Back to results
US 10,538,523 B2Granted
4-(biphen-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I) as GABA receptor modulators for use in the treatment of epilepsy and pain
AssigneePfizer Inc.
InventorsKevin Neil Dack, Robert McKenzie Owen, David Cameron Pryde
Life of this patent
Estimating the term…
Abstract
The present invention relates to pyrazolopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined in the description. The pyrazolopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They may useful in the treatment of a number of conditions, including pain and epilepsy.
Claims19
A compound according to formula (I)
- or a pharmaceutically acceptable salt thereof, wherein
- X is selected from —S(O)2— and —C(O)—;
- R1 is selected from (C2-C4)alkyl, (C3-C5)cycloalkyl and methyl-substituted (C3-C5)cycloalkyl;
- R2 is selected from H, F, Cl, OCH3 and CN;
- R3 is selected from H, F, CHF2, OCH3 and CN;
- when X is —S(O)2— then
- R4 is selected from (C1-C4)alkyl, (C3-C5)cycloalkyl, NH2 and NH(C1-C4)alkyl, and R5 is H;
- or
- R4 and R5 together are —CH2CH2— or —N(CH3)CH2—;
- and
- when X is —C(O)— then
- R4 is selected from NH2 and NH(C1-C4)alkyl, and R5 is H;
- or
- R4 and R5 together are —N(CH3)CH2—.
11 more elements
Dependencies are inferred from the claim text.