Back to results
US 7,064,207 B2Granted
Androgen receptor antagonists
AssigneeWarner-Lambert Company
InventorsDaniel Y. Du, Matthew Colin Thor Fyfe, Martin James Procter, Karen Lesley Schofield, Vilasben Kanji Shah, Geoffrey Martyn Williams
Life of this patent
Estimating the term…
Abstract
The present invention is directed to a new class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives to their use as androgen antagonists, and to relieve conditions associated with inappropriate activation of the androgen receptor.
Claims16
A compound of the formula:
- in which:
- a. M is NZ or O;
- b. Z is represented by H or C1–C4 alkyl;
- c. R1 is represented by hydrogen, (C1–C2)alkyl, optionally substituted with one or more halogens, or (C1–C2)alkoxy, optionally substituted with 1 or more halogens;
- d. R2 is absent, or may represent up to 2 substituents selected from the group consisting of halogen, nitrile, hydroxy, (C1–C4)alkyl, (C2–C4)alkenyl, (C2–C4)alkynyl, (C1–C4)alkoxy, (C1–C2)alkyl substituted with 1 or more halogens, (C1–C2)alkoxy substituted with one or more halogens, SR4, and NR4R5;
- e. A is represented by —S(O2);
- f. B completes a heterocyclic ring;
- g. R3 may be absent, or may represent up to 2 substituents selected from the group consisting halogen, hydroxy, nirrile, (C1–C4)alkoxy, (C1–C4)alkyl, optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted phenyl, —[CH2]mC(O)OR4, —[CH2]mC(O)R4, —[CH2]mC(O)NR4R5, (C1–C4)alkylR6, —[CH2]n—Y[—CH2]m—X—[CH3]q, (C3–C8)cycloalkyl, and —SR4;
- h. R4 is represented by hydrogen, (C1–C4)alkyl, optionally substituted benzyl, optionally substituted phenyl, optionally substituted heteroaryl, or optionally substituted heterocyclic or R4 and R5 together with the adjacent nitrogen atom can combine to form a heterocyclic or heteroaryl ring;
- i. R5 is represented by hydrogen, optionally substituted phenyl, (C1–C4)alkyl, or optionally substituted benzyl;
- j. R6 is represented by optionally substituted phenyl, optionally substituted heteroaryl, or optionally substituted heterocyclic;
- k. n is an integer selected from 1, 2, 3, or 4;
- l. Y is absent, or is represented by O, C(O), OH, SH, or S;
- m. m is represented by an integer selected from 0, 1, 2, 3, or 4;
- n. X is absent, or is represented by O, C(O), OH, SH or S;
- and
- o. q is represented by the integer 0 or 1;
- or a pharmaceutically acceptable salt, or solvate, thereof:
- with the previsio that:
- 1) if both X and Y are present, then m is not zero, and 2) if M is represented by oxygen, then R1 must be trifluoromethyl.
17 more elements
Dependencies are inferred from the claim text.