113885-20-4

Upstream product

• 113885-19-1 N-cyanoacetyl-N'-isopropyl-urea 
• 691-60-1 N-isopropylurea 
• 105-34-0 methyl 2-cyanoacetate 
• 105-56-6 ethyl 2-cyanoacetate 

Relevant academic research and scientific papers

SUBSTITUTED XANTHINE DERIVATIVES

The present invention relates to compounds of formula (I) a process for their manufacture, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion ch

SUBSTITUTED XANTHINE DERIVATIVES

The present invention relates to compounds of formula (I) a process for their manufacture, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels. R1, R2, R3, R4 and R5 have meanings given in the description.

NOVEL SUBSTITUTED XANTHINE DERIVATIVES

The present invention relates to substituted xanthine derivatives, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels.

Pteridines. Part CXIX: A new pteridine - Purine transformation

A variety of pyrimidine precursors 12-25 were converted into a series of new 7-hydroxylumazines (=7-hydroxypteridine-2,4(1H,3H)-diones) 26-35 which functioned as starting materials for the transformation into the corresponding 7-chlorolumazines 36-45. Subsequent reaction with hydrazine led to the 7-hydrazinolumazines 46-55 which gave on nitrosation the 7-azidolumazines 1 and 56-64. These compounds were subjected to short heating in xylene whereby 1 and 56-61 showed a new pteridine-purine interconversion in forming a new type of 1,3-disubstituted or 3-substituted xanthin-8-amine-derived nitrilium ylides (2,3,6,7-tetrahydro-N-methylidyne-2,6-dioxo-1H-purin-8-aminium ylides) 11 and 65-70. The presence of an additional 6-alkyl substituent in the 7-azidolumazines 63 and 64 or of an unsubstituted N(3) position in 62 caused further rearrangement to xanthine-9-carbonitriles 71-73. Prolonged heating of 7-azido-1,3-dimethyllumazine (1) also afforded theophylline-9-carbonitrile (=1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-9H-purine-9-carbonitrile; 5). The nitrilium ylide function was established by NMR and UV spectra as well as by elemental analyses. Confirmation of the nitrilium ylide structures was suggested by the result of the heating of 1,3-dimethyl-N-methylidynexanthin-8-aminium ylide 11 in EtOH or of 1 in pentan-1-ol leading to 8-aminotheophylline (=8-amino-3,7-dihydro-1,3-dimethyl-1H-purin-2,6-dione; 74).

XANTHINE DERIVATIVES AS A2B ADENOSINE RECEPTOR ANTAGONISTS

Disclosed are compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

A2B adenosine receptor antagonists

Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

A novel ring closure reaction for the preparation of 6-aminouracils with an α-branched 1-substituent

The preparation of 6-aminouracil derivatives is described involving a novel, silicon-promoted ring closure reaction. Condensation of N-substituted urea with cyanoacetic acid yields cyanoacetylureas, which are heated in hexamethyldisilazane/trimethylchlorosilane to afford N-substituted 6- aminouracils. Previously unaccessible derivatives bearing an α-branched 1- substituent, including 6-amino-1-(1-phenylethyl)uracil were obtained.