155272-05-2Relevant academic research and scientific papers
An efficient route to xanthine based A2A adenosine receptor antagonists and functional derivatives
Labeaume, Paul,Dong, Ma,Sitkovsky, Michail,Jones, Elizabeth V.,Thomas, Rhiannon,Sadler, Sara,Kallmerten, Amy E.,Jones, Graham B.
supporting information; experimental part, p. 4155 - 4157 (2010/10/21)
A one-pot route to 8-substituted xanthines has been developed from 5,6-diaminouracils and carboxaldehydes. Yields are good and the process applicable to a range of substrates including a family of A2A adenosine receptor antagonists. A new route to the KW-6002 family of antagonists is presented including a pro-drug variant, and application to related image contrast agents developed.
Synthesis of 8-substituted xanthines via 5,6-diaminouracils: an efficient route to A2A adenosine receptor antagonists
Dong, Ma,Sitkovsky, Mikhail,Kallmerten, Amy E.,Jones, Graham B.
, p. 4633 - 4635 (2008/09/21)
A one-pot route to 8-substituted xanthines has been developed from 5,6-diaminouracils and carboxaldehydes. The process, promoted by (bromodimethyl)sulfonium bromide, is mild and efficient and eliminates the need for external oxidants. Yields are good and the process is applicable to a range of substrates including a family of A2A adenosine receptor antagonists. Preparation of a new analog of the antagonist KW-6002 is presented, and in situ bromination of aryl substituted products demonstrated.
Xanthine derivatives
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, (2008/06/13)
The present invention relates to novel xanthine derivatives and pharmaceutically acceptable salts thereof, represented by Formula (I): STR1 wherein R1, R2, and R3 independently represent hydrogen, lower alkyl, lower alkeny
Antidepressants
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, (2008/06/13)
The present invention relates to an antidepressant containing as an active ingredient a xanthine derivative or a pharmaceutically acceptable salt thereof, the xanthine derivative being represented by Formula (I) : STR1 in which R1, R2, and R3 represent independently hydrogen, lower alkyl, lower alkenyl; R4 represents cycloalkyl, --(CH2)n --R5 (in which R5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4), or STR2 (in which Y1 and Y2 represent independently hydrogen, halogen or lower alkyl; and Z represents substituted or unsubstituted aryl, STR3 (in which R6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m represents an integer of 1 to 3), or a substituted or unsubstituted heterocyclic group); and X1 and X2 represent independently O or S.
Therapeutic agent for Parkinson's disease
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, (2008/06/13)
Agents for the treatment of Parkinson''s disease contain, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: STR1 in which R 1, R 2 are R 3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R 4 represents cycloalkyl, --(CH 2) n --R 5 (in which R 5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4), or STR2 in which Y 1 and Y 2 represent independently hydrogen, halogen, or lower alkyl; and Z represents substituted or unsubstituted aryl, STR3 in which R 6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m represents an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X 1 and X 2 represent independently O or S.
