BRPI0919873B8 - compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas - Google Patents

compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas

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Publication number
BRPI0919873B8
BRPI0919873B8 BRPI0919873A BRPI0919873A BRPI0919873B8 BR PI0919873 B8 BRPI0919873 B8 BR PI0919873B8 BR PI0919873 A BRPI0919873 A BR PI0919873A BR PI0919873 A BRPI0919873 A BR PI0919873A BR PI0919873 B8 BRPI0919873 B8 BR PI0919873B8
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Brazil
Prior art keywords
pharmaceutical compositions
kinase inhibitors
pyrimidine compounds
preparation processes
substituted pyrazol
Prior art date
Application number
BRPI0919873A
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English (en)
Inventor
Zhang Gan
Haas Julia
W Andrews Steven
Jiang Yutong
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Array Biopharma Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41328903&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0919873(B8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of BRPI0919873A2 publication Critical patent/BRPI0919873A2/pt
Publication of BRPI0919873B1 publication Critical patent/BRPI0919873B1/pt
Publication of BRPI0919873B8 publication Critical patent/BRPI0919873B8/pt

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C07D519/02Ergot alkaloids of the cyclic peptide type
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

compostos de pirazol[1,5-a]pirimidina substituídos, composição farmacêutica compreendendo os referidos compostos, e processo para a preparação dos mesmos. compostos de fórmula i: no qual r1, r2, r3, r4, x, y e n tem o significado dado na especificação, são inibidores de quinases trk e são úteis no tratamento das doenças que podem ser tratados com um inibidor de quinase trk.
BRPI0919873A 2008-10-22 2009-10-21 compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas BRPI0919873B8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10761608P 2008-10-22 2008-10-22
PCT/US2009/061519 WO2010048314A1 (en) 2008-10-22 2009-10-21 SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS

Publications (3)

Publication Number Publication Date
BRPI0919873A2 BRPI0919873A2 (pt) 2019-02-05
BRPI0919873B1 BRPI0919873B1 (pt) 2020-04-14
BRPI0919873B8 true BRPI0919873B8 (pt) 2021-05-25

Family

ID=41328903

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0919873A BRPI0919873B8 (pt) 2008-10-22 2009-10-21 compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas

Country Status (38)

Country Link
US (11) US8513263B2 (pt)
EP (4) EP2350071B1 (pt)
JP (5) JP5600111B2 (pt)
KR (5) KR101652189B1 (pt)
CN (2) CN102264736B (pt)
AR (2) AR074052A1 (pt)
AU (1) AU2009308465B2 (pt)
BR (1) BRPI0919873B8 (pt)
CA (1) CA2741313C (pt)
CL (1) CL2011000880A1 (pt)
CO (1) CO6440551A2 (pt)
CR (1) CR20110261A (pt)
CY (4) CY1118199T1 (pt)
DK (4) DK3372605T3 (pt)
ES (4) ES2456346T3 (pt)
HR (3) HRP20140309T1 (pt)
HU (4) HUE030413T2 (pt)
IL (3) IL212341A0 (pt)
LT (4) LT3372605T (pt)
LU (1) LUC00150I2 (pt)
ME (1) ME03010B (pt)
MX (1) MX2011004204A (pt)
MY (1) MY169791A (pt)
NL (1) NL301033I2 (pt)
NO (2) NO3106463T3 (pt)
NZ (1) NZ592809A (pt)
PL (4) PL2725028T3 (pt)
PT (4) PT3106463T (pt)
RS (3) RS53247B (pt)
RU (1) RU2018131134A (pt)
SG (3) SG10201900514RA (pt)
SI (4) SI2350071T1 (pt)
SM (2) SMT201800244T1 (pt)
TR (1) TR201807039T4 (pt)
TW (4) TWI577680B (pt)
UA (1) UA106054C2 (pt)
UY (1) UY32192A (pt)
WO (1) WO2010048314A1 (pt)

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