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US 7,547,706 B2Granted
1H-pyrimido[4,5-b]indole derivatives, their preparation and therapeutic use
AssigneeSanofi-Aventis
InventorsJacques Froissant, Frank Marguet, Anne Olivier-Bandini, Frederic Puech
Life of this patent
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Abstract
The invention concerns compounds of general formula (I): Wherein n, X, Y, R1 and R2 are as defined herein. The invention also concerns a method for preparing the compounds and their therapeutic use.
Claims13
A compound of formula (I):
- in which:
- n represents the number 0 or 1;
- X represents a hydrogen or halogen atom;
- Y represents an OR3 group or an NR4R5 group;
- R1 represents a hydrogen atom or a (C1-C6)alkyl group;
- R2 represents a (C1-C6)alkyl group, a phenyl or a monocyclic or bicyclic heterocycle, said phenyl or heterocycle groups optionally bearing one or more halogen atoms and/or one or more (C1-C6)alkyl, (C1-C6)alkoxyl, (C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)alkylamino (C1-C6)alkyl or (C1-C6)dialkylamino (C1-C6)alkyl groups;
- R3 represents a hydrogen atom, a (C1-C6)alkyl group or a benzyl;
- and
- R4 and R5 each represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group, or else R4 and R5 form, with the nitrogen atom that they bear, an aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl or piperazinyl, optionally substituted by a (C1-C6)alkyl, phenyl or heterocycle;
- or
- a salt of said compound or a hydrate or a solvate of said compound or said salt.
8 more elements
A compound of formula (VII):
- in which
- OTf represents a triflate group;
- X represents a hydrogen or halogen atom;
- R1 represents a hydrogen atom or a (C1-C6)alkyl group;
- and
- R2 represents a (C1-C6)alkyl group, a phenyl or a monocyclic or bicyclic heterocycle, said phenyl or heterocycle groups optionally bearing one or more halogen atoms and/or one or more (C1-C6)alkyl, (C1-C6)alkoxyl, (C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)alkylamino (C1-C6)alkyl or (C1-C6)dialkylamino (C1-C6)alkyl groups.
3 more elements
A compound of formula (IX):
- in which
- X represents a hydrogen or halogen atom;
- R′ represents a (C1-C6)alkyl;
- R1 represents a hydrogen atom or a (C1-C6)alkyl group;
- R2 represents a (C1-C6)alkyl group, a phenyl or a monocyclic or bicyclic heterocycle, said phenyl or heterocycle groups optionally bearing one or more halogen atoms and/or one or more (C1-C6)alkyl, (C1-C6)alkoxyl, (C1-C6)alkoxy (C1-C6)alkyl, (C1-C6)alkylamino (C1-C6)alkyl or (C1-C6)dialkylamino (C1-C6)alkyl groups;
- and
- R4 and R5 each represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group, or else R4 and R5 form, with the nitrogen atom that they bear, an aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl or piperazinyl, optionally substituted by a (C1-C6)alkyl, phenyl or heterocycle.
4 more elements
A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, a hydrate or a solvate of said compound in combination with at least one pharmaceutically acceptable excipient:
- in which:
- n represents the number 0 or 1;
- X represents a hydrogen or halogen atom;
- Y represents an OR3 group or an NR4R5 group;
- R1 represents a hydrogen atom or a (C1-C6)alkyl group;
- R2 represents a (C1-C6)alkyl group, a phenyl or a monocyclic or bicyclic heterocycle, said phenyl or heterocycle groups optionally bearing one or more halogen atoms and/or one or more (C1-C6)alkyl, (C1-C6)alkoxyl, (C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)alkylamino (C1-C6)alkyl or (C1-C6)dialkylamino (C1-C6)alkyl groups;
- R3 represents a hydrogen atom, a (C1-C6)alkyl group or a benzyl;
- and
- R4 and R5 each represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group, or else R4 and R5 form, with the nitrogen atom that they bear, an aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl or piperazinyl, optionally substituted by a (C1-C6)alkyl, phenyl or heterocycle.
6 more elements
Dependencies are inferred from the claim text.