Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-05-11
2000-11-07
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514274, 514275, 514277, 514332, 514335, 514336, 514337, 514338, 514340, 514341, 514342, 544310, 544331, 544333, 546256, 546261, 546264, 546266, 5462684, 5462761, 5462804, 5462817, 5462824, 546285, A61K 31505, A61K 3144, C07D40100, C07D21328, C07D40900
Patent
active
061437514
DESCRIPTION:
BRIEF SUMMARY
This invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations including them and methods for their preparation.
European Patent Applications EP-A-0 264 114 and EP-A-0 267 439 disclose certain phenylalkyl- and phenylalkoxypyridine alkanol derivatives and their use as platelet-activating factor (PAF) antagonists.
A series of structurally distinct compounds have now been found to be useful for the modulation of inflammatory conditions. In a first aspect the present invention therefore provides a compound of formula I: ##STR1## wherein; X is O, S or CH.sub.2 ; 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; 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.sup.9, --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: 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; or C.sub.1-10 alkyl (optionally substituted by one or more fluorine atoms); 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,
Alkyl, alkylene and alkenylene groups, whether alone or part of another group, can be straight chained or branched and can be optionally substituted by one or more fluorine atoms and optionally interrupted by one or more oxygen atoms.
Suitably X is O, S or CH.sub.2. Preferably X is O.
Suitably 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. Preferably R.sup.1 and R.sup.2 are both hydrogen or one is hydrogen and the other is methyl.
Suitably 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.sup.9, --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. More than one substituent can be present. Preferred
REFERENCES:
patent: 5977105 (1999-11-01), Cheshire et al.
Cheshire David
Cladinggboel David
Cooper Martin
Hardern David
Hirst Simon
AstraZeneca UK Limited
Schroeder Ben
Shah Mukund J.
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