Applied Research Systems Ars Holding N.v.

Laboratoires Serono S.a.

Gerardo Burton

Carlos P Lantos

Adriana Silvia Veleiro

The present invention is related to novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues, their use as antiglucocorticoids for the treatment and/or prophylaxis of disease associated to an excess of glucocorticoids. In particular, the invention relates to the use of novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues for treating Cushing's syndrome, iatrogenic hypercortisolism or depression. Also the present invention is related to methods of preparing the novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues.

Sulphur analogues of 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) for treating excess of glucocorticoids

The present invention relates to a novel method for preparing 21-hydroxy-6,19-oxidopro-gesterone (21OH-6OP) and/or its 21-acetate, 21-propionate, 21-hemisuccinate, 21-phosphate, 21-oleate derivatives. 21OH-6OP and its ester derivatives are antiglucocorticoids for the treatment or prophyl axis of diseases associated to an excess of glucocorticoids, in particular for treating Cushing's syndrome, iatrogenic hypercortisolism or depression.

Method for the preparation of 21-hydroxy-6,19-oxidoprogesterone (21 oh-6op)

Sulfur analogues of 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) for treating excess of glucocorticoids

The comformationally highly bent steroid 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) has been found to be a selective antiglucocoriticoid virtually lacking mineralococorticoid or glucocorticoid properties as well as affinity for MR or PR and is used for the treating of diseases associated with an excess of glucocordcoids in the body, such as the Cushing's syndrome or depression.

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Florida, Argentina

Gerardo Burton