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1. 发明授权

US06329338B1 Derivatives of cyclodepsipeptide PF1022 substance 失效
标题翻译：环糊精PF1022物质的衍生物
公开(公告)号：US06329338B1
公开(公告)日：2001-12-11
申请号：US09043558
申请日：1998-05-20
申请人： Osamu Sakanaka , Yumiko Okada , Makoto Ohyama , Maki Matsumoto , Masaaki Takahashi , Yasushi Murai , Katsuharu Iinuma , Achim Harder , Norbert Mencke , Gerhard Bonse , Peter Jeschke
发明人： Osamu Sakanaka , Yumiko Okada , Makoto Ohyama , Maki Matsumoto , Masaaki Takahashi , Yasushi Murai , Katsuharu Iinuma , Achim Harder , Norbert Mencke , Gerhard Bonse , Peter Jeschke
IPC分类号： A61K3812
CPC分类号： C07D273/00 , Y02P20/55
摘要： Novel derivatives of PF1022 substance, which are cyclodepsipeptides represented by the general formula (I) shown below or their salts are useful as anthelmintic agent for prevention or treatment of parasitic infections.
摘要翻译： PF1022物质的新型衍生物，其为由下述通式（I）表示的环缩缩肽或其盐，可用作预防或治疗寄生虫感染的驱肠剂。

2. 发明授权

US5747448A Derivatives of cyclodepsipeptide PF 1022 失效
标题翻译：环糊精肽PF 1022的衍生物
公开(公告)号：US5747448A
公开(公告)日：1998-05-05
申请号：US505213
申请日：1995-09-08
申请人： Makoto Ohyama , Maki Ohishi , Yumiko Okada , Masao Koyama , Shinjiro Sumi , Yasushi Murai , Masayuki Takagi , Tadaaki Okada , Osamu Sakanaka , Toshio Yoneta , Katsuharu Iinuma , Seiji Shibahara
发明人： Makoto Ohyama , Maki Ohishi , Yumiko Okada , Masao Koyama , Shinjiro Sumi , Yasushi Murai , Masayuki Takagi , Tadaaki Okada , Osamu Sakanaka , Toshio Yoneta , Katsuharu Iinuma , Seiji Shibahara
IPC分类号： C07D273/00 , A61K38/15 , C07K11/02
CPC分类号： C07D273/00
摘要： Novel PF 1022 derivatives--cyclodepsipeptides represented by the below-described formula (I)--and acid addition salts thereof, which have been synthesized according to the present invention, have anthelmintic activities against various parasitic worms which are parasitic on human bodies, domestic animals and pet animals. They are therefore useful as anthelmintics for the prevention or treatment of parasitic infections. ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Y and Z have been defined herein.
摘要翻译： PCT No.PCT / JP94 / 00252 Sec。 371日期1995年9月8日 102（e）1995年9月8日PCT PCT 1994年2月18日PCT公布。出版物WO94 / 19334 日期1994年9月1日根据本发明合成的由下述式（I）表示的新型PF1022衍生物 - 环缩酚酸肽及其酸加成盐对于寄生于人的各种寄生虫具有驱虫活性身体，家畜和宠物。因此，它们可用作预防或治疗寄生虫感染的驱虫剂。式（I）：其中R1，R2，R3，R4，Q，X，Y和Z在本文中已经定义。

3. 发明授权

US06288223B1 Process for the selective preparation of Z-isomers of 3-2(substituted vinyl)cephalosporins 有权
标题翻译：选择性制备3-2（取代乙烯基）头孢菌素的Z-异构体的方法
公开(公告)号：US06288223B1
公开(公告)日：2001-09-11
申请号：US09446380
申请日：2000-02-18
申请人： Yumiko Okada , Masamichi Sukegawa , Tatsuo Watanabe , Hiroyuki Iwasawa , Yasushi Murai , Katsuharu Iinuma
发明人： Yumiko Okada , Masamichi Sukegawa , Tatsuo Watanabe , Hiroyuki Iwasawa , Yasushi Murai , Katsuharu Iinuma
IPC分类号： C07D50104
CPC分类号： C07D501/00 , Y02P20/55
摘要： There can be produced, at a high selectivity and in a high yield, the Z-isomer of a 7-N-unsubstituted or substituted-amino-3-[2-(4-substituted or unsubstituted-thiazol-5-yl) vinyl]-3-cephem-4-carboxylic acid or an ester thereof having the general formula (IV) wherein R1 denotes a hydrogen atom, a mono-valent amino-protecting group or a 2-(2-N-protected or unprotected aminothiazol-4-yl)- 2-alkoxyiminoacetyl group, R2 denotes a hydrogen atom, or R1 and R2 as taken together mean one di-valent amino-protecting group, R3 denotes a hydrogen atom, pivaloyloxymethyl group or a carboxyl-protecting group and R8 denotes an alkyl group and so on, by a process comprising reacting a 7-N-unsubstituted or substituted-amino-3-[(tri-substituted-phosphoranylidene) methyl]-3-cephem-4-carboxylic acid or an ester thereof having the general formula (I) wherein R1, R2 and R3 each have the same meanings as defined above, and R4 denotes a lower alryl group or an aryl group, with a 4-substituted or unsubstituted-thiazol-5-carbaldehyde in a mixed solvent consisting of a mixture of one or more chlorinated hydrocarbon solvent(s) with one or more lower alkanol(s) at a low temperature of +5° C. or below. According to the processes of this invention, the production of such E-isomer of the compound (IV) that is of lower antibacterial activity than that of the Z-isomer can be suppressed remarkedly. Further, the Z-isomer of a high purity can be produced efficiently in a facile way.
摘要翻译：可以以高选择性和高产率制备7-N-未取代或取代的氨基-3- [2-（4-取代或未取代的 - 噻唑-5-基）乙烯基的Z-异构体 ] - 3-头孢烯-4-羧酸或其具有通式（IV）的酯，其中R 1表示氢原子，一价氨基保护基或2-（2-N-保护或未保护的氨基噻唑-2-基） 4-烷氧基亚氨基乙酰基，R 2表示氢原子，或者R 1和R 2一起表示一个二价氨基保护基，R 3表示氢原子，新戊酰氧基甲基或羧基保护基，R 8表示烷基等，通过包括使7-N - 未取代的或取代的氨基-3 - [（三取代的亚正膦基）甲基] -3-头孢烯-4-羧酸或其酯具有通式（I）其中R1，R2和R3各自具有与上述相同的含义，R4表示低级烯丙基或芳基，具有4-取代或未取代的t 在一个或多个氯化烃溶剂与一种或多种低级链烷醇的混合物中，在+ 5℃或更低的低温下混合的混合溶剂中，根据本发明的方法，能够显着抑制抗Z活性降低的化合物（Ⅳ）的这种E-异构体的生产。此外，可以以简便的方式有效地制备高纯度的Z-异构体。

4. 发明授权

US07002009B2 Crystalline tricyclic triazolobenzazepine derivative 失效
标题翻译：结晶三环三氮杂苯并氮杂衍生物
公开(公告)号：US07002009B2
公开(公告)日：2006-02-21
申请号：US10500157
申请日：2002-12-25
申请人： Shin-Ichi Kitahara , Hanae Furukawa , Toshihiro Yamaguchi , Sachiko Miyamoto , Yumiko Okada
发明人： Shin-Ichi Kitahara , Hanae Furukawa , Toshihiro Yamaguchi , Sachiko Miyamoto , Yumiko Okada
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are novel crystalline 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine and a pharmaceutical composition comprising the same.
摘要翻译：公开了新的结晶2-（1-异丙氧羰基氧基-2-甲基丙基）-7,8-二甲氧基-4（5H），10-二氧代-2H-1,2,3-三唑并[4,5-c] [1] 苯并吖庚因和包含其的药物组合物。

5. 发明授权

US5704896A Endoscope apparatus with lens for changing the incident angle of light for imaging 失效
标题翻译：具有镜头的内窥镜装置，用于改变用于成像的光的入射角
公开(公告)号：US5704896A
公开(公告)日：1998-01-06
申请号：US424108
申请日：1995-04-19
申请人： Souhei Fukunishi , Yumiko Okada , Tadashi Sekiguchi
发明人： Souhei Fukunishi , Yumiko Okada , Tadashi Sekiguchi
IPC分类号： A61B1/05 , G02B23/24
CPC分类号： G02B23/2423 , A61B1/05
摘要： A solid-state image pickup device has a photosensitive chip and an array of microlenses arranged on the incident side of the photosensitive chip. A correction lens is arranged on the incident side of the microlens array to reduce incident angles of light entering the microlenses. The solid-state image pickup device may be incorporated in a head of an endoscope of an endoscopic apparatus to receive light from an optical system arranged in the head. The head includes a unit for changing paths of light to the microlenses to reduce incident angles of the light entering the microlenses.
摘要翻译：固态摄像装置具有感光芯片和布置在感光芯片入射侧的微透镜阵列。在微透镜阵列的入射侧设置校正透镜，以减少进入微透镜的光的入射角。固态图像拾取装置可以结合在内窥镜装置的内窥镜的头部中以从布置在头部中的光学系统接收光。头包括用于将光线路径改变为微透镜以减少进入微透镜的光的入射角的单元。

6. 发明申请

US20050080270A1 Process for producing 1 2 3 triazole compound 失效
标题翻译： 1 2 3三唑化合物的制备方法
公开(公告)号：US20050080270A1
公开(公告)日：2005-04-14
申请号：US10502392
申请日：2003-02-03
申请人： Shohei Yasuda , Koreaki Imura , Yumiko Okada , Shinichiro Tsujiyama
发明人： Shohei Yasuda , Koreaki Imura , Yumiko Okada , Shinichiro Tsujiyama
IPC分类号： C07D249/04
CPC分类号： C07D249/04 , Y02P20/55
摘要： Disclosed is a process for efficiently producing a compound represented by formula (I): wherein R1 represents aryl, amino, alkyl, or alkoxy; R2 represents a protective group of the carboxylic acid; and R3 represents an alkali metal, a hydrogen atom, alkyl, aryl, alkylsulfonyl, arylsulfonyl, or trialkylsilyl. This process is characterized by reacting a compound of formula (II) with a compound of formula (III) in the presence of a transition metal compound.
摘要翻译：公开了一种有效制备由式（I）表示的化合物的方法：其中R 1表示芳基，氨基，烷基或烷氧基; R 2表示羧酸的保护基; R 3表示碱金属，氢原子，烷基，芳基，烷基磺酰基，芳基磺酰基或三烷基甲硅烷基。该方法的特征在于使式（II）化合物与式（III）化合物在过渡金属化合物存在下反应。

7. 发明授权

US07238812B2 Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic agents 失效
标题翻译：三环三氮代氮杂吖庚因衍生物，其制备方法和抗过敏剂
公开(公告)号：US07238812B2
公开(公告)日：2007-07-03
申请号：US11269828
申请日：2005-11-09
申请人： Yasuo Ohtsuka , Toshio Nishizuka , Sohjiro Shiokawa , Seiji Tsutsumi , Mami Kawaguchi , Hideo Kitagawa , Hiromi Takata , Takashi Shishikura , Toyoaki Ishikura , Kenichi Fushihara , Yumiko Okada , Sachiko Miyamoto , Maki Shiobara
发明人： Yasuo Ohtsuka , Toshio Nishizuka , Sohjiro Shiokawa , Seiji Tsutsumi , Mami Kawaguchi , Hideo Kitagawa , Hiromi Takata , Takashi Shishikura , Toyoaki Ishikura , Kenichi Fushihara , Yumiko Okada , Sachiko Miyamoto , Maki Shiobara
IPC分类号： C07D249/04
CPC分类号： C07D487/04 , C07C59/76 , C07C69/738 , C07D249/04 , C07D401/12 , C07F9/6561
摘要： Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereon. The compounds are useful as antiallergic agents and exhibit excellent bioavailability. wherein R1 represents hydrogen, OH, alkyl or phenyl alkyl, R2, R3, R4, and R5 represent hydrogen, halogen, optionally protected hydroxyl, formyl, optionally substituted alkyl, alkenyl, alkoxy or the like, and Q represents a group selected from the following groups (i) to (iv), halogen, or alkoxy:
摘要翻译：提供了形式或前体药物的三环三唑并苯并吖嗪衍生物。根据本发明的化合物是由式（I）表示的化合物及其上的药理学上可接受的盐和溶剂合物。这些化合物可用作抗过敏剂并且表现出优异的生物利用度。其中R 1表示氢，OH，烷基或苯基烷基，R 2，R 3，R 4，和R 5表示氢，卤素，任意保护的羟基，甲酰基，任选取代的烷基，烯基，烷氧基等，Q表示选自以下组（i）至（iv）中的基团，卤素或烷氧基：

8. 发明授权

US07238719B2 Process for producing 1,2,3-Triazole compounds 失效
标题翻译：制备1,2,3-三唑化合物的方法
公开(公告)号：US07238719B2
公开(公告)日：2007-07-03
申请号：US10502392
申请日：2003-02-03
申请人： Shohei Yasuda , Koreaki Imura , Yumiko Okada , Shinichiro Tsujiyama
发明人： Shohei Yasuda , Koreaki Imura , Yumiko Okada , Shinichiro Tsujiyama
IPC分类号： A61K31/41 , C07D249/04
CPC分类号： C07D249/04 , Y02P20/55
摘要： Disclosed is a process for efficiently producing a compound represented by formula (I): wherein R1 represents aryl, amino, alkyl, or alkoxy; R2 represents a protective group of the carboxylic acid; and R3 represents an alkali metal, a hydrogen atom, alkyl, aryl, alkylsulfonyl, arylsulfonyl, or trialkylsilyl. This process is characterized by reacting a compound of formula (II) with a compound of formula (III) in the presence of a transition metal compound.
摘要翻译：公开了一种有效制备由式（I）表示的化合物的方法：其中R 1表示芳基，氨基，烷基或烷氧基; R 2表示羧酸的保护基; R 3表示碱金属，氢原子，烷基，芳基，烷基磺酰基，芳基磺酰基或三烷基甲硅烷基。该方法的特征在于使式（II）化合物与式（III）化合物在过渡金属化合物存在下反应。

9. 发明授权

US06372735B1 Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic 有权
标题翻译：三环三氮苯并氮杂衍生物，其制备方法和抗过敏剂
公开(公告)号：US06372735B1
公开(公告)日：2002-04-16
申请号：US09509494
申请日：2000-03-29
申请人： Yasuo Ohtsuka , Toshio Nishizuka , Sohjiro Shiokawa , Seiji Tsutsumi , Mami Kawaguchi , Hideo Kitagawa , Hiromi Takata , Takashi Shishikura , Toyoaki Ishikura , Kenichi Fushihara , Yumiko Okada , Sachiko Miyamoto , Maki Shiobara
发明人： Yasuo Ohtsuka , Toshio Nishizuka , Sohjiro Shiokawa , Seiji Tsutsumi , Mami Kawaguchi , Hideo Kitagawa , Hiromi Takata , Takashi Shishikura , Toyoaki Ishikura , Kenichi Fushihara , Yumiko Okada , Sachiko Miyamoto , Maki Shiobara
IPC分类号： A61K3155
CPC分类号： C07D487/04 , C07C59/76 , C07C69/738 , C07D249/04 , C07D401/12 , C07F9/6561
摘要： Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereof. The compounds are useful as antiallergic agents and exhibit excellent bioavailability. wherein R1 represents hydrogen, OH, alkyl or phenyl alkyl, R2, R3, R4, and R5 represent hydrogen, halogen, optionally protected hydroxyl, formyl, optionally substituted alkyl, alkenyl, alkoxy or the like, and Q represents a group selected from the following groups (i) to (iv), halogen, or alkoxy:
摘要翻译：提供了形式或前体药物的三环三唑并苯并吖嗪衍生物。根据本发明的化合物是由式（I）表示的化合物及其药理学上可接受的盐和溶剂化物。该化合物可用作抗过敏药物并且表现出优异的生物利用度。其中R1代表氢，OH，烷基或苯基烷基，R2，R3，R4和R5代表氢，卤素，任选保护的羟基，甲酰基，任选取代的烷基，烯基，烷氧基和Q表示选自以下组（i）至（iv）中的基团，卤素或烷氧基：

10. 发明申请

US20060074074A1 Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic agents 失效
标题翻译：三环三氮代氮杂吖庚因衍生物，其制备方法和抗过敏剂
公开(公告)号：US20060074074A1
公开(公告)日：2006-04-06
申请号：US11269828
申请日：2005-11-09
申请人： Yasuo Ohtsuka , Toshio Nishizuka , Sohjiro Shiokawa , Seiji Tsutsumi , Mami Kawaguchi , Hideo Kitagawa , Hiromi Takata , Takashi Shishikura , Toyoaki Ishikura , Kenichi Fushihara , Yumiko Okada , Sachiko Miyamoto , Maki Shiobara
发明人： Yasuo Ohtsuka , Toshio Nishizuka , Sohjiro Shiokawa , Seiji Tsutsumi , Mami Kawaguchi , Hideo Kitagawa , Hiromi Takata , Takashi Shishikura , Toyoaki Ishikura , Kenichi Fushihara , Yumiko Okada , Sachiko Miyamoto , Maki Shiobara
IPC分类号： A61K31/55 , C07D487/02 , C07D249/16
CPC分类号： C07D487/04 , C07C59/76 , C07C69/738 , C07D249/04 , C07D401/12 , C07F9/6561
摘要： Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereon. The compounds are useful as antiallergic agents and exhibit excellent bioavailability. wherein R1 represents hydrogen, OH, alkyl or phenyl alkyl, R2, R3, R4, and R5 represent hydrogen, halogen, optionally protected hydroxyl, formyl, optionally substituted alkyl, alkenyl, alkoxy or the like, and Q represents a group selected from the following groups (i) to (iv), halogen, or alkoxy:
摘要翻译：提供了形式或前体药物的三环三唑并苯并吖嗪衍生物。根据本发明的化合物是由式（I）表示的化合物及其上的药理学上可接受的盐和溶剂合物。这些化合物可用作抗过敏剂并且表现出优异的生物利用度。其中R 1表示氢，OH，烷基或苯基烷基，R 2，R 3，R 4，和R 5表示氢，卤素，任意保护的羟基，甲酰基，任选取代的烷基，烯基，烷氧基等，Q表示选自以下组（i）至（iv）中的基团，卤素或烷氧基：

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