Novel benzyl azetidine derivatives as sphingosine 1-phosphate (s1p) receptor modulators
AssigneeAllergan, Inc.
InventorsWenkui K. Fang, Liming Wang, Ken Chow, Evelyn G. Corpuz, Wha Bin Im
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Abstract
The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Claims10
A compound having Formula I, its enantiomers, diastereoisomers, hydrates, solvates, crystal forms and individual isomers, tautomers or a pharmaceutically acceptable salt thereof,
- wherein:
- A is C6-10 aryl;
- B is C3-8 cycloalkyl;
- R1 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R2 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R3 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R4 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R5 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R6 is H, halogen, —OC1-8 alkyl, C1-6 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R7 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R8 is halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- L is CH2;
- R9 is H, hydroxyl or C1-6 alkyl;
- R10 is H or C1-8 alkyl;
- R11 is H or C1-8 alkyl;
- and
- a is 0 or 1.
A method of treating a disorder associated with sphingosine-1-phosphate receptor modulation, which comprises administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of at least one compound of Formula I
- wherein:
- A is C6-10 aryl;
- B is C3-8 cycloalkyl;
- R1 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R2 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R3 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R4 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R5 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R6 is H, halogen, —OC1-8 alkyl, C1-6 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R7 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- R8 is halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R9, NR10R11 or hydroxyl;
- L is CH2;
- R9 is H, hydroxyl or C1-6 alkyl;
- R10 is H or C1-8 alkyl;
- R11 is H or C1-8 alkyl;
- and
- a is 0 or 1.
Dependencies are inferred from the claim text.