52854-14-5

Usage

Uses

Used in Pharmaceutical Industry:
4-CHLORO-6-METHOXY-5-NITROPYRIMIDINE is used as a key intermediate in the synthesis of drugs, leveraging its biological activity for the development of new therapeutic agents. Its structural versatility allows for the creation of compounds with potential applications in treating various diseases and conditions.
Used in Agricultural Industry:
In the agricultural sector, 4-CHLORO-6-METHOXY-5-NITROPYRIMIDINE is utilized as a precursor in the production of pesticides. Its antimicrobial properties contribute to the development of effective agents for controlling pests and diseases in crops, thereby enhancing agricultural productivity.
Used in Medicinal Chemistry and Drug Discovery:
4-CHLORO-6-METHOXY-5-NITROPYRIMIDINE is employed as a chemical building block in medicinal chemistry for the design and synthesis of novel pyrimidine-based compounds. Its unique structure and biological activity make it a promising candidate for drug discovery, with potential applications in the treatment of various medical conditions.
Overall, 4-CHLORO-6-METHOXY-5-NITROPYRIMIDINE's diverse applications across different industries highlight its importance as a versatile chemical compound with significant potential in pharmaceutical development, agriculture, and medicinal chemistry.

InChI:InChI=1/C5H4ClN3O3/c1-12-5-3(9(10)11)4(6)7-2-8-5/h2H,1H3

Upstream product

• 4316-93-2 4,6-dichloro-5-nitropyrimidine 
• 124-41-4 sodium methylate 
• 67-56-1 methanol 

Downstream Products

• 136038-63-6 1-phenyl-2-methyl-3-ethoxycarbonyl-5-(5'-nitro-6'-methoxypyrimid-4'-yl)oxyindole 
• 136038-67-0 5-(6-Methoxy-5-nitro-pyrimidin-4-yloxy)-1-(4-methoxy-phenyl)-2-methyl-1H-indole-3-carboxylic acid ethyl ester 
• 136038-68-1 1-phenyl-2-dimethylaminomethyl-3-ethoxycarbonyl-5-(5'-nitro-6'-methoxypyrimid-4'-yl)oxyindole 
• 136038-70-5 2-Diethylaminomethyl-5-(6-methoxy-5-nitro-pyrimidin-4-yloxy)-1-phenyl-1H-indole-3-carboxylic acid ethyl ester 
• 136038-72-7 2-Diethylaminomethyl-5-(6-methoxy-5-nitro-pyrimidin-4-yloxy)-1-p-tolyl-1H-indole-3-carboxylic acid ethyl ester 
• 136038-73-8 2-Diethylaminomethyl-5-(6-methoxy-5-nitro-pyrimidin-4-yloxy)-1-(4-methoxy-phenyl)-1H-indole-3-carboxylic acid ethyl ester 
• 77696-41-4 5-nitro-4-methoxy-6-(2,2-diphenylhydrazino)pyrimidine 
• 100114-07-6 (6-methoxy-5-nitro-pyrimidin-4-yl)-methyl-amine 
• 144216-57-9 4-methoxy-5H-pyrrolo<3,2-d>pyrimidine 
• 148214-81-7 5-acetylamino-4-iodo-6-methoxy-2-methylpyrimidine 
• 689298-05-3 3'-(1-methyl-5-nitro-6-oxo-1,6-dihydropyrimidin-4-ylamino)biphenyl-2-carbonitrile 
• 15579-82-5 4-methoxy-pyrimidin-5-ylamine 

Relevant academic research and scientific papers

Discovery of 5-Nitro-6-thiocyanatopyrimidines as Inhibitors of Cryptococcus neoformans and Cryptococcus gattii

Opportunistic infections from pathogenic fungi present a major challenge to healthcare because of a very limited arsenal of antifungal drugs, an increasing population of immunosuppressed patients, and increased prevalence of resistant clinical strains due to overuse of the few available antifungals. Cryptococcal meningitis is a life-threatening opportunistic fungal infection caused by one of two species in the Cryptococcus genus, Cryptococcus neoformans and Cryptococcus gattii. Eighty percent of cryptococcosis diseases are caused by C. neoformans that is endemic in the environment. The standard of care is limited to old antifungals, and under a high standard of care, mortality remains between 10 and 30%. We have identified a series of 5-nitro-6-thiocyanatopyrimidine antifungal drug candidates using in vitro and computational machine learning approaches. These compounds can inhibit C. neoformans growth at submicromolar levels, are effective against fluconazole-resistant C. neoformans and a clinical strain of C. gattii, and are not antagonistic with currently approved antifungals.

C5A RECEPTOR MODULATORS

The present invention relates to derivatives of formula (I) wherein ring A, X, Y, Z, R1, R2, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as C5a receptor modulators.

Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases

New pyridin-2(1h)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

PYRIDIN-2 (1H) -ONE DERIVATIVES USEFUL AS MEDICAMENTS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISORDERS, TRANSPLANT REJECTION, IMMUNE-MEDIATED AND INFLAMMATORY DISEASES

Compoundshaving the chemical structure of formula (I) are disclosed; as well as process for theirpreparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

NITROGENATED FUSED RING DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USE OF THE SAME FOR MEDICAL PURPOSES

[Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, -OW1, -SW1, -COW2, -NW3W4, -SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, -CO-Y, -SO2-Y -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.

7-SUBSTITUTED 3-NITRO-PYRAZOLO `1,5-A! PYRIMIDINES

The present invention relates to compounds of Formula (I): wherein R1 is as defined in the claims. The compounds have specific affinity for the GABAA receptor and are therefore useful in the treatment and prevention of diseases modul

MIDAZOPYRAZINONES AND IMIDAZOTRIAZINONES DERIVATES AS GABA-A RECEPTOR ANXIOLYTIC

The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein -U-V- represents -CH=CH-, or -CH2-CH2-, -N=CH- or -CH=N-; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a -NH- or -OCH2- linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, -SO2Ra, -SO2NRaRb, -CORa, -CO2Ra or -CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group;pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.

Structure-activity relationship of N-[2-(dimethylamino)-6-[3-(5-methyl-4- phenyl-1H-imidazol-1-yl)propoxy]phenyl]-N'-pentylurea and analogues. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity

We have discovered N-butyl-N'-[2-(dimethylamino)-6-[3-(4-phenyl-1H- imidazol-1-yl)propoxy]phenyl]urea (4), a novel, potent, and systemically bioavailable inhibitor of ACAT (acylCoA:cholesterol O-acyltransferase). The structure-activity relationships (SARs) of this lead compound 4 were investigated by systematic modification of four regions in the molecule. The compounds prepared in this study were tested for in vitro inhibitory activity toward both aortic and intestinal ACATs, and selected compounds were further tested for in vivo hypocholesterolemic activity. The studies not only resulted in the discovery of N-[2-(dimethylamino)-6-[3-(5-methyl-4-phenyl- 1H-imidazol-1-yl)propoxy]phenyl]-N'-pentylurea (24), with potent activity and moderate plasma level after oral administration, but also revealed the SAR in each modified region. Four compounds (4, 13, 14, 24) were further selected for testing of in vivo antiatherosclerotic activity; 4, 13, and 24 reduced atherosclerotic plaque development to 38-45% of the control value in terms of area, while 14 did not have a significant antiatherosclerotic effect.