Agency for Science, Technology and Research

Soo Yei Ho

Athisayamani Jeyaraj Duraiswamy

Jenefer Alam

Stephanie Eliane Blanchard

Vikrant Arun Adsool

Wei Ling Wang

Anders Poulsen

Thomas Hugo Keller

Shi Hua Ang

Sum Wai Eldwin Tan

The present invention relates to compounds of general Formula (I), and/or tautomers, enantiomers, solvates, hydrates, and pharmaceutically acceptable salts thereof. The present invention also relates to compounds of Formula (I) for use in therapy, methods of treating isoprenylcysteine carboxyl methyltransferase (ICMT) related disorders or uses of compounds of Formula (I) in the manufacture of a medicament for the treatment of ICMT-related disorders, wherein the disorder is cancer and/or progeria. The present invention further relates to processes for synthesizing compounds of Formula (I).

Compounds useful as inhibitors of isoprenylcysteine carboxyl methyltransferase

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 (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). 

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Singapore, Singapore

Soo Yei Ho