N.sup.2 -naphthalenesulfonyl-L-arginine derivatives, and the pha

Details N.sup.2 -naphthalenesulfonyl-L-arginine derivatives, and the pha N.sup.2 -naphthalenesulfonyl-L-arginine derivatives, and the pha

1976-03-29

1977-12-13

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Parasitic organism or component thereof or substance...

2601125R, 260239A, 260239B, 260239E, 260268BC, 260288R, 260288D, 26029362, 260302R, 260302A, 2603067R, 260307R, 260307FA, 260307H, 2603261, 26032611R, 26032633, 2603265SF, 26050114, 260518R, 260556B, 424177, 424244, 424246, 424248, 424250, 560251, 560 10, 424258, 424316, 424319, 424270, 424321, 544 3, 424272, 544 54, 544 58, 424274, 544 63, 544 88, 424309, 544 98, 544159, 424311, A61K 31445, C07D21116

Patent

active

040629635

ABSTRACT:
N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the class consisting of (1) alkoxy, alkenyloxy, cycloalkoxy and halogenated alkoxy, respectively containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms; ##STR2## wherein R.sub.1 and R.sub.2 are members selected from the class consisting of hydrogen, alkyl, aryl, alkenyl and cycloalkyl, respectively containing not more than 10 carbon atoms, and aralkyl and cycloalkylalkyl, respectively containing not more than 15 carbon atoms, and substituted alkyl containing not more than 20 carbon atoms, said substituent being selected from the class consisting of alkoxy, alkoxycarbonyl, acyl, acyloxy, arylcarbamoyl and N,N-polymethylenecarbamoyl, respectively containing not more than 10 carbon atoms, and carboxy; and ##STR3## wherein Z is a divalent group containing up to 10 carbon atoms, which consists of more than one group selected from the class consisting of methylene --CH.sub.2 --, monosubstituted methylene ##STR4## wherein R.sub.3 is selected from the class consisting of alkyl, acyl, alkoxy and alkoxycarbonyl, respectively containing not more than 10 carbon atoms, and carbamoyl, and disubstituted methylene ##STR5## wherein R.sub.4 and R.sub.5 are alkyl groups of not more than 10 carbon atoms, and which may further contain at least one member selected from the class consisting of oxy-O-, thio -S-, cycloalkylene of not more than 10 carbon atoms, imino ##STR6## alkyl-substituted imino ##STR7## wherein R.sup.6 is an alkyl group of not more than 10 carbon atoms, acyl-substituted imino ##STR8## wherein R.sub.7 is an alkyl group of not more than 10 carbon atoms, and phenylene ##STR9## which may be arranged in any order and complete the ##STR10## ring together with the said methylene, monosubstituted methylene or disubstituted methylene, and R' is a member selected from the class consisting of 1-naphthyl substituted 2-, 3-, 4-, 6-, 7- or 8-dialkylamino, respectively, containing not more than 20 carbon atoms, and 1-naphthyl substituted with 5-dialkylamino containing 3-20 carbon atoms, 2-naphthyl substituted dialkylamino containing not more than 20 carbon atoms.

REFERENCES:
patent: 3622615 (1971-11-01), Nicolaides et al.
patent: 3978045 (1976-08-01), Okamoto et al.
Morrison et al., "Organic Chemistry," 2nd ed., Allyn and Bacon, Inc., Boston (1966), pp. 666-667.

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