427-40-7

Upstream product

• 58113-20-5 1-acetyl-α-(4-fluorophenyl)-α-phenyl-4-piperidinemethanol 
• 25519-79-3 1-(4-benzoylpiperidin-1-yl)ethanone 
• 460-00-4 1-Bromo-4-fluorobenzene 
• 25519-80-6 4-(benzoyl)piperidine hydrochloride 

Downstream Products

• 1383479-19-3 C₂₇H₃₀FN₃O₃S₂ 
• 60284-74-4 1-[3-(p-acetyl-o-methoxyphenoxy) propyl]-4-(α-p-fluorophenyl-α-hydroxy)benzylpiperidine 

Relevant academic research and scientific papers

Synthesis and SAR of selective small molecule neuropeptide y Y2 receptor antagonists

Highly potent and selective small molecule neuropeptide Y Y2 receptor antagonists are reported. The systematic SAR exploration of a hit molecule N-(4-ethoxyphenyl)-4-[hydroxy(diphenyl)methyl]piperidine-1-carbothioamide, identified from HTS, led to the discovery of highly potent NPY Y2 antagonists 16 (CYM 9484) and 54 (CYM 9552) with IC50 values of 19 nM and 12 nM respectively.

4-[diaryl)hydroxymethyl]-1-piperidinealkylcarboxylic acids, salts and esters useful in the treatment of allergic disorders

Novel compounds useful in the treatment of allergic disorders and having the formula: STR1 where Ar and Ar1 are pyridinyl, phenyl, or substituted phenyl and where Y is --OH,--O? M≈ m,--O--loweralkyl, --O--Aryl, or NR1 R2 (R1, R2 =H, loweralkyl, aryl) are herein disclosed.

4-[(diaryl)hydromethyl]-1-piperidinealkanols and esters and carbamates thereof useful in the treatment of allergic disorders

Novel compounds of the formula: STR1 are disclosed wherein Ar and Ar1 are phenyl, sustituted phenyl or pyridinyl, "alk" is a C1 -C12 straight or branched hydrocarbon chain, and R is H, loweralkylcarbonyl, arylcarbonyl, or aminocarbonyl where the amino is unsubstituted or substituted by one or two groups selected from loweralkyl or aryl. The compounds of this invention are useful in the treatment of allergic disorders.

Aryl(alkyland alkylene)-N-((phenoxy and phenylthio)alkyl) aminoheterocyclics as cardiovascular, anthihistaminic, antisecretory and antiallergy agents

A method of treating cardiac dysfunction, the effects of histamine, and gastric secretion excesses with aryl(alkyl and alkylene)-N-[(phenoxy and phenythio)alkyl]aminoheterocyclics corresponding to the formula: STR1 wherein Ar is phenyl or substituted phenyl; R is phenyl, substituted phenyl, pyridinyl or cycloalkyl; A is hydrogen, hydroxy, cyano, amido and amino; Q is --CH2 --, --CH--, or --CHOH--; d and n are zero or one and the dotted lines form double bonds consistent with the valence of carbon; p is zero, one or two; m is one to six inclusive; B is oxygen, nitrogen, sulfur, sulfinyl or sulfonyl; z is zero or one; l is zero or one; W is hydrogen, loweralkyl, halo, nitro, loweralkoxy or hydroxy; X is hydrogen, loweralkyl, halogen, loweralkoxy or hydroxy; Y is --CH(OH)CH2 OH, --CH(OH)C(O)OH, --C(O)C(O)OH, --C(O)CH2 OH,--C(O)C(O)OCH3, --C(O)C(O)OC2 H5, --CH2 C(O)OC2 H5, --CH(OH)C(O)OCH3, --CH(OH)C(O)OC2 H5 or --C(O)CH2 OC(O)CH3 ; and the pharmaceutically acceptable salts thereof; in addition to the above methods of treatment, compounds wherein (B)z is oxygen are useful in a method of treating Gell and Coombs type 1 allergic responses in mammals.

Arylalkylheterocyclic amines,N-substituted by aryloxyalkyl group in a method for allergy treatment

A method of inhibiting Type 1 allergic responses in a living animal body with substituted heterocyclic amines is disclosed wherein the active agents are expressed generally by the formula which includes certain known and certain known compounds: STR1 wherein P is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is --CH--, CH2 -- or STR2 n is zero or one and when Q is --CH-- and n is one, a double bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the α carbon and a carbon of the central heterocyclic amine ring; Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition, R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values: 2H-1-benzopyran-2-one,4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4H-1-benzopyran-4-one, 1,4-benzodioxanloweralkyl-2-yl or 1,1'-biphenyl-4-yl and the pharmaceutically acceptable salts thereof.

Synthesis and Antiallergy Activity of 4-(Diarylhydroxymethyl)-1-piperidines and Structurally Related Compounds

A series of 4-(diarylhydroxymethyl)-1-piperidines was synthesized and evaluated for antiallergy activity.Several analogues had potent activity in the passive foot anaphylaxis (PFA) assay, an IgE-mediated model useful in the detection of compounds possessing antiallergic activity.In particular 1--1-piperidinyl>propoxy>-3-methoxyphenyl>ethanone (1, AHR-5333) was more potent than oxatomide and terfenadine in this assay.

4-[(α,α-diaryl)-hydroxymethyl]-1-piperidinylalkyl-cyclic carbamate derivatives as allergic response inhibitors

4-[(α,α-Diaryl)-hydroxymethyl]-1-piperidinylalkylcyclic carbamate derivatives having the formula: STR1 wherein; R is hydrogen, loweralkyl, cycloalkyl, phenyl and substituted phenyl; Ar and Ar1 are phenyl, substituted phenyl or pyridinyl; alk is a straight or branched hydrocarbon chain; R1 is loweralkyl substituted for hydrogen on a ring carbon. The compounds are useful antihistamines and in controlling allergic response.

1-Substituted-4-benzylpiperidines

Novel 1-substituted-4-benzylpiperidines having α-substituents on the 4-benzyl moiety useful as antiinflammatory agents, sedatives, and tranquilizers are represented by the formula SPC1 Wherein R represents acetyl, aryloxyloweralkyl, aroylloweralkylcarbamo