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。

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：US20080295189A1

公开(公告)日：2008-11-27

申请号：US11662281

申请日：2005-09-12

申请人： Noboru Teramoto ,  Hidehiro Ilda ,  Takuya Hayashi ,  Yoichiro Ohta

发明人： Noboru Teramoto ,  Hidehiro Ilda ,  Takuya Hayashi ,  Yoichiro Ohta

IPC分类号： A01K67/00

CPC分类号： G09B23/306 ,  A01K67/027 ,  A01K2227/106 ,  A01K2227/108 ,  A01K2267/0375 ,  A61B6/037 ,  A61B6/486 ,  A61B6/504 ,  A61B6/507 ,  A61B6/508 ,  A61K49/0008

摘要： The present invention relates to a method for generating a non-human model animal of an arterial occlusive disease, wherein the method is characterized in that an artery is occluded at a specific site by ligating it or with an autologous blood clot. In particular, the present invention relates to a method and a kit for generating a cardiac infarction model, as well as a cardiac infarction animal model obtained by employing the method or kit, characterized in that in a non-human experimental animal, a blood vessel is ligated downstream of an arterial site of the heart to be occluded, followed by occluding the artery at said site. In addition, the present invention also relates to a method and a system for generating a non-human animal model of arterial embolus, as well as an arterial embolus animal model obtained by employing the method or system, characterized by adding an coagulating agent to autologous blood to form an autologous blood clot and subsequently employing an angiographic apparatus in delivering the autologous blood clot into an artery.

摘要翻译： 本发明涉及一种用于产生动脉闭塞性疾病的非人类模型动物的方法，其中所述方法的特征在于通过将动脉栓塞或与自体血块栓塞在特定部位闭塞动脉。 特别地，本发明涉及用于产生心肌梗死模型的方法和试剂盒，以及通过使用该方法或试剂盒获得的心肌梗塞动物模型，其特征在于，在非人实验动物中，血管 在心脏的动脉部位的下游连接以封闭，然后在所述部位闭塞动脉。 此外，本发明还涉及一种用于产生动脉栓塞的非人动物模型的方法和系统，以及通过采用该方法或系统获得的动脉栓塞动物模型，其特征在于将自体增加凝血剂 血液以形成自体血块，随后使用血管造影装置将自体血凝块输送到动脉中。