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1. 发明授权

US4639521A Isoquinoline derivatives 失效
标题翻译：异喹啉衍生物
公开(公告)号：US4639521A
公开(公告)日：1987-01-27
申请号：US878527
申请日：1986-06-20
申请人： Kunio Sannohe , Kengo Otsuka , Toshohiko Ito , Masahiko Maruyama , Takafumi Kitano , Makoto Hirayama
发明人： Kunio Sannohe , Kengo Otsuka , Toshohiko Ito , Masahiko Maruyama , Takafumi Kitano , Makoto Hirayama
IPC分类号： A61K31/47 , A61K31/472 , A61P9/04 , C07D217/24 , C07D401/04
CPC分类号： C07D401/04 , C07D217/24
摘要： Isoquinoline derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 denotes a hydrogen or halogen atom, or a nitro or acetyl group, and R.sub.2 denotes a hydrogen atom, or a methyl, methoxy, phenyl, 4-pyridyl or 2-pyridyl group, and therapeutically acceptable salts thereof have high cardiotonic activity and low toxicity.
摘要翻译：由通式（I）表示的异喹啉衍生物：其中R1表示氢或卤素原子，或硝基或乙酰基，R2表示氢原子，或甲基，甲氧基，苯基，4- 吡啶基或2-吡啶基，其治疗上可接受的盐具有高强度活性和低毒性。

2. 发明授权

US4782154A Isoquinoline derivatives 失效
标题翻译：异喹啉衍生物
公开(公告)号：US4782154A
公开(公告)日：1988-11-01
申请号：US75828
申请日：1987-07-17
申请人： Tatsuo Kaiho , Seitaro Kajiya , Kengo Otsuka , Masahiko Maruyama , Makoto Hirayama
发明人： Tatsuo Kaiho , Seitaro Kajiya , Kengo Otsuka , Masahiko Maruyama , Makoto Hirayama
IPC分类号： A61K31/47 , A61P9/00 , A61P9/04 , C07D401/04 , C07D217/16
CPC分类号： C07D401/04
摘要： The isoquinoline derivatives represented by the following general formula (I) are useful as cardiotonics having high cardiotonic activity and low toxicity: ##STR1## where R.sub.1 represents a lower C.sub.1 -C.sub.4 alkyl group or cyclopropyl group,R.sub.2 represents formyl group, lower C.sub.1 -C.sub.4 alkanoyl group and benzoyl group, lower C.sub.1 -C.sub.4 alkyl group, lower C.sub.1 -C.sub.4 alkenyl group, lower C.sub.1 -C.sub.4 hydroxy substituted alkyl group, C.sub.1 -C.sub.4 perfluoroalkyl group andR.sub.3 represents 4-pyridyl group or 2-pyridyl group respectively,and the therapeutically acceptable salts thereof are also useful as cardiotonics.
摘要翻译：由以下通式（I）表示的异喹啉衍生物可用作具有高强度活性和低毒性的强心剂：其中R 1表示低级C 1 -C 4烷基或环丙基，R 2表示甲酰基，低级 C1-C4烷酰基和苯甲酰基，低级C1-C4烷基，低级C1-C4烯基，低级C1-C4羟基取代烷基，C1-C4全氟烷基，R3分别代表4-吡啶基或2-吡啶基，其治疗上可接受的盐也可用作强心剂。

3. 发明授权

US08354529B2 Polyamine derivative and polyol derivative 有权
标题翻译：多胺衍生物和多元醇衍生物
公开(公告)号：US08354529B2
公开(公告)日：2013-01-15
申请号：US13289013
申请日：2011-11-04
申请人： Naruyoshi Mita , Mitsuaki Chida , Masaru Kawaguchi , Kengo Otsuka , Naoshi Nagai , Takaaki Yamazaki , Tetsuya Ichihashi
发明人： Naruyoshi Mita , Mitsuaki Chida , Masaru Kawaguchi , Kengo Otsuka , Naoshi Nagai , Takaaki Yamazaki , Tetsuya Ichihashi
IPC分类号： C07D401/14 , C08K5/3492 , C08L101/00 , C09K15/30
CPC分类号： C09K15/30 , C07D401/14 , C07D493/10 , C08K5/34926 , C09K15/16
摘要： A novel polyamine derivative, or polyol derivative, having a piperidylaminotriazine skeleton; salts of such compounds; a process for producing them; an organic material stabilizer comprising any of such compounds; a method of stabilizing an organic material; and a stabilized organinc material. Compounds of the general formula: (1) (wherein X is N(R4) or an oxygen atom; R1 is an n-valent hydrocarbon group; R2 is an hydrogen atom or an alkyl; R3 is a hydrogen atom, an alkyl, an alkoxy or an acyl; R4 is a hydrogen atom or an alkyl; and n is an integer of 3 to 16) are effective in the stabilization of an organic material against deterioration by light, heat, oxygen, ozone and electromagnetic waves, such as X-rays and γ-rays.
摘要翻译：具有哌啶基氨基三嗪骨架的新型多胺衍生物或多元醇衍生物; 这些化合物的盐; 一个生产它们的过程; 包含任何这些化合物的有机材料稳定剂; 稳定有机材料的方法; 和稳定的有机金属材料。通式为（1）的化合物（其中X为N（R4）或氧原子; R1为n价烃基; R2为氢原子或烷基; R3为氢原子，烷基，烷氧基或酰基; R 4为氢原子或烷基，n为3〜16的整数）可有效地抑制有机材料的光，热，氧，臭氧和电磁波的劣化，例如X 射线和γ射线。

4. 发明申请

US20120053270A1 POLYAMINE DERIVATIVE AND POLYOL DERIVATIVE 有权
标题翻译：聚氨酯衍生物和多元醇衍生物
公开(公告)号：US20120053270A1
公开(公告)日：2012-03-01
申请号：US13289013
申请日：2011-11-04
申请人： NARUYOSHI MITA , Mitsuaki Chida , Masaru Kawaguchi , Kengo Otsuka , Naoshi Nagai , Takaaki Yamazaki , Tetsuya Ichihashi
发明人： NARUYOSHI MITA , Mitsuaki Chida , Masaru Kawaguchi , Kengo Otsuka , Naoshi Nagai , Takaaki Yamazaki , Tetsuya Ichihashi
IPC分类号： C08K5/3492 , C08L23/06 , C08L23/12 , C07D401/14 , C07D493/10
CPC分类号： C09K15/30 , C07D401/14 , C07D493/10 , C08K5/34926 , C09K15/16
摘要： A novel polyamine derivative, or polyol derivative, having a piperidylaminotriazine skeleton; salts of such compounds; a process for producing them; an organic material stabilizer comprising any of such compounds; a method of stabilizing an organic material; and a stabilized organinc material. Compounds of the general formula: (1) (wherein X is N(R4) or an oxygen atom; R1 is an n-valent hydrocarbon group; R2 is an hydrogen atom or an alkyl; R3 is a hydrogen atom, an alkyl, an alkoxy or an acyl; R4 is a hydrogen atom or an alkyl; and n is an integer of 3 to 16) are effective in the stabilization of an organic material against deterioration by light, heat, oxygen, ozone and electromagnetic waves, such as X-rays and γ-rays.
摘要翻译：具有哌啶基氨基三嗪骨架的新型多胺衍生物或多元醇衍生物; 这些化合物的盐; 一个生产它们的过程; 包含任何这些化合物的有机材料稳定剂; 稳定有机材料的方法; 和稳定的有机金属材料。通式为（1）的化合物（其中X为N（R4）或氧原子; R1为n价烃基; R2为氢原子或烷基; R3为氢原子，烷基，烷氧基或酰基; R 4为氢原子或烷基，n为3〜16的整数）可有效地抑制有机材料的光，热，氧，臭氧和电磁波的劣化，例如X 射线和γ射线。

5. 发明授权

US5532349A Process for producing 1-(2'-deoxy-.beta.-D-erythro-pentofuranosyl)-5-trifluoromethyluracil derivatives 失效
标题翻译： 1-（2'-脱氧-β-D-赤型 - 呋喃戊糖基）-5-三氟甲基尿嘧啶衍生物的制备方法
公开(公告)号：US5532349A
公开(公告)日：1996-07-02
申请号：US275455
申请日：1994-07-15
申请人： Nobuya Kawauchi , Nobuyuki Fukazawa , Hiroki Ishibashi , Kengo Otsuka
发明人： Nobuya Kawauchi , Nobuyuki Fukazawa , Hiroki Ishibashi , Kengo Otsuka
IPC分类号： C07H19/06 , C07H19/073 , A61K31/70
CPC分类号： C07H19/06
摘要： A process for producing 1-(2'-deoxy-B-D-erythropentofuranosyl)-5-trifluoromethyluracil derivatives having the formula as shown below: ##STR1## wherein X.sup.1 and X.sup.2 are independently hydrogen or halogen, comprising:(a) reacting 5-trifluoromethyl-5,6-dihydrouracil with alkylsulfoxide in the presence of a halogen and and acid to obtain 5-trifluoromethyluracil;(b) reacting the obtained 5-trifluoromethyluracil with a silylating agent to obtain 5-trifluoromethyl-2,4 -bis(trimethylsilyloxy)uracil; and(c) reacting the obtained 5-trifluoromethyl-2,4-bis(trimethylsilyloxy)uracil with a protected 2-deoxyalpha-D-erthro-pentofuranosyl)halide derivative in chloroform solvent in the presence of fluoride ion and in the presence of a copper compound as a catalyst.The resulting, deblocked nucleosides are useful as antiviral and antitumor agents.
摘要翻译：一种制备具有下式的1-（2'-脱氧-β-赤式呋喃糖基）-5-三氟甲基尿嘧啶衍生物的方法：其中X1和X2独立地是氢或卤素，包括：（a）使5-三氟甲基 -5,6-二氢尿嘧啶与烷基亚砜在卤素存在下反应，得到5-三氟甲基尿嘧啶; （b）使所得5-三氟甲基尿嘧啶与甲硅烷基化试剂反应，得到5-三氟甲基-2,4-双（三甲基甲硅烷氧基）尿嘧啶; 和（c）使得到的5-三氟甲基-2,4-双（三甲基甲硅烷氧基）尿嘧啶与受保护的2-脱氧-α-D-戊硫基呋喃糖基）卤化物衍生物在氯仿溶剂中，在氟离子存在下，在铜化合物作为催化剂。所得到的解封核苷可用作抗病毒和抗肿瘤剂。

6. 发明授权

US5434155A Quinoline derivative fumarates 失效
标题翻译：喹啉衍生物富马酸盐
公开(公告)号：US5434155A
公开(公告)日：1995-07-18
申请号：US76589
申请日：1993-06-15
申请人： Nobuyuki Fukazawa , Tuneji Suzuki , Kengo Otsuka , Osamu Yano , Daiji Iwata , Yukichi Kawai
发明人： Nobuyuki Fukazawa , Tuneji Suzuki , Kengo Otsuka , Osamu Yano , Daiji Iwata , Yukichi Kawai
IPC分类号： A61K31/47 , A61K31/496 , A61P35/00 , C07D215/20 , A61K31/495 , C07D401/00
CPC分类号： C07D215/20
摘要： Compounds having an activity to stimulate the carcinostatic effect of carcinostatic agents, which can be expressed by the following general formula (1): ##STR1## in which A is ##STR2## (in which R.sub.1, R.sub.2 and R.sub.3 are each independent and represent a hydrogen atom or a phenyl group) are made into fumarates so as to improve their oral absorbability and solubility in water without interfering with their effects.
摘要翻译：具有刺激制癌剂的致癌作用的化合物，其可以由以下通式（1）表示：其中A为（其中R 1，R 2和R 3各自独立地为并且表示氢原子或苯基）制成富马酸盐，以便改善其在水中的口服吸收性和溶解性而不影响其效果。

7. 发明授权

US5463061A Process for production of glycide derivative 失效
标题翻译：制备糖苷衍生物的方法
公开(公告)号：US5463061A
公开(公告)日：1995-10-31
申请号：US175397
申请日：1994-01-13
申请人： Nobuyuki Fukazawa , Tsuneji Suzuki , Nobuya Kawauchi , Hironori Komatsu , Kengo Otsuka , Yuki Nakajima
发明人： Nobuyuki Fukazawa , Tsuneji Suzuki , Nobuya Kawauchi , Hironori Komatsu , Kengo Otsuka , Yuki Nakajima
IPC分类号： C07D303/22 , C07D303/23 , C07D405/12 , C07D215/20
CPC分类号： C07D303/22 , C07D405/12
摘要： A glycide derivative represented by the following general formula (I) is produced by reacting a hydroxyaryl or heteroaryl represented by A-OH with glycidyl tosylate in the presence of a cesium base as a base. Thereby, an aryl glycidyl ether derivative, which is an important intermediate for drug production, can be produced easily and reliably. Particularly when optically active glycidyl tosylate is used, said compound can be obtained at a high optical purity. ##STR1## wherein A represents an aryl group or a heteroaryl group.
摘要翻译： PCT No.PCT / JP93 / 00626 Sec。 371日期1994年1月13日 102（e）日期1994年1月13日PCT提交1993年5月13日PCT公布。公开号WO93 / 23386 日期：1月25日。由以下通式（I）表示的糖苷衍生物是通过使羟基芳基或由A-OH表示的杂芳基与甲苯磺酸缩水甘油酯在铯基作为碱的存在下反应制备的。因此，可以容易且可靠地制造作为药物生产的重要中间体的芳基缩水甘油醚衍生物。特别是当使用光学活性的甲苯磺酸缩水甘油酯时，可以高光学纯度获得所述化合物。（I）其中A表示芳基或杂芳基。

8. 发明授权

US5232923A Catechol derivatives and pharmaceutical preparations containing same 失效
标题翻译：儿茶酚衍生物和含有它的药物制剂
公开(公告)号：US5232923A
公开(公告)日：1993-08-03
申请号：US689098
申请日：1991-04-22
申请人： Nobuyuki Fukazawa , Kengo Otsuka , Shimada Shizuo , Yukio Miyama , Fumiaki Ikeda , Tatsuo Kaiho
发明人： Nobuyuki Fukazawa , Kengo Otsuka , Shimada Shizuo , Yukio Miyama , Fumiaki Ikeda , Tatsuo Kaiho
IPC分类号： C07C235/34 , C07C235/36 , C07C235/38 , C07D207/16 , C07D211/60 , C07D295/185
CPC分类号： C07D295/185 , C07C235/34 , C07C235/36 , C07C235/38 , C07D207/16 , C07D211/60 , C07C2101/14 , C07C2103/74
摘要： Catechol derivatives which produce nerve growth factor in particular tissues of the brain are disclosed. These derivatives provide preventive and therapeutic effects for regressive disorders of the central nervous system including senile dementia of the Alzheimer type.
摘要翻译：公开了在脑的特定组织中产生神经生长因子的儿茶酚衍生物。这些衍生物为包括阿尔茨海默氏型老年性痴呆的中枢神经系统的退行性疾病提供预防和治疗作用。

9. 发明授权

US5204348A Heterocyclic compounds and anticancer-drug potentiaters conaining them as effective components 失效
标题翻译：杂环化合物和抗癌药物增效剂使其成为有效成分
公开(公告)号：US5204348A
公开(公告)日：1993-04-20
申请号：US780472
申请日：1991-12-03
申请人： Nobuyuki Fukazawa , Makoto Odate , Tsuneji Suzuki , Kengo Otsuka , Takashi Tsuruo , Wakao Sato
发明人： Nobuyuki Fukazawa , Makoto Odate , Tsuneji Suzuki , Kengo Otsuka , Takashi Tsuruo , Wakao Sato
IPC分类号： C07D215/20 , C07D215/22 , C07D215/227 , C07D215/26 , C07D215/36 , C07D215/38 , C07D217/02 , C07D239/74 , C07D241/42 , C07D401/12 , C07D405/12
CPC分类号： C07D215/227 , C07D215/20 , C07D215/26 , C07D215/36 , C07D215/38 , C07D217/02 , C07D239/74 , C07D241/42 , C07D401/12 , C07D405/12
摘要： Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.
摘要翻译：由以下通式表示的新型杂环化合物可用作对抗癌药物掺入癌细胞具有增强作用的抗癌药物增效剂，所述化合物通过例如使通过使杂环反应获得的环氧化合物与表卤代醇与胺衍生物的化合物。

10. 发明授权

US08076478B2 Polyamine derivative and polyol derivative 有权
标题翻译：多胺衍生物和多元醇衍生物
公开(公告)号：US08076478B2
公开(公告)日：2011-12-13
申请号：US11795216
申请日：2006-01-18
申请人： Naruyoshi Mita , Mitsuaki Chida , Masaru Kawaguchi , Kengo Otsuka , Naoshi Nagai , Takaaki Yamazaki , Tetsuya Ichihashi
发明人： Naruyoshi Mita , Mitsuaki Chida , Masaru Kawaguchi , Kengo Otsuka , Naoshi Nagai , Takaaki Yamazaki , Tetsuya Ichihashi
IPC分类号： C07D401/14 , C08K5/3492 , C08L101/00 , C09K15/30
CPC分类号： C09K15/30 , C07D401/14 , C07D493/10 , C08K5/34926 , C09K15/16
摘要： A novel polyamine derivative, or polyol derivative, having a piperidylaminotriazine skeleton; salts of such compounds; a process for producing them; an organic material stabilizer comprising any of such compounds; a method of stabilizing an organic material; and a stabilized organic material. Compounds of the general formula: (1) (wherein X is N(R4) or an oxygen atom; R1 is an n-valent hydrocarbon group; R2 is a hydrogen atom or an alkyl; R3 is a hydrogen atom, an alkyl, an alkoxy or an acyl; R4 is a hydrogen atom or an alkyl; and n is an integer of 3 to 16) are effective in the stabilization of an organic material against deterioration by light, heat, oxygen, ozone and electromagnetic waves, such as X-rays and γ-rays.
摘要翻译：具有哌啶基氨基三嗪骨架的新型多胺衍生物或多元醇衍生物; 这些化合物的盐; 一个生产它们的过程; 包含任何这些化合物的有机材料稳定剂; 稳定有机材料的方法; 和稳定的有机材料。通式（1）的化合物（其中X为N（R4）或氧原子; R1为n价烃基; R2为氢原子或烷基; R3为氢原子，烷基，烷氧基或酰基; R 4为氢原子或烷基，n为3〜16的整数）可有效地抑制有机材料的光，热，氧，臭氧和电磁波的劣化，例如X 射线和γ射线。

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