17Beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
AssigneeSchering Corporation
InventorsKamil Paruch, Timothy Guzi
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Abstract
In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17β-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.
Claims37
A compound represented by the structural formula:
- wherein:
- X is CH or N;
- Z is O or N(R6);
- R1 and R2 are the same or different, each being independently selected from the group consisting of aryl, heteroaryl, aralkyl and heteroaralkyl, wherein each of said aryl, heteroaryl, aralkyl and heteroaralkyl 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 halogen, alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, heterocyclyl, CF3, CN, —OCF3, —OR6, —C(O)R7, —NR6R7, —C(O)OR6, —C(O)NR6R7, —SR6, —S(O2)R7, —S(O2)NR6R7, —N(R6)S(O2)R7, —N(R6)C(O)R7 and —N(R6)C(O)NR6R7;
- R3 is H or —OR6, with the proviso that when X is N, R3 is not —OR6;
- R4 is selected from the group consisting of H, alkyl, aryl, cycloalkyl, aralkyl, heteroaryl, heteroaralkyl and heterocyclyl;
- m is a number from 0 to 4, and when m is more than 1, the R4 groups can be the same or different and are independently selected;
- R5 is —C(O)R7 or —S(O2)R7;
- R6 is selected from the group consisting of H, alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl and heterocyclyl, wherein each of said alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl and heterocyclyl 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 halogen, alkyl, aryl, cycloalkyl, CF3, OCF3, CN, —OR7, —NHR7, —N(R7)2, —CH2OR7, —C(O)R7, —C(O)OR7, —C(O)NHR7, —C(O)N(R7)2, —SR7, —S(O2)R , —S(O2)NHR7, —S(O2)N(R7)2, —N(R7)S(O2)R7, —N(R7)C(O)R7, —N(R7)C(O)NHR7 and —N(R7)C(O)N(R7)2;
- and
- R7 is selected from the group consisting of alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, —OR6, —NHR6, and —N(R6)2, wherein each of said alkyl, heteroaralkyl, aryl, heteroaryl and aralkyl can be unsubstituted or optionally substituted with one or more moieties which can be the same or different, each moiety being independently selected from the group consisting of halogen, alkyl, aryl, cycloalkyl, CF3, OCF3, CN, —OR6, —NHR6, —N(R6)2, —CH2OR6, —C(O)OR6, —C(O)NHR6, —C(O)N(R6)2, —SR6, —S(O2)R6, —S(O2)NHR6, —S(O2)N(R6)2, —N(R6)S(O2)R6, —N(R6)C(O)R6, —N(R7)C(O)NHR6 and —N(R7)C(O)N(R7)2, further wherein the two R6 or the two R7 groups in the moieties —N(R6)2 and —N(R7)2 respectively can be the same or different and are independently selected, and still further wherein any two adjacent alkyl substituents on an aryl or heteroaryl can be joined together to form a methylenedioxy or ethylenedioxygroup.
A compound of the formula:
- or isomer thereof, or a pharmaceutically acceptable salt or solvate of said compound or of said isomer.
Dependencies are inferred from the claim text.