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OwnerJeroen Van Rheenen, Wilhelmus G.H.M. Muijselaar +1inventors
InventorsJeroen Van Rheenen, Wilhelmus G.H.M. Muijselaar, Hendrik Teunissen
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This invention relates to a process for the preparation of 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride, a partial dopamine-D2 receptor agonist and a full serotonin 5-HT1A receptor agonist. 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride The invention also relates to polymorphic forms of said compound, as well as to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, to methods for preparing intermediates useful for their synthesis, and to methods for preparing compositions containing these compounds. The invention also relates to the use of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in conditions or diseases of the central nervous system, caused by disturbances of the dopaminergic and/or serotonergic systems, for example: anxiety disorders (including generalized anxiety, panic disorder and obsessive compulsive disorder), depression, autism, schizophrenia, Parkinson's disease, restless leg syndrome, and disturbances of cognition and memory.
The α-polymorph of 7-[(4-methyl)-1-piperazinyl]-2(3H)-benzoxazolone hydrochloride, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic reflexes, expressed in degrees of diffraction angle 2 θ, at about:
A pharmaceutical composition comprising, in addition to a pharmaceutically acceptable carrier and at least one pharmaceutically acceptable auxiliary substance, a pharmacologically active amount of the α-polymorph of 7-[(4-methyl)-1-piperazinyl]-2(3H)-benzoxazolone hydrochloride, as an active ingredient, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic reflexes, expressed in degrees of diffraction angle 2 θ, at about:
A method for treating at least one central nervous system disorder chosen from anxiety disorders, depression, autism, schizophrenia, Parkinson's disease, restless leg syndrome, and disturbances of cognition and memory, the method comprising administering a pharmaceutical composition to a patient in need thereof, said composition comprising the α-polymorph of 7-[(4-methyl)-1-piperazinyl]-2(3H)-benzoxazolone hydrochloride, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic reflexes, expressed in degrees of diffraction angle 2 θ, at about:
A method for preparing an α-polymorph of 7-[(4-methyl)-1-piperazinyl]-2(3H)-benzoxazolone hydrochloride, comprising:
Dependencies are inferred from the claim text.