17a-hydroxylase/C17,20-lyase inhibitors

Patent metadata

Field	Value
Publication number	US-9339501-B2
Application number	US-201514682504-A
Country	US
Kind code	B2
Filing date	Apr 9, 2015
Priority date	Apr 28, 2011
Publication date	May 17, 2016
Grant date	May 17, 2016

Abstract

The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof,

where R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase/C 17,20 -lyase inhibitors.

First claim

What is claimed is:

1. A method for treating prostate cancer comprising the step of administering a compound of Formula (I)

wherein
R 1 is
(i) phenyl optionally substituted with 1 to 3 substituents selected from halo, —CN, —OH, (C 1 -C 6 )alkyl, halo-substituted (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, —NH 2 , —NH(C 1 -C 4 )alkyl, —N((C 1 -C 4 )alkyl) 2 , —NHC(O)—(C 1 -C 4 )alkyl, —C(O)NH 2 , —C(O)—NH(C 1 -C 4 )alkyl, —C(O)—N((C 1 -C 4 )alkyl) 2 , (C 3 -C 5 )cycloalkyl, or a 5- to 6-membered heterocycle,
(ii) phenyl fused to an additional phenyl, a 5- to 6-membered heteroaryl, a 5- to 6-membered partially or fully saturated cycloalkyl, or a 5- to 6-membered partially or fully saturated heterocycle, where said fused phenyl is optionally substituted with 1 to 4 substituents each independently selected from halo, —CN, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy-substituted (C 1 -C 4 )alkyl, halo-substituted (C 1 -C 4 )alkyl, (C 3 -C 5 )cycloalkyl, oxo, —NH 2 , —NH(C 1 -C 4 )alkyl, —N((C 1 -C 4 )alkyl) 2 , —NHC(O)—(C 1 -C 4 )alkyl, or ═N—OH,
(iii) 5- to 6-membered heteroaryl optionally substituted with 1 to 3 substituents each independently selected from halo, —CN, —OH, (C 1 -C 6 )alkyl, halo-substituted (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, —NH 2 , —NH(C 1 -C 4 )alkyl, —N((C 1 -C 4 )alkyl) 2 , —NHC(O)—(C 1 -C 4 )alkyl, —C(O)NH 2 , —C(O)—NH(C 1 -C 4 )alkyl, —C(O)—N((C 1 -C 4 )alkyl) 2 , (C 3 -C 5 )cycloalkyl, or a 5- to 6-membered heterocycle, or
(iv) 5- to 6-membered heteroaryl fused to another 5- to 6-membered heteroaryl, phenyl, 5- to 6-membered partially or fully saturated cycloalkyl, or a 5- to 6-membered partially or fully saturated heterocycle, where said fused heteroaryl is optionally substituted with 1 to 4 substituents each independently selected from halo, —CN, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy-substituted (C 1 -C 4 )alkyl, halo-substituted (C 1 -C 4 )alkyl, (C 3 -C 5 )cycloalkyl, oxo, —NH 2 , —NH(C 1 -C 4 )alkyl, —N((C 1 -C 4 )alkyl) 2 , —NHC(O)—(C 1 -C 4 )alkyl, or ═N—OH;
R 2 and R 5 are each independently CH 3 or H;
R 3 and R 4 are each independently CH 3 or H, or taken together with the carbon atoms to which they are attached form a cyclopropyl; and
R 6 is (C 3 -C 5 )cycloalkyl, where the cycloalkyl is optionally substituted with hydroxy;

or a pharmaceutically acceptable salt thereof, to a subject in need of such treatment.

2. The method of claim 1 , wherein the compound of Formula (I) has the structure of:

Assignees

• Bock Mark Gary
• Gaul Christoph
• Gummadi Venkateshwar Rao
• Sengupta Saumitra
• Novartis Ag

Inventors

• Bock Mark Gary
• Gaul Christoph
• Gummadi Venkateshwar Rao
• Sengupta Saumitra

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K31/506 Primary

  not condensed and containing further heterocyclic rings · CPC title

• C07D409/14

  containing three or more hetero rings · CPC title

• C07D405/14

  containing three or more hetero rings · CPC title