Octahydro-2H-pyrido[1,2-a] pyrazine compounds
AssigneeLes Laboratories Servier
InventorsSolo Goldstein, Guillaume Poissonnet, Jean-Gilles Parmentier, Pierre Lestage, Brian Lockhart
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AssigneeLes Laboratories Servier
InventorsSolo Goldstein, Guillaume Poissonnet, Jean-Gilles Parmentier, Pierre Lestage, Brian Lockhart
Estimating the term…
A compound selected from those of formula (I): 1 wherein: Ra represents linear or branched (C1-C6)alkylene, X represents a group selected from W1, —C(W1)—W2—, —W2—C(W1)—, —W2—C(W1)W2—, —W2-Ra- and —CH(OR1)— wherein W1, W2 and R1 are as defined in the description, when Y represents aryl or heteroaryl, or X represents a group selected from single bond, —C(W1)—, —W2—C(W1)—, —W2-Ra and —CH(OR1)— wherein W1, W2, Ra and R1 are as defined hereinbefore, when Y represents a fused bicyclic group, of formula: 2 wherein: A represents nitrogen-containing heterocycle having from 4 to 7 ring members that is unsaturated or partially saturated and optionally contains a second hetero atom, B represents phenyl ring optionally substituted by one or more groups as defined in the description, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, medicinal products containing the same are useful in the treatment of cognitive deficiencies.
1- A compound selected from those of formula (I):
2- A compound of claim 1, wherein Ra represents linear (C2-C5)alkylene, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
3- A compound of claim 1, wherein R2 represents hydrogen, linear or branched (C1-C6)alkyl, or linear or branched (C1-C6)-acyl, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
4- A compound of claim 1, wherein it represent a compound of formula (IA):
5- A compound of claim 4, wherein X represents oxygen, and groups —C(W1)—W2—, —W2—C(W1)— and —N(R2)— wherein W1 represents oxygen, W2 represents oxygen or a group —NR2 and R2 represents hydrogen, linear or branched (C1-C6)alkyl, aryl, aryl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, and linear or branched (C1-C6)acyl, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
6- A compound of claim 4, wherein Y, represents phenyl optionally substituted by from 1 to 3 halogen, cyano, hydroxy, linear or branched (C1-C6)alkoxy, aryloxy, aryl-(C1-C6)alkoxy in which the alkoxy moiety is linear or branched, linear or branched (C1-C6)alkyl, linear or branched trihalo-(C1-C6)-alkyl, methylenedioxy and ethylenedioxy, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
7- A compound of claim 1, wherein it represent a compound of formula (IB):
8- A compound of claim 7, wherein Y2 represents a group of formula:
9- A compound of claim 7, wherein Y2 represents 2,3-dihydro-1H-indol-1-yl, 1H-indol-1-yl, 1H-indazol-1-yl, 1H-benzimidazol-1-yl, 3,4-dihydro-2H-quinol-1-yl, 2,3-dihydro-1H-4-quinolon-1-yl, 3,4-dihydro-2H-quinoxalin-1-yl and 2,3-dihydro-4H-1,4-benzoxazin-4-yl, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
10- A compound of claim 7, wherein X represents single bond, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
11- A compound of claim 1 which is:
12- A compound of claim 1 which is:
13- A method for treating a living body afflicted with a disease requiring antagonists of type H3 central histamine receptors, comprising the step of administering to the living body an amount of a compound of claim 1 which is effective for alleviation of said conditions.
14- The method of claim 13 for treating a living body afflicted with cognitive deficiencies associated with cerebral ageing and with neurodegenerative diseases, or with a disease like mood disorders, convulsive attacks, attention deficit hyperactivity syndromes, obesity and pain, comprising the step of administering to the living body an amount of a compound of claim 1 which is effective for alleviation of said conditions.
15- A method for treating a living body afflicted with cognitive deficiencies associated with Alzheimer's disease, Parkinson's disease, Pick's disease, Korsakoff's disease, and frontal and sub-cortical dementia of vascular or other origin, comprising the step of administering to the living body an amount of a compound of claim 1 which is effective for alleviation of said conditions.
16- A pharmaccutical composition useful in the claim 13 method, comprising as active principle an effective amount of a compound as claimed 1, together with one or more pharmaccutical acceptable excipients or vehicles.
17- A pharmeccutical composition useful in the claim 14 method comprising the step of administering to the living body an amount of a compound of claim 1 which is effective for alleviation of said conditions.
18- A pharmaccutical compostion useful in the claim 15 method comprising the step of administering to the living body an amount of a compound of claim 1 which is effective for alleviation of said conditions.