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US 8,507,686 B2Granted
Substituted bicyclic methyl azetidines as sphingosine-1 phosphate receptors modulators
AssigneeAllergan, Inc.
InventorsJanet A. Takeuchi, Ling Li, Wha Bin Im
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel substituted bicyclic methyl azetidine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
Claims7
A compound having Formula I, its individual enantiomers, individual diastereoisomers, and individual isomers, individual tautomers or a pharmaceutically acceptable salt thereof
- wherein:
- represents a single bond,
- or a double bond
- represents a single bond,
- or a double bond
- or a triple bond
- A is substituted or unsubstituted C6-10 aryl, substituted or unsubstituted heterocycle, substituted or unsubstituted C5-8 cycloalkyl, substituted or unsubstituted C5-8 cycloalkenyl, or hydrogen;
- R2 is hydrogen, halogen, —OC1-3 alkyl, substituted or unsubstituted C1-3 alkyl, CN, C(O)R7, NR8R9 or hydroxyl;
- R3 is OPO3H2, carboxylic acid, PO3H2, substituted or unsubstituted C1-6 alkyl, —S(O)2H, —P(O)MeOH, —P(O)(H)OH or OR10;
- R4 is hydrogen, halogen, —OC1-3 alkyl, substituted or unsubstituted C1-3 alkyl, CN, C(O)R7, NR8R9 or hydroxyl;
- R5 is hydrogen, halogen, —OC1-3 alkyl, substituted or unsubstituted C1-3 alkyl, CN, C(O)R7, NR8R9 or hydroxyl;
- R6 is hydrogen, halogen, —OC1-3 alkyl, substituted or unsubstituted C1-3 alkyl, CN, C(O)R7, NR8R9 or hydroxyl;
- R7 is hydrogen, OR10 or substituted or unsubstituted C1-3 alkyl;
- R8 is hydrogen or substituted or unsubstituted C1-3 alkyl;
- R9 is hydrogen or substituted or unsubstituted C1-3 alkyl;
- R10 is hydrogen or substituted or unsubstituted C1-3 alkyl;
- L1 is O, S, NH or CH2;
- L2 is O, S, NH, a direct bond or CH2;
- a is 0 or 1;
- b is 0, 1, 2 or 3;
- c is 0, 1, 2 or 3;
- d is 0, 1, 2 or 3;
- with the provisos
- when a is 1 then
- represents
- or
- or
- or
- or
- or
- and
- when a is 0 then R1 is O, S, NH, or CH2.
29 more elements
Dependencies are inferred from the claim text.