CA2789427A1 - Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction - Google Patents

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

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Publication number
CA2789427A1
CA2789427A1 CA 2789427 CA2789427A CA2789427A1 CA 2789427 A1 CA2789427 A1 CA 2789427A1 CA 2789427 CA2789427 CA 2789427 CA 2789427 A CA2789427 A CA 2789427A CA 2789427 A1 CA2789427 A1 CA 2789427A1
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Canada
Prior art keywords
optionally substituted
aryl
heteroaryl
cycloalkyl
alkyl
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Abandoned
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CA 2789427
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English (en)
French (fr)
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
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Vanderbilt University
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Vanderbilt University
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Publication of CA2789427A1 publication Critical patent/CA2789427A1/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
    • 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
    • A61K31/4164—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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    • 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
    • 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
    • A61K31/435—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
    • A—HUMAN NECESSITIES
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    • A61K31/4965—Non-condensed pyrazines
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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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    • A61K31/495—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
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • 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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  • Psychiatry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
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  • Hospice & Palliative Care (AREA)
  • 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)
CA 2789427 2010-02-11 2011-02-11 Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction Abandoned CA2789427A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US30348110P 2010-02-11 2010-02-11
US61/303,481 2010-02-11
US201161430521P 2011-01-06 2011-01-06
US61/430,521 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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CA2789427A1 true CA2789427A1 (en) 2011-08-18

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CA 2789427 Abandoned CA2789427A1 (en) 2010-02-11 2011-02-11 Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Country Status (17)

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.
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
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
EP3626717A1 (en) 2013-10-14 2020-03-25 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
US9663486B2 (en) 2013-10-14 2017-05-30 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
EP3134404A1 (en) 2014-04-25 2017-03-01 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
US9980945B2 (en) 2015-01-13 2018-05-29 Vanderbilt University Benzoisoxazole-substituted compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
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
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