Pegylated T1249 polypeptide
AssigneeHoffmann-La Roche Inc.
InventorsPascal Sebastian Bailon, Chee-Youb Won
Life of this patent
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Abstract
Pegylated T1249 polypeptide compounds are provided. Also provided are pharmaceutical compositions containing pegylated T1249 polypeptide compounds, and methods of making. Further provided are methods of inhibiting HIV infection using such compounds and compositions.
Claims149
A compound of formula (I),
- 9
- wherein
- R1 is a capping group,
- m is from 1 to 17,
- n is from 10 to 1,000,
- p is from 1 to 3, and
- NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
A compound of formula:
- CH3—O—(CH2—CH2—O)n—CH2—CH2—O—CH2—CH2—CH2-NHT1249 (III)
- wherein n is from 10 to 1,000 and NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
A pharmaceutical composition comprising, in admixture with a pharmaceutically acceptable excipient, a compound of formula:
- 12
- wherein
- R1 is a capping group,
- m is from 1 to 17,
- n is from 10 to 1,000,
- p is from 1 to 3, and
- NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
A pharmaceutical composition comprising, in admixture with a pharmaceutically acceptable excipient, a compound of formula:
- CH3—O—(CH2—CH2—O)n—CH2—CH2—O—CH2-CH2—CH2-NHT1249 (III)
- wherein n is from 10 to 1,000 and NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
A method of inhibiting HIV infection comprising administering a pharmaceutical composition comprising, in admixture with a pharmaceutically acceptable excipient, a compound of formula:
- 15
- wherein
- R1 is a capping group,
- m is from 1 to 17,
- n is from 10 to 1,000,
- p is from 1 to 3, and
- NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
86 A method according to claim 83, wherein R1 is selected from the group consisting of hydrogen, hydroxy, lower alkyl, lower alkoxy, lower cycloalkyl, lower alkenyl, aryl, and heteroaryl.
A method of inhibiting HIV infection comprising administering a pharmaceutical composition comprising, in admixture with a pharmaceutically acceptable excipient, a compound of formula:
- CH3—O—(CH2—CH2—O)n—CH2—CH2—O—CH2-CH2—CH2-NHT1249 (III)
- wherein n is from 10 to 1,000 and NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
A compound of formula:
- 18
- wherein
- R1 is methoxy,
- m is 1,
- n is from 100 to 750,
- p is 3, and
- NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
A pharmaceutical composition comprising, in admixture with a pharmaceutically acceptable excipient, a compound of formula:
- 19
- wherein
- R1 is methoxy,
- m is 1,
- n is from 100 to 750,
- p is 3, and
- NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
A method of inhibiting HIV infection comprising administering a pharmaceutical composition comprising, in admixture with a pharmaceutically acceptable excipient, a compound of formula:
- 20
- wherein
- R1 is methoxy,
- m is 1,
- n is from 100 to 750,
- p is 3, and
- NHT1249 is a T1249 polypeptide covalently bonded through its terminal α-amino group.
A method for attaching a polyethylene glycol molecule to a T1249 polypeptide comprising reacting a T1249 polypeptide with a polyethylene glycol aldehyde of formula:
- 21
- wherein
- R1 is a capping group,
- m is from 1 to 17,
- n is from 10 to 1,000, and
- p is from 1 to 3;
- to produce a compound of formula:
- R1—(CH2CH2O)n—CH2CH2—O—(CH2)m—CO—NH—(CH2)p—CH2—NH-T1249 (I)
- wherein the polyethylene glycol aldehyde molecule is bonded to the N-terminal amino group of the T1249 polypeptide.
Dependencies are inferred from the claim text.