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1. 发明授权

US5519139A Aminopyrimidine derivatives and their production and use 失效
标题翻译：氨基嘧啶衍生物及其生产和使用
公开(公告)号：US5519139A
公开(公告)日：1996-05-21
申请号：US448193
申请日：1995-05-23
申请人： Toshikazu Ohtsuka , Moriyasu Masui , Takami Takeda , Michio Masuko , Katsuaki Ohba
发明人： Toshikazu Ohtsuka , Moriyasu Masui , Takami Takeda , Michio Masuko , Katsuaki Ohba
IPC分类号： A01N43/54 , C07D239/42 , C07D239/46 , C07D405/12 , C07D239/30 , C07D239/34 , C07D401/04
CPC分类号： C07D239/42 , A01N43/54 , C07D239/47 , C07D405/12
摘要： There is disclosed a novel 4-aminopyrimidine derivative containing an optionally esterified carboxyl group at the 5-position which has potent fungicidal activity as well as insecticidal and miticidal activity. The compound is useful as agricultural fungicides, insecticides and miticides. There are also disclosed a process for producing the above compound and agricultural fungicidal, insecticidal and miticidal compositions
摘要翻译：公开了一种新的4-氨基嘧啶衍生物，其在5位含有任选酯化的羧基，其具有强的杀真菌活性以及杀虫和杀螨活性。该化合物可用作农业杀真菌剂，杀虫剂和杀螨剂。还公开了制备上述化合物和农业杀真菌剂，杀虫剂和杀螨剂组合物的方法

2. 发明授权

US5439911A Aminopyrimidine derivatives and their production and use 失效
标题翻译：氨基嘧啶衍生物及其生产和使用
公开(公告)号：US5439911A
公开(公告)日：1995-08-08
申请号：US168217
申请日：1993-12-17
申请人： Toshikazu Ohtsuka , Moriyasu Masui , Takami Takeda , Michio Masuko , Katsuaki Ohba
发明人： Toshikazu Ohtsuka , Moriyasu Masui , Takami Takeda , Michio Masuko , Katsuaki Ohba
IPC分类号： A01N43/54 , C07D239/42 , C07D239/46 , C07D405/12
CPC分类号： C07D239/42 , A01N43/54 , C07D239/47 , C07D405/12
摘要： There is disclosed a novel 4-aminopyrimidine derivative containing an optionally esterified carboxyl group at the 5-position which has potent fungicidal activity as well as insecticidal and miticidal activity. The compound is useful as agricultural fungicides, insecticides and miticides. There are also disclosed a process for producing the above compound and agricultural fungicidal, insecticidal and miticidal compositions.
摘要翻译：公开了一种新的4-氨基嘧啶衍生物，其在5位含有任选酯化的羧基，其具有强的杀真菌活性以及杀虫和杀螨活性。该化合物可用作农业杀真菌剂，杀虫剂和杀螨剂。还公开了制备上述化合物和农业杀真菌剂，杀虫剂和杀螨剂组合物的方法。

3. 发明申请

US20120022251A1 METHOD OF PRODUCING PYRONE AND PYRIDONE DERIVATIVES 有权
标题翻译：生产吡咯和吡咯烷酮衍生物的方法
公开(公告)号：US20120022251A1
公开(公告)日：2012-01-26
申请号：US13260063
申请日：2010-03-26
申请人： Yukihito Sumino , Kazuya Okamoto , Moriyasu Masui , Toshiyuki Akiyama
发明人： Yukihito Sumino , Kazuya Okamoto , Moriyasu Masui , Toshiyuki Akiyama
IPC分类号： C07D498/14 , C07D471/14 , C07D405/06 , C07D471/04 , C07D309/40 , C07D213/79
CPC分类号： C07D498/14 , C07D213/80 , C07D309/32 , C07D309/40 , C07D405/06 , C07D471/04 , C07D471/14
摘要： The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
摘要翻译：本发明提供了作为合成抗流感药物的新型中间体的吡喃酮衍生物和吡啶酮衍生物，其制造方法及其使用方法。

4. 发明申请

US20100240703A1 OXYIMINO COMPOUNDS AND THE USE THEREOF 有权
标题翻译： OXYIMINO化合物及其用途
公开(公告)号：US20100240703A1
公开(公告)日：2010-09-23
申请号：US12602441
申请日：2008-05-30
申请人： Moriyasu Masui , Hidenori Mikamiyama , Naoki Tsuno
发明人： Moriyasu Masui , Hidenori Mikamiyama , Naoki Tsuno
IPC分类号： A61K31/445 , C07D211/96 , A61P29/00 , A61P25/00 , A61P9/06 , A61P9/12 , G01N33/53
CPC分类号： C07D211/96
摘要： The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ═O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及（式I）的氧亚氨基化合物及其药学上可接受的盐，前药和溶剂化物，其中：Y是CO或SOm; Z是氢，每个任选取代的低级烷基，低级烯基，芳基，杂环基等.R 1和R 2各自独立地为氢，各自为任选取代的低级烷基，低级烯基，环烷基，芳基，杂环基等，各X独立地为= 任选取代的低级烷基，氰基，硝基等，m为1或2，p为O，1或2，q为O或1.本发明还涉及式I的用途化合物，以治疗，预防或改善对钙通道阻断，特别是N型钙通道的阻滞作用。本发明的化合物特别适用于治疗疼痛。

5. 发明授权

US06251949B1 Oxime derivatives, hydrazone derivatives and use thereof 失效
标题翻译：肟衍生物，腙衍生物及其用途
公开(公告)号：US06251949B1
公开(公告)日：2001-06-26
申请号：US09457672
申请日：1999-12-09
申请人： Moriyasu Masui , Norihiko Tanimoto , Kuniyoshi Nishida
发明人： Moriyasu Masui , Norihiko Tanimoto , Kuniyoshi Nishida
IPC分类号： A61K3115
CPC分类号： C07D213/30 , A01N37/50 , A01N41/06 , A01N41/10 , A01N43/40 , A01N43/46 , A01N43/80 , A01N47/16 , C07C251/36 , C07C251/48 , C07C251/52 , C07C251/54 , C07C251/74 , C07C259/06 , C07D207/12 , C07D211/42 , C07D211/46 , C07D211/58 , C07D211/72 , C07D243/08 , C07D261/02 , C07D295/185 , C07D295/26 , C07D333/16 , C07D401/12
摘要： Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof wherein R1 represents an optionally substituted aryl, an optionally substituted alkyl or the like; R2 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R3 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R4 and R5, which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R4 and R5 may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR6 wherein R6 represents a hydrogen atom, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted alkanoyl, or an optionally substituted aroyl; Z represents an oxygen atom or a sulfur atom; and a wavy line (˜) represents the configuration of an E isomer, a Z isomer, or a mixture thereof.
摘要翻译：具有杀真菌活性并由通式（I）表示的化合物及其盐和水合物，其中R 1表示任选取代的芳基，任选取代的烷基等; R 2表示任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的芳基，任选取代的杂环基等; R 3表示任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的芳基磺酰基，任选取代的杂环基团等; R 4和R 5可以相同或不同，表示氢原子，任选取代的烷基或任选取代的烷氧基，或者R 4和R 5可以与相邻的氮原子一起形成任选取代的单环或多环; X和Y可以相同或不同，表示每个氧原子或NR 6，其中R 6表示氢原子，任选取代的烷基，任选取代的芳基，任选取代的烷酰基或任选取代的芳酰基; Z表示氧原子或硫原子; 波浪线（〜）表示E异构体，Z异构体或其混合物的构型。

6. 发明申请

US20140051691A1 OXAZINE DERIVATIVES AND A PHARMACEUTICAL COMPOSITION FOR INHIBITING BACE1 CONTAINING THEM 有权
标题翻译：氧化衍生物和用于抑制含有它们的BACE1的药物组合物
公开(公告)号：US20140051691A1
公开(公告)日：2014-02-20
申请号：US14113327
申请日：2012-04-25
申请人： Moriyasu Masui , Yasunori Mitsuoka , Syuhei Yoshida , Ken-ichi Kusakabe , Naohiro Onodera , Noriyuki Kurose
发明人： Moriyasu Masui , Yasunori Mitsuoka , Syuhei Yoshida , Ken-ichi Kusakabe , Naohiro Onodera , Noriyuki Kurose
IPC分类号： C07D413/14 , C07D413/12
CPC分类号： C07D413/14 , C07D413/12
摘要： The present invention provides a compound of formula (I): wherein —X═ is —CR7═ or —N═, ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2 a and R2 b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, R5 is hydrogen, substituted or unsubstituted alkyl or the like, each R6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins.
摘要翻译：本发明提供式（I）化合物：其中-X =是-CR 7 =或-N =，环B是取代或未取代的碳环或取代或未取代的杂环，R 1是取代或未取代的烷基等， R2a和R2b各自独立地为氢，取代或未取代的烷基等，R3和R4各自独立地为氢，卤素，取代或未取代的烷基等，R5为氢，取代或未取代的烷基等，各R6 独立地为卤素，羟基，取代或未取代的烷基等，R 7为氢，卤素，羟基，取代或未取代的烷基等，p为0〜3的整数，或其药学上可接受的盐，抑制淀粉样蛋白β生成，特别是抑制BACE1的作用，并且其可用作由淀粉样蛋白β蛋白的产生，分泌和/或沉积诱导的疾病的治疗或预防剂。

7. 发明申请

US20120238557A1 AMINOTHIAZINE OR AMINOOXAZINE DERIVATIVE HAVING AMINO LINKER 审中-公开
标题翻译：氨基酸或具有氨基酸的氨基酸衍生物
公开(公告)号：US20120238557A1
公开(公告)日：2012-09-20
申请号：US13508899
申请日：2010-11-12
申请人： Moriyasu Masui , Kousuke Anan
发明人： Moriyasu Masui , Kousuke Anan
IPC分类号： A61K31/541 , C07D279/06 , A61P25/28 , C07D413/12 , A61K31/54 , A61K31/5355 , C07D417/12
CPC分类号： C07D413/12 , A61K9/0019 , A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2054 , C07D279/06 , C07D417/12
摘要： The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-β proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3, R4, R5, X, L1, L2, A, ring B and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
摘要翻译：本发明提供了用于治疗由淀粉样蛋白的生产，分泌或沉积诱导的疾病的药物。蛋白质，例如下述通式（I）的化合物，其中R1，R2a，R2b，R3，R4，R5，X，L1，L2，A，环B和虚线在说明书中定义，其药学上可接受的盐或其溶剂合物。

8. 发明授权

US5502252A Process of producing intermediates for use in production of alkoxyiminoacetamides and intermediates to be used therein 失效
公开(公告)号：US5502252A
公开(公告)日：1996-03-26
申请号：US339254
申请日：1994-11-10
申请人： Akira Takase , Hiroyuki Kai , Kuniyoshi Nishida , Moriyasu Masui
发明人： Akira Takase , Hiroyuki Kai , Kuniyoshi Nishida , Moriyasu Masui
IPC分类号： C07D215/12 , C07C51/58 , C07C59/84 , C07C59/88 , C07C59/90 , C07C227/02 , C07C229/42 , C07C231/02 , C07C233/56 , C07C235/72 , C07C235/78 , C07C237/20 , C07C249/08 , C07C319/12 , C07C319/20 , C07C323/62 , C07D215/20 , C07D215/36 , C07D239/26 , C07D239/34 , C07D239/38 , C07D239/42 , C07D261/08 , C07D261/10 , C07D261/12 , C07D261/14 , C07D263/32 , C07D263/36 , C07D263/46 , C07D263/48 , C07D263/56 , C07D263/58 , C07D277/62 , C07D303/38 , C07D413/04 , C07C233/05
CPC分类号： C07C59/84 , C07C231/02 , C07C249/08
摘要： There is disclosed a process of producing an .alpha.-ketamide as an intermediate for use in the production of various alkoxyiminoacetamide compounds which are useful as fungicides. Also disclosed is an intermediate to be used in this process.

9. 发明授权

US09018219B2 Fused aminodihydropyrimidine derivative 有权
标题翻译：熔融氨基二氢嘧啶衍生物
公开(公告)号：US09018219B2
公开(公告)日：2015-04-28
申请号：US13881112
申请日：2011-10-27
申请人： Moriyasu Masui , Genta Tadano
发明人： Moriyasu Masui , Genta Tadano
IPC分类号： A01N43/90 , A61K31/519 , C07D239/70 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2═X3 is CR5—CR6═CR7, N—CR6═CR7, CR5—N═CR7 or CR5—CR6═N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid β production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid β proteins.
摘要翻译：本发明例如提供以下化合物：其中环A为取代或未取代的碳环或取代或未取代的杂环，X1-X2 = X3为CR5-CR6 = CR7，N-CR6 = CR7，CR5-N = CR7或CR5-CR6 = N，R1是取代或未取代的烷基，取代或未取代的烯基等，R2a和R2b各自独立地为氢，取代或未取代的烷基等，R4a，R4b，R5，R6和R7各自为独立地是氢，卤素，羟基，取代或未取代的烷基等，其药学上可接受的盐或其溶剂合物具有抑制淀粉样蛋白的作用; 生产，特别是BACE1抑制活性，并且可用作治疗由淀粉样蛋白的生产，分泌或沉积诱导的疾病的药物。蛋白质。

10. 发明授权

US08895551B2 Acrylamide compounds and the use thereof 有权
标题翻译：丙烯酰胺化合物及其用途
公开(公告)号：US08895551B2
公开(公告)日：2014-11-25
申请号：US13260185
申请日：2010-04-02
申请人： Hidenori Mikamiyama , Akira Matsumura , Moriyasu Masui , Kosuke Anan , Kayoko Hata
发明人： Hidenori Mikamiyama , Akira Matsumura , Moriyasu Masui , Kosuke Anan , Kayoko Hata
IPC分类号： A61K31/5377 , C07D265/30 , A61K31/445 , C07D211/68 , C07D401/00 , C07D405/00 , C07D211/70 , C07D211/96
CPC分类号： C07D211/70 , C07D211/96
摘要： The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及下述式I的丙烯酰胺化合物。本发明还涉及使用式I化合物来治疗或预防对阻塞钙通道，特别是N型钙通道有响应的病症。本发明的化合物特别适用于治疗疼痛。

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