Novartis Ag

Novartis Pharma Gmbh

Philipp Janser

Nikolaus Johannes Stiefl

Wolfgang Miltz

Henri Mattes

Juraj Velcicky

Nina Gommermann

Christopher Farady

Angela Mackay

Anette Von Matt

Eric Vangrevelinghe

Catherine Fooks Solovay

Nichola Smith

Birgit Bollbuck

Rene Hersperger

Emil Pfenninger

René Hersperger

Hans Juerg Wuethrich

Achim Schlapbach

Jean Quancard

Daniela Angst

Lászlo Révész

Ulf Neumann

Rudolf Wälchli

Jörg Eder

Alastair DenholmMritain

Rudolf Wálchi

Alastair Novartis Horsham Research Ctre Denholm

The present invention relates to novel thienopyrrolotriazinacetamide compounds of Formula (I): wherein R, Rand Rare defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

NLRP3 inflammasome inhibitors

The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R, R, R, R, Rand Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Aryl benzylamine compounds

A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: (I) wherein the variants R and X are defined in the specification. 

Aryl carboxylic acid cyclohexyl amide derivatives

A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the variants R, R9, Z, X, Q and Y are defined in the specification.

Chemokine receptor antagonists

A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the variants R, R9, Z, X, Q and Y are defined in the specification. 

A compound of formula I or a pharmaceutically acceptable salt, ester or prodrug thereof wherein the variables have the meanings as defined in the specification. Further disclosed are a method of inhibiting IKK activity using a compound of formula I, a method of inhibiting production of TNF using a compound of formula I, a compound of formula I for use as a pharmaceutical, a pharmaceutical composition comprising a compound of formula I, and use of a compound of formula I in the manufacture of a medicament for use as an immunosuppressant or anti-inflammatory agent. 

2-aminopyrimidine derivatives and their medical use

Novel hydroxamic acid derivatives, e.g., of formula (I), wherein R, R, Rand Rare as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of autoimmune and inflammatory diseases, e.g., multiple sclerosis and rheumatoid arthritis. Methods of making the compounds, novel intermediates, and pharmaceutical compositions comprising the compounds are provided. 

Hydroxamic acid derivatives

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Basel, Switzerland

Philipp Janser