Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2007-02-27
2007-02-27
Tsang, Cecilia J. (Department: 1654)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S237500, C514S317000, C514S322000, C514S394000, C548S304400, C548S305400, C548S335500, C564S152000, C544S139000, C544S159000, C546S199000, C546S229000
Reexamination Certificate
active
11440727
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, —(C1–C8)alkyl or —(C1–C8)alkyl substituted by hydroxy;B is —(C1–C6)alkylguanidino, —(C1–C6)alkyl(4-imidazolyl), —(C1–C6)alkylamino, p-aminophenylalkyl(C1–C6)—, p-guanidinophenylalkyl(C1–C6)— or 4-pyridinylalkyl(C1–C6)—;D is —(CO)—, —(CO)—(C1–C6)alkylene or —(C1–C6)alkylene;E is a single bond or —(C1–C6)alkylene;Z is —NH2, —NH—(C1–C6)alkylcarboxamide, —NH— (C1–C6)alkyl, —NH— (N-benzyl), —NH-cyclo (C5–C7)alkyl, —NH-2-(1-piperidyl)ethyl, —NH-2-(1-pyrrolidyl)ethyl, —NH-2-(1-pyridyl)ethyl, —NH-2-(morpholino)ethyl, -morpholino, -piperidyl, —OH, —(C1–C6)alkoxy, —O-benzyl or —O-halobenzyl;R1, R2and R3are, independent of one another, -hydrogen, -arylcarbonylamino, —(C1–C6)alkoylamino, —(C1–C6)alkylamino, —(C1–C6)alkyloxy, —(C1–C6)alkylaminocarbonyl, -carboxy, —OH, -benzoyl, -p-halogenobenzoyl, -methyl, —S-(2,4-dinitrophenyl), —S-(3-nitro-2-pyridinesulfenyl), -sulfonyl, -trifluoromethyl, —(C1–C6)alkylaminocarbonylamino, -halo or -amino;R4and R5are, independent of one another, -hydrogen, —(C1–C6)alkyl, -methyloxy, -nitro, -amino, -arylcarbonylamino, —(C1–C6)alkoylamino, —(C1–C6)alkylamino, -halo or —OH.
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Bernatchez-Lemaire Irma
Le Hoang-Thanh
Lemaire Simon
Kosar Andrew D.
Tsang Cecilia J.
University of Ottawa
Welsh & Katz Ltd.
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