Enterprise Therapeutics Limited

Tmem16a Limited

Thomas Beauregard Schofield

Duncan Alexander Hay

Jonathan David Hargrave

Naomi Went

Clive McCarthy

Clive Mccarthy

Edward Walker

Christopher Charles Stimson

Stephen Collingwood

Peter Neville Ingram

Chun Yan Ma

Abdul Kadar Shaikh

Sarah Ellam

Matthew Raymond Smith

Spencer Charles Robert Napier

Craig Stephen Buxton

Matthew Habgood

Spencer Napier

Compounds of general formula (I): wherein R, R, R, R, R, RX, X, Z and Y are as defined herein are positive modulators of the calcium-activated chloride channel (CaCC), TMEM16A. The compounds are useful for treating diseases and conditions affected by modulation of TMEM16A, particularly respiratory diseases and conditions.

Compounds

Compounds of general formula (I) wherein R, R, R, R, Rand X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.

Substituted benzodiazoliums as ENaC inhibitors

Compounds of general formula (I) wherein R, R, R, Rand X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.

Compounds with activity as inhibitors of the epithelial sodium channel (ENaC)

The present invention discloses bis(pentahydroxyhexyl)amino substituted 2-{[(3-amino-pyrazin-2-yl)formamido]methyl}-1H-1,3-benzodiazol-3-ium derivatives of formula (I) as inhibitors of ENaC and are of use in the treatment of respiratory diseases and conditions, skin conditions or ocular conditions, wherein the respiratory disease or condition is e.g. cystic fibrosis, chronic obstructive pulmonary disease (COPD), chronic bronchitis, emphysema, bronchiectasis, including non-cystic fibrosis bronchiectasis, and asthma; the skin condition is e.g. psoriasis, atopic dermatitis and ichthyosis; and the ocular condition is e.g. dry eye disease. 

Bis(pentahydroxyhexyl)amino substituted 2-{[(3-amino-pyrazin-2-yl)formamido]methyl}-1H-1,3-benzodiazol-3-ium derivatives as ENaC inhibitors for treating respiratory diseases

Compounds of general formula (I): wherein R, R, R, R, R, R* X, X, Z and Y are as defined herein are positive modulators of the calcium-activated chloride channel (CaCC), TMEM16A. The compounds are useful for treating diseases and conditions affected by modulation of TMEM16A, particularly respiratory diseases and conditions. 

The invention relates to compounds of general formula (I): wherein R, R, R, Rand Xare as defined herein. The compounds are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions. 

Growing community of inventors

Abingdon, United Kingdom

Thomas Beauregard Schofield