5 results about "Pimavanserin" patented technology

This invention discloses a method for preparing pimozide, which involves acylation of 4-isobutoxybenzylamine acetate with carbonyl diimidazole under alkaline conditions, followed by condensation reaction with N-(4-fluorobenzyl)-1-methylpiperidine-4-amine in a reducing solvent, and then post-treatment to obtain the product. The method uses stable 4-isobutoxybenzylamine acetate as raw material, which avoids the introduction of impurities by 4-isobutoxybenzylamine. Combined with the condensation reaction under a reducing solvent, the generation of impurities can be effectively avoided. The product has stable quality, is simple to operate, has low production cost, and is suitable for industrial production.

A preparation method of a solid preparation of pimavanserin, which improves the flowability of pimavanserin powder in the preparation process, improves the stability of the active ingredient content in the solid preparation, and has the characteristics of rapid dissolution and release and good compression molding.

The invention relates to a pimavanserin orally disintegrating tablet as well as a preparation method and application thereof. The pimavanserin orally disintegrating tablet comprises pimavanserin or a salt thereof with unimodal particle size distribution, a disintegrating agent, a filling agent, a flavoring agent, a lubricating agent and a flow aid. The preparation method comprises four steps of API refining, premixing, total mixing and tabletting. The orally disintegrating tablet is especially suitable for Parkinson's disease psychosis with the following symptoms: (1) swallowing is difficult, and the tablet cannot be taken with water; and / or (2) the compound is sensitive to bitter taste and has a Tibetan medicine behavior; and / or (3) diabetes combined with Parkinson's disease psychosis.

1,5-dihydro-2,4-benzodiazepine-3-one derivatives, such as a compound represented by formula I, acts on 5-HT2A and 5-HT2C receptors. The selectivity for 5-HT2A is superior or similar to pimavanserin. The derivative is used for treating schizophrenia or Parkinson's disease, dementia-related behavioral disorders, and psychosis. The antipsychotic activity of the compound is equivalent to that of pimavanserin, the side effects of sedation and worsening of exercise are less than those of pimavanserin, and cardiotoxicity is less than that of pimavanserin.

The invention relates to stable oral formulations of pimavanserin or its pharmaceutically acceptable salts, provided in the form of ready-to-use liquids, powders for reconstitution, orally dispersible tablets, and kits containing pre-measured powder and a liquid vehicle for reconstitution. These formulations are stable for longer periods and are palatable, thereby improving patient compliance and adherence in the treatment of psychosis associated with Parkinson's disease.