 Treatment of sexual dysfunction in certain patient groups |
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| Treatment of sexual dysfunction in certain patient groups |
| OF THE INVENTION The present invention relates to methods for the treatment of sexual dysfunction ... |
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| OF THE INVENTION It is believed that one skilled in the art can, based on the description herein, ... |
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| OF THE INVENTION The technetium compounds of the present invention which have been found most ... |
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Antiproliferative substituted 5-thiapyrimidinone and 5-selenopyrimidinone compounds
| Details |
Inventors: Varney, Michael D.; Romines, William H.; Palmer, Cynthia L.; Deal, Judith G.;
Assignee: Agouron Pharmaceuticals, Inc. (La Jolla, CA)
Primary Examiner: Raymond; Richard L.
Assistant Examiner: Rao; Deepak R.
Attorney, Agent or Firm: Fitzpatrick, Cella, Harper & Scinto
Novel derivatives of 5-thia- and 5-selenopyrimidinone are sound to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents. |
|
DETAILED DESCRIPTION What is claimed is: 1.
A compound having the formula I ##STR39## wherein: A represents sulfur or selenium; Z represents a substituted or unsubstituted mono- or fused or nonfused poly-carbocyclic or heterocyclic radical; R.
sub.
1 and R.
sub.
2 represent, independently, H or C.
sub.
1 to C.
sub.
6 alkyl or other readily lyzable groups; and R.
sub.
3 represents H or a straight, branched or cyclic C.
sub.
1 to C.
sub.
6 alkyl group optionally carrying one or more halogen, hydroxyl or amine groups; or a pharmaceutically acceptable salt thereof.
2.
An antiproliferative composition comprising a compound having the formula I: ##STR40## wherein: A represents sulfur or selenium; Z represents a substituted or unsubstituted-mono- or fused or nonfused poly-carbocyclic or heterocyclic radical; R.
sub.
1 and R.
sub.
2 represent, independently, H, C.
sub.
1 to C.
sub.
6 alkyl or other readily lyzable groups; and R.
sub.
3 represents H or straight, branched or cyclic C.
sub.
1 to C.
sub.
6 alkyl group optionally carrying one or more halogen, hydroxyl or amine groups; or a pharmaceutically acceptable salt thereof; in combination with a pharmaceutically acceptable carrier.
3.
A process for inhibiting the growth and proliferation of the cells of microorganisms and of higher organisms, which process comprises administering to a host in need of such treatment an effective amount of a compound having the structural formula I ##STR41## wherein: A represents sulfur or selenium; Z represents a substituted or unsubstituted mono- or fused or nonfused poly-carbocyclic or heterocyclic radical; R.
sub.
1 and R.
sub.
2 represent, independently, H, C.
sub.
1 to C.
sub.
6 alkyl or other readily lyzable groups; and R.
sub.
3 represents H or straight, branched or cyclic C.
sub.
1 to C.
sub.
6 alkyl group optionally carrying one or more halogen, hydroxyl or amine groups; or a pharmaceutically acceptable salt thereof.
4.
A process for inhibiting GARFT comprising the step of administering to a host in need of such inhibition an effective amount of a compound having the formula I: ##STR42## wherein: A represents sulfur or selenium; Z represents a substituted or unsubstituted mono- or fused or nonfused poly-carbocyclic or heterocyclic radical; R
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Vasodialators 
