公开(公告)号：US20150175541A1

公开(公告)日：2015-06-25

申请号：US14417387

申请日：2013-07-29

申请人： TAISHO PHARMACEUTICAL CO., LTD

发明人： Tetsuo Takayama ,  Tsuyoshi Shibata ,  Fumiyasu Shiozawa ,  Kenichi Kawabe ,  Yuki Shimizu ,  Makoto Hamada ,  Akira Hiratate ,  Masato Takahashi ,  Fumihito Ushiyama ,  Takahiro Oi ,  Yoshihisa Shirasaki ,  Daisuke Matsuda ,  Chie Koizumi ,  Sota Kato

IPC分类号： C07D211/90 ,  C07D221/20 ,  C07D401/12 ,  C07D215/56 ,  C07D405/06 ,  C07D413/06 ,  C07D491/107 ,  C07D417/06

CPC分类号： C07D211/90 ,  C07D207/36 ,  C07D209/54 ,  C07D215/56 ,  C07D221/20 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D409/06 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07D471/10 ,  C07D491/107 ,  C07D498/04

摘要： There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I′): (in the above-mentioned general formula (I′), W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.

摘要翻译： 提供由通式（I'）表示的具有优异PHD2抑制作用的化合物：（在上述通式（I'）中，W，Y，R 2，R 3，R 4和Y 4如上所述 ）或其药学上可接受的盐。

公开(公告)号：US09045466B2

公开(公告)日：2015-06-02

申请号：US14235686

申请日：2012-07-27

申请人： Tetsuya Tanikawa ,  Yasunobu Ushiki ,  Fumihito Ushiyama ,  Toru Yamaguchi ,  Naoya Ono ,  Keiko Yamamoto ,  Risa Tsuruta ,  Yasuhiro Tsutsui ,  Noritomo Fujino ,  Ayumu Mori

发明人： Tetsuya Tanikawa ,  Yasunobu Ushiki ,  Fumihito Ushiyama ,  Toru Yamaguchi ,  Naoya Ono ,  Keiko Yamamoto ,  Risa Tsuruta ,  Yasuhiro Tsutsui ,  Noritomo Fujino ,  Ayumu Mori

IPC分类号： C07D417/12 ,  C07D417/04 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08

CPC分类号： C07D417/12 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08 ,  C07D417/04

摘要： An amidine compound represented by formula (I) (wherein A1 represents a nitrogen atom or a group represented by formula CR6; A2 and A3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R2 and R3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a C1-6 alkoxy group; and R4 and R5 are the same as or different from each other and independently represent a hydrogen atom, a C1-6 haloalkyl group, a C1-6 alkyl group or the like) or a salt thereof. The compound is useful as an anti-fungal agent.

摘要翻译： 由式（I）表示的脒化合物（其中A1表示氮原子或式CR6表示的基团; A2和A3彼此相同或不同，并且独立地表示氮原子或由式CH表示的基团; R1表示可以被1〜5个独立地选自取代基（2）等的取代基取代的芳基; R2和R3彼此相同或不同，独立地表示氢原子，卤素原子， C 1-6烷基，C 1-6卤代烷基或C 1-6烷氧基; R 4和R 5彼此相同或不同，独立地表示氢原子，C1-6卤代烷基，C1 -6烷基等）或其盐。 该化合物可用作抗真菌剂。

公开(公告)号：US20150141669A1

公开(公告)日：2015-05-21

申请号：US14403790

申请日：2013-05-31

申请人： TAISHO PHARMACEUTICAL CO., LTD.

发明人： Takashi Hashihayata ,  Norikazu Otake ,  Naoki Miyakoshi ,  Kazunari Sakagami

IPC分类号： C07D317/50 ,  C07D317/40 ,  C07C229/50

CPC分类号： C07D317/50 ,  A61K31/265 ,  A61K31/357 ,  C07C229/50 ,  C07C237/04 ,  C07C237/20 ,  C07C271/24 ,  C07C323/60 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/18 ,  C07C2603/74 ,  C07D207/08 ,  C07D307/88 ,  C07D317/40

摘要： Provided are a fluorine-containing amino acid prodrug represented by general formula (I) that makes a fluorine-containing amino acid which is a group 2 metabotropic glutamate receptor agonist into a prodrug, or a pharmaceutically acceptable salt thereof. More specifically, provided is a prodrug that increases the in vivo exposure and enhances the oral absorbability and other mucosal absorbability of a parent compound that acts on group 2 metabotropic glutamate receptors as an agent for the treatment or prevention of diseases in which group 2 metabotropic glutamate receptors are said to be involved, such as: schizophrenia, anxiety disorder and its related diseases, depression, bipolar disorder, epilepsy, developmental disorders, sleep disorders, and other neuropsychiatric diseases; and drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, movement disorders associated with muscular rigidity, cerebral ischemia, cerebral insufficiency, spinal cord disorders, cephalopathy, and other neurological diseases.

摘要翻译： 本发明提供一种通式（I）所示的含氟氨基酸前药，其为前体药物中含有2族代谢型谷氨酸受体激动剂的含氟氨基酸或其药学上可接受的盐。 更具体地，提供了增加体内暴露并增强作用于第2组代谢型谷氨酸受体的母体化合物的口服吸收性和其它粘膜吸收性的前药，其作为治疗或预防其中组2代谢型谷氨酸的疾病 受体被称为涉及，如：精神分裂症，焦虑症及其相关疾病，抑郁症，双相情感障碍，癫痫，发育障碍，睡眠障碍和其他神经精神疾病; 药物依赖，认知障碍，阿尔茨海默病，亨廷顿氏舞蹈病，帕金森氏病，与肌肉紧张相关的运动障碍，脑缺血，脑功能不全，脊髓障碍，头痛和其他神经系统疾病。

公开(公告)号：US08642626B2

公开(公告)日：2014-02-04

申请号：US13812437

申请日：2011-07-29

申请人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto

发明人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto

IPC分类号： A61K31/4439 ,  A61K31/415 ,  C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D403/06 ,  C07D401/06

CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04

摘要： Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.

摘要翻译： 本发明提供由式[I]表示的新化合物或其对II类代谢型谷氨酸（m-Glu）受体具有拮抗作用的药学上可接受的盐。 化合物或其药学上可接受的盐可用作疾病的预防或治疗剂，例如新的情绪障碍（抑郁和双相性精神障碍），焦虑症（广泛性焦虑症，惊恐障碍，强迫症，社会焦虑症， 创伤性应激障碍，特异性恐惧症和急性应激障碍），精神分裂症，阿尔茨海默病，认知功能障碍，痴呆，药物依赖，惊厥，震颤，疼痛，睡眠障碍等。

公开(公告)号：US08618312B2

公开(公告)日：2013-12-31

申请号：US12950609

申请日：2010-11-19

申请人： Mitsuaki Hirotsuka ,  Joji Sasaki ,  Hiroaki Kamiyama ,  Motoko Oshida ,  Takaaki Ishii

发明人： Mitsuaki Hirotsuka ,  Joji Sasaki ,  Hiroaki Kamiyama ,  Motoko Oshida ,  Takaaki Ishii

IPC分类号： C07D327/04 ,  C07D317/72

CPC分类号： C12P7/62 ,  C07C67/31 ,  C07C67/313 ,  C07C67/32 ,  C07C67/327 ,  C07C67/343 ,  C07C2602/18 ,  C07D317/72 ,  C07C69/757 ,  C07C69/732

摘要： Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative.

摘要翻译： 作为代谢型谷氨酸受体调节剂有用的双环[3.1.0]己烷衍生物的制备可以通过以下制备方法来实现：包括将由式（II）表示的化合物转化成由式（III）表示的化合物与 在不使用昂贵的光学活性羟基羟基酯作为起始原料的情况下，在微生物衍生的酶的存在下，不需要超低温反应的氟化反应。 此外，由于不对称合成可以在更接近最终产物的阶段进行，所以制造方法可用作可大量生产双环[3.1.0]己烷衍生物的制备方法。

公开(公告)号：US20130197217A1

公开(公告)日：2013-08-01

申请号：US13824174

申请日：2011-09-30

申请人： Takeshi Kuwada ,  Mitsukane Yoshinaga ,  Tomoko Ishizaka ,  Daisuke Wakasugi ,  Shin-ichi Shirokawa ,  Nobutaka Hattori ,  Youichi Shimazaki ,  Naoki Miyakoshi

发明人： Takeshi Kuwada ,  Mitsukane Yoshinaga ,  Tomoko Ishizaka ,  Daisuke Wakasugi ,  Shin-ichi Shirokawa ,  Nobutaka Hattori ,  Youichi Shimazaki ,  Naoki Miyakoshi

IPC分类号： C07D249/12 ,  C07D403/10 ,  C07D401/10 ,  C07D401/04 ,  C07D451/06 ,  C07D413/10 ,  C07D491/107 ,  C07D498/08

CPC分类号： C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D405/12 ,  C07D413/10 ,  C07D413/14 ,  C07D451/06 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

摘要： The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.

摘要翻译： 本发明提供对精氨酸 - 加压素1b受体或其药学上可接受的盐具有拮抗作用的由式（1A）表示的1,2,4-三唑酮衍生物，并提供包含该化合物或其盐作为活性物质的药物组合物 成分，特别是在疾病如情绪障碍，焦虑障碍，精神分裂症，阿尔茨海默病，帕金森病，亨廷顿舞蹈病，进食障碍，高血压，胃肠道疾病，药物成瘾，癫痫，脑梗死等疾病中表现出有利的药代动力学的治疗或预防药物 ，脑缺血，脑水肿，头部损伤，炎症，免疫相关疾病或脱发。

公开(公告)号：US20130137865A1

公开(公告)日：2013-05-30

申请号：US13814869

申请日：2011-08-11

申请人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto ,  Hideaki Amada ,  Hiroki Urabe ,  Rie Nishikawa ,  Shuhei Kashiwa ASHIWA

发明人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto ,  Hideaki Amada ,  Hiroki Urabe ,  Rie Nishikawa ,  Shuhei Kashiwa ASHIWA

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D403/04 ,  C07D231/38

CPC分类号： C07D413/14 ,  C07D231/38 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04

摘要： A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.

摘要翻译： 由式[I]表示的化合物和所述化合物的药学上可接受的盐是对II族代谢型谷氨酸（mGlu）受体具有拮抗作用的新化合物及其药学上可接受的盐，并且作为新的预防或治疗剂是有效的 用于诸如情绪障碍（抑郁障碍，双相情感障碍等），焦虑障碍（广泛性焦虑症，恐慌症，强迫症，社会焦虑症，创伤后应激障碍，特异性恐怖症，急性应激障碍等） ，精神分裂症，阿尔茨海默病，认知障碍，痴呆，药物依赖，抽搐，发抖，疼痛，睡眠障碍等。

公开(公告)号：US08420115B2

公开(公告)日：2013-04-16

申请号：US11628062

申请日：2005-05-25

申请人： Hiroshi Ikuta ,  Toshio Yajima

发明人： Hiroshi Ikuta ,  Toshio Yajima

IPC分类号： A61K9/10

CPC分类号： A61K9/0095 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/5026 ,  A61K31/7048

摘要： Disclosed herein are oral preparations and their production process. The oral preparations are each composed of a complex and a coating composition applied on the complex. The complex has been obtained by dispersing or dissolving a drug having an unpleasant taste and a gastric high-molecular compound in a low melting-point substance heated to and molten at its melting point or higher and granulating the resulting mixture. The coating composition is composed of an insoluble high-molecular compound and a disintegrator at a weight ratio of from 80:20 to 99:1. In the form of microparticles or the like that contain the drug having the unpleasant taste, each oral preparation according to the present invention can maintain the masking of the unpleasant taste of the drug and the release profile of the drug even under acidic conditions.

摘要翻译： 本文公开了口服制剂及其制备方法。 口服制剂各自由应用于复合物的复合物和涂料组合物组成。 通过将具有令人不愉快的味道的药物和胃高分子化合物分散或溶解在加热至其熔点或熔点以上的熔融物质的低熔点物质中并将所得混合物造粒而获得复合物。 涂料组合物由不溶解的高分子化合物和崩解剂组成，重量比为80:20至99:1。 以含有不愉快味道的药物的微粒等的形式，即使在酸性条件下，本发明的口服制剂也能够保持药物的令人不快的味道和药物的释放特性的掩蔽。

公开(公告)号：US20120316177A1

公开(公告)日：2012-12-13

申请号：US13578323

申请日：2011-02-10

申请人： Noriyuki Hirasawa ,  Nobuyoshi Kamikido ,  Akihiko Tasaki ,  Shusei Ito

发明人： Noriyuki Hirasawa ,  Nobuyoshi Kamikido ,  Akihiko Tasaki ,  Shusei Ito

IPC分类号： A61K31/501 ,  A61P11/06

CPC分类号： A61K31/501 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2095

摘要： Disclosed is a sustained release preparation which releases a poorly soluble medicinal agent in a pH-independent manner. Also disclosed is a sustained release preparation which is capable of controlling the Cmax of a medicinal agent to an adequate amount and is thus capable of maintaining the level of the medicinal agent in the blood to a level at which medicinal effects can be expected for a long period of time. Specifically disclosed is a sustained release preparation which is characterized by containing a pharmaceutically acceptable salt of 4-bromo-6-[3-(4-chlorophenyl)propoxy]-5-(3-pyridylmethylamino)-3(2H)-pyridazinone, and hypromellose. An organic acid is blended in the sustained release preparation in an amount of less than 1% by mass.

摘要翻译： 公开了一种以pH不依赖的方式释放难溶性药物的缓释制剂。 还公开了一种能够将药剂的Cmax控制在足够量的缓释制剂，因此能够将血液中的药剂的水平维持在长期以来可以预期药效的水平 一段的时间。 具体公开的是持续释放制剂，其特征在于含有4-溴-6- [3-（4-氯苯基）丙氧基] -5-（3-吡啶基甲基氨基）-3（2H） - 哒嗪酮的药用盐， 羟丙甲纤维素 持续释放制剂中的有机酸以小于1质量％的量共混。

公开(公告)号：US08329694B2

公开(公告)日：2012-12-11

申请号：US11993652

申请日：2006-06-22

申请人： Taro Kiyoto ,  Tadashi Tanaka ,  Yasuhiro Tsutsui ,  Junichi Ando ,  Mai Motono ,  Yasuko Kawaguchi ,  Toshiya Noguchi ,  Yasunobu Ushiki ,  Fumihito Ushiyama ,  Hiroki Urabe

发明人： Taro Kiyoto ,  Tadashi Tanaka ,  Yasuhiro Tsutsui ,  Junichi Ando ,  Mai Motono ,  Yasuko Kawaguchi ,  Toshiya Noguchi ,  Yasunobu Ushiki ,  Fumihito Ushiyama ,  Hiroki Urabe

IPC分类号： A61K31/495

CPC分类号： C07D405/14 ,  C07D215/227 ,  C07D401/06 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

摘要： A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.

摘要翻译： 由通式表示的含氮杂环化合物或其药学上可接受的盐，其具有强的抗菌活性和高安全性。 因此，这些化合物可用作抗革兰氏阳性细菌，革兰氏阴性细菌和耐药细菌的抗菌剂。