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    • 2. 发明授权
    • Cinnamic acid derivatives
    • 肉桂酸衍生物
    • US06329362B1
    • 2001-12-11
    • US09270408
    • 1999-03-16
    • Sarah Catherine ArchibaldJohn Clifford HeadGraham John WarrellowJohn Robert Porter
    • Sarah Catherine ArchibaldJohn Clifford HeadGraham John WarrellowJohn Robert Porter
    • A61K3103
    • C07D213/82A61K38/00C07C233/81C07K5/06139C07K5/06191Y10S514/826Y10S514/858Y10S514/863Y10S514/866Y10S514/885Y10S514/886Y10S514/887
    • Compounds of formula (1) are described: wherein L1 is a covalent bond or a linker atom or group; R is a carboxylic acid (—CO2H) or a derivative threof; R6 and R7 which may be the same or different is each an atom or group —L2(Alk2)tL3R12 in which L2, L3, Alk2 and t are as previously defined and R12 is a hydrogen or halogen atom or an —OR9, —NR9R10, —NO2, —CN, —CO2R9, —CONR9R10, —COR9, —N(R9)COR10, —N(R9)CSR10, —SO2N(R9)(R10), —N(R9)SO2R9, —N(R9)CON(R10)(R11), —N(R9)CSN(R10)(R11), —N(R9)SO2N(R10)(R11), or an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group provided that R6 and R7 are not both hydrogen atoms and when R7 is a hydrogen atom then R4 and R5 is each a hydrogen or halogen atom or an alkyl, alkoxy or nitro group; and the salts, solvates, hydrates and N-oxides thereof, for use in modulating cell adhesion. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    • 描述了式(1)的化合物:其中L 1是共价键或连接原子或基团; R是羧酸(-CO 2 H)或衍生物; R 6和R 7可以相同或不同,各自为原子或 基团-L2(Alk2)tL3R12,其中L2,L3,Alk2和t如前定义,R12是氢或卤素原子或-OR9,-NR9R10,-NO2,-CN,-CO2R9,-CONR9R10,-COR9 ,-N(R9)COR10,-N(R9)CSR10,-SO2N(R9)(R10),-N(R9)SO2R9,-N(R9)CON(R10)(R11) (R 10)(R 11),-N(R 9)SO 2 N(R 10)(R 11)或任选取代的脂族,杂脂族,脂环族,杂脂族,芳族或杂芳族基团,条件是R 6和R 7不是氢原子, 氢原子然后R4和R5各自为氢或卤素原子或烷基,烷氧基或硝基; 和其盐,溶剂合物,水合物和N-氧化物,用于调节细胞粘附。化合物能够抑制α4整联蛋白与其配体的结合,并且可用于预防和治疗免疫或炎症性疾病。
    • 3. 发明授权
    • Chemical entity (endipalene) in the treatment of psoriasis
    • 化学实体(endipalene)治疗牛皮癣
    • US06291534B1
    • 2001-09-18
    • US09485700
    • 2000-05-25
    • Giorgio Endrici
    • Giorgio Endrici
    • A61K3103
    • A61K31/09
    • In the literature, a correlation between the inhibition of 5-lipoxygenase and anti-inflammatory and immunomodulatory activity sufficient to effectively treat psoriasis, is known. It seems that, in particular, the excellent results can be obtained with lonapalene (6-chloro-2,3-dimethoxynaphthalendioldiacetate). However, the clinical use of lonapalene has not been successful most likely due to the significant number of side effects. With these considerations, after various studies, we have identified a molecule which we have patented with the name of endipalene, which seems to guarantee notable therapeutic results without side effects.
    • 在文献中,已知5-脂氧合酶抑制与足以有效治疗牛皮癣的抗炎和免疫调节活性之间的相关性。 看来特别地,可以用美萘醌(6-氯-2,3-二甲氧基萘二酮二乙酸酯)得到优异的结果。 然而,由于副作用大量,洛帕那的临床应用并不成功。 有了这些考虑,经过各种研究,我们已经确定了一种我们已经获得专利的分子,其名称为endipalene,似乎可以保证明显的治疗效果而没有副作用。