Introduction: Autotaxin (ATX) is a secreted enzyme that hydrolyzes lysophosphatidylcholine to lysophosphatidic acid (LPA) and choline. The ATX/LPA axis has received increasing interest in recent years because both the enzyme ATX and the bioactive lipid LPA are involved in various pathological conditions such as tumor progression and metastasis, fibrotic diseases, autoimmune diseases, arthritis, chronic hepatitis, obesity and impaired glucose homeostasis. Thus, a great effort has been devotd in developing synthetic ATX inhibitors as new agents to treat various diseases including cancer and fibrotic diseases.Areas covered: This review article summarizes the autotaxin inhibitors presented in patent literature from October 2012 to August 2016 and their biological evaluation, discussing their activities in vitro and in vivo.Expert opinion: During the recent years, there has been an intensive effort on the discovery of potent and selective ATX inhibitors. Although various synthetic inhibitors have been ...

Autotaxin inhibitors: a patent review (2012-2016).

Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.

Dihydropyrrolopyridine inhibitors of ROR-gamma

Compounds of formula (I) 
wherein R 1 , R 2 , A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.

Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors

The invention provides novel compounds having the general formula (I) wherein R1, Y, A, W, R2, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds.

New octahydro-pyrrolo[3,4-c]-pyrrole derivatives and analogs thereof as autotaxin inhibitors

Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.

Modulators of ror-gamma

The invention provides novel compounds having the general formula (I) wherein R1 is selected from substituted phenyl, pyridinyl or thiophenyl, R2 is selected from optionally substituted aminosulphonylphenyl, aminosulphonylpyridinyl, aminosulphonylthiophenyl or aminosulphonylthiazolyl, X is nitrogen or carbon, Y is a linking group, Z is a direct bond or a linking group, m = 0-5, n = 0-5 with the proviso that m+n is 2-5, compositions including the compounds and the use of the compounds in the treatment or prophylaxis of ocular conditions.

Di Giorgio Patrick

Papers

Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors

Heterocyclic compounds useful as dual atx/ca inhibitors