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31. 发明授权

US07960369B2 Receptor function regulator 有权
标题翻译：受体功能调节剂
公开(公告)号：US07960369B2
公开(公告)日：2011-06-14
申请号：US10534081
申请日：2003-11-06
申请人： Kohji Fukatsu , Shinobu Sasaki , Shuji Hinuma , Yasuaki Ito , Nobuhiro Suzuki , Masataka Harada , Tsuneo Yasuma
发明人： Kohji Fukatsu , Shinobu Sasaki , Shuji Hinuma , Yasuaki Ito , Nobuhiro Suzuki , Masataka Harada , Tsuneo Yasuma
IPC分类号： A61K31/535
CPC分类号： C07C255/24 , A61K31/192 , A61K31/195 , A61K31/216 , A61K31/343 , A61K31/381 , A61K31/401 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/437 , C07C59/64 , C07C59/68 , C07C59/72 , C07C59/74 , C07C59/76 , C07C59/90 , C07C65/24 , C07C69/734 , C07C69/736 , C07C217/48 , C07C217/58 , C07C217/76 , C07C235/42 , C07C255/54 , C07C317/28 , C07C323/19 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D209/12 , C07D277/36 , C07D277/42 , C07D277/64 , C07D295/13 , C07D307/91 , C07D333/32 , C07D333/54 , C07D333/62 , C07D333/78 , C07D471/04
摘要： The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.
摘要翻译：本发明的GPR40受体功能调节剂包含具有芳香环的化合物和能释放阳离子的基团，可用作胰岛素促分泌素或预防或治疗糖尿病等的药剂。

32. 发明申请

US20080160033A1 Novel Screening Method 审中-公开
标题翻译：新型筛选方法
公开(公告)号：US20080160033A1
公开(公告)日：2008-07-03
申请号：US10542408
申请日：2004-01-15
申请人： Yasuaki Ito , Ryo Fujii , Shuji Hinuma , Shoji Fukusumi , Minoru Maruyama
发明人： Yasuaki Ito , Ryo Fujii , Shuji Hinuma , Shoji Fukusumi , Minoru Maruyama
IPC分类号： A61K39/395 , G01N33/68 , C07H21/04 , C07K14/705 , C12N5/06 , A61P5/00 , A61P35/00 , A61P31/12 , A61P3/00 , C12P21/02 , C12N15/63 , A61K31/711 , G01N33/566
CPC分类号： C07K14/723 , A61K31/711 , C07K14/705 , G01N2333/726 , G01N2500/02
摘要： By using a G protein-coupled receptor protein comprising the same or substantially the same as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 3 or SEQ ID NO: 8, or a salt thereof, and a fatty acid, a compound or its salt that changes the binding property of the receptor protein or a salt thereof to the fatty acid can be efficiently screened.
摘要翻译：通过使用包含与SEQ ID NO：1，SEQ ID NO：3或SEQ ID NO：8表示的氨基酸序列相同或基本相同的G蛋白偶联受体蛋白或其盐，和脂肪酸可以有效地筛选改变受体蛋白质或其盐与脂肪酸的结合性的化合物或其盐。

33. 发明授权

US06538107B1 G protein coupled receptor protein production, and use thereof 失效
标题翻译： G蛋白偶联受体蛋白质的产生及其用途
公开(公告)号：US06538107B1
公开(公告)日：2003-03-25
申请号：US09461436
申请日：1999-12-14
申请人： Shuji Hinuma , Yasuaki Ito , Ryo Fujii
发明人： Shuji Hinuma , Yasuaki Ito , Ryo Fujii
IPC分类号： C07K14435
CPC分类号： C12Q1/6876 , C07K14/705 , C07K14/70571 , C07K14/723 , C12Q1/6809 , C12Q1/6883
摘要： DNA primers effective in screening G protein coupled receptor protein-encoding DNA fragments are provided. The primers which are complementary to nucleotide sequences that are in community with (homologous to) the nucleotide sequences encoding amino acid sequences corresponding to or near the first membrane-spanning domain or the sixth membrane-spanning domain each of known various G protein coupled receptor proteins were designed and synthesized. Methods of amplifying G protein coupled receptor protein-encoding DNAs using the above DNA primers, and novel target G protein coupled receptor protein-encoding DNAs are also provided. Screening of DNA libraries can be efficiently carried out. Human pituitary gland or amygdala-derived and mouse pancreas-derived G protein coupled receptor proteins, etc. or salts thereof, partial peptides thereof, DNAs coding for the above G protein coupled receptor proteins, processes for producing the above G protein coupled receptor proteins, methods of determining ligands for the above G protein coupled receptor proteins, methods of screening compounds that inhibit the binding between the ligand and the G protein coupled receptor proteins or screening kits therefor, compounds or salts thereof obtained by the above screening method or the screening kit, pharmaceutical compositions containing the above compounds or salts thereof, and antibodies against the above protein coupled receptor proteins or partial peptides thereof are provided.
摘要翻译：提供了有效筛选编码G蛋白偶联受体蛋白的DNA片段的DNA引物。与与编码对应于或接近第一跨膜结构域或第六跨膜结构域的氨基酸序列的核苷酸序列（同源的）的核苷酸序列互补的引物，每个已知的各种G蛋白偶联受体蛋白被设计和合成。还提供了使用上述DNA引物扩增G蛋白偶联受体蛋白质编码DNA的方法，以及新的靶向G蛋白偶联受体蛋白质编码DNA。可以有效地进行DNA文库的筛选。人类垂体腺或来自扁桃体的小鼠胰腺衍生的G蛋白偶联受体蛋白等，或其盐，其部分肽，编码上述G蛋白偶联受体蛋白质的DNA，用于产生上述G蛋白偶联受体蛋白质的方法，确定上述G蛋白偶联受体蛋白质的配体的方法，筛选抑制配体和G蛋白偶联受体蛋白质或其筛选试剂盒之间的结合的化合物的方法，通过上述筛选方法获得的化合物或其盐或筛选试剂盒提供含有上述化合物或其盐的药物组合物和针对上述蛋白质偶联受体蛋白质或其部分肽的抗体。

34. 发明申请

US20070117840A1 Receptor antagonist 审中-公开
标题翻译：受体拮抗剂
公开(公告)号：US20070117840A1
公开(公告)日：2007-05-24
申请号：US10549889
申请日：2004-03-16
申请人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Yoshihiro Banno , Hiromi Yoshida , Hirokazu Matsumoto
发明人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Yoshihiro Banno , Hiromi Yoshida , Hirokazu Matsumoto
IPC分类号： A61K31/4704
CPC分类号： A61K31/4704
摘要： A compound represented by the formula (I): wherein ring A represents an aromatic ring; X represents a bond, oxygen, NR4 (R4 represents hydrogen, a hydrocarbon group, or a heterocyclic group), or alkylene; R1 represents a hydrocarbon group, or a heterocyclic group; R2 represents —COYR5 (Y represents a bond, alkylene, oxygen, sulfur, or NR6 (R6 represents hydrogen, a hydrocarbon group, or a heterocyclic group), and R5 represents a hydrocarbon group, or a heterocyclic group), a hydrocarbon group, or a heterocyclic group; and R3 represents a hydrocarbon group, a heterocyclic group, optionally substituted hydroxy, optionally substituted amino, or —S(O)nR7 (R7 represents a hydrocarbon group, or a heterocyclic group, and n is 0 to 2), a salt of the compound, or a prodrug or either is useful as an agent for modulating the function of an RFRP receptor.
摘要翻译：由式（I）表示的化合物：其中环A表示芳环; X表示键，氧，NR 4（R 4表示氢，烃基或杂环基）或亚烷基; R 1表示烃基或杂环基; R 2表示-COYR 5（Y表示键，亚烷基，氧，硫或NR 6（R 6） SUP>表示氢，烃基或杂环基），R 5表示烃基或杂环基），烃基或杂环基; 和R 3表示烃基，杂环基，任选取代的羟基，任选取代的氨基或-S（O）n R 7 （R 7表示烃基或杂环基，n为0〜2），化合物或前药的盐或其可用作调节其功能的试剂 RFRP受体。

35. 发明申请

US20060199795A1 Receptor agonists 失效
标题翻译：受体激动剂
公开(公告)号：US20060199795A1
公开(公告)日：2006-09-07
申请号：US10543997
申请日：2004-01-27
申请人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Takashi Miki , Yuji Kawamata , Satoru Oi , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
发明人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Takashi Miki , Yuji Kawamata , Satoru Oi , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
IPC分类号： A61K31/554 , A61K31/553 , A61K31/5513
CPC分类号： C07D267/14 , A61K31/4353 , A61K31/5513 , A61K31/553
摘要： The present invention provides a TGR5 receptor agonist comprising a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring; and ring B′ is a 5- to 8-membered ring having one or more substituents or a salt thereof or a prodrug thereof, which is useful for the treatment of various diseases.
摘要翻译：本发明提供一种TGR5受体激动剂，其包含由下式表示的稠环化合物：其中环A为任选取代的芳环; 环B'是具有一个或多个取代基的5-至8-元环或其盐或其前药，其可用于治疗各种疾病。

36. 发明授权

US07045497B1 Use of peptide 失效
标题翻译：使用肽
公开(公告)号：US07045497B1
公开(公告)日：2006-05-16
申请号：US09868885
申请日：1999-12-22
申请人： Hirokazu Matsumoto , Chieko Kitada , Shuji Hinuma
发明人： Hirokazu Matsumoto , Chieko Kitada , Shuji Hinuma
IPC分类号： A61K38/11 , A61K38/16 , C07K14/00 , C07H21/04
CPC分类号： A61K38/2257
摘要： The present invention relates to use of peptide to which G-protein coupled receptor protein recognizes as a ligand. Since the ligand polypeptide of the present invention has a stimulating action on oxytocin secretion, it is useful as a drug for ameliorating, preserving or treating various diseases related to oxytocin secretion such as uterine inertia, atonic hemorrhage, placental expulsion, subinvolution and the like.
摘要翻译：本发明涉及G蛋白偶联受体蛋白识别为配体的肽的用途。由于本发明的配体多肽对催产素分泌具有刺激作用，因此可用作改善，保存或治疗与催产素分泌相关的各种疾病如子宫惯性，失声性出血，胎盘排出，亚溶解等的药物。

37. 发明授权

US5241053A Fused proteins comprising glycoprotein gD of HSV-1 and LTB 失效
标题翻译：包含HSV-1和LTB的糖蛋白gD的融合蛋白
公开(公告)号：US5241053A
公开(公告)日：1993-08-31
申请号：US577915
申请日：1990-09-05
申请人： Yukio Fujisawa , Shuji Hinuma , Aki Mayumi , Tatsuo Yamamoto
发明人： Yukio Fujisawa , Shuji Hinuma , Aki Mayumi , Tatsuo Yamamoto
IPC分类号： A61K39/00 , A61K47/48 , C07K14/035 , C07K14/245
CPC分类号： C07K14/245 , A61K47/4833 , C07K14/005 , A61K39/00 , C07K2319/40 , C07K2319/55 , C12N2710/16622
摘要： Disclosed are (1) a fused protein comprising heat-labile enterotoxin B subunit and a protein heterologous to heat-labile enterotoxin, (2) a recombinant DNA containing a nucleotide sequence coding for the above fused protein, (3) a transformant harboring the above recombinant DNA, (4) a method for producing the fused protein which comprises cultivating the above transformant, producing and accumulating the above fused protein in a culture, and collecting the fused protein, and (5) a method for purifying a fused protein comprising a herpes simplex virus surface antigen and heat-labile enterotoxin B subunit, which comprises cultivating a transformant harboring a recombinant DNA containing a nucleotide sequence coding for the fused protein, producing an accumulating the fused protein in a culture, collecting the fused protein and subjecting the collected fused protein to purification processes comprising cationic exchange chromatography and gel permeation chromatography.
摘要翻译：公开了（1）包含热不稳定肠毒素B亚基和与热不稳定肠毒素异源的蛋白质的融合蛋白，（2）含有编码上述融合蛋白的核苷酸序列的重组DNA，（3）含有上述重组DNA，（4）生产融合蛋白的方法，包括培养上述转化体，在培养物中产生和积累上述融合蛋白，并收集融合蛋白，和（5）纯化融合蛋白的方法，单纯疱疹病毒表面抗原和热不稳定肠毒素B亚基，其包括培养含有编码融合蛋白的核苷酸序列的重组DNA的转化体，产生在培养物中积聚融合蛋白，收集融合蛋白并使收集的融合蛋白与包含阳离子交换层析和凝胶渗透色谱的纯化方法。

38. 发明授权

US07927821B2 Methods of screening for compounds which bind G protein-coupled receptors 失效
标题翻译：筛选结合G蛋白偶联受体的化合物的方法
公开(公告)号：US07927821B2
公开(公告)日：2011-04-19
申请号：US11578325
申请日：2005-04-11
申请人： Ryo Fujii , Shoichi Okubo , Kazunori Nishi , Shuji Hinuma , Masaaki Mori
发明人： Ryo Fujii , Shoichi Okubo , Kazunori Nishi , Shuji Hinuma , Masaaki Mori
IPC分类号： G01N33/53 , G01N33/567 , G01N33/566 , C07K1/00 , C07K14/00 , C07K17/00
CPC分类号： G01N33/76 , A61K31/403 , A61K31/4155 , A61K31/4523 , A61K38/1796 , C07K14/705 , G01N2333/726
摘要： The present invention provides a method of screening an agonist or antagonist to a G protein-coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, which comprises using the receptor protein or a salt thereof and the ligand or a salt thereof; etc. The present invention is useful for screening agents for the prevention/treatment of, e.g., leukopenia, leukemia, lymphoma, malignant tumor, ulcerative colitis, rheumatoid arthritis, inflammatory bowel disorders, tonsil disorders, collagen disease, inflammatory disease, leukocytosis, heart failure, inherited muscle disorders, muscular dystrophy, neuromuscular degenerative disease, myocardial infarction, obesity, mellitus diabetes, hyperlipemia, arteriosclerosis, metabolic syndrome, thrombocytopenia, thrombocytosis, cancer, pulmonary edema, multiple organ failure, etc.
摘要翻译：本发明提供筛选G蛋白偶联受体蛋白的激动剂或拮抗剂的方法，其包含与SEQ ID NO：1所示的氨基酸序列相同或基本上相同的氨基酸序列，或其盐，其包含使用受体蛋白或其盐和配体或其盐; 本发明可用于预防/治疗例如白细胞减少症，白血病，淋巴瘤，恶性肿瘤，溃疡性结肠炎，类风湿性关节炎，炎性肠病，扁桃体病，胶原病，炎性疾病，白细胞增多症，心脏病失败，遗传性肌肉疾病，肌营养不良症，神经肌肉退行性疾病，心肌梗死，肥胖症，糖尿病，高脂血症，动脉硬化，代谢综合征，血小板减少症，血小板增多症，癌症，肺水肿，多器官衰竭等。

39. 发明授权

US07833722B2 Ligands for G protein-coupled receptor protein and use thereof 失效
标题翻译： G蛋白偶联受体蛋白质的配体及其用途
公开(公告)号：US07833722B2
公开(公告)日：2010-11-16
申请号：US11587631
申请日：2005-04-26
申请人： Ryo Fujii , Masataka Harada , Shuji Hinuma
发明人： Ryo Fujii , Masataka Harada , Shuji Hinuma
IPC分类号： G01N33/53
CPC分类号： C07K14/705 , A61K31/7088 , A61K38/00 , G01N33/6896 , G01N33/74 , G01N2333/726 , G01N2500/04
摘要： The present invention provides a method of screening an agonist/antagonist of a G protein-coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, which comprises using the receptor protein or its salt and a ligand or its salt; and so on. The screening method of the present invention is useful for screening an agent for the prevention/treatment of nervous system diseases or neuropathic pains.
摘要翻译：本发明提供筛选G蛋白偶联受体蛋白激动剂/拮抗剂的方法，其包含与SEQ ID NO：1所示的氨基酸序列相同或基本上相同的氨基酸序列，或其盐，其包含使用受体蛋白或其盐和配体或其盐; 等等。本发明的筛选方法可用于筛选用于预防/治疗神经系统疾病或神经性疼痛的药剂。

40. 发明授权

US06187788B1 Condensed-ring thiophene derivatives, their production and use 失效
标题翻译：缩环噻吩衍生物，其生产和使用
公开(公告)号：US06187788B1
公开(公告)日：2001-02-13
申请号：US09164349
申请日：1998-10-01
申请人： Shuichi Furuya , Nobuo Choh , Koichi Kato , Shuji Hinuma
发明人： Shuichi Furuya , Nobuo Choh , Koichi Kato , Shuji Hinuma
IPC分类号： A61K31437
CPC分类号： C07D495/04
摘要： A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g. a pregnancy controlling agent and a menstrual cycle controlling agent); can be used as a contraceptive of male or female, as an ovulation-inducing agent of female; can be used as an infertility treating agent by using a rebound effect owing to a stoppage of administration thereof; is useful as modulating estrous cycles in animals in the field of animal husbandry, as an agent fro improving the quality of edible meat or promoting the growth of animals; is useful as an agent of spawning promotion in fish.
摘要翻译：促性腺激素释放激素拮抗组合物，其包含任选取代的稠合双环化合物，其由同质或杂的5至7元环和同质或异构的5至7元环组成，作为用于预防或治疗几种激素依赖性疾病，例如性激素依赖性癌症（例如前列腺癌，子宫颈癌，乳腺癌，垂体腺瘤），良性前列腺肥大，子宫肌瘤，子宫内膜异位症，早熟性青春期，闭经，经前综合征，多囊卵巢综合征和寻常型痤疮; 作为两性生育调节剂（例如妊娠控制剂和月经周期控制剂）是有效的; 可作为男性或女性的避孕方法，作为女性的排卵诱导剂; 可以通过使用由于其施用停止而产生的反弹效应而用作不育处理剂; 可用作调整动物饲养领域的发情周期，作为提高食用肉质量或促进动物生长的药剂; 作为鱼类产卵促销的代理人是有用的。

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