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公开(公告)号:US20100160255A1
公开(公告)日:2010-06-24
申请号:US11997021
申请日:2006-07-28
申请人: Makoto Kamata , Kohji Fukatsu , Tohru Yamashita , Naoki Furuyama , Satoshi Endo
发明人: Makoto Kamata , Kohji Fukatsu , Tohru Yamashita , Naoki Furuyama , Satoshi Endo
IPC分类号: A61K31/695 , C07D471/10 , A61K31/4545 , C07D211/06 , A61P3/04 , A61P9/12 , A61P3/06 , A61P9/00 , A61P3/10 , C07D498/10 , A61K31/5386 , C07D487/10 , A61K31/499 , C07F7/02 , C07D413/14 , A61K31/5377
CPC分类号: C07D513/10 , C07D221/20 , C07D401/04 , C07D471/10 , C07D487/10 , C07D491/10 , C07F7/1804
摘要: The present invention provides a compound represented by the formula (I): wherein E is an optionally substituted cyclic group; D is a carbonyl group or a sulfonyl group; A is CH or N; ring P is an optionally further substituted 5- to 7-membered ring; ring Q is an optionally further substituted 5- to 7-membered nonaromatic ring; and ring R is an optionally further substituted and optionally condensed 5- to 7-membered nonaromatic ring, or a salt thereof. The compound of the present invention has an ACC inhibitory activity, is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties in the efficacy, duration of activity, specificity, low toxicity and the like.
摘要翻译: 本发明提供由式(I)表示的化合物:其中E为任选取代的环状基团; D是羰基或磺酰基; A是CH或N; 环P是任选进一步取代的5-至7-元环; 环Q是任选进一步取代的5-至7-元非芳族环; 并且环R是任选进一步取代的和任选缩合的5-至7-元非芳族环或其盐。 本发明化合物具有ACC抑制活性,可用于预防或治疗肥胖症,糖尿病,高血压,高脂血症,心力衰竭,糖尿病并发症,代谢综合征,肌肉减少症等,并且具有优异的功效特性, 活动持续时间,特异性,低毒性等。
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公开(公告)号:US06534496B1
公开(公告)日:2003-03-18
申请号:US09402806
申请日:1999-10-07
申请人: Yuji Ishihara , Yukio Fujisawa , Naoki Furuyama
发明人: Yuji Ishihara , Yukio Fujisawa , Naoki Furuyama
IPC分类号: A61K3155
CPC分类号: C07D401/06 , A61K31/4523 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4745 , A61K31/55 , A61K31/553 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要: The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.
摘要翻译: 本发明的目的是提供一种用于肥胖和肥胖相关疾病的糖尿病的预防和/或治疗药物,其具有降低的中枢副作用的风险和使用的高普遍性。 本发明的另一个目的是提供一种药物组合物,其包含下式的化合物:其中Ar表示可被取代和/或缩合的苯基; n表示1〜10的整数, R表示氢或可被取代的烃基,其在其n次可能不相同; R可以与Ar或Ar的取代基结合; Y表示可以取代的氨基或可被取代的含氮饱和杂环基或其盐,其可用于生热剂,抗肥胖剂,脂解剂或预防和/或 治疗肥胖相关疾病的药物。
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公开(公告)号:US07833972B2
公开(公告)日:2010-11-16
申请号:US12371525
申请日:2009-02-13
摘要: A method of suppressing the differentiation of an adipocite and/or lipid accumulation in an adipocyte, which comprises contacting the adipocyte with a protein comprising the amino acid sequence of SEQ ID NO: 2 or a salt thereof, or with a polynucleotide comprising a sense strand sequence encoding a protein comprising the amino acid sequence of SEQ ID NO: 2.
摘要翻译: 一种抑制脂肪细胞中脂肪和/或脂肪积累分化的方法,其包括将脂肪细胞与包含SEQ ID NO:2的氨基酸序列或其盐的蛋白质或与包含有义链的多核苷酸接触 编码包含SEQ ID NO:2的氨基酸序列的蛋白质的序列。
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公开(公告)号:US20060110384A1
公开(公告)日:2006-05-25
申请号:US10520783
申请日:2003-07-09
IPC分类号: A61K39/395 , G01N33/53 , C07H21/04 , C12P21/06 , C07K14/705
摘要: The present invention provides a novel secretory/membrane protein associated with adipocyte differentiation and/or metabolism function, specifically, an adipocyte-derived secretory/membrane protein containing amino acid sequence which is the same or substantially the same as an amino acid sequence represented by SEQ ID NOS: 2, 4, 6, 8, 10, 12, 14, 16, 18, 20 or 22, a nucleic acid encoding it, an antibody therefor, a method of screening prophylactic and/or therapeutic agents for diseases involving abnormality of adipocyte differentiation/metabolism function using it and/or a kit for the screening, a prophylactic and/or therapeutic agent for the diseases or a diagnostic agent containing the membrane protein.
摘要翻译: 本发明提供了与脂肪细胞分化和/或代谢功能相关的新型分泌/膜蛋白,具体地,含有脂肪细胞的分泌/膜蛋白的氨基酸序列与SEQ ID NO:1所示的氨基酸序列相同或基本上相同 2号,4号,6号,8号,10号,14号,16号,18号,20号,12号,14号,18号,20号或22号,编码它的核酸,其抗体,筛选涉及异常的疾病的预防和/或治疗剂的方法 使用其的脂肪细胞分化/代谢功能和/或用于筛选的试剂盒,用于疾病的预防和/或治疗剂或含有所述膜蛋白的诊断剂。
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公开(公告)号:US20090203608A1
公开(公告)日:2009-08-13
申请号:US12371525
申请日:2009-02-13
摘要: The present invention provides a novel secretory/membrane protein associated with adipocyte differentiation and/or metabolism function, specifically, an adipocyte-derived secretory/membrane protein containing amino acid sequence which is the same or substantially the same as an amino acid sequence represented by SEQ ID NOS: 2, 4, 6, 8, 10, 12, 14, 16, 18, 20 or 22, a nucleic acid encoding it, an antibody therefor, a method of screening prophylactic and/or therapeutic agents for diseases involving abnormality of adipocyte differentiation/metabolism function using it and/or a kit for the screening, a prophylactic and/or therapeutic agent for the diseases or a diagnostic agent containing the membrane protein.
摘要翻译: 本发明提供了与脂肪细胞分化和/或代谢功能相关的新型分泌/膜蛋白,具体地,含有脂肪细胞的分泌/膜蛋白的氨基酸序列与SEQ ID NO:1所示的氨基酸序列相同或基本上相同 2号,4号,6号,8号,10号,14号,16号,18号,20号,12号,14号,18号,20号或22号,编码它的核酸,其抗体,筛选涉及异常的疾病的预防和/或治疗剂的方法 使用其的脂肪细胞分化/代谢功能和/或用于筛选的试剂盒,用于疾病的预防和/或治疗剂或含有所述膜蛋白的诊断剂。
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