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1. (WO2007007149) ANDROGEN MODULATORS
Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

CLAMS

What is claimed is:

1. A compound of the formula:


in which;
a) X is represented by halogen, cyano, Ci-C6 alkyl, C1-C6 alkoxy, NO2 , haloalkoxy, or haloalkyl,
b) X2 is represented by hydrogen, halogen, cyano, Ci-C6 alkyl, C1-C6
alkoxy, NO2, haloalkoxy, or haloalkyl,
c) A is represented by a (C1-C )alkylene group, which may be optionally substituted,
d) R1 is represented by hydrogen, halogen, Ci-C6 alkyl, Ci-C6 alkoxy,
hydroxy, haloalkoxy, or haloalkyl,
e) R2 is represented by hydrogen, halogen, Ci-C6 alkyl, Ci-C6 alkoxy,
hydroxy, haloalkoxy, or haloalkyl,
f) X3 is represented by a substituent selected from the group consisting of:
i) hydrogen,
ii) (Cj-C^alkyl, optionally substituted,
iii) (C2-C2o)alkenyl, optionally substituted,
iv) (C2-C2o)alkynyl, optionally substituted,
v) (C3_C10)cycloalkyl, optionally substituted,
vi) (c3-C10) cycloalkyKCj-φalkyl, in which the alkyl and
cycloalkyl moieties may each be optionally substituted,
vii) (C6-C10)aryl optionally substituted,
viii) (C8-C10)aryl (Cj-C^alkyl, in which the alkyl and aryl moieties
may each be optionally substituted,
ix) heteroaryl, optionally substituted, x) heteroaryl(C1.C6)alkyl, in which the heteroaryl and alkyl
moieties may each be optionally substituted,
xi) heterocyclic, optionally substituted,
xii) heterocyclic(CrC6)alkyl, in which the alkyl and heterocyclic
moieties may each be substituted,
xiii) (CH2)Z OR3,
xiv) (CH2)Z-NR3R4,
xv) (CH2)Z-COOR3,
xvi) (CH2)Z-CONR4R3,
xvii) (CH2)Z-NR4COR3,
xviii) (CH2)Z-OCOR3,
xix) (CH2)Z-C(O)R3,
XX) (CH2)Z-C(O)C(O)NR3R4,
xxi) (CH2)Z-SOXR3,
xxii) (CH2)Z-SO2NR3R4,
xxiii) (CH2)Z-NR4-SO2R3
z is represented by an integer from 1 to 6,
x is represented by an integer from 0 to 2
g) R3 is represented by a substituent selected from the group consisting of
hydrogen, (C1-C6)alkyl which may be optionally substituted, optionally
substituted (C6-C10)aryl, and (C6-C10)aryl (Cj-φalkyl, in which the alkyl and aryl moieties may each be optionally substituted, and;
h) R4 is represented by hydrogen, Cj-C6 alkyl, or C6-Ci0 aryl.

2. A compound according to claim 1 in which X2 is hydrogen.

3. A compound according to claim 1 or 2 in which X1 is trifluoromethyl.

4. A compound according to claim 1, 2, or 3 in which A is a C3 to Ce alkylene moiety.

5. A compound according to claim 1, 2, 3, or 4 in which R1 and R2 are each
hydrogen'

6. Use of a compound according to any one of claims 1-5 as a medicine.

7. Use of a compound according to any one of claims 1-5 in the manufacture of a medicament for inhibiting activation of the androgen receptor.

8. Use of a compound according to any one of claims 1-5 in the manufacture of a medicament for alleviating a condition selected from the group consisting of hormone dependent cancers, benign hyperplasia of the prostate, acne, hirsutism, excess sebum, alopecia, premenstrual syndrome, lung cancer, precocious puberty, osteoporosis, hypogonadism, age-related decrease in muscle mass, and anemia.

9. A pharmaceutical composition comprising a compound according to any one of claims 1-5 in admixture with one or more pharmaceutically acceptable excipients.

10. A topical pharmaceutical formulation comprising a compound according to any one of claims 1-5 in admixture with or more pharmaceutically acceptable
excipients suitable for dermal application.

11. An article of manufacture comprising a compound according to any one of claims 1-5, packaged for retail distribution, which advises a consumer how to utilize the compound to alleviate a condition selected from the group consisting of acne, alopecia, and oily skin.