Method for increasing Hydration of the mucosa and the Evacuation of the mucosa by Treatment with bloquadores of sodium channels and osmolytes

摘要

Methods and components for treating diseases by increasing the purification and moisture of puppets, using an effective number of currently defined sodium channel blockers, and osmoolito for a person who needs more puppet purification and moisture. Claim 14: a compound comprising (a) a sodium channel blocker represented by formula (1), wherein X is h, halogen, methyl trifluoride, low tar, unsubstituted or substituted phenyl, low tar uncle, phenyl low tar uncle, low tar sulfur, or phenyl low tar sulfur, and h, Hydroxy, commodity,M-r8, - (CH2O (nnnnnnn8, - (CH2O) m-r8 (CH2) n-zg-r7, -(CH2) m-nr10-ch2 (chr8) (chr8) n-ch2or8, - (CH2) n-co2r7, or according to formula (2);R3 and R4 belong to group H independently and are represented by formula (3),lower alkyl, hydroxy lower alkyl, phenyl, lower phenylalkyl, (halophenyl)-lower alkyl, (lower alkylphenylalkyl), (alkoxyphenyl) lower-lower alkyl, naphthyl-lower alkyl, or pyridyl-lower alkyl, with the proviso that by at least one of R3 and R4 is a group represented by formula (3) in which each RL is, independently -R7, - (CH2) n-OR8, -O- (CH2) m-OR8, - (CH2) n-NR7R10, -O- (CH2) m-NR7R10, (CH2) n (CHOR8) (CHOR8) n-CH2OR8, -O- (CH2) m (CHOR8) (CHOR8) n-CH2OR8, - (CH2CH2O) m -R8, -O- (CH2CH2O) m-R8, - (CH2CH2O) m- CH2CH2NR7R10, -O- (CH2CH2O) m-CH2CH2NR7R10, - (CH2) nC (= O) NR7R10, -O- (CH2) mC ( = O) NR7R10, - (CH2) n- (Z) g-R7, -O- (CH2) m- (Z) g-R7,- (CH2) n-NR10-CH2 (CHOR8) (CHOR8) n-CH2OR8, -O- (CH2) m-NR10-CH2 (CHOR8) (CHOR8) n-CH2OR8, - (CH2) n-CO2R7, -O - (CH2) m-CO2R7, -OSO3H, -O-glucuronide, -O-glucose, formulas (4) or (2),Each or every is an integer from 0 to 10, and each P is an integer from 0 to 10, provided that the sum of O and P in each adjacent chain is from 1 to 10; each x is independent, O, N10, C (= O),CHOH C (3DN-R10)CHNR7R10, or represents a simple link; each R5 is, independently, - (CH2) m-OR8, -O- (CH2) m-OR8, - (CH2) n-NR7R10, -O- (CH2) m-NR7R10, (CH2) n (CHOR8) ( CHOR8) n-CH2OR8, -O- (CH2) m (CHOR8) (CHOR8) n- CH2OR8, - (CH2CH2O) m-R8, -O- (CH2CH2O) m-R8, - (CH2CH2O) m-CH2CH2NR7R10, - O- (CH2CH2O) m-CH2CH2NR7R10, - (CH2) nC (= O) NR7R10, -O- (CH2) mC (= O) NR7R10, - (CH2) n- (Z) g-R7, -O- ( CH2) m- (Z) g-R7, - (CH2) n-NR10-CH2 (CHOR8) (CHOR8) n-CH2OR8, -O- (CH2) m-NR10-CH2 (CHOR8) (CHOR8) n- CH2OR8 , - (CH2) n-CO2R7, -O- (CH2) m-CO2R7, -OSO3H, -O-glucuronide, -O-glucose, formulas (4),(2) o (5)each R6 is independently -R7, -OR11, -N (R7) 2, - (CH2) m-OR8, -O- (CH2) m-OR8, - (CH2) n-NR7R10, -O- (CH2) m-NR7R10, (CH2) n (CHOR8) (CHOR8) n-CH2OR8, -O- (CH2) m (CHOR8) (CHOR8) n-CH2OR8, - (CH2CH2O) m-R8, -O- (CH2CH2O) m -R8, - (CH2CH2O) m-CH2CH2NR7R10, -O- (CH2CH2O) m-CH2CH2NR7R10, - (CH2) nC (= O) NR7R10, -O- (CH2) mC (= O) NR7R10, - (CH2) n - (Z) g-R7, -O- (CH2) m- (Z) g-R7, - (CH2) n-NR10-CH2 (CHOR8) (CHOR8) n-CH2OR8, -O- (CH2) m- NR10-CH2 (CHOR8) (CHOR8) n-CH2OR8, - (CH2) n-CO2R7, -O- (CH2) m-CO2R7, -OSO3H, -O-glucuronide, -O-glucose, formulas (4) or ( two),In this case, if two r6s are - or11 and are distributed adjacent to each other in a phenyl ring, the tar parts of the two r6s can be connected to form a methylenedioxy group, then each R7 is an independent h or low tar; each R8 is an independent h, low tar, (= O) - R11, Gluc, 2. Tetrahydropyridine, or formula (5);each R9 is, independently -CO2R7, -CON (R7) 2, -SO2CH3, or -C (= O) R7; each R10 is independently H, -SO2CH3, -CO2R7, -C (= O) NR7R9, -C (= O) R7, or -CH2- (CHOH) n-CH2OH; each Z is, independently, CHOH, C (= O),Nr7r10, C = nr10, or nr10; each R11 is a lower tar; each R11 is an integer from 1 to 6; each m is an integer from 1 to 7; each n is an integer from 0 to 7; each q is a separate c-r5, c-r6, or N atom, Up to three Q atoms in the ring are N atoms, and at least one q is c-r5; or pharmaceutically acceptable salts thereof, including all counterparts, tropospheric and racemic mixtures; and (b) a permeable active compound. Requirement 17: constituted in accordance with requirement 14,Formula (1) represents the same sodium channel blocker as formula group (6).