| abstract |
600006 ORL-1 receptor antagonists of formula I, their uses, and methods for their preparation are described. ORL-1 antagonists are deemed to be useful; in the treatment of depression and/or the treatment of excess body fat, obesity, and/or weight maintenance post treatment for being overweight or obese, or in the treatment of migraine. Certain compounds have also demonstrated through animal models that the compounds of the present disclosure are useful for the treatment of migraine. Particularly the following compounds are disclosed: [2-[4-[(2-chloro-4,4-difluoro-spiro[5H-thieno[2,3-c]pyran-7,4’-piperidine]-1’-yl)methyl]-3-methyl-pyrazol-1-yl]-3-pyridyl]methanol; 2-chloro-4,4-difluoro-1’-[[3-methyl-1-[3-(pyrazol-1-ylmethyl)-2-pyridyl]pyrazol-4-yl]methyl]spiro[5H-thieno[2,3-c]pyran-7,4’-piperidine]; [4-[(2-chloro-4,4-difluoro-spiro[5H-thieno[2,3-c ]pyran-7,4’-piperidine]-1’-yl)methyl]-1-(3-fluoro-2-pyridyl)pyrazol-3-yl]methanol and [2-[4-[(2-Chloro-4,4-difluoro-spiro[5H -thieno[2,3-c ]pyran-7,4’-piperidine]-1’-yl)methyl]-3-methyl-pyrazol-1-yl]-3-pyridyl]methanol. |