60285-09-8

Upstream product

• 106088-85-1 4-(4-fluorobenzoyl)-1-(2-hydroxyethyl)piperidine 
• 25519-78-2 4-(4-fluorobenzoyl)piperidine hydrochloride 
• 540-51-2 2-bromoethanol 
• 56346-57-7 (4-fluorophenyl)-piperidin-4-ylmethanone 

Downstream Products

• 269061-57-6 8-{4-[N-(5-(2-(4-(4-fluorobenzoyl)piperidine)ethyloxy)-3,4-dihydro-2H-1-benzopyran-3-ylmethyl)-N-(t-butyloxycarbonyl)amino]butyl}-8-azaspiro[4.5]decane-7,9-dione 
• 131952-42-6 4-[(4-Chlorophenyl)phenylmethyl]-1-{2-[4(4-fluorobenzoyl) piperidino]ethyl}piperazine 2.6-dione hydrochloride 

Relevant academic research and scientific papers

Substituted 3-amino and/or 3-aminomethyl-3,4-dihydro-2H-1-benzopyrans: Synthesis and biological activity

A series of new 3-amino, 3-aminomethyl-5-alkoxy-3,4-dihydro-2H-1-benzopyran and 5'-alkoxy-3',4'-dihydrospiro[piperazine-2,3'(2'H)-benzopyran] derivatives was prepared and evaluated for affinity at 5-HT(1A), 5-HT(2A) and D2 receptors. Two of the

Substituted cyclic amine compound, production process thereof and pharmaceutical composition for circulatory organ use containing the same

A substituted cyclic amine compound represented by the following general formula (1) STR1 wherein each of R1 to R5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or the like, A represents a carbonyl group or a sulfonyl group, B represents a methine moiety or a nitrogen atom, D represents a methine moiety, a nitrogen atom or =N(→O)-- and n is an integer of 2 to 3; and synthetic methods thereof. The inventive compound is useful in preventing and treating circulatory organ-related diseases such as hypertension, ischemic heart disease, cerebrovascular disease, peripheral circulatory disease and the like.

3-[2-[4-(4-Fluorobenzoyl)piperidin-1-yl]ethyl]- 5,6,7,8-tetrahydro-4(3H)-quinazolinones: Serotonin 5-HT(2A) receptor antagonists endowed with potent central action

A series of 5,6,7,8-tetrahydro-4(3H)-quinazolinones substituted at the 3-position with 4-benzoyl-1-ethylpiperidine, 4-(4-fluorobenzoyl)-1-ethylpiperidine, 4-[bis-(4-fluorophenyl)methylene]-1-ethylpiperidine, or 4-(4-fluorophenyl)-1-propylpiperazine have been prepared and evaluated in binding assays to determine their affinity at serotonin 5-HT(2A) receptors as well as in a functional test, ie, wet dog shakes (WDS) induced by L-5-hydroxytryptophan (L-5-HTP), a behavioural response which is mediated by stimulation of 5-HT(2A) receptors. Among the compounds prepared, 3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-5,6,7,8-tetrahydro-4(3H) -quinazolinone (10a) and 2-methyl-3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-5,6,7,8-tetrahydro -4(3H)-quinazolinone (10b) proved to be the most potent 5-HT(2A) receptor antagonists. In binding assays, the two compounds displayed similar affinity for 5-HT(2A) receptors in the nanomolar range to ketanserin and ritanserin. In the WDS test, they were even more potent than ketanserin and ritanserin. Compound 10b, which was found to possess the highest potency and duration of action in the WDS test, was chosen for a preliminary evaluation of its ability to inhibit ethanol intake in rats, a response linked to blockade of the central 5-HT(2A) receptors. This compound significantly reduced ethanol intake in rats from the first day of treatment. The results of the present study indicate that 10b is a potent centrally acting antagonist at 5-HT(2A), receptors.

(Aryl(alkyl)carbonyl)-heterocyclic compounds, compositions and use

The invention relates to a compound selected from those of formula (I): STR1 wherein Ar, n, B and A are as defined in the description, to their optical isomers, and to their addition salts there of with a pharmaceutically-acceptable acid or base. Medicinal product which is useful for treating pain and treating or preventing pathologies which require psychotropic agents.

1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones

1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones of the formula STR1 wherein R is hydrogen or fluoro, R1 is hydrogen, fluoro chloro, bromo or trifluoromethyl, and n is 2 to 4, having anticonvulsant activity and useful as anti-anxiety agents, are disclosed.