| US 7,485,645 B2 | ||
| 17β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases | ||
| Timothy J. Guzi, Chatham, N.J. (US); Yi-Tsung Liu, Morris Township, N.J. (US); Ronald J. Doll, Convent Station, N.J. (US); Anil Saksena, Upper Montclair, N.J. (US); Viyyoor M. Girijavallabhan, Parsippany, N.J. (US); and Jonathan A. Pachter, East Setauket, N.Y. (US) | ||
| Assigned to Schering Corporation, Kenilworth, N.J. (US) | ||
| Filed on Aug. 09, 2007, as Appl. No. 11/836,530. | ||
| Application 11/836530 is a division of application No. 11/360711, filed on Feb. 23, 2006, granted, now 7,271,175. | ||
| Application 11/360711 is a division of application No. 10/735983, filed on Dec. 15, 2003, granted, now 7,053,091. | ||
| Claims priority of provisional application 60/434101, filed on Dec. 17, 2002. | ||
| Prior Publication US 2008/0004248 A1, Jan. 03, 2008 | ||
| Int. Cl. A61K 31/497 (2006.01); A61K 31/435 (2006.01) | ||
| U.S. Cl. 514—253.01 [514/253.03; 514/290] | 2 Claims |
1. A method at inhibiting type 3 17β-hydroxysteroid dehydrogenase, comprising administering a therapeutically effective amount
of at least one compound represented by the structural formula:
 wherein:
X is CH;
Y is N;
G is C(═O);
R is selected from the group consisting of alkyl, —OR4, aryl, heteroaryl, heteroaryloxy, heterocyclyl, heterocyclyloxy, cycloalkyl, cycloalklyloxy, —N(R4)2 where the two R4 moieties can be the same or different, —(CH2)n-aryl, —(CH2)n-heteroaryl, —(CH2)n-heterocyclyl and —(CH2)n-cycloalkyl, wherein each of said alkyl, aryl, heteroaryl, and cycloalkyl can be unsubstituted or optionally independently
substituted with one or more moieties which can be the same or different, each moiety being independently selected from the
group consisting of alkyl, alkyl, aryl, heteroaryl, —OR4, heterocyclyl, heterocyclyloxy, cycloalkyl, cycloalklyloxy, —N(R4)2 where the two R4 groups can be the same or different, —C(O)R4, and —C(O)N(R4)2 where the two R4 moieties can be the same or different;
one of a, b, c and d in ring I represents N or N+O−, and the remaining a, b, c and d positions represent C(R1) or C(R2); or
each of a, b, c, and d are independently selected from C(R1) or C(R2);
R1 and R2 can be the same or different, each being independently selected from the group consisting of:
H, halo, —CF3, —OR4, —C(O)R4, —OCF3, —SR4, —S(O)nR5, benzotriazol-1-yloxy, tetrazol-5-ylthio, alkynyl, alkenyl wherein said alkenyl can be unsubstituted or optionally substituted
with halo, —OR4 or —C(O)OR4, alkyl wherein said alkyl can be unsubstituted or optionally substituted with halo, —OR4 or —C(O)OR4, —N(R4)2 where the two R4 moieties can be the same or different, —NO2, —OC(O)R5, —C(O)OR4, —CN, −N(R4)C(O)OR4, —SR5C(O)OR4, and —SR5N(R4)2 (provided that R5 in —SR5N(R4)2 is not —CH2—) wherein each R4 is independently selected;
the dotted line between carbon atoms 5 and 6 represents an optional bond, such that when a double bond is present, A and B
can be the same or different, each being independently selected from the group consisting of —R4, halo, —OR4, —C(O)OR4, —OC(O)OR4 or —OC(O)R4, and when no double bond is present between carbon atoms 5 and 6, A and B can be the same or different, each being independently
selected from the group consisting of (H2), —(OR5)2, (H and halo), (dihalo), (H and R5), (R5)2, (H and —OC(O)R4), (H and —OR4), (═O), and (H, (═NOR4) or (—O—(CH2)p—O—) wherein p is 2, 3 or 4);
R3 is selected from the group consisting of H, alkyl, alkoxy and alkoxyalkyl;
R4 is selected from the group consisting of H, alkyl, aryl and aralkyl;
R5 is alkyl or aryl;
R6 is H or alkyl;
n is a number from 1-4; and
q is a number from 1-8;
to a patient in need of such inhibition.
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