US 12,077,530 B2
Chemical compounds
Bernard Christophe Barlaam, Cambridge (GB); Daniel Hillebrand O'Donovan, Cambridge (GB); Samantha Jayne Hughes, Cambridge (GB); Thomas Andrew Moss, Cambridge (GB); Johannes Wilhelmus Maria Nissink, Cambridge (GB); James Stewart Scott, Cambridge (GB); and Bin Yang, Waltham, MA (US)
Assigned to ASTRAZENECA AB, Södertälje (SE)
Filed by AstraZeneca AB, Sodertalje (SE)
Filed on Feb. 17, 2021, as Appl. No. 17/177,617.
Application 17/177,617 is a continuation of application No. 16/774,268, filed on Jan. 28, 2020, granted, now 10,961,241.
Application 16/774,268 is a continuation of application No. 16/155,041, filed on Oct. 9, 2018, granted, now 10,590,130.
Application 16/155,041 is a continuation of application No. 15/782,904, filed on Oct. 13, 2017, granted, now 10,131,663, issued on Nov. 20, 2018.
Claims priority of provisional application 62/435,159, filed on Dec. 16, 2016.
Claims priority of provisional application 62/411,799, filed on Oct. 24, 2016.
Prior Publication US 2021/0284636 A1, Sep. 16, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/4745 (2006.01); A61K 31/497 (2006.01); A61K 45/06 (2006.01); C07D 471/04 (2006.01)
CPC C07D 471/04 (2013.01) [A61K 31/4745 (2013.01); A61K 31/497 (2013.01); A61K 45/06 (2013.01)] 11 Claims
 
1. A method for the treatment of cancer sensitive to inhibition of ERα in a warm-blooded animal in need of such treatment, which comprises administering to the animal an effective amount of a compound of Formula (I):

OG Complex Work Unit Chemistry
wherein:
A is CR2 or N;
G is CR3 or N;
D is CR4 or N;
E is CR5 or N;
Q is O, NH or NMe;
R1 is CH2F, CHF2 or CF3;
R2 is H, F, Cl, Me, CN, OMe or OEt;
R3 is H or F;
R4 is H, F, CN or OMe;
R5 is H or F;
R6 is H, Me, CH2F, CHF2 or CF3;
R7 is H or Me;
R8 is C1-3 alkyl, CH2F, CHF2, CF3 or C3-4 cycloalkyl;
R9 is Me, F or CH2F;
R10 is Me, F, CH2F, CHF2, CF3, CH2OMe or CH2OH;
R11 is H or F; or
R10 and R11 taken together with the carbon atom to which they are attached form a cyclopropyl ring or an oxetane ring;
R12 is independently selected from F or Me;
R13 is H or F; and
a is 0, 1 or 2;
or a pharmaceutically acceptable salt thereof.