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1. 发明申请

US20070099986A1 Preventives/remedies for urinary disturbance 审中-公开
标题翻译：预防/治疗尿路障碍
公开(公告)号：US20070099986A1
公开(公告)日：2007-05-03
申请号：US11589903
申请日：2006-10-31
申请人： Yuji Ishichi , Koichi Iwanaga , Tomomi Ikemoto , Hiroaki Yamamoto , Shokyo Miki
发明人： Yuji Ishichi , Koichi Iwanaga , Tomomi Ikemoto , Hiroaki Yamamoto , Shokyo Miki
IPC分类号： A61K31/343 , A61K31/36 , C07D319/14 , A61K31/18 , C07C311/18
CPC分类号： C07C311/37 , C07C45/46 , C07C49/813 , C07C2602/08 , C07D307/79 , C07D319/18 , C07D405/04
摘要： A compound represented by the formula: wherein Ar represents a group represented by the formula: (wherein Y represents methylene or an oxygen atom, R1 represents aminosulfonyl, C1-6 alkylaminosulfonyl, C1-6 alkylcarbonylamino or C1-6 alkylsulfonylamino, R2 represents a hydrogen atom or C1-6 alkyl, R3 represents C1-6 alkyl, and R4 represents a hydrogen atom or C1-6 alkyl); X represents a carbonyl group, or a methylene group which may be substituted with a hydroxy group; and L represents an optionally substituted C4-5 alkylene group, or a salt thereof is provided.
摘要翻译：由下式表示的化合物：其中Ar表示由下式表示的基团：其中Y表示亚甲基或氧原子，R 1表示氨基磺酰基，C 1-6烷基，烷基氨基磺酰基，C 1-6烷基羰基氨基或C 1-6烷基磺酰基氨基，R 2表示氢原子或C 1-6 - / SUB烷基，R 3表示C 1-6烷基，R 4表示氢原子或C 1-6 烷基）; X表示羰基或可被羟基取代的亚甲基; L表示任意取代的C 4〜5亚烷基，或其盐。

2. 发明授权

US06849738B2 Processes for the production of thienopyrimidine derivatives 失效
标题翻译：噻吩并嘧啶衍生物的制备方法
公开(公告)号：US06849738B2
公开(公告)日：2005-02-01
申请号：US10220233
申请日：2001-02-27
申请人： Koichiro Fukuoka , Hiroaki Yamamoto , Kazuhiro Kimura , Junichi Kawakami , Shokyo Miki
发明人： Koichiro Fukuoka , Hiroaki Yamamoto , Kazuhiro Kimura , Junichi Kawakami , Shokyo Miki
IPC分类号： C07D333/38 , C07D495/04
CPC分类号： C07D495/04 , C07D333/38
摘要： The present invention provides a process for producing an intermediate for thienopyrimidine derivatives having the GnRH antagonistic activity at an industrial large scale.The process for production of the present invention relates to a process for producing a compound represented by the formula (III): wherein respective symbols have the same meanings as those described below, or a salt thereof, which comprises subjecting a compound represented by the formula (I): wherein R1 denotes hydrogen, nitro, halogen, phthalimido, mono- or di-(alkylcarbonyl)amino or alkoxy, or a salt thereof, to an acid halogenating reaction, which is successively reacted with malonic acid ester and magnesium alkoxide, treated with an acid, and reacted with sulfur and a compound represented by the formula: NCCH2COOR2 [wherein R2 denotes alkyl or aryl], or a salt thereof, in the presence of primary amine. According to the process of production of the present invention, thienopyrimidine derivatives having the GnRH antagonistic activity can be produced effectively and at an industrial large scale by a high yield and simple method.
摘要翻译：本发明提供了一种在工业上大规模生产具有GnRH拮抗活性的噻吩并嘧啶衍生物的中间体的方法。本发明的制备方法涉及一种由式（III）表示的化合物的制备方法：其中各自符号具有与下述相同的含义或其盐，其包括使由式（I）表示的化合物：其中R 1表示氢，硝基，卤素，苯二甲酰亚氨基，单 - 或二 - （烷基羰基）氨基或烷氧基或其盐与酸卤化反应反应，该酸卤化反应与丙酸和烷氧基镁连续反应，用酸处理，并与硫和式NCCH 2 COOR 2表示的化合物反应[其中 R 2表示烷基或芳基]或其盐，在伯胺的存在下。根据本发明的制造方法，可以通过高产率和简单的方法有效地以工业规模生产具有GnRH拮抗活性的噻吩并嘧啶衍生物。

3. 发明授权

US07049441B2 Process for preparation of benzylpiperidine compounds 失效
标题翻译：苄基哌啶化合物的制备方法
公开(公告)号：US07049441B2
公开(公告)日：2006-05-23
申请号：US10939293
申请日：2004-09-10
申请人： Shokyo Miki , Mitsuhiro Takeda , Koji Nakamoto
发明人： Shokyo Miki , Mitsuhiro Takeda , Koji Nakamoto
IPC分类号： C07D211/70
CPC分类号： C07D401/12 , C07D211/34 , C07D211/62 , C07D211/70 , C07D211/96 , C07F9/094 , C07F9/4056 , Y02P20/55
摘要： According to the process as shown in the following scheme having a step for reacting Compound (I) with Compound (II) to produce Compound (III), benzylpiperidine compounds useful as synthesis starting materials of pharmaceutical agents, agricultural chemicals and the like can be produced conveniently by a short step: wherein R1 is a hydrogen atom or an amino-protecting group, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, and R3 is a lower alkyl group.
摘要翻译：根据具有使化合物（I）与化合物（II）反应生成化合物（III）的步骤的方法所示的方法，可以制备用作药剂，农药等的合成原料的苄基哌啶化合物方便地通过短步骤：其中R 1是氢原子或氨基保护基，R 2是氢原子，任选具有取代基的烃基，烷氧基任选具有取代基的基团或任选具有取代基的杂环基，R 3是低级烷基。

4. 发明申请

US20100105922A1 PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME 有权
标题翻译：制备熔融咪唑化合物的方法，稳定形式的改性试剂及其制备方法
公开(公告)号：US20100105922A1
公开(公告)日：2010-04-29
申请号：US12648022
申请日：2009-12-28
申请人： Jun-Ichi Kawakami , Koji Nakamoto , Shigeru Nuwa , Syoji Handa , Shokyo Miki
发明人： Jun-Ichi Kawakami , Koji Nakamoto , Shigeru Nuwa , Syoji Handa , Shokyo Miki
IPC分类号： C07D233/64 , C07C27/04
CPC分类号： C07D233/64 , C07D487/04 , C07F3/06
摘要： The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I); and a Reformatsky reagent in a stable form suitable for the process.In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.
摘要翻译：本发明提供了用于生产由通式（I）表示的类固醇C17,20裂解酶抑制剂的工业上有利的方法; 和一种适用于该方法的稳定形式的Reformatsky试剂。在本发明中，通式（I）表示的化合物是通过在金属氢化物络合物的存在下，通过在Reformatsky反应中还原由特定的羰基化合物得到的特定的β-羟基酯化合物衍生物或其盐和金属卤化物，然后使其进行闭环反应。在上述Reformatsky反应中，使用由通式BrZnCH 2 COOC 2 H 5表示的化合物或由式（BrZnCH2COOC2H5.THF）2表示的化合物的晶体的稳定溶液是有用的。

5. 发明授权

US06313301B1 Thienopyridine derivatives, their intermediates and production thereof 失效
标题翻译：噻吩并吡啶衍生物，其中间体及其制备
公开(公告)号：US06313301B1
公开(公告)日：2001-11-06
申请号：US09446542
申请日：1999-12-22
申请人： Shokyo Miki , Koichiro Fukuoka , Masahiro Akita , Junichi Kawakami , Shuichi Furuya , Yoichiro Ishimaru
发明人： Shokyo Miki , Koichiro Fukuoka , Masahiro Akita , Junichi Kawakami , Shuichi Furuya , Yoichiro Ishimaru
IPC分类号： C07D47104
CPC分类号： C07D495/04
摘要： The present invention provides an intermediate for producing a thienopyridine derivative useful as a GnRH antagonist as well as an efficient and safe method for producing the same in an industrial scale at a high yield.
摘要翻译：本发明提供了用作GnRH拮抗剂的噻吩并吡啶衍生物的制造中间体，以及高产率的工业规模的高效安全的制造方法。

6. 发明授权

US08093403B2 Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 有权
标题翻译：稠合咪唑化合物的制备方法，稳定形式的重格列烷基试剂及其制备方法
公开(公告)号：US08093403B2
公开(公告)日：2012-01-10
申请号：US12648022
申请日：2009-12-28
申请人： Jun-Ichi Kawakami , Shigeru Nuwa , Shokyo Miki
发明人： Jun-Ichi Kawakami , Shigeru Nuwa , Shokyo Miki
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , C07D487/04 , C07F3/06
摘要： The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I); and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.
摘要翻译：本发明提供了用于生产由通式（I）表示的类固醇C17,20裂解酶抑制剂的工业上有利的方法; 和一种适用于该方法的稳定形式的Reformatsky试剂。在本发明中，通式（I）表示的化合物是通过在金属氢化物络合物的存在下，通过在Reformatsky反应中还原由特定的羰基化合物得到的特定的β-羟基酯化合物衍生物或其盐和金属卤化物，然后使其进行闭环反应。在上述Reformatsky反应中，使用由通式BrZnCH 2 COOC 2 H 5表示的化合物或由式（BrZnCH2COOC2H5.THF）2表示的化合物的晶体的稳定溶液是有用的。

7. 发明授权

US07662974B2 Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 失效
标题翻译：稠合咪唑化合物的制备方法，稳定形式的重格列烷基试剂及其制备方法
公开(公告)号：US07662974B2
公开(公告)日：2010-02-16
申请号：US10500999
申请日：2003-01-09
申请人： Jun-ichi Kawakami , Koji Nakamoto , Shigeru Nuwa , Syoji Handa , Shokyo Miki
发明人： Jun-ichi Kawakami , Koji Nakamoto , Shigeru Nuwa , Syoji Handa , Shokyo Miki
IPC分类号： C07F3/06
CPC分类号： C07D233/64 , C07D487/04 , C07F3/06
摘要： The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I): and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.
摘要翻译：本发明提供了用于生产由通式（I）表示的类固醇C17,20裂解酶抑制剂的工业上有利的方法：和适于该方法的稳定形式的Reformatsky试剂。在本发明中，通式（I）表示的化合物是通过在金属氢化物络合物的存在下，通过在Reformatsky反应中还原由特定的羰基化合物得到的特定的β-羟基酯化合物衍生物或其盐，金属卤化物，然后使其进行闭环反应。在上述Reformatsky反应中，使用由通式BrZnCH 2 COOC 2 H 5表示的化合物或由式（BrZnCH2COOC2H5.THF）2表示的化合物的晶体的稳定溶液是有用的。

8. 发明授权

US5804601A Aromatic hydroxamic acid compounds, their production and use 失效
标题翻译：芳香族异羟肟酸化合物，其生产和使用
公开(公告)号：US5804601A
公开(公告)日：1998-09-08
申请号：US629623
申请日：1996-04-09
申请人： Kaneyoshi Kato , Shokyo Miki , Ken-ichi Naruo , Hideki Takahashi
发明人： Kaneyoshi Kato , Shokyo Miki , Ken-ichi Naruo , Hideki Takahashi
IPC分类号： C07C259/06 , C07D215/14 , C07D215/20 , C07D217/14 , C07D235/16 , C07D263/56 , C07D277/64 , C07D513/04 , A61K31/165
CPC分类号： C07D263/56 , C07C259/06 , C07D215/14 , C07D215/20 , C07D217/14 , C07D235/16 , C07D277/64 , C07D513/04
摘要： The present invention relates to a compound of the formula: ##STR1## wherein Ar represents an optionally substituted aromatic group; Q represents a divalent aliphatic hydrocarbon group; R.sub.1 represents hydrogen, cyano, an optionally substituted hydrocarbon group, a group of the formula: ##STR2## wherein R.sup.3 and R.sub.4 independently represent hydrogen, acyl or an optionally substituted hydrocarbon group, or R.sup.3 and R.sup.4 jointly form a ring, or acyl; R.sup.2 represents acyl; ......... represents a single bond or a double bond; m represents 1 or 2 or a salt, a process of producing thereof and an anti-neurodegenerative composition.
摘要翻译：本发明涉及下式的化合物：其中Ar表示任选取代的芳族基团; Q表示二价脂族烃基; R 1表示氢，氰基，任选取代的烃基，下式的基团：其中R 3和R 4独立地表示氢，酰基或任选取代的烃基，或者R 3和R 4共同形成环或酰基; R2代表酰基; + E，ovs ......... + EE表示单键或双键; m表示1或2或其盐，其制备方法和抗神经变性组合物。

9. 发明申请

US20120077985A1 PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME 失效
标题翻译：制备熔融咪唑化合物的方法，稳定形式的改性试剂及其制备方法
公开(公告)号：US20120077985A1
公开(公告)日：2012-03-29
申请号：US13305411
申请日：2011-11-28
申请人： Jun-ichi Kawakami , Shigeru Nuwa , Shokyo Miki
发明人： Jun-ichi Kawakami , Shigeru Nuwa , Shokyo Miki
IPC分类号： C07D403/04
CPC分类号： C07D233/64 , C07D487/04 , C07F3/06
摘要： The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I); and a Reformatsky reagent in a stable form suitable for the process.In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.
摘要翻译：本发明提供了用于生产由通式（I）表示的类固醇C17,20裂解酶抑制剂的工业上有利的方法; 和一种适用于该方法的稳定形式的Reformatsky试剂。在本发明中，通式（I）表示的化合物是通过在金属氢化物络合物的存在下，通过在Reformatsky反应中还原由特定的羰基化合物得到的特定的β-羟基酯化合物衍生物或其盐和金属卤化物，然后使其进行闭环反应。在上述Reformatsky反应中，使用由通式BrZnCH 2 COOC 2 H 5表示的化合物或由式（BrZnCH2COOC2H5.THF）2表示的化合物的晶体的稳定溶液是有用的。

10. 发明申请

US20060094877A1 Process for preparation of benzylpiperidine compounds 审中-公开
公开(公告)号：US20060094877A1
公开(公告)日：2006-05-04
申请号：US11294626
申请日：2005-12-05
申请人： Shokyo Miki , Mitsuhiro Takeda , Koji Nakamoto
发明人： Shokyo Miki , Mitsuhiro Takeda , Koji Nakamoto
IPC分类号： C07F9/02 , C07D401/02
CPC分类号： C07D401/12 , C07D211/34 , C07D211/62 , C07D211/70 , C07D211/96 , C07F9/094 , C07F9/4056 , Y02P20/55
摘要： According to the process as shown in the following scheme having a step for reacting Compound (I) with Compound (II) to produce Compound (III), benzylpiperidine compounds useful as synthesis starting materials of pharmaceutical agents, agricultural chemicals and the like can be produced conveniently by a short step: wherein R1 is a hydrogen atom or an amino-protecting group, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, and R3 is a lower alkyl group.

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