280772-00-1

Usage

Uses

Used in Pharmaceutical Industry:
1-METHANESULFONYL-PIPERIDINE-4-CARBOXYLIC ACID is used as a key intermediate in the synthesis of various pharmaceuticals for its ability to contribute to the molecular diversity and structural complexity of drug candidates. Its presence in the molecular framework can enhance the pharmacological properties of the final drug products.
Used in Agrochemical Industry:
In the agrochemical sector, 1-METHANESULFONYL-PIPERIDINE-4-CARBOXYLIC ACID is utilized as a precursor in the development of new agrochemicals, such as pesticides and herbicides. Its chemical properties allow for the creation of compounds with specific target pest or weed control profiles, contributing to more effective and selective crop protection agents.
Used in Organic Synthesis:
1-METHANESULFONYL-PIPERIDINE-4-CARBOXYLIC ACID is employed as a versatile building block in organic synthesis, enabling the creation of a wide range of chemical compounds with potential applications across various industries. Its reactivity and functional group compatibility make it a preferred choice for chemists looking to construct complex molecular architectures.
Used in Therapeutic Research:
1-METHANESULFONYL-PIPERIDINE-4-CARBOXYLIC ACID has been studied for its potential therapeutic applications in the treatment of various medical conditions. Its unique chemical structure allows for exploration in drug discovery, where it may contribute to the development of novel treatments for unmet medical needs.

Upstream product

• 217487-18-8 1-methanesulfonylpiperidine-4-carboxylic acid ethyl ester 
• 498-94-2 isonipecotic acid 
• 124-63-0 methanesulfonyl chloride 
• 2971-79-1 isonipecotic acid methyl ester 
• 320424-42-8 methyl 1-(methylsulfonyl)piperidine-4-carboxylate 
• 847495-08-3 1-methanesulfonyl-piperidine-4-carboxylic acid benzyl ester 
• 1126-09-6 4-carbethoxypiperidine 

Downstream Products

• 280769-13-3 N-(5-chloropyridin-2-yl)-2-[(1-methylsulfonylpiperidin-4-ylcarbonyl)amino]benzamide 
• 333986-31-5 N-(3-chloropropyl)-N-(3,4-dichlorophenyl)-1-(methylsulfonyl)piperidine-4-carboxamide 
• 241138-40-9 1-(methylsulfonyl)piperidine-4-carbonyl chloride 

Relevant academic research and scientific papers

Optimization of Small Molecules That Sensitize HIV-1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity

With approximately 37 million people living with HIV worldwide and an estimated 2 million new infections reported each year, the need to derive novel strategies aimed at eradicating HIV-1 infection remains a critical worldwide challenge. One potential strategy would involve eliminating infected cells via antibody-dependent cellular cytotoxicity (ADCC). HIV-1 has evolved sophisticated mechanisms to conceal epitopes located in its envelope glycoprotein (Env) that are recognized by ADCC-mediating antibodies present in sera from HIV-1 infected individuals. Our aim is to circumvent this evasion via the development of small molecules that expose relevant anti-Env epitopes and sensitize HIV-1 infected cells to ADCC. Rapid elaboration of an initial screening hit using parallel synthesis and structure-based optimization has led to the development of potent small molecules that elicit this humoral response. Efforts to increase the ADCC activity of this class of small molecules with the aim of increasing their therapeutic potential was based on our recent cocrystal structures with gp120 core.

SMALL MOLECULES THAT SENSITIZE HIV-1 INFECTED CELLS TO ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY

Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R1-R7, X, X', Y, Y', Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.

CCR5 antagonists as anti-HIV-1 agents. Part 3: Synthesis and biological evaluation of piperidine-4-carboxamide derivatives

Replacement of the 5-oxopyrrolidin-3-yl fragment in the previously reported lead structure with a 1-acetylpiperidin-4-yl group led to the discovery of a novel series of potent CCR5 antagonists. Introduction of small hydrophobic substituents on the central phenyl ring increased the binding affinity, providing low to sub-nanomolar CCR5 antagonists. The selected compound 11f showed excellent antiviral activity against CCR5-using HIV-1 replication in human peripheral blood mononuclear cells (EC50 = 0.59 nM) and an acceptable pharmacokinetic profile in dogs.

PROTEASOME INHIBITORS AND METHODS OF USING THE SAME

The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

PROCESS FOR PREPARATION OF BENZYLPIPERIDINE COMPOUNDS

According to the process as shown in the following scheme having a step for reacting Compound (I) with Compound (II) to produce Compound (III), benzylpiperidine compounds useful as synthesis starting materials of pharmaceutical agents, agricultural chemicals and the like can be produced conveniently by a short step: wherein R1 is a hydrogen atom or an amino-protecting group, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, and R3 is a lower alkyl group.

Cyclic amine compounds as CCR5 antagonists

A compound of formula (I) (wherein R1is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1and R2may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y?(R5is a hydrocarbon group; Y?is a counter anion); R3is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1is a bond, CO or SO2; G2is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3aliphatic hydrocarbon which may be substituted; provided that J is methine when G2is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).