Chiesi Farmaceutici S.p.a.

Glaxo Group Limited

Pulmagen Therapeutics (inflammation) Limited

F. Hoffmann-la Roche Ag

Christine Edwards

Wei Li

Patrizia Tisselli

Janusz Jozef Kulagowski

Robert Andrew Heald

Po-wai Yuen

David Edward Clark

Nicholas Charles Ray

Snahel Patel

Alessandro Accetta

Gurdip Bhalay

Anna Maria Capelli

Arnaud Jean Francois Auguste Cheguillaume

Jonathan Mark Sutton

Carmelida Capaldi

Mark Edward Zak

Fabio Rancati

Harry Finch

Simon Charles Goodacre

Yun-Xing Cheng

Toby Jonathan Blench

Elizabeth O'Connor

Simon John Fawcett MacDonald

Garry Fenton

Gordon G Weingarten

Matthew W Cartwright

Andrea Nuzzi

Janus Kulagowski

Elizabeth Anne Skidmore

Mohammed Sajad

The invention relates to compounds of formula (I) inhibiting Rho Kinase that are meta tyrosine derivatives, processes for preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

Meta tyrosine derivatives as rho-kinase inhibitors

The invention relates to compounds of formula (I) inhibiting Rho Kinase that are oxidazole derivatives, processes for preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). 

Oxadiazole derivatives as Rho-Kinase Inhibitors

The invention relates to compounds of formula I inhibiting Rho Kinase that are tyrosine analogues derivatives, processes of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

Azaindole derivatives as Rho-kinase inhibitors

The invention relates to compounds of formula (I) inhibiting Rho Kinase that are tyrosine analogues derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). 

Tyrosine analogues derivatives as Rho-kinase inhibitors

Bicyclic dihydropyrimidine-carboxamide compounds of formula I described herein inhibit Rho Kinase and may be used for the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

Tyrosine amide derivatives as Rho-Kinase inhibitors

Bicyclic dihydropyrimidine-carboxamide compounds of formula I described herein inhibit Rho Kinase and may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), and pulmonary arterial hypertension (PAH).

Bicyclic dihydropyrimidine-carboxamide derivatives as Rho-Kinase inhibitors

Tyrosine amide compounds of formula I described herein inhibit Rho Kinase and may be used for the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

Tyrosine amide derivatives as Rho-kinase inhibitors

Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C&#x2014;Ror N; &#x2014;X&#x2014;X&#x2014; is CR&#x2550;N&#x2014; or &#x2014;NR&#x2014;CO&#x2014;; and R-R, R, Rand Rare as defined in the claims. 

Pyrimidine derivatives and their use in the treatment of respiratory diseases such a COPD

Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C&#x2014;Ror N; &#x2014;X&#x2014;X&#x2014; is CR&#x2550;N&#x2014; or &#x2014;NR&#x2014;CO&#x2014;; and R-R, Rand Rare as defined in the claims. 

Pyrimidine derivatives and their use in the treatment of respiratory diseases such as COPD

Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.

Compounds

The subject invention provides compounds of formula (I): Including monomers and multimers thereof that are inhibitors of human neutrophil elastase (HNE) activity and are useful in the treatment of diseases or conditions in which HNE plays a part.

Tetrahydropyrrolopyrimidinediones and their use in therapy

The compound of formula (I) is an inhibitor of human neutrophil elastase, useful for inhalation treatment of pulmonary inflammation. 

Pyrrolopyrimidinedione and its therapeutic use

The subject invention provides compounds of formula (1): including monomers and multimers thereof that are inhibitors of human neutrophil elastase (HNE) activity and are useful in the treatment of diseases or conditions in which HNE plays a part.

The present invention is directed to compounds of formula (I): whereinR represents a methyl or an ethyl groupX represents N, C&#x2014;H or C&#x2014;CHwhen X represents C&#x2014;H or C&#x2014;CH, Y represents Nwhen X represents N, Y represents C&#x2014;Hand physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

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Saffron Walden, United Kingdom

Christine Edwards