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US 6,143,751 AGranted
Pyridine derivatives and pharmaceutical compositions containing them
AssigneeAstraZeneca UK Limited
InventorsDavid Cheshire, David Cladinggboel, Martin Cooper, David Hardern, Simon Hirst, Carol Manners, Michael Stocks
Life of this patent
Estimating the term…
Abstract
Compounds of the formula (I) wherein X, R.sup.1, R.sup.2, and Ar.sup.1 as defined in the specification. The compounds are useful medicaments, particularly in the treatment of asthma or rhinitis.
Claims11
A compound of formula I:
- ##STR53## wherein;
- X is O, S or CH.sub.2 ;
- R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group;
- Ar.sup.1 is a fused bicyclic ring system containing one or more heteroatoms, a fused tricyclic ring system optionally containing an oxygen atom, or Ar.sup.1 is a group R.sup.3 --R.sup.4 where one of R.sup.3 /R.sup.4 is a phenyl ring and the other is a 5- or 6-membered heterocyclic ring containing one or more heteroatoms, each Ar.sup.1 group being optionally substituted by halo, nitro, C.sub.1-6 alkyl (optionally substituted by one or more fluorine atoms), CN, --Y--NR.sup.6 C(O)NR.sup.7 --R.sup.8, --O--Y--C(O)NR.sup.7 R.sup.8, --O--Y--C(S)NR.sup.7 R.sup.8, --Y--C(O)NR.sup.7 R.sup.8, --Y--C(S)NR.sup.7 R.sup.8, --Y--SO.sub.2 NR.sup.7 R.sup.8, --Y--NR.sup.7 R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, C(O)NR.sup.7 R.sup.8, C(S)NR.sup.7 R.sup.8, C(O)R.sup.9, --OC(O)R.sup.9, --Y--OR.sup.9, --Y--CO.sub.2 R, --Y--NR.sup.10 C(O)NR.sup.11 --Z--R.sup.12, SO.sub.2 NR.sup.10, C(O)NR.sup.7 R.sup.8, --Y--SO.sub.2 NHNR.sup.7 R.sup.8, --Y--C(O)NR.sup.11 --Z--R.sup.12, --Y--C(S)NR.sup.11 --Z--R.sup.12, N(R.sup.10)SO.sub.2 R.sup.11, N(R.sup.10)C(O)R.sup.11 or N(R.sup.10)CO.sub.2 R.sup.11 where:
- Y is a bond, C.sub.1-6 alkylene or C.sub.2-6 alkenylene;
- R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-6 alkyl or together with the nitrogen atom to which they are attached form an optionally substituted 5- to 7-membered heterocyclic ring optionally containing a further heteroatom selected from nitrogen, oxygen or sulfur;
- R.sup.5, R.sup.6, R.sup.9, R.sup.11 and R.sup.10 are independently hydrogen or C.sub.1-10 alkyl (optionally substituted by one or more fluorine atoms);
- Z is C.sub.1-6 alkylene;
- and
- R.sup.12 is a group NR.sup.10 C(O)R.sup.11, NR.sup.10 CO.sub.2 R.sup.11, OR.sup.5, NR.sup.7 R.sup.8 or CO.sub.2 R.sup.13 where R.sup.5, R.sup.7, R.sup.8, R.sup.10 and R.sup.11 are as defined above and R.sup.13 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkylaryl or aryl optionally substituted by hydroxy, or a salt or solvate thereof,
- provided that R.sup.4 is not thiazinyl, thiazolyl or alkyl substituted thiazolyl, and
- provided that when R.sup.4 is a pyridyl ring, said ring has one or more substituents as defined above other than alkyl groups.
9 more elements
Dependencies are inferred from the claim text.