41103-17-7

Usage

Uses

Used in Pharmaceutical Industry:
4-Chloro-pyrimidine-5-carboxylic acid ethyl ester is used as a synthetic reagent for the development of novel orally active non-peptide angiotensin II antagonists. These antagonists are important in the treatment of hypertension and other cardiovascular diseases by blocking the effects of angiotensin II, a potent vasoconstrictor.
In the synthesis process, the compound's ester group can be hydrolyzed to form the corresponding carboxylic acid, which can then be further modified to create the desired angiotensin II antagonists. The chlorinated pyrimidine core provides a versatile scaffold for the attachment of various functional groups, allowing for the fine-tuning of the biological activity and pharmacokinetic properties of the resulting compounds.

InChI:InChI=1/C7H7ClN2O2/c1-2-12-7(11)5-3-9-4-10-6(5)8/h3-4H,2H2,1H3

Upstream product

• 4786-52-1 ethyl 4-hydroxypyrimidine-5-carboxylate 
• 87-13-8 diethyl 2-ethoxymethylenemalonate 
• 105-53-3 diethyl malonate 
• 4786-52-1 ethyl 3,4-dihydro-4-oxopyrimidine-5-carboxylate 

Downstream Products

• 84332-00-3 methyl 4-methoxypyrimidine-5-carboxylate 
• 143631-76-9 4-{[2'-(2-Trityl-2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-pyrimidine-5-carboxylic acid ethyl ester 
• 143618-35-3 4-{Butyl-[2'-(2-trityl-2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-pyrimidine-5-carboxylic acid ethyl ester 
• 6454-67-7 ethyl 4-(3-trifluoromethylanilino)pyrimidine-5-carboxylate 
• 1328624-09-4 ethyl 4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)pyrimidine-5-carboxylate 
• 1352805-02-7 4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)pyrimidine-5-carboxylic acid 
• 1328624-10-7 methyl 2-((4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)pyrimidin-5-carbnyl)amino)-3-hydroxypropanoate 
• 885685-56-3 lithium 4-{[20(tritylthio)ethyl]amino}pyrimidine-5-carboxylate 

Relevant academic research and scientific papers

HETEROCYCLIC COMPOUND AND USE THEREOF

Provided is a heterocyclic compound that can have an antagonistic action on an NMD A receptor containing the NR2B subunit and that is expected to be useful as a prophylactic or therapeutic agent for depression, bipolar disorder, migraine, pain, peripheral symptoms of dementia and the like. A compound represented by the formula (I), wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.

Hetero-aromatic compound and its use in medicine

The invention provides a hetero-aromatic compound or a stereisomer, geometric isomer, tautomer, despinner, nitrogen oxide, hydrate, solvate, metabolite, metabolism precursor and pharmaceutically acceptable salt or prodrug thereof, which is used for treating proliferative diseases. The invention also discloses a pharmaceutical composition containing the compound and an application of the compound or pharmaceutical composition thereof in preparation of a medicine for treating proliferative diseases.

Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists

4-Phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists are reported. Several 4-phenoxynicotinamide derivatives were found to activate human and mouse TGR5 (hTGR5 and mTGR5) with EC50 values in the low nanomolar range. Compound 23g, with an EC50 value of 0.72 nM on hTGR5 and an EC 50 value of 6.2 nM on mTGR5, was selected for further in vivo efficacy studies. This compound exhibited a significant dose-dependent glucagon-like peptide-1 (GLP-1) secretion effect. A single oral dose of 23g (50 mg/kg) significantly reduced blood glucose levels in db/db mice and caused a 49% reduction in the area under the blood glucose curve (AUC)0-120min following an oral glucose tolerance test (OGTT) in imprinting control region (ICR) mice. However, 23g stimulated gallbladder filling, which might result in side effects to the gallbladder.

Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors

11β-HSD1 is increasingly seen as an attractive target for the treatment of type II diabetes and other elements of the metabolic syndrome. In this program of work we describe how a series of neutral 2-thioalkyl-pyridine 11β-HSD1 inhibitors were optimized in terms of their pharmacokinetic properties to give compounds with excellent bioavailability in both rat and dog through a core change to pyrimidine. A potential reactive metabolite issue with 4-thioalkyl-pyrimidines was circumvented by a switch from sulfur to carbon substitution.

NOVEL PYRIMIDINE DERIVATIVE FOR INHIBITING THE GROWTH OF CANCER CELLS

The present invention provides a novel pyrimidine derivative or pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same, which can effectively inhibit the growth of cancer cells induced by the overexpression of EGFR incl

AZA-BENZOFURANYL COMPOUNDS AND METHODS OF USE

The invention relates to azabenzofuranyl compounds of Formula (I) with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzofuranyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

PITUITARY ADENYLATE CYCLASE ACTIVATING PEPTIDE (PACAP) RECEPTOR (VPAC2) AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE

This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These modified peptides function in vivo as agonists of the VPAC2 receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.

GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE

This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These GLP-1 modified peptides function in vivo as agonists of the GLP-1 receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.

GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE (GIP) RECEPTOR AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE

This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These modified peptides function in vivo as agonists of the GIP receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.

NEUROPEPTIDE Y4 RECEPTOR AGONISTS

This invention provides peptides that act as selective NPY4 receptor agonists in vitro and are efficacious in vivo to reduce food intake. The invention is a peptide selected from a specific group of derivatized PP-related peptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the peptides to said mammal to reduce food intake and body weight.