US 2015/0175622 A1Published application

3-o-heteroaryl-ingenol

AssigneeLEO Laboratories Limited

InventorsXifu Liang, Thomas Högberg, Bjarne Nørremark, Kristoffer Månsson, Carsten Ryttersgaard, Gunnar Grue-Sørensen

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Abstract

The present invention relates to a compound according to formula (I) wherein R1 represents 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.

Claims28

Dependent claims

A compound according to the general formula I

wherein R1 represents heteroaryl, and wherein R1 is optionally substituted with one or more substituents independently selected from R2;
wherein R2 represents cyano or halogen;
or R2 represents (C1-C6)alkyl, (C2-C6)alkenyl, (C1-C6)alkoxy, (C3-C6)cycloalkyl, halo(C1-C6)alkyloxy, heterocycloalkyl, aryl or heteroaryl;
said (C1-C6)alkyl optionally being substituted with one or more substituents independently selected from the group consisting of halogen, cyano, hydroxyl and oxo;
or R2 represents —NRaCORb, —CONRaRb, —COORa, —OCORa, —ORa, —OCONRaRb, —NRaCOORb, —NRaSO2Rb, —SO2NRaRb, —SO2Ra, —S(O)Ra or —NRaRb;
wherein Ra and Rb are each independently selected from the group consisting of hydrogen, (C1-C4)alkyl, halo(C1-C4)alkyl, hydroxy(C1-C4)alkyl, cyano(C1-C4)alkyl, aryl, heteroaryl, (C3-C6)cycloalkyl and heterocycloalkyl;
or two adjacent R2's join together to form a 5-7 membered non-aromatic carbocyclic or heterocyclic ring together with the carbon or nitrogen atoms to which they are attached;
and pharmaceutically acceptable salts, hydrates, solvates or pharmaceutically acceptable and physiologically cleavable esters thereof.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application: 14/409,374Filed 21 Jun 2013
Priority: 26 Jun 2012
Published: 25 Jun 2015
Term ends: Not estimatedThe source records don’t support an estimate.

Classification40 codes

C07D 495/04
In which the condensed system contains two hetero rings: ortho-condensed systems
A61K 8/49
Containing organic compounds: containing heterocyclic compounds
A61K 8/4926
With one nitrogen as the only hetero atom: having six membered rings
A61K 8/4946
With more than one nitrogen as the only hetero atom: imidazoles or their condensed derivatives, e.g. benzimidazoles

Family

Application61/664,398Us provisional application · filed 26 Jun 2012
Application61/763,206Us provisional application · filed 11 Feb 2013
US 9,422,309 B2Related patent
US 2015/0175622 A1This patent

From the US filing history. Foreign family members aren’t listed.

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