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1. 发明授权

US07223859B2 Method for producing (R)-3-[4-(trifluoromethyl) phenylamino]-pentanoic acid amide derivative 失效
标题翻译：（R）-3- [4-（三氟甲基）苯基氨基] - 戊酸酰胺衍生物的制备方法
公开(公告)号：US07223859B2
公开(公告)日：2007-05-29
申请号：US10801141
申请日：2004-03-16
申请人： Tatsuyoshi Tanaka , Masanobu Sugawara , Hirofumi Maeda , Akira Nishiyama , Yoshihiko Yasohara , Nobuo Nagashima
发明人： Tatsuyoshi Tanaka , Masanobu Sugawara , Hirofumi Maeda , Akira Nishiyama , Yoshihiko Yasohara , Nobuo Nagashima
IPC分类号： C07D205/02 , C07C233/00
CPC分类号： C07D205/08 , C07C231/02 , C07C309/66 , C07C309/73
摘要： The present invention provides a method for easily producing an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative useful for an intermediate for pharmaceutical products, particularly an inhibitor of a cholesteryl ester transfer protein (CETP) from easily available raw materials. In the present invention, (S)-N-[4-(trifluoromethyl)phenyl]-3-hydroxypentanoic acid amide prepared from easily available raw materials leads a production of (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone to give (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide. Furthermore, (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone is reacted with a carbamic acid ester to give an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative.
摘要翻译：本发明提供了一种容易地制备用于药物产品中间体（特别是胆固醇酯转移蛋白（CETP）抑制剂）的（R）-3- [4-（三氟甲基）苯基氨基] - 戊酸酰胺衍生物的方法，容易获得的原料。在本发明中，由容易获得的原料制备的（S）-N- [4-（三氟甲基）苯基] -3-羟基戊酸酰胺导致（R）-4-乙基-1- [4-（三氟甲基））苯基] -2-氮杂环丁酮，得到（R）-3- [4-（三氟甲基）苯基氨基] - 戊酸酰胺。此外，将（R）-4-乙基-1- [4-（三氟甲基）苯基] -2-氮杂环丁酮与氨基甲酸酯反应，得到（R）-3- [4-（三氟甲基）苯基氨基] - 戊酸酰胺衍生物。

2. 发明申请

US20050014818A1 Process for producing optically active chroman derivative and intermediate 审中-公开
标题翻译：光学活性苯并二氢吡喃衍生物和中间体的制备方法
公开(公告)号：US20050014818A1
公开(公告)日：2005-01-20
申请号：US10494671
申请日：2002-11-07
申请人： Masaru Mitsuda , Tatsuyoshi Tanaka , Yoshihiko Yasohara
发明人： Masaru Mitsuda , Tatsuyoshi Tanaka , Yoshihiko Yasohara
IPC分类号： C07C39/24 , C07C303/28 , C07C303/30 , C07C309/66 , C07C309/73 , C07D311/20 , C07D405/06 , C12P7/22 , C07D311/74 , A61K31/353
CPC分类号： C07D405/06 , C07C39/24 , C07C39/245 , C07C303/28 , C07C309/66 , C07C309/73 , C07D311/20 , C12P7/22
摘要： A process for easily producing various optically active chroman derivatives that are useful as pharmaceutical intermediates from inexpensive starting materials is provided. Cyclic hemiacetal (1) obtained from dihydrocoumarin through one step is asymmetrically reduced to produce an optically active halohydrin derivative (3), and the optically active halohydrin derivative (3) is cyclized to produce an optically active chroman derivative (13):
摘要翻译：提供了一种易于制备可用作廉价起始材料的药物中间体的各种光学活性苯并二氢吡喃衍生物的方法。通过一步从二氢香豆素获得的环状半缩醛（1）被不对称地还原以产生光学活性的卤代醇衍生物（3），并将光学活性卤代醇衍生物（3）环化以产生光学活性苯并二氢吡喃衍生物（13）：

3. 发明授权

US08071600B2 Derivatives of 4-piperazin-1-yl-4-benzo[B]thiophene suitable for the treatment of CNS disorders 有权
标题翻译：适用于治疗CNS疾病的4-哌嗪-1-基-4-苯并[b]噻吩的衍生物
公开(公告)号：US08071600B2
公开(公告)日：2011-12-06
申请号：US11991146
申请日：2006-08-31
申请人： Hiroshi Yamashita , Hideaki Kuroda , Nobuaki Ito , Shin Miyamura , Kunio Oshima , Jun Matsubara , Haruka Takahashi , Tae Fukushima , Satoshi Shimizu , Kazumi Kondo , Yohji Sakurai , Takeshi Kuroda , Shinichi Taira , Motohiro Itotani , Tatsuyoshi Tanaka
发明人： Hiroshi Yamashita , Hideaki Kuroda , Nobuaki Ito , Shin Miyamura , Kunio Oshima , Jun Matsubara , Haruka Takahashi , Tae Fukushima , Satoshi Shimizu , Kazumi Kondo , Yohji Sakurai , Takeshi Kuroda , Shinichi Taira , Motohiro Itotani , Tatsuyoshi Tanaka
IPC分类号： A61K31/496 , A61K31/55 , A61K31/551 , C07D333/54 , C07D409/12 , C07D409/14 , A61K31/536 , A61K31/5415 , C07D407/12 , C07D413/12 , C07D417/12
CPC分类号： C07D409/12 , C07D333/54 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D487/08 , C07D491/113
摘要： A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
摘要翻译：由式（1）表示的杂环化合物或其盐：其中R 2表示氢原子或低级烷基; A表示低级亚烷基或低级亚烯基; R1表示芳基或杂环基。本发明的化合物具有广泛的精神障碍治疗范围，包括中枢神经系统疾病，无副作用和高安全性。

4. 发明授权

US07582781B2 Optically active halohydrin derivative and process for producing optically active epoxy alcohol derivative from the same 失效
标题翻译：光学活性卤代醇衍生物及其制备光学活性环氧醇衍生物的方法
公开(公告)号：US07582781B2
公开(公告)日：2009-09-01
申请号：US10563635
申请日：2004-07-05
申请人： Kazumi Okuro , Tatsuyoshi Tanaka , Masaru Mitsuda , Kenji Inoue
发明人： Kazumi Okuro , Tatsuyoshi Tanaka , Masaru Mitsuda , Kenji Inoue
IPC分类号： C07D301/24 , C07D301/26 , C07D405/06 , C07C33/26 , C07C69/353 , C07F7/04
CPC分类号： C07C67/29 , C07B2200/07 , C07C29/10 , C07D301/24 , C07C33/46
摘要： The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxy alcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.
摘要翻译：本发明提供了一种工业上安全，易于操作的方法，用于制备用作药物的廉价可得材料的中间体的光学活性环氧醇衍生物，并且还提供了作为环氧醇衍生物的重要中间体的新型卤代醇衍生物。此外，本发明提供了通过使卤代醇与三唑磺酰胺反应来制备三唑抗真菌剂的中间体的方法，该方法包括少量的步骤。制备光学活性环氧醇衍生物的方法包括使光学活性的α-取代的丙酸酯衍生物与卤代乙酸衍生物在碱的存在下反应以制备光学活性的卤代酮衍生物，使所得到的卤代酮衍生物与芳基金属化合物立体选择性地制备卤代醇衍生物，除去卤代醇衍生物的羟基的取代基，并用碱进行环氧化。此外，制备三唑抗真菌剂中间体的方法包括使卤代醇衍生物与三唑磺酰胺反应，该方法包括少量步骤。

5. 发明授权

US4564619A Carbostyril derivative 失效
标题翻译：碳青霉烯衍生物
公开(公告)号：US4564619A
公开(公告)日：1986-01-14
申请号：US528887
申请日：1983-09-02
申请人： Tatsuyoshi Tanaka , Kazuyoshi Nagami , Shigeharu Tamada , Kazuyuki Nakagawa
发明人： Tatsuyoshi Tanaka , Kazuyoshi Nagami , Shigeharu Tamada , Kazuyuki Nakagawa
IPC分类号： C07D215/22 , C07D215/227 , C07D401/12 , A61K31/47
CPC分类号： C07D215/227 , C07D401/12
摘要： Carbostyril derivative or a pharmaceutically acceptable acid addition salt thereof, having excellent platelate aggregation inhibitory effect, calcium antagonism, hypotensive effect and phosphodiesterase inhibitory effect are useful as prophylactic or treating agents for thrombosis, circulation improving agents for coronary blood flow such as coronary vasodilators, hypotensive agents and phosphodiesterase inhibitors. Furthermore, the carbostyril derivatives are weak in heart rate increasing activity and also in cardiac muscle contraction increasing activity, and the carbostyril derivatives are useful agents for curing and treating heart diseases such as cardiac angina and myocardial infarction caused by hypercoagulability of the platelets. Processes are disclosed for preparation of the carbostyril derivatives.
摘要翻译：具有极好的铂性聚集抑制作用，钙拮抗作用，降血压作用和磷酸二酯酶抑制作用的卡波他特里尔衍生物或其药学上可接受的酸加成盐可用作血栓形成的预防或治疗剂，用于冠状动脉血管扩张剂的血液循环改善剂，降血压药剂和磷酸二酯酶抑制剂。此外，喹诺酮衍生物的心率增加活性弱，心肌收缩增加活性也较弱，而喹诺酮衍生物可用于治疗和治疗由心血管病和心肌梗塞引起的血小板高凝状态引起的心脏病。公开了制备喹诺酮衍生物的方法。

6. 发明授权

US08207370B2 Process for producing optically active beta-hydroxy-alpha-aminocarboxylic acid ester 失效
标题翻译：光学活性β-羟基-α-氨基羧酸酯的制备方法
公开(公告)号：US08207370B2
公开(公告)日：2012-06-26
申请号：US12311325
申请日：2007-09-26
申请人： Tatsuya Honda , Tatsuyoshi Tanaka , Masaru Mitsuda
发明人： Tatsuya Honda , Tatsuyoshi Tanaka , Masaru Mitsuda
IPC分类号： C07C209/50 , C07C209/46 , C07C209/00 , C07C229/06
CPC分类号： C07B53/00 , C07C227/16 , C07C231/12 , C07C229/22 , C07C233/18 , C07C233/47
摘要： It is an objective of the present invention to produce an anti-form of an optically active β-hydroxy-α-aminocarboxylic acid ester efficiently, simply and industrially advantageously. The objective can be accomplished by directly and selectively producing the anti-form of the optically active β-hydroxy-α-aminocarboxylic acid ester by asymmetric reduction of a β-keto-α-aminocarboxylic acid ester using an optically active amine complex as a catalyst. Further, the β-keto-α-aminocarboxylic acid ester as a raw material can be produced at a high yield by reacting a glycine derivative with a carboxylic acid derivative.
摘要翻译：本发明的目的是在工业上有效地有效地制备光学活性的α-羟基-α-氨基羧酸酯的抗反型剂。该目的可以通过使用光学活性胺络合物不对称还原反应形式的光学活性的β-羟基-α-氨基羧酸酯来直接和选择性地制备催化剂此外，可以通过使甘氨酸衍生物与羧酸衍生物反应，以高产率制备作为原料的α-酮-α-氨基羧酸酯。

7. 发明授权

US07888362B2 Piperazine-substituted benzothiophenes for treatment of mental disorders 有权
标题翻译：哌嗪取代的苯并噻吩用于治疗精神障碍
公开(公告)号：US07888362B2
公开(公告)日：2011-02-15
申请号：US11659005
申请日：2006-04-12
申请人： Hiroshi Yamashita , Nobuaki Ito , Shin Miyamura , Kunio Oshima , Jun Matsubara , Hideaki Kuroda , Haruka Takahashi , Satoshi Shimizu , Tatsuyoshi Tanaka
发明人： Hiroshi Yamashita , Nobuaki Ito , Shin Miyamura , Kunio Oshima , Jun Matsubara , Hideaki Kuroda , Haruka Takahashi , Satoshi Shimizu , Tatsuyoshi Tanaka
IPC分类号： A61K31/496 , C07D409/12
CPC分类号： C07D409/12 , C07D409/14
摘要： The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
摘要翻译：本发明提供由通式（1）表示的杂环化合物：本发明化合物具有广泛的精神障碍治疗谱，包括中枢神经系统疾病，副作用高，安全性高。

8. 发明申请

US20100179322A1 Piperazine-substituted benzothiophenes for treatment of mental disorders 有权
标题翻译：哌嗪取代的苯并噻吩用于治疗精神障碍
公开(公告)号：US20100179322A1
公开(公告)日：2010-07-15
申请号：US11659005
申请日：2006-04-12
申请人： Hiroshi Yamashita , Nobuaki Ito , Shin Miyamura , Kunio Oshima , Jun Matsubara , Hideaki Kuroda , Haruka Takahashi , Satoshi Shimizu , Tatsuyoshi Tanaka
发明人： Hiroshi Yamashita , Nobuaki Ito , Shin Miyamura , Kunio Oshima , Jun Matsubara , Hideaki Kuroda , Haruka Takahashi , Satoshi Shimizu , Tatsuyoshi Tanaka
IPC分类号： C07D409/14
CPC分类号： C07D409/12 , C07D409/14
摘要： The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
摘要翻译：本发明提供由通式（1）表示的杂环化合物：本发明化合物具有广泛的精神障碍治疗谱，包括中枢神经系统疾病，副作用高，安全性高。

9. 发明授权

US5942641A Fluorenone derivatives, process for preparing the same and central or peripheral nerve degeneration repair and protective agent 失效
标题翻译：芴酮衍生物，制备相同和中枢或周围神经变性修复和保护剂的方法
公开(公告)号：US5942641A
公开(公告)日：1999-08-24
申请号：US381865
申请日：1995-02-07
申请人： Tatsuyoshi Tanaka , Yohji Sakurai , Nobutaka Fujisawa , Osamu Hongoh , Takao Nishi
发明人： Tatsuyoshi Tanaka , Yohji Sakurai , Nobutaka Fujisawa , Osamu Hongoh , Takao Nishi
IPC分类号： C07C49/747 , C07C49/755 , C07C49/757 , C07C65/24 , C07C69/00 , C07C225/18 , C07C229/14 , C07C255/36 , C07C323/22 , C07D213/70 , C07D233/60 , C07D233/84 , C07D235/28 , C07D239/42 , C07D241/20 , C07D263/14 , C07D295/116 , C07D521/00 , A61K31/12 , C07C49/215
CPC分类号： C07D213/70 , C07C225/18 , C07C229/14 , C07C255/36 , C07C323/22 , C07C49/747 , C07C49/755 , C07C49/757 , C07C65/24 , C07C69/00 , C07D231/12 , C07D233/56 , C07D233/84 , C07D235/28 , C07D239/42 , C07D241/20 , C07D249/08 , C07D263/14 , C07D295/116 , C07C2101/14 , C07C2103/00 , C07C2103/18
摘要： The present invention provides a novel fluorenone derivatives represented by the formula: ##STR1## wherein R.sup.a -R.sup.g are defined in the specification, and a method for repairing and protecting central or peripheral nerve degeneration comprising use of a fluorenone derivative represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 p and q are as defined in the specification as an active component.
摘要翻译： PCT No.PCT / JP94 / 00966 Sec。 371日期：1995年2月7日 102（e）1995年2月7日PCT PCT 1994年6月15日PCT公布。公开号WO95 / 00468 日期1995年1月5日本发明提供了一种由下式表示的新型芴酮衍生物：其中Ra-Rg在说明书中定义，以及修复和保护中枢或周围神经变性的方法，其包括使用由式：其中R1，R2和q如说明书中定义为活性组分。

10. 发明申请

US20110213031A1 NOVEL TYPE I NATURAL CERAMIDE DERIVATIVE AND METHOD FOR PRODUCING SAME 失效
标题翻译：新型I型天然陶瓷衍生物及其生产方法
公开(公告)号：US20110213031A1
公开(公告)日：2011-09-01
申请号：US13121094
申请日：2009-09-30
申请人： Tatsuyoshi Tanaka , Kazumi Okuro
发明人： Tatsuyoshi Tanaka , Kazumi Okuro
IPC分类号： A61K31/231 , C07C235/74 , C07C235/76 , A61K31/23 , A61K31/232 , C07C231/02 , A61P17/00
CPC分类号： A61Q19/00 , A61K8/68 , C07B2200/07 , C07C235/08
摘要： The present invention aims to provide a novel type I natural ceramide derivative having a structure more similar to that of a type I natural ceramide composed of sphingosine and an ω-acyloxy long-chain carboxylic acid; and a method for producing the same. The derivative is provided by reacting an ω-acyloxy long-chain fatty acid derivative with dihydrosphingosine or a salt thereof. The thus produced novel type I natural ceramide derivative, when combined with other ceramides, can significantly improve the compatibility of ceramides, which facilitates preparation of a composition containing ceramides, such as a moisturizer or a cosmetic, and also increases the storage stability of the composition.
摘要翻译：本发明旨在提供一种具有与鞘氨醇和ω-酰氧基长链羧酸组成的I型天然神经酰胺更类似的结构的新型I型天然神经酰胺衍生物; 及其制造方法。该衍生物通过ω-酰氧基长链脂肪酸衍生物与二氢鞘氨醇或其盐反应来提供。由此产生的新型I型天然神经酰胺衍生物与其他神经酰胺组合时，可以显着改善神经酰胺的相容性，其有助于制备含有神经酰胺（例如保湿剂或化妆品）的组合物，并且还增加了组合物的储存稳定性。

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