Claims for Patent: 4,650,807

Summary for Patent: 4,650,807

Title:	Antihistaminic compositions and methods containing pyridine derivatives
Abstract:	This disclosure describes a compound of Formula I ##STR1## (including its pharmaceutically acceptable salts and esters) which has potent antihistamine activity which is substantially free from sedative effects and which has little or no anticholinergic effects.
Inventor(s):	Findlay; John W. A. (Chapel Hill, NC), Coker; Geoffrey G. (Bromley, GB)
Assignee:	Burroughs Wellcome Co. (Research Triangle Park, NC)
Application Number:	06/753,791
Patent Claims:	1. A method of obtaining an antihistaminic effect in a mammal in need thereof comprising the oral, rectal, topical, nasal, ophthalmic or parenteral administration to said mammal of an effective antihistaminic amount of the compound of formula (I), ##STR10## or a pharmaceutically acceptable salt thereof. 2. The method of claim 1 wherein the mammal is a human. 3. The method of claim 2 wherein the compound of formula (I) is administered as the hydrochloride salt. 4. The method of claim 2 wherein the compound of formula (I) is administered as the sulfate salt. 5. The method of claim 2 wherein the compound of formula (I) is administered as the sodium salt. 6. The method of claim 2 wherein the compound of formula (I) is administered as the potassium salt. 7. The method of claim 2 in which the hydrochloride salt of the compound is orally administered. 8. The method of claim 1 in which the compound is administered orally and the mammal is a human. 9. The method of claim 8 in which the hydrochloride salt is administered. 10. A method of providing an antihistaminic and decongestant effect in a mammal which comprises the oral, rectal, topical, nasal, ophthalmic or parenteral administration to said mammal of a composition comprising an effective antihistaminic amount of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid or a pharmaceutically acceptable salt thereof and an effective decongestant amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor. 11. The method of claim 10 in which a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1-E-enyl)-2-pyridyl)acrylic acid and a pharmaceutically acceptable salt of pseudoephedrine are administered. 12. The method of claim 1 in which the salts are administered orally. 13. A pharmaceutical composition comprising an effective antihistaminic amount of the compound of formula (I), ##STR11## or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier therefor. 14. The composition as claimed in claim 13 in unit dosage form. 15. The composition as claimed in claim 14, in the form of a tablet, syrup, suppository or sterile aqueous preparation. 16. A composition containing 0.25 mg to 20 mg of a compound of formula (I) ##STR12## or a pharmaceutically acceptable salt thereof calculated as the free compound and a pharmaceutically acceptable carrier therefor. 17. The composition according to claim 16 in a capsule. 18. The composition according to claim 16 in the form of a tablet. 19. A composition containing 0.25 mg to 20 mg of a compound of formula (I) ##STR13## or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable liquid carrier therefor. 20. A composition comprising an effective antihistaminic amount of (E)-3-(6-3-pyrrolidino-1-(4-Tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid or a pharmaceutically acceptable salt thereof and an effective decongestant amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor. 21. The composition of claim 20 comprising an effective antihistaminic amount of a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid and an effective decongestant amount of a pharmaceutically acceptable salt of psuedophedrine and a pharmaceutically acceptable carrier therefor. 22. A tablet or capsule suitable for oral administration containing an effective antihistaminic amount of the hydrochloride salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid together with a pharmaceutically acceptable carrier therefor. 23. A pharmaceutical composition containing 0.25 mg to 20 mg of a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid together with a pharmaceutically acceptable carrier therefor. 24. The composition of claim 23 in which the salt is the hydrochloride salt. 25. A pharmaceutical composition for oral administration containing an effective antihistaminic amount of a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridylacrylic acid and a pharmaceutically acceptable liquid carrier therefor. 26. The composition of claim 25 in which the salt is the hydrochloride.