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US 8,076,329 B2Granted
Histamine H3-receptor ligands and their therapeutic applications
AssigneeBioprojet
InventorsIsabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz, Olivier Labeeuw
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Abstract
The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
Claims12
A compound of formula (I):
- wherein R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring of formula:
- with m=4 or 5, each Rb is independently identical or different, and Rb is a hydrogen or a C1-C4 alkyl, or 2 Rb form together a bond so as to form a bicyclic ring, chosen from:
- R is chosen from:
- a) a pyridyl group, or a cycloalkyl, each optionally substituted with one or more of Halogen atom, C1-C4 alkyl, O—C1-C4 alkyl, OH, or NR3R4;
- and where the N atom within the pyridyl ring may be in the form of N-Oxide (N+—O−), or
- bicyclic aryl substituted with one or more of Halogen atom, C1-C4 alkyl, O—C1-C4 alkyl, OH, NR3R4, —C2-C4 alkenyl or —C2-C4 alkynyl,
- where alkyl, alkenyl or alkynyl is optionally substituted with a heterocycle, or NR3R4;
- wherein R3, R4 are independently hydrogen, a straight or branched C1-C4 alkyl or an aryl group or taken together with the nitrogen atom to which they are attached form a saturated or partially unsaturated monocyclic or bicyclic heterocycle or heteroaryl optionally comprising one or more further heteroatoms and/or optionally substituted with one or more of Halogen atom, C1-C4 alkyl, O—C1-C4 alkyl or OH;
- or their pharmaceutically acceptable salts, or their optical isomers, racemates, diastereomers or enantiomers.
6 more elements
A compound of formula (I):
- wherein R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring of formula:
- with m=4 or 5, each Rb is independently identical or different, and Rb is a hydrogen or a C1-C4 alkyl, or 2 Rb form together a bond so as to form a bicyclic ring, chosen from:
- R is chosen from:
- a pyridyl group, where the pyridyl may be in the form of N-Oxide (N+—O−),
- or their pharmaceutically acceptable salts, or their optical isomers, racemates, diastereomers or enantiomers.
2 more elements
A pharmaceutical composition comprising a compound of formula (I′) with a pharmaceutically acceptable excipient or carrier, wherein said formula (I′) is:
- wherein R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring of formula:
- with m=4 or 5, each Rb is independently identical or different, and Rb is a hydrogen or a C1-C4 alkyl, or 2 Rb form together a bond so as to form a bicyclic ring, chosen from:
- R is chosen from:
- a) a pyridyl group, or a cycloalkyl, each optionally substituted with one or more of Halogen atom, C1-C4 alkyl, O—C1-C4 alkyl, OH or NR3R4 and where the N atom within the pyridyl ring may be in the form of N-Oxide (N+—O−), or
- bicyclic aryl substituted with one or more of Halogen atom, C1-C4 alkyl, O—C1-C4 alkyl, OH, NR3R4, —C2-C4, alkenyl or —C2-C4 alkynyl,
- where alkyl, alkenyl or alkynyl is optionally substituted with a heterocycle, or NR3R4;
- wherein R3, R4 are independently hydrogen, a straight or branched C1-C4 alkyl or an aryl group or taken together with the nitrogen atom to which they are attached form a saturated or partially unsaturated monocyclic or bicyclic heterocycle or heteroaryl optionally substituted with one or more of Halogen atom, C1-C4 alkyl, O—C1-C4 alkyl, or OH;
- or their pharmaceutically acceptable salts, or their optical isomers, racemates, diastereomers or enantiomers.
5 more elements
Dependencies are inferred from the claim text.