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.

Date of Patent:
Feb. 27, 2007

Filed:

May. 25, 2006
Applicants:

Simon Lemaire, Aylmer, CA;

Irma Bernatchez-lemaire, Aylmer, CA;

Hoang-thanh Le, Ottawa, CA;

Inventors:

Simon Lemaire, Aylmer, CA;

Irma Bernatchez-Lemaire, Aylmer, CA;

Hoang-Thanh Le, Ottawa, CA;

Assignee:

University of Ottawa, Ottawa, CA;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 31/535 (2006.01); A61K 31/445 (2006.01); A61K 31/415 (2006.01); C07D 235/04 (2006.01); C07D 235/06 (2006.01); C07D 235/08 (2006.01); C07D 403/02 (2006.01); C07D 211/26 (2006.01); C07D 211/32 (2006.01); C07D 295/00 (2006.01); C07D 295/12 (2006.01); C07D 233/61 (2006.01); C07D 265/30 (2006.01);
U.S. Cl.
CPC ...
Abstract

The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activities. wherein: A is -hydrogen, —(C–C)alkyl or —(C–C)alkyl substituted by hydroxy; B is —(C–C)alkylguanidino, —(C–C)alkyl(4-imidazolyl), —(C–C)alkylamino, p-aminophenylalkyl(C–C)—, p-guanidinophenylalkyl(C–C)— or 4-pyridinylalkyl(C–C)—; D is —(CO)—, —(CO)—(C–C)alkylene or —(C–C)alkylene; E is a single bond or —(C–C)alkylene; Z is —NH, —NH—(C–C)alkylcarboxamide, —NH— (C–C)alkyl, —NH— (N-benzyl), —NH-cyclo (C–C)alkyl, —NH-2-(1-piperidyl)ethyl, —NH-2-(1-pyrrolidyl)ethyl, —NH-2-(1-pyridyl)ethyl, —NH-2-(morpholino)ethyl, -morpholino, -piperidyl, —OH, —(C–C)alkoxy, —O-benzyl or —O-halobenzyl; R, Rand Rare, independent of one another, -hydrogen, -arylcarbonylamino, —(C–C)alkoylamino, —(C–C)alkylamino, —(C–C)alkyloxy, —(C–C)alkylaminocarbonyl, -carboxy, —OH, -benzoyl, -p-halogenobenzoyl, -methyl, —S-(2,4-dinitrophenyl), —S-(3-nitro-2-pyridinesulfenyl), -sulfonyl, -trifluoromethyl, —(C–C)alkylaminocarbonylamino, -halo or -amino; Rand Rare, independent of one another, -hydrogen, —(C–C)alkyl, -methyloxy, -nitro, -amino, -arylcarbonylamino, —(C–C)alkoylamino, —(C–C)alkylamino, -halo or —OH.


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