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1. 发明授权

US06468992B1 Phosphonic acid diester derivatives 失效
标题翻译：膦酸二酯衍生物
公开(公告)号：US06468992B1
公开(公告)日：2002-10-22
申请号：US09674145
申请日：2000-12-13
申请人： Yasuhiro Sakai , Kazuyoshi Miyata , Kenichi Kawamura , Yoshihiko Tsuda , Yasuhide Inoue
发明人： Yasuhiro Sakai , Kazuyoshi Miyata , Kenichi Kawamura , Yoshihiko Tsuda , Yasuhide Inoue
IPC分类号： C07F940
CPC分类号： C07F9/4065 , C07F9/4006 , C07F9/58 , C07F9/650952
摘要： The present invention provides novel phosphonic acid diester derivatives useful as medicines. The phosphonic acid diester derivatives are represented by the general formula: wherein R1 represents amino group, N-lower alkylamino group, N-lower alkenylamino group, or the like; R2 and R3 represent hydrogen atom, lower alkyl group, halogen atom, lower alkoxy group, or the like; R4 represents hydrogen atom, lower alkyl group or phenyl(lower)alkyl group; R5 and R6 represent lower alkyl group; X, Y and Z represent that all of them are carbon atoms or one of them is nitrogen atom and the other two are carbon atoms; Q represents a single bond or alkylene group; or the pharmacologically acceptable salts thereof.
摘要翻译：本发明提供了可用作药物的新型膦酸二酯衍生物。膦酸二酯衍生物由以下通式表示：其中R1表示氨基，N-低级烷基氨基，N-低级链烯基氨基等; R2和R3表示氢原子，低级烷基，卤素原子，低级烷氧基等; R4表示氢原子，低级烷基或苯基（低级）烷基; R5和R6表示低级烷基; X，Y和Z表示全部为碳原子或其中一个为氮原子，另外两个是碳原子; Q表示单键或亚烷基;或其药理学上可接受的盐。

2. 发明申请

US20050256087A1 Phosphonic acid diester compounds 失效
标题翻译：膦酸二酯化合物
公开(公告)号：US20050256087A1
公开(公告)日：2005-11-17
申请号：US10838297
申请日：2004-05-05
申请人： Yasuhiro Sakai , Kazuyoshi Miyata , Takahiro Tomoyasu , Akiyoshi Kuroda , Yasuhide Inoue , Akifumi Hagi , Shinya Miki , Norihiro Yoshinaga , Masako Doi , Yoshihiko Tsuda , Seiichirou Kanou
发明人： Yasuhiro Sakai , Kazuyoshi Miyata , Takahiro Tomoyasu , Akiyoshi Kuroda , Yasuhide Inoue , Akifumi Hagi , Shinya Miki , Norihiro Yoshinaga , Masako Doi , Yoshihiko Tsuda , Seiichirou Kanou
IPC分类号： A61K31/675 , C07F9/6506 , C07F9/6509 , C07F9/6558
CPC分类号： C07F9/65586 , C07F9/65068 , C07F9/65583
摘要： The present invention provides a phosphonic acid diester compound represented by General Formula wherein R1, R2, R3 and R4 are the same or different, and represent hydrogen, halogen, lower alkyl or lower alkoxy; R5 is phenyl having on the phenyl ring 1-3 substituents selected from the group consisting of lower alkyl, halogen-substituted lower alkyl, lower alkoxy, halogen-substituted lower alkoxy, phenoxy, benzyloxy, hydroxyl, halogen, nitro, lower alkylthio, di(lower alkyl)amino, lower alkanolyamino, pyrrolidinyl and phenyl, or the like, provided that R5 is not mono(lower alkoxy)pheny; and R6 is lower alkyl; and an ACAT-1 inhibitor containing the compound as an active ingredient.
摘要翻译：本发明提供由通式其中R 1，R 2，R 3和R 4代表的膦酸二酯化合物， / SUB>相同或不同，代表氢，卤素，低级烷基或低级烷氧基; R 5是在苯环上具有1-3个选自低级烷基，卤素取代的低级烷基，低级烷氧基，卤素取代的低级烷氧基，苯氧基，苄氧基，羟基，卤素，硝基，低级烷硫基，二（低级烷基）氨基，低级链烷氨基，吡咯烷基和苯基等，条件是R 5不是单（低级烷氧基）苯基; 和R 6是低级烷基; 和含有该化合物作为活性成分的ACAT-1抑制剂。

3. 发明授权

US5985858A Phosphonic diester derivatives 失效
标题翻译：膦酸二酯衍生物
公开(公告)号：US5985858A
公开(公告)日：1999-11-16
申请号：US91946
申请日：1998-06-26
申请人： Kazuyoshi Miyata , Yasuhiro Sakai , Yasuo Shoji , Yoshihiko Tsuda , Yasuhide Inoue , Keigo Sato , Shinya Miki
发明人： Kazuyoshi Miyata , Yasuhiro Sakai , Yasuo Shoji , Yoshihiko Tsuda , Yasuhide Inoue , Keigo Sato , Shinya Miki
IPC分类号： C07F9/6509 , C07F9/6539 , C07F9/6553 , C07F9/6558 , C07F9/6561 , A61K31/67 , A61K31/675
CPC分类号： C07F9/650964 , C07F9/6539 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要： A phosphonic diester derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group, a lower alkyl group, a halogen atom, a halogen-substituted lower alkyl group, a lower alkanoyl group, a nitro group, a benzoyl group, a cyano group, an N-lower alkylcarbamoyl group, an N-phenyl-lower alkylcarbamoyl group, an N-(halogen-substituted phenyl)carbamoyl group and an N,N-di-lower alkylcarbamoyl group; a 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group as a substituent; a thiazolyl group; a pyridyl group which may be substituted by a halogen atom; a benzothiazol-2-yl group having 1 to 2 lower alkoxy groups on the phenyl ring; or a 4,5-dihydrothieno[3,2-e]benzothiazol-2-yl group; R.sup.2 represents a hydrogen atom or a phenyl lower alkyl group; R.sup.3 and R.sup.4 each represents a lower alkyl group; and A represents a heterocyclic ring selected from the group consisting of a pyrazine ring, a thiophene ring and a phenyl-substituted thiazole ring; the derivative being of value as an agent for treating and preventing hyperlipidemia, diabetes and cataract, or as an antitumor agent.
摘要翻译： PCT No.PCT / JP96 / 03775第 371日期：1998年6月26日 102（e）日期1998年6月26日PCT 1996年12月24日PCT公布。公开号WO97 / 24360 PCT 日期：1997年7月10日由下式（1）表示的膦酸二酯衍生物：其中R1表示环烷基; 可以具有1〜3个选自低级烷氧基，低级烷基，卤素原子，卤素取代的低级烷基，低级烷酰基，硝基，苯甲酰基的取代基的苯基，氰基，N-低级烷基氨基甲酰基，N-苯基 - 低级烷基氨基甲酰基，N-（卤素取代的苯基）氨基甲酰基和N，N-二低级烷基氨基甲酰基; 具有卤素取代的低级烷基作为取代基的1,3,4-噻二唑-2-基; 噻唑基可被卤素原子取代的吡啶基; 在苯环上具有1至2个低级烷氧基的苯并噻唑-2-基; 或4,5-二氢噻吩并[3,2-e]苯并噻唑-2-基; R2表示氢原子或苯基低级烷基; R3和R4各自表示低级烷基; A表示选自吡嗪环，噻吩环和苯基取代的噻唑环的杂环; 该衍生物作为治疗和预防高脂血症，糖尿病和白内障或作为抗肿瘤剂的药剂是有价值的。

4. 发明授权

US07259155B2 Phosphonic diester derivatives 失效
标题翻译：膦酸二酯衍生物
公开(公告)号：US07259155B2
公开(公告)日：2007-08-21
申请号：US10838297
申请日：2004-05-05
申请人： Yasuhiro Sakai , Kazuyoshi Miyata , Takahiro Tomoyasu , Akiyoshi Kuroda , Yasuhide Inoue , Akifumi Hagi , Shinya Miki , Norihiro Yoshinaga , Masako Doi , Yoshihiko Tsuda , Seiichirou Kanou
发明人： Yasuhiro Sakai , Kazuyoshi Miyata , Takahiro Tomoyasu , Akiyoshi Kuroda , Yasuhide Inoue , Akifumi Hagi , Shinya Miki , Norihiro Yoshinaga , Masako Doi , Yoshihiko Tsuda , Seiichirou Kanou
IPC分类号： A61K31/517 , A61K31/675 , A01N43/54 , C07D239/72 , C07D265/32 , C07D413/00 , C07F9/02 , C07D401/00 , C07D403/02 , C07F9/28 , C07F9/547
CPC分类号： C07F9/65586 , C07F9/65068 , C07F9/65583
摘要： The present invention provides a phosphonic acid diester compound represented by General Formula wherein R1, R2, R3 and R4 are the same or different, and represent hydrogen, halogen, lower alkyl or lower alkoxy; R5 is phenyl having on the phenyl ring 1–3 substituents selected from the group consisting of lower alkyl, halogen-substituted lower alkyl, lower alkoxy, halogen-substituted lower alkoxy, phenoxy, benzyloxy, hydroxyl, halogen, nitro, lower alkylthio, di(lower alkyl)amino, lower alkanolyamino, pyrrolidinyl and phenyl, or the like, provided that R5 is not mono(lower alkoxy)pheny; and R6 is lower alkyl; and an ACAT-1 inhibitor containing the compound as an active ingredient.
摘要翻译：本发明提供由通式其中R 1，R 2，R 3和R 4代表的膦酸二酯化合物， / SUB>相同或不同，代表氢，卤素，低级烷基或低级烷氧基; R 5是在苯环上具有1-3个选自低级烷基，卤素取代的低级烷基，低级烷氧基，卤素取代的低级烷氧基，苯氧基，苄氧基，羟基，卤素，硝基，低级烷硫基，二（低级烷基）氨基，低级链烷氨基，吡咯烷基和苯基等，条件是R 5不是单（低级烷氧基）苯基; 和R 6是低级烷基; 和含有该化合物作为活性成分的ACAT-1抑制剂。

5. 发明授权

US5376665A Phosphonic diester derivatives 失效
标题翻译：膦酸二酯衍生物
公开(公告)号：US5376665A
公开(公告)日：1994-12-27
申请号：US182145
申请日：1994-01-14
申请人： Kazuyoshi Miyata , Yasuo Shoji , Yoshihiko Tsuda , Kazuhiko Tsutsumi , Yasuhide Inoue , Chieko Naba , Yasuhisa Kurogi
发明人： Kazuyoshi Miyata , Yasuo Shoji , Yoshihiko Tsuda , Kazuhiko Tsutsumi , Yasuhide Inoue , Chieko Naba , Yasuhisa Kurogi
IPC分类号： A61K31/675 , C07F9/6506 , C07F9/653 , C07F9/6541 , C07F9/6561 , C07D235/04 , A61K31/415 , A61K31/44 , C07D221/04
CPC分类号： C07F9/6561 , C07F9/65068 , C07F9/65324 , C07F9/6541
摘要： The invention provides a phosphonic diester derivative of the general formula ##STR1## The phosphonic diester derivative of the invention has hypoglycemic and hypolipidemic activities, for instance, and is of value as an antidiabetic or anti-hyperlipidemic agent.

6. 发明授权

US5798344A Phosphonic ester derivatives of quinazolinones 失效
标题翻译：喹唑啉酮的膦酸酯衍生物
公开(公告)号：US5798344A
公开(公告)日：1998-08-25
申请号：US704740
申请日：1996-09-05
申请人： Yasuhisa Kuroki , Kazuyoshi Miyata , Yoshihiko Tsuda , Yasuhide Inoue , Jun Kanaya , Keigo Sato
发明人： Yasuhisa Kuroki , Kazuyoshi Miyata , Yoshihiko Tsuda , Yasuhide Inoue , Jun Kanaya , Keigo Sato
IPC分类号： C07F9/6512 , A61K31/675
CPC分类号： C07F9/65128
摘要： The invention provides a phosphonic diester derivative of the formula: ##STR1## wherein R.sup.1 -R.sup.7 are substituent groups, as defined in the specification. The derivatives according to the invention are useful as therapeutic or preventive compositions for hyperlipidemia, hypertension, and diabetes.
摘要翻译： PCT No.PCT / JP95 / 00303 Sec。 371日期：1996年9月5日 102（e）1996年9月5日PCT提交1995年2月27日PCT公布。第WO95 / 24410BC号公报日期1995年9月14日本发明提供下式的膦酸二酯衍生物：其中R 1 -R 7是如说明书中所定义的取代基。根据本发明的衍生物可用作高脂血症，高血压和糖尿病的治疗或预防组合物。

7. 发明授权

US5624918A Phosphonic diester derivatives 失效
标题翻译：膦酸二酯衍生物
公开(公告)号：US5624918A
公开(公告)日：1997-04-29
申请号：US387907
申请日：1995-02-05
申请人： Yasuhisa Kurogi , Kazuyoshi Miyata , Shizuo Nakamura , Mitsuyoshi Kondo , Takeshi Iwamoto , Chieko Naba , Yoshihiko Tsuda , Yasuhide Inoue , Jun Kanaya , Keigo Sato
发明人： Yasuhisa Kurogi , Kazuyoshi Miyata , Shizuo Nakamura , Mitsuyoshi Kondo , Takeshi Iwamoto , Chieko Naba , Yoshihiko Tsuda , Yasuhide Inoue , Jun Kanaya , Keigo Sato
IPC分类号： C07F9/6512 , C07F9/6558 , A61K31/675
CPC分类号： C07F9/65583 , C07F9/65128
摘要： The present invention provides a phosphonic diester derivative of the following general formula (1): ##STR1## wherein A represents an oxygen atom or a sulfur atom; R.sup.1, R.sup.2, R.sup.9 and R.sup.10 are the same or different and they each represent a hydrogen atom, a lower alkoxy group, a nitro group, a lower alkyl group, a halogen-substituted lower alkyl group or a halogen atom; R.sup.3 represents a phenyl group, --B--R.sup.6 (wherein B represents an oxygen atom or a sulfur atom and R.sup.6 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, a phenyl group, a phenyl(lower)alkyl group optionally having a halogen atom as a substituent on the phenyl ring, a phenoxy(lower)alkyl group, a lower alkoxycarbonyl(lower)alkyl group, a carboxy(lower)alkyl group or a lower alkenyl group) or --NR.sup.7 R.sup.8 (wherein R.sup.7 and R.sup.8 and are the same or different and they each represent a hydrogen atom, a lower alkyl group, an amino group or a cycloalkyl group or combinedly represent a lower alkylene group); and R.sup.4 and R.sup.5 are the same or different and they each represent a hydrogen atom or a lower alkyl group.The derivative of the present invention is useful as therapeutic agents for hyperlipidemic diseases, hypertension, diabetes and the like.
摘要翻译： PCT No.PCT / JP94 / 00883 Sec。 371日期1995年2月15日 102（e）1995年2月15日PCT PCT 1994年5月31日PCT公布。公开号WO95 / 00524 日本1995年1月5日本发明提供下述通式（1）的膦酸二酯衍生物：其中A表示氧原子或硫原子; R 1，R 2，R 9和R 10相同或不同，它们各自表示氢原子，低级烷氧基，硝基，低级烷基，卤素取代的低级烷基或卤素原子; R3表示苯基-B-R6（其中B表示氧原子或硫原子，R6表示氢原子，低级烷基，环烷基，苯基，苯基（低级）烷基，任选具有苯基环上的取代基的卤原子，苯氧基（低级）烷基，低级烷氧基羰基（低级）烷基，羧基（低级）烷基或低级烯基）或-NR7R8（其中R7和R8和它们各自表示氢原子，低级烷基，氨基或环烷基，或者组合表示低级亚烷基）。 R 4和R 5相同或不同，它们各自表示氢原子或低级烷基。本发明的衍生物可用作高脂血症，高血压，糖尿病等的治疗剂。

8. 发明授权

US5922866A Process for preparing quinazolin-4-one derivatives 失效
标题翻译：喹唑啉-4-酮衍生物的制备方法
公开(公告)号：US5922866A
公开(公告)日：1999-07-13
申请号：US11826
申请日：1998-02-25
申请人： Kazuyoshi Miyata , Yasuhisa Kurogi , Yasuhiro Sakai , Yoshihiko Tsuda
发明人： Kazuyoshi Miyata , Yasuhisa Kurogi , Yasuhiro Sakai , Yoshihiko Tsuda
IPC分类号： C07D239/90 , C07D239/91 , C07F9/6512 , C07F9/32 , C07F9/40 , C07D239/96
CPC分类号： C07D239/91 , C07D239/90 , C07F9/65122 , C07F9/65127 , C07F9/65128
摘要： The present invention provides a novel process for preparing a series of quinazolin-4-one derivatives in high yields with reduced amounts of byproducts, the process comprising reacting, in the presence of a base, a trialkylsilyl halide with a compound represented by the formula ##STR1## wherein; R.sup.5 is a phenyl group which may have 1 to 3 substituents each selected from a lower alkyl group, a lower alkoxy group or a halogen atom, a lower alkyl group, a phenyl-lower alkyl group which may have a halogen atom as a substituent on the phenyl ring, a lower alkenyl group, a lower alkoxy-lower alkyl group or a lower alkynyl group; R.sup.6 is a lower alkyl group, a halogen-substituted lower alkyl group, a lower alkoxycarbonyl group or a phenyl group which may have, as a substituent, a lower alkyl group or a group of the formula ##STR2## wherein A is an oxygen atom or a single bond, Z is a lower alkylene group, R.sup.7 is a lower alkyl group and R.sup.8 is a lower alkoxy group, a phenyl group or a phenyl-lower alkoxy group which may have a halogen atom on the phenyl ring;to produce the quinazolin-4-one derivatives which is valuable as pharmaceuticals or intermediates for synthesis thereof and represented by the formula ##STR3## wherein R.sup.1,R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as defined above.
摘要翻译： PCT No.PCT / JP96 / 02388 Sec。 371日期：1998年2月25日 102（e）1998年2月25日PCT PCT 1996年8月26日PCT公布。公开号WO97 / 08153 日期1997年3月6日本发明提供了一种制备一系列具有降低量副产物的喹唑啉-4-酮衍生物的新方法，该方法包括在碱存在下使三烷基甲硅烷基卤化物与化合物由下式表示： R5是可以具有1〜3个选自低级烷基，低级烷氧基或卤素原子的取代基的苯基，低级烷基，可具有卤素原子作为取代基的苯基 - 低级烷基苯环，低级烯基，低级烷氧基 - 低级烷基或低级炔基; R6是低级烷基，卤素取代的低级烷基，低级烷氧基羰基或苯基，其可以具有低级烷基或下式基团的取代基：其中A是氧原子或单键，Z为低级亚烷基，R7为低级烷基，R8为低级烷氧基，苯基或在苯环上可具有卤素原子的苯基 - 低级烷氧基; 以产生作为药物或其合成中间体而有价值的喹唑啉-4-酮衍生物，由下式表示，其中R 1，R 2，R 3，R 4，R 5和R 6如上所定义。

9. 发明授权

US5527786A Phosphonic diester derivatives 失效
标题翻译：膦酸二酯衍生物
公开(公告)号：US5527786A
公开(公告)日：1996-06-18
申请号：US424345
申请日：1995-04-19
申请人： Kazuyoshi Miyata , Yasuhisa Kurogi , Yoshihiko Tsuda , Kazuhiko Tsutsumi , Takeshi Iwamoto , Chieko Naba
发明人： Kazuyoshi Miyata , Yasuhisa Kurogi , Yoshihiko Tsuda , Kazuhiko Tsutsumi , Takeshi Iwamoto , Chieko Naba
IPC分类号： C07F9/655 , A61K31/675 , A61K31/665 , C07F9/28
CPC分类号： C07F9/65522
摘要： The present invention provides a phosphonic diester derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and they each represent a hydrogen atom, a lower alkyl group, a halogen atom, a cyano group, a hydroxyl group, or a lower alkoxy group optionally having a halogen atom, a phenyl group or a hydroxypiperidino group as a substituent; R.sup.4 represents a hydrogen atom, a lower alkoxy group, a halogen atom, or a lower alkyl group optionally having a halogen atom or a cyano group as a substituent; and R.sup.5 and R.sup.6 are the same or different and they each represent a hydrogen atom or a lower alkyl group.The derivative of the present invention has excellent hypolipidemic, vasodepressor and hypoglycemic activities and is useful as therapeutic and preventive agents for hyperlipidemic diseases, hypertension and diabetes.
摘要翻译： PCT No.PCT / JP94 / 01307 Sec。 371日期1995年04月19日 102（e）1995年4月19日PCT PCT 1994年8月8日PCT公布。出版物WO95 / 06051 日本3月2日公开本发明提供下式的膦酸二酯衍生物：其中R 1，R 2和R 3相同或不同，它们各自表示氢原子，低级烷基，卤素原子，氰基，羟基或任选具有卤素原子的低级烷氧基，苯基或羟基哌啶子基作为取代基; R4表示氢原子，低级烷氧基，卤素原子或任选具有卤素原子或氰基作为取代基的低级烷基; R 5和R 6相同或不同，它们各自表示氢原子或低级烷基。本发明的衍生物具有优异的降血脂，血管抑制剂和降血糖活性，可用作高脂血症和高血压病和糖尿病的治疗和预防剂。

10. 发明申请

US20070041866A1 Aqueous solution of olanexidine, method of preparing the aqueous solution, and disinfectant 有权
标题翻译：奥兰西汀的水溶液，水溶液的制备方法和消毒剂
公开(公告)号：US20070041866A1
公开(公告)日：2007-02-22
申请号：US11588395
申请日：2006-10-27
申请人： Kazuyoshi Miyata , Yasuhide Inoue , Akifumi Hagi , Motoya Kikuchi , Hitoshi Ohno , Kinji Hashimoto , Kinue Ohguro , Tetsuya Sato , Hidetsugu Tsubouchi , Hiroshi Ishikawa , Takashi Okamura , Koushi Iwata
发明人： Kazuyoshi Miyata , Yasuhide Inoue , Akifumi Hagi , Motoya Kikuchi , Hitoshi Ohno , Kinji Hashimoto , Kinue Ohguro , Tetsuya Sato , Hidetsugu Tsubouchi , Hiroshi Ishikawa , Takashi Okamura , Koushi Iwata
IPC分类号： A61L2/18 , A01N37/52
CPC分类号： A61K9/0014 , A01N47/44 , A61K31/155 , A61K31/191 , A61K31/522 , A61K45/06 , A61K47/12 , A61L2/18 , A01N37/36 , A01N25/32 , A01N2300/00 , A61K2300/00
摘要： The present invention provides a disinfectant that contains olanexidine in a concentration sufficient to exhibit an effective bactericidal effect, and that has hardly any side effects such as skin irritation. Specifically, the present invention provides a disinfectant containing an aqueous solution that contains olanexidine and at least an equimolar amount of gluconic acid, and substantially contains neither an acid other than gluconic acid nor a salt of the acid other than gluconic acid.
摘要翻译：本发明提供一种消毒剂，其含有浓度足以显示出有效杀菌作用的奥拉西丁，并且几乎没有任何副作用，例如皮肤刺激。具体而言，本发明提供一种含有含有奥拉西丁和至少等摩尔量葡萄糖酸的水溶液的消毒剂，除了葡萄糖酸以外，基本上既不含葡萄糖酸以外的酸也不含有酸。

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