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US 12,624,002 B2Granted
Dimers for use in synthesis of peptidomimetics
AssigneeThe Feinstein Institutes for Medical Research
InventorsYousef Al-Abed, Ahmad Altiti
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Abstract
Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
Claims19
A compound of Formula (I):
- and salts thereof, wherein
- A is N-phthalimidyl or NR3R4, wherein (i) R3 is H and R4 is 9-fluorenylmethoxycarbonyl or 2-(3,5-dimethoxyphenyl) propan-2-yloxycarbonyl or (ii) R3 and R1 are connected and together form a side chain radical of proline and R4 is tert-butoxycarbonyl, 9-fluorenylmethoxycarbonyl or 2-(3,5-dimethoxyphenyl) propan-2-yloxycarbonyl;
- A1 is H or absent;
- A2 is H or absent;
- X is selected from the group consisting of imidazolyl, benzotriazolyl, S-D, and O-L;
- D is H, Cl, an alkyl, an aryl or a heteroaryl;
- L is imidazolyl or benzotriazolyl;
- R1 and R2 is each independently selected from the group consisting of side chain radicals of amino acids selected from the group consisting of side chain radicals of aspartic acid, phenylalanine, alanine, histidine, glutamic acid, tryptophan, valine, leucine, lysine, methionine, threonine, tyrosine, isoleucine, arginine, glycine, asparagine, serine, and glutamine;
- Z1 and Z2 is each independently C or N;
- and
- at least one of Z1 and Z2 is N.
8 more elements
A compound of Formula (I):
- and salts thereof, wherein
- A is NR3R4, wherein (i) R3 is H and R4 is 9-fluorenylmethoxycarbonyl or 2-(3,5-dimethoxyphenyl) propan-2-yloxycarbonyl or (ii) R3 and R1 are connected and together form a side chain radical of proline and R4 is tert-butoxycarbonyl, 9-fluorenylmethoxycarbonyl or 2-(3,5-dimethoxyphenyl) propan-2-yloxycarbonyl;
- A1 is H or absent;
- A2 is H or absent;
- X is selected from the group consisting of imidazolyl, benzotriazolyl, S-D, and O-L;
- D is H, Cl, an alkyl, an aryl or a heteroaryl;
- L is imidazolyl or benzotriazolyl;
- R1 and R2 is each independently selected from the group consisting of side chain radicals of amino acids selected from the group consisting of side chain radicals of aspartic acid, phenylalanine, alanine, histidine, glutamic acid, tryptophan, valine, leucine, lysine, methionine, threonine, tyrosine, isoleucine, arginine, glycine, asparagine, serine, and glutamine;
- and
- Z1 is N and Z2 is C, or Z1 is C and Z2 is N.
7 more elements
Dependencies are inferred from the claim text.