会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 2. 发明授权
    • Heteroaryl N-hydroxy amides and ureas with polar substituents as
5-lipoxygenase inhibitors
    • US4992464A
    • 1991-02-12
    • US430710
    • 1989-11-01
    • Dee W. BrooksJames B. SummersKaren E. RodriquesRobert G. MakiJoseph F. DellariaJames H. HolmsJimmie L. Moore
    • Dee W. BrooksJames B. SummersKaren E. RodriquesRobert G. MakiJoseph F. DellariaJames H. HolmsJimmie L. Moore
    • C07D209/14C07D307/81C07D333/58A61K31/38C07D333/56
    • C07D333/58C07D209/14C07D307/81
    • Compounds, compositions a method of inhibiting lipoxygenase and treating related disorders are disclosed. The compounds are of the formula:Ar-A(R.sub.2).sub.n -N(OM)-CZ-R.sub.1whereinAr is ##STR1## where X is O, S, SO.sub.2 or NR.sub.3 ;R.sub.3 is hydrogen, alkyl, alkylaryl, alkoyl, alkylakoyl, aroyl or alkylaroyl;Y is hydrogen, halogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, --OR, --SR, --COOR, --COR, --CON(R).sub.2, --OCOR, --N(R).sub.2, --O(CH).sub.2, --SO.sub.2 R, --SO.sub.2 N(R).sub.2, --O(CH.sub.2).sub.p OR, --CN, --NO.sub.2, --O(CH).sub.p O(CH.sub.2).sub.p OR or --CF.sub.3 ;R is hydrogen, hydroxyl, alkyl, alkylaryl or aryl;m is 0 to 5;p is 1 to 4;A is C.sub.1 -C.sub.12 alkylene or C.sub.2 -C.sub.14 alkenylene;R.sub.2 is --OR, --SR, --COOR, --COR, --CON(R).sub.2, --OCOR, --N(R).sub.2, --O(CH.sub.2).sub.y CON(R).sub.2, --O(CH.sub.2).sup.y OR, --CN, --NO.sub.2, 1-tetrazolo, C.sub.4 -C.sub.8 cyclic amido, imidazolo, --O(CH.sub.2).sub.y O(CH.sub.2).sub.y OR, --CF.sub.3, --N(R) COCHR--NH(R), CONHCH(R)CO.sub.2 R, --OCOCHR-NH(R), --CR(NHR)CONR, --CR(NHR)COR, morpholino, --NH(CH.sub.2).sub.y OH, --N[(CH.sub.2).sub.y OH].sub.2, --N.sub.3, --SO.sub.2 N(R).sub.2, --N(R)COR, --N(R)COOR, --N(R)CON(R).sub.2, --C(.dbd.NOH)NHOH or --C(.dbd.NOH)NH.sub.2 where R is as defined above, y is 1 to 4 and --N(R).sub.2 can form a heterocyclic ring of 5-8 atoms;M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable group;Z is oxygen or sulfur; andR.sub.1 us hydrogen, alkyl, alkenyl, --NR.sub.4 R.sub.5, --NCOR.sub.6 or --Q--(R.sub.2).sub.2 where R.sub.4 and R.sub.5 independently selected from the group consisting of hydrogen, hydroxyl, alkyl, substituted alkyl with 1-3 substituents selected from the group consisting of R.sub.2 as defined above, acyl, aryl and CON(R).sub.2 is as defined above, R.sub.6 is hydrogen alkyl, alkylaryl, aryl or NR.sub.4 R.sub.5 where R.sub.4 and R.sub.5 are as defined above and where NR.sub.4 R.sub.5 can form a heterocyclic ring of a 5-8 atoms, Q is alkyl, alkenyl or aryl and z is 0 to 3; provided when n is O, R.sub.1 is not hydrogen, alkyl, alkenyl, or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are as defined above; and the pharmaceutically acceptable salts thereof.
    • 3. 发明授权
    • Indole carboxylate derivatives which inhibit leukotriene biosynthesis
    • 抑制白细胞三烯生物合成的吲哚羧酸衍生物
    • US5288743A
    • 1994-02-22
    • US979138
    • 1992-11-20
    • Dee W. BrooksKeith W. WoodsKaren E. Rodriques
    • Dee W. BrooksKeith W. WoodsKaren E. Rodriques
    • C07D209/30C07D401/12C07D403/12C07D409/12C07D417/12A61K31/405C07D277/04
    • C07D401/12C07D209/30C07D403/12C07D409/12C07D417/12
    • Compounds of the structure ##STR1## where A is straight or branched divalent alkylene or divalent cycloalkylene, R.sub.1 is selected from hydrogen; alkylthio; optionally substituted phenylthio; optionally substituted phenylalkylthio; optionally substituted 2-, 3-, and 4-pyridyl; optionally substituted 2-, and 3-thienylthio; and optionally substituted 2-thiazolythio, R.sub.2 is selected from --COOB; --COOalkyl; --COOalkyl(carbocyclic aryl); --CONR.sub.5 R.sub.6 ; --COR.sub.6 ; and --OH, R.sub.3 is selected from phenylalkyl and heteroarylalkyl, and R.sub.4 is selected from optionally substituted alkoxy(carbocyclic aryl); optionally substituted carbocyclic aryloxy; optionally substituted heteroarylalkoxy; and optionally substituted heteroaryloxy are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
    • 其中A是直链或支链二价亚烷基或二价亚环烷基的结构化合物,其中A选自氢; 烷硫基 任选取代的苯硫基; 任选取代的苯基烷硫基; 任选取代的2-,3-和4-吡啶基; 任选取代的2-和3-噻吩基硫基; 和任选取代的2-噻唑硫基,R2选自-COOB; -COO烷基; -COO烷基(碳环芳基); -CONR5R6; -COR6; 和-OH,R 3选自苯基烷基和杂芳基烷基,并且R 4选自任选取代的烷氧基(碳环芳基); 任选取代的碳环芳氧基; 任选取代的杂芳基烷氧基; 和任选取代的杂芳氧基是脂氧合酶的有效抑制剂,从而抑制白细胞三烯的生物合成。 这些化合物可用于治疗或改善过敏性和炎性疾病状态。