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US 8,299,103 B2Granted
Compounds which selectively modulate the CB2 receptor
AssigneeBoehringer Ingelheim International GmbH
InventorsAlessandra Bartolozzi, Eugene Richard Hickey, Doris Riether
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Claims15
A compound of the formula (I)
- wherein:
- ring A is a 5-membered heteroaryl ring;
- R1 is hydrogen, C1-10 alkyl or C3-10 cycloalkyl which is optionally substituted with 1-3 C1-10 alkyl, each R1 or it's substituent is optionally halogenated;
- R2 is methyl substituted with 1 heterocyclyl, each substituent on R2 where possible is optionally halogenated or substituted with 1 to 3 C1-6 alkyl, C1-6 acyl, C1-6 alkyl sulfonyl, cyano, aryl, oxo or hydroxyl;
- R3 and R3′ are independently hydrogen or C1-6 alkyl optionally halogenated with the proviso that R3 and R3′ cannot simultaneously be hydrogen;
- R4 is hydrogen or methyl;
- R5 is chosen from
- m is 0, 1, 2 or 3;
- R6 is hydrogen, C1-4 alkyl or C1-4 alkoxy;
- R7 and R8 are each independently hydrogen, or C1-4 alkyl with the proviso that both R7 and R8 cannot be hydrogen;
- and wherein R7 and R8 optionally can cyclize to form a C3-7 cycloalkyl ring;
- R9 is C1-6 alkyl or aryl;
- ring B is a 5-6 membered heterocyclic ring;
- n is 0, 1 or 2;
- wherein any carbon atom on the formula (I) or any R substituent listed above is optionally partially or fully halogenated where possible;
- or a pharmaceutically acceptable salt thereof.
13 more elements
A compound of the formula (II)
- wherein
- of the formula (II) is chosen from column A1-A8 in the table, and
- of the formula (II) is chosen from column B1-B19 in the table,
- A1
- B1
- A2
- B2
- A3
- B3
- A4
- B4
- A5
- B5
- A6
- B6
- A7
- B7
- A8
- B8
- B9
- B10
- B11
- B12
- B13
- B14
- B15
- B16
- B17
- B18
- B19
- or a pharmaceutically acceptable salt thereof.
28 more elements
A compound chosen from
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.