CA2866143C - Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use - Google Patents

Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use Download PDF

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Publication number
CA2866143C
CA2866143C CA2866143A CA2866143A CA2866143C CA 2866143 C CA2866143 C CA 2866143C CA 2866143 A CA2866143 A CA 2866143A CA 2866143 A CA2866143 A CA 2866143A CA 2866143 C CA2866143 C CA 2866143C
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Prior art keywords
pyrimidin
pyrazolo
carboxylate
piperazine
methoxypyridin
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CA2866143A
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English (en)
French (fr)
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CA2866143A1 (en
Inventor
Yingzhi Bi
Kenneth Gordon Carson
Giovanni Cianchetta
Michael Alan Green
Godwin KUMI
Alan Main
Yulian Zhang
Glenn Gregory ZIPP
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Lexicon Pharmaceuticals Inc
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Lexicon Pharmaceuticals Inc
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Publication of CA2866143A1 publication Critical patent/CA2866143A1/en
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    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2866143A 2012-03-09 2013-03-05 Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use Active CA2866143C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261608765P 2012-03-09 2012-03-09
US61/608,765 2012-03-09
PCT/US2013/029056 WO2013134228A1 (en) 2012-03-09 2013-03-05 PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE

Publications (2)

Publication Number Publication Date
CA2866143A1 CA2866143A1 (en) 2013-09-12
CA2866143C true CA2866143C (en) 2020-08-04

Family

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CA2866143A Active CA2866143C (en) 2012-03-09 2013-03-05 Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use

Country Status (25)

Country Link
US (3) US8946415B2 (enExample)
EP (1) EP2834243B1 (enExample)
JP (1) JP6418950B2 (enExample)
KR (1) KR101965025B1 (enExample)
CN (1) CN104302649B (enExample)
AR (1) AR090292A1 (enExample)
AU (1) AU2013230128B2 (enExample)
BR (1) BR112014022000A8 (enExample)
CA (1) CA2866143C (enExample)
DK (1) DK2834243T3 (enExample)
ES (1) ES2676224T3 (enExample)
HU (1) HUE038786T2 (enExample)
IL (1) IL234486A (enExample)
IN (1) IN2014DN07384A (enExample)
MX (2) MX381849B (enExample)
NZ (1) NZ630721A (enExample)
PL (1) PL2834243T3 (enExample)
PT (1) PT2834243T (enExample)
RU (1) RU2014140735A (enExample)
SG (1) SG11201405561RA (enExample)
TR (1) TR201808280T4 (enExample)
TW (1) TW201341386A (enExample)
UY (1) UY34668A (enExample)
WO (1) WO2013134228A1 (enExample)
ZA (1) ZA201406149B (enExample)

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IL275059B2 (en) * 2017-12-15 2023-11-01 Pyramid Biosciences Inc 5-(2-(5,2-difluorophenyl)pyrrolidin-1-yl)-3-(1H-pyrazol-1-yl)pyrazolo[5,1-A]pyrimidine derivatives and related compounds as TRK kinase inhibitors for cancer therapy
RS63787B1 (sr) 2017-12-19 2022-12-30 Turning Point Therapeutics Inc Makrociklična jedinjenja za lečenje bolesti
CN109456331B (zh) 2017-12-22 2020-06-05 深圳市塔吉瑞生物医药有限公司 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途
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TW202028209A (zh) * 2018-09-27 2020-08-01 大陸商重慶複創醫藥研究有限公司 作為RET激酶抑制劑的取代的咪唑[1,2-a]吡啶和[1,2,4]三唑[1,5-a]吡啶化合物
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Also Published As

Publication number Publication date
SG11201405561RA (en) 2014-10-30
TW201341386A (zh) 2013-10-16
HUE038786T2 (hu) 2018-11-28
RU2014140735A (ru) 2016-04-27
EP2834243B1 (en) 2018-04-25
ZA201406149B (en) 2016-06-29
CA2866143A1 (en) 2013-09-12
JP2015509535A (ja) 2015-03-30
HK1201257A1 (en) 2015-08-28
WO2013134228A1 (en) 2013-09-12
US20130253194A1 (en) 2013-09-26
UY34668A (es) 2013-10-31
IN2014DN07384A (enExample) 2015-04-24
MX2014010589A (es) 2014-09-18
MX345830B (es) 2017-02-17
TR201808280T4 (tr) 2018-07-23
US9403832B2 (en) 2016-08-02
IL234486A (en) 2016-10-31
BR112014022000A2 (pt) 2017-06-20
US20150183792A1 (en) 2015-07-02
CN104302649B (zh) 2017-06-23
US8946415B2 (en) 2015-02-03
AU2013230128B2 (en) 2017-08-17
EP2834243A1 (en) 2015-02-11
US20170129896A1 (en) 2017-05-11
MX381849B (es) 2025-03-13
CN104302649A (zh) 2015-01-21
BR112014022000A8 (pt) 2021-06-15
KR101965025B1 (ko) 2019-04-02
PT2834243T (pt) 2018-08-01
ES2676224T3 (es) 2018-07-17
NZ630721A (en) 2016-12-23
PL2834243T3 (pl) 2018-09-28
AU2013230128A1 (en) 2014-09-25
DK2834243T3 (en) 2018-07-23
JP6418950B2 (ja) 2018-11-07
KR20140138864A (ko) 2014-12-04
AR090292A1 (es) 2014-11-05

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