 (en) 2017-03-02
EP3105222B1 (en) 2018-04-11
JP6841891B2 (ja) 2021-03-10
AU2019204525B2 (en) 2021-01-21
JP2020055847A (ja) 2020-04-09
CN106164067A (zh) 2016-11-23
EP3105222A1 (en) 2016-12-21
WO2015121660A1 (en) 2015-08-20
PL3105222T3 (pl) 2018-09-28
US9884845B2 (en) 2018-02-06
EA034927B1 (ru) 2020-04-07
CN113264921A (zh) 2021-08-17
CN110522731B (zh) 2022-08-02
US20200002311A1 (en) 2020-01-02
MX371353B (es) 2020-01-27
AU2015216957A1 (en) 2016-07-14
SG11201607058PA (en) 2016-10-28
US11634406B2 (en) 2023-04-25
EP3105223A1 (en) 2016-12-21
JP2017505784A (ja) 2017-02-23
BR112016015838A2 (pt) 2017-08-08
WO2015121444A1 (en) 2015-08-20
AU2015216705A1 (en) 2016-08-18
EP3418279B1 (en) 2021-01-20
JP2017505794A (ja) 2017-02-23
MX371312B (es) 2020-01-24
PT3357919T (pt) 2020-02-20
CN113264921B (zh) 2024-09-13
ES2774249T3 (es) 2020-07-20
MX2016010572A (es) 2016-11-29
CN110522731A (zh) 2019-12-03
US9447076B2 (en) 2016-09-20
TR201809072T4 (tr) 2018-07-23
KR102413704B1 (ko) 2022-06-24
US20210179584A1 (en) 2021-06-17
CN106573914B (zh) 2021-05-28
TWI664967B (zh) 2019-07-11
JP2020015743A (ja) 2020-01-30
US20170182039A1 (en) 2017-06-29
US11142515B2 (en) 2021-10-12
EP3357919B1 (en) 2019-11-20
EA201691625A1 (ru) 2017-01-30
BR112016015838B1 (pt) 2023-05-09
ES2677595T3 (es) 2018-08-03
EP3357919A1 (en) 2018-08-08
US10294216B2 (en) 2019-05-21
TW201620518A (zh) 2016-06-16
CN106164067B (zh) 2019-09-10
DK3357919T3 (da) 2020-02-17
TW201620895A (zh) 2016-06-16
AU2019204525A1 (en) 2019-07-18
CA2938924C (en) 2023-01-31
CA2938924A1 (en) 2015-08-20
MX2016010571A (es) 2017-01-05
US10045980B2 (en) 2018-08-14
TWI751099B (zh) 2022-01-01
JP6952085B2 (ja) 2021-10-20
US9624196B2 (en) 2017-04-18
HK1259444A1 (en) 2019-11-29
AU2015216957B2 (en) 2019-04-04

Similar Documents

Publication Publication Date Title
JP6952085B2 (ja) キナーゼ阻害剤としてのピラゾリル尿素
JP2017502033A (ja) キナーゼインヒビターとして有用な尿素誘導体
JP2016515606A (ja) キナーゼ阻害剤として有用な尿素誘導体
HK40051658A (en) Pyrazolyl-ureas as kinase inhibitors
HK40051658B (zh) 作为激酶抑制剂的吡唑基-脲
HK1232532B (en) Pyrazolyl-ureas as kinase inhibitors
HK1232532A1 (en) Pyrazolyl-ureas as kinase inhibitors
CA2939355C (en) Substituted 1-pyrazolyl-3-naphthyl-urea compound with anti-inflammatory properties
HK1232533B (en) Aromatic heterocyclic compounds as antiinflammatory compounds
HK1232533A1 (en) Aromatic heterocyclic compounds as antiinflammatory compounds

Legal Events

Date Code Title Description
A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20170726

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180207

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180207

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180919

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20180920

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20181218

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20190219

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190319

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190322

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20190807

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190906

R150 Certificate of patent or registration of utility model

Ref document number: 6586098

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250