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1. 发明授权

US6080750A Pyrimidine compound and anti-rotavirus composition 失效
标题翻译：嘧啶化合物和抗轮状病毒组合物
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。

2. 发明申请

US20120258042A1 COMBINED USE OF TGF-B SIGNALING INHIBITOR AND ANTITUMOR AGENT 审中-公开
标题翻译： TGF-B信号抑制剂和抗肿瘤剂的组合使用
公开(公告)号：US20120258042A1
公开(公告)日：2012-10-11
申请号：US13401230
申请日：2012-02-21
申请人： Kazunori KATAOKA , Kohei MIYAZONO , Mitsunobu KANO , Younsoo BAE , Nobuhiro NISHIYAMA , Kosei HIRAKAWA , Masakazu YASHIRO , Manabu Node
发明人： Kazunori KATAOKA , Kohei MIYAZONO , Mitsunobu KANO , Younsoo BAE , Nobuhiro NISHIYAMA , Kosei HIRAKAWA , Masakazu YASHIRO , Manabu Node
IPC分类号： A61K31/4709 , A61K31/444 , A61K31/506 , A61P35/00 , A61K39/395 , A61K47/48 , A61K39/44 , A61K51/10 , A61K31/4439 , A61K31/5025
CPC分类号： A61K45/06 , A61K31/4439 , A61K31/4709 , A61K31/5025 , A61K31/506 , A61K31/7088 , A61K38/1793 , A61K47/60
摘要： The combined use of a TGF-β signaling inhibitor and an antitumor active substance or an imaging agent modified by a drug-encapsulating macromolecular micelle, or the like, is provided. The selective delivery capability of the antitumor active substance or the imaging agent to the target is improved, increasing the antitumoral activity in the target.
摘要翻译：结合使用TGF- 提供了通过药物封装的大分子胶束等改性的信号抑制剂和抗肿瘤活性物质或成像剂。提高了抗肿瘤活性物质或成像剂对目标物的选择性递送能力，增加了靶标中的抗肿瘤活性。

3. 发明授权

US06384228B2 Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 失效
标题翻译：卤代吡啶基 - 氮杂环戊烷衍生物及其中间体的合成方法
公开(公告)号：US06384228B2
公开(公告)日：2002-05-07
申请号：US09462379
申请日：2000-01-07
申请人： Manabu Node , Daisaku Nakamura , Toshio Fujiwara , Shogo Ichihashi
发明人： Manabu Node , Daisaku Nakamura , Toshio Fujiwara , Shogo Ichihashi
IPC分类号： C07D21170
CPC分类号： C07D487/04
摘要： The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
摘要翻译：本发明涉及一种合成光学活性卤代吡啶基 - 氮杂环戊烷衍生物的方法及其中间体，其包括由光学活性丙酮二羧酸酯衍生物制备光学活性的丙烯-1,3-二羧酸酯衍生物，然后进行通过7-氮杂双环[2.2.1]庚烷衍生物得到目的产物。

4. 发明授权

US5106970A Optically active 4-morpholino-2-(1-naphthylmethyl)-4-oxobutyric acid 2'-hydroxy-1,1'binaphthalen-2-yl 失效
标题翻译：光学活性的4-吗啉-2-（1-萘甲基）-4-氧代丁酸2'-羟基-1,1'-联苯-2-基
公开(公告)号：US5106970A
公开(公告)日：1992-04-21
申请号：US724628
申请日：1991-07-02
申请人： Kaoru Fuji , Manabu Node , Fujie Tanaka
发明人： Kaoru Fuji , Manabu Node , Fujie Tanaka
IPC分类号： C07D295/18 , A61K31/535 , A61K31/5375 , A61P9/12 , C07D295/185
CPC分类号： C07D295/185
摘要： Optically active 4-morpholino-2-(1-naphthylmethyl)-4-oxobutyric acid 2'-hydroxy-1,1'-binaphthalen-2-yl represented by formula (I): ##STR1## wherein * indicates an asymmetric carbon atom, which is prepared by reacting 4-morpholino-4-oxobutyric acid 2'-hydroxy-1,1'-binaphthalen-2-yl represented by formula (II): ##STR2## with a 1-halomethylnaphthalene in the presence of a base. The compound (I) is a useful intermediate for preparing pharmaceuticals such as a renin inhibitors.

5. 发明申请

US20090186076A1 Combined Use of TGF-Beta Signaling Inhibitor and Antitumor Agent 审中-公开
标题翻译：组合使用TGF-β信号传导抑制剂和抗肿瘤剂
公开(公告)号：US20090186076A1
公开(公告)日：2009-07-23
申请号：US12223463
申请日：2006-08-30
申请人： Kazunori Kataoka , Kohei Miyazono , Mitsunobu Kano , Younsoo Bae , Nobuhiro Nishiyama , Kosei Hirakawa , Masakazu Yashiro , Manabu Node
发明人： Kazunori Kataoka , Kohei Miyazono , Mitsunobu Kano , Younsoo Bae , Nobuhiro Nishiyama , Kosei Hirakawa , Masakazu Yashiro , Manabu Node
IPC分类号： A61K9/127 , A61K31/7088 , A61K39/395 , A61K51/00
CPC分类号： A61K45/06 , A61K31/4439 , A61K31/4709 , A61K31/5025 , A61K31/506 , A61K31/7088 , A61K38/1793 , A61K47/60
摘要： The combined use of a TGF-β signaling inhibitor and an antitumor active substance or an imaging agent modified by a drug-encapsulating macromolecular micelle, or the like, is provided. The selective delivery capability of the antitumor active substance or the imaging agent to the target is improved, increasing the antitumoral activity in the target.
摘要翻译：提供了组合使用TGF-β信号传导抑制剂和抗肿瘤活性物质或通过药物封装的大分子胶束等改性的成像剂。抗肿瘤活性物质或成像剂对靶标的选择性递送能力得到改善，提高了靶标中的抗肿瘤活性。

6. 发明授权

US06486323B1 Process for producing optically active tropinonemonocarboxylic acid derivative 有权
标题翻译：光学活性托品酮一羧酸衍生物的制备方法
公开(公告)号：US06486323B1
公开(公告)日：2002-11-26
申请号：US09806592
申请日：2001-03-30
申请人： Manabu Node , Soichi Nakamura , Daisaku Nakamura
发明人： Manabu Node , Soichi Nakamura , Daisaku Nakamura
IPC分类号： C07D45102
CPC分类号： C12P17/10 , C12P41/00 , C12P41/005
摘要： An optically active tropinonemonocarboxylic acid ester derivative useful as an intermediate for synthesis of optically active tropane derivatives was obtained by reacting succindialdehyde with an organic amine and acetonedicarboxylic acid ester to obtain a tropinonedicarboxylic acid ester derivative, and then subjecting this derivative to enzyme-catalyzed asymmetric dealkoxy-carbonylation. Since anhydroecgonine methyl ester derived from the optically active tropinone-monocarboxylic acid ester derivative by reduction and dehydration had the same direction of optical rotation as in the case of anhydroecgonine methyl ester obtained from natural cocaine, it was proved that the obtained optically active tropinonemonocarboxylic acid ester derivative had the same absolute configuration as that of natural cocaine. The yield of the optically active tropinonemonocarboxylic acid ester derivative from the asymmetric dealkoxycarbonylation was 30 to 50 mol %, and its optical purity was 70 to 97% ee. In addition, it was found that a crystalline optically active anhydroecgonine carboxylic acid ester derivative can be obtained by reducing and then dehydrating the optically active tropinonemonocarboxylic acid ester derivative and that its optical purity can easily be increased by recrystallization.
摘要翻译：通过使琥珀醛与有机胺和丙酮二羧酸酯反应得到托品酮二羧酸酯衍生物，然后将该衍生物进行酶催化的不对称脱烷基，得到用作合成光学活性托烷衍生物的中间体的光学活性托品酮单羧酸酯衍生物羰基化。由于通过还原和脱水衍生自光学活性的托品酮 - 单羧酸酯衍生物的脱氢异君子酸甲酯具有与从天然可卡因得到的脱氢山梨醇甲酯的情况相同的旋光方向，所以证明得到的光学活性托品酮单羧酸酯衍生物具有与天然可卡因相同的绝对构型。来自不对称脱烷基羰基化反应的光学活性托品酮二羧酸酯衍生物的收率为30〜50摩尔％，光学纯度为70〜97％ee。此外，发现通过使光学活性托品酮一羧酸酯衍生物还原然后使其脱水，可以得到结晶光学活性的脱氢gon根化羧酸酯衍生物，并且可以通过重结晶容易地提高其光学纯度。

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