Back to results
US 9,434,734 B2Granted
Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
AssigneeDomain Therapeutics
InventorsStanislas Mayer, Stephan Schann
Life of this patent
Estimating the term…
Abstract
The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.
Claims15
A compound of formula (I):
- wherein:
- A is N or C(H);
- B is aryl or heteroaryl;
- each R1 is independently selected from R5, halogen, —CF3, —CN, —OR5, —OCF3, —NR5R6,—COOR5, tetrazolyl, —SO3H, —B(OH)2, —CONR5R6, —COR5, —SR5, —SOR5, —SO2R5, —SO2NR5R6, —NR5COR6, —NR5SO2R6 or —OCOR5;
- n1 is 1,2 or 3;
- each R2 is independently selected from R5, halogen, —CF3, —CN, —OR5, —OCF3, —NR5R6, —COOR5, —CONR5R6, —COR5, —SR5, —SOR5, —SO2R5, SO2NR5R6, —NR5COR6, —NR5SO2R6, or —OCOR5;
- n2 is 1, 2 or 3;
- R3 is a -L-R7 group, wherein:
- L is a bond or C1-C4 alkylene, wherein one or more —CH2— units comprised in said alkylene are each optionally replaced by a group independently selected from —O—,—NR5—, —CO—, —S—, —SO—, or —SO2—;
- and
- R7 is selected from hydrogen, halogen, —CF3, —CN, an optionally substituted C1-C4 alkyl, an optionally substituted cycloalkyl, an optionally substituted heterocycloalkyl, an optionally substituted aryl, or an optionally substituted heteroaryl, wherein said C1-C4 alkyl, said cycloalkyl, said heterocycloalkyl, said aryl or said heteroaryl is optionally substituted with one or more groups independently selected from R5, halogen, —CF3, —CN, —NR5R6, —CONR5R6, —COR5, —OR5, —SR5, —SOR5, —SO2R5, —SO2N R5R6, —NR5COR6, —NR5SO2R6, —OCOR5, —COOR5, tetrazolyl, —SO3H, or —B(OH)2;
- R4 is selected from an optionally substituted C1-C4 alkyl, an optionally substituted cycloalkyl, or an optionally substituted heterocycloalkyl, wherein said C1-C4 alkyl is optionally substituted with one or more groups independently selected from cycloalkyl, halogen, —CF3, —CN, —OH or —O(C1-C4 alkyl), and further wherein said cycloalkyl or said heterocycloalkyl is optionally substituted with one or more groups independently selected from C1-C4 alkyl, cycloalkyl, halogen, —CF3, —CN, —OH or —O(C1-C4 alkyl);
- and
- each R5 and each R6 is independently selected from hydrogen, an optionally substituted C1-C4 alkyl, an optionally substituted cycloalkyl, or an optionally substituted heterocycloalkyl, wherein said C1-C4 alkyl is optionally substituted with one or more groups independently selected from halogen, —CF3, —CN, —OH, —O(C1-C4 alkyl), —NH2, —NH(C1-C4 alkyl) or —N(C1-C4 alkyl)(C1-C4 alkyl), and further wherein said cycloalkyl and said heterocycloalkyl are each optionally substituted with one or more groups independently selected from C1-C4 alkyl, halogen, —CF3, —CN, —OH, —O(C1-C4 alkyl), —NH2, —NH(C1-C4 alkyl) or —N(C1-C4 alkyl)(C1-C4 alkyl);
- or a pharmaceutically acceptable salt, solvate or prodrug thereof.
12 more elements
Dependencies are inferred from the claim text.