Claims for Patent: 5,292,756

Summary for Patent: 5,292,756

Title:	Novel sulfonamide fibrinogen receptor antagonists
Abstract:	A series of non-peptide derivatives of the formula
Inventor(s):	Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman
Assignee:	Medicure International Inc , Eisai Corp of North America
Application Number:	US07/860,747
Patent Claims:	1. A compound of the structural formula ##STR216## and the pharmaceutically acceptable salts thereof, wherein R4 isaryl, C1-10 alkyl, or C4-10 aralkyl,wherein aryl is phenyl, pyridyl, thienyl, tetrazole or oxazale; R5 is ##STR217## wherein R8 is hydroxy or C1-10 alkyloxy, ##STR218## wherein R9 and R10 are selected from the group consisting of hydrogen, C1-10 alkyl and phenyl C1-4 alkyl; Z is ##STR219## p is zero or one; and m is an integer from two to six. 2. A compound of claim 1, ##STR220## and the pharmaceutically acceptable salts thereof, wherein R4 isaryl, C1-10 alkyl, or C4-10 aralkyl,wherein aryl is phenyl, pyridyl, thiophenyl, tetrazole, or oxazole; R5 is ##STR221## wherein R8 is hydroxy or C1-10 alkyloxy, ##STR222## wherein R9 and R10 are selected from the group consisting of hydrogen, C1-10 alkyl and phenyl C1-4 alkyl; Z is O; p is zero or one; and m is an integer from two to six. 3. A compound as claimed in claim 2, of the structural formula ##STR223## 4. A compound as claimed in claim 2, of the structural formula ##STR224## 5. A compound as claimed in claim 2, of the structural formula ##STR225## 6. A compound of claim 1 selected from the group consisting of2-S-(2-Styrylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride; 2-S-(Phenylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride; 2-S-(2-Phenethylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride; 2-S-(2-Thienylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride; {2-[4-[4-Piperidin-4-yl)butyloxyphenyl]1-n-butylsulfonylamino)}ethanephosphonic acid ethyl ester; {2-[4-[4-Piperidin-4-yl)butyloxyphenyl]1n-butylsulfonylamino)}ethanephosphonic acid; and Ethyl-2-S-Benzylsulfonylamino-3-[4-(piperidin-4-yl)butyloxyphenyl]propionate; 2-S-(Butylsulfonylamino)-3-[4-(piperidin-4-yl)-1,1-dimethyl-butyloxyphenyl]propionic acid; and 3-S-(Butylsulfonylamino)-4-[4-piperidin-4-yl)butyloxyphenyl]butanoic acid. 7. A pharmaceutical composition, comprising a compound as claimed in claim 2, and a pharmaceutically acceptable carrier. 8. A pharmaceutical composition, comprising the compound as claimed in claim 3, and a pharmaceutically acceptable carrier. 9. A pharmaceutical composition, comprising the compound as claimed in claim 4, and a pharmaceutically acceptable carrier. 10. A pharmaceutical composition, comprising the compound as claimed in claim 5, and a pharmaceutically acceptable carrier. 11. A pharmaceutical composition, comprising a compound as claimed in claim 6, and a pharmaceutically acceptable carrier. 12. A method of blocking fibrinogen from acting at its platelet receptor site in a mannal, comprising the step of administering to said mammal a pharmacologically effective amount of a compound as claimed in claim 2. 13. The method as claimed in claim 12, wherein said compound is ##STR226## 14. The method as claimed in claim 12, wherein said compound is ##STR227## 15. The method as claimed in claim 12, wherein said compound is ##STR228## 16. The method as claimed in claim 12, wherein said compound is selected from2-S-(2-Styrylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride; 2-S-(Phenylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]-propionic acid hydrochloride; 2-S-(2-Phenethylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride; 2-S-(2-Thienylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride; {2-[4-[4-Piperidin-4-yl)butyloxyphenyl]-1-n-butylsulfonylamino)}ethanephosphonic acid ethyl ester; {2-[4-[4-Piperidin-4-yl)butyloxyphenyl]-1-n-butylsulfonylamino)}ethanephosphonic acid; and Ethyl-2-S-Benzylsulfonylamino-3-[4-(piperidin-4-yl)butyloxyphenyl]propionate; 2-S-(Butylsulfonylamino)-3-[4-(piperidin-4-yl)-1,1-dimethyl-butyloxphenyl]propionic acid; and 3-S-(Butylsulfonylamino)-4-[4-piperidin-4-yl)butyloxyphenyl]butanoic acid.