The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 02, 1999

Filed:

Nov. 04, 1997
Applicant:
Inventors:

Graham John Warrellow, Northwood, GB;

Ewan Campbell Boyd, Tullibody, GB;

Rikki Peter Alexander, High Wycombe, GB;

Assignee:
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K / ; A61K / ; C07D / ; C07D / ;
U.S. Cl.
CPC ...
514336 ; 514340 ; 514341 ; 514342 ; 514343 ; 514277 ; 5142278 ; 514255 ; 5142355 ; 514318 ; 546339 ; 546193 ; 544 586 ; 544360 ; 544124 ;
Abstract

Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is optionally substituted alkyl; X is --O--, --S-- or --N(R.sup.8)-, where R.sup.8 is hydrogen or alkyl; R.sup.2 is optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 is --(CH.sub.2).sub.n Ar, where Ar is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur and nitrogen atoms, wherein Ar is substituted by an optionally substituted C.sub.3-9 cycloaliphatic group optionally containing one or more heteroatoms selected from oxygen, sulphur or --N(R.sup.8)-, and n is zero or an integer 1, 2 or 3; R.sup.5 is --(CH.sub.2).sub.n Ar' where Ar' is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms or is Ar; R.sup.6 is hydrogen or optionally substituted alkyl; and R.sup.7 is hydrogen or optionally substituted alkyl; or a salt, solvate or hydrate thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.


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