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Antagonistic activity and promotive compounds of B-2 adrenergic receptor
Antagonistic activity and promotive compounds of B-2 adrenergic receptor
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机译:B-2肾上腺素受体的拮抗活性和促发化合物
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摘要
Compounds that act as the opposite of muscle receptors, as enhancers for adrenaline B2 receptors, formulation processes, compounds containing these components, therapeutic uses, and combinations with other pharmaceutical active ingredients. 1. Characteristic requirement 1: a compound whose q is a set of formula (2) because it is a general formula (1);Choose (3) or (4) from a combination of two different equations, 2 and 1,where A¹ and A² are independently absent or selected from C₁₋₁₂alkylene, C₃₋₈cycloalkylene and C₃₋₈heterocycloalkylene optionally substituted with one or more substituents selected from C₁₋₆alkyl, aryl-C₁₋₆alkyl and heteroaryl-C₁₋₆alkyl; B is absent or selected from C₃₋₈cycloalkylene, C₃₋₈heterocycloalkylene, arylene or heteroarylene optionally substituted with one or more groups selected from -OH, halogens, -CN, C₁₋₆alkyl, C₁₋₆alkoxy, C₁₋₆haloalkyl, C₁₋ ₆haloalkoxy and aryl-C₁₋₆alkyl; C is absent or is selected from -O-,-C (O) --OC (o)..- (O) CO-- yes.-S (O) --S (O) - y -N (R) -Or one of the c1-c23 remains of formula group (5),where R⁷ is independently H in each case or is selected from linear or branched C₁₋₈alkyl, aryl-C₁₋₆alkyl, arylsulfanyl, arylsulfinyl, arylsulfonyl, C₃₋₈cycloalkyl, C₃₋₈heterocycloalkyl, aryl, and heteroaryl; D is absent or is selected from C₁₋₁₂alkylene, C₂₋₁₂alkenylene, C₂₋₆alkylene, arylene, heteroarylene, C₃₋₈cycloalkylene, C₃₋₈heterocycloalkylene; wherein said arylene, heteroarylene, C₃₋₈cycloalkylene and C₃₋₈heterocycloalkylene is optionally substituted with one or more groups selected from -OH, halogen, -CN, C₁₋₆alkyl, C₁₋₆alkoxy,C₁₋₆haloalkyl, C₁₋₆haloalkoxy and aryl-C₁₋₆alkyl; n is in each case independently 0 or an integer between 1 and 3; m is in each case independently an integer between 1 and 3; E is absent or is selected from -O-,- No. 8311st --No. 8311-c (o);-C (o) - No. 8311a;-OC (o)..-C (O) - (CH) -O--NR -C (O) - (CH) -O--8311-c (o) - 8311-y-s -;G is arileno or heterosexual, optionally replaced by one or more alternatives selected from the halogen atoms.-SH, -NO₂,-CN -CON (R)-NH832222,-NHCOR⁶,-CO₂R⁶,C₁₋₁₀alkylsulfanyl, C₁₋₁₀alkylsulfinyl, C₁₋₁₀alkylsulfonyl, C₁₋₁₀alkyl, aryl, haloaryl, heteroaryl and C₁₋₁₀alkoxy; R¹ is selected from C₃₋₈cycloalkyl, C₃₋₈heterocycloalkyl, aryl, heteroaryl, aryl-C₁₋₆alkyl, heteroaryl-C₁₋₆alkyl and C₃₋₈cycloalkyl-C₁₋₆alkyl, optionally substituted with one or more groups independently selected from halogen, C₁₋₈alkyl, and C₁₋₁₀alkoxy; s is 0 or an integer between 1 and 3;R² is a nitrogen-containing group that can be selected from: a group (a) that is -NR³R⁴ where R³ and R⁴ are independently hydrogen or C₁₋₄alkyl; and a group (b) residues of formula J1-J5 selected from the group of formulas (6);R83099 is a formula group (7);P is an integer of 0 or 1 to 4; q is an integer of 0 or 1 to 4; P is absent or selected from the division group consisting of O, s, so, so, so;CO NR CH 3DCH N (R) SON (R) COO N (R) C (O)SO N (R)OC (o) n (r8310) and C (o) n (r8310);W is selected from H, C₁₋₆alkyl, C₃₋₈cycloalkyl, aryl and heteroaryl, optionally substituted with one or more substituents independently selected from halogen atoms, -OH, oxo (= O),-SH, -NO₂,-CN -CON (R)-NH832222,-NHCOR⁶,-CO₂R⁶,C₁₋₁₀alkylsulfanyl, C₁₋₁₀alkylsulfinyl, C₁₋₁₀alkylsulfonyl, C₁₋₁₀alkyl and C₁₋₁₀alkoxy; R⁶ is in each case independently H or is selected from C₁₋₁₀alkyl, C₁₋₆haloalkyl, C₂₋₆alquinyl, C₂₋₆alkenyl, C₃₋₈cycloalkyl, heteroaryl and aryl optionally substituted with one or more substituents selected from halogen atoms, - OH, oxo (= O),-SH, -NO₂,-CN, -CONH₂,-COOH, C₁₋₁₀alkoxycarbonyl, C₁₋₁₀alkylsulfanyl, C₁₋₁₀alkylsulfinyl, C₁₋₁₀alkylsulfonyl, C₁₋₁₀alkyl and C₁₋₁₀alkoxy; and pharmaceutically acceptable salts or solvates thereof.
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