402927-97-3

Usage

Uses

Used in Pharmaceutical Industry:
1-(METHYLSULFONYL)PIPERIDIN-4-AMINE is used as a key intermediate in the synthesis of pharmaceuticals for its ability to contribute to the development of new drugs with potential antiviral and antitumor properties. Its structural features make it a valuable component in the creation of molecules that can target specific biological pathways.
Used in Agrochemical Industry:
In the agrochemical sector, 1-(METHYLSULFONYL)PIPERIDIN-4-AMINE serves as a crucial building block for the preparation of agrochemicals, potentially enhancing crop protection and management through the development of novel compounds with targeted pest and disease control capabilities.
Used in Neurological Disorder Treatment:
1-(METHYLSULFONYL)PIPERIDIN-4-AMINE is being studied for its potential role in the treatment of neurological disorders, given its capacity to be integrated into compounds that may modulate neuronal functions and offer therapeutic benefits for various conditions.
Used as a Precursor in Organic Synthesis:
Beyond its direct applications, 1-(METHYLSULFONYL)PIPERIDIN-4-AMINE also acts as a precursor in organic synthesis, enabling the preparation of a range of biologically active compounds that can be further utilized in research and development across multiple scientific disciplines.

InChI:InChI=1/C6H14N2O2S/c1-11(9,10)8-4-2-6(7)3-5-8/h6H,2-5,7H2,1H3

Upstream product

• 402927-96-2 C₁₄H₂₀N₂O₄S 
• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 287953-38-2 (1-methanesulfonyl-piperidin-4-yl)carbamic acid tert-butyl ester 

Downstream Products

• 1253734-10-9 5-(2,6-difluorophenyl)-3-{[1-(methylsulphonyl)piperidin-4-yl]amino}-7-ethynyl-1H-pyrazolo[4,3-c]isoquinoline 
• 1345836-49-8 5-(2,6-difluorophenyl)-3-{[1-(ethylsulphonyl)piperidin-4-yl]amino}-1-{[2-(trimethylsilyl)ethoxy]methyl}-1H-pyrazolo[4,3-c]isoquinoline-7-carbonitrile 
• 1253734-16-5 methyl 5-(2,6-difluorophenyl)-3-{[1-(methylsulphonyl)piperidin-4-yl]amino}-1H-pyrazolo[4,3-c]isoquinoline-7-carboxylate 
• 1253734-26-7 methyl 5-(2,6-difluorophenyl)-3-{[1-(methylsulphonyl)piperidin-4-yl]amino}-1-{[2-(trimethylsilyl)ethoxy]methyl}-1H-pyrazolo[4,3-c]isoquinoline-7-carboxylate 
• 1253734-27-8 methyl 5-(2,6-difluorophenyl)-3-{[1-(methylsulphonyl)piperidin-4-yl]amino}-2-{[2-(trimethylsilyl)ethoxy]methyl}-2H-pyrazolo[4,3-c]isoquinoline-7-carboxylate 
• 741713-40-6 Ro 4584820 

Relevant academic research and scientific papers

Heteroaryl compound and application thereof

The invention discloses a heteroaryl compound and application thereof, and provides a heteroaryl compound as shown in a formula I, a tautomer, a stereoisomer or a pharmaceutically acceptable salt thereof. The compound has good tumor inhibition activity, e

Structure-based design of benzo[e]isoindole-1,3-dione derivatives as selective GSK-3β inhibitors to activate Wnt/β-catenin pathway

Deregulation of Wnt/β-catenin pathway is closely related to the pathogenesis of neurodegenerative diseases such as Alzheimer's disease (AD), and glycogen synthase kinase 3β (GSK-3β), the central negative regulator of Wnt pathway, is regarded as an important target for these diseases. Here, we report a series of benzo[e]isoindole-1,3-dione derivatives as selective GSK-3β inhibitors by rational-design and synthesis, which show high selectivity against GSK-3β over Cyclin-dependent kinase 2 (CDK2), and significantly activate the cellular Wnt/β-catenin pathway. The structure-activity relationship of these GSK-3β inhibitors was also explored by in silico molecular docking.

NOVEL 3-(INDOL-3-YL)-PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE

The present invention relates to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.

NOVEL (CYANO-DIMETHYL-METHYL)-ISOXAZOLES AND -[1,3,4]THIADIAZOLES

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

Disclosed are (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

Discovery of [4-amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5- yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity

The cyclin-dependent kinases (CDKs) and their cyclin partners are key regulators of the cell cycle. Since deregulation of CDKs is found with high frequency in many human cancer cells, pharmacological inhibition of CDKs with small molecules has the potential to provide an effective strategy for the treatment of cancer. The 2,4-diamino-5-ketopyrimidines 6 reported here represent a novel class of potent and ATP-competitive inhibitors that selectively target the cyclin-dependent kinase family. This diaminopyrimidine core with a substituted 4-piperidine moiety on the C2-amino position and 2-methoxybenzoyl at the C5 position has been identified as the critical structure responsible for the CDK inhibitory activity. Further optimization has led to a good number of analogues that show potent inhibitory activities against CDK1, CDK2, and CDK4 but are inactive against a large panel of serine/threonine and tyrosine kinases (Ki > 10 μM). As one of these representative analogues, compound 39 (R547) has the best CDK inhibitory activities (Ki = 0.001, 0.003, and 0.001 μM for CDK1, CDK2, and CDK4, respectively) and excellent in vitro cellular potency, inhibiting the growth of various human tumor cell lines including an HCT116 cell line (IC50 = 0.08 μM). An X-ray crystal structure of 39 bound to CDK2 has been determined in this study, revealing a binding mode that is consistent with our SAR. Compound 39 demonstrates significant in vivo efficacy in the HCT116 human colorectal tumor xenograft model in nude mice with up to 95% tumor growth inhibition. On the basis of its superior overall profile, 39 was chosen for further evaluation and has progressed into Phase I clinical trial for the treatment of cancer.

6-Substituted pyrido-pyrimidines

The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.

Imidazo-substituted compounds as p38 kinase inhibitors

The present invention discloses compounds corresponding to formula I: wherein A, Z, Z1, Y, R1 and R2 are as defined in the specification, as well as pharmaceutical formulations, methods of making and uses thereof.