Heterocyclic amide derivatives as p2x7 receptor antagonists
US-2015361097-A1 · Dec 17, 2015 · US
US8969552B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-8969552-B2 |
| Application number | US-66542805-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 14, 2005 |
| Priority date | Oct 14, 2004 |
| Publication date | Mar 3, 2015 |
| Grant date | Mar 3, 2015 |
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The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R a and wherein Ar may also carry 1 or 2 radicals R b ; X is N or CH; Y is O, S, —CH═N—, —CH═CH— or —N═CH—; A is CH 2 , O or S; E is CR 6 R 7 or NR 3 ; R 1 is C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, formyl or C 1 -C 3 -alkylcarbonyl; R 1a is H, C 2 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, or R 1a and R 2 together are (CH 2 ) n with n being 2 or 3, or R 1a and R 2a together are (CH 2 ) n with n being 2 or 3; R 2 and R 2a are independently of each other H, CH 3 , CH 2 F, CHF 2 or CF 3 ; R 3 is H or C 1 -C 4 -alkyl; R 6 , R 7 independently of each other are selected from H, C 1 -C 2 -alkyl and fluorinated C 1 -C 2 -alkyl; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
Opening claim text (preview).
We claim: 1. An aromatic compound of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar is substituted with 1 radical R a , wherein R a is selected from the group consisting of C 2 -C 6 alkyl, fluorinated C 2 -C 6 alkyl, fluorinated C 3 -C 6 cycloalkyl, fluoromethyl, difluoromethyl, fluoromethoxy, difluorome…
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