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1. 发明授权

US08114902B2 2-aminobutanol compound and use thereof for medical purposes 有权
标题翻译： 2-氨基丁醇化合物及其用于医疗用途
公开(公告)号：US08114902B2
公开(公告)日：2012-02-14
申请号：US12226745
申请日：2007-04-27
申请人： Masatoshi Kiuchi , Mitsuharu Nakamura , Maiko Hamada , Kunio Sugahara
发明人： Masatoshi Kiuchi , Mitsuharu Nakamura , Maiko Hamada , Kunio Sugahara
IPC分类号： A61K31/335 , C07D319/06
CPC分类号： C07F9/653 , C07C217/64 , C07C225/16 , C07C309/65 , C07C323/32 , C07C323/38 , C07C323/41 , C07D333/22 , C07D333/34 , C07F9/091
摘要： Disclosed is a 2-aminobutanol compound represented by the following formula (I) or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof, as well as a production method of the 2-aminobutanol compound of formula (I). The 2-aminobutanol compounds of formula (I) have few side effects including bradycardia and have superior peripheral blood lymphocyte-decreasing effects.
摘要翻译：公开了由下式（I）表示的2-氨基丁醇化合物或其药学上可接受的酸加成盐或其水合物或其溶剂合物，以及式（I）的2-氨基丁醇化合物的制备方法）。式（I）的2-氨基丁醇化合物具有很少的副作用，包括心动过缓，并且具有优异的外周血淋巴细胞减少作用。

2. 发明授权

US06288061B1 Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US06288061B1
公开(公告)日：2001-09-11
申请号：US09598216
申请日：2000-06-21
申请人： Hiroyuki Sueoka , Jouji Yasuoka , Akira Nishiyama , Masatoshi Kiuchi , Katsuya Yamamoto , Kunio Sugahara , Syuji Ehara , Kei Sakata
发明人： Hiroyuki Sueoka , Jouji Yasuoka , Akira Nishiyama , Masatoshi Kiuchi , Katsuya Yamamoto , Kunio Sugahara , Syuji Ehara , Kei Sakata
IPC分类号： A61K314178
CPC分类号： C07D401/04 , C07D233/66 , C07D403/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof. The compounds of the formulas (I) and (XII) and pharmaceutically acceptable salts thereof of the present invention inhibit IL-4 and IL-5 production by Th2 cells and are effective for the prophylaxis and treatment of allergic diseases such as atopic dermatitis, bronchial asthma, allergic rhinitis and the like.
摘要翻译：本发明涉及下式（I）的咪唑衍生物，其中R 1是氢，任选取代的烷基等，R 2是氢，任选取代的烷基等，R 3是任选取代的杂芳基，R 4是任选取代的环烷基，任选地取代的苯基等，条件是当R 1为氢时，R 2和R 4相同或不同，并且各自为苯基或被卤素原子取代的苯基，低级烷基或低级烷氧基，R 3为被苯基取代的苯并噻唑基或噻唑基，咪唑下式（Ⅻ）的衍生物，其中R 6是任选取代的苯基或任选取代的杂芳基且R 7是取代的苯基，及其药学上可接受的盐。本发明的式（I）和（XII）化合物及其药学上可接受的盐抑制Th2细胞的IL-4和IL-5产生，对预防和治疗变应性疾病如特应性皮炎，支气管哮喘，过敏性鼻炎等。

3. 发明授权

US08476260B2 Antitumor agent 有权
标题翻译：抗肿瘤剂
公开(公告)号：US08476260B2
公开(公告)日：2013-07-02
申请号：US12810564
申请日：2008-12-26
申请人： Shinji Miyoshi , Shinsuke Ooike , Kazunori Iwata , Hidemasa Hikawa , Kunio Sugahara
发明人： Shinji Miyoshi , Shinsuke Ooike , Kazunori Iwata , Hidemasa Hikawa , Kunio Sugahara
IPC分类号： A61P35/00 , A61P43/00 , A61K31/55 , A61K45/00 , C07D495/14
CPC分类号： A61K31/551 , C07D495/14
摘要： The present invention relates to a novel antitumor agent containing a compound that inhibits binding between acetylated histone and a bromodomain-containing protein, preferably a thienotriazolodiazepine compound represented by the following formula (I) wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof or a hydrate or solvate as an active ingredient.
摘要翻译：本发明涉及含有抑制乙酰化组蛋白与含溴结构域的蛋白质之间的结合的化合物的新型抗肿瘤剂，优选下述式（I）表示的噻吩并三氮唑并氮化合物，其中各符号如说明书中所定义，或药学上可接受的盐或水合物或溶剂化物作为活性成分。

4. 发明申请

US20100286127A1 ANTITUMOR AGENT 有权
标题翻译：抗菌剂
公开(公告)号：US20100286127A1
公开(公告)日：2010-11-11
申请号：US12810564
申请日：2008-12-26
申请人： Shinji Miyoshi , Shinsuke Ooike , Kazunori Iwata , Hidemasa Hikawa , Kunio Sugahara
发明人： Shinji Miyoshi , Shinsuke Ooike , Kazunori Iwata , Hidemasa Hikawa , Kunio Sugahara
IPC分类号： A61K31/551 , C07D495/14 , A61P35/00
CPC分类号： A61K31/551 , C07D495/14
摘要： The present invention relates to a novel antitumor agent containing a compound that inhibits binding between acetylated histone and a bromodomain-containing protein, preferably a thienotriazolodiazepine compound represented by the following formula (I) wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof or a hydrate or solvate as an active ingredient.
摘要翻译：本发明涉及含有抑制乙酰化组蛋白与含溴结构域的蛋白质之间的结合的化合物的新型抗肿瘤剂，优选下述式（I）表示的噻吩并三氮唑并氮化合物，其中各符号如说明书中所定义，或药学上可接受的盐或水合物或溶剂化物作为活性成分。

5. 发明申请

US20100041643A1 THIENOTRIAZOLODIAZEPINE COMPOUND AND MEDICINAL USE THEREOF 有权
标题翻译：苯并噻唑啉酮化合物及其药物用途
公开(公告)号：US20100041643A1
公开(公告)日：2010-02-18
申请号：US11916015
申请日：2006-05-30
申请人： Kunitomo Adachi , Hidemasa Hikawa , Maiko Hamada , Jun-ichi Endoh , Seigo Ishibuchi , Naoto Fujie , Minoru Tanaka , Kunio Sugahara , Kouichi Oshita , Meguru Murata
发明人： Kunitomo Adachi , Hidemasa Hikawa , Maiko Hamada , Jun-ichi Endoh , Seigo Ishibuchi , Naoto Fujie , Minoru Tanaka , Kunio Sugahara , Kouichi Oshita , Meguru Murata
IPC分类号： A61K31/551 , C07D495/14
CPC分类号： C07D495/14
摘要： [Solving means] A thienotriazolodiazepine compound of the following formula (I) a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound. [Effect]Since this compound has an inhibitory action on costimulatory signal from CD28 on T cell, it is useful for the prophylaxis or suppression of rejection reaction in transplantation of organ or bone marrow and the like, and the prophylaxis or treatment of autoimmune diseases or allergic diseases.
摘要翻译： [解决方案]下述式（I）的噻吩并三唑并氮杂化合物是含有该化合物作为有效成分的药剂，以及噻吩并三唑并氮杂化合物的制造中间体和制造方法。 [效果]由于该化合物对T细胞上的CD28的共刺激信号具有抑制作用，因此可用于预防或抑制移植器官或骨髓等中的排斥反应，以及预防或治疗自身免疫性疾病或过敏性疾病

6. 发明授权

US08809304B2 Amine compound and use thereof for medical purposes 有权
标题翻译：胺化合物及其用于医疗用途
公开(公告)号：US08809304B2
公开(公告)日：2014-08-19
申请号：US12086419
申请日：2006-12-15
申请人： Masatoshi Kiuchi , Kaoru Marukawa , Nobutaka Kobayashi , Kunio Sugahara
发明人： Masatoshi Kiuchi , Kaoru Marukawa , Nobutaka Kobayashi , Kunio Sugahara
IPC分类号： C07C215/00 , A01N57/00 , A61K31/66 , A01N57/10 , A01N37/00 , A61K31/185 , C07D319/06 , C07F9/09 , C07F9/40 , C07F9/6527 , C07C323/32 , C07F9/653 , C07C323/43 , C07C255/54 , C07C217/64
CPC分类号： C07C235/34 , C07C217/64 , C07C235/78 , C07C255/54 , C07C271/16 , C07C323/32 , C07C323/43 , C07D319/06 , C07F7/1804 , C07F9/09 , C07F9/091 , C07F9/141 , C07F9/4056 , C07F9/6527 , C07F9/653
摘要： A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(═O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH═CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.
摘要翻译：由下式（I）表示的新型胺化合物，其免疫抑制作用优异，排斥抑制作用等，并且显示降低的副作用，例如心动过缓等，或其药学上可接受的酸加成盐或水合物或溶剂合物，以及含有该化合物和药学上可接受的载体的药物组合物。其中R为氢原子或P（= O）（OH）2，X为氧原子或硫原子，Y为CH 2 CH 2或CH = CH，R 1为氰基或碳数为1至4的烷基，通过卤素原子，R 2是碳数为1至4的烷基，并且任选地被羟基或卤素原子取代，R 3和R 4可以相同或不同，各自为氢原子或碳数为1至4的烷基，n为5-8。

7. 发明申请

US20090082311A1 2-Aminobutanol Compound and Use Thereof for Medical Purposes 有权
标题翻译： 2-氨基丁醇化合物及其用途
公开(公告)号：US20090082311A1
公开(公告)日：2009-03-26
申请号：US12226745
申请日：2007-04-27
申请人： Masatoshi Kiuchi , Mitsuharu Nakamura , Maiko Hamada , Kunio Sugahara
发明人： Masatoshi Kiuchi , Mitsuharu Nakamura , Maiko Hamada , Kunio Sugahara
IPC分类号： A61K31/137 , C07C215/20 , C07C69/34 , C07D317/30 , A61P37/00 , A61K31/675 , A61K31/662 , A61K31/216 , C07F9/653 , A61K31/357
CPC分类号： C07F9/653 , C07C217/64 , C07C225/16 , C07C309/65 , C07C323/32 , C07C323/38 , C07C323/41 , C07D333/22 , C07D333/34 , C07F9/091
摘要： The present invention provides a novel compound having few side effects such as bradycardia and the like and having superior peripheral blood lymphocyte-decreasing effect.The present invention provides a 2-aminobutanol compound represented by the following formula (I) wherein R1 is a hydrogen atom or P(═O) (OH)2, R2 is an alkyl having 1 to 4 carbon atoms optionally substituted by hydroxyl group(s) or optionally substituted by halogen atom(s), R3 is a hydrogen atom; a halogen atom; cyano; an alkyl having 1 to 4 carbon atoms optionally substituted by halogen atom(s); or an acyl having 2 to 5 carbon atoms optionally substituted by halogen atom(s), X is an oxygen atom, a sulfur atom, carbonyl or NR4 wherein R4 is a hydrogen atom or an alkyl having 1 to 4 carbon atoms, Ar1 is an optionally substituted arylene or an optionally substituted heteroarylene, and Ar2 is an optionally substituted aryl or an optionally substituted heteroaryl, provided that when X is an oxygen atom, Ar1 is phenylene and Ar2 is phenyl, then the phenyl for Ar2 should be substituted, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof, as well as a production method of the above-mentioned 2-aminobutanol compound.
摘要翻译：本发明提供一种副作用少的新型化合物，如心动过缓等，具有优异的外周血淋巴细胞减少作用。本发明提供由下式（I）表示的2-氨基丁醇化合物，其中R 1为氢原子或P（-O）（OH）2，R 2为任选被羟基取代的具有1至4个碳原子的烷基或任选被卤素原子取代，R 3是氢原子; 卤素原子; 氰基; 任选被卤素原子取代的碳原子数1〜4的烷基; 或任选被卤素原子取代的具有2至5个碳原子的酰基，X是氧原子，硫原子，羰基或NR 4，其中R 4是氢原子或具有1至4个碳原子的烷基，Ar 1是任选取代的亚芳基或任选取代的亚杂芳基，Ar 2是任选取代的芳基或任选取代的杂芳基，条件是当X是氧原子时，Ar 1是亚苯基，Ar 2是苯基，则Ar 2的苯基应该被取代，或其药学上可接受的酸加成盐或其水合物或其溶剂合物，以及上述2-氨基丁醇化合物的制备方法。

8. 发明授权

US08129361B2 Amine compound and pharmaceutical use thereof 有权
标题翻译：胺化合物及其药物用途
公开(公告)号：US08129361B2
公开(公告)日：2012-03-06
申请号：US12664366
申请日：2008-06-13
申请人： Masatoshi Kiuchi , Kaoru Tashiro , Maiko Hamada , Kunio Sugahara
发明人： Masatoshi Kiuchi , Kaoru Tashiro , Maiko Hamada , Kunio Sugahara
IPC分类号： A61K31/045 , A61K31/137 , C07C215/20 , C07C215/28
CPC分类号： C07C255/54 , C07C217/70 , C07C255/59 , C07C317/32 , C07C323/19 , C07C323/32 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D211/14 , C07D295/08 , C07D307/79 , C07D317/22 , C07D317/62 , C07D333/16 , C07D333/28 , C07D333/56 , C07F9/091 , C07F9/5456 , C07F9/653 , C07F9/65517 , C07F9/655345 , C07F9/655354 , C07F9/65586
摘要： Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.
摘要翻译：提供了具有优异的外周血淋巴细胞减少作用和优异的免疫抑制作用，排斥抑制作用等的下述式（I）表示的新型胺化合物，其表现出例如心动过缓等的副作用降低，或其药学上可接受的酸加成盐或其水合物或其溶剂合物。其中每个符号如说明书中所定义。

9. 发明授权

US08044042B2 Thienotriazolodiazepine compound and medicinal use thereof 有权
标题翻译：噻吩并三唑并氮杂化合物及其药用
公开(公告)号：US08044042B2
公开(公告)日：2011-10-25
申请号：US11916015
申请日：2006-05-30
申请人： Kunitomo Adachi , Hidemasa Hikawa , Maiko Hamada , Jun-ichi Endoh , Seigo Ishibuchi , Naoto Fujie , Minoru Tanaka , Kunio Sugahara , Kouichi Oshita , Meguru Murata
发明人： Kunitomo Adachi , Hidemasa Hikawa , Maiko Hamada , Jun-ichi Endoh , Seigo Ishibuchi , Naoto Fujie , Minoru Tanaka , Kunio Sugahara , Kouichi Oshita , Meguru Murata
IPC分类号： A61P1/04 , A61P3/10 , A61P13/12 , A61P17/00 , A61P19/02 , A61P25/00 , A61P27/14 , A61P29/00 , A61P37/00 , A61P43/00 , A61K31/551 , C07D495/14
CPC分类号： C07D495/14
摘要： A thienotriazolodiazepine compound of the following formula (I) a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound. Since this compound has an inhibitory action on costimulatory signal from CD28 on T cell, it is useful for the prophylaxis or suppression of rejection reaction in transplantation of organ or bone marrow and the like, and the prophylaxis or treatment of autoimmune diseases or allergic diseases.
摘要翻译：下式（I）的噻吩并三唑并噻嗪类化合物是含有该化合物作为活性成分的药剂，以及噻吩并三唑并噻吩类化合物的制造中间体和制造方法。由于该化合物对T细胞上的CD28的共刺激信号具有抑制作用，因此可用于预防或抑制移植器官或骨髓等中的排斥反应，以及预防或治疗自身免疫疾病或过敏性疾病。

10. 发明申请

US20100179216A1 AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF 有权
标题翻译：胺化合物及其药物用途
公开(公告)号：US20100179216A1
公开(公告)日：2010-07-15
申请号：US12664366
申请日：2008-06-13
申请人： Masatoshi Kiuchi , Kaoru Tashiro , Maiko Hamada , Kunio Sugahara
发明人： Masatoshi Kiuchi , Kaoru Tashiro , Maiko Hamada , Kunio Sugahara
IPC分类号： A61K31/135 , C07D319/06 , C07C255/58 , C07C229/36 , C07C217/62 , C07C271/16 , A61K31/357 , A61K31/277 , A61K31/225 , A61K31/27 , A61P37/00 , A61P37/06 , A61P37/08
CPC分类号： C07C255/54 , C07C217/70 , C07C255/59 , C07C317/32 , C07C323/19 , C07C323/32 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D211/14 , C07D295/08 , C07D307/79 , C07D317/22 , C07D317/62 , C07D333/16 , C07D333/28 , C07D333/56 , C07F9/091 , C07F9/5456 , C07F9/653 , C07F9/65517 , C07F9/655345 , C07F9/655354 , C07F9/65586
摘要： Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.
摘要翻译：提供了具有优异的外周血淋巴细胞减少作用和优异的免疫抑制作用，排斥抑制作用等的下述式（I）表示的新型胺化合物，其表现出例如心动过缓等的副作用降低，或其药学上可接受的酸加成盐或其水合物或其溶剂合物。其中每个符号如说明书中所定义。

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