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US 9,868,766 B2Granted
Peptides as oxytocin agonists
AssigneeHoffmann-La Roche Inc.
InventorsCaterina Bissantz, Konrad Bleicher, Christophe Grundschober
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Abstract
The invention relates to compounds of formula wherein variables are defined herein. It has been found that the present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrom.
Claims6
A compound of formula
- wherein
- R1 is hydroxy or amino;
- R2 is sec-butyl or isobutyl;
- R3 is lower alkyl, lower alkyl substituted by hydroxy, —(CH2)2C(O)—NH2, —(CH2)3—NH2 or —CH2-five membered aromatic heterocyclic group;
- R4 is hydrogen or lower alkyl;
- R5 is hydrogen or lower alkyl;
- or
- R4 and R5 may form together with the N and C atom to which they are attached a pyrrolidine ring, optionally substituted by hydroxy or halogen, a piperidine ring or an azetidine ring;
- R6 is hydrogen, lower alkyl, lower alkyl substituted by hydroxy, —(CH2)2C(O)OH, —(CH2)2C(O)NH2, benzyl optionally substituted by amino or hydroxy, —CH2-five membered aromatic heterocyclic group, indolyl, —CH2-cycloalkyl, cycloalkyl, —(CH2)2—S— lower alkyl or is —(CH2)1-4—NH2;
- R6′ is hydrogen or lower alkyl;
- or
- R6 and R6′ are together cycloalkyl;
- X is —C(O)—CHR—NR′—C(O)—;
- R/R′ are independently from each other hydrogen or lower alkyl;
- m is 2;
- o is 0 or 1;
- or a pharmaceutically acceptable acid addition salt, a racemic mixture or its corresponding enantiomer thereof.
14 more elements
Dependencies are inferred from the claim text.