Leo Laboratories Limited

Thomas Högberg

Xifu Liang

Gunnar Grue-Sørensen

Kristoffer Månsson

Per Vedsø

Thomas Vifian

Anders Klarskov Petersen

Anne Marie Horneman

Bjarne Nørremark

Carsten Ryttersgaard

Gunnar Grue-sørensen

Bjarne NØRREMARK

The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is &#x2014;NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use&#x2014;alone or in combination with one or more other pharmaceutically active compounds&#x2014;in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

Ingenol-3-acylates III and ingenol-3-carbamates

The invention relates to compounds of general formula I, (I), wherein R is wherein R is aryl substituted by R3; or R is (C3-Ci3)-cycloalkyl, (C3-Ci3)-cycloalkenyl or (C7-Ci3)-cycloalkynyl optionally substituted by R4; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use&#x2014;alone or in combination with one or more other pharmaceutically active compounds&#x2014;in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis. 

3-acyl-ingenols II

The present invention relates to a compound according to formula (I) wherein Rrepresents optionally substituted heteroaryl, and pharmaceutically acceptable salts, hydrates, solvates or pharmaceutically acceptable and physiologically cleavable esters thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. diseases associated with hyperplasia, neoplasia or dysplasia, with said compounds, to methods of treatment of cosmetic indications with said compounds, and to the use of said compounds in the manufacture of medicaments. 

3-O-heteroaryl-ingenol

The invention relates to compounds of general formula (I) wherein R is (C-C)alkyl, (C-C)alkenyl or (C-C)alkynyl; wherein R is substituted with R1; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use&#x2014;alone or in combination with one or more other pharmaceutically active compounds&#x2014;in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis. 

Ingenol-3-acylates I

The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is &#x2014;NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use&#x2014;alone or in combination with one or more other pharmaceutically active compounds&#x2014;in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis. 

The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II).  Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.

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Ballerup, Denmark

Thomas Högberg