68 results about "Pimavanserin" patented technology

As disclosed herein, co-administration of pimavanserin with an agent that ameliorates one or more cholinergic abnormalities can have a synergistic effect on the efficacy of the agent. Disclosed herein are compositions which include pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities. Also disclosed herein are methods for ameliorating or treating a disease condition characterized by one or more cholinergic abnormalities that can include administering pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities.

As disclosed herein, co-administration of pimavanserin with an agent that ameliorates one or more cholinergic abnormalities can have a synergistic effect on the efficacy of the agent. Disclosed herein are compositions which include pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities. Also disclosed herein are methods for ameliorating or treating a disease condition characterized by one or more cholinergic abnormalities that can include administering pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities.

Disclosed herein are methods for obtaining N-(4-fluorobenzyl)-N-(l-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (pimavanserin) comprising the step of contacting an intermediate according to Formula (A) or a salt thereof, with an intermediate Formula B, or a salt thereof, to produce pimavanserin or a salt thereof wherein Y is -ORi or -NR2aR2b; R3 is hydrogen or substitutedor unsubstituted heteroalicyclyl, R4 is substituted or unsubstituted aralkyl; X is -OR22 or -NR23R24; (wherein R22 is hydrogen or substituted or unsubstituted C1-6alkyl and one of R23 and R24 is hydrogen and the other is hydrogen or N- methylpiperidin-4-yl); and R21 is -OCH2CH(CH3)2 or F; Also disclosed herein is the tartrate salt of N-(4-fluorobenzyl)-N-(l-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt.

The invention discloses a pimavanserin intermediate and a preparation method of pimavanserin. A structural general formula of the pimavanserin intermediate is shown in the description; the pimavanserin intermediate is prepared by carrying out reductive amination on 4-isobutoxybenzaldehyde and carbamate; a synthesis route is shown in the description; the pimavanserin is obtained through ammonolysisreaction. According to the preparation method of the pimavanserin intermediate, the target intermediate is obtained in one step through reductive amination reaction and reaction steps of the pimavanserin are extremely simplified; used raw materials are safe and the cost is low; reaction conditions are moderate and phosgene which has great toxicity and is uneasy to operate is not used, so that thepreparation method is easy to realize in industry; the intermediate and a product are easy to separate and purify, and the next-step reaction can be directly carried out to prepare the pimavanserin,without the need of separating the pimavanserin; the preparation method is simple to operate and the yield is higher than that of the prior art; the synthesis cost of the pimavanserin is reduced.

The invention discloses a preparation method of pimavanserin. The preparation method comprises the following steps of mixing 1-(4-fluorobenzyl)-1-(4-methylpiperidyl)urea, 4-isobutoxybenzaldehyde and tetraisopropyl titanate in a solvent, reducing through hydroborate, and then obtaining the pimavanserin through purification. A synthesis method provided by the invention is succinct and high-efficiency, mild in reaction condition, easy to control and high in yield.

The invention discloses a preparation method of a pimavanserin key intermediate. A synthesis route comprises a process shown in the description. According to the method disclosed by the invention, used raw materials are safe and the cost is low, so that the production cost is effectively reduced. The method disclosed by the invention has moderate reaction conditions and the utilization of phosgenewhich has great toxicity and is not easy to operate can be avoided, so that the method is easy to realize in industry.

The invention belongs to the field of pharmaceutic preparation, and particularly relates to a pimavanserin tablet and a preparation method thereof. The pimavanserin tablet is composed of active components of pimavanserin, colloidal silicon dioxide, polyethylene glycol, a filling agent selected from dextrin, corn starch, pregelatinized starch, cellulose microciystalline, mannitol and lactose, a disintegrating agent selected from carboxymethyl starch sodium, croscarmellose sodium, low-substituted hydroxypropyl cellulose and crospovidone, and a lubricating agent selected from magnesium stearate,talcum powder, and sodium stearyl fumarate. The pimavanserin tablet has good stability, and can significantly improve drug dissolution and bioavailability.

The invention belongs to the field of medicine preparations and relates to a tartaric acid pimavanserin oral instant film and a preparation method thereof. The tartaric acid pimavanserin oral instant film is good in taste, can be quickly dissolved in the oral cavity when taken without water, and is particularly suitable for the aged and patients suffering from dysphagia. A preparation process of the tartaric acid pimavanserin oral instant film is simple and easy to implement, auxiliary materials are common and moderate in price, and industrial prospects are good. Each tartaric acid pimavanserin oral instant film contains 20 mg of tartaric acid pimavanserin. The invention further provides the preparation process of the tartaric acid pimavanserin oral instant film.

The invention relates to application of pimavanserin in preparation of antitumor drugs, belongs to the technical field of medicines, and particularly relates to novel application of pimavanserin in preparation of antitumor drugs. The structural formula of the pimavanserin is shown in the formula I. The biological activity test of the compound shows that the compound has antitumor activity and is a novel antitumor drug.

The invention discloses a method for preparing a pimavanserin hemitartrate crystal form B. The method comprises the following steps: adding pimavanserin hemitartrate into water; and after the pimavanserin hemitartrate is dissolved, concentrating and drying to obtain the pimavanserin hemitartrate crystal form B, wherein the weight-to-volume ratio of the pimavanserin hemitartrate to the water is 1:(4-6) g / ml. By using the nontoxic harmless water as the solvent, the pimavanserin hemitartrate crystal form B is successfully prepared. Besides, the method is simple and convenient, has the advantages of high safety, environment friendliness, high production efficiency and favorable economic benefits, and is very suitable for industrialized production.

The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.

The invention relates to a one-pot preparation method for pimavanserin. The method prepares pimavanserin (a compound IV) from 4-isobutoxybenzylamine as shown in a formula (II) or a salt thereof, a carbonylation reagent as shown in a formula (III) and N-(4-fluorobenzyl)-1-methylpiperidin-4-amine as shown in a formula (I) by using a one-pot process. The method is highly efficient, high in yield, low in cost, safe, environment friendly and suitable for industrial production, and has great application value.

The invention belongs to the field of pharmaceutical preparations and particularly relates to a pimavanserin nanocrystalline capsule and a preparation method thereof. The preparation method comprisesthe following steps: 1) adding pimavanserin and poloxamer 188 to water, and carrying out mixing to obtain a mixed solution; 2) homogenizing the mixed solution for 3 times to obtain a suspension; 3) performing spray drying on the suspension in a spray dryer; and 4) after mixing with other auxiliary materials, performing capsule filling. The prepared pimavanserin capsule can significantly increase the dissolution rate so as to improve the bioavailability of the medicine in vivo.

Combinations of 5-HT2A inverse agonists or antagonists such as pimavanserin with antipsychotics such as risperidone are shown to induce a rapid onset of antipsychotic action and increase the number of responders when compared to therapy with the antipsychotic alone. These effects can be achieved at a low dose of the antipsychotic, thereby reducing the incidence of side effects. The combinations are also effective at decreases the incidence of weight gain and increased glucose or prolactin levels caused by the antipsychotic.