发明名称 Treatment of allergic conditions using indanyloxy-alkanol derivatives
摘要 p-Allyl or cycloalkyl phenoxy alkanols and esters are provided having the structure: <IMAGE> in which: R1 is an alkyl group having from one to six carbon atoms, preferably tertiary, and still more preferably tertiary-butyl; or a bivalent cycloalkylene group condensed with the phenyl group at adjacent ring carbons thereof, such as in indane; R2 is lower alkyl having from one to three carbon atoms or hydrogen; R3 is hydroxyl or an ester group selected from the group consisting of COOR4 and OOCR4 derived from unsubstituted and hydroxy-substituted monocarboxylic acids and COOR5OOC and OOCR5COO derived from unsubstituted and hydroxy-substituted dicarboxylic acids, the acids being selected from the group consisting of aliphatic acids, including carbamic acid, having from one to about twelve carbon atoms, cycloaliphatic acids having from three to about twelve carbon atoms; carbocyclic aromatic acids having from six to about twenty carbon atoms; and nitrogen heterocyclic aromatic acids having from five to about twelve carbon atoms, R4 being monovalent aliphatic, cycloaliphatic, aromatic, or nitrogen heterocyclic aromatic, and R5 being divalent aliphatic, cycloaliphatic, aromatic, or nitrogen heterocyclic aromatic, the acids being esterified with aliphatic alcohols having from one to six carbon atoms; and carbonic acid monoalkyl esters, the alkyl having from one to three carbon atoms; and n1, n2 and n3 represent the number of CH2, C(R2)2 and CH2 groups, respectively, and are numbers within the range from 0 to 10; and at least one of n1, n2 and n3 is other than zero. These compounds inhibit abnormal tissue reactivity due to specific allergic hypersensitivity or due to specific irritants by inhibiting the release of chemical mediators that are responsible for the symptoms of allergic diseases, including allergic rhinitis, asthma, hypersensitivity of the skin and of the gastrointestinal canal, and the many symptoms of irrigation and inflammation produced by irritants and inflammation-causing substances, and prevent rejection of transplanted cells and organs and particularly of bone marrow and insulin-producing Langerhans cell.
申请公布号 US4816491(A) 申请公布日期 1989.03.28
申请号 US19870047379 申请日期 1987.05.07
申请人 BERGER, FRANK M. 发明人 BERGER, FRANK M.;DEGRAW, JOSEPH I.;JOHNSON, HOWARD L.
分类号 C07C43/205;C07C43/215;C07C43/23;C07C51/367;C07D213/80;(IPC1-7):C07C43/23;A61K31/045;A61K31/085 主分类号 C07C43/205
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