Claims for Patent: 4,076,828

Summary for Patent: 4,076,828

Title:	Method of treating helminthiasis by parenteral administration of sulfoxide derivatives of benzimidazoles
Abstract:	A method is provided for treating or inhibiting helminthiasis by parenterally administering sulfoxide derivatives of benzimidazoles having the structure ##STR1## wherein R.sup.1 is lower alkyl or phenyl-lower alkyl, R.sup.2 and R.sup.3 may be the same or different and are hydrogen or lower alkyl, R.sup.4 is cycloalkyl, and m is 0 to 3, n is 0 to 3, m + n being .ltoreq. 5. Pharmaceutical compositions for use in the above method are also provided.
Inventor(s):	Haugwitz; Rudiger D. (Titusville, NJ), Cruthers; Larry R. (Flemington, NJ)
Assignee:	E. R. Squibb & Sons, Inc. (Princeton, NJ)
Application Number:	05/769,632
Patent Claims:	1. A method of treating or preventing helminthiasis, which comprises parenterally administering to a mammalian host an effective amount of a compound of the structure ##STR69## wherein R.sup.1 is lower alkyl, phenyl-lower alkyl, R.sup.2 and R.sup.3 are the same or different and are selected from the group consisting of hydrogen or lower alkyl, and R.sup.4 is cycloalkyl, m is 0 to 3, n is 0 to 3 and m + n is .ltoreq. 5, dispersed in a non-toxic nonpyrogenic physiologically acceptable carrier. 2. The method as defined in claim 1 where in said compound R.sup.1 is lower alkyl or benzyl. 3. The method as defined in claim 1 where in said compound R.sup.2 and R.sup.3 are hydrogen or methyl. 4. The method as defined in claim 1 wherein in said compound R.sup.4 contains 3 to 12 carbons. 5. The method as defined in claim 1 where in said compound m is 0 and n is 0, and R.sup.2 and R.sup.3 are hydrogen. 6. The method as defined in claim 1 wherein said compound has the name [5-[(cyclopropylmethyl)sulfinyl]-1H-benzimidazol-2-yl]carbamic acid, methyl ester. 7. The method as defined in claim 1 wherein said compound has the name [5-[(cyclobutylmethyl)sulfinyl]-1H-benzimidazol-2-yl]carbamic acid, methyl ester. 8. The method as defined in claim 1 wherein said compound has the name [5-[(cyclohexylmethyl)sulfinyl]-1H-benzimidazol-2-yl]carbamic acid, methyl ester. 9. The method as defined in claim 1 wherein said compound is administered subcutaneously. 10. The method as defined in claim 1 wherein said compound is administered intravenously. 11. An injectable composition for use in treating or preventing helminthiasis in mammalian species comprising an effective amount of a compound of the structure ##STR70## wherein R.sup.1 is lower alkyl, phenyl-lower alkyl, R.sup.2 and R.sup.3 are the same or different and are selected from the group consisting of hydrogen or lower alkyl, and R.sup.4 is cycloalkyl, m is 0 to 3, n is 0 to 3 and m + n is .ltoreq. 5, and a non-toxic non-pyrogenic physiologically acceptable carrier therefor selected from the group consisting of benzyl benzoate, 1,3-butylene glycol, ethyl oleate, glyceryl triacetate, mixtures thereof and a mixture of benzyl benzoate and sesame oil. 12. The composition as defined in claim 11 wherein said compound has the name [5-[(cyclopropylmethyl)sulfinyl]-1H-benzimidazol-2-yl]carbamic acid, methyl ester. 13. An injectable composition for use in treating or preventing helminthiasis in mammalian species comprising an effective amount of a compound of the structure ##STR71## wherein R.sup.1 is lower alkyl, phenyl-lower alkyl, R.sup.2 and R.sup.3 are the same or different and are selected from the group consisting of hydrogen or lower alkyl, and R.sup.4 is cycloalkyl, m is 0 to 3, n is 0 to 3 and m + n is .ltoreq. 5, and physiologically acceptable salts thereof, and sterile water for injection USP as a carrier therefor. 14. The composition as defined in claim 13 wherein said compound has the name [5-[(cyclopropylmethyl)sulfinyl]-1H-benzimidazol-2-yl]carbamic acid, methyl ester. 15. The composition as defined in claim 13 further including a non-toxic physiologically acceptable suspending agent. 16. The composition as defined in claim 15 wherein said suspending agent is carboxymethyl cellulose.

Details for Patent 4,076,828

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Sharp & Dohme Corp.	ZOSTAVAX	zoster vaccine live	For Injection	125123	05/25/2006		2039-09-23