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1. 发明申请

WO2013051159A1 NOP RECEPTOR ANTAGONIST 审中-公开
标题翻译： NOP受体拮抗剂
公开(公告)号：WO2013051159A1
公开(公告)日：2013-04-11
申请号：PCT/JP2011/073464
申请日：2011-10-05
申请人： NIPPON SHINYAKU CO., LTD. , OKANO, Masahiko , OYAMA, Tatsuya
发明人： OKANO, Masahiko , OYAMA, Tatsuya
IPC分类号： C07D239/94 , A61K31/517 , A61P3/04 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00
CPC分类号： C07D239/94
摘要： A novel excellent non-opioid branch of the opioid peptide family of receptors antagonist is provided, which exhibit an analgesic effect on a varuous pains. The present invention is directed to a non-opioid branch of the opioid peptide family of receptors antagonist represented by the general formula [1] or a pharmaceutically acceptable salt thereof. In the general formula [1], R 1 represents hydrogen or the like, R 2 represents hydrogen or the like, R 3 and R 4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen, R 5 is combined with R 6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy, R 6 represents (1) alkyl, (2) cycloalkyl, (3) phenyl, (4) a 5- to 10-membered aromatic heterocyclic group containing 1 to 3 heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or (5) -N(R 61 )(R 62 ).
摘要翻译：提供了阿片类肽受体拮抗剂家族的优异的非阿片样物质分支，其对变性疼痛具有镇痛作用。本发明涉及由通式[1]表示的受体拮抗剂阿片样肽家族的非阿片样物质分支或其药学上可接受的盐。在通式[1]中，R 1表示氢等，R 2表示氢等，R 3和R 4相同或不同，表示氢，烷基，烷氧基或卤素，R 5与R 6一起表示亚烷基或代表氢，羟基，烷基，苯基或烷氧基，R6表示（1）烷基，（2）环烷基，（3）苯基，（4）含有1至3个选自以下的杂原子的5至10元芳族杂环基：的氮原子，氧原子和硫原子，或（5）-N（R61）（R62）。

2. 发明申请

WO2008093207A1 INTAKE SYSTEM FOR VEHICLE INTERNAL COMBUSTION ENGINE 审中-公开
标题翻译：用于车辆内燃机的吸入系统
公开(公告)号：WO2008093207A1
公开(公告)日：2008-08-07
申请号：PCT/IB2008/000191
申请日：2008-01-29
申请人： TOYOTA JIDOSHA KABUSHIKI KAISHA , SAITO, Haruhiko , OYAMA, Tatsuya
发明人： SAITO, Haruhiko , OYAMA, Tatsuya
IPC分类号： F02B27/02 , F02M35/02 , F02M35/10
CPC分类号： F02M35/10321 , F02B27/005 , F02M35/02 , F02M35/10013 , F02M35/108 , F02M35/161 , Y02T10/146
摘要： An intake system (10, 20) for a vehicle internal combustion engine is provided in which a first air intake duct (16), having an air intake inlet (16a) to inhale external air, is connected to an air cleaner box (14). A second air intake duct (17, 27) is also connected to the air cleaner box. The air intake inlet is closer to the air cleaner box than the second air intake duct is. The cross section area of a second air intake duct is greater than the cross section area of the first air intake duct. The center axis of the second air intake duct at an end on the side of a second air intake opening (12, 22) intersects with the center axis of the first air intake duct at an end on the side of a first air intake opening (11).
摘要翻译：提供了一种用于车辆内燃机的进气系统（10,20），其中具有吸入外部空气的进气口（16a）的第一进气管道（16）连接到空气滤清器箱（14）。第二进气管道（17,27）也连接到空气滤清器箱。进气口比第二进气管更靠近空气滤清器箱。第二进气管道的横截面面积大于第一进气管道的横截面面积。在第二进气口（12,22）侧的端部处的第二进气管道的中心轴线与第一进气口侧的端部处的第一进气管道的中心轴线相交 11）。

3. 发明公开

EP1275657A1 PEPTIDE DERIVATIVES AND MEDICINAL COMPOSITIONS 审中-公开
标题翻译： PEPTID-DERIVATE UND MEDIZINISCHE ZUSAMMENSETZUNGEN
公开(公告)号：EP1275657A1
公开(公告)日：2003-01-15
申请号：EP01921846.0
申请日：2001-04-16
申请人： Nippon Shinyaku Co., Ltd.
发明人： ISHIYAMA, Kouichi , TEREDA, Tomohiro , OYAMA, Tatsuya , OHGI, Tadaaki
IPC分类号： C07K5/062 , C07K5/065 , C07K5/083 , C07K5/087 , C07K5/103 , C07K5/107 , A61P25/04 , A61P25/22 , A61K38/05 , A61K38/06 , A61K38/07 , A61P43/00
CPC分类号： C07K5/1016 , A61K38/00 , C07K5/0812 , C07K5/1027 , C07K7/56
摘要： An object of the present invention is to provide a novel nociceptin receptor agonist.
The present invention relates to a peptide derivative represented by the following general formula (1):
(in which A represents alkylene, -(CH 2 )nCO- or a group represented by the following formula (2) or (3):

wherein n represents an integer of 1 to 8; X and Y are same or different and each represents -CONH- or -CH 2 NH-; R 1 , R 2 and R 3 are same or different and each represents alkyl, aryl or heteroaryl; Z represents -CON(R 4 )R 5 or -CH 2 N(R 4 )R 5 ; and R 4 and R 5 are same or different and each represents hydrogen, alkyl, aryl or heteroaryl) or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition according to the present invention is useful as a nociceptin receptor agonist.
摘要翻译：本发明的目的是提供一种新的伤害感受肽受体激动剂。本发明涉及由以下通式（1）表示的肽衍生物：（其中A表示亚烷基， - （CH 2）nCO-或由下式（2）或（3）表示的基团：其中n表示1至8的整数; X和Y相同或不同，各自表示-CONH-或-CH 2 NH-; R 1，R 2和R 3相同或不同的，并且各自表示烷基，芳基或杂芳基; Z表示-CON（R 4）R 5或-CH 2 N（R 4）R 5;且R 4和R 5是相同或不同，各自表示氢，烷基，芳基或杂芳基）或其药学上可接受的盐。根据本发明的药物组合物可用作伤害感受肽受体激动剂。

4. 发明公开

EP1371376A1 ANTIPRURITICS 审中-公开
标题翻译：抗菌药品
公开(公告)号：EP1371376A1
公开(公告)日：2003-12-17
申请号：EP02705294.3
申请日：2002-03-18
申请人： Nippon Shinyaku Co., Ltd.
发明人： OYAMA, Tatsuya , SAKANO, Kyoko
IPC分类号： A61K45/00 , A61K31/517 , A61P17/04 , C07D239/94 , C07D239/96 , C07D401/06
CPC分类号： C07D401/06 , A61K31/00 , A61K31/517 , C07D239/94
摘要： The present invention relates to an antipruritic agent comprising a nociceptin antagonist as an active ingredient. The nociceptin antagonist can be used as a preventive or remedy for diseases associated with itching (for example, atopic dermatitis and urticaria), local pruritus cutaneous caused by insect excretion and secretion, nodular prurigo, kidney dialysis, diabetes, blood disease, liver disease, kidney disease, incretion and metabolic disorder, viscera malignant tumor, hyperthyroidism, autoimmune disease, multiple sclerosis, neurologic disease, psychoneurosis, allergic conjunctivitis, spring catarrh, atopic keratoconjunctivitis, or itching caused by excess use of laxuries and drugs because it has excellent scrtaching behavior suppressing effect, that is, antiitching effect and antipruritic effect.
摘要翻译：本发明涉及含有伤害感受肽拮抗剂作为活性成分的止痒剂。伤害感受肽拮抗剂可用作与瘙痒相关疾病（例如特应性皮炎和荨麻疹）的预防或治疗，由昆虫排泄和分泌引起的皮肤局部瘙痒，结节性痒疹，肾透析，糖尿病，血液病，肝脏疾病，肾脏疾病，增生和代谢紊乱，内脏恶性肿瘤，甲状腺机能亢进，自身免疫性疾病，多发性硬化症，神经系统疾病，精神病，过敏性结膜炎，春季卡他性，特应性角膜结膜炎，或由于过度使用松弛症和药物引起的瘙痒，因为它具有优异的刮伤行为抑制作用，即防止止痛作用和止痒作用。

5. 发明授权

EP1944298B1 QUINAZOLINE DERIVATIVE AND PHARMACEUTICAL 有权转让
标题翻译：喹唑啉衍生物和制药
公开(公告)号：EP1944298B1
公开(公告)日：2013-01-09
申请号：EP06811143.4
申请日：2006-10-03
申请人： Nippon Shinyaku Co., Ltd.
发明人： OKANO, Masahiko , OYAMA, Tatsuya
IPC分类号： C07D239/94 , A61K31/517 , A61P1/16 , A61P3/00 , A61P3/10 , A61P5/00 , A61P5/16 , A61P7/00 , A61P13/12 , A61P17/04 , A61P25/00 , A61P25/08 , A61P25/18
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14

6. 发明公开

EP2141168A1 HETEROARYL DERIVATIVES 审中-公开
标题翻译： HETEROARYLDERIVATE
公开(公告)号：EP2141168A1
公开(公告)日：2010-01-06
申请号：EP08739335.1
申请日：2008-03-28
申请人： Nippon Shinyaku Co., Ltd.
发明人： MATSUOKA, Masato , OYAMA, Tatsuya
IPC分类号： C07D491/048 , A61K31/4355 , A61K31/4365 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/55 , A61P3/04 , A61P13/10 , A61P21/00 , A61P25/02 , A61P25/22 , A61P25/24 , A61P29/00 , C07D495/04
CPC分类号： C07D491/048 , C07D495/04
摘要： The present invention relates to a compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof.

In the formula [1], either of X and Y is CH and the other is oxygen or sulfur; R is hydrogen, etc.; Z is hydrogen, etc.; Ar is phenyl, etc.; and n is 1 or 2 and m is 1 or 2, excluding the compounds where both of n and m are 2.
Also provided is a pharmaceutical composition conprising the compound or a pharmaceutically-acceptable salt thereof as an active ingredient. The composition is usable as an agent for the prevention or a treatment of depression, panic disorder, anxiety, obsessive-compulsive disorder, chronic pain, fibromyalgia, obesity, stress urinary incontinence. overactive bladder, etc.
摘要翻译：本发明涉及由下式[1]表示的化合物或其药学上可接受的盐。在式[1]中，X和Y中的任一个是CH，另一个是氧或硫; R是氢等; Z是氢等; Ar是苯基等; n为1或2，m为1或2，不包括n和m都为2的化合物。还提供了令化合物或其药学上可接受的盐作为活性成分的药物组合物。该组合物可用作预防或治疗抑郁症，恐慌症，焦虑症，强迫症，慢性疼痛，纤维肌痛，肥胖症，压力性尿失禁的药剂。膀胱过动症等

7. 发明公开

EP1944298A1 QUINAZOLINE DERIVATIVE AND PHARMACEUTICAL 有权转让
标题翻译： CHINAZOLINDERIVAT UND PHARMAZEUTIKUM
公开(公告)号：EP1944298A1
公开(公告)日：2008-07-16
申请号：EP06811143.4
申请日：2006-10-03
申请人： Nippon Shinyaku Co., Ltd.
发明人： OKANO, Masahiko , OYAMA, Tatsuya
IPC分类号： C07D239/94 , A61K31/517 , A61P1/16 , A61P3/00 , A61P3/10 , A61P5/00 , A61P5/16 , A61P7/00 , A61P13/12 , A61P17/04 , A61P25/00 , A61P25/08 , A61P25/18
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： It is intended to provide a novel quinazoline derivative with less skin irritation and an excellent action of strongly suppressing scratching behavior and a pharmaceutical composition containing the quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivative represented by the general formula [1] or a pharmaceutically acceptable salt thereof. In the general formula [1], R 1 represents hydrogen or the like, R 2 represents hydrogen or the like, R 3 and R 4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen, R 5 is combined with R 6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy, R 6 represents (1) alkyl, (2) cycloalkyl, (3) phenyl, (4) a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or (5) -N(R 61 ) (R 62 ).
摘要翻译：本发明提供一种新颖的喹唑啉衍生物，其具有较少的皮肤刺激性和强烈抑制刮擦行为的优异作用，以及含有喹唑啉衍生物作为活性成分的药物组合物。本发明涉及由通式[1]表示的喹唑啉衍生物或其药学上可接受的盐。在通式[1]中，R 1表示氢等，R 2表示氢等，R 3和R 4相同或不同，表示氢，烷基，烷氧基或卤素，R 5与R 6表示亚烷基或代表氢，羟基，烷基，苯基或烷氧基，R 6表示（1）烷基，（2）环烷基，（3）苯基，（4）5至10元芳族杂环基，三个选自氮原子，氧原子和硫原子的杂原子，或（5）-N（R 61）（R 62）。

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