220655-09-4

Usage

Uses

Used in Pharmaceutical Industry:
TERT-BUTYL THIOMORPHOLINE-4-CARBOXYLATE is used as a reactant for the preparation of aromatic heterocyclic ureas, which are known for their anti-inflammatory properties. These compounds are valuable in the development of medications aimed at reducing inflammation and alleviating pain associated with various conditions, such as arthritis, tendinitis, and other inflammatory disorders.

Upstream product

• 123-90-0 Thiomorpholin 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 73286-70-1 N-(tert-butoxycarbonyl)-3-pyrroline 
• 39093-93-1 thiomorpholine 1,1-dioxide 
• 278788-74-2 tert-butyl thiomorpholine-4-carboxylate-1-oxide 
• 215791-95-0 tert-butyl thiomorpholine-4-carboxylic acid-1,1-dioxide 

Relevant academic research and scientific papers

HETEROCYCLIC COMPOUNDS

Provided herein are compounds of formula (I) which comprise a thiomorpholine 1,1-dioxide or 1-imino-thiomorpholine 1-oxide moiety, or pharmaceutically acceptable salts of any of the foregoing, pharmaceutical compositions that include a compound described herein (including salts of the compound) and methods of synthesizing the same. Also provided are methods of treating Hepatitis B viral (HBV) infections using a compound of formula (I), or pharmaceutically acceptable salts thereof.

Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria

We previously discovered a series of novel biaryloxazolidinone analogues bearing a hydrazone moiety with potent antibacterial activity. However, the most potent compound OB-104 exhibited undesirable chemical and metabolic instability. Herein, novel biaryloxazolidinone analogues were designed and synthesized to improve the chemical and metabolic stability. Compounds 6a-1, 6a-3, 14a-1, 14a-3 and 14a-7 showed significant antibacterial activity against the tested Gram-positive bacteria as compared to radezolid and linezolid. Further studies indicated that most of them exhibited improved water solubility and chemical stability. Compound 14a-7 had MIC values of 0.125–0.25 μg/mL against all tested Gram-positive bacteria, and showed excellent antibacterial activity against clinical isolates of antibiotic-susceptible and antibiotic-resistant bacteria. Moreover, it was stable in human liver microsome. From a safety viewpoint, it showed non-cytotoxic activity against hepatic cell and exhibited lower inhibitory activity against human MAO-A compared to linezolid. The potent antibacterial activity and all these improved drug-likeness properties and safety profile suggested that compound 14a-7 might be a promising drug candidate for further investigation.

PYRROLIDINE GLYCOSIDASE INHIBITORS

Compounds of formula (I) wherein A, W, R3b, Z and p have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.

Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents

A series of linezolid analogues containing a hydrazone moiety were designed, synthesized and evaluated for their antibacterial activity. Most compounds exhibited more potent antibacterial activity against S.aureus, MRSA, MSSA, LREF and VRE pathogens as compared with linezolid and radezolid. Compounds 9a, 9c, 9f, 9g, 10m and 10t were more potent against tested clinical isolates of MRSA, MSSA, VRE and LREF as compared to linezolid. Compound 9a exhibited comparable activity with linezolid against human MAO-A for safety evaluation and showed moderate metabolism in human liver microsome. The most promising compound 9a showed remarkable antibacterial activity against S.aureus, MRSA, MSSA, LREF and VRE pathogens with MIC value of 0.0675 mg/mL, respectively, which was 15- to 30-fold more potent than linezolid.

Neurotrophic factor tyrosine kinase receptor inhibitor

The invention provides a neurotrophic factor tyrosine kinase receptor inhibitor. The tyrosine kinase receptor inhibitor provided by the invention has a tricyclic parent core structure, can inhibit theactivity of Trk kinase and can be used for treating mammalian diseases mediated by the Trk kinase.

Novel Potent Proline-Based Metalloproteinase Inhibitors: Design, (Radio)Synthesis, and First in Vivo Evaluation as Radiotracers for Positron Emission Tomography

As dysregulation of matrix metalloproteinase (MMP) activity is associated with a wide range of pathophysiological processes like cancer, atherosclerosis, and arthritis, MMPs represent a valuable target for the development of new therapeutics and diagnostic tools. We herein present the chiral pool syntheses, in vitro evaluation, and SAR studies of a series of d- and l-proline- as well as of (4R)-4-hydroxy-l-proline-derived MMP inhibitors possessing general formula 1. Some of the synthesized hydroxamic acids were found to be potent MMP inhibitors with IC50 values in the nanomolar range, also demonstrating no off-target effects toward the other tested Zn2+-dependent metalloproteases (ADAMs and meprins). Utilizing the structure of the (2S,4S)-configured 4-hydroxyproline derivative 4, a selective picomolar inhibitor of MMP-13, the radiolabeled counterpart [18F]4 was successfully synthesized. The radiotracer's biodistribution in mice as well as its serum stability were evaluated for assessing its potential use as a MMP-13 targeting PET imaging agent.

Salt, resist composition and a manufacturing method of a resist pattern

PROBLEM TO BE SOLVED: To provide a salt capable of obtaining a resist pattern having excellent focus margin, to provide an acid generator, and to provide a resist composition etc.SOLUTION: The salt is represented by formula (I) [wherein, Ris hydroxy or al

SUBSTITUTED NICOTINAMIDE DERIVATIVES AS KINASE INHIBITORS

The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Heterobicyclic thiophene compounds and methods of use

Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Quinolinone-carboxamide compounds

The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.