Loloatin derivatives and analogs
OwnerMichael T. Kellyinventor
Life of this patent
Estimating the term…
Abstract
Several cyclic decapeptides having antibiotic activity are disclosed. The decapeptides are active against both gram positive and gram negative bacteria.
Claims55
A pharmaceutically acceptable salt of a compound wherein the compound is selected from the group consisting of:
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:1);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:2);
- and
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Trp-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:3).
A pharmaceutically acceptable derivative of a poly(amino acid) compound selected from the group consisting of:
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:1);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:2);
- and
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Trp-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:3)
- wherein at least one amino acid of the poly(amino acid) compound is an ester derivative of an amino acid sidechain containing a carboxylic acid group, or amide derivative of an amino acid sidechain containing a carboxylic acid group or an ether derivative of an amino acid sidechain containing a hydroxyl group.
A pharmaceutically acceptable salt of a compound selected from the group consisting of:
- cycloVal-Orn-Leu-Tyr-Pro-Phe-Phe-Asn-Asp-Tyr! (SEQ ID NO:76);
- cycloVal-Orn-Leu-Tyr-Pro-Phe-Phe-Asn-Asp-Trp! (SEQ ID NO:77);
- and
- cycloVal-Orn-Leu-Tyr-Pro-Trp-Phe-Asn-Asp-Trp! (SEQ ID NO:78).
The salt of a compound wherein the compound has a formula selected from the group:
- cycloVal-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:80);
- cycloL-Val-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:81);
- cycloL-Val-L-Orn-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:82);
- cycloL-Val-L-Orn-L-Leu-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:83);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:84);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:85);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:86);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-Asn-L-Asp-L-Tyr! (SEQ ID NO:87);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-Asp-L-Tyr! (SEQ ID NO:88);
- and
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-Tyr! (SEQ ID NO:89.
The salt of compound wherein the compound has a formula selected from the group:
- cycloVal-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:90);
- cycloL-Val-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:91);
- cycloL-Val-L-Orn-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:92);
- cycloL-Val-L-Orn-L-Leu-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:93);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:94);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-Phe-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:95);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:96);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-Asn-L-Asp-L-Trp! (SEQ ID NO:97);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-Asp-L-Trp! (SEQ ID NO:98);
- and
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-Trp! (SEQ ID NO:99).
The salt of a compound wherein the compound has a formula selected from the group:
- cycloVal-L-Orn-L-Leu-D-Tyr-L-Pro-L-Trp-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:100);
- cycloL-Val-Orn-L-Leu-D-Tyr-L-Pro-L-Trp-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:101);
- cycloL-Val-L-Orn-Leu-D-Tyr-L-Pro-L-Trp-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:102);
- cycloL-Val-L-Orn-L-Leu-Tyr-L-Pro-L-Trp-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:103);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-Pro-L-Trp-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:104);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-Trp-D-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:105);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Trp-Phe-L-Asn-L-Asp-L-Trp! (SEQ ID NO:106);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Trp-D-Phe-Asn-L-Asp-L-Trp! (SEQ ID NO:107);
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Trp-D-Phe-L-Asn-Asp-L-Trp! (SEQ ID NO:108);
- and
- cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Trp-D-Phe-L-Asn-L-Asp-Trp! (SEQ ID NO:109).
A pharmaceutically acceptable derivative of a poly(amino acid) compound selected from the group consisting of:
- cycloVal-Orn-Leu-Tyr-Pro-Phe-Phe-Asn-Asp-Tyr! (SEQ ID NO:76);
- cycloVal-Orn-Leu-Tyr-Pro-Phe-Phe-Asn-Asp-Trp! (SEQ ID NO:77);
- and
- cycloVal-Orn-Leu-Tyr-Pro-Trp-PheAsn-Asp-Trp! (SEQ ID NO:78)
- wherein the derivative is an ether derivative of an amino acid sidechain containing a hydroxyl group, or an ester derivative of an amino acid sidechain containing a carboxylic acid group or amide derivative of an amino acid sidechain containing a carboxylic acid group.
A pharmaceutically acceptable salt of the compound cycloL-Val-L-Orn-L-Leu-D-Tyr-L-Pro-L-Phe-D-Phe-L-Asn-L-Asp-L-Tyr! (SEQ ID NO:1).
Dependencies are inferred from the claim text.