IP Library Granted Patent US 8,816,122
Granted Patent B2
US 8,816,122 · App. 12/839,808 · Granted Aug 26, 2014

Prostratin analogs, bryostatin analogs, prodrugs, synthetic methods, and methods of use

Inventors: Paul A. Wender (Menlo Park, CA); Lars V. Heumann (Redwood City, CA); Rainer Kramer (Freiburg im Bresigau, DE); Carolyn Gauntlett (Singapore, SG); Elizabeth Mieuli (Redwood City, CA); Dennis Fournogerakis (Stanford, CA); Pierre-Luc Boudreault (Sherbrooke, CA); Adam Schrier (Redwood City, CA); Brian DeChristopher (Mountain View, CA)
Assignee: The Board of Trustees of the Leland Stanford Junior University
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Quick Facts
Patent No.
US 8,816,122
App. No.
12/839,808
Granted
Aug 26, 2014
Kind
B2
Abstract

Embodiments of the present disclosure provide for prostratin analogs, bryostatin analogs, prodrugs of prostratin and prostratin analogs, methods of making prostratin analogs, and methods of making prodrugs of prostratin and prostratin analogs, methods of use of prostratin analogs, bryostatin analogs, and prodrugs thereof, and the like.

Claims (14)

1. A compound according to the formula:

wherein X in each instance is independently selected from: O, S, and N;

wherein R 1 is a mono- or di-substituent, depending on X, selected from: H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted biaryl, substituted or unsubstituted fused aryl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;

wherein R2 is a mono- or di-substituent, depending on X, and is H; and

wherein R3 is a mono- or di-substituent selected from: H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted biaryl, substituted or unsubstituted fused aryl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl, alkoxy, acetoxy, phenyloxy, alkylthio, phenylthio, halogen, alkylamino, or diphenylamino,

wherein when X in XR 1 is 0, then R1 is —C(═O)CH 2 -FMA, or —C(═O)CH(CH 3 )-FMA, where FMA is selected from the group consisting of: an unsubstituted heteroaryl, substituted or unsubstituted fused aryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted biaryl,

or R 1 is —C(═O)-FMA, then FMA is selected from the group consisting of: a substituted or unsubstituted heteroaryl, substituted or unsubstituted fused aryl, substituted cycloalkyl, and substituted or unsubstituted biaryl.

2. The compound according to claim 1 , where X is O.

3. The compound according to claim 1 , where the compound has a protein kinase C stimulatory activity.

4. The composition of claim 1 , wherein one of the X groups is selected from: S and N, and wherein the other of the X groups is selected from: O, S, and N.

5. A compound according to Formula II described below:

wherein R is selected from the group consisting of: substituted cycloalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted biaryl, and substituted or unsubstituted fused aryl.

6. The compound of claim 1 , wherein when X in XR 1 is O, then R 1 is —C(═O)CH(CH 3 )-FMA, where FMA is selected from the group consisting of: heteroaryl, substituted or unsubstituted fused aryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted biaryl.

7. The compound of claim 1 , where R3 is selected from: substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted biaryl, substituted or unsubstituted fused aryl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl, alkoxy, acetoxy, phenyloxy, alkylthio, phenylthio, halogen, alkylamino, or diphenylamino.

Assignments (2)
CONFIRMATORY LICENSE Recorded Sep 28, 2011
From: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 026979/0275 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2010
From: WENDER, PAUL A.; HEUMANN, LARS V.; KRAMER, RAINER; GAUNTLETT, CAROLYN; MIEULI, ELIZABETH; FOURNOGERAKIS, DENNIS; BOUDREAULT, PIERRE-LUC; SCHRIER, ADAM; DECHRISTOPHER, BRIAN
To: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
Reel/Frame 024954/0056 →
Continuity (2)
Provisional Application 61226802 · Jul 20, 2009
Related Publication 20110014699A1 · Jan 20, 2011