Leo Laboratories Limited

Leo-pharma A/s

Leo Pharmaceutical Products, Ltd.

Gunnar Grue-Sørensen

Xifu Liang

Thomas Högberg

Kristoffer Månsson

Carsten Ryttersgaard

Per Vedsø

Daniel Rodriguez Greve

Søren Christian Schou

Thomas Vifian

Anthony Murray

Ernst T Binderup

Erik Rytter Ottosen

Anders Klarskov Petersen

Anette Graven Sams

Simon Feldbæk Nielsen

Anne Marie Horneman

Bjarne Nørremark

Henrik Pedersen

Tina Dahlerup Poulsen

Simon Felbdæk Nielsen

Mikael Tranholm

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 invention relates to compounds of general formula (I) wherein R, R, R, R, m and n are defined as defined herein, 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, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immuno-suppression would be desirable for example in organ transplantation. 

Homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof

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 A, R, R, R, R, R, R, m and n are defined as defined herein, 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, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation. 

Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors

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.

Method of producing ingenol-3-angelate

Use of vitamin D-derivatives in the treatment of osteoporosis and related bone disorders, as well as novel vitamin D3-derivatives

Growing community of inventors

Roskilde, Denmark

Gunnar Grue-Sørensen