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Publication Number
US-11008366-B2
Publication Date
2021-05-18
Expiration Date
Abstract
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
Core Innovation
The disclosure describes peptidomimetic macrocycles having an amino acid sequence that is at least 80% identical to SEQ ID NO: 760, including embodiments at least 90% identical and embodiments where the amino acid sequence is SEQ ID NO: 760. The macrocycles are used in a method of treating neutropenia, thrombocytopenia, or anemia in a subject by administering an effective amount of the peptidomimetic macrocycle.
The peptidomimetic macrocycle is defined by Formula I with residues and substituents A-E and related structural-variable ranges, including capping group placement where residue D comprises the capping group. The disclosure also includes structural motif constraints that the peptidomimetic macrocycle includes an α-helix.
The document further provides peptidomimetic macrocycle sequence tables, including linear and cross-linked variants with specified i→i+4 or i→i+7 linking positions and numbered x-link connections. It also contains sequence and chemistry legends for interpreting sequence strings, including amino acid abbreviations, termini-related abbreviations, olefin amino acids, and crosslinker notations.
Claims Coverage
The claim coverage centers on administering a peptidomimetic macrocycle to treat neutropenia, thrombocytopenia, or anemia, with the core sequence requirement defined relative to SEQ ID NO: 760. Six inventive features are identified across the independent and dependent claims, including sequence identity thresholds, Formula I structural definition, capping group placement, and an α-helix motif.
Treating neutropenia, thrombocytopenia, or anemia with a peptidomimetic macrocycle
Administering an effective amount of a peptidomimetic macrocycle to a subject to treat neutropenia, thrombocytopenia, or anemia, wherein the peptidomimetic macrocycle comprises an amino acid sequence that is at least 80% identical to SEQ ID NO: 760.
High-identity peptidomimetic macrocycle sequence relative to SEQ ID NO: 760
The peptidomimetic macrocycle comprises an amino acid sequence that is at least 90% identical to SEQ ID NO: 760.
Exact SEQ ID NO: 760 peptidomimetic macrocycle sequence
The peptidomimetic macrocycle comprises an amino acid sequence specified as SEQ ID NO: 760.
Formula I-defined peptidomimetic macrocycle structure
The method is characterized by using a peptidomimetic macrocycle having Formula I, with residues and substituents defined by structural-variable ranges and integer indices.
Capping group included in residue D of Formula I
In the method, D comprises the capping group.
α-helix motif in the peptidomimetic macrocycle
The peptidomimetic macrocycle includes an α-helix.
Overall, the claim set covers treating neutropenia, thrombocytopenia, or anemia using a peptidomimetic macrocycle whose amino acid sequence matches SEQ ID NO: 760 to at least 80%, with dependent embodiments at least 90% or exactly SEQ ID NO: 760. Structural narrowing is provided by Formula I, residue D capping, and an α-helix requirement.
Stated Advantages
Improved cellular uptake.
Improved pharmacokinetic properties.
Improved bioavailability and blood circulation.
Reduced immunogenicity.
Increased frequency of administration is discussed in the document’s described context.
Documented Applications
Treating neutropenia.
Treating thrombocytopenia.
Treating anemia.
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