公开(公告)号：US06172228B2

公开(公告)日：2001-01-09

申请号：US09453223

申请日：1999-12-03

申请人： Kenichi Kashima ,  Yasuhiko Sakamoto ,  Yoichiro Ohta ,  Kenji Kawanishi ,  Shigetaka Takemura ,  Yasuko Takemura

发明人： Kenichi Kashima ,  Yasuhiko Sakamoto ,  Yoichiro Ohta ,  Kenji Kawanishi ,  Shigetaka Takemura ,  Yasuko Takemura

IPC分类号： C07D40106

CPC分类号： C07D295/088 ,  C07D213/38

摘要： A process for advantageously preparing a piperazinesulfonamide derivative represented by the general formula (III): wherein R1 is hydrogen atom, a straight or branched chain alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a halogen atom, hydroxyl group, trifluoromethyl group, nitro group or amino group; R2 is a phenyl group which may have as substituents on its phenyl ring 1 to 3 groups selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a halogen atom, hydroxyl group, trifluoromethyl group, nitro group and amino group, 2-pyridyl group, 3-pyridyl group or 4-pyridyl group; each of R3 and R4 is independently hydrogen atom, a straight or branched chain alkyl group having 1 to 6 carbon atoms, a hydroxyalkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms, or a phenyl group which may be substituted; and Y is an alkylene group having 1 to 12 carbon atoms, and a salt thereof.

摘要翻译： 一种有利地制备由通式（III）表示的哌嗪磺酰胺衍生物的方法：其中R1是氢原子，具有1至6个碳原子的直链或支链烷基，具有1至4个碳原子的烷氧基，卤素原子 ，羟基，三氟甲基，硝基或氨基; R2是可以在其苯环上具有取代基的苯基，其选自具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基，卤素原子，羟基 三氟甲基，硝基和氨基，2-吡啶基，3-吡啶基或4-吡啶基; R 3和R 4各自独立地为氢原子，具有1至6个碳原子的直链或支链烷基，具有1至4个碳原子的羟基烷基，具有3至8个碳原子的环烷基或苯基， 被替代 Y为碳原子数1〜12的亚烷基及其盐。

公开(公告)号：US6080750A

公开(公告)日：2000-06-27

申请号：US852118

申请日：1997-05-06

申请人： Masakatsu Hisaki ,  Yoichiro Ohta ,  Kenji Kawanishi ,  Yasuko Ichigobara ,  Fuzuki Iwakura ,  Masanobu Azuma ,  Tatsuo Suzutani ,  Manabu Node ,  Kiyoharu Nishide

发明人： Masakatsu Hisaki ,  Yoichiro Ohta ,  Kenji Kawanishi ,  Yasuko Ichigobara ,  Fuzuki Iwakura ,  Masanobu Azuma ,  Tatsuo Suzutani ,  Manabu Node ,  Kiyoharu Nishide

IPC分类号： C07D239/47 ,  A61K31/505 ,  A61P31/12 ,  C07D239/48 ,  C07D239/50 ,  C07D239/52 ,  C07D405/12

CPC分类号： C07D239/48 ,  C07D239/50

摘要： A pyrimidine compound of the formula [I] ##STR1## wherein R1 is H, C.sub.1 -C.sub.4 lower alkyl, halogen atom, --OH, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.6 hydroxy(lower)alkoxy or --NH.sub.2 ; R2 is H, --NH.sub.2 or --NHCOCH.sub.3 ; R3 is --NR5(CH.sub.2)i--CH.sub.2 OH; R4 is H, halogen atom, --NH.sub.2, --CN, --CHO, --CH.sub.2 OH, --COOH, --CH.sub.2 NH.sub.2, --CONH.sub.2 or --CH.dbd.N--A wherein A is --OH, C.sub.1 -C.sub.4 lower alkyl or C.sub.1 -C.sub.4 lower alkoxy; R5 is H or C.sub.1 -C.sub.4 lower alkyl; and i is an integer of 1 to 4, and an anti-rotavirus agent comprising, as an active ingredient, a compound of the formula [I] wherein R3 is a group selected from the following: ##STR2## The novel pyrimidine compound of the present invention and related derivatives thereof have superior anti-rotavirus action and are useful for the prophylaxis and treatment of rotaviral diseases.

摘要翻译： 式[I]的嘧啶化合物，其中R 1是H，C 1 -C 4低级烷基，卤素原子，-OH，C 1 -C 4低级烷氧基，C 1 -C 6羟基（低级）烷氧基或-NH 2; R2是H，-NH2或-NHCOCH3; R3是-NR5（CH2）i-CH2OH; R4是H，卤素原子，-NH2，-CN，-CHO，-CH2OH，-COOH，-CH2NH2，-CONH2或-CH = N-A，其中A是-OH，C1-C4低级烷基或C1-C4低级烷氧基; R5是H或C1-C4低级烷基; i为1〜4的整数，作为活性成分的抗轮状病毒药，其中，R 3为选自下述的基团的式[I]的化合物：本发明的新型嘧啶化合物和 其相关衍生物具有优异的抗轮状病毒作用，并且可用于预防和治疗轮状病毒疾病。