Agency for Science, Technology and Research

Athisayamani Jeyaraj Duraiswamy

Soo Yei Ho

Jenefer Alam

Stephanie Eliane Blanchard

Vikrant Arun Adsool

Wei Ling Wang

Kassoum Nacro

Lohitha Rao Chennamaneni

Anders Poulsen

The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway wherein R, R, R, Rand Rare each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.

Purine diones as Wnt pathway modulators

The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein.

WNT pathway modulators

The present invention relates to compounds of Formula (Ib-I) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases. 

Bicyclic heterocyclic derivatives as MNK1 and MNK2 modulators and uses thereof

The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein each of R, R, R, R, R, W, X, Y, Z, and n is as defined herein.

The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R, R, R, Rand Rare each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3. 

The present invention relates to dihydropyrazolo[1,5-a]pyrimidine compounds of formula I, defined herein, as WNT pathways modulators, processes for making them, and pharmaceutical compositions comprising them. Methods of treatment of conditions mediated by WNT pathway signalling including cancer, fibrosis, stem cell and diabetic retinopathy, rheumatoid arthritis, psoriasis and myocardial infarction, comprising the compounds of formula I are also provided. 

Wnt pathway modulators

The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein Rrepresents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from Calkoxy); optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C-6alkyl, Calkoxy, Chaloalkyl, Chaloalkoxy and halo); or -alkylaryl; Rrepresents H; or alkyl; Rrepresents H; or alkyl; U, V and W represent &#x2014;(CH)&#x2014;; or U and V together represent &#x2014;CH&#x2550;CH&#x2014; and W represents C&#x2550;O; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from Calkyl, Calkoxy, Chaloalkyl, Chaloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from Calkyl, Calkoxy, &#x2014;C(O)OCalkyl, &#x2014;C(O)Calkyl and &#x2014;C(O)NHCalkyl); and Z represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from Calkyl, Calkoxy, Chaloalkyl, Chaloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from Calkyl, Calkoxy, &#x2014;C(O)OCalkyl, &#x2014;C(O)Calkyl and &#x2014;C(O)NHCalkyl). 

Maleimide derivatives as modulators of wnt pathway

The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.

Growing community of inventors

Singapore, Singapore

Athisayamani Jeyaraj Duraiswamy