301219-11-4

Usage

Uses

Used in Pharmaceutical Research and Drug Development:
4-(3-OXO-4-PHENYL-BUTYRYL)-PIPERIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER is used as a chemical compound in pharmaceutical research and drug development for its potential therapeutic properties in treating central nervous system disorders.
Used in the Treatment of Central Nervous System Disorders:
In the pharmaceutical industry, 4-(3-OXO-4-PHENYL-BUTYRYL)-PIPERIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER is used as a therapeutic agent for the treatment of disorders such as schizophrenia and anxiety, due to its potential impact on the central nervous system.
Used in Medicinal Chemistry Research:
4-(3-OXO-4-PHENYL-BUTYRYL)-PIPERIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER is utilized as a target in medicinal chemistry research, where its unique chemical structure and properties are explored for the development of novel pharmaceutical agents.
Used in Drug Delivery Systems:
In the formulation of drug delivery systems, 4-(3-OXO-4-PHENYL-BUTYRYL)-PIPERIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER is used to improve solubility and bioavailability, thanks to its tert-butyl ester functionality.

Upstream product

• 101-41-7 benzeneacetic acid methyl ester 
• 206989-61-9 4-acetyl-1-(t-butoxycarbonyl)piperidine 
• 109-72-8 n-butyllithium 
• 84358-13-4 N-[(tert-butoxy)carbonyl]piperidine-4-carboxylic acid 
• 530-62-1 1,1'-carbonyldiimidazole 
• 103-79-7 1-phenyl-acetone 

Downstream Products

• 313512-98-0 4-(5-benzyl-1-ethyl-(1H)-pyrazol-3-yl)-1-(t-butoxycarbonyl)piperidine 
• 301219-12-5 4-(3-Benzyl-1-ethyl-(1H-pyrazol-5-yl))-1-(tert-butoxy-carbonyl)piperidine 
• 795310-84-8 4-(5-benzyl-2-methyl-2H-pyrazol-3-yl)-piperidine-1-carboxylic acid tert-butyl ester 
• 301219-25-0 4-(3-Benzyl-(1H-pyrazol-5-yl))-1-(tert-Butoxycarbonyl)-piperidine, trifluoroacetic acid salt 
• 301219-33-0 4-(5-Benzyl-isoxazol-3-yl)-1-(tert-butoxycarbonyl)piperidine 
• 301219-39-6 4-(3-benzyl-isoxazol-5-yl)-piperidine 
• 301219-37-4 4-(5-Benzyl-isoxazol-3-yl)piperidine 
• 301209-01-8 (R)-{(3S,4S)-3-[4-(5-Benzyl-2-ethyl-2H-pyrazol-3-yl)-piperidin-1-ylmethyl]-4-phenyl-pyrrolidin-1-yl}-cyclohexyl-acetic acid 

Relevant academic research and scientific papers

N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists

The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains

Replacement of the flexible connecting chains between the piperidine moiety and an aromatic group in previous CCR5 antagonists with heterocycles, such as pyrazole and isoxazole, provided potent CCR5 antagonists with excellent anti-HIV-1 activity in vitro. SAR studies revealed optimal placement of an unsubstituted nitrogen atom in the heterocycle to be meta to the bond connected to the 4-position of piperidine. Truncation of a benzyl group to a phenyl group afforded compounds with dramatically improved oral bioavailability, albeit with reduced activity.

CHEMICAL COMPOUNDS

Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).

Modulators of CCR5 chemokine receptor activity

Compounds of Formula I: (wherein R1, R2, R3, R4, Q, and X are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Pyrrolidine modulators of chemokine receptor activity

The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R14and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.