Merck Frosst Canada & Co.

Merck Frosst Canada, Inc.

Merck Canada Inc.

Mario Girard

Daniel Guay

Pierre A Hamel

Yves Girard

Yves Ducharme

Richard Frenette

Richard W Friesen

Marc Blouin

Sebastien Laliberte

Bernard Cote

Evelyn Martins

Richard Freisen

Cedrickx Godbout

Yongxin Han

Zhaoyin Wang

Cameron Black

Michel L Belley

John Colucci

Jason Burch

Chun Li

Helene Perrier

Sylvie Prescott

Julie Farand

Daaniel Guay

The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included. 

Quinoline derivatives as EP4 antagonists

Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.

Tri-aryl-substituted-ethane PDE4 inhibitors

Alkyne-aryl phosphodiesterase-4 inhibitors

1-biaryl-1,8-naphthyridin-4-one phosphodiesterase-4 inhibitors

The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3&prime;,5&prime;-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4).

Heterosubstituted pyridine derivatives as PDE4 inhibitors

Heterosubstituted pyridine derivatives as PDE 4 inhibitors

The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Diphenyl stilbenes as prodrugs to COX-2 inhibitors

The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). ##STR1## The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.

Tri-aryl ethane derivatives as PDE IV inhibitors

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Saint-Lazare, Canada

Mario Girard