US2021230159A1PendingUtilityA1
4h-pyrido[1,2-a]pyrimidin-4-one compounds
Est. expiryDec 2, 2034(~8.4 yrs left)· nominal 20-yr term from priority
Inventors:Penelope Jane HugginsJack Gordon ParsonsKevin Jeffrey BarnhamElisabeth Colette Louise GautierAntony Vincent Robinson
C07F 3/06C07D 498/14C07D 471/04A61P 25/00C07F 1/08A61K 31/519
70
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Claims
Abstract
The present invention relates to compounds of the formula I or II: (I) (II) processes for their preparation and their use as pharmaceutical agents or compositions in the treatment, of neurological disorders.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound of formula Ic:
in which
R 2 is (CH 2 ) n NR 9 R 10 ,
R 5 is H or C 1-4 alkyl;
R 6 is H or halo; provided that one of R 5 and R 6 is not hydrogen;
R 8 is H, C 1-4 alkyl or (CH 2 ) n aryl; and
R 9 and R 10 together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocyclyl in which the heterocyclyl group is optionally substituted with a C 1-4 alkyl aryl group in which the aryl group may be optionally substituted with one or two substituents selected from C 1-6 alkyl, halo, CF 3 , hydroxy, C 1-6 alkoxy or OCF 3 ;
n is 0, 1, 2 or 3;
each 5 or 6 membered heterocyclyl group may have 1, 2, 3 or 4 heteroatoms selected from O, S and N and may be saturated, unsaturated or aromatic;
or a pharmaceutically acceptable salt, stereoisomer or geometric isomer thereof.
2 . A compound according to claim 1 which is a compound of formula Ic wherein R 2 is (CH 2 ) n NR 9 R 10 ; R 5 is H or C 1-4 alkyl; and R 6 is halo.
3 . A compound according to claim 1 wherein R 5 is hydrogen and R 6 is chloro.
4 . A compound according to claim 1 wherein R 9 and R 10 form a piperidine ring.
5 . A compound according to claim 4 wherein the piperidine ring is substituted with CH 2 phenyl in which the phenyl group is optionally substituted with one or two substituents selected from C 1-6 alkyl, halo, CF 3 , hydroxy, C 1-6 alkoxy or OCF 3 .
6 . A compound of according to claim 1 which is
7 . A compound of formula II
in which
R 2 is (CH 2 ) n NR 9 R 10 ,
R 5 is H or C 1-4 alkyl;
R 6 is H or halo; provided that one of R 5 and R 6 is not hydrogen;
R 8 is H, C 1-4 alkyl or (CH 2 ) n aryl; and
R 9 and R 10 together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocyclyl in which the heterocyclyl group is optionally substituted with a C 1-4 alkyl aryl group in which the aryl group may be optionally substituted with one or two substituents selected from C 1-6 alkyl, halo, CF 3 , hydroxy, C 1-6 alkoxy or OCF 3 ;
n is 0, 1, 2 or 3;
each 5 or 6 membered heterocyclyl group may have 1, 2, 3 or 4 heteroatoms selected from O, S and N and may be saturated, unsaturated or aromatic;
or a pharmaceutically acceptable salt, stereoisomer or geometric isomer thereof;
and
M is transition metal.
8 . A pharmaceutical agent comprising an effective amount of the compound according to claim 1 , or a pharmaceutically acceptable salt or stereoisomer or geometric isomer thereof and a pharmaceutically acceptable carrier.
9 . A pharmaceutical agent comprising an effective amount of the compound according to claim 6 , or a pharmaceutically acceptable salt or stereoisomer or geometric isomer thereof and a pharmaceutically acceptable carrier.
10 . A pharmaceutical agent comprising an effective amount of the compound according to claim 7 , or a pharmaceutically acceptable salt or stereoisomer or geometric isomer thereof and a pharmaceutically acceptable carrier.Join the waitlist — get patent alerts
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