首页> 外国专利> Compound or a salt thereof, peptide or a balance, derived from benzene or a domestic salt, method to inhibit ap-1, agent to prevent and treat a disease in which ap-1 overexpression and an autoimmune disease participate, and, ap-1 inhibitor

Compound or a salt thereof, peptide or a balance, derived from benzene or a domestic salt, method to inhibit ap-1, agent to prevent and treat a disease in which ap-1 overexpression and an autoimmune disease participate, and, ap-1 inhibitor

机译:源自苯或家庭盐的化合物或其盐,肽或天平,抑制ap-1的方法,预防和治疗ap-1过表达和自身免疫性疾病参与的疾病的试剂和ap-1抑制剂

摘要

"COMPOUND OR A SALT OF THE SAME, PEPTIDE OR A SAME BALANCE, DERIVED FROM BENZENE OR A DOMESTIC SALT, METHOD FOR INHIBITING AP-1, AGENT TO PARRUPT AND TREAT A DISEASE IN WHICH PARTICIPATES IN AN OVEREXPRESSION OF AP-1 AND A DISEASE, EUTOAUTOAUTO , AP-1 INHIBITOR. A compound Comprising the atom that corresponds to N ~ 3 ~ and two or more atoms selected from N ~ 1 ~, N ~ 2 ~, N ~ 4 ~ and N ~ 5 ~, ditostomes constitute the pharmacophore represented by the following formula: where N ^ 1 ^ represents an atom to which a donating hydrogen atom in a hydrogen bonding donor group is attached or an atom that accepts hydrogen bonding in a group that accepts hydrogen bonding; N ~ 3 ~ represents an atom that accepts hydrogen bonding in a group that accepts hydrogen bonding; and N ~ 2 ~, N ~ 4 ~ and N ~ 5 ~ independently represent an arbitrary carbon atom that constitutes a hydrophobic group; and defined by the interatomic distances between N ~ 1 ~, N ~ 2 ~, N ~ 3 ~, N ~ 4 ~ and N ~ 5 ~; and in the optimized three-dimensional structure, the distances between the atom correspond to N ~ 3 ~ and the atoms that correspond to the two or more atoms selected from N ~ 1 ~, N ~ 2 ~, N ~ 4 ~ and N ~ 5 ~ in their spherical structure optimized, are the interatomic distances without a pharmacophore; or a salt thereof; inhibits the activity of the AP-1 transcription factor and is usable as an agent to prevent and treat diseases in which AP-1e overexpression is involved and as an AP1 inhibitor.
机译:“由苯或本国盐衍生的相同,肽或相同平衡的化合物或盐,用于抑制AP-1的方法,该方法可诱使和治疗参与AP-1过表达和疾病的疾病,EUTOAUTOAUTO,AP-1抑制剂。一种化合物,它包含对应于N〜3〜的原子和两个或多个选自N〜1〜,N〜2〜,N〜4〜和N〜5〜的原子,下式表示的药效基团:其中,N ^ 1 ^表示与氢键结合的供体基团中的氢原子键合的原子或在与氢键结合的基团中的氢键原子; N〜3〜表示氢键基团中的氢键原子; N〜2〜,N〜4〜和N〜5〜独立地表示构成疏水基的任意碳原子;由N〜1之间的原子间距离定义〜,N〜2〜,N〜3〜,N〜4〜和N〜5〜;并在op中有限的三维结构,原子之间的距离对应于N〜3〜和对应于两个或多个选自N〜1〜,N〜2〜,N〜4〜和N〜5〜in的原子的原子优化的球形结构是无药效团的原子间距离。或其盐;抑制AP-1转录因子的活性,可用作预防和治疗涉及AP-1e过表达的疾病的试剂和AP1抑制剂。

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