37454-52-7

Upstream product

• 110-91-8 morpholine 
• 51-20-7 5-bromouracil 
• 2435-76-9 5-diazouracil 
• 132785-87-6 5-Diazo-6-morpholin-4-yl-dihydro-pyrimidine-2,4-dione 

Downstream Products

• 280582-23-2 4-(2,4-dichloropyrimidin-5-yl)morpholine 

Relevant academic research and scientific papers

Novel 4-substituent-N-(1-substituent-1H-pyrazol-4-yl)-5-morpholinopyrimidin-2-amine derivatives and use thereof

A novel 4 -substituted - N N - (1-substituted - 111H-pyra -4 - yl) -5 - morpholinopyrimidine -2 - amine derivative compound or a pharmaceutically acceptable salt thereof. A pharmaceutical composition for preventing or treating JAK3-related diseases and a method for preventing or treating JAK3-related diseases using the same as an active ingredient are provided.

ACID CERAMIDASE INHIBITORS AND THEIR USE AS MEDICAMENTS

The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I

ACID CERAMIDASE INHIBITORS AND THEIR USE AS MEDICAMENTS

The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I

Discovery of a new class of highly potent inhibitors of acid ceramidase: Synthesis and structure-activity relationship (SAR)

Acid ceramidase (AC) is an intracellular cysteine amidase that catalyzes the hydrolysis of the lipid messenger ceramide. By regulating ceramide levels in cells, AC may contribute to the regulation of cancer cell proliferation and senescence and to the response to cancer therapy. We recently identified the antitumoral agent carmofur (4a) as the first nanomolar inhibitor of intracellular AC activity (rat AC, IC50 = 0.029 μM). In the present work, we expanded our initial structure-activity relationship (SAR) studies around 4a by synthesizing and testing a series of 2,4-dioxopyrimidine-1- carboxamides. Our investigations provided a first elucidation of the structural features of uracil derivatives that are critical for AC inhibition and led us to identify the first single-digit nanomolar inhibitors of this enzyme. The present results confirm that substituted 2,4-dioxopyrimidine-1-carboxamides are a novel class of potent inhibitors of AC. Selected compounds of this class may represent useful probes to further characterize the functional roles of AC.

Synthesis of substituted uracils by the reactions of halouracils with selenium, sulfur, oxygen and nitrogen nucleophiles under focused microwave irradiation

Under microwave irradiation, the nucleophilic substitution reactions of halouracils with selenium, sulfur, oxygen and nitrogen nucleophiles was complete within several minutes with yields up to 99%. The method using microwave irradiation is superior to th

INDAZOLINONE COMPOSITIONS USEFUL AS KINASE INHIBITORS

The present invention provides compounds of formula (I): These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.

Thermal and Rhodium Acetate Catalyzed Reactions of 5-Diazouracil with Nucleophiles

In the presence of rhodium acetate 5-diazouracil reacts with varied secondary amines, azoles and thiols to give 5-substituted-uracils efficiently.