650579-82-1

Upstream product

• 214834-18-1 tert-butyl 4-carbamothioylpiperidine-1-carboxylate 
• 534-07-6 1,3-Dichloroacetone 
• 864068-79-1 tert- butyl 4-(4-(hydroxymethyl)thiazol-2-yl)piperidine-1-carboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 91419-48-6 4-carbamoyl-piperidine-1-carboxylic acid tert-butyl ester 
• 39546-32-2 4-carboxamidopiperidine 

Downstream Products

• 1037793-62-6 4-[4-(4-methanesulfonylbenzyloxymethyl)thiazol-2-yl]piperidine-1-carboxylic acid tert-butyl ester 
• 1037791-19-7 4-[4-(4-methanesulfonylphenoxymethyl)thiazol-2-yl]piperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Novel heterocyclic amide piperidine derivative as well as preparation method and application thereof in hypoglycemic drugs

The invention belongs to the technical field of drug synthesis, and particularly relates to a novel heterocyclic amide piperidine derivative and a preparation method thereof, and application of the derivative as a GPR119 agonist in hypoglycemic drugs. An MTT experiment shows that the novel heterocyclic amide piperidine derivative synthesized by the research group has the prospect of developing the hypoglycemic drugs.

Design and biological evaluation of tetrahydropyridine derivatives as novel human GPR119 agonists

A series of novel tetrahydropyridine derivatives were prepared and evaluated using cell-based measurements. Systematic optimization of general structure G-1 led to the identification of compound 35 (EC50 = 4.9 nM) and 37 (EC50 = 8.8 nM) with high GPR119 agonism activity and moderate clog P. Through single and long-term pharmacodynamic experiments, we found that compound 35 showed a hypoglycemic effect and may have an effect on improving basal metabolic rate in DIO mice. Both in vitro and in vivo tests indicated that compound 35 was a potential potent GPR119 agonist in allusion to T2DM treatment.

OXYMETHYLENE ARYL COMPOUNDS FOR TREATING INFLAMMATORY GASTROINTESTINAL DISEASES OR GASTROINTESTINAL CONDITIONS

Use of oxymethylene aryl GPRl 19 agonists, and optionally DPP IV inhibitors and optionally metformin, for the treatment of inflammatory gastrointestinal diseases or gastrointestinal conditions involving malabsorption of nutrients and/or fluids are provide

Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists

A series of 4-(phenoxymethyl)thiazole derivatives was synthesized and evaluated for their GPR119 agonistic effect. Several 4-(phenoxymethyl)thiazoles with pyrrolidine-2,5-dione moieties showed potent GPR119 agonistic activities. Among them, compound 27 and 32d showed good in vitro activity with an EC50 value of 49 nM and 18 nM, respectively with improved human and rat liver microsomal stability compare with MBX-2982. Compound 27 & 32d did not exhibit significant CYP inhibition, hERG binding, and cytotoxicity. Moreover, these compounds lowered the glucose excursion in mice in an oral glucose-tolerance test.

Receptor-Type Kinase Modulators and Methods of Use

The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases

PREPARATION OF 5-ETHYL-2-{4-[4-(4-TETRAZOL-1-YL-PHENOXYMETHYL)-THIAZOL-2-YL]-PIPERIDIN-1-YL}-PYRIMIDINE

Processes and intermediates for the synthesis of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine are provided.

COMPOSITIONS OF 5-ETHYL-2--PYRIMIDINE

This invention relates to the field of pharmaceutical chemistry and, more specifically, to pharmaceutical formulations as well as to intermediates used to prepare such formulations and to methods for manufacturing such formulations.

HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS

Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.

FUNGICIDAL AMIDES

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, insert Formula 1 here wherein R1, R2, A, G, W1, Q, X, Z, and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.