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US 2019/0337924 A1Published application
Substituted hydantoin and thiohydantoin derivatives as androgen receptor antagonists
AssigneeJanssen Pharmaceutica NV
InventorsGilles Bignan, Peter J Connolly, Jan Hickson, Lieven Meerpoel, Vineet Pande, Zhuming Zhang, Jonathan Branch, Christian Rocaboy, Luis B Trabalón Escolar
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Abstract
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the antagonism of one or more androgen receptor types. Such compounds are represented by Formula (I) as follows: wherein R1a, R2a, R2b, Z, X, Y, and G are defined herein.
Claims26
A compound of Formula (I)
- wherein
- Z is S;
- R1 is selected from the group consisting of chloro, methyl, methoxy, difluoromethyl, and trifluoromethyl;
- R2a and R2b is an unsubstituted or substituted C3-C10heterocyclyl pyrrolidinyl;
- wherein said substituted C3-C10heterocyclyl is optionally independently substituted with a C1-3alkyl or cyclopropyl substituent;
- X is C;
- Y is C;
- G is selected from the group consisting of g1
- wherein R3 is selected from the group consisting of hydrogen;
- C1-6alkyl optionally independently substituted with a substituent selected from hydroxy, methoxy, cyano, or fluoro;
- C3-6cycloalkyl optionally independently substituted with a substituent selected from hydroxy or fluoro;
- and —C(O)OR4, wherein R4 is C1-6alkyl or —CH2(C6-10aryl) wherein C6-10aryl is optionally substituted with a methoxy substituent;
- such that a substituent on C1-6alkyl or C3-6cycloalkyl is attached at a carbon atom other than the carbon atom directly attached to the G-nitrogen atom;
- wherein any nitrogen-containing heterocyclic substituent of G is optionally substituted with an oxido substituent to form an N-oxide;
- or an enantiomer, diastereomer, or pharmaceutically acceptable salt form thereof.
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Dependencies are inferred from the claim text.