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71. 发明授权

US4902337A Herbicidal hydantoin derivatives 失效
标题翻译：除草剂乙内酰脲衍生物
公开(公告)号：US4902337A
公开(公告)日：1990-02-20
申请号：US92193
申请日：1987-09-02
申请人： Kenji Hirai , Takamasa Fuchikami , Atsuko Fujita , Hiroaki Hirose , Masahiro Yokota , Shoin Nagato
发明人： Kenji Hirai , Takamasa Fuchikami , Atsuko Fujita , Hiroaki Hirose , Masahiro Yokota , Shoin Nagato
IPC分类号： A01N43/50 , C07D233/96
CPC分类号： C07D233/96
摘要： Novel hydantoin derivative which is represented by the formula: ##STR1## (wherein X and Y represent a halogen atom, R.sup.1 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group or an alkynyl group, R.sup.2 represents a hydrogen atom, an alkyl group, an alkenyl group or an alkynyl group, and R.sup.3 and R.sup.4 independently represent a hydrogen atom or a lower alkyl group), and a herbicide containing said derivative as effective ingredient.This hydantoin derivative exhibit excellent weed-killing activity for harmful weeds and low phytotoxicity for crop plants.

72. 发明授权

US4699925A Biphenylylpropionic acid derivative and pharmaceutical composition containing the same 失效
标题翻译：联苯基丙酸衍生物和含有它们的药物组合物
公开(公告)号：US4699925A
公开(公告)日：1987-10-13
申请号：US531535
申请日：1983-09-12
申请人： Katsuhiro Uchida , Shozo Masumoto , Masao Tohno , Mitsuo Mimura , Makoto Okumura , Kiyonoshin Ichikawa , Misako Matsumura
发明人： Katsuhiro Uchida , Shozo Masumoto , Masao Tohno , Mitsuo Mimura , Makoto Okumura , Kiyonoshin Ichikawa , Misako Matsumura
IPC分类号： C07D307/33 , A61K31/22 , A01N37/10 , A61K31/23 , A61K31/235
CPC分类号： C07D307/33
摘要： Biphenylylpropionic acid derivatives of the formula: ##STR1## wherein R is an alkylcarbonyloxyalkyl group or an alkenylcarbonyloxyalkyl group having the formula: ##STR2## wherein R.sup.1 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 8 carbon atoms and m is 0 or an integer of 1. The compounds have excellent anti-inflammatory, analgesic and antipyretic activities. Moreover, the compounds have no irritation, rapid and long-acting, and high safety margin.
摘要翻译：其中R是烷基羰氧基烷基或具有下式的链烯基羰氧基烷基：其中R1是具有1至15个碳原子的烷基或具有2至8个碳原子的链烯基的双苯甲酰基丙酸衍生物和 m为0或整数1.化合物具有优异的抗炎，止痛和解热活性。此外，化合物无刺激，快速，长效，安全性高。

73. 发明授权

US4613505A Ester of flurbiprofen and emulsion containing the same 失效
标题翻译：氟比洛芬酯和含有相同的乳液
公开(公告)号：US4613505A
公开(公告)日：1986-09-23
申请号：US622244
申请日：1984-06-19
申请人： Yutaka Mizushima , Katsuhiro Uchida , Shozoh Masumoto , Masao Tohno , Yoshinobu Hashimoto , Kazumasa Yokoyama , Hiroyuki Okamoto , Kiichiro Nabeta , Tadakazu Suyama
发明人： Yutaka Mizushima , Katsuhiro Uchida , Shozoh Masumoto , Masao Tohno , Yoshinobu Hashimoto , Kazumasa Yokoyama , Hiroyuki Okamoto , Kiichiro Nabeta , Tadakazu Suyama
IPC分类号： A61K9/107 , A61K31/215 , A61K31/365 , A61P25/04 , A61P29/00 , C07D307/33 , A61K31/235 , A61K31/685
CPC分类号： A61K31/365 , A61K31/215 , A61K9/1075
摘要： There is provided a fat emulsion of an ester of flurbiprofen having the formula ##STR1## wherein R is a group of the formula ##STR2## wherein R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, R.sub.2 is a C.sub.1 -C.sub.15 alkyl group or a C.sub.2 -C.sub.8 alkenyl group, and m is zero or an integer of 1; or a lactone group of the formula ##STR3## wherein R.sub.3 and R.sub.4 are same as or different from each other and are a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, and n is an integer of 1 or 2.The emulsion containing particles of a vegetable oil dissolving the ester can be orally or parenterally administered to human or animal for analgesia, antiphlogosis and antipyresis in various diseases and exhibits a high activity with small amounts in terms of flurbiprofen as compared with flurbiprofen itself.
摘要翻译：提供了一种氟比洛芬的酯的脂肪乳剂，其具有式“IMAGE”，其中R是下式的基团：其中R 1是氢原子或C 1 -C 3烷基，R 2是C 1 -C 15烷基或C 2 -C 8烯基，m为0或1的整数; 或式“IMAGE”的内酯基团，其中R 3和R 4彼此相同或不同，为氢原子或C 1 -C 3烷基，n为1或2的整数。溶解酯的植物油可以口服或肠胃外给予人或动物用于各种疾病的镇痛，消炎和除血，并且与氟比洛芬本身相比，在氟比洛芬方面表现出较低的活性。

74. 发明授权

US4537999A Process for a production of dinitrophenyl ethers 失效
标题翻译：生产二硝基苯醚的方法
公开(公告)号：US4537999A
公开(公告)日：1985-08-27
申请号：US534145
申请日：1983-09-21
申请人： Tetsuya Ogawa , Shinichi Saitoh , Takeshi Inoi , Masaji Kato , Heitaro Obara
发明人： Tetsuya Ogawa , Shinichi Saitoh , Takeshi Inoi , Masaji Kato , Heitaro Obara
IPC分类号： C07C67/00 , C07C201/00 , C07C201/12 , C07C205/33 , C07C205/36 , C07C205/37 , C07C205/38 , C07C41/14 , C07C79/35
CPC分类号： C07C201/12
摘要： A process for the production of dinitrophenyl ethers having the general formula [III]: ##STR1## wherein, one of R.sub.1 and R.sub.2 is a nitro radical, and the other is a hydrogen atom or a straight-chain, branched-chain or cyclic, saturated or unsaturated hydrocarbon radical containing from 1 to 10 carbon atoms, and R.sub.3 is a radical selected from the group consisting of (i) a straight-chain, branched-chain or cyclic, saturated or unsaturated hydrocarbon radical containing from 2 to 10 carbon atoms, (ii) a straight-chain hydrocarbon radical having one phenyl group as a substituent and containing from 1 to 5 carbon atoms, (iii) a phenyl radical, and (iv) a phenyl radical with one or more than one substituents selected from the group consisting of a nitro group, a halogen group, a saturated or unsaturated hydrocarbon group containing from 1 to 5 carbon atoms and an alkoxy group containing from 1 to 4 carbon atoms, by reacting a compound represented by the formula [I]: ##STR2## wherein, R.sub.1 and R.sub.2 have the above-mentioned meanings, and a compound represented by the general formula [II]:R.sub.3 OH [II]wherein, R.sub.3 has the above-mentioned meaning, in the presence of an alkaline compound. This process has greater ease compared with the classical synthetic processes using a halogen compound intermediate.
摘要翻译：制备具有通式[III]的二硝基苯基醚的方法：其中，R1和R2之一是硝基，另一个是氢原子或直链，支链或环状的，含有1至10个碳原子的饱和或不饱和烃基，R 3是选自（i）含有2至10个碳原子的直链，支链或环状，饱和或不饱和烃基的基团，（ii）具有一个苯基作为取代基且含有1至5个碳原子的直链烃基，（iii）苯基，和（iv）具有一个或多于一个取代基的苯基，所述取代基选自通过使式[I]表示的化合物反应，由硝基，卤素基，含有1至5个碳原子的饱和或不饱和烃基和含有1至4个碳原子的烷氧基组成的基团： [I]其中，R1和R2 具有上述含义，和由通式[II]表示的化合物：R3OH [II]其中R3具有上述含义，在碱性化合物的存在下。与使用卤素化合物中间体的经典合成方法相比，该方法更容易。

75. 发明授权

US4532254A Inhibitor of aldose reductase 失效
标题翻译：醛糖还原酶抑制剂
公开(公告)号：US4532254A
公开(公告)日：1985-07-30
申请号：US476153
申请日：1983-03-17
申请人： Jun Okuda , Ichitomo Miwa , Kazuhiro Inagaki , Tokunaru Horie , Mitsuru Nakayama
发明人： Jun Okuda , Ichitomo Miwa , Kazuhiro Inagaki , Tokunaru Horie , Mitsuru Nakayama
IPC分类号： C07D311/30 , A61K31/35
CPC分类号： C07D311/30 , Y10S514/866
摘要： An inhibitor of aldose reductase which contains, as the effective ingredient, a flavone derivative having the following formula: ##STR1## wherein R.sub.1 is hydrogen atom or hydroxyl group, R.sub.2 is hydroxyl group or methoxyl group or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The inhibitor is useful for preventing, reducing or treating complications of diabetes.
摘要翻译：含有作为有效成分的具有下式的黄酮衍生物的醛糖还原酶抑制剂：其中R 1是氢原子或羟基，R 2是羟基或甲氧基或其药学上可接受的盐，和药学上可接受的盐可接受的载体该抑制剂可用于预防，减少或治疗糖尿病并发症。

76. 发明授权

US4515977A Process for preparing optically active [S]-2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran and salts thereof 失效
标题翻译：制备光学活性的[S] -2-乙酰基-7-（2-羟基-3-异丙基氨基丙氧基）苯并呋喃及其盐的方法
公开(公告)号：US4515977A
公开(公告)日：1985-05-07
申请号：US475925
申请日：1983-03-16
申请人： Jun Nakano , Teruo Nakanishi , Kazuhiko Kimura
发明人： Jun Nakano , Teruo Nakanishi , Kazuhiko Kimura
IPC分类号： C07D301/02 , C07D307/86 , C07D407/12
CPC分类号： C07D407/12 , C07D301/02 , C07D307/86
摘要： [S]-(+)-2-acetyl-7-(2,3-epoxypropoxy)benzofuran (SEBF) is prepared by subjecting 2-acetyl-7-hydroxybenzofuran and [R]-glycidol to dehydration condensation in an inert organic solvent in the presence of triphenylphosphine and a dialkyl azodicarboxylate. The [S]-(+)-2-acetyl-7-(2,3-epoxypropoxy)benzofuran can be easily converted into [S]-2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran ([S]-befunolol) or salts thereof which are useful as a .beta.-adrenergic blocking agent, by reacting it with isopropylamine.
摘要翻译：通过使2-乙酰基-7-羟基苯并呋喃和[R] - 缩水甘油在惰性有机溶剂中脱水缩合制备[S] - （+） - 2-乙酰基-7-（2,3-环氧丙氧基）苯并呋喃（SEBF）在三苯基膦和偶氮二羧酸二烷基酯存在下。 [S] - （+） - 2-乙酰基-7-（2,3-环氧丙氧基）苯并呋喃可以容易地转化为[S] -2-乙酰基-7-（2-羟基-3-异丙基氨基丙氧基）苯并呋喃（[ S] - 非诺洛尔）或其盐，其可用作β-肾上腺素能阻断剂，通过与异丙胺反应。

77. 发明授权

US4460576A Peptide and hormone agent containing the same as effective ingredient 失效
标题翻译：含有与有效成分相同的肽和激素剂
公开(公告)号：US4460576A
公开(公告)日：1984-07-17
申请号：US463604
申请日：1983-02-03
申请人： Hiroshi Kawauchi
发明人： Hiroshi Kawauchi
IPC分类号： A61K38/00 , A61K38/04 , C07K7/08 , C07K14/575 , C07K14/60 , C07C103/52 , A61K37/02
CPC分类号： C07K7/08 , C07K14/60 , A61K38/00 , Y10S930/12 , Y10S930/26
摘要： A peptide having the structural formula (I): ##STR1## wherein Glx is Glu or Gln, and the following physical properties: (1) Ultraviolet Absorption Spectrum: Max 280 nm.,(2) Ehrlich reaction, Sakaguchi reaction and Pauly's reaction: positive,(3) Basic,(4) Soluble in water, methanol and acetic acid, slightly soluble in ethyl acetate, butyl acetate, ethyl ether, hexane, petroleum ether, benzene and chloroform, and(5) white powderhas a specifically GH-releasing effect and no species-specificity.The peptide is useful not only for human dwarfism and wound repair but also for stimulating a growth of domestic animal.
摘要翻译：具有结构式（I）的肽：其中Glx是Glu或Gln，以及以下物理性质：（1）紫外线吸收光谱：最大280nm，（2）Ehrlich反应，Sakaguchi反应和（3）碱性，（4）溶于水，甲醇和乙酸，微溶于乙酸乙酯，乙酸丁酯，乙醚，己烷，石油醚，苯和氯仿，（5）白色粉末特别是GH释放作用，没有物种特异性。该肽不仅用于人类侏儒症和伤口修复，而且用于刺激家畜的生长。

78. 发明授权

US4440749A Preventive and treating agent for blood lipids abnormality and/or arteriosclerosis 失效
标题翻译：血脂异常和/或动脉硬化的预防和治疗剂
公开(公告)号：US4440749A
公开(公告)日：1984-04-03
申请号：US484313
申请日：1983-04-12
申请人： Shigemi Fujisaki , Takashi Fujisaki , Junichi Yoshida , Yasuhiro Fujisaki
发明人： Shigemi Fujisaki , Takashi Fujisaki , Junichi Yoshida , Yasuhiro Fujisaki
IPC分类号： A61K38/46 , A61K9/50 , A61K38/48 , A61P3/06 , A61P9/10 , A61K37/48
CPC分类号： A61K38/482 , A61K38/4886 , A61K9/5042 , C12Y304/2404
摘要： A preventive and treating agent for blood lipids abnormally and/or arteriosclerosis comprises a proteolytic enzyme as an effective ingredient.
摘要翻译：用于血脂异常和/或动脉硬化的预防和治疗剂包括蛋白水解酶作为有效成分。

79. 发明申请

US20210395197A1 CRYSTALLINE FORM OF SOFPIRONIUM BROMIDE AND PREPARATION METHOD THEREOF 有权
公开(公告)号：US20210395197A1
公开(公告)日：2021-12-23
申请号：US17364445
申请日：2021-06-30
申请人： Kaken Pharmaceutical Co., Ltd. , Brickell Biotech, Inc.
发明人： Kazuyoshi MARUBAYASHI , Masahito WATANABE , Herbert R. BRINKMAN
IPC分类号： C07D207/12 , A61K9/00 , C07C59/147
摘要： A cocrystal containing the 1′R-diastereomer and the 1′S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1′R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.

80. 发明申请

US20210291211A1 AIRLESS CONTAINER 有权
公开(公告)号：US20210291211A1
公开(公告)日：2021-09-23
申请号：US17264764
申请日：2018-09-03
申请人： KAKEN PHARMACEUTICAL CO., LTD. , KITANO CO., LTD.
发明人： Katsunori SHIMAKURA , Masayoshi TAKAOKA , Tatsuro NAGAO
IPC分类号： B05B11/00
摘要： An airless container includes a cylindrical container body storing a contained material, which is a fluid, in an airtight state, and a pump attached to an upper edge portion of the container body and configured to externally discharge the contained material. The airless container further includes a bottom lid that closes a lower opening portion of a container bottom portion of the container body, and a piston in the container body between the pump and the bottom lid, which is slidable in the container body in an airtight state. The piston includes a flexible piece that is deformable in a portion that comes into contact with the bottom lid. The flexible piece is deformable against the sliding of the piston toward the bottom lid.

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