Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-12-02
2000-12-12
Dees, Jose' G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142312, 5142315, 5142338, 5142342, 544 70, 544106, 544107, 544111, 544124, A61K 31535, C07D29500, C07D26530, C07D26500
Patent
active
061599670
ABSTRACT:
Compounds of the formula and quaternary ammonium ions thereof, wherein R.sup.1 and R.sup.2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4, alkenylene; D is oxygen; E is C.sub.2 alkylene; G is C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene; and L is --C(R.sup.4)(R.sup.5), wherein R.sup.4 and R.sup.5 together with the carbon atom to which they are attached represent a C.sub.5 -C.sub.10 cycloalkyl or a C.sub.5 -C.sub.10 heterocyclic. Especially preferred are compounds wherein L represents ##STR1## wherein J is a C.sub.1 -C.sub.6 alkylene; Ar is a ring carbocyclic or aromatic heterocyclic and S*.fwdarw.O is a sulfoxide in which the sulfur atom is in the 5-configuration. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK.sub.1 and NK.sub.2 receptors.
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Timothy P. Burkholder et al, "Identification and Chemical Synthesis of MDL 105,212, A Non-Peptide Tachykinin Antagonist with High Affinity for NK.sub.1 and NK.sub.2 Receptors", Bioorg. Med. Chem. Lett., 6, No. 8, 1996, pp. 951-956.
Database WPI, Derwent Abstract, AN 95-382750 of WO 95/28389 of Oct. 1996.
Fukazawa Tetsuya
Ishibashi Koki
Ito Kazuhiro
Kurata Hitoshi
Nakajima Katsuyoshi
Dees Jos,e G.
Qazi Sabiha N.
Sankyo Company Limited
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