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Details for Patent: 4,657,918

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Details for Patent: 4,657,918

Title: 3-[6-[3-pyrrolidino-1-(4-tolyl)prop-1e-enyl]-2-pyridyl]propionic acid and derivatives having anti-histaminic activity
Abstract:This disclosure describes compounds of Formula I. ##STR1## (including their pharmaceutically acceptable salts and esters) which have potent antihistamine activity which are substantially free from sedative effects.
Inventor(s): Findlay; John W. A. (Chapel Hill, NC), Coker; Geoffrey G. (Bromley, GB2)
Assignee: Burroughs Wellcome Co. (Research Triangle Park, NC)
Filing Date:Sep 25, 1985
Application Number:06/779,877
Claims:1. A compound of formula (I) ##STR11## a straight or branched lower alkyl (1-4 carbon atoms) ester, or a pharmaceutically acceptable salt thereof; wherein R.sup.1 is (CH.sub.2).sub.n, n is an integer 1-7, or R.sup.2 and R.sup.3 are the same or different and are hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen to which they are attached form a azacyclobutane, pyrrolidine or piperdine ring; R.sup.4 is hydrogen, halogen, C.sub.1-4 alkoxy or C.sub.1-4 alkoxy or C.sub.1-4 alkyl optionally substituted by one to three halogen atoms.

2. 3-{6-[3-Pyrrolidino-1-(4-tolyl)prop-1E-enyl]-2-pyridyl}propionic acid.

3. A pharmaceutically acceptable salt of 3-{6-[3-Pyrrolidino-1-(4-tolyl)prop-1E-enyl]-2-propionic acid.

4. The hydrochloride salt of claim 3.

5. A method of providing an antihistiminic effect in a mammal in need thereof comprising administering to said mammal an effective antihistimatic amount of the compound of formula (I), ##STR12## or a pharmaceutically acceptable salt thereof; wherein R.sup.1 is (CH.sub.2).sub.n, n is an integer 1-7; R.sup.2 and R.sup.3 are the same or different and are hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen to which they are attached form a azayclobutane, pyrrolidine, or piperdine ring; R.sup.4 is hydrogen, C.sub.1-4 alkoxy or C.sub.1-4 alkyl optionally substituted by one to three halogen atoms.

6. A method of obtaining an antihistiminic effect in a mammal in need thereof comprising administering of an effective antihistiminic amount of the compound of claim 2 to said mammal.

7. A method of obtaining an antihistiminic effect in a mammal in need thereof comprising administering of an effective antihistiminic amount of claim 3 to said mammal.
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