C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/5.1
C07K 14/70 (2006.01)
Patent
CA 1187872
Abstract of the Disclosure Compounds of the formula Image and pharmaceutically acceptable non-toxic acid addition salts thereof, in which R is hydrogen, methyl, or ethyl; A is the residue of a D-amino acid selected from Ala, Abu, Nva, Val, Nle, Leu, Ile, Gly(Al), Gly(Cp), Met, Cys(Me), Met(O), Cys(Me)(O), Ser, Thr, and Hse; R1 is hydrogen, C1-C3 primary alkyl, cyclo- propylmethyl, allyl, or propargyl; X is bromo, iodo, chloro, C1-C3 alkyl, tri- fluoromethyl, or C1-C2 alkoxy; B is the residue of a D- or L-amino acid lacking its carboxyl moiety and selected from Gly, Ala, Abu, Nva, Val, Nle, Leu, Ile, Pgl, Cys(Me), Cys(Me)(O), Cys(Me)(02), Cys(Et), Cys(Et)(O), Cys(Et)(O2), Met, Met(O), Met(02), Eth, Eth(O), Eth(02), Ser(Me), Ser(Et), Hse(Me), and Hse(Et) as well as any of such residues substituted at the amino nitrogen by a C1-C3 primary alkyl; Z is -CH20R2, Image , or Image , in which R2 is hydrogen or C1-C3 alkyl; subject to the proviso that, when R1 is other than hydrogen, B is the residue of an amino acid that lacks substitution at the amino nitrogen; which are useful analgesic agents, are described.
388253
Gesellschen Paul D.
Shuman Robert T.
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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