Claims
- 1. N.sup.2 -naphthalenesulfonyl-L-argininamides having the formula ##STR15## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is selected from the group consisting of naphthyl, 5,6,7,8-tetrahydronaphth-1-yl, 5,6,7,8-tetrahydronaphth-2-yl and naphthyl substituted with one or two substituents selected from the group consisting of halo, nitro, cyano, hydroxy, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, and di(C.sub.1 -C.sub.10) alkylamino; R.sub.2 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, phenyl, naphthyl, phenyl-C.sub.1 -C.sub.6 -alkyl, and naphthyl-C.sub.1 -C.sub.2 alkyl; Z is oxy, thio, or sulfinyl; and n is an integer of 0 or 1.
- 2. The compound of claim 1, wherein R.sub.1 is selected from the group consisting of 1-naphthyl, 2-naphthyl, 5,6,7,8-tetrahydro-1-naphthyl, 5,6,7,8-tetrahydro-2-naphthyl, 6-methyl-2-naphthyl, 6-methyl-1-naphthyl, 7-methyl-1-naphthyl, 7-methyl-2-naphthyl, 6-ethyl-2-naphthyl, 6,7-dimethyl-1-naphthyl, 6,7-dimethyl-2-naphthyl, 6-isopropyl-2-naphthyl, 5-chloro-1-naphthyl, 6-chloro-2-naphthyl, 6-bromo-1-naphthyl, 5-hydroxy-1-naphthyl, 7-hydroxy-2-naphthyl, 5-dimethylamino-1-naphthyl, 5-dimethylamino-2-naphthyl, 5-diethylamino-1-naphthyl, 6-dimethylamino-1-naphthyl and 6-dimethylamino-2-naphthyl, 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; and R.sub.2 is hydrogen, ethyl or tert-butyl; Z is oxy, thio or sulfinyl; and n is an integer of 0 or 1.
- 3. The compound of claim 2, wherein Z is thio and n is 0.
- 4. The compound of claim 2, wherein Z is oxy, thio or sulfinyl, and n is 1.
- 5. A compound of claim 4, which is 4-[N.sup.2 -(7-methoxy-2-naphthalenesulfonyl)-L-arginyl]thiomorpholine-3-carboxylic acid.
- 6. A compound of claim 4, which is 4-[N.sup.2 -(6,7-dimethoxy-2-naphthalenesulfonyl)-L-arginyl]morpholine-3-carboxylic acid.
- 7. A compound of claim 4, which is 4-[N.sup.2 -(7-methoxy-2-naphthalenesulfonyl)-L-arginyl]morpholine-3-carboxylic acid.
- 8. A pharmaceutical composition for inhibiting activity and suppressing activation of thrombin in vivo, which comprises an amount effective to inhibit activity and suppress activation of thrombin in vivo, of a compound of claim 1 and a pharmaceutically acceptable carrier.
- 9. A method of inhibiting activity and suppressing activation of thrombin in vivo, which comprises administering to a patient an amount effective to inhibit activity and suppress activation of thrombin in vivo, of the N.sup.2 -naphthalenesulfonyl-L-argininamide of claim 1.
CROSS REFERENCE TO RELATED APPLICATIONS
This application is a continuation in part of applications Ser. No. 671,436 March 29, 1976, and Ser. No. 671,568 filed Mar. 29, 1976, now Pat. No. 4,049,645, issued Sept. 20, 1977, which in turn are divisionals of application Ser. No. 622,390 filed Oct. 14, 1975, now abandoned.
Related Publications (1)
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Number |
Date |
Country |
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671568 |
Mar 1976 |
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Divisions (1)
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Number |
Date |
Country |
Parent |
622390 |
Oct 1975 |
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Continuation in Parts (1)
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Number |
Date |
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Parent |
671436 |
Mar 1976 |
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