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US 2007/0167445 A1Published application
Androgen receptor modulator compounds and methods
OwnerRobert Higuchi, Kristen Arienti +5inventors
InventorsRobert Higuchi, Kristen Arienti, Neelakandha Mani, Barbara Pio, Lin Zhi, Penghui Chen, Thomas Caferro
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Abstract
Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.
Claims3
A compound having the formula:
- wherein:
- Rx is selected from among C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, allyl, aryl, arylalkyl, heteroaryl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, cycloalkyl, heteroalkyl, haloalkyl, allyl, aryl, arylalkyl, heteroaryl, alkynyl, and alkenyl are optionally substituted with halogen, C1-C4 alkyl, or C1-C4 haloalkyl;
- R4 is selected from among hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, aryl, arylalkyl, heteroaryl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, cycloalkyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, alkynyl, and alkenyl are optionally substituted with halogen, C1-C4 alkyl, or C1-C4 haloalkyl;
- and
- R13 is selected from among hydrogen, C1-C8 alkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, C3-C8 cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, heteroalkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, alkynyl, and alkenyl groups are optionally substituted.
2 more elements
A compound having the formula:
- wherein:
- Rx is selected from among C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, allyl, aryl, arylalkyl, heteroaryl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, cycloalkyl, heteroalkyl, haloalkyl, allyl, aryl, arylalkyl, heteroaryl, alkynyl, and alkenyl are optionally substituted with halogen, C1-C4 alkyl, or C1-C4 haloalkyl;
- R4 is selected from among hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, aryl, arylalkyl, heteroaryl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, cycloalkyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, alkynyl, and alkenyl are optionally substituted with halogen, C1-C4 alkyl, or C1-C4 haloalkyl;
- R6 is selected from among hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, aryl, arylalkyl, heteroaryl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, cycloalkyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, alkynyl, and alkenyl are optionally substituted with halogen, C1-C4 alkyl, or C1-C4 haloalkyl;
- and
- R13 is selected from among hydrogen, C1-C8 alkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, C3-C8 cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, heteroalkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, alkynyl, and alkenyl groups are optionally substituted.
3 more elements
A compound having the formula:
- wherein:
- R6 is selected from among hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, aryl, arylalkyl, heteroaryl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, cycloalkyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, alkynyl, and alkenyl are optionally substituted with halogen, C1-C4 alkyl, or C1-C4 haloalkyl;
- R7 is selected from among hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, aryl, arylalkyl, heteroaryl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, cycloalkyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, alkynyl, and alkenyl are optionally substituted with halogen, C1-C4 alkyl, or C1-C4 haloalkyl;
- and
- R13 is selected from among hydrogen, C1-C8 alkyl, C1-C8 heteroalkyl, C1-C8 haloalkyl, C3-C8 cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, C2-C8 alkynyl, and C2-C8 alkenyl, wherein the alkyl, heteroalkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, alkynyl, and alkenyl groups are optionally substituted.
2 more elements
Dependencies are inferred from the claim text.