BR112012020273A8 - compostos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno e pirazolotiazol como pontencializadores alostéricos de mglur4, composições e métodos de tratamento de disfunção neurológica - Google Patents

compostos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno e pirazolotiazol como pontencializadores alostéricos de mglur4, composições e métodos de tratamento de disfunção neurológica

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Publication number
BR112012020273A8
BR112012020273A8 BR112012020273A BR112012020273A BR112012020273A8 BR 112012020273 A8 BR112012020273 A8 BR 112012020273A8 BR 112012020273 A BR112012020273 A BR 112012020273A BR 112012020273 A BR112012020273 A BR 112012020273A BR 112012020273 A8 BR112012020273 A8 BR 112012020273A8
Authority
BR
Brazil
Prior art keywords
pyrazolothiophene
pyrazolopyrazine
pyrazolopyridine
pyrazolopyrimidine
allosteric
Prior art date
Application number
BR112012020273A
Other languages
English (en)
Portuguese (pt)
Other versions
BR112012020273A2 (pt
Inventor
M Niswender Colleen
R Hopkins Corey
W Lindsley Craig
W Engers Darren
M Salovich James
Jeffrey Conn P
D Gogliotti Rocco
Cheung Yiu-Yin
Original Assignee
Univ Vanderbilt
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 Univ Vanderbilt filed Critical Univ Vanderbilt
Publication of BR112012020273A2 publication Critical patent/BR112012020273A2/pt
Publication of BR112012020273A8 publication Critical patent/BR112012020273A8/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/41—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
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • 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
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    • 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
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    • 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
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • 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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    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
BR112012020273A 2010-02-11 2011-02-11 compostos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno e pirazolotiazol como pontencializadores alostéricos de mglur4, composições e métodos de tratamento de disfunção neurológica BR112012020273A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30348110P 2010-02-11 2010-02-11
US201161430521P 2011-01-06 2011-01-06
PCT/US2011/024618 WO2011100607A1 (en) 2010-02-11 2011-02-11 Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction

Publications (2)

Publication Number Publication Date
BR112012020273A2 BR112012020273A2 (pt) 2017-08-29
BR112012020273A8 true BR112012020273A8 (pt) 2017-12-26

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US (2) US9163015B2 (enExample)
EP (1) EP2533639A4 (enExample)
JP (1) JP5883399B2 (enExample)
KR (1) KR20130029368A (enExample)
CN (1) CN102892288B (enExample)
AU (1) AU2011215638B2 (enExample)
BR (1) BR112012020273A8 (enExample)
CA (1) CA2789427A1 (enExample)
CL (1) CL2012002225A1 (enExample)
EA (1) EA201290774A1 (enExample)
IL (1) IL221390A0 (enExample)
MX (1) MX2012009378A (enExample)
PH (1) PH12012501621A1 (enExample)
SG (1) SG183263A1 (enExample)
TN (1) TN2012000400A1 (enExample)
WO (1) WO2011100607A1 (enExample)
ZA (1) ZA201206416B (enExample)

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JP2012516355A (ja) 2009-01-28 2012-07-19 ヴァンダービルト ユニバーシティー ｍＧＬｕＲ４アロステリック増強剤としての置換された１，１，３，３−テトラオキシドベンゾ［ｄ］［１，３，２］ジチアゾール、組成物、および神経機能不全を治療する方法
US8759377B2 (en) 2009-11-23 2014-06-24 Vanderbilt University Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
PH12012501621A1 (en) * 2010-02-11 2012-10-22 Univ Vanderbilt Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
EP2755976B1 (en) 2011-09-15 2018-07-18 Novartis AG 6-substituted 3-(quinolin-6-ylthio)-[1,2,4]triazolo[4,3-a]pyridines as c-met tyrosine kinase inhibitors
WO2013060029A1 (en) * 2011-10-28 2013-05-02 Merck Sharp & Dohme Corp Allosteric modulators of metabotropic glutamate receptors
EP2791108B1 (en) 2011-12-15 2016-07-27 Pfizer Limited Sulfonamide derivatives
EP2863912A4 (en) 2012-06-20 2015-11-04 Univ Vanderbilt SUBSTITUTED BICYCLIC ALKOXYPYRAZOL ANALOGUES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
AU2014211728B2 (en) * 2013-02-04 2018-05-17 Merck Patent Gmbh Spiro-quinazolinone derivatives useful for the treatment of neurological diseases and conditions
KR102211310B1 (ko) * 2013-05-10 2021-02-03 장쑤 한서 파마슈티칼 캄파니 리미티드 [1,2,4]트라이아졸[4,3-에이]피리딘 유도체, 그의 제조 방법 또는 그의 의학적 용도
MD4635C1 (ro) 2013-10-14 2020-01-31 Eisai R&D Management Co., Ltd. Compuşi de chinolină substituiţi selectiv
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US10221172B2 (en) 2015-01-13 2019-03-05 Vanderbilt University Benzothiazole and benzisothiazole-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US9980945B2 (en) 2015-01-13 2018-05-29 Vanderbilt University Benzoisoxazole-substituted compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
WO2016123629A1 (en) * 2015-01-30 2016-08-04 Vanderbilt University Indazole and azaindazole substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
WO2016123627A1 (en) * 2015-01-30 2016-08-04 Vanderbilt University Isoquiniline and napthalene-substituted compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction
WO2016172547A1 (en) * 2015-04-24 2016-10-27 Vanderbilt University Substituted imidazopyridine and triazolopyridine analogs as positive allosteric modulators of muscarinic acetylcholine receptor m1
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