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Imidazolona and pyrazolone derivatives as inhibitors of Human neutrophils Elastase (HNE)
专利权人:
CHIESI FARMACEUTICI S.P.A.
发明人:
JENNINGS, ANDREW STEPHEN ROBERT,ARMANI, ELISABETTA,CAPALDI, CARMELIDA
申请号:
ARP170101443
公开号:
AR108609A1
申请日:
2017.05.26
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
The derivatives of pidan and pyrazolum, which have the property of inhibiting the neutral elasticity of human beings, are used for treatment. 1. Requirement 1: a compound (1) with formula characteristics,or a pharmaceutically acceptable salt thereof, where X is -C or -N; Y is C or N, where X and Y are not simultaneously C or N; R¹ is selected from the group consisting of -C₁₋₆ linear or branched alkyl, -C₃₋₆ cycloalkyl, -C₃₋₆ heterocycloalkyl and aryl-C₁₋₆ alkylene-,a. In any of them, c83231;A select (2) from the formula group residues,where Q is -CH or N; R² is selected from the group consisting of -C₁₋₆ alkyl, aryl-C₁₋₆ alkylene- and heteroaryl-C₁₋₆ alkylene-;R³ is -C₁₋₆ alkylene-N⁺RᵃRᵇRᶜ or heteroaryl-C₁₋₆ alkylene; Rᵃ is -C₁₋₆ alkyl; Rᵇ is -C₁₋₆ alkyl; Rᶜ is selected from the group consisting of -C₁₋₆ alkyl, aryl-C₁₋₆ alkylene and heteroaryl-C₁₋₆ alkylene- or Rᵃ and Rᵇ can form a heterocycloalkyl with the atom N⁺,wherein said heterocycloalkyl and heteroaryl may be optionally substituted with one or more C₁₋₆ alkyl; where the nitrogen atom in the heterocycloalkyl and heteroaryl groups may be quaternized; and where the dotted lines connecting X to the carbon atom at position 4 and Y, indicate that when X is N, then the double bond is in position 4-5, and when Y is N, then the double bond is found in position 3 - 4.Derivados de imidazolona y pirazolona que tienen propiedades inhibitorias de la elastasa de neutrófilos humana, y su uso en terapia. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde X es -C o -N; Y es C o N, donde X e Y no son simultáneamente C o N; R¹ se selecciona entre el grupo que consiste en -C₁₋₆ alquilo lineal o ramificado, -C₃₋₆ cicloalquilo, -C₃₋₆ heterocicloalquilo y aril-C₁₋₆ alquileno-, donde cualquiera de dichos -C₃₋₆ cicloalquilo, -C₃₋₆ heterocicloalquilo y aril-C₁₋₆ alquileno- puede estar opcionalmente sustituido con -C₁₋₆ haloalquil-C(O)- lineal o ramificado, -C₁
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