Anhydro-and isomer-a-21978c cyclic peptides
DC CAFC
First Claim
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1. A An isolated compound of the formula 1 in which R is C5-C14-alkanoyl;
- R1, R2, R3, R4 and R5 are hydrogen;
or a pharmaceutically acceptable salt thereof; and
wherein the alanine is D-alanine and the serine is D-serine.
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Abstract
Two new groups of A-21978C cyclic peptides, anhydro- and isomer-A21978C peptide derivatives, have antibacterial activity and are useful as intermediates. The two groups are prepared via transpeptidation of the parent cyclic peptides. Pharmaceutical formulations containing the new peptides as active ingredients and methods of treating infections caused by susceptible Gram-positive bacteria with the formulations are also provided.
The invention also provides an antibacterial composition containing the new drug substance LY 146032 in substantially pure form.
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Citations
31 Claims
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1. A An isolated compound of the formula 1
in which R is C5-C14-alkanoyl; - R1, R2, R3, R4 and R5 are hydrogen;
or a pharmaceutically acceptable salt thereof; and
wherein the alanine is D-alanine and the serine is D-serine. - View Dependent Claims (3, 4, 5, 6, 12, 14, 17)
- R1, R2, R3, R4 and R5 are hydrogen;
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2. A An isolated compound of the formula 2
in which R is C5-C14-alkanoyl; - R1, R2, R3, R4 and R5 are hydrogen;
or a pharmaceutically acceptable salt thereof; and
wherein the alanine is D-alanine and the serine is D-serine. - View Dependent Claims (7, 8, 9, 10, 11, 13, 15, 16)
- R1, R2, R3, R4 and R5 are hydrogen;
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18. An antibiotic composition comprised of a combination of a compound of formula 1, a compound of formula 2 and a compound of formula 3, or pharmaceutically acceptable salts thereof, wherein the formula 1 compound is
in which R is a C10 alkanoyl; - R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine;
the formula 2 compound isin which R is a C10 alkanoyl;
R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine; and
the formula 3 compound is an A21978C cyclic peptide ofwherein RN is n-decanoyl; and
wherein the total amount of the compound of formula 1 and the compound of formula 2, or salts thereof, in the combination is less than 6 weight percent.- View Dependent Claims (19, 21, 22, 23, 24, 25, 29)
- R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine;
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20. An antibiotic composition useful for the treatment of bacterial infections comprising a combination of a compound of formula 1, a compound of formula 2 and a compound of formula 3, or pharmaceutically acceptable salts thereof, wherein the formula 1 compound is
in which R is a C10 alkanoyl; - R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine;
the formula 2 compound isin which R is C10 alkanoyl;
R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine; and
the formula 3 compound is an effective antibacterial amount of an A21978C cyclic peptide compound ofwherein RN is n-decanoyl, in substantially pure form.
- R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine;
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26. A pharmaceutical formulation comprising a combination of a compound of formula 1, a compound of formula 2 and a compound of formula 3, or pharmaceutically acceptable salts thereof, wherein the formula 1 compound is
in which R is a C10 alkanoyl; - R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine;
the formula 2 compound isin which R is a C10 alkanoyl;
R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine; and
the formula 3 compound is an A21978C cyclic peptide ofwherein RN is n-decanoyl; and
wherein the total amount of the compound of formula 1 and the compound of formula 2, or salts thereof, in the combination is less than 6 weight percent, and the pharmaceutical formulation further comprises from about 0.1 to about 90 weight percent of the A21978C cyclic peptide of formula 3.- View Dependent Claims (27, 28)
- R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine;
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30. A pharmaceutical composition comprised of a combination of a compound of formula 1, a compound of formula 2 and a compound of formula 3, or pharmaceutically acceptable salts thereof, wherein the formula 1 compound is
in which R is a C10 alkanoyl; - R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine;
the formula 2 compound isin which R is a C10 alkanoyl;
R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine; and
the formula 3 compound is an A21978C cyclic peptide ofwherein RN is n-decanoyl; and
the total amount of the compound of formula 1 and the compound of formula 2, or salts thereof, in the combination is less than 6 weight percent; and
wherein an effective dose of the compound or salt of formula 3 is between about 0.1 and about 100 mg/kg of the compound;
or its pharmaceutically acceptable salt.- View Dependent Claims (31)
- R1, R2, R3, R4 and R5 are hydrogen, and wherein the alanine is D-alanine and the serine is D-serine;
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Litigation Data
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Current AssigneeCubist Pharmaceuticals, LLC (Merck & Co., Inc.)
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Original AssigneeEli Lilly and Company
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InventorsDebono, Manuel, Baker, Patrick J., Farid, Khadiga Z., Molloy, R. Michael
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Primary Examiner(s)Ponnaluri, Padmashri
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Application NumberUS09/547,357Time in Patent Office2,198 DaysField of Search514/9, 514/2, 530/317, 530/320US Class Current514/2.3CPC Class CodesA61K 38/00 Medicinal preparations cont...C07K 7/02 Linear peptides containing ...C07K 7/08 having 12 to 20 amino acids...
