Peptide skeletal muscle relaxants

Details Peptide skeletal muscle relaxants Peptide skeletal muscle relaxants

1994-09-09

1996-02-27

Warden, Jill

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530331, 530345, A61K 3806

Patent

active

054948983

ABSTRACT:
Novel diquaternary polypeptides possessing skeletal muscle relaxation activity represented by the formulae: ##STR1## wherein: R is lower alkyl; R.sub.1 and R.sub.2 are lower alkyl or R.sub.1 and R.sub.2, together with the nitrogen to which they are attached form a heterocyclic ring having 5 to 7 member atoms; R.sub.3 is lower alkyl, [N,N-di(lower alkyl)-3-piperidinium].sup.(+), or [N,N-di(lower alkyl)-4-piperidinium].sup.(+) R.sub.4 is selected from the group consisting of t-butyl, benzyl or fluorenylmethyl; A.sub.1 is selected from the group consisting of trans-4-acetoxyproline, phenylalanine, glutamic acid-.gamma.-methyl ester, or proline; AA.sub.2 is selected from the group consisting of phenylalanine, leucine, 3-(2-naphthyl)alanine, 3-(1-naphthyl)alanine, and 3-cyclohexylalanine; AA.sub.3 is proline when R.sub.3 is [N,N-di(lower alkyl)-3-piperidinium].sup.(+) or [N,N-di(lower alkyl)-4-piperidinium].sup.(+), and is Orn(.delta.-N.sup.(+) --R--R.sub.1 --R.sub.2) or Lys(.epsilon.-N.sup.(+) --R--R.sub.1 --R.sub.2) when R.sub.3 ia lower alkyl; AA.sub.4 is Orn(.delta.-N.sup.(+)--R--R.sub.1 --R.sub.2) or Lys(.epsilon.-N.sup.(+) --R--R.sub.1 --R.sub.2); Z.sup.(-) is a pharmaceutically acceptable anion; and (R).sub.m R.sub.1 R.sub.2 N.sup.(+) represents the acceptable anion; (R).sub.m R.sub.1 R.sub.2 N.sup.(+) -- represents the alpha amino group of AA.sub.1 ; and m represents an integer of 0 or 1 with the proviso that m is zero only when AA.sub.1 is trans-4-acetoxyproline or proline.

REFERENCES:
patent: 5190924 (1993-03-01), Konteatis

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