Novartis Ag

Agency for Science, Technology and Research

Agency for Science, Technology and Research (a*star)

Thomas Hugo Keller

Clive McCarthy

Bernard Cuenoud

Ian Bruce

Roger John Taylor

Neil John Press

Alastair Denholm

Gaynor Elizabeth Pilgrim

David Andrew Sandham

Simon James Watson

David Beattie

Emma Budd

Catherine LeBlanc

Wei Ling Wang

Graham Charles Bloomfield

Anders Poulsen

Darren Mark Le Grand

Louise Clare Kirman

Soo Yei Ho

Judy Fox Hayler

Gang Wang

Wei Hung

Mrinalini Sachin Oza

Cathy Ritchie

Shi Hua Ang

Nicola Press

Barbara Valade

Lewis Whithead

Gaynor Elizabeth Woodward

Congbao Kang

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

There are provided new heterobifunctional agents designed to mediated formation of protein-protein dimers and promote ubiquitination of a protein of the dimer. Also provided are methods of synthesizing the agents, pharmaceutical formulations including the agents, and methods of using the agents to treat, ameliorate or cure diseases characterized by protein over-expression or malfunction.

Therapeutic compounds and methods of use thereof

Compounds of formula I in free or salt form, wherein R, R, Rand Rhave the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Inhibitors of phosphatidylinositol 3-kinase

Compounds of formula I in free or salt form, wherein R, R, R, Rand Rhave the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

5-Phenylthiazole derivatives and their use as p13 kinase inhibitors

Compounds of formula I in free or salt form, wherein R, Rand Rhave the meanings as indicated in the specification, are useful for treating conditions mediated by of phosphodiesterase type 4 or the down-regulation or inhibition of TNF-&#x3b1; release, particularly obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

[1,7]naphthyridines as PDE4 inhibitors

The invention relates to compounds of formula I in free or salt form, where Ris a monovalent aromatic group having up to 10 carbon atoms, and Ris a cycloaliphatic group having up to 8 ring carbon atoms. Compositions containing them, methods for their preparation and their use as pharmaceuticals are also described.

Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (PDE4) inhibitors

Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals

Organic compounds

Growing community of inventors

Singapore, Singapore

Thomas Hugo Keller