Aryl furan derivatives as PDE IV inhibitors
AssigneeMerck & Co., Inc.
InventorsHelene Perrier, Yongxin Han, Christopher Bayly, Dwight Mac Donald, Andre Giroux, Robert N. Young
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Abstract
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.
Claims9
A compound of Formula I ##STR63## or a pharmaceutically acceptable salt thereof wherein:
- Ar.sub.1 is an aromatic ring selected from phenyl, pyridinyl, or furyl, optionally substituted with up to two substituents, each substituent independently is:
- a) C.sub.1-6 alkyl, optionally substituted with --OH, --CO.sub.2 H, CO.sub.2 C.sub.1-3 alkyl, or CN,
- b) C.sub.1-6 alkoxy,
- c) C.sub.1-3 alkylthio,
- d) C.sub.1-3 alkylsulfonyl,
- e) C.sub.1-3 fluoroalkyl, optionally substituted with --OH,
- f) halo,
- g) --OH,
- h) --CO.sub.2 H, or
- i) --CO.sub.2 C.sub.1-3 alkyl;
- Ar.sup.2 is an aromatic ring selected from phenyl, benzothiazolyl, benzoxazolyl, pyrimidinyl, pyridinyl, purinyl or imidazolyl, optionally substituted with up to two substituents, each substituent independently is:
- 1) C.sub.1-6 alkyl,
- 2) C.sub.1-6 alkoxy,
- 3) --OH,
- 4) halo, or
- 5) CF.sub.3 ;
- R.sub.2 is
- a) hydrogen or
- b) C.sub.1-3 alkyl;
- and
- R.sub.3 is phenyl, pyridinyl, quinolinyl or furyl, optionally substituted with up to two substituents, each substituent independently is:
- a) C.sub.1-3 alkyl,
- b) C.sub.1-3 fluoroalkyl,
- c) C.sub.1-6 alkoxy,
- d) C.sub.1-3 fluoroalkoxy,
- e) C.sub.1-3 alkylthio,
- f) halo, or
- g) --OH.
Dependencies are inferred from the claim text.