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US 6,555,570 B2Granted
Compounds with growth hormone releasing properties
AssigneeNovo Nordisk A/S
InventorsThomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
Life of this patent
Estimating the term…
Abstract
Compounds of peptide mimetic nature having the general formula I wherein a and b are independently 1 or 2, R1 and R2 are independently H or C1-6alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
Claims16
A compound of formula I
- wherein
- R1 is hydrogen or C1-6-alkyl optionally substituted with aryl;
- R2 is C1-6-alkyl optionally substituted with aryl;
- a and b are independently 1 or 2;
- G is —O—(CH2)k—R27,
- J is —O—(CH2)l—R32,
- wherein
- R27, R28, R29, R30, R31, R32, R33, R34, R35 and R36 are hydrogen, halogen, aryl ,C1-6-alkyl or C1-6-alkoxy;
- k and l are independently 0, 1 or 2;
- D is
- R7—NH—(CR8R9)p−(CH2)m—M—(CHR10)o—(CH2)n—
- wherein
- R7, R8, R9 and R10 are independently hydrogen or C1-6 alkyl optionally substituted with halogen, amino, hydroxyl or aryl;
- n and m are independently 0, 1, 2, or 3;
- o and p are independently 0 or 1;
- M is —CR11═CR11a—, aryl, —O—, or —S—;
- R11 and R11a are independently hydrogen or C1-6-alkyl optionally substituted with aryl,
- E is
- —CONR12R13,
- wherein
- R12 is hydrogen or C1-6-alkyl optionally substituted with halogen, —CONR22R23, —N(R22)R23, —CF3, hydroxyl, C1-6-alkoxy, C1-6-alkoxy carbonyl, C1-6-alkylcarbonyloxy or aryl;
- R13 is
- wherein
- Q is —CH< or —N<,
- K and L are independently —CH2—, —CO—, —O—, —S—, —NR26— or a valence bond,
- where R26 is hydrogen or C1-6 alkyl, with the proviso that when Q is —CH<, at least one of K and L is —NR26—;
- t and u are independently 0, 1, 2, 3 or 4;
- R22 and R23 are independently hydrogen or C1-6 alkyl;
- v and w are independently 0, 1, 2 or 3;
- or a pharmaceutically acceptable salt thereof.
27 more elements
Dependencies are inferred from the claim text.