The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Feb. 27, 1996
Filed:
Sep. 09, 1994
Yea-Shun Cheng, Doylestown, PA (US);
Zenon D Konteatis, South Orange, NJ (US);
Mark J Macielag, Branchburg, NJ (US);
David C Palmer, Clinton, NJ (US);
Ohmeda Pharmaceutical Products Division Inc., Liberty Corner, NJ (US);
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.