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US 10,246,422 B2Granted
Heterocyclic compounds and use thereof in medicine and in cosmetics
AssigneeGalderma Research & Development
InventorsJean-Francois Fournier, Laurence Clary, Etienne Thoreau
Life of this patent
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Abstract
The invention relates to novel heterocyclic compounds of general formula (I), as well as their pharmaceutically acceptable salts, and their enantiomers. The invention also relates to the use thereof as a medicinal product, preferably in the prevention and/or treatment of inflammatory diseases with a neurogenic component or use thereof as a cosmetic. The compounds of the present invention act as antagonists of the CGRP-R receptor.
Claims18
A heterocyclic compound of formula (I), or an enantiomer thereof, or a pharmaceutically acceptable salt thereof,
- wherein,
- Y is —CH2, —C(O), —C(CH3)2, or a spirocyclopropyl;
- R1 is
- R2, R3, and R6, which may be identical or different, are a hydrogen atom, F, or —CH3;
- R4 is a hydrogen atom, an alkyl, an alkene, an alkyne, a cycloalkyl, a cycloalkene, an aralkyl, a heteroaralkyl, or one of the following:
- R5 is a halogen;
- an alkyl;
- a cycloalkyl optionally substituted with R13, R14, and/or R15;
- an alkene;
- a cycloalkene;
- an alkyne;
- an ether;
- or one of the following:
- with Het representing 1 to 3 nitrogen atoms among the 6 atoms of the aromatic ring, and these nitrogen atoms may, independently of one another, be substituted with an oxygen atom to form an N-oxide group;
- R7 is
- with n=0 or 1;
- R8 and R9, which may be identical or different, are a hydrogen atom, F, or —CH3;
- R10 is hydrogen atom, —OR11, —SR11, —NR11R12, —S(O)R11, —SO2R11, —OC(O)R11, —CO2R11, a halogen, —NO2, —CN, —C(O)NR11R12, —CF3, or —OCF3;
- R11 and R12, which may be identical or different, are a hydrogen atom, a C1-C6 alkyl, CF3, or an ether;
- R13, R14, and R15, which may be identical or different, are a hydrogen atom, a C1-C6 alkyl, a cycloalkyl, —OR16, —NR16R17, a halogen, —OCF3, —CF3, —CN, —CO2R16, —CONR16R17, —NO2, —OCH2OR16, —SR16, —S(O)R16, —SO2R16, or an ether;
- A, B, and D, which may be identical or different, are a C, N, O, or S atom;
- R16 and R17, which may be identical or different, are a hydrogen atom, a C1-C6 alkyl, or —C(O)R18;
- Z is —CH2, O, or —NR18;
- and
- R18 is a hydrogen atom or a C1-C3 alkyl.
22 more elements
Dependencies are inferred from the claim text.