Pyrrolidine derivatives as antiasthmatics

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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548557, 548413, 514 91, A61K 3140, C07D20710, C07F 902

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active

049161520

ABSTRACT:
The invention relates to novel compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkoxycarbonyl, phenylsulfonyl, phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, nitro, lower alkoxy, mono (or di or tri)halo(lower)alkyl and lower alkyl, phenylcarbamoyl, lower alkylsulfonyl, benzoyl or thienylsulfonyl;
R.sup.2 is phenylsulfonyl or phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, lower alkyl, lower alkoxy and mono(or di or tri)halo(lower)alkyl,
R.sup.3 is carboxy(lower)alkyl, lower alkyl substituted with carboxy and 1 to 3 halogen atom(s), esterified carboxy(lower)alkyl, carbamoyl(lower)alkyl, lower alkylsulfonylcarbamoyl(lower)alkyl, phenylsulfonylcarbamoyl(lower)alkyl, carboxyphenyl, esterified carboxyphenyl, carboxy, esterified carboxy, hydroxy(lower)alkyl, sulfino(lower)alkyl, phosphono(lower)alkyl, di(lower)alkoxyphosphoryl(lower)alkyl or halo(lower)alkyl,
R.sup.7 is hydrogen or lower alkyl, and
A is ##STR2## in which R.sup.8 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof, useful as therapeutic agents for thrombosis, asthma and nephritis.

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Frans M. Kaspersen et al.: J.C.S. Perkin I 1975, pp. 1617-1622.
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Patrick E. Hanna et al.: Journal of Medical Chemistry, 1973, vol. 16, No. 9, pp. 963-967.
A. M. Sepulchre et al.: Carbohyd. Res., 14 (1970) 1-8.
A. M. Sepulchre et al.: C. R. Acad. Sc. Paris, t. 268 (3 March, 1969), pp. 849-851.
Frans M. Kaspersen et al.: Heterocycles 2 (1974), pp. 15-19.

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