Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1999-03-19
2000-07-04
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514311, 514326, 514314, 514317, 514318, 514319, 514320, 514321, 514323, 514324, 514329, 544105, 544106, 546153, 546155, 546157, 546174, 546194, 546196, 546197, 546202, 546205, 546207, 546209, 546210, 546213, 546214, 546223, 546224, A61K 3140, A61K 31445, C07D20714, C07D21156
Patent
active
060839430
ABSTRACT:
A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C.sub.2 -C.sub.4 alkylene; Z is a valence bond or C.sub.1 -C.sub.6 alkylene; R.sup.1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.3 is hydrogen, hydroxy or the like; R.sup.4 is substituted or unsubstituted benzyl or the like. Typical examples are (2S*,3S*,4R*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy-benzyl)amino]-5-me thyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-2- phenylpiperidine. The novel substituted azaheterocyclecarboxylic acids in this invention have excellent substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.
REFERENCES:
patent: 5232929 (1993-08-01), Desai et al.
Ikunaka Masaya
Nakane Masami
Shishido Yuji
Ginsburg Paul H.
Kifle Bruck
Pfizer Inc
Raymond Richard L.
Richardson Peter C.
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