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US 8,012,992 B2Granted
Aza-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
AssigneeAllergan, Inc.
InventorHaiqing Yuan
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Abstract
The present invention provides compounds are disclosed herein having the formula: Wherein n is 1 or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl; R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, —O—(C1-6 alkyl), —NH—(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O—(C1-6 alkyl), aryl, heteroaryl, —C(═O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X═O, NH, —C(═O)— or —N═CH—; and Each L is independently alkylene and carbonyl. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
Claims9
A compound having the formula:
- wherein n is 1 and indicates the number of enchained nitrogen atoms in the condensed 6 member ring;
- m is 0 or 1;
- R1 is aryl, heteroaryl or alkyl;
- R2 is selected from the group consisting of isopropyl, cyclobutyl and cyclopentyl;
- R3 is selected from the group consisting of aryl, heteroaryl, or alkyl;
- R4 is H, OH, —O—(C1-6 alkyl), —NH—(C1-6 alkyl), and oxide;
- R5 is selected from the group consisting of H, halogen, C1-6 alkyl, O—(C1-6 alkyl), aryl, heteroaryl, —C(═O)(C1-6 alkyl), substituted and un-substituted oxazolin-2-yl;
- X is selected from the group consisting of O, NH, —C(═O)— and —N═CH—;
- and
- L is selected from the group consisting of alkylene, and carbonyl.
7 more elements
Dependencies are inferred from the claim text.