Indole derivatives

Details Indole derivatives Indole derivatives

2008-02-15

2010-02-02

Bernhardt, Emily (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S254030, C540S575000, C544S367000

Reexamination Certificate

active

07655645

ABSTRACT:
The invention relates to indole derivative having the general Formula Iwherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2and X3are independently selected from N, O, S and CH; Y represents CH2, O, S or SO2; R1is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN or halogen; R2, R2′, R3, R3′, R4, R4′, R5and R5′ are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO—OR8; or one pair of geminal substituents R3and R3′ or R5and R5′ together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2and R5together represent a methylene or an ethylene bridge, and R2′, R3, R3′, R4, R4′ and R5′ are hydrogen; n is 1 or 2; R6is H, (C1-4)alkyl (optionally substituted with OH, (C1-4)alkyloxy, CO—NR9R10, CO—OR11or 1,2,4-oxadiazol-3-yl), SO2NR12R13or COOR14; R7is H or halogen; R8is (C1-4)alkyl; R9and R10are independently hydrogen, (C1-4)alkyl or (C3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11is H or (C1-4)alkyl; R12and R13are independently H or (C1-4)alkyl; R14is (C1-6)alkyl; or a pharmaceutically acceptable salt thereof, as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.

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PCT International Search Report dated Apr. 23, 2008 and Written Opinion dated Apr. 23, 2008 for corresponding PCT Application No. PCT/EP2008/052141.

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