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US 10,208,089 B2Granted
Modulation of complement activity
AssigneeRa Pharmaceuticals, Inc.
InventorsMichelle 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
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Abstract
The present invention provides modulators of complement activity. Also provided are methods of utilizing such modulators as therapeutics.
Claims21
A polypeptide of the formula R1-Xaa0-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-R2, wherein:
- R1 is selected from the group consisting of an acetyl group, H, an acyl group, a heptanoyl group, an amide, a carbamate, urea, polyethylene glycol (PEG), hydroxyalkyl starch and chloroacetic acid, or is absent;
- Xaa0 is absent or Met;
- Xaa1 is selected from the group consisting of Cys, Lys, (S)-2-amino-5-azidopentanoic acid, and 3-thiopropionic acid, or is absent;
- Xaa2 is selected from the group consisting of Val, Ala, and D-Ala, or is absent;
- Xaa3 is selected from the group consisting of Glu, norvaline, and Ala, or is absent;
- Xaa4 is selected from the group consisting of Arg, Cys, Ala, Ser, and norvaline, or is absent;
- Xaa5 is selected from the group consisting of Phe, Tyr, N-methyl-tyrosine, and Ala, or is absent;
- Xaa6 is selected from the group consisting of Cys, Glu, N-methyl-glutamic acid, Asp, (S)-2-aminopent-4-ynoic acid, and Ala;
- Xaa7 is selected from the group consisting of Asp, Asn, N-methyl-asparagine, alpha-methyl L-aspartic acid, (S)-2-amino-3-(1H-tetrazol-5-yl)propanoic acid, N-methyl-aspartic acid, cycloleucine, 4-amino-tetrahydro-pyran-4-carboxylic acid, and Ala;
- Xaa8 is selected from the group consisting of tert-butylglycine, Val and Ala;
- Xaa9 is Tyr;
- Xaa10 is selected from the group consisting of 7-azatryptophan, Trp, 3-aminomethyl-L-phenyalanine, N-methyl-tryptophan, and 1-methyl-tryptophan;
- Xaa11 is Glu;
- Xaa12 is Tyr;
- Xaa13 is Pro;
- Xaa14 is selected from the group consisting of cyclohexylglycine, phenylglycine, D-phenylglycine, N-methyl-phenylglycine, amino isobutyric acid, and Ala, or is absent;
- Xaa15 is selected from the group consisting of norvaline, Lys, and Pro, or is absent;
- Xaa16 is absent or selected from the group consisting of N-ε-palmitoyl lysine, N-ε-lauryl lysine, N-ε-capryl lysine, N-ε-caprylic lysine, B20, B28, K14, Cys, and Lys;
- and
- R2 is —NH2 or is absent.
17 more elements
Dependencies are inferred from the claim text.