IP Library Granted Patent US 10,316,023
Granted Patent B2
US 10,316,023 · App. 15/449,706 · Granted Jun 11, 2019

Therapeutic compounds and uses thereof

Inventors: Brian K. Albrecht (Cambridge, MA); Alexandre Cote (Cambridge, MA); Terry Crawford (South San Francisco, CA); Martin Duplessis (Cambridge, MA); Andrew Charles Good (Cambridge, MA); Yves LeBlanc (Cambridge, MA); Steven Magnuson (South San Francisco, CA); Christopher G. Nasveschuk (Cambridge, MA); Richard Pastor (South San Francisco, CA); F. Anthony Romero (South San Francisco, CA); Alexander M. Taylor (Cambridge, MA)
Assignees: GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS, INC.
C07D403/12A61K31/53A61K45/06A61P35/00C07D249/12C07D253/075C07D401/04C07D401/12C07D403/04
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Quick Facts
Patent No.
US 10,316,023
App. No.
15/449,706
Granted
Jun 11, 2019
Kind
B2
Abstract

The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R 1 , R 3 -R 6 , X, and each R e have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Claims (22)

1. A compound of formula (I), or a salt thereof:

wherein:

R 1 is selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and carbocyclyl;

R 3 is selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and carbocyclyl;

and the group:

is selected from the group consisting of:

provided that when R 1 is methyl, R 3 is methyl, X is N(H), R 4 is H, R 6 is H and each Re is CH 3 ;

then R 5 is not phenyl; and

provided the compound is not:

or a salt thereof.

2. The compound of claim 1 wherein the group:

is selected from the group consisting of:

3. The compound or salt of claim 1 , which is selected from the group consisting of:

or a salt thereof.

4. A composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof

and a pharmaceutically acceptable adjuvant, carrier, or vehicle.

5. A method for treating ovarian cancer or renal cell carcinoma in an animal comprising administering to the animal a compound of claim 1 or a pharmaceutically acceptable salt thereof.

6. A method of treating ovarian cancer or renal cell carcinoma in an individual comprising administering to the individual (a) a compound of claim 1 or a pharmaceutically acceptable salt thereof, and (b) a cytotoxic agent.

7. The compound of claim 1 , wherein R 1 is methyl.

8. The compound of claim 1 , wherein R 3 is methyl.

9. A method of treating ovarian cancer or renal cell carcinoma in an animal comprising administering to the animal a compound of formula:

or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 22, 2019
From: ALBRECHT, BRIAN K.; COTE, ALEXANDRE; DUPLESSIS, MARTIN; GOOD, ANDREW CHARLES; LEBLANC, YVES; NASVESCHUK, CHRISTOPHER C.; TAYLOR, ALEXANDER M.
To: CONSTELLATION PHARMACEUTICALS, INC.
Reel/Frame 048679/0213 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 22, 2019
From: CRAWFORD, TERRY; MAGNUSON, STEVEN; PASTOR, RICHARD; ROMERO, F. ANTHONY
To: GENENTECH, INC.
Reel/Frame 048679/0262 →
Continuity (3)
Continuation PCTUS2015048174 · Sep 2, 2015
Provisional Application 62046770 · Sep 5, 2014
Related Publication 20170334883A1 · Nov 23, 2017