Claims
- 1. An N.sup.2 -arylsulfonyl-L-argininamide having the formula (I): ##STR816## or a pharmaceutically acceptable salt thereof, wherein R is ##STR817## wherein R.sub.1 is --COOR.sub.3 wherein R.sub.3 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.12 aralkyl or 5-indanyl; each R.sub.2 independently is hydrogen, C.sub.1 -C.sub.10 alkyl, phenyl, C.sub.1 -C.sub.5 alkoxy, C.sub.2 -C.sub.6 alkoxycarbonyl or carboxy; n is an integer of 1 to 4, R.sub.1 is substituted into the piperidine ring at the 2 or 3-position; and R.sub.2 is substituted into the piperidine ring at the 2, 3, 4, 5 or 6-position; and Ar is 5, 6, 7, 8-tetrahydronaphthyl or naphthyl each of which is optionally substituted with at least one substituent selected from the group consisting of halo, hydroxy, nitro, cyano and C.sub.1 -C.sub.10 alkyl.
- 2. The compound of claim 1 wherein R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.1 -C.sub.5 alkoxy.
- 3. The compound of claim 1, wherein R.sub.1 is substituted into the piperidine ring at the 2 position.
- 4. A pharmaceutical composition which comprises an antithrombotically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
- 5. A method of inhibiting activity and suppressing activation of thrombin in vivo which comprises administering to a mammal a pharmaceutical effective amount of a compound of claim 1.
Priority Claims (9)
Number |
Date |
Country |
Kind |
49-128774 |
Nov 1974 |
JA |
|
49-128775 |
Nov 1974 |
JA |
|
49-136695 |
Nov 1974 |
JA |
|
49-136697 |
Nov 1974 |
JA |
|
50-23268 |
Feb 1975 |
JA |
|
50-23635 |
Feb 1975 |
JA |
|
50-26768 |
Mar 1975 |
JA |
|
50-29357 |
Mar 1975 |
JA |
|
50-29358 |
Mar 1975 |
JA |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a continuation-in-part of the following applications:
Ser. No. 653,217 of Jan. 28, 1976
Ser. No. 713,486 of Aug. 11, 1976
Ser. No. 671,568 of Mar. 29, 1976
Ser. No. 703,704 of July 8, 1976
The Ser. No. 671,568 is a divisional of Ser. No. 622,390 filed Oct. 14, 1975, now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
3622615 |
Nicolaides et al. |
Nov 1971 |
|
3978045 |
Okamoto et al. |
Aug 1976 |
|
Related Publications (3)
|
Number |
Date |
Country |
|
713486 |
Aug 1976 |
|
|
703704 |
Jul 1976 |
|
|
671568 |
Mar 1976 |
|
Divisions (1)
|
Number |
Date |
Country |
Parent |
622390 |
Oct 1975 |
|
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
653217 |
Jan 1976 |
|