Back to results
US 2012/0231999 A1Published application
Peptidic glp-2 agonists
AssigneeFerring B.V.
InventorsSudarkodi Alagarsamy, Guangcheng Jiang, Pierre Riviere, Claudio Daniel Schteingart, Javier Sueiras-Diaz
Life of this patent
Estimating the term…
Abstract
Novel GLP-2 analogs with improved pharmacokinetic properties are described as well as their use in the treatment of disease.
Claims26
A compound of formula I:
- wherein:
- R1 is chosen from the group consisting of H, alkyl, aralkyl and aryl;
- a is chosen from the group consisting of 0, 1, 2, 3, 4, 5, 6, and 7;
- R2 is a heteroaryl;
- b is 1 or 2;
- R3 and R4 are each independently selected from the group consisting of H and alkyl;
- c and d are each independently chosen from the group consisting of 0 and 1;
- R5 is chosen from the group consisting of, H and alkyl;
- e is chosen from the group consisting of 1, 2, 3, and 4;
- R6 is chosen from the group consisting of H, alkyl, cycloalkyl, aryl, biaryl, heteroaryl, and —C(O)—NH2, wherein R6 attaches so that the amino acid formed is in the D configuration;
- f is chosen from the group consisting of 0, 1, 2, and 3, with the proviso that if R6 is other than H, f is not 0;
- R7 is chosen from the group consisting of alkyl, cycloalkyl, aryl, biaryl, diaryl, heteroaryl and
- —C(O)—NH2;
- g is chosen from the group consisting of 1, 2, and 3;
- R8 is chosen from the group consisting of H, alkyl, —CH(OH)—CH3;
- h is chosen from the group consisting of 0, 1, 2, and 3;
- X1 is Gln or Arg;
- X2, X3, and X4 are each independently present or absent and if present, independently selected from the group consisting of Val, Leu, Ile, Ser, Thr, Asp, and Glu;
- Z is NR9R10 or OH, wherein:
- R9 and R10 are each independently selected from the group consisting of hydrogen, alkyl, heteroalkyl, cycloalkyl, aryl, heteroaryl, heteroaralkyl, aralkyl, and (CH2)x—[(CH2)2—O]—(CH2)x—[NH—C(O)—CH2—O—CH2]z—C(O)—NHR11, wherein:
- R11 is H or —[(CH2)2—O]y—(CH2)x—C(O)—NH2
- each x is independently selected from the group consisting of 0, 1, 2, and 3,
- each y is independently selected from the group consisting of 3, 4, 5, and 6,
- z is 0 or 1, and
- R9 and R10 are optionally joined to form a 4- to 7-membered ring which may be a heterocycle or a heteroaryl;
- and pharmaceutically acceptable salts thereof.
23 more elements
-31. (canceled)
Dependencies are inferred from the claim text.