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2. 发明授权

KR100450005B1 PDEⅢ와PDEⅣ및TNF를억제하는신규한이미드 失效
公开(公告)号：KR100450005B1
公开(公告)日：2005-01-15
申请号：KR1019980704910
申请日：1996-12-24
申请人： 셀진 코포레이션
发明人： 밀러조지더블유 , 쉬르메리
IPC分类号： C07D209/46
CPC分类号： C07D209/48 , C07D209/46
摘要： 1. Use of a compound of the formula in which: one of R and R is R -X and the other is hydrogen, nitro, cyano, trifluoromethyl, carbo(lower)alkoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, lower alkyl, alkylamino, lower alkoxy, halo, HF2CO, F3CO or R -X-; R is monocycloalkyl, bicycloalkyl or benzocycloalkyl of up to 18 carbon atoms, tetrahydropyran or tetrahydrofuran; X is a carbon-carbon bond, -CH2-, -O- or -N=; R is (i) o-phenylene, unsubstituted or substituted with 1 or more substituents each selected independently from nitro, cyano, halo, trifluoromethyl, carbo(lower)alkoxy, acetyl, or carbamoyl, unsubstituted or substituted with lower alkyl, acetoxy, carboxy, hydroxy, amino, lower alkylamino, lower acylamino, aminoalkyl, or lower alkoxy; (ii) the vicinally divalent residue of pyridine, pyrrolidine, imidizole, naphthalene, or thiophene, wherein the divalent bonds are on vicinal ring carbon atoms; (iii) a vicinally divalent cycloalkyl or cycloalkenyl of 4-10 carbon atoms, unsubstituted or substituted with one or more substituents each selected independently from the group consisting of nitro, cyano, halo, trifluoromethyl, carbo(lower)alkoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, lower alkylamino, lower alkyl, lower alkoxy, or phenyl; (iv) vinylene di-substituted with lower alkyl; or (v) ethylene, unsubstituted or monosubstituted or disubstituted with lower alkyl; R is -CO-, -CH2- or -CH2CO-; Y is -COZ, -CN, -OR , lower alkyl or aryl, Z is -NH2, -OH, -NHR, -R , or -OR ; R is hydrogen or lower alkyl; R is lower alkyl or benzyl, and n has a value of 0, 1, 2, or 3, wherein the term "lower" denotes from 1 to 6 carbon atoms, for the manufacture of a medicament for treating cancer.
摘要翻译： 1.式＆lt; CHEM＆gt;化合物的用途，其中：R 1，并且R 2是是低级烷基氨基，低级烷氧基，卤素，HF 2 CO，F 3 CO 或R 3 -X-; R＆LT 3的密度; 是至多18个碳原子的单环烷基，双环烷基或苯并环烷基，四氢吡喃或四氢呋喃; X是碳 - 碳键，-CH 2 - ， - O-或-N =; 为r 5个（i）未取代的或被1个或多个取代基取代的邻亚苯基，所述取代基各自独立地选自硝基，氰基，卤素，三氟甲基，碳（低级）烷氧基，乙酰基或氨基甲酰基，未被取代或被低级烷基，乙酰氧基，羧基，羟基，氨基，低级烷基氨基，低级酰基氨基，氨基烷基或低级烷氧基; （ii）吡啶，吡咯烷，咪唑，萘或噻吩的邻位二价残基，其中二价键在邻位环碳原子上; （iii）4-10个碳原子的邻位二价环烷基或环烯基，其未被取代或被一个或多个独立选自硝基，氰基，卤素，三氟甲基，碳（低级）烷氧基，乙酰基，氨基甲酰基，乙酰氧基，羧基，羟基，氨基，低级烷基氨基，低级烷基，低级烷氧基或苯基; （iv）用低级烷基二取代的亚乙烯基; 或（v）未取代的或被低级烷基单取代或二取代的亚乙基; 为r 6个是-CO - ， - CH 2 - 或-CH 2 CO-; Y是-COZ，-CN，-OR 8，低级烷基或芳基，Z是-NH 2，-OH，-NHR，-R 9或-OR 9; 为r 8是氢。是氢或低级烷基; 为r 9基是低级烷基或苄基，并且n具有0,1,2或3的值，其中术语“低级” 表示1至6个碳原子，用于制造治疗癌症的药物。

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