Claims for Patent: 11,965,040
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Summary for Patent: 11,965,040
| Title: | Modulation of complement activity |
| Abstract: | The present invention provides modulators of complement activity. Also provided are methods of utilizing such modulators as therapeutics. |
| Inventor(s): | Michelle Denise Hoarty, Ketki Ashok Dhamnaskar, Daniel Elbaum, Kristopher Josephson, Kelley Cronin Larson, Zhong Ma, Nathan Ezekiel Nims, Alonso Ricardo, Kathleen Seyb, Guo-Qing Tang, Douglas A. Treco, Zhaolin Wang, Ping Ye, Hong Zheng, Sarah Jacqueline Perlmutter, Robert Paul Hammer |
| Assignee: | UCB Inc |
| Application Number: | US17/236,247 |
| Patent Claims: |
1. A pharmaceutical composition comprising: a polypeptide that binds complement component C5, the polypeptide comprising the formula R1-Tyr-Xaa0-Glu-Tyr-R2, wherein: R1 comprises a polypeptide; Xaa0 is selected from the group consisting of Trp, azaTrp, N-methyl Trp, 1-methyl Trp, and 3-aminomethyl Phe; and R2 comprises a polypeptide; a pharmaceutically acceptable carrier or excipient. 2. The pharmaceutical composition of claim 1, wherein the polypeptide comprises a bridging moiety between two amino acids. 3. The pharmaceutical composition of claim 2, wherein the R1 polypeptide comprises the formula Xaa1-Val-Glu-Arg-Xaa2-Xaa3, wherein: Xaa1 is Cys or Lys; Xaa2 is Phe or Ala; and Xaa3 is Cys or Asp. 4. The pharmaceutical composition of claim 3, wherein the polypeptide comprises a bridging moiety between Xaa1 and Xaa3. 5. The pharmaceutical composition of claim 4, wherein the R1 polypeptide comprises the formula Xaa1-Val-Glu-Arg-Xaa2-Xaa3-Xaa4, wherein Xaa4 is selected from the group consisting of Asp, Ala, (S)-2-amino-3-(1H-tetrazol-5-yl)propanoic acid, alpha-methyl Asp, N-methyl Asp, cycloleucine, and 4-amino-tetrahydro-pyran-4-carboxylic acid. 6. The pharmaceutical composition of claim 5, wherein the R1 polypeptide comprises the formula Xaa1-Glu-Arg-Xaa2-Xaa3-Xaa4-Xaa5, wherein Xaa5 is selected from the group consisting of tert-butylglycine and Val. 7. The pharmaceutical composition of claim 1, wherein the R2 polypeptide comprises the formula Pro-Xaa6-Xaa7, wherein: Xaa6 is selected from the group consisting of cyclohexylglycine, phenylglycine (Phg), D-Phg, N-methyl Phg, Ala, and amino isobutyric acid, or is absent; and Xaa7 is selected from the group consisting of Lys, norvaline, and Pro, or is absent. 8. The pharmaceutical composition of claim 7, wherein Xaa7 is Lys. 9. The pharmaceutical composition of claim 8, wherein the Xaa7 Lys is conjugated with a lipid. 10. The pharmaceutical composition of claim 8, wherein the Xaa7 Lys comprises a modified lysine residue selected from the group consisting of N-ε-palmitoyl lysine, N-ε-lauryl lysine, N-ε-capryl lysine, N-ε-caprylic lysine, N-ε-(PEG2-γ-glutamic acid-N-α-octadecanedioic acid)lysine, N-ε-(PEG24-γ-glutamic acid-N-α-hexadecanoyl)lysine, and N-ε-1-(4,4-dimethyl-2,6-dioxocyclohex-1-ylidene)-3-methylbutyl-L-lysine. 11. The pharmaceutical composition of claim 1, wherein the polypeptide comprises an N-terminal acetyl group. 12. The pharmaceutical composition of claim 1, wherein the polypeptide comprises a C-terminal —NH2. |
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