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Generated: September 19, 2017

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Title: Novel sulfonamide fibrinogen receptor antagonists
Abstract:A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
Inventor(s): Duggan; Mark E. (Narberth, PA), Egbertson; Melissa S. (Ambler, PA), Halczenko; Wasyl (Hatfield, PA), Hartman; George D. (Lansdale, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:07/860,747
Patent Claims: 1. A compound of the structural formula ##STR216## and the pharmaceutically acceptable salts thereof, wherein R.sup.4 is

aryl,

C.sub.1-10 alkyl, or

C.sub.4-10 aralkyl,

wherein aryl is phenyl, pyridyl, thienyl, tetrazole or oxazale;

R.sup.5 is ##STR217## wherein R.sup.8 is hydroxy or C.sub.1-10 alkyloxy, ##STR218## wherein R.sup.9 and R.sup.10 are selected from the group consisting of hydrogen, C.sub.1-10 alkyl and phenyl C.sub.1-4 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 R.sup.4 is

aryl,

C.sub.1-10 alkyl, or

C.sub.4-10 aralkyl,

wherein aryl is phenyl, pyridyl, thiophenyl, tetrazole, or oxazole;

R.sup.5 is ##STR221## wherein R.sup.8 is hydroxy or C.sub.1-10 alkyloxy, ##STR222## wherein R.sup.9 and R.sup.10 are selected from the group consisting of hydrogen, C.sub.1-10 alkyl and phenyl C.sub.1-4 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 of

2-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]propioni c 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)}ethanephosph onic acid ethyl ester;

{2-[4-[4-Piperidin-4-yl)butyloxyphenyl]1n-butylsulfonylamino)}ethanephospho nic acid; and

Ethyl-2-S-Benzylsulfonylamino-3-[4-(piperidin-4-yl)butyloxyphenyl]propionat e;

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 from

2-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]propioni c 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)}ethanephosp honic acid ethyl ester;

{2-[4-[4-Piperidin-4-yl)butyloxyphenyl]-1-n-butylsulfonylamino)}ethanephosp honic acid; and

Ethyl-2-S-Benzylsulfonylamino-3-[4-(piperidin-4-yl)butyloxyphenyl]propionat e;

2-S-(Butylsulfonylamino)-3-[4-(piperidin-4-yl)-1,1-dimethyl-butyloxphenyl]p ropionic acid; and

3-S-(Butylsulfonylamino)-4-[4-piperidin-4-yl)butyloxyphenyl]butanoic acid.
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