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US 7,601,874 B2Granted
Indene derivatives as pharmaceutical agents
AssigneeAquinox Pharmaceuticals Inc.
InventorsJeffery R Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
Life of this patent
Estimating the term…
Abstract
Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
Claims3
A compound of formula (Ia):
- wherein:
- the A, C or D ring is independently fully saturated;
- C1, C4, C11, C12, C15 and C16 are each independently substituted with two hydrogens;
- C9 and C14 are each independently substituted with hydrogen;
- R1 is —OR7;
- R2 is —R8—OR7;
- R3 is —R10—N(R7)2;
- R4a and R4b together form alkylidene or haloalkylidene;
- R5 is alkyl;
- R6 is hydrogen, —R8—OR7 or —R8—N(R7)2;
- each R7 is independently selected from the group consisting of hydrogen, —R10—OR9, —R10—N(R9)2, alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl and optionally substituted heteroarylalkyl;
- each R8 is independently selected from the group consisting of a direct bond, a straight or branched alkylene chain, and a straight or branched alkenylene chain;
- each R9 is independently selected from the group consisting of hydrogen, alkyl, aryl and aralkyl;
- and
- each R10 is independently selected from the group consisting of a straight or branched alkylene and a straight or branched alkenylene chain,
- as a single stereoisomer, a mixture of stereoisomers, or as a racemic mixture of stereoisomers;
- or a pharmaceutically acceptable salt.
14 more elements
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula (Ia):
- wherein:
- the A, C or D ring is independently fully saturated;
- C1, C4, C11, C12, C15 and C16 are each independently substituted with two hydrogens;
- C9 and C14 are each independently substituted with hydrogen;
- R1 is —OR7;
- R2 is —R8—OR7;
- R3 is —R10—N(R7)2;
- R4a and R4b together form alkylidene or haloalkylidene;
- R5 is alkyl;
- R6 is hydrogen, —R8—OR7 or —R8—N(R7)2;
- each R7 is independently selected from the group consisting of hydrogen, —R10—OR9, —R10—N(R9)2, alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl and optionally substituted heteroarylalkyl;
- each R8 is independently selected from the group consisting of a direct bond, a straight or branched alkylene chain, and a straight or branched alkenylene chain;
- each R9 is independently selected from the group consisting of hydrogen, alkyl, aryl and aralkyl;
- and
- each R10 is independently selected from the group consisting of a straight or branched alkylene and a straight or branched alkenylene chain,
- as a single stereoisomer, a mixture of stereoisomers, or as a racemic mixture of stereoisomers;
- or a pharmaceutically acceptable salt.
14 more elements
Dependencies are inferred from the claim text.