Compounds and methods for treating AIDS and HIV infections
Macrocycle containing carbamate compounds that inhibit HIV proteolytic enzymes and processes for preparing them are described. Compositions and methods for treating a patient infected with HIV are described.
1. A compound of the formula
or a pharmaceutically acceptable salt thereof; wherein
R 2 and R 3 are hydrogen;
R 5 is arylalkyl, which is optionally substituted;
X 4 is SO 2 ;
X 5 is oxygen;
L 1 and L 2 are independently alkylene, which is optionally substituted;
W is (H)C═C(H);
Q 2 is substituted aryl; and
Z is a bicyclic heterocycle, which is optionally substituted.
2. The compound of claim 1 wherein L 1 is CH 2 (CH 2 ) m CH 2 ; L 2 is CH 2 (CH 2 ) n CH 2 ; m is from 0 to about 4; and n is from 0 to about 4.
3. The compound of claim 1 wherein L 1 is CH 2 CH 2 CH 2 CH 2 .
4. The compound claim 2 wherein m is 2; and n is 0.
5. The compound of claim 1 wherein Z is a bicycle heterocycle comprising at least one oxygen.
6. The compound of claim 1 wherein Z has the formula,
which is optionally substituted, wherein
* indicates the point of attachment; t is 0 to 4;
W 1 is optionally substituted alkylene;
W 2 represents optionally substituted alkylene; and
W 3 is optionally substituted alkylene.
7. The compound of claim 1 wherein Z has formula
where * indicates the point of attachment.
8. The compound of claim 1 wherein R 5 is optionally substituted benzyl.
9. The compound of claim 1 wherein Q 2 is substituted 1,2-phenylene.
10. The compound of claim 1 wherein Q 2 is 4-methoxy-1,2-phenylene.
11. The compound of claim 1 which is a compound of the formula
wherein R is selected from the group consisting of
12. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 and one or more of a carrier, diluent, excipient therefor, or a combination thereof.
13. A method for treating a patient in need of relief from HIV/AIDS disease, the method comprising the step of administering to the patient a therapeutically effective amount of the compound of claim 1 .
14. The compound of claim 1 having the formula:
or a pharmaceutically acceptable salt thereof.
15. The compound of claim 1 having the formula:
or a pharmaceutically acceptable salt thereof.