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1. 发明申请

US20090105136A1 NPY Y2 Agonist for Use as Therapeutic Agent for Disease Accompanied by Diarrhea 审中-公开
标题翻译： NPY Y2激动剂用作腹泻伴随疾病的治疗剂
公开(公告)号：US20090105136A1
公开(公告)日：2009-04-23
申请号：US11921483
申请日：2006-06-06
申请人： Jun Suzuki , Ryuichi Moriya , Hiroyasu Hirose , Akio Kanatani
发明人： Jun Suzuki , Ryuichi Moriya , Hiroyasu Hirose , Akio Kanatani
IPC分类号： A61K38/16 , C07K14/00 , G01N33/53 , A61P1/12 , C12Q1/02 , G01N33/68
CPC分类号： G01N33/5041 , A61K38/22 , G01N33/5023 , G01N33/74 , G01N2333/5755 , G01N2800/06
摘要： An NPY Y2 agonist is used as a therapeutic agent for a disease accompanied by diarrhea. A compound capable of treating the disease can be evaluated and screened by examining the compound on the targeting to an NPY Y2 receptor. An agent capable of inhibiting the diarrhea by a novel mechanism of action; and a method for evaluation of a compound, including the screening for the agent.
摘要翻译：使用NPY Y2激动剂作为伴有腹泻的疾病的治疗剂。可以通过检查靶向化合物至NPY Y2受体来评估和筛选能够治疗该疾病的化合物。能够通过新的作用机制抑制腹泻的药剂; 以及化合物的评价方法，包括筛选试剂。

2. 发明申请

US20090029406A1 Npy Y4 Agonist as Therapeutic Agent for Disease Accompanied by Intestinal Tract Dysfunction 审中-公开
标题翻译： Npy Y4激动剂作为伴随肠道功能障碍的疾病治疗剂
公开(公告)号：US20090029406A1
公开(公告)日：2009-01-29
申请号：US12223573
申请日：2007-02-23
申请人： Jun Suzuki , Ryuichi Moriya , Hiroyasu Hirose , Tetsuya Kanno , Akio Kanatani
发明人： Jun Suzuki , Ryuichi Moriya , Hiroyasu Hirose , Tetsuya Kanno , Akio Kanatani
IPC分类号： G01N33/68 , G01N33/53 , C12Q1/02 , C07K2/00
CPC分类号： C07K14/57545 , A61K38/00 , A61K38/22 , G01N33/5023 , G01N33/5041 , G01N2333/5755 , G01N2800/06
摘要： The present invention has its object to provide an agent capable of ameliorating the intestinal tract dysfunction through a novel mechanism of action. It also has its object to provide a method for the evaluation of a compound, including the screening of the agent. A disease accompanied by intestinal tract dysfunction can be ameliorated or treated by using an NPY Y4 agonist as a therapeutic agent. A compound capable of ameliorating or treating a disease accompanied by intestinal tract dysfunction can be evaluated or screened by evaluating a compound targeting to an NPY Y4 receptor.
摘要翻译：本发明的目的是提供能够通过新的作用机制改善肠道功能障碍的药剂。本发明的目的还在于提供一种化合物的评估方法，包括筛选试剂。伴随肠道功能障碍的疾病可以通过使用NPY Y4激动剂作为治疗剂来改善或治疗。可以通过评估靶向NPY Y4受体的化合物来评估或筛选能够改善或治疗伴随肠道功能障碍的疾病的化合物。

3. 发明申请

US20100184648A1 Therapeutic agent for non-alcoholic fatty liver disease, and screening method for drug candidate compound for treatment or prevention of non-alcoholic fatty liver disease 审中-公开
标题翻译：非酒精性脂肪肝疾病的治疗剂和用于治疗或预防非酒精性脂肪性肝病的药物候选化合物的筛选方法
公开(公告)号：US20100184648A1
公开(公告)日：2010-07-22
申请号：US11887060
申请日：2006-03-28
申请人： Akira Gomori , Akane Ishihara , Hisashi Iwasa , Jun Suzuki , Makoto Ito , Akio Kanatani
发明人： Akira Gomori , Akane Ishihara , Hisashi Iwasa , Jun Suzuki , Makoto Ito , Akio Kanatani
IPC分类号： A61K38/12 , A61K31/506 , A61P1/16 , G01N33/53 , C12Q1/02 , C12Q1/68
CPC分类号： G01N33/74 , A61K31/00 , G01N2500/00 , G01N2800/085
摘要： A therapeutic agent for a non-alcoholic fatty liver disease comprising a melanin-concentrating hormone receptor antagonist as an active ingredient, which is developed based on a novel mechanism of action that a melanin-concentrating hormone receptor is involved in non-alcoholic fatty liver diseases. A method for screening a drug candidate compound for the treatment or prevention of a non-alcoholic fatty liver disease by utilizing the mechanism.
摘要翻译：一种非酒精性脂肪肝疾病的治疗剂，其包含黑色素浓缩激素受体拮抗剂作为活性成分，其基于黑色素浓缩激素受体参与非酒精性脂肪肝疾病的新作用机制而开发。一种通过利用该机制筛选用于治疗或预防非酒精性脂肪性肝病的药物候选化合物的方法。

4. 发明申请

US20080118436A1 Pathological Animal Model For Non-Alcoholic Fatty Hepatitis 审中-公开
标题翻译：非酒精性脂肪性肝炎的病理动物模型
公开(公告)号：US20080118436A1
公开(公告)日：2008-05-22
申请号：US11663155
申请日：2005-09-13
申请人： Jun Suzuki , Hisashi Iwaasa , Minoru Sasaki , Makoto Ito , Akio Kanatani
发明人： Jun Suzuki , Hisashi Iwaasa , Minoru Sasaki , Makoto Ito , Akio Kanatani
IPC分类号： A61K49/00 , A61K31/65
CPC分类号： A61K49/0008 , G01N33/5088 , G01N2800/085
摘要： An object of the present invention is to provide a pathologic model animal more accurately reflecting the pathologic conditions of nonalcoholic steatohepatitis patients, and the present invention provides the pathologic model animal for nonalcoholic steatohepatitis produced by continuously administering a tetracycline antibiotic to an animal having its body weight significantly increased compared with that of a group fed with a normal diet by feeding it with a high-fat diet.
摘要翻译：本发明的目的是提供一种更准确地反映非酒精性脂肪性肝炎患者的病理状况的病理模型动物，本发明提供了通过将四环素抗生素连续给予其体重的动物而产生的非酒精性脂肪性肝炎的病理模型动物通过喂养高脂肪饮食，与正常饮食组相比显着增加。

5. 发明授权

US08268842B2 Fused ring 4-oxopyrimidine derivative 有权
标题翻译：稠环4-氧代嘧啶衍生物
公开(公告)号：US08268842B2
公开(公告)日：2012-09-18
申请号：US12378163
申请日：2009-02-11
申请人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/519 , A61K31/517 , A01N43/54
CPC分类号： C07D239/91 , A61K31/517 , A61K31/55 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/08 , A61K2300/00
摘要： The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).]
摘要翻译：本发明提供下述式（I）表示的化合物或其药学上可接受的盐，其具有组胺H3受体拮抗剂或反向激动剂活性，可用于预防或治疗代谢性疾病，循环系统疾病或神经系统疾病 [其中，例如，Ar为通过从苯中除去2个氢原子形成的二价基团，X 1为氮原子，硫原子或氧原子，R 1为5〜6元杂芳基，环A为5- 至6元杂芳基环，R 2和R 3为氨基或烷基氨基，X 2由式（II）表示：（其中R 4和R 5为低级烷基，n为2至4的整数）。

6. 发明授权

US07834182B2 Piperidine derivative 失效
标题翻译：哌啶衍生物
公开(公告)号：US07834182B2
公开(公告)日：2010-11-16
申请号：US12381099
申请日：2009-03-06
申请人： Norikazu Ohtake , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani , Sayaka Mizutani
发明人： Norikazu Ohtake , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani , Sayaka Mizutani
IPC分类号： C07D401/14 , C07D403/14 , A61K31/4545 , A61K31/496 , A61K31/454 , A61K31/4523 , A61K31/506 , A61P3/04 , A61P3/10 , C07D401/12 , C07D401/02 , C07D401/06
CPC分类号： C07D211/58 , A61K31/454
摘要： Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia, repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X1 and X2 independently represent a nitrogen atom or CH; Y represents a specific group; X3 represents Os—(CH2)m; R1 and R2 independently resent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.
摘要翻译：提供组胺H3受体拮抗剂; 代谢系统疾病如肥胖症，糖尿病，激素分泌障碍，高脂血症，痛风，脂肪肝，循环系统疾病，例如心动过速，急性/充血性心功能不全，心肌梗塞，冠状动脉硬化等的预防和/或补救措施，高血压，肾病，睡眠障碍和伴有睡眠障碍的各种疾病，例如特发性睡眠过多，重度睡眠过多，睡眠周期性运动障碍，睡眠呼吸暂停综合征，昼夜节律紊乱，慢性疲劳综合征，REM睡眠障碍，老年性失眠，夜间工人睡眠躁狂，特发性失眠，重复性失眠，真实失眠，电解质代谢紊乱; 注意力缺陷/多动症，记忆障碍，阿尔茨海默氏病，帕金森病，睡眠障碍，识别障碍，运动障碍，中枢神经系统疾病和中枢神经系统疾病如贪食症，情绪障碍，忧郁症，焦虑症，癫痫，del妄，感觉异常，dysosmia，癫痫，吗啡抵抗，麻醉依赖，酒精依赖。组胺H3受体拮抗剂包括式（I）的哌啶衍生物化合物[其中X1和X2独立地表示氮原子或CH; Y表示特定组; X3表示Os-（CH2）m; R1和R2分别独立地表示氢原子，卤素原子，直链或支链低级烷基，低级烷氧基或被2或3个氟原子取代的乙酰基; s为0或1; 和m是使（m + s）0或1至4]的整数]或其药学上可接受的盐。

7. 发明授权

US07790731B2 Crystal form of 2-methyl-3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone 失效
标题翻译： 2-甲基-3- {4- [3-（1-吡咯烷基）丙氧基]苯基} -5-三氟甲基-4（3H） - 喹唑啉酮的晶型
公开(公告)号：US07790731B2
公开(公告)日：2010-09-07
申请号：US11884138
申请日：2006-02-13
申请人： Akio Kanatani , Nagaaki Sato , Tsuyoshi Nagase , Shigeru Tokita
发明人： Akio Kanatani , Nagaaki Sato , Tsuyoshi Nagase , Shigeru Tokita
IPC分类号： A61K31/517
CPC分类号： C07D239/91 , A61K31/517 , A61K45/06
摘要： The present invention is directed to a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that is useful for example in the treatment of sleep disorders or various sleep disorder-associated diseases.
摘要翻译：本发明涉及例如在治疗中有用的2-甲基3- {4- [3-（1-吡咯烷基）丙氧基]苯基} -5-三氟甲基-4（3H） - 喹唑啉酮的I型晶体的睡眠障碍或各种睡眠障碍相关疾病。

8. 发明授权

US07547693B2 Piperidine derivative 失效
标题翻译：哌啶衍生物
公开(公告)号：US07547693B2
公开(公告)日：2009-06-16
申请号：US10574087
申请日：2004-09-21
申请人： Norikazu Ohtake , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani , Sayaka Mizutani
发明人： Norikazu Ohtake , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani , Sayaka Mizutani
IPC分类号： C07D401/14 , C07D401/12 , C07D401/02 , C07D401/06 , A61K31/4545 , A61K31/496 , A61K31/454 , A61K31/4523 , C07D403/14 , A61K31/506 , A61P3/04 , A61P3/10
CPC分类号： C07D211/58 , A61K31/454
摘要： Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnnia, repetitive hypersomnnia, true hypersomnnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder, and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X1 and X2 independently represent a nitrogen atom or CH; Y represents a specific group; X3 represents Os—(CH2)m; R1 and R2 independently represent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.
摘要翻译：提供组胺H3受体拮抗剂; 代谢系统疾病如肥胖症，糖尿病，激素分泌障碍，高脂血症，痛风，脂肪肝，循环系统疾病，例如心动过速，急性/充血性心功能不全，心肌梗塞，冠状动脉硬化等的预防和/或补救措施，高血压，肾病，睡眠障碍和伴有睡眠障碍的各种疾病，例如特发性超嗜酸症，重复性嗜睡症，真实嗜睡症，发作性睡眠，睡眠周期性运动障碍，睡眠呼吸暂停综合征，昼夜节律紊乱，慢性疲劳综合征，REM睡眠障碍，老年性失眠，夜间工作人员睡眠躁狂，特发性失眠，重复性失眠，真实失眠，电解质代谢障碍，以及中枢和周围神经系统疾病如贪食症，情绪障碍，忧郁症，焦虑症，癫痫，del妄，痴呆，注射缺陷/多动症，记忆障碍，阿尔茨海默病，帕金森病，睡眠障碍，识别障碍，运动障碍，感觉异常，dysosmia，癫痫，吗啡抵抗，麻醉依赖，酒精依赖。组胺H3受体拮抗剂包括式（I）的哌啶衍生物化合物[其中X1和X2独立地表示氮原子或CH; Y表示特定组; X3表示Os-（CH2）m; R1和R2独立地表示氢原子，卤素原子，直链或支链低级烷基，低级烷氧基或被2或3个氟原子取代的乙酰基; s为0或1; 和m是使（m + s）0或1至4]的整数]或其药学上可接受的盐。

9. 发明申请

US20090023163A1 Method of Measuring Enzyme Activity and Method of Evaluating Compound 审中-公开
标题翻译：测定酶活性的方法和评价化合物的方法
公开(公告)号：US20090023163A1
公开(公告)日：2009-01-22
申请号：US11886700
申请日：2006-03-29
申请人： Shigeru Tokita , Ken Shimamura , Yasuhisa Miyamoto , Hidefumi Kitazawa , Akio Kanatani
发明人： Shigeru Tokita , Ken Shimamura , Yasuhisa Miyamoto , Hidefumi Kitazawa , Akio Kanatani
IPC分类号： C12Q1/25 , G01N33/53
CPC分类号： C12Q1/25 , C12Q1/48 , G01N2333/91051 , G01N2500/04
摘要： It is intended to provide a method of measuring an activity, which is a method of measuring an activity of an enzymatic reaction in which a lipid-soluble reaction product is formed by catalyzing an addition reaction of two or more kinds of substrates, characterized by comprising a labeling step in which any one of the substrates is labeled, a reaction step in which an enzymatic reaction is carried out in the presence of an enzyme, all substrates and an acceptor, and a detection step in which the reaction product is detected by bringing the labeled molecule and a molecule to be detected close to each other via the acceptor and transferring an energy generated by the labeled molecule to the molecule to be detected, and a method of evaluating a compound utilizing the method of measuring an activity. By the methods of the invention, it is possible to perform a treatment from the enzymatic reaction to the measurement of an enzyme activity with the simple steps and it is possible to provide a method of measuring an enzyme activity which can be applied to an HTS evaluation system.
摘要翻译：旨在提供测定活性的方法，该方法是通过催化两种或更多种基质的加成反应来测量其中形成脂溶性反应产物的酶反应的活性的方法，其特征在于包括标记任何一种底物的标记步骤，在酶的存在下进行酶反应的反应步骤，所有底物和受体，以及检测步骤，其中通过将待标记的分子和待检测的分子通过受体彼此接近并将由标记的分子产生的能量转移到待检测的分子上，以及使用测定活性的方法评估化合物的方法。通过本发明的方法，可以通过简单的步骤进行从酶反应到酶活性测定的处理，并且可以提供可应用于HTS评价的酶活性的测定方法系统。

10. 发明申请

US20070299070A1 2-Arylcarboxamide-Nitrogenous Heterocycle Compound 失效
标题翻译： 2-芳基甲酰胺 - 含氮杂环化合物
公开(公告)号：US20070299070A1
公开(公告)日：2007-12-27
申请号：US11663038
申请日：2005-09-30
申请人： Takao Suzuki , Minoru Moriya , Shunji Sakuraba , Sayaka Mizutani , Hisashi Iwaasa , Akio Kanatani
发明人： Takao Suzuki , Minoru Moriya , Shunji Sakuraba , Sayaka Mizutani , Hisashi Iwaasa , Akio Kanatani
IPC分类号： A61K31/5377 , A61K31/4025 , A61K31/4045 , A61P1/00 , A61P13/00 , A61P21/00 , A61P27/00 , A61P37/00 , A61P5/00 , C07D413/14 , C07D413/10 , C07D403/10 , C07D401/12 , C07D401/10 , C07D401/02 , C07D209/04 , A61P9/00 , A61P7/00 , A61P43/00 , A61P3/00 , A61P25/00 , A61P15/00 , A61P11/00 , A61K31/4439 , A61K31/454
CPC分类号： C07D209/42 , C07D235/24 , C07D401/12
摘要： A compound represented by the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents —N—, —CH—, et al; Y, represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.
摘要翻译：由式[I]表示的化合物：其中R 1和R 2相同或不同，各自表示C 1-6烷基，烷基，C 3-8环烷基等; R 3a，R 3b和R 4相同或不同，各自表示氢，C 1-6 烷基等; X表示-N-，-CH-等; Y表示单键，C 1-3亚烷基等; Y 2表示C 1-4亚烷基，氧（C 1-4烷基亚烷基）等; Ar 1表示单环芳族碳环基团，单环芳族杂环基团等; 和Ar 2代表5或6元芳族碳环基团，芳族杂环基团等。该化合物起着黑色素浓缩激素受体拮抗剂的作用，可用作例如肥胖症的治疗剂等。

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