- Discovery of novel aldose reductase inhibitors characterized by an alkoxy-substituted phenylacetic acid core
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In continuation of our effort aimed towards the development of novel aldose reductase inhibitors, several phenylacetic acids bearing an alkoxy substituent in position 3 or 4, respectively, were prepared and screened. The latter represent formal ring openi
- Rakowitz, Dietmar,Gmeiner, Andreas,Matuszczak, Barbara
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- COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES
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The present disclosure relates to compounds according to Formulae (I), (II) and (VIII), useful for treating diseases.
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- PROCESS FOR THE MANUFACTURING OF PIMAVANSERIN
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The present invention relates to a new process for manufacturing 1 -(4-fluorobenzyl)-3-(4-iso- butoxyphenyl)-1 -(1 -methylpiperidin-4-yl)urea, with the INN name pimavanserin, and its hemi- tartrate salt. Said process comprises the following step: contacting 2-(4-isobutoxyphenyl)acetic acid with N-(4-fluorobenzyl)-1 -methylpiperidin-4-amine in the presence of a base and diphe- nylphosphoryl azide (DPPA) to obtain pimavanserin.
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- Synthesis method of 4-isobutoxy benzylamine
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The invention discloses a synthesis method of 4-isobutoxy benzylamine. 4-hydroxyphenylacetic acid serves as a raw material to generate 4-hydroxyphenylacetic acid methylester through an esterificationreaction; 4-hydroxyphenylacetic acid methylester is subjected to a substitution reaction to generate 4-methyl isobutoxyphenylacetic acid, and 4-isobutoxyphenylacetic acid is obtained after the obtained product is hydrolyzed; 4-isobutoxyphenylacetamide is generated through an acylation reaction; and N-(4-hydroxy benzyl)methyl carbamate is generated through a Hofmann degradation reaction, and a target product is obtained through hydrolysis. The raw materials used in the synthesis method are cheap and easy to get, the reaction condition is mild, post-treatment is simple, column chromatography isnot needed, the product can be obtained easily, and the yield is higher.
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- PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF PIMAVANSERIN
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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.
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Paragraph 0164
(2018/04/17)
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- Preparation method of 5-HT2A inverse agonist ACP-103
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The invention discloses a preparation method of 5-HT2A inverse agonist ACP-103. The method includes: in the presence of borohydride, subjecting 4-fluorobenzylamine and N-methyl-4-piperidone to reaction to obtain a compound as shown in the formula 3; in the presence of inorganic base, subjecting methyl 4-hydroxyphenylacetate and 1-bromo-2-methylpropane to reaction to obtain a compound as shown in the formula 6; subjecting the compound as shown in the formula 6 to reaction with inorganic base to obtain a compound as shown in the formula 7; subjecting the compound as shown in the formula 7 to reaction with an acyl chloride reagent to obtain a compound as shown in the formula 8; in the presence of tetrabutylammonium bromide, subjecting the compound as shown in the formula 8 to reaction with sodium azide to obtain a compound as shown in the formula 9; subjecting the compound as shown the formula 9 and the compound as shown in the formula 3 to reaction to obtain the compound ACP-103 as shown in the structural formula. The preparation method of the 5-HT2A inverse agonist ACP-103 is mild in reaction condition and high in yield.
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- An example of designed multiple ligands spanning protein classes: Dual MCH-1R antagonists/DPPIV inhibitors
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A ligand-based approach to identify potential starting points for a dual MCH-1R antagonist/DPPIV inhibitor medicinal chemistry program was undertaken. Potential ligand pairs were identified by analysis of MCH-1R and DPPIV in vitro data. A highly targeted
- Gattrell, William T.,Sambrook Smith, Colin P.,Smith, Alun J.
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p. 2464 - 2469
(2012/05/19)
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- N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECEPTOR AGENTS
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Disclosed herein are isolated forms of the compounds of Formula (I), (II), (III), (IV) and (V), or a pharmaceutically acceptable salt, prodrug, hydrate, solvate, polymorph, or ester thereof. Also disclosed are methods of inhibiting an activity of a serotonin receptor, methods inhibiting an activation of a serotonin receptor, and methods of alleviating or treating various disease conditions and side effects.
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Page/Page column 15
(2009/04/24)
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- SUBSTITUTED UREAS
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Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders.
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Page/Page column 21
(2008/12/08)
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- USE OF 4-AMINO-PIPERIDINES FOR TREATING SLEEP DISORDERS
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Inverse agonists and antagonists of serotonin receptors are disclosed for use in treating sleep disorders such as insomnia, and specifically sleep maintenance insomnia. The compound increase slow wave sleep, decrease the number of awakenings after sleep onset, and decrease the time awake after sleep onset.
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- N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECPTOR AGENTS
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Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.
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