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Details for Patent: 5,827,858

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Details for Patent: 5,827,858

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): Kalish; Vincent J. (San Diego, CA), Reich; Siegfried Heinz (San Diego, CA), Tatlock; John H. (Poway, CA), Rodriguez; Michael J. (Indianapolis, IN)
Assignee: Agouron Pharmaceuticals, Inc. (N/A)
Filing Date:Jun 07, 1995
Application Number:08/478,020
Claims:1. A compound of the formula: ##STR137## 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 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.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 one or more of Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 may be a member of a spiro ring, and 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;

E is carbon or nitrogen;

Q.sub.9 is selected from hydrogen, halogen, hydroxyl, mercapto, and substituted and unsubstituted alkoxyl, aryloxyl, thioether, amino, alkyl, and aryl, where Q.sub.9 may form part of a ring; ##STR138## is a monocyclic or polycyclic carbocycle or heterocycle, which is optionally further substituted, and when ##STR139## is heterocycle, each heterocyclic ring has one to three heteroatoms independently selected from nitrogen, oxygen, and sulfur; and

B.sub.1 and B.sub.2 form part of a ring having from 3 to 5 members, which ring is optionally further substituted and optionally has from one to three heteroatoms independently selected from nitrogen, oxygen, and sulfur; where when ##STR140## is a carbocycle, the ring formed partly by B.sub.1 and B.sub.2 is a heterocycle; or a prodrug or pharmaceutically acceptable salt of said compound.

2. A compound, prodrug, or pharmaceutically acceptable salt according to claim 1, wherein E is carbon.

3. A compound, prodrug, or pharmaceutically acceptable salt according to claim 1, wherein Q.sub.3 is substituted or unsubstituted aryl or thioether.

4. A compound, prodrug, or pharmaceutically acceptable salt according to claim 1, wherein E is nitrogen.

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

6. A pharmaceutical composition comprising:

(a) an active ingredient that is:

(i) a compound of the formula: ##STR141## 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 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.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 one or more of Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 may be a member of a spiro ring, and 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;

E is carbon or nitrogen;

Q.sub.9 is selected from hydrogen, halogen, hydroxyl, mercapto, and substituted and unsubstituted alkoxyl, aryloxyl, thioether, amino, alkyl, and aryl, where Q.sub.9 may form part of a ring; ##STR142## is a monocyclic or polycyclic carbocycle or heterocycle, which is optionally further substituted, and when ##STR143## is heterocycle, each heterocyclic ring has one to three heteroatoms independently selected from nitrogen, oxygen, and sulfur; and

B.sub.1 and B.sub.2 form part of a ring having from 3 to 5 members, which ring is optionally further substituted and optionally has from one to three heteroatoms independently selected from nitrogen, oxygen, and sulfur; where when ##STR144## is a carbocycle, the ring formed partly by B.sub.1 and B.sub.2 is a heterocycle; or

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

(b) a pharmaceutically acceptable carrier.

7. A pharmaceutical composition according to claim 6, wherein E is carbon.

8. A pharmaceutical composition according to claim 6, wherein Q.sub.3 is substituted or unsubstituted aryl or thioether.

9. A pharmaceutical composition according to claim 6, wherein E is nitrogen.

10. A pharmaceutical composition according to claim 6, wherein Q.sub.1 is hydrogen and Q.sub.2 is substituted or unsubstituted alkyl.

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

a compound of the formula: ##STR145## 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 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.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 one or more of Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 may be a member of a spiro ring, and 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;

E is carbon or nitrogen;

Q.sub.9 is selected from hydrogen, halogen, hydroxyl, mercapto, and substituted and unsubstituted alkoxyl, aryloxyl, thioether, amino, alkyl, and aryl, where Q.sub.9 may form part of a ring; ##STR146## is a monocyclic or polycyclic carbocycle or heterocycle, which is optionally further substituted, and when ##STR147## is heterocycle, each heterocyclic ring has one to three heteroatoms independently selected from nitrogen, oxygen, and sulfur; and B.sub.1 and B.sub.2 form part of a ring having from 3 to 5 members, which ring is optionally further substituted and optionally has from one to three heteroatoms independently selected from nitrogen, oxygen, and sulfur; where when ##STR148## is a carbocycle, the ring formed partly by B.sub.1 and B.sub.2 is a heterocycle;

or a prodrug or pharmaceutically acceptable salt of said compound.

12. A method according to claim 11, wherein E is carbon.

13. A method according to claim 11, wherein Q.sub.3 is substituted or unsubstituted aryl or thioether.

14. A method according to claim 11, wherein E is nitrogen.

15. A method according to claim 11, wherein Q.sub.1 is hydrogen and Q.sub.2 is substituted or unsubstituted alkyl.
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