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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 84163-77-9, molcular formula is C12H13FN2O, introducing its new discovery. Product Details of 84163-77-9

A series of novel 7-[3-(1-piperidinyl)propoxy]chromenones was synthesized and tested as potential antipsychotics in several in vitro and in vive assays. The compounds possessed good affinity for D2 receptors, together with a greater affinity for 5-HT2 receptors, a profile which has been proposed as a model for atypical antipsychotics. Several agents also displayed a high potency in the climbing mice assay on oral administration, suggesting a potent antipsychotic effect as compared to reference standards. Compound 23 was selected for further pharmacological evaluation. Induction of catalepsy and inhibition of stereotypies weaker than standards, along with a lower increase in serum prolactin levels, were indicative of a potential atypical profile for this compound. From these results, 7-[3-[4-(6-fluoro- 1,2-benzisoxazol-3-yl)piperidin1-yl]propoxy]-3-(hydroxymethyl)chromen-4-one (23, abaperidone) has been proposed for clinical evaluation in humans as a potential atypical antipsychotic.

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Piperidine – Wikipedia,
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We describe a practical and efficient route for synthesis of 2- aminomethyl-1,2,3,9-tetrahydro-4H-carbazol-4-ones using an effective Fisher indole methodology. The most active compounds, 4b (QF 2003B) and 4c (QF 2004B), with pKi (5-HT(2A)/D2) ratio of 1.28 show an antipsychotic profile according to Meltzer’s classification.

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Piperidine – Wikipedia,
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Pyrroloazepine derivatives

A method for treating a circulatory disease or condition in a mammal, which entails administering to the mammal an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof: whereinthe ring P represented by ?is a pyrrole ring having the following structure: wherein R1 represents C1-C8 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkyl-alkyl, C6-C14 aryl or C7-C22 aralkyl, which are optionally substituted; and R2 represents H or C1-C8 alkyl, which is optionally substituted; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H, but, when the bond is absent, Z1 and Z2 are both H; Z1 represents H and Z2 represents a group OR3, in which R3 represents H, C1-C8 alkyl, or C7-C22 aralkyl, which are optionally substituted; Z1 and Z2 both represent groups SR4, in which R4 represents C1-C8 alkyl or C7-C22 aralkyl, which are optionally substituted; or Z1 and Z2 are combined together to represent O, a group NOR5, in which R5 represents H, or C1-C8 alkyl or C2-C3 alkylenedithio, which are optionally substituted; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W is CH, C= or N, m is for 0 or 1, n is for 1, 2 or 3, G is O, S, C=O, sulfinyl, sulfonyl, alkylene, alkenylene or acetal; E1 and E2 is H or C1-C8 alkyl; and D represents an aromatic hydrocarbon or an aromatic heterocyclic ring. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is therapeutically useful in the treatment of circulatory diseases and/or conditions related thereto.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H17861N – PubChem

 

Discovery of 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole

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Chemistry is traditionally divided into organic and inorganic chemistry. HPLC of Formula: C12H13FN2O. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 84163-77-9

Thiophene compound

Thiophene compounds of the formula STR1 wherein each symbol is as defined in the specification, their pharmaceutically acceptable salts, pharmaceutical compositions containing said compound and additives for pharmaceuticals, and antipsychotics containing said compound as an active ingredient. The compound of the present invention has pharmacological actions required of antipsychotic, such as motility suppressing action, anti-apomorphine action, mothamphetamine antagonistic action, tetrabenazine-induced blepharoptosis enhancing action, and the like. The compound of the present invention is useful as an antipsychotic having less extrapyramidal side-effects or a non-benzodiazepine type antianxiety agent.

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Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands

A series of novel alpha-tetralone and alpha-tetralol derivatives was synthesized, and their binding affinities for 5-HT2A and D 2 receptors, the most important targets implicated in the anti-schizophrenia drug action, were evaluated to elucidate how substitutions in the aromatic ring of the pharmacophore affect to the affinity or selectivity for these receptors. The replacement of the H-7 in the tetrahydronaphthalene system by an amino group resulted in privileged 5-HT2A affinity of the 6-fluorobenzo[d]isoxazol derivative 36 and the alcohol 25 both showing a pKi value for 5-HT2A higher than 8.3 and good binding affinities for D2 receptor leading to a Meltzer’s ratio characteristic of an atypical antipsychotic profile. Additionally, a small collection of 3-aminomethyltetralone derivatives was prepared and examined here for their affinities and selectivities as 5-HT2A/D2 dual ligands. Compound 11 shows the best profile with good pKi values for 5-HT2A and D2 receptors leading to a Meltzer’s ratio characteristic of a typical antipsychotic behaviour. These three compounds behaved as competitive antagonists of both 5-HT2A and D2 receptors, and might be promising pharmacological tools for the investigation of the dual function of the 5HT2A-D2 ligands.

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Piperidine – Wikipedia,
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PROCESS FOR PREPARING PALIPERIDONE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

The present invention discloses the process for the preparation of paliperidone and its pharmaceutically acceptable salts comprising (a) condensing 2-amino-3-hydroxy- pyridine with 2-acetylbutyro lactone in the presence of an acid catalyst to isolate 9- hydroxy-3-(2-hydroxyethyl)-2-rnethyl-4H-pyrido[l, 2-a] pyrimidin-4-one; treating 9- hydroxy-3-(2-hydroxyethyl)-2-methyl-4H-pyrido[l, 2-a] pyrimidin-4-one with a chlorinating agent; hydrogenating the product in the presence of one or more lewis acids to obtain 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[l,2-a]- pyrimidin-4-one; and condensing3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2- methyl-4H-pyrrido[l,2-a]-pyrimidin-4-one. The present invention also discloses processes for the preparation of intermediates useful in the preparation of paliperidone and its pharmaceutically acceptable salts.

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Piperidine – Wikipedia,
Piperidine | C5H17779N – PubChem

 

Discovery of 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 84163-77-9 is helpful to your research. category: piperidines

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BENZISOXAZOLE PIPERIDINYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING THE DERIVATIVES AND THEIR USE

The invention relates to a benzisoxazolyl piperidine derivative having the following general formula, a salt or a hydrate thereof, wherein R, X, Y, R? and T are defined as in the specification. Such compounds have serotonin system modulating effects such as antagonizing effect on 5-HT2A and inhibitory effect on 5-HT reuptake. The compounds have good analgesic and sedative activities with mild toxic and side effects. The invention also relates to a composition comprising said derivative and the use thereof.

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Synthesis and characterization of novel 6-fluoro-4-piperidinyl-1,2- benzisoxazole amides and 6-fluoro-chroman-2-carboxamides: Antimicrobial studies

Novel derivatives of 6-fluoro-4-piperidinyl-1,2-benzisoxazole amides 4(I-VI) were obtained by the condensation of different acid chlorides with 6-fluoro-3-piperidin-4yl-benzo[d]isoxazole. Also, 6-fluoro-chroman-2- carboxamides 6(I-III) were synthesized by using nebulic acid chloride with different amines in presence of triethylamine as acid scavenger and dichloroethane as solvent. The synthesized compounds were characterized by IR, 1H NMR, and CHN analysis. These molecules were evaluated for their efficacy as antimicrobials in vitro by disc diffusion and microdilution method against pathogenic strains such as Bacillus substilis, Escherichia coli, Pseudomonas fluorescens, Xanthomonas campestris pvs, X. oryzae, Aspergillus niger, A. flavus, Fusarium oxysporum, Trichoderma species, F. monaliforme, and Penicillum species. Compounds 4I, 4IV, 4V, 6I, 6II and 6III showed better inhibitory activity than compared to standard drugs. Among these compounds, 4IV and 6III showed potent inhibitory activity against all the strains and found to be nonstrain dependent. The title compounds represent a novel class of potent antimicrobial agents.

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Piperidine – Wikipedia,
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