Drechsleranol derivatives, processes for their preparation and their use
AssigneeAventis Pharma Deutschland GmbH
InventorsClaudia Eder, Michael Kurz, Luigi Toti
Life of this patent
Estimating the term…
Abstract
The present invention provides novel drechsleranol compounds of formula (I) which are formed by the microorganism Drechslera australiensis, ST 003360, DSM 14093, or a fungus ST 004112, DSM 14524, during fermentation. A process for their preparation, pharmaceutical compositions containing said drechsleranols, their use for the treatment and/or prophylaxis of degenerative neuropathies, such as, Alzheimer's disease, or psychiatric disorders, such as depression, sleep disturbances or seasonally related affective disorders, and their use as chelating agents or antioxidants are also disclosed and claimed. 1
Claims21
A compound of formula (I)
- 7
- wherein:
- R is H, or a group of the formula —(CH(OR2))5—CH2—OR2;
- R1 and R2 independently are H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl, wherein said C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl are optionally mono- or disubstituted by —OH, ═O, —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl, —NH—C2-C6-alkenyl, —NH2 or halogen, wherein said —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl and —NH—C2-C6-alkenyl substitutents are optionally substituted by —CN, —NH—C(O)—(C1-C6-alkyl) or ═NOH;
- or
- a stereoisomeric form thereof, or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition having JNK-3 inhibitory activity comprising a pharmaceutically acceptable carrier and an effective JNK-3 inhibitory amount of a compound of formula (I)
- 10
- wherein:
- R is H, or a group of the formula —(CH(OR2))5—CH2—OR2;
- R1 and R2 independently are H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl, wherein said C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl are optionally mono- or disubstituted by —OH, ═O, —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl, —NH—C2-C6-alkenyl, —NH2 or halogen, wherein said —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl and —NH—C2-C6-alkenyl substitutents are optionally substituted by —CN, —NH—C(O)—(C1-C6-alkyl) or ═NOH;
- or
- a stereoisomeric form thereof, or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition having hCK1ε inhibitory activity comprising a pharmaceutically acceptable carrier and an effective hCKIε inhibitory amount of a compound of formula (I)
- 11
- wherein:
- R is H, or a group of the formula —(CH(OR2))5—CH2—OR2;
- R1 and R2 independently are H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl, wherein said C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl are optionally mono- or disubstituted by —OH, ═O, —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl, —NH—C2-C6-alkenyl, —NH2 or halogen, wherein said —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl and —NH—C2-C6-alkenyl substitutents are optionally substituted by —CN, —NH—C(O)—(C1-C6-alkyl) or ═NOH;
- or
- a stereoisomeric form thereof, or a pharmaceutically acceptable salt thereof.
A method of inhibiting JNK-3 activity to treat a disease or disorder which comprises administering to a patient in need of said treatment an effective JNK-3 inhibitory amount of a compound of formula (I):
- 12
- wherein:
- R is H, or a group of the formula —(CH(OR2))5—CH2—OR2;
- R1 and R2 independently are H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl, wherein said C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl are optionally mono- or disubstituted by —OH, ═O, —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl, —NH—C2-C6-alkenyl, —NH2 or halogen, wherein said —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl and —NH—C2-C6-alkenyl substitutents are optionally substituted by —CN, —NH—C(O)—(C1-C6-alkyl) or ═NOH;
- or
- a stereoisomeric form thereof, or a pharmaceutically acceptable salt thereof.
A method of inhibiting hCKIε activity to treat a disease or disorder which comprises administering to a patient in need of said treatment an effective hCKIε inhibitory amount of a compound of formula (I):
- 13
- wherein:
- R is H, or a group of the formula —(CH(OR2))5—CH2—OR2;
- R1 and R2 independently are H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl, wherein said C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C6-C10-aryl are optionally mono- or disubstituted by —OH, ═O, —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl, —NH—C2-C6-alkenyl, —NH2 or halogen, wherein said —O—C1-C6-alkyl, —O—C2-C6-alkenyl, C6-C10-aryl, —NH—C1-C6-alkyl and —NH—C2-C6-alkenyl substitutents are optionally substituted by —CN, —NH—C(O)—(C1-C6-alkyl) or ═NOH;
- or
- a stereoisomeric form thereof, or a pharmaceutically acceptable salt thereof.
The strain Drechslera australiensis, ST 003360, DSM 14093.
The strain ST 004112, DSM 14524.
Dependencies are inferred from the claim text.