TN2012000400A1 - Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction - Google Patents

Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction

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Publication number
TN2012000400A1
TN2012000400A1 TNP2012000400A TN2012000400A TN2012000400A1 TN 2012000400 A1 TN2012000400 A1 TN 2012000400A1 TN P2012000400 A TNP2012000400 A TN P2012000400A TN 2012000400 A TN2012000400 A TN 2012000400A TN 2012000400 A1 TN2012000400 A1 TN 2012000400A1
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TN
Tunisia
Prior art keywords
compounds
methods
pyrazolothiophene
pyrazolopyrazine
pyrazolopyridine
Prior art date
Application number
TNP2012000400A
Other languages
English (en)
Inventor
P Jeffrey Conn
Craig W Lindsley
Corey R Hopkins
Colleen M Niswender
Rocco D Gogliotti
James M Salovich
Darren W Engers
Yiu-Yin Cheung
Original Assignee
Univ Vanderbilt
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Filing date
Publication date
Application filed by Univ Vanderbilt filed Critical Univ Vanderbilt
Publication of TN2012000400A1 publication Critical patent/TN2012000400A1/en

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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
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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
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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
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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
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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
    • A61K31/519—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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    • 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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  • General Chemical & Material Sciences (AREA)
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  • Neurology (AREA)
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  • Psychiatry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
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  • Endocrinology (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)
TNP2012000400A 2010-02-11 2012-08-09 Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction TN2012000400A1 (en)

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

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TN2012000400A1 true TN2012000400A1 (en) 2014-01-30

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TNP2012000400A TN2012000400A1 (en) 2010-02-11 2012-08-09 Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction

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Country Link
US (2) US9163015B2 (cg-RX-API-DMAC7.html)
EP (1) EP2533639A4 (cg-RX-API-DMAC7.html)
JP (1) JP5883399B2 (cg-RX-API-DMAC7.html)
KR (1) KR20130029368A (cg-RX-API-DMAC7.html)
CN (1) CN102892288B (cg-RX-API-DMAC7.html)
AU (1) AU2011215638B2 (cg-RX-API-DMAC7.html)
BR (1) BR112012020273A8 (cg-RX-API-DMAC7.html)
CA (1) CA2789427A1 (cg-RX-API-DMAC7.html)
CL (1) CL2012002225A1 (cg-RX-API-DMAC7.html)
EA (1) EA201290774A1 (cg-RX-API-DMAC7.html)
IL (1) IL221390A0 (cg-RX-API-DMAC7.html)
MX (1) MX2012009378A (cg-RX-API-DMAC7.html)
PH (1) PH12012501621A1 (cg-RX-API-DMAC7.html)
SG (1) SG183263A1 (cg-RX-API-DMAC7.html)
TN (1) TN2012000400A1 (cg-RX-API-DMAC7.html)
WO (1) WO2011100607A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201206416B (cg-RX-API-DMAC7.html)

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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
EP2533639A4 (en) * 2010-02-11 2013-08-21 Univ Vanderbilt PYRAZOLOPYRIDIN, PYRAZOLOPYRZIN, PYRAZOLOPYRIMIDIN, PYRAZOLOTHIOPHEN AND PYRAZOLOTHIAZOL COMPOUNDS AS ALLOSTERIC MGLUR4 POTENTRANS AND COMPOUNDS AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTIONS
MX339302B (es) 2011-09-15 2016-05-19 Novartis Ag 3-(quinolin-6-il-tio)-[1,2,4]-triazolo-[4,3-a]-piridinas 6-sustituidas como cinasas de tirosina.
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EP2791108B1 (en) 2011-12-15 2016-07-27 Pfizer Limited Sulfonamide derivatives
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WO2014117920A1 (en) * 2013-02-04 2014-08-07 Merck Patent Gmbh Spiro-quinazolinone derivatives useful for the treatment of neurological diseases and conditions
WO2014180182A1 (zh) * 2013-05-10 2014-11-13 江苏豪森药业股份有限公司 [1,2,4]三唑并[4,3-a]吡啶类衍生物，其制备方法或其在医药上的应用
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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
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
US10227343B2 (en) 2015-01-30 2019-03-12 Vanderbilt University Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, 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
UY36654A (es) 2015-04-29 2016-10-31 Janssen Pharmaceutica Nv Azabenzimidazoles con propiedades moduladoras del receptor ampa y composiciones farmacéuticas que los contienen
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