Compounds useful for molecular imaging of cells expressing estrogen receptors are provided. Also provided are intermediates for making the compounds and methods of making the compounds using a modular convergent strategy. Further, methods of making the intermediates are described, as well as methods of diagnosing disease in a subject by using the compounds as imaging agents.

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R.sub.1 and R.sub.2 is hydrogen or C.sub.1-C.sub.8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R.sub.3 is hydrogen or wherein R.sub.5 represents C.sub.1-C.sub.8 straight, branched alkyl chain or cycloalkyl; R.sub.4 is hydrogen or halogen; R.sub.6 is hydrogen or halogen;

##STR00001##

The present invention discloses a process for the preparation of 16, 17-acetals of pregnane derivatives having formula I ##STR00001##
wherein each substituent is independently selected from; R.sub.1 is H or CH.sub.3; R.sub.2 is C.sub.1-C.sub.6 linear or branched alkyl, alkynyl group or cycloalkyl group; aryl or heteroaryl group; or R.sub.1 and R.sub.2 combine to form saturated, unsaturated C.sub.3-C.sub.6 cyclic or heterocyclic ring; R.sub.3 and R.sub.4 are same or different and each independently represents H or halogen; R.sub.5 is OH or OCOR wherein R represents H or C.sub.1-C.sub.6 linear, branched or cyclic alkyl group that may be substituted.

The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.

The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.