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    • 7. 发明申请
    • COMPOUNDS AND COMPOSITIONS FOR TREATING DISEASES ASSOCIATED WITH SERINE PROTEASE, PARTICULARLY TRYPTASE, ACTIVITY
    • 用于治疗与丝氨酸蛋白酶,特异性TRYPTASE,活性相关的疾病的化合物和组合物
    • WO1998045275A1
    • 1998-10-15
    • PCT/US1997021849
    • 1997-12-01
    • AXYS PHARMACEUTICALS CORPORATIONCHURCH, Timothy, J.CUTSHALL, Neil, ScottGANGLOFF, Anthony, R.JENKINS, Thomas, E.LINSELL, Martin, S.LITVAK, JoaneRICE, Kenneth, D.SPENCER, Jeffrey, R.WANG, Vivian, R.
    • AXYS PHARMACEUTICALS CORPORATION
    • C07D235/20
    • C07D231/12C07D233/56C07D235/20C07D249/08C07D401/14C07D403/14C07D413/06C07D413/14C07D471/04C07F7/0812
    • Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. A preferred aspect of the invention are compounds of Formula (II) in which: the dashed lines independently represent optional bonds; each R independently is (C1-6)alkyl, (C1-6)alkyloxy, halo or hydroxy; each R independently is (C1-6)alkyl, (C1-6)alkyloxy, halo or hydroxy; X is -C(O)- or -CR R -, X is -CH(R )n1- or -C(R )n1=, wherein R is amino(N1-4)azolidinyl, amino(N1-4)azolyl, (N1-4)azolidinyl, (N1-4)azolyl, -NHC(NH)NR R , -C(NR )R , -C(NH)NHR , -C(NH)NR R or -(CR R )yNH2, or X is -N= or -NH(R )n1-, wherein R is -C(NR )R , -C(NH)NHR or -C(NH)NR R , wherein each R independently is hydrogen or (C1-6)alkyl and each R independently is (C1-6)alkyl; and X is -CH(R )- or -C(R )=, wherein R is -R , -OR , -N(R )R , -SR , -S(O)R , -S(O)2R , -S(O)2OR , -S(O)2N(R )R , -N(R )S(O)2R , -C(O)R , -C(O)OR , -C(O)N(R )R , -N(R )C(O)R , -OC(O)N(R )R , -N(R )C(O)OR , -(CH2)n4N(R )C(O)N(R )R , -OP(O)(OR )OR or -C(O)N(R )CH(COOH)R , or X is -N= or -N(R )-, wherein R is -C(O)R , -C(O)OR , -C(O)N(R )R , -OC(O)N(R )R or -C(O)N(R )CH(COOH)R , wherein R , R and R are as defined in the Summary of the Invention; R is hydrogen or (C1-4)alkyl, R is hydrogen or (C1-4) alkyl, which alkyl optionally is substituted with one to two substituents independently selected from (C1-4)alkyloxy, hydroxy and sulfo, R is hydrogen or methyl and R is hydrogen, methyl or hydroxy. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.
    • 描述了有效预防和治疗肥大细胞介导的炎症性疾病的新型化合物,组合物和方法。 本发明的优选方面是式(II)的化合物,其中:虚线独立地表示任选的键; 每个R 2独立地为(C 1-6)烷基,(C 1-6)烷氧基,卤素或羟基; 每个R 3独立地为(C 1-6)烷基,(C 1-6)烷氧基,卤素或羟基; X 3为-C(O) - 或-CR 7 R 8 - ,X 8为-CH(R 1)n1或-C(R 1)n1 = 其中R 1是氨基(N1-4)唑烷基,氨基(N1-4)唑基,(N1-4)唑烷基,(N1-4)唑基,-NHC(NH)NR9R9, -C(NR 9)R 9,-C(NH)NHR 10,-C(NH)NR 10 R 10或 - (CR 11 R 11)y NH 2, 或X 8是-N =或-NH(R 1)n1-,其中R 1是-C(NR 9)R 9,-C(NH)NHR 10或 -C(NH)NR 10 R 10,其中每个R 9独立地是氢或(C 1-6)烷基,每个R 10独立地是(C 1-6)烷基; 并且X 9为-CH(R 4) - 或-C(R 4)=,其中R 4为-R 12,-OR 12,-N(R 13) )R 12,-SR 12,-S(O)R 12,-S(O)2 R 12,-S(O)2OR 12,-S(O)2 N( R 13),-N(R 13)S(O)2 R 12,-C(O)R 12,-C(O)OR 12,-C( O)N(R 13)R 12,-N(R 13)C(O)R 12,-OC(O)N(R 13)R 12,-N (R 13)C(O)OR 12, - (CH 2)n 4 N(R 13)C(O)N(R 13)R 12,-OP(O) 13)或OR 12或-C(O)N(R 14)CH(COOH)R 12或X 9是-N =或-N(R 4) - ,其中 R 4是-C(O)R 12,-C(O)OR 12,-C(O)N(R 13)R 12,-OC(O) R 12或-C(O)N(R 14)CH(COOH)R 12,其中R 12,R 13和R 14如 发明概述; R 5为氢或(C 1-4)烷基,R 6为氢或(C 1-4)烷基,该烷基任选被一至两个独立地选自(C 1-4)烷氧基,羟基和 磺基,R 7是氢或甲基,R 8是氢,甲基或羟基。 化合物,组合物和方法对于预防和治疗与呼吸道相关的炎性疾病如哮喘和过敏性鼻炎以及其它类型的免疫性炎症性疾病如类风湿性关节炎,结膜炎和炎性肠病是有效的, 各种皮肤病学条件,以及某些病毒状况。 这些化合物包括肥大细胞蛋白酶类胰蛋白酶的有效和选择性抑制剂。 用于治疗这些病症的组合物包括口服,吸入,局部和肠胃外制剂以及包含这些制剂的装置。