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Claims for Patent: 5,952,343

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Claims for Patent: 5,952,343

Title: HIV protease inhibitors
Abstract:HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
Inventor(s): Dressman; Bruce A. (Indianapolis, IN), Fritz; James E. (Greenwoode, IN), Hornback; William J. (Indianapolis, IN), Kaldor; Stephen W. (Indianapolis, IN), Kalish; Vincent J. (San Diego, CA), Munroe; John E. (Indianapolis, IN), Reich; Siegfried Heinz (San Diego, CA), Tatlock; John H. (Poway, CA), Shepherd; Timothy A. (Indianapolis, IN), Rodriguez; Michael J. (Indianapolis, IN)
Assignee: Agouron Pharmaceuticals, Inc. (
Application Number:08/481,831
Patent Claims: 1. A compound of the formula (1) ##STR132## wherein: Q.sub.1 and Q.sub.2 are independently selected from hydrogen and substituted and unsubstituted alkyl and aryl, and Q.sub.1 and Q.sub.2 may form a ring with G;

Q.sub.3 is selected from mercapto and substituted and unsubstituted alkoxyl, aryloxyl, thioether, amino, alkyl, cycloalkyl, saturated and partially saturated heterocycle, and aryl;

Q.sub.4 -Q.sub.8 are independently selected from hydrogen, hydroxyl, mercapto, nitro, halogen, --O--J, wherein J is a substituted or unsubstituted hydrolyzable group, and substituted and unsubstituted alkoxyl, aryloxyl, thioether, sulfinyl, sulfonyl, amino, alkyl, cycloalkyl, saturated and partially saturated heterocycle, aryl, and L.sub.6 C(O)L.sub.4, wherein L.sub.6 is a single bond, --O or --N, and further wherein L.sub.4 is alkyl, hydroxyl, alkoxyl or hydrogen; and further wherein any one or more of Q.sub.4 -Q.sub.8 may be a member of a spiro ring and any two of Q.sub.4 -Q.sub.8 may together be members of a ring;

Y and G are independently selected from oxygen, --N--H, --N-alkyl, sulfur, selenium, and two hydrogen atoms;

D is nitrogen;

E is carbon or nitrogen;

Q.sub.9 is selected from hydrogen, halogen, hydroxyl, mercapto, and substituted and unsubstituted alkyoxyl, aryloxyl, thioether, amino, alkyl, and aryl, wherein Q.sub.9 may form part of a ring;

A is a carbocycle or heterocycle, which is optionally further substituted, and when A is heterocycle, each ring has from one to three hetero atoms independently selected from nitrogen, oxygen, and sulfur; and

B is ##STR133## wherein B.sub.1 and B.sub.2 form part of a ring having 6 to 10 members, which ring is optionally further substituted and optionally has from one to three hetero atoms indendently selected from nitrogen, oxygen, and sulfur;

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising:

(a) an effective amount of the compound of claim 1; and

(b) a pharmaceutically acceptable carrier therefor.

3. A method of inhibiting HIV protease, comprising administering to a host an effective amount of the compound of claim 1.

4. A compound of the formula: ##STR134## wherein: Q.sub.1 and Q.sub.2 are each independently selected from hydrogen and substituted and unsubstituted alkyl and aryl;

Q.sub.3 is substituted or unsubstituted aryl or thioether;

Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 are each independently selected from hydrogen, hydroxyl, mercapto, nitro, halogen, --O--J, where J is a substituted or unsubstituted hydrolyzable group, and substituted and unsubstituted alkoxyl, aryloxyl, thioether, sulfinyl, sulfonyl, amino, alkyl, cycloalkyl, saturated and partially saturated heterocycle, aryl, and L.sub.6 C(O)L.sub.4, where L.sub.6 is a single bond, --O or --N, and further where L.sub.4 is alkyl, hydroxyl, alkoxyl or hydrogen; and further wherein any two of Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 may together be members of a ring; and

B.sub.1 and B.sub.2 form part of a ring having 6 to 10 members, which ring is optionally substituted and optionally has from one to three hetero atoms independently selected from nitrogen, oxygen, and sulfur;

or a prodrug or pharmaceutically acceptable salt of said compound.

5. A compound, prodrug, or pharmaceutically acceptable salt according to claim 4, wherein the ring formed by part of B.sub.1 and B.sub.2 has 6 members and is carbocyclic.

6. A compound, prodrug, or pharmaceutically acceptable salt according to claim 4, wherein Q.sub.1 is unsubstituted S-phenyl.

7. A compound, prodrug, or pharmaceutically acceptable salt according to claim 4, wherein Q.sub.1 is hydrogen and Q.sub.2 is substituted or unsubstituted alkyl.

8. A compound, prodrug, or pharmaceutically acceptable salt according to claim 4, wherein said compound is an essentially pure stereoisomer.

9. A pharmaceutically acceptable mesylate salt according to claim 4.

10. A compound, prodrug, or pharmaceutically acceptable salt according to claim 7, wherein Q.sub.2 is hydroxy(C.sub.1 -C.sub.4)alkyl.

11. A pharmaceutical composition comprising:

(a) an active ingredient that is:

(i) a compound of the formula: ##STR135## wherein: Q.sub.1 and Q.sub.2 are each independently selected from hydrogen and substituted and unsubstituted alkyl and aryl;

Q.sub.3 is substituted or unsubstituted aryl or thioether;

Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 are each independently selected from hydrogen, hydroxyl, mercapto, nitro, halogen, --O--J, where J is a substituted or unsubstituted hydrolyzable group, and substituted and unsubstituted alkoxyl, aryloxyl, thioether, sulfinyl, sulfonyl, amino, alkyl, cycloalkyl, saturated and partially saturated heterocycle, aryl, and L.sub.6 C(O)L.sub.4, where L.sub.6 is a single bond, --O or --N, and further where L.sub.4 is alkyl, hydroxyl, alkoxyl or hydrogen; and further wherein any two of Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 may together be members of a ring; and

B.sub.1 and B.sub.2 form part of a ring having 6 to 10 members, which ring is optionally substituted and optionally has from one to three hetero atoms independently selected from nitrogen, oxygen, and sulfur; or

(ii) a prodrug or pharmaceutically acceptable salt of said compound; and

(b) a pharmaceutically acceptable carrier.

12. A pharmaceutical composition according to claim 11, wherein the ring formed by part of B.sub.1 and B.sub.2 has 6 members and is carbocyclic.

13. A pharmaceutical composition according to claim 11, wherein Q.sub.1 is unsubstituted S-phenyl.

14. A pharmaceutical composition according to claim 11, wherein Q.sub.1 is hydrogen and Q.sub.2 is substituted or unsubstituted alkyl.

15. A pharmaceutical composition according to claim 11, wherein the compound is an essentially pure stereoisomer.

16. A pharmaceutical composition according to claim 11, wherein said compound, prodrug, or pharmaceutically acceptable salt is a pharmaceutically acceptable mesylate salt.

17. A pharmaceutical composition according to claim 11, wherein the compound is an essentially pure stereoisomer and:

Q.sub.1 is hydrogen and Q.sub.2 is t-butyl;

Q.sub.3 is unsubstituted S-phenyl; and

the ring formed by part of B.sub.1 and B.sub.2 has 6 members and is carbocyclic.

18. A method of inhibiting HIV protease, comprising administering to a host an effective amount of:

a compound of the formula: ##STR136## wherein: Q.sub.1 and Q.sub.2 are each independently selected from hydrogen and substituted and unsubstituted alkyl and aryl;

Q.sub.3 is substituted or unsubstituted aryl or thioether;

Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 are each independently selected from hydrogen, hydroxyl, mercapto, nitro, halogen, --O--J, where J is a substituted or unsubstituted hydrolyzable group, and substituted and unsubstituted alkyoxyl, aryloxyl, thiether, sulfinyl, sulfonyl, amino, alkyl, cycloalkyl, saturated and partially saturated heterocycle, aryl, and L.sub.6 C(O)L.sub.4, where L.sub.6 is a single bond, --O or --N, and further where L.sub.4 is alkyl, hydroxyl, alkoxyl or hydrogen; and further wherein any two of Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 may together be members of a ring; and

B.sub.1 and B.sub.2 form part of a ring having 6 to 10 members, which ring is optionally substituted and optionally has from one to three hetero atoms independently selected from nitrogen, oxygen, and sulfur;

or a prodrug or pharmaceutically acceptable salt of said compound.

19. A method according to claim 18, wherein the ring formed by part of B.sub.1 and B.sub.2 has 6 members and is carbocyclic.

20. A method according to claim 18, wherein Q.sub.3 is unsubstituted S-phenyl.

21. A method according to claim 18, wherein Q.sub.1 is hydrogen and Q.sub.2 is substituted or unsubstituted alkyl.

22. A method according to claim 18, wherein the compound is an essentially pure stereoisomer.

23. A method according to claim 18, wherein said compound, prodrug, or pharmaceutically acceptable salt is a pharmaceutically acceptable mesylate salt.

24. A method according to claim 18, wherein the compound is an essentially pure stereoisomer and:

Q.sub.1 is hydrogen and Q.sub.2 is t-butyl;

Q.sub.3 is unsubstituted S-phenyl; and

the ring formed by part of B.sub.1 and B.sub.2 has 6 members and is carbocyclic.
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