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US 2014/0228344 A1Published application
Alkene azetidine derivatives as sphingosine 1-phosphate (s1p) receptor modulators
AssigneeAllergan, Inc.
InventorsWenkui K. Fang, Ken Chow, Evelyn G. Corpuz
Life of this patent
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Abstract
The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Claims13
A compound represented by Formula I, or an E geometric isomer, or a Z geometric isomer, or a mixture of an E and a Z geometric isomers, or an enantiomer, or a diastereoisomer, or a tautomer, or a zwitterion, or a pharmaceutically acceptable salt thereof:
- wherein:
- A is optionally substituted C6-10 aryl, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl or optionally substituted C3-8 cycloalkenyl;
- B is optionally substituted C6-10 aryl, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl or optionally substituted C3-8 cycloalkenyl;
- R1 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R2 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R3 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R4 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C (O)R11, NR12R13 or hydroxyl;
- R5 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R6 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, NR12R13 or hydroxyl;
- R7 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, optionally substituted C6-10 aryl, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C3-8 cycloalkenyl, NR12R13 or hydroxyl;
- R8 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, optionally substituted C6-10 aryl, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C3-8 cycloalkenyl, NR12R13 or hydroxyl;
- R9 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, optionally substituted C6-10 aryl, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C3-8 cycloalkenyl, NR12R13 or hydroxyl;
- R10 is H, halogen, —OC1-8 alkyl, optionally substituted C1-8 alkyl, CN, C(O)R11, optionally substituted C6-10 aryl, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C3-8 cycloalkenyl, NR12R13 or hydroxyl;
- L1 is O, S, S(O), NH or CH2;
- L2 is O, S or CHR12,
- R11 is OH or optionally substituted C1-8 alkyl;
- a is 1, 2, 3, 4, 5 or 6;
- R12 is H or optionally substituted C1-8 alkyl;
- and
- R13 is H or optionally substituted C1-8 alkyl.
17 more elements
Dependencies are inferred from the claim text.