287953-38-2

Usage

Uses

Used in Pharmaceutical Industry:
Tert-butyl (1-(Methylsulfonyl)piperidin-4-yl)carbamate is used as a pharmaceutical agent for its potential therapeutic properties. Its unique structure allows it to interact with specific biological targets, making it a promising candidate for the development of new drugs.
Used in Agrochemical Industry:
In the agrochemical industry, tert-butyl (1-(Methylsulfonyl)piperidin-4-yl)carbamate may be utilized in the development of pesticides or other crop protection products. Its chemical properties could contribute to the effectiveness of these products in managing pests and diseases in agriculture.
Used in Specialty Chemicals Industry:
Tert-butyl (1-(Methylsulfonyl)piperidin-4-yl)carbamate may also find applications in the specialty chemicals industry, where its unique structure and properties can be leveraged for specific purposes, such as in the synthesis of other complex organic compounds or as intermediates in chemical reactions.

Upstream product

• 124-63-0 methanesulfonyl chloride 
• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 87120-72-7 1-(tert-butoxycarbonyl)-4-aminopiperidine 

Downstream Products

• 651057-01-1 1-(methylsulfonyl)piperidin-4-amine hydrochloride 
• 741713-40-6 Ro 4584820 
• 402927-97-3 4-amino-1-methanesulfonylpiperidine 

Relevant academic research and scientific papers

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 (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.

HETEROCYCLIC COMPOUND

The present invention provides to a compound having melanin-concentrating hormone receptor antagonistic action and low toxicity, and useful as a agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound re

PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S

The invention provides compounds of the formula (I), or salts, tautomers, N-oxides or solvates thereof wherein: R1 is selected from: (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group R0; (e) a group R a; (f) a group Rlb; (g) a group Rlc; (h) a group Rld; and 0) 2,6-difluorophenylamino ; wherein R )0υ, r R> llaa, T Rj I1bD, T R) I1cC, r R> Iidα, r R?2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdkl or cdk2) and glycogen synthase kinase-3 activity.

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.

2,6-Diaminopyridine derivatives

Novel 2,6-diaminopyridine derivatives of formula wherein R1 and R2 are as defined below, are disclosed. These compounds inhibit cyclin-dependent kinases. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 2,6-diaminopyridine derivatives.