公开(公告)号：US20100267695A1

公开(公告)日：2010-10-21

申请号：US12741307

申请日：2008-11-26

申请人： Satoshi Hayashibe ,  Shingo Yamasaki ,  Nobuyuki Shiraishi ,  Hiroaki Hoshii ,  Takahiko Tobe

发明人： Satoshi Hayashibe ,  Shingo Yamasaki ,  Nobuyuki Shiraishi ,  Hiroaki Hoshii ,  Takahiko Tobe

IPC分类号： A61K31/55 ,  A61K31/538 ,  A61K31/435 ,  A61K31/4365 ,  C07D223/32 ,  C07D265/34 ,  C07D495/04 ,  C07D491/048 ,  C07D221/16 ,  A61P25/22 ,  A61P25/16 ,  A61P25/28 ,  A61P25/24 ,  A61P25/06 ,  A61P25/30 ,  A61P25/18

CPC分类号： C07D209/94 ,  C07D221/16 ,  C07D223/32 ,  C07D265/34 ,  C07D333/78 ,  C07D401/06 ,  C07D401/12 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/06

摘要： [Problems] To provide a compound which is useful as an NMDA receptor antagonist.[Means for Solution] The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.

摘要翻译： [问题]提供可用作NMDA受体拮抗剂的化合物。 [解决方案]本发明人研究了具有NMDA受体拮抗作用的化合物，并证实本发明的稠合茚满酮化合物具有优异的NMDA受体拮抗作用，从而完成了本发明。 本发明的稠合吲哚化合物具有优异的NMDA受体拮抗作用，可用作阿尔茨海默氏病，脑血管性痴呆，帕金森病，难治性抑郁症，注意力缺陷多动障碍，偏头痛等的预防和/或治疗剂 。

公开(公告)号：US07815939B2

公开(公告)日：2010-10-19

申请号：US11458582

申请日：2006-07-19

申请人： Yuki Kasashima ,  Ippei Kurimoto ,  Hitoshi Kawai

发明人： Yuki Kasashima ,  Ippei Kurimoto ,  Hitoshi Kawai

IPC分类号： A61K9/24 ,  A61K9/16

CPC分类号： A61K9/5078 ,  A61K9/5047

摘要： Regarding an object of sufficient suppression of unpleasant taste in the oral cavity and quick dissolution in the gastrointestinal tract, which is generated when a drug having a strong unpleasant taste such as bitterness, astringency and the like is applied to a quickly disintegrating preparations in the oral cavity, this invention has achieved the aforementioned object for the first time by employing a constitution of coating a coat of a water-soluble polymer and a specified ratio of a pH-independent water-insoluble polymer and hydroxypropylcellulose.

摘要翻译： 关于在口腔中充分抑制不愉快味道和快速溶解在胃肠道中的目的，当将具有强烈令人不快的味道（例如苦味，涩味等）的药物施用于口服的快速崩解制剂时产生 本发明通过使用涂布水溶性聚合物的涂层和与pH无关的水不溶性聚合物和羟丙基纤维素的规定比例的结构第一次实现了上述目的。

公开(公告)号：US20100261770A1

公开(公告)日：2010-10-14

申请号：US12745755

申请日：2008-12-18

申请人： Masanori Suzuki ,  Masashi Ukai ,  Akiyoshi Ohtake ,  Mai Koda

发明人： Masanori Suzuki ,  Masashi Ukai ,  Akiyoshi Ohtake ,  Mai Koda

IPC分类号： A61K31/426 ,  A61P13/00

CPC分类号： A61K31/426 ,  A61K31/18 ,  A61K2300/00

摘要： [Problems] To provide a pharmaceutical composition which is useful as a pharmaceutical composition for improving lower urinary tract symptoms.[Means for Solution] A pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (R)-5-(2-{[2-(2-ethoxyphenoxy)ethyl)amino]propyl}-2-methoxybenzene-1-sulfonamide or a pharmaceutically acceptable salt thereof, as active ingredients, particularly a pharmaceutical composition for improving lower urinary tract symptoms, more specifically a pharmaceutical composition for improving lower urinary tract symptoms associated with benign prostatic hyperplasia.

摘要翻译： [问题]提供可用作改善下尿路症状的药物组合物的药物组合物。 [解决方案]包含（R）-2-（2-氨基噻唑-4-基）-4' - {2 - [（2-羟基-2-苯基乙基）氨基]乙基}乙酰苯胺或其药学上可接受的药物组合物 其盐和（R）-5-（2 - {[2-（2-乙氧基苯氧基）乙基）氨基]丙基} -2-甲氧基苯-1-磺酰胺或其药学上可接受的盐作为活性成分，特别是药物组合物 用于改善下尿路症状，更具体地说是用于改善与良性前列腺增生相关的下尿路症状的药物组合物。

公开(公告)号：US20100256151A1

公开(公告)日：2010-10-07

申请号：US12753415

申请日：2010-04-02

申请人： Junya OHMORI ,  Makoto KASAI ,  Takenori KIMURA ,  Noritaka HAMADA ,  Ryo MIZOGUCHI ,  Satoshi MIYAMOTO ,  Noriyuki KAWANO

发明人： Junya OHMORI ,  Makoto KASAI ,  Takenori KIMURA ,  Noritaka HAMADA ,  Ryo MIZOGUCHI ,  Satoshi MIYAMOTO ,  Noriyuki KAWANO

IPC分类号： A61K31/53 ,  C07D403/12 ,  A61P25/28

CPC分类号： A61K31/53 ,  C07D403/12

摘要： Anytime obtained is uniform crystal of N-(4-fluorophenyl)-N′-phenyl-N″-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound A) and/or N,N′-bis (4-fluorophenyl)-N″-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound B) as a medicament or a starting material for the preparation of the medicament, and provided are a fumarate of the compound A and/or the compound B having excellent stability and a novel crystal thereof. A salt of the compound A and/or the compound B with fumaric acid enables uniform crystal to be anytime obtained, and thus, it is a compound that is very useful as a medicament or a starting material for the preparation of the medicament having excellent stability.

摘要翻译： 得到的N-（4-氟苯基）-N'-苯基-N“ - （嘧啶-2-基甲基）-1,3,5-三嗪-2,4,6-三胺（化合物A）和 /或N，N'-二（4-氟苯基）-N“ - （嘧啶-2-基甲基）-1,3,5-三嗪-2,4,6-三胺（化合物B）作为药物或起始物 用于制备药物的材料，并且提供具有优异的稳定性和新颖结晶的化合物A和/或化合物B的富马酸盐。 化合物A和/或化合物B与富马酸的盐能够随时获得均匀的结晶，因此，作为制备具有优异稳定性的药物的药物或原料非常有用的化合物 。

公开(公告)号：US20100256113A1

公开(公告)日：2010-10-07

申请号：US12680301

申请日：2008-09-25

申请人： Kenichi Onda ,  Kenichiro Imamura ,  Fumie Sato ,  Hiroyuki Moritomo ,  Yasuharu Urano ,  Yuki Sawada ,  Naoki Ishibashi ,  Keita Nakanishi ,  Kazuhiro Yokoyama ,  Shigetada Furukawa ,  Kazuhiro Momose

发明人： Kenichi Onda ,  Kenichiro Imamura ,  Fumie Sato ,  Hiroyuki Moritomo ,  Yasuharu Urano ,  Yuki Sawada ,  Naoki Ishibashi ,  Keita Nakanishi ,  Kazuhiro Yokoyama ,  Shigetada Furukawa ,  Kazuhiro Momose

IPC分类号： A61K31/4709 ,  C07D215/233 ,  C07D405/12 ,  C07D401/12 ,  C07D413/12 ,  A61K31/47 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4725 ,  A61K31/55 ,  A61K31/553

CPC分类号： C07D401/12 ,  C07D215/233 ,  C07D401/06 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/107

摘要： As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.

摘要翻译： 作为对NAD（P）H氧化酶抑制剂的广泛研究的结果，本发明人发现，在2位具有被杂原子等取代的烷基的喹诺酮衍生物具有优异的NAD（P）H氧化酶 抑制活性，完成了本发明。 本发明的化合物具有基于NAD（P）H氧化酶抑制活性的活性氧产生抑制活性，因此可用作糖尿病预防和/或治疗药物，糖耐量异常，高脂血症，脂肪肝 ，糖尿病并发症等。

公开(公告)号：US20100240697A1

公开(公告)日：2010-09-23

申请号：US12740699

申请日：2008-10-30

申请人： Masanori Suzuki ,  Masashi Ukai ,  Akiyoshi Ohtake

发明人： Masanori Suzuki ,  Masashi Ukai ,  Akiyoshi Ohtake

IPC分类号： A61K31/4725 ,  A61P13/00

CPC分类号： A61K31/4725 ,  A61K31/426 ,  A61K2300/00

摘要： [Problems] To provide a pharmaceutical composition which is useful as a therapeutic agent for overactive bladder.[Means for Solution] A pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof, as active ingredients, in particular a pharmaceutical composition for improving various symptoms accompanying overactive bladder, such as urinary urgency, pollakiuria and/or urinary incontinence

摘要翻译： [问题]提供可用作膀胱过度活动症的治疗剂的药物组合物。 [解决方案]包含（R）-2-（2-氨基噻唑-4-基）-4' - {2 - [（2-羟基-2-苯基乙基）氨基]乙基}乙酰苯胺或其药学上可接受的药物组合物 的盐和（3R） - 奎宁环-3-基（1S）-1-苯基-1,2,3,4-四氢异喹啉-2-羧酸酯或其药学上可接受的盐作为活性成分，特别是用于 改善伴随膀胱过动症的各种症状，如尿急，尿频和/或尿失禁

公开(公告)号：US20100227866A1

公开(公告)日：2010-09-09

申请号：US12600894

申请日：2008-05-26

申请人： Hiroyuki Hisamichi ,  Itsuro Shimada ,  Tsukasa Ishihara ,  Tomofumi Takuwa ,  Takafumi Shimizu ,  Noriko Ishikawa ,  Kyoichi Maeno ,  Norio Seki

发明人： Hiroyuki Hisamichi ,  Itsuro Shimada ,  Tsukasa Ishihara ,  Tomofumi Takuwa ,  Takafumi Shimizu ,  Noriko Ishikawa ,  Kyoichi Maeno ,  Norio Seki

IPC分类号： A61K31/4725 ,  C07D401/12 ,  C07D401/14 ,  A61K31/53 ,  A61K31/506 ,  A61P1/00 ,  A61P35/00

CPC分类号： A61K31/4725 ,  A61K31/435 ,  A61K31/439 ,  A61K31/445 ,  A61K31/472 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  C07D217/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04

摘要： [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS).[Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

摘要翻译： [问题]提供药物，特别是可用作肠易激综合征（IBS）治疗剂的化合物。 [解决问题的手段]发现在4-位具有酰胺基的四氢异喹啉-1-酮衍生物或其药学上可接受的盐具有优异的铃蟾肽2（BB2）受体拮抗作用。 还发现四氢异喹啉-1-酮衍生物对肠运动障碍是高度有效的。 从上述可以看出，本发明的四氢异喹啉-1-酮衍生物可用作与BB2受体，特别是IBS相关疾病的治疗剂。

公开(公告)号：US07786106B2

公开(公告)日：2010-08-31

申请号：US12356376

申请日：2009-01-20

申请人： Tsukasa Ishihara ,  Fukushi Hirayama ,  Keizo Sugasawa ,  Yuji Koga ,  Takeshi Kadokura ,  Takeshi Shigenaga

发明人： Tsukasa Ishihara ,  Fukushi Hirayama ,  Keizo Sugasawa ,  Yuji Koga ,  Takeshi Kadokura ,  Takeshi Shigenaga

IPC分类号： A61K31/551 ,  C07D243/08

CPC分类号： C07D401/12 ,  C07D211/26 ,  C07D401/14 ,  C07H15/203 ,  C07H15/26

摘要： There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4′-bromo-2′-[(5-chloro-2-pyridyl) carbamoyl]-6′-β-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2′-(2-acetamido-2-deoxy-β-D-glucopyranosyloxy)-4′-bromo-6′-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.

摘要翻译： 提供了基于活化凝血因子X的抑制具有抗凝血作用的化合物，并且可用作血栓形成或栓塞引起的疾病的抗凝剂或预防/治疗剂。 有效成分是诸如4'-溴-2' - [（5-氯-2-吡啶基）氨基甲酰基] -6' - （b-）-D-吡喃半乳糖氧基-1-异丙基哌啶-4-甲酰苯胺，2' - （ -2'-乙酰氨基-2-脱氧-α-D-吡喃葡萄糖基氧基）-4'-溴-6' - [（5-氯-2-吡啶基）氨基甲酰基] -1-异丙基哌啶-4-甲酰苯胺等或其盐 。

公开(公告)号：US20100216778A1

公开(公告)日：2010-08-26

申请号：US12714608

申请日：2010-03-01

申请人： Nobuaki TAKESHITA

发明人： Nobuaki TAKESHITA

IPC分类号： A61K31/551 ,  A61K31/4409 ,  A61K31/415 ,  A61K31/165 ,  A61P29/00 ,  A61P19/02

CPC分类号： A61K31/166 ,  A61K31/4164 ,  A61K31/4409 ,  A61K31/551

摘要： Since a ROCK inhibitor exerts a potent analgesic effect by a single dose after the onset of a cartilage-related disease such as osteoarthritis, and can regenerate or suppress destruction of cartilage tissue and alleviate pain associated with cartilage diseases by multiple doses, administration of an therapeutically effective amount of the ROCK inhibitor to a patient with cartilage-related disease such as osteoarthritis or rheumatoid arthritis can treat the patient with cartilage-related disease and the ROCK inhibitor is thus useful.

摘要翻译： 由于ROCK抑制剂在与软骨相关疾病如骨关节炎发生之后通过单次剂量发挥有效的镇痛作用，并且可以再生或抑制软骨组织的破坏并且通过多次剂量减轻与软骨疾病相关的疼痛，施用治疗 对软骨相关疾病如骨关节炎或类风湿性关节炎的患者的有效量的ROCK抑制剂可以治疗患有软骨相关疾病的患者，因此ROCK抑制剂是有用的。

公开(公告)号：US07758317B2

公开(公告)日：2010-07-20

申请号：US10571122

申请日：2004-09-08

申请人： Koji Mukai ,  Fujio Ito ,  Satoru Takahashi

发明人： Koji Mukai ,  Fujio Ito ,  Satoru Takahashi

IPC分类号： F04B3/00 ,  F04B5/00

CPC分类号： G01N30/12 ,  G01N1/2226 ,  G01N7/16 ,  G01N2030/128 ,  G01N2030/205

摘要： A method for analysis of solvent evaporation patterns includes: continuously evacuating the gas of a single-component or multicomponent solvent evaporated under desired evaporation conditions from an object containing the single-component or multicomponent solvent housed in an airtight container, with evacuation means from the airtight container to an exhaust path connected to an exhaust port of the evacuation means; sampling a gas at predetermined time intervals from a desired point between the airtight container and the outlet of the exhaust path with the continuous evacuation maintained; measuring the solvent gas contained in the sampled gas; and determining an evaporation pattern of the solvent from the object under the desired evaporation conditions, from results of the measurement.

摘要翻译： 用于分析溶剂蒸发图案的方法包括：将所需蒸发条件下蒸发的单组分或多组分溶剂的气体从包含容纳在气密容器中的单组分或多组分溶剂的物体中连续排出，并从气密 容器连接到排气装置的排气口的排气路径; 从密封容器和排气通道出口之间的期望点以预定的时间间隔取样气体，同时保持连续排气; 测量采样气体中所含的溶剂气体; 以及在所需的蒸发条件下从测量结果中确定来自物体的溶剂的蒸发图案。