Claims
- 1. N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamides having the formula: ##STR7## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is naphthyl substituted with at least one C.sub.1 -C.sub.5 alkoxy; R.sub.2 is C.sub.2 -C.sub.10 alkylthioalkyl; R.sub.c is C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; and n is an integer of 1, 2 or 3.
- 2. The compound of claim 1, wherein R.sub.1 is naphthyl substituted with one or two C.sub.1 -C.sub.3 alkoxy; R.sub.2 is C.sub.2 -C.sub.6 alkylthioalkyl; R.sub.3 is C.sub.1 -C.sub.6 alkyl, phenyl or C.sub.7 -C.sub.10 aralkyl.
- 3. The compound of claim 1, wherein R.sub.1 is selected from the group consisting of 5-methoxy-1-naphthyl, 6-methoxy-2-naphthyl, 7-methoxy-2-naphthyl, 4,6-dimethoxy-2-naphthyl, 6,7-dimethoxy-2-naphthyl and 6,7-diethoxy-2-naphthyl; R.sub.2 is selected from the group consisting of 2-methylthioethyl, 2-ethylthioethyl and 3-methylthiopropyl; and R.sub.3 is methyl, ethyl, tert-butyl, phenyl or benzyl.
- 4. The compound of claim 3, which is N.sup.2 -(6,7-dimethoxy-2-naphthalenesulfonyl)-L-arginyl-N-(2-ethylthioethyl)glycine tert-butyl ester.
- 5. A method for inhibiting activity and suppressing activation of thrombin in vivo which comprises administering to a mammal a pharmaceutically effective amount of an N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamide having the formula: ##STR8## or the pharmaceutically acceptable salts thereof, wherein R.sub.1 is naphthyl substituted with at least one C.sub.1 -C.sub.5 alkoxy; R.sub.2 is C.sub.2 -C.sub.10 alkylthioalkyl; R.sub.3 is C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; and n is an integer of 1, 2 or 3.
BACKGROUND OF THE INVENTION
This application is a C-I-P Application of U.S. patent application Ser. No. 649,219, filed on Jan. 14, 1976, now U.S. Pat. No. 4,018,913.
US Referenced Citations (3)
Number |
Name |
Date |
Kind |
3131174 |
Schwyzer |
Apr 1964 |
|
4018913 |
Okamoto et al. |
Apr 1977 |
|
4018915 |
Okamoto et al. |
Apr 1977 |
|
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
649219 |
Jan 1976 |
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