New bensulfonylaminopyridin-2-yl derivatives useful for treating a condition mediated by the modulation of 11-beta-hydroxysteroid dihydrogenase e.g. diabetes or metabolic syndrome

摘要

Bensulfonylaminopyridin-2-yl derivatives, their salts and solvate are new. Bensulfonylaminopyridin-2-yl derivatives of formula R 1-SO bN(R 4)T(CR 7R 6) n-C(R 5)(R 6)W (I), their salts and solvate are new. R 11-6C alkyl, (CR 7R 8) t-3-10C cycloalkyl, (CR 7R 8) t-3-10C aryl or (CR 7R 8) t-4-10C membered heteroaryl (all optionally substituted by 1 -5 R 9 groups); b and k : 1 or 2; n and j : 0 - 2; t,u,p,q and v : 0 - 5; T : 6-10 membered heterocycle containing at least one N; W : C(O)N(R 2)(R 3), C(O)OR 2 or 5 membered heterocyclyl (optionally substituted by 1 -5 R 9 groups); R 2 - R 6H or R 1; R 2R 3N : 4-10 membered heterocyclyl; R 5C+R 6C : 3-6 membered cycloalkyl ring or 3-7 menbered heterocyclyl ring; R 7 or R 8H or 1-6C alkyl (optionally substituted by 1 -5 R 9 groups); R 9halo, CN, NO 2, CF 3, CHF 2, OCF 3, azido, OH, 1-6C alkoxy, 1-6C alkyl, 2-8C alkenyl, 2-6C alkynyl, C(O)R 10, C(O)OR 11, OC(O)R 11, N(R 11)C(O)R 12, C(O)N(R 11)(R 12), N(R 11)(R 12), N(R 11)(OR 12), S(O)-1-6C alkyl, S(O) kN(R 11)(R 12), OS(O) 2R 10, NR 11S(O) k(R 12), (CR 13R 14) v-1-6C aryl, (CR 13R 14) v-4-10 membered heterocyclyl, (CR 13R 14) qC(O)(CR 13R 14) v-6-10C aryl, (CR 13R 14) qC(O)(CR 13R 14) v-4-10 membered heterocyclyl, (CR 13R 14) v-O-(CR 13R 14) q-6-10C aryl, (CR 13R 14) v-O-(CR 13R 14) q-4-10 membered heterocyclyl, (CR 13R 14) qS(O) j- (CR 13R 14) v-8-10C aryl or (CR 13R 14) qS(O) j- (CR 13R 14) v-4-10 membered heterocyclyl (where any carbon of 1-6C alkyl, 6-10C aryl or 4-10 membered heterocyclyl is optionally substituted by halo, CN, NO 2, CF 3, CHF 2, OCF 3, azido, OR 15, C(O)R 15, C(O) OR 15, OC(O)R 15, NR 15C(O)R 16, C(O)NR 15R 16, NR 15R 16, NR 15(OR 16), 1-6C alkyl, 2-8C alkenyl, 2-6C alkynyl, (CR 17R 18) u(6-10C aryl) or(CR 17R 18) u(4-10 membered heterocyclyl); R 10 - R 181-6C alkyl, (CR 19R 20) p(6-10C aryl) (both alkyl and aryl optionally substituted by (S 1), (CR 19R 20) p-4-10 membered heterocyclyl (optionally substituted by 1 - 3 (S 1) and oxo); S 1halo, CN, NO 2, CF 3, CHF 2, OCF 3, NR 21R 22, CH 2F, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, OH or 1-6C alkoxy; and R 19 - R 22H or 1-6C alkyl. Where any of the above substituents comprising methyl, methylene, methine which is not attached to halo, SO or SO 2, or N, O or S, optionally bears on the group a substituent Oh, halo, 1-6C alkyl, 1-0C alkoxy, amino, NH(1-6C alkyl) or N(alkyl)(1-6C alkyl) ACTIVITY : Antidiabetic; Anorectic; ophthalmological; Antilipemic; Osteopathic; Antitubercular, Tuberculostatic; Antiarteriosclerotic; Nootropic; Antidepressant; Virucide; Antiinflammatory; Hepatotropic; Hypotensive. MECHANISM OF ACTION : 11-beta -Hydroxysteroid dihydrogenase inhibitor. Test details are not given. (I) Showed Ki values less than 1 to 480 nm.