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N-sulfamoyl-n-benzopiranpiperidinas as carbonic anhydrase inhibitors.

机译:N-氨磺酰基-n-苯并吡喃哌啶子酸酯为碳酸酐酶抑制剂。

摘要

A compound of Formula I ** (See formula) ** in which: R1 and R2 are independently selected from the group consisting of: hydrogen, C1 to C4 alkyl, C4 to C7 cycloalkyl; or R1 and R2 together form a 5- or 6-membered ring which may optionally contain 1 to 2 heteroatoms independently selected from the group consisting of nitrogen and / or oxygen and which also may be substituted by optionally substituted aryl, heteroaryl or arylenehalogenalkyl optionally substituted; R3 to R6 are independently selected from the group consisting of: hydrogen; halogen; C1 to C4 alkyl; C2 to C4 alkenyl, optionally substituted with aryl; C1 to C4 alkoxy; C1 to C4 alkoxy substituted with halogen provided that the alpha-carbon atom is substituted by other halogen than fluorine if any; C2 to C4; NSO2alquilo C1 to C4; NH2; NO2; C1 to C4 aminoalkyl; C2 to C8 aminodialkyl; cyano; I oxyaryl; I oxyalkylenearyl; I oxiarilenoalquilo; oxialquilenoarilenoalcoxi; C2 to C8 ester; C1 to C8 amido; oxialquilenocarbonilalquilo C2 to C8; oxialquilenoxialquilo C2 to C8; amidoxialquilo C1 to C4; aryl, optionally substituted; heteroaryl, optionally substituted; condensed aryl, optionally substituted; heteroaryl fused, optionally substituted; or R3 and R6 have the same meaning as above and wherein R4 and R5 together form a 5- or 6-membered ring which may optionally contain 1 to 3 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur and you may optionally bear 1 or 2 double bonds and may also contain a carbonyl group and which also may be substituted by C1 to C4 haloalkyl C1 to C4, optionally substituted aryl and / or heteroaryl optionally substituted; or R5 and R6 have the same meaning as above and wherein R3 and R4 together form a 5- or 6-membered ring which may optionally contain 1 to 3 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur and you may optionally bear 1 or 2 double bonds and may also contain a carbonyl group and which also may be substituted by C1 to C4 haloalkyl C1 to C4, optionally substituted aryl and / or heteroaryl optionally substituted; or R3 and R4 have the same meaning as above and wherein R5 and R6 together form a 5- or 6-membered ring which may optionally contain 1 to 3 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur and you may optionally bear 1 or 2 double bonds and may also contain a carbonyl group and which also may be substituted by C1 to C4 haloalkyl C1 to C4, optionally substituted aryl and / or heteroaryl optionally substituted; YX is selected from the group consisting of: HC = CH, CH2-CH2, O = C-CH2, and (HO) (H) C-CH2; and its acid addition salt of physiologically acceptable.
机译:式I **(参见式)**的化合物,其中:R 1和R 2独立地选自:氢,C 1 -C 4烷基,C 4 -C 7环烷基;或R 1和R 2一起形成5或6元环,其可任选地含有1-2个独立地选自氮和/或氧的杂原子,并且还可以被任选地取代的芳基,杂芳基或亚芳基卤代烷基取代; R3至R6独立地选自:氢;卤素; C1至C4烷基; C2-C4烯基,任选地被芳基取代; C1至C4烷氧基; C1-C4被卤素取代的烷氧基,条件是α-碳原子被氟以外的卤素取代。 C2至C4; NSO2alquilo C1至C4; NH2; NO2; C1至C4氨基烷基; C2至C8氨基二烷基;氰基; I氧芳基; I氧亚烷基芳基; I oxiarilenoalquilo; oxialquilenoarilenoalcoxi; C2至C8酯; C1至C8酰胺基; oxialquilenocarbonilalquilo C2至C8; oxialquilenoxialquilo C2至C8; mid虫基C1至C4;芳基,任选地被取代;杂芳基,任选地被取代;任选取代的稠合芳基;杂芳基稠合,任选取代;或R 3和R 6具有与上文相同的含义,其中R 4和R 5一起形成5元或6元环,该环可以任选地包含1-3个独立地选自氮,氧和硫的杂原子,并且您可以任选地带有1或2个双键,并且还可以包含羰基,并且还可以被C1至C4的卤代烷基C1至C4,任选取代的芳基和/或任选取代的杂芳基取代;或R 5和R 6具有与上文相同的含义,其中R 3和R 4一起形成5或6元环,其可任选地包含1-3个独立地选自氮,氧和硫的杂原子,并且您可以任选地带有1或2个双键,并且还可以包含羰基,并且还可以被C1至C4的卤代烷基C1至C4,任选取代的芳基和/或任选取代的杂芳基取代;或R 3和R 4具有与上文相同的含义,其中R 5和R 6一起形成5元或6元环,该环可以任选地含有1-3个独立地选自氮,氧和硫的杂原子,并且你可以任选地带有1或2个双键,并且还可以包含羰基,并且还可以被C1至C4的卤代烷基C1至C4,任选取代的芳基和/或任选取代的杂芳基取代; YX选自:HC = CH,CH 2 -CH 2,O = C-CH 2和(HO)(H)C-CH 2;及其酸式加成盐生理上可接受。

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