Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists

Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists

The disclosure relates to a family of pharmaceutical compositions of metabotropic glutamate 5 receptor (mGlu5) antagonists or a pharmacologically acceptable salt thereof. The compositions form a layered pellet which contain the therapeutic active compound, a rate release controlling polymer and pH r...

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Bibliographische Detailangaben
Hauptverfasser: HUANG JINGJUN, SHAH NAVNIT HARGOVINDAS, LINDENSTRUTH KAI, KOENNINGS STEPHANIE, CHATTERJI ASHISH, SANDHU HARPREET K
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Beschreibung
Zusammenfassung:The disclosure relates to a family of pharmaceutical compositions of metabotropic glutamate 5 receptor (mGlu5) antagonists or a pharmacologically acceptable salt thereof. The compositions form a layered pellet which contain the therapeutic active compound, a rate release controlling polymer and pH responding polymer (that is ionic and non-ionic polymers) polymer, binder and fillers in either matrix pellet, matrix tablet or coated pellets. The core of the therapeutic active compound contains an azole (either pyrazole or imidazole), a pyridine and an alkyne group. The compositions provide a pH-independent in vitro release profile with NMT 70 % in one hour, NMT 85 % in 4 hour, and NLT 80 % in 8 hours. The compositions are useful for the treatment of CNS disorders, such as Treatment- Resistant Depression (TRD) and Fragile X Syndrome.