EA036452B1 - Гетероциклические амиды в качестве ингибиторов киназ - Google Patents

Гетероциклические амиды в качестве ингибиторов киназ Download PDF

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Publication number
EA036452B1
EA036452B1 EA201792535A EA201792535A EA036452B1 EA 036452 B1 EA036452 B1 EA 036452B1 EA 201792535 A EA201792535 A EA 201792535A EA 201792535 A EA201792535 A EA 201792535A EA 036452 B1 EA036452 B1 EA 036452B1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
substituted
phenyl
membered heteroaryl
optionally substituted
Prior art date
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EA201792535A
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English (en)
Russian (ru)
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EA201792535A1 (ru
Inventor
Нилл Эндрю Андерсон
Дипак Бандиопадхиаи
Ален Клод-Мари Доган
Фредерик Ж. Донш
Патрик М. Эйдам
Николя Эрик Фоше
Николя С. Жорж
Филип Энтони Харрис
Дзае У. Дзеонг
Брайан У. Кинг
Кларк А. Сехон
Джемма Виктория Уайт
Дэвид Дафф Висноски
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Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед
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Publication of EA201792535A1 publication Critical patent/EA201792535A1/ru
Publication of EA036452B1 publication Critical patent/EA036452B1/ru

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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/435—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • C07D401/02—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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
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    • 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
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
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    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
EA201792535A 2015-05-19 2016-05-19 Гетероциклические амиды в качестве ингибиторов киназ EA036452B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562163552P 2015-05-19 2015-05-19
US201562167359P 2015-05-28 2015-05-28
US201562197602P 2015-07-28 2015-07-28
PCT/IB2016/052948 WO2016185423A1 (en) 2015-05-19 2016-05-19 Heterocyclic amides as kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201792535A1 EA201792535A1 (ru) 2018-10-31
EA036452B1 true EA036452B1 (ru) 2020-11-12

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EA201792535A EA036452B1 (ru) 2015-05-19 2016-05-19 Гетероциклические амиды в качестве ингибиторов киназ

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US (4) US10590085B2 (enExample)
EP (1) EP3298002B1 (enExample)
JP (3) JP6700311B2 (enExample)
KR (1) KR20180004733A (enExample)
CN (2) CN112370452A (enExample)
AU (2) AU2016263156B2 (enExample)
CA (1) CA2986102C (enExample)
CL (1) CL2017002908A1 (enExample)
CO (1) CO2017011754A2 (enExample)
CR (1) CR20170524A (enExample)
CY (1) CY1124187T1 (enExample)
DK (1) DK3298002T3 (enExample)
DO (1) DOP2017000267A (enExample)
EA (1) EA036452B1 (enExample)
ES (1) ES2848398T3 (enExample)
HR (1) HRP20210300T1 (enExample)
HU (1) HUE053564T2 (enExample)
IL (1) IL255246A0 (enExample)
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MA (1) MA42109B1 (enExample)
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MY (1) MY192059A (enExample)
NZ (1) NZ736665A (enExample)
PE (1) PE20180508A1 (enExample)
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Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006002421A2 (en) 2004-06-24 2006-01-05 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
SI1945632T1 (sl) 2005-11-08 2014-03-31 Vertex Pharmaceuticals Incorporated Heterocikliäśni modulatorji za prenaĺ alce z atp-vezavno kaseto
AU2006332726B2 (en) 2005-12-28 2012-12-13 Vertex Pharmaceuticals Incorporated. Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
NZ581259A (en) 2007-05-09 2012-07-27 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
SI2639224T1 (sl) 2007-12-07 2016-12-30 Vertex Pharmaceuticals Incorporated Postopek za pripravo cikloalkilkarboksiamido-piridinskih benzojskih kislin
AU2008333845C1 (en) 2007-12-07 2014-01-16 Vertex Pharmaceuticals Incorporated Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
CN102245573B (zh) 2008-02-28 2013-11-20 沃泰克斯药物股份有限公司 作为cftr调节剂的杂芳基衍生物
US12458635B2 (en) 2008-08-13 2025-11-04 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
AU2010226400B2 (en) 2009-03-20 2016-07-14 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
LT3150198T (lt) 2010-04-07 2021-12-10 Vertex Pharmaceuticals Incorporated 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il)benzoinės rūgšties farmacinė kompozicija ir jos įvedimas
CA2865519C (en) 2012-02-27 2018-01-02 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions comprising a solid dispersion of n-[2,4-bis(1,1-dimethylethyl0-5-hydroxyphenyl-1]-1,4-dihydro-4-oxoquinolone-3-carboxamide for treating cystic fibrosis
BR112016010403A2 (pt) 2013-11-12 2017-08-08 Vertex Pharma Processo de preparação de composições farmacêuticas para o tratamento de doenças mediadas por cftr
CA2968130C (en) 2014-11-18 2022-08-16 Vertex Pharmaceuticals Incorporated Process of conducting high throughput testing high performance liquid chromatography
EP3224245B1 (en) 2014-12-24 2018-09-12 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
TWI730959B (zh) 2015-05-19 2021-06-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺
TW201831464A (zh) * 2016-11-18 2018-09-01 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺
JP2020509009A (ja) 2017-02-27 2020-03-26 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ キナーゼ阻害剤としての複素環式アミド
CA3063934A1 (en) * 2017-05-17 2018-11-22 Denali Therapeutics Inc. Kinase inhibitors and uses thereof
WO2019086494A1 (en) 2017-10-31 2019-05-09 F. Hoffmann-La Roche Ag Bicyclic sulfones and sulfoxides and methods of use thereof
WO2019224773A1 (en) * 2018-05-23 2019-11-28 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors
WO2019224774A1 (en) * 2018-05-23 2019-11-28 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors
WO2020044206A1 (en) 2018-08-29 2020-03-05 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors for use in the treatment cancer
TW202043229A (zh) 2019-01-11 2020-12-01 瑞士商赫孚孟拉羅股份公司 雙環酮化合物及其使用方法
CN109912574A (zh) * 2019-05-06 2019-06-21 合肥工业大学 一种二氢吡唑类化合物及其制备方法和用途
JP7367062B2 (ja) * 2019-05-09 2023-10-23 ▲勁▼方医▲薬▼科技（上海）有限公司 ビス複素環式カルボニル置換ジヒドロピラゾール化合物、その調製方法、及びその医薬的使用
MX2021014228A (es) * 2019-05-22 2022-02-21 Agios Pharmaceuticals Inc Formas cristalinas de sal de n-(4-(4 (ciclopropilmetil)piperazin 1- carbonil)fenil)quinolin-8-sulfonamida.
US11718612B2 (en) 2019-09-06 2023-08-08 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase I for the treatment of disease
IL291665B2 (en) 2019-09-27 2025-07-01 Univ Texas Inhibitors of receptor interacting protein kinase i for the treatment of disease
CA3162605A1 (en) 2019-11-26 2021-06-03 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase i for the treatment of disease
JP7764398B2 (ja) * 2020-05-20 2025-11-05 シロナックス リミテッド． アゼチジン環状尿素類
US20230192662A1 (en) * 2020-05-20 2023-06-22 Sironax Ltd. Receptor-Interacting Protein 1 Inhibitors Including Piperazine Heterocyclic Amide Ureas
IL298188A (en) 2020-05-20 2023-01-01 Sironax Ltd Circular structures of piperazine
TW202214617A (zh) 2020-06-02 2022-04-16 法商賽諾菲公司 作為ｒｉｐｋ１抑制劑之異㗁唑啶及其用途
EP4341247A4 (en) * 2021-05-20 2025-07-02 Sironax Ltd RIP1 MODULATORS COMPRISING CYCLIC AZETIDINE UREAS, PREPARATIONS AND USES THEREOF
JP7406672B2 (ja) 2021-08-10 2023-12-27 アッヴィ・インコーポレイテッド ニコチンアミド系ｒｉｐｋ１阻害剤
AU2022388696A1 (en) 2021-11-11 2024-06-27 Genzyme Corporation Isoxazolidines as ripk1 inhibitors and use thereof
KR20240131425A (ko) * 2022-01-04 2024-08-30 베이징 사이텍-엠큐 파마슈티컬즈 리미티드 카르보닐 가교된 헤테로시클릭 화합물, 및 이의 조성물 및 적용
US11816144B2 (en) * 2022-03-31 2023-11-14 Pinterest, Inc. Hair pattern determination and filtering
CN115326999B (zh) * 2022-10-12 2022-12-27 深圳市海滨制药有限公司 一种奥司他韦环氧中间体及其异构体的检测方法
WO2024233547A1 (en) 2023-05-10 2024-11-14 Genzyme Corporation Isoxazolidines as ripk1 inhibitors and use thereof
CN121079291A (zh) 2023-05-10 2025-12-05 建新公司 作为ripk1抑制剂的异噁唑烷及其使用
WO2024233544A1 (en) 2023-05-10 2024-11-14 Genzyme Corporation Isoxazolidines as ripk1 inhibitors and use thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0295695A2 (en) * 1987-06-17 1988-12-21 MITSUI TOATSU CHEMICALS, Inc. Pyrazoline derivatives and agents for treating cerebrovascular diseases containing the same as active ingredient
WO2014125444A1 (en) * 2013-02-15 2014-08-21 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH062742B2 (ja) * 1987-06-17 1994-01-12 三井東圧化学株式会社 新規２‐ピラゾリン類及びそれを有効成分とする脳血管障害治療剤
US4895947A (en) 1987-12-17 1990-01-23 Mitsui Toatsu Chemicals, Inc. Process for producing 1-acyl-2-pyrazoline derivative
CL2004000366A1 (es) 2003-02-26 2005-01-07 Pharmacia Corp Sa Organizada B USO DE UNA COMBINACION DE UN COMPUESTO DERIVADO DE PIRAZOL INHIBIDOR DE QUINASA p38, Y UN INHIBIDOR DE ACE PARA TRATAR DISFUNCION RENAL, ENFERMEDAD CARDIOVASCULAR Y VASCULAR, RETINOPATIA, NEUROPATIA, EDEMA, DISFUNCION ENDOTELIAL O INSULINOPATIA.
CA2524274A1 (en) 2003-05-02 2004-11-18 Elan Pharmaceuticals, Inc. 4-bromo-5-(2-chloro-benzoylamino)-1h-pyrazole-3-carboxylic acid (1-(aminocarbonyl)eth-1-yl) amide derivatives and related compounds as bradykinin b1 receptor antagonists for the treatment of inflammatory diseases
AR052559A1 (es) 2005-01-21 2007-03-21 Astex Therapeutics Ltd Derivados de pirazol para inhibir cdk's y gsk's
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
CA2772760A1 (en) * 2008-12-23 2010-07-01 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
KR101911105B1 (ko) 2010-09-21 2018-10-23 에자이 알앤드디 매니지먼트 가부시키가이샤 제약 조성물
WO2012125544A2 (en) * 2011-03-11 2012-09-20 President And Fellows Of Harvard College Necroptosis inhibitors and methods of use therefor
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
EP3224245B1 (en) * 2014-12-24 2018-09-12 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
TWI730959B (zh) 2015-05-19 2021-06-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺
CN108602809B (zh) 2015-12-04 2022-09-30 戴纳立制药公司 异噁唑烷衍生的受体相互作用蛋白激酶1(ripk 1)的抑制剂
TW201831464A (zh) 2016-11-18 2018-09-01 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺
JP2020509009A (ja) 2017-02-27 2020-03-26 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ キナーゼ阻害剤としての複素環式アミド

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0295695A2 (en) * 1987-06-17 1988-12-21 MITSUI TOATSU CHEMICALS, Inc. Pyrazoline derivatives and agents for treating cerebrovascular diseases containing the same as active ingredient
WO2014125444A1 (en) * 2013-02-15 2014-08-21 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
LIU, XIN-HUA: "Synthesis and biological activity of arylpyrazole derivatives", HECHENG HUAXUE / CHINESE JOURNAL OF SYNTHETIC CHEMISTRY, CHENGDU YUJI HUAXUESUO, CN, vol. 15, no. 2, 1 January 2007 (2007-01-01), CN, pages 212 - 215, XP008180688, ISSN: 1005-1511 *
LIU, XIN-HUA; ZHU, JING; PAN, CHUN-XIU; SONG, BAO-AN: "Synthesis and fungicidal activity of novel 5-arylpyrazole derivatives", CHINESE JOURNAL OF APPLIED CHEMISTRY - YINGYONG HUAXUE, KEXUE CHUBANSHE, CN, vol. 24, no. 10, 1 January 2007 (2007-01-01), CN, pages 1162 - 1166, XP008180689, ISSN: 1000-0518 *
WANG YANG; CHENG FEI XIONG; YUAN XIAO LONG; TANG WEN JIAN; SHI JING BO; LIAO CHEN ZHONG; LIU XIN HUA: "Dihydropyrazole derivatives as telomerase inhibitors: Structure-based design, synthesis, SAR and anticancer evaluationin vitroandin vivo", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 112, 6 February 2016 (2016-02-06), NL, pages 231 - 251, XP029450402, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2016.02.009 *
XIAO XUAN; NI YONG; JIA YING-MING; ZHENG MIN; XU HAN-FEI; XU JUN; LIAO CHENZHONG: "Identification of human telomerase inhibitors having the core ofN-acyl-4,5-dihydropyrazole with anticancer effects", BIORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM , NL, vol. 26, no. 6, 10 February 2016 (2016-02-10), Amsterdam , NL, pages 1508 - 1511, XP029436559, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2016.02.025 *
XIN-HUA LIU; BAN-FENG RUAN; JING-XIN LIU; BAO-AN SONG; LING-HONG JING; JUN LI; YANG YANG; HAI-LIANG ZHU; XING-BAO QI;: "Design and synthesis of-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents", BIORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM , NL, vol. 21, no. 10, 23 March 2011 (2011-03-23), Amsterdam , NL, pages 2916 - 2920, XP028208748, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2011.03.066 *

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