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    • 18. 发明申请
    • HETEROALKYL AND HETEROARYLTHIOALKYL THIOPHENOLIC COMPOUNDS AS 5-LIPOXYGENASE INHIBITORS
    • 作为5-LIPOXYGENASE抑制剂的异戊醇和异戊醇锂噻二醇化合物
    • WO1996012703A1
    • 1996-05-02
    • PCT/US1995012263
    • 1995-10-02
    • G.D. SEARLE & CO.KHANNA, Ish, KumarSTEALEY, Michael, AllanWEIER, Richard, Mathias
    • G.D. SEARLE & CO.
    • C07D215/22
    • C07D215/227C07D209/08C07D235/06C07D263/58C07D471/04
    • The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein: R and R are each alkyl; n is an integer of from 1 to 5; p is an integer of from 0 to 1; q is an integer of from 0 to 3; r is an integer of from 0 to 1; and R is a bicyclic group, with the proviso that when R and R are each alkyl, and p, q and r are each O, R is not a napthylmethyl group. These compounds are inhibitors of 5-lipoxygenase, and are useful for the treatment of 5-lipoxygenase mediated conditions, including inflammation-associated disorders and allergic and hypersensitivity reactions. The present invention also provides pharmaceutical compositions comprising a therapeutically-effective amount of a compound of formula (I) in combination with a pharmaceutically-acceptable carrier, and methods for treating 5-lipoxygenase mediated conditions, inflammation-associated disorders and allergies in an animal comprising administering a therapeutically-effective amount of a compound of formula (I) to the animal.
    • 本发明提供式(I)化合物及其药学上可接受的盐,其中:R 1和R 2各自为烷基; n为1〜5的整数, p是0到1的整数; q为0〜3的整数; r为0〜1的整数; 并且R 3是双环基团,条件是当R 1和R 2各自为烷基且p,q和r各自为O时,R 3不是萘基甲基。 这些化合物是5-脂氧合酶的抑制剂,并且可用于治疗5-脂氧合酶介导的病症,包括炎症相关疾病和过敏性和超敏反应。 本发明还提供药物组合物,其包含治疗有效量的式(I)化合物与药学上可接受的载体的组合,以及用于治疗动物中的5-脂氧合酶介导的病症,炎症相关疾病和过敏症的方法,包括 向动物施用治疗有效量的式(I)化合物。
    • 19. 发明申请
    • SUBSTITUTED-PHENYL(N,N'-CYCLOALKYL/ALKYL CARBOXAMIDE)-1H/3H-IMIDAZO[4,5-b]PYRIDINE COMPOUNDS AS PAF ANTAGONISTS
    • 取代的苯基(N,N'-环烷基/烷基羧酰胺)-1H / 3H-咪唑并[4,5-b]吡啶化合物作为PAF拮抗剂
    • WO1994012500A1
    • 1994-06-09
    • PCT/US1993010976
    • 1993-11-17
    • G.D. SEARLE & CO.WEIER, Richard, MathiasKHANNA, Ish, KumarSTEALEY, Michael, AllanJULIEN, Janet, AnneLENTZ, Kirk, Thomas
    • G.D. SEARLE & CO.
    • C07D471/04
    • C07D471/04C07F7/1804
    • A class of N,N'-cycloalkyl/alkyl benzamides of certain 1H-imidazo[4,5-b]pyridine and 3H-imidazo[4,5-b]pyridine compounds is described for treating cardiovascular and immuno-inflammatory related disorders mediated by platelet activating factor (PAF). Compounds of particular interest are those of formula (I), wherein each of X and X is independently selected from nitrogen atom and -CH-, with the proviso that when one of X and X is selected as nitrogen atom, then the other of X and X must be -CH-; wherein R is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, halophenyl, alkylsilyloxyalkyl, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and dialkylaminoalkyl; wherein each of R , R , R and R is independently selected from hydrido, hydroxy, alkyl, alkoxy, fluoro, chloro, bromo, haloalkyl, alkylthio, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, cyano, amino, monoalkylamino and dialkylamino; wherein each of R and R is independently selected from hydrido, alkyl, cycloalkyl, bicycloalkyl, heteroaryl, aryl, alkenyl and cycloalkenyl, and wherein any of said R and R substituents may be further substituted with one or more groups selected from linear or branched lower alkyl, lower alkoxy, fluoro, chloro and bromo; or a pharmaceutically-acceptable salt thereof.
    • 描述了某些1H-咪唑并[4,5-b]吡啶和3H-咪唑并[4,5-b]吡啶化合物的一类N,N'-环烷基/烷基苯甲酰胺,用于治疗心血管和免疫炎性相关病症介导 通过血小板激活因子(PAF)。 特别感兴趣的化合物是式(I)的化合物,其中X a和X b各自独立地选自氮原子和-CH-,条件是当X a和X b中的一个 >选择为氮原子,则X a和X b中的另一个必须为-CH-; 其中R 1选自氢,烷基,羟基烷基,烷氧基烷基,苯基,卤代苯基,烷基甲硅烷氧基烷基,氨基,单烷基氨基,二烷基氨基,氨基烷基,单烷基氨基烷基和二烷基氨基烷基。 其中R 5,R 6,R 7和R 8各自独立地选自氢,羟基,烷基,烷氧基,氟,氯,溴,卤代烷基,烷硫基,烷氧基烷基,羟烷基,烷硫基烷基, 氰基,氨基,单烷基氨基和二烷基氨基; 其中R 9和R 10各自独立地选自氢,烷基,环烷基,双环烷基,杂芳基,芳基,烯基和环烯基,并且其中所述R 9和R 10取代基中的任一个可以进一步 被一个或多个选自直链或支链的低级烷基,低级烷氧基,氟,氯和溴的基团取代; 或其药学上可接受的盐。