[go: up one dir, main page]

PE20180508A1 - Amidas heterociclicas como inhibidores de quinasa - Google Patents

Amidas heterociclicas como inhibidores de quinasa

Info

Publication number
PE20180508A1
PE20180508A1 PE2017002383A PE2017002383A PE20180508A1 PE 20180508 A1 PE20180508 A1 PE 20180508A1 PE 2017002383 A PE2017002383 A PE 2017002383A PE 2017002383 A PE2017002383 A PE 2017002383A PE 20180508 A1 PE20180508 A1 PE 20180508A1
Authority
PE
Peru
Prior art keywords
phenyl
heterocyclic amides
kinase inhibitors
fluoropyridin
methanone
Prior art date
Application number
PE2017002383A
Other languages
English (en)
Inventor
Niall Andrew Anderson
Deepak Bandyopadhyay
Alain Claude-Marie Daugan
Frederic G Donche
Patrick M Eidam
Nicolas Eric Faucher
Nicolas S George
Philip Anthony Harris
Jae U Jeong
Bryan W King
Clark A Sehon
Gemma Victoria White
David Duff Wisnoski
Original Assignee
Glaxosmithkline Ip Dev Ltd
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 Glaxosmithkline Ip Dev Ltd filed Critical Glaxosmithkline Ip Dev Ltd
Publication of PE20180508A1 publication Critical patent/PE20180508A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (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)

Abstract

Se refiere a amidas heterociclicas de formula I, en donde R1 es alcoxi (C1-C4)-CH2-, fenil-alcoxi(C1-C4)-CH2-, entre otros; R2 es un grupo fenilo, cicloalquilo(C3-C6), entre otros; R3 es H o halogeno Tiene como compuesto preferidos: (5-(5-fluoropiridin-3-il)-4,5-dihidro-1H-pirazol-1-il)(1-(5-metilpirimidin-2-il)piperidin-4-il)metanona; (1-(5-fluoropiridin-2-il)piperidin-4-il)(5-fenil-4,5-dihidro-1H-pirazol-1-il)metanona, entre otros. La presente invencion es util para el tratamiento de enfermedades mediadas por la quinasa RIP1, ejemplos de estan enfermedades son la necrosis programada, psoriasis, dermatitis atopica, entre otras
PE2017002383A 2015-05-19 2016-05-19 Amidas heterociclicas como inhibidores de quinasa PE20180508A1 (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
PE20180508A1 true PE20180508A1 (es) 2018-03-09

Family

ID=56080431

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017002383A PE20180508A1 (es) 2015-05-19 2016-05-19 Amidas heterociclicas como inhibidores de quinasa

Country Status (35)

Country Link
US (4) US10590085B2 (es)
EP (1) EP3298002B1 (es)
JP (3) JP6700311B2 (es)
KR (1) KR20180004733A (es)
CN (2) CN112370452A (es)
AU (2) AU2016263156B2 (es)
CA (1) CA2986102C (es)
CL (1) CL2017002908A1 (es)
CO (1) CO2017011754A2 (es)
CR (1) CR20170524A (es)
CY (1) CY1124187T1 (es)
DK (1) DK3298002T3 (es)
DO (1) DOP2017000267A (es)
EA (1) EA036452B1 (es)
ES (1) ES2848398T3 (es)
HR (1) HRP20210300T1 (es)
HU (1) HUE053564T2 (es)
IL (1) IL255246A0 (es)
LT (1) LT3298002T (es)
MA (1) MA42109B1 (es)
MX (1) MX383935B (es)
MY (1) MY192059A (es)
NZ (1) NZ736665A (es)
PE (1) PE20180508A1 (es)
PH (1) PH12017502090A1 (es)
PL (1) PL3298002T3 (es)
PT (1) PT3298002T (es)
RS (1) RS61568B1 (es)
SG (1) SG11201708707UA (es)
SI (1) SI3298002T1 (es)
SM (1) SMT202100101T1 (es)
TW (1) TWI730959B (es)
UY (1) UY36680A (es)
WO (1) WO2016185423A1 (es)
ZA (1) ZA201707176B (es)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104788328B (zh) 2004-06-24 2017-09-12 沃泰克斯药物股份有限公司 Atp‑结合弹夹转运蛋白的调控剂
DK2774925T3 (en) 2005-11-08 2017-02-27 Vertex Pharma Heterocyclic modulators of ATP binding cassette transporters
WO2007079139A2 (en) 2005-12-28 2007-07-12 Vertex Pharmaceuticals, Inc. Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
AU2008251504B2 (en) 2007-05-09 2013-07-18 Vertex Pharmaceuticals Incorporated Modulators of CFTR
EP2639222B1 (en) 2007-12-07 2016-08-31 Vertex Pharmaceuticals Incorporated Process for producing cycloalkylcarboxiamido-pyridine benzoic acids
LT2225230T (lt) 2007-12-07 2017-01-25 Vertex Pharmaceuticals Incorporated 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il) benzoinės rūgšties kietos formos
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
SG10201504084QA (en) 2009-03-20 2015-06-29 Vertex Pharma 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
JP2015504920A (ja) 2012-01-25 2015-02-16 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の製剤
CN109966264A (zh) 2012-02-27 2019-07-05 沃泰克斯药物股份有限公司 药物组合物及其施用
KR102280372B1 (ko) 2013-11-12 2021-07-22 버텍스 파마슈티칼스 인코포레이티드 Cftr 매개된 질환 치료용 약제학적 조성물의 제조 방법
PL3221692T3 (pl) 2014-11-18 2021-12-06 Vertex Pharmaceuticals Inc. Sposób przeprowadzania testowania o wysokiej przepustowości za pomocą wysokosprawnej chromatografii cieczowej
KR102596723B1 (ko) 2014-12-24 2023-11-01 내셔널 인스티튜트 오브 바이올로지칼 사이언시스, 베이징 괴사 억제제
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
EP3585782A1 (en) 2017-02-27 2020-01-01 GlaxoSmithKline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
TWI794232B (zh) * 2017-05-17 2023-03-01 美商戴納立製藥公司 激酶抑制劑及其用途
CR20200168A (es) 2017-10-31 2020-07-12 Hoffmann La Roche Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos
WO2019224774A1 (en) * 2018-05-23 2019-11-28 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors
WO2019224773A1 (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
WO2020146615A1 (en) * 2019-01-11 2020-07-16 Genentech, Inc. Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof
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
EP3967682A4 (en) * 2019-05-09 2023-01-11 Genfleet Therapeutics (Shanghai) Inc. BISHETEROCYCLIC CARBONYL-SUBSTITUTED DIHYDROPYRAZOLE COMPOUND, PROCESS FOR PRODUCTION THEREOF AND PHARMACEUTICAL USE THEREOF
US20230192618A1 (en) * 2019-05-22 2023-06-22 Agios Pharmaceuticals, Inc. Crystalline salt forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide
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
BR112022010082A2 (pt) 2019-11-26 2022-08-30 Univ Texas Composto de fórmula estrutural i ou sal do mesmo, composição farmacêutica, uso do composto e uso da composição farmacêutica
US20230192662A1 (en) * 2020-05-20 2023-06-22 Sironax Ltd. Receptor-Interacting Protein 1 Inhibitors Including Piperazine Heterocyclic Amide Ureas
BR112022023506A2 (pt) * 2020-05-20 2022-12-20 Sironax Ltd Composto, composição farmacêutica, uso do composto e método de uso de um composto
EP4153582A4 (en) 2020-05-20 2024-06-19 Sironax Ltd. PIPERAZINE-TYPE CYCLIC UREAS
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
WO2022194259A1 (en) * 2021-03-18 2022-09-22 Sironax Ltd. Receptor-interacting protein 1 inhibitors, preparations, and uses thereof
JP2024517504A (ja) * 2021-05-20 2024-04-22 シロナックス リミテッド． アゼチジン環状尿素を含めたｒｉｐ１調節物質、その調製、及び使用
EP4301744A1 (en) 2021-08-10 2024-01-10 AbbVie Inc. Nicotinamide ripk1 inhibitors
WO2023083847A1 (en) 2021-11-11 2023-05-19 Sanofi Isoxazolidines as ripk1 inhibitors and use thereof
CN116496256B (zh) * 2022-01-04 2025-03-28 北京赛特明强医药科技有限公司 羰基桥连杂环类化合物、及其组合物与应用
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
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
WO2024233547A1 (en) 2023-05-10 2024-11-14 Genzyme Corporation Isoxazolidines as ripk1 inhibitors and use thereof
CN121127467A (zh) 2023-05-10 2025-12-12 建新公司 作为ripk1抑制剂的异噁唑烷及其用途

Family Cites Families (17)

* 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
HU199825B (en) * 1987-06-17 1990-03-28 Mitsui Toatsu Chemicals Process for production of new derivatives of pirasoline and medical compositions containing them
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.
US20070161633A1 (en) 2003-05-02 2007-07-12 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
AR052660A1 (es) 2005-01-21 2007-03-28 Astex Therapeutics Ltd Derivados de pirazol para inhibir la cdk's y gsk's
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
AU2009329879A1 (en) * 2008-12-23 2011-08-11 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
EP2619182B1 (en) 2010-09-21 2016-11-09 Eisai R&D Management Co., Ltd. Pharmaceutical composition
US9643977B2 (en) * 2011-03-11 2017-05-09 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
TWI648274B (zh) 2013-02-15 2019-01-21 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類 （二）
KR102596723B1 (ko) * 2014-12-24 2023-11-01 내셔널 인스티튜트 오브 바이올로지칼 사이언시스, 베이징 괴사 억제제
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
EP3585782A1 (en) 2017-02-27 2020-01-01 GlaxoSmithKline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors

Also Published As

Publication number Publication date
CO2017011754A2 (es) 2018-02-09
MA42109A (fr) 2018-03-28
KR20180004733A (ko) 2018-01-12
JP2021138731A (ja) 2021-09-16
US10590085B2 (en) 2020-03-17
IL255246A0 (en) 2017-12-31
US20210253532A1 (en) 2021-08-19
MY192059A (en) 2022-07-25
NZ736665A (en) 2024-10-25
RS61568B1 (sr) 2021-04-29
MA42109B1 (fr) 2021-03-31
CL2017002908A1 (es) 2018-04-20
AU2016263156B2 (en) 2018-12-06
CN112370452A (zh) 2021-02-19
AU2019201480B2 (en) 2020-06-11
HUE053564T2 (hu) 2021-07-28
TWI730959B (zh) 2021-06-21
AU2016263156A1 (en) 2017-11-16
US11485710B2 (en) 2022-11-01
CA2986102A1 (en) 2016-11-24
PT3298002T (pt) 2020-12-28
ZA201707176B (en) 2019-05-29
JP6700311B2 (ja) 2020-05-27
US20200165205A1 (en) 2020-05-28
SMT202100101T1 (it) 2021-03-15
BR112017024941A2 (pt) 2018-07-31
EA036452B1 (ru) 2020-11-12
PL3298002T3 (pl) 2021-06-14
DK3298002T3 (da) 2021-02-15
HRP20210300T1 (hr) 2021-04-02
MX383935B (es) 2025-03-14
ES2848398T3 (es) 2021-08-09
JP7204821B2 (ja) 2023-01-16
MX2017014809A (es) 2018-02-09
SI3298002T1 (sl) 2021-04-30
AU2019201480A1 (en) 2019-03-28
CA2986102C (en) 2024-01-02
UY36680A (es) 2016-12-30
JP2018515555A (ja) 2018-06-14
SG11201708707UA (en) 2017-12-28
DOP2017000267A (es) 2018-01-31
AU2019201480C1 (en) 2021-11-25
CR20170524A (es) 2018-01-22
CN107624111A (zh) 2018-01-23
CY1124187T1 (el) 2022-05-27
US20180134665A1 (en) 2018-05-17
US20230120185A1 (en) 2023-04-20
LT3298002T (lt) 2021-01-11
JP2020143079A (ja) 2020-09-10
US10899716B2 (en) 2021-01-26
EA201792535A1 (ru) 2018-10-31
WO2016185423A1 (en) 2016-11-24
PH12017502090A1 (en) 2018-05-07
EP3298002A1 (en) 2018-03-28
CN107624111B (zh) 2020-11-03
HK1245244A1 (en) 2018-08-24
JP6893271B2 (ja) 2021-06-23
EP3298002B1 (en) 2020-12-16
TW201718508A (zh) 2017-06-01

Similar Documents

Publication Publication Date Title
PE20180508A1 (es) Amidas heterociclicas como inhibidores de quinasa
PE20181074A1 (es) Compuestos heteroaromaticos como inhibidores de btk
MX2018015563A (es) Acidos de carbamoiloximetil triazol ciclohexilo como antagonistas de acido lisofosfatidico (lpa).
CO2019006622A2 (es) Derivados de pirazol como inhibidores de malt1
MX2022009998A (es) Formas cristalinas de la n-(4-(4-(ciclopropilmetil)piperazin-1- carbonil)fenil)quinolin-8-sulfonamida.
CO2018007738A2 (es) Derivados de tiohidantoína sustituidos como antagonistas del receptor de andrógenos
PE20180024A1 (es) Triazolopirazinonas como inhibidores de pde1
CO2017002714A2 (es) Ácido 4-(3-fluoro-3-(2-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)etil)pirrolidin-1-il)-3-(3-(2-metoxietoxi)fenil)butanoico, o una sal del mismo
CO2017006230A2 (es) Compuestos de n-((het)arilmetil)-heteroaril-carboxamidas como inhibidores de calicreína plasmática
CU20200080A7 (es) Kit que comprende un inhibidor de lats para el suministro ocular
CU24389B1 (es) Compuestos de heterociclilo bicíclico como inhibidores de irak4
PE20161225A1 (es) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
PH12017500416A1 (en) Compounds and compositions as raf kinase inhibitors
CL2016002382A1 (es) Derivados de quinoxalina útiles como moduladores de fgfr quinasa
EA201890594A1 (ru) Арильные, гетероарильные и гетероциклические соединения для лечения заболеваний
PE20181078A1 (es) Derivados de 8-[6-[3-(amino) propoxi]-3-piridil]1-isopropilimidazo[4,5-c]quinolin-2-ona como moduladores selectivos de la cinasa de la ataxia telangiectasia mutada (atm) para el tratamiento del cancer
EA201691872A1 (ru) Гетероциклические соединения для применения в лечении pi3k-гамма-опосредованных расстройств
UY35998A (es) 1-(3-(tert-BUTIL)1-(p-TOLIL)-1H-PIRAZOL-5-IL)-3-(4-((2-((6-ETILPIRAZIN-2-IL)AMINO)PIRIDIN-4-IL)METOXI)NAFTALEN-1-IL) UREA Y SUS SALES DERIVADAS FARMACÉUTICAMENTE ACEPTABLES, COMO INHIBIDORES DE P38 M AP QUINASA
EA201690713A1 (ru) Гетероциклические соединения и их применения
BR112018001017A2 (pt) inibidores do receptor de fator-1 de estimulação de colônia (csf-1r)
EA201790395A1 (ru) Производные аминотриазина, подходящие для применения в качестве соединений-ингибиторов tank-связывающей киназы
EA201600589A1 (ru) Ингибиторы диацилглицеринацилтрансферазы 2 для применения в лечении метаболических и связанных с метаболизмом расстройств
MX2019006893A (es) Inhibidores heterociclicos de mct4.
MX373234B (es) Derivados de 2,4-tiazolidindiona en el tratamiento de trastornos del sistema nervioso central.
PE20170947A1 (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1