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US 8,541,397 B2Granted
Alkyne and alkene derivatives as sphingosine 1-phosphate-1 receptor modulators
AssigneeAllergan, Inc.
InventorsSantosh C. Sinha, Smita Bhat, Evelyn Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
Life of this patent
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Abstract
The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Claims8
A compound having Formula I, its enantiomers, diastereoisomers, or a pharmaceutically acceptable salt thereof,
- wherein:
- represents a double bond “—CR14═CR15—”;
- A is C6-10 aryl, heterocycle, C3-8 cycloakyl or C3-8 cycloalkenyl;
- B is C6-10 aryl, heterocycle, C3-8 cycloakyl or C3-8 cycloalkenyl;
- R1 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R2 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R3 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R4 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R5 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R6 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R7 is H, halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R11, C6-10 aryl, heterocycle, C3-8 cycloakyl, C3-8 cycloalkenyl, NR12R13 or hydroxyl;
- R8 is the same or independently halogen, —OC1-8 alkyl, C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- L1 is O, S, NH or CH2;
- R9 is H or C1-6 alkyl;
- L2 is CHR14 or O;
- R10 is H, OPO3H2, carboxylic acid, hydroxyl, PO3H2, —S(O)2H, —P(O)MeOH or —P(O)(H)OH;
- R11 is H or C1-8 alkyl;
- a is 0, 1, 2 or 3;
- b is 0 or 1;
- R12 is H or C1-8 alkyl;
- R13 is H or C1-8 alkyl;
- R14 is H, hydroxyl or C1-8 alkyl;
- R15 is H or C1-8 alkyl;
- R16 is O, S, C(O) or CH2;
- and
- c is 0 or 1;
- with the proviso that the compound of Formula I is not of structure
24 more elements
Dependencies are inferred from the claim text.