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概览

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

HTR3(5-羟色胺受体3)	1

关联

2

项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的药物

Indisetron Hydrochloride

盐酸吲地司琼

靶点

HTR3

作用机制

5-HT3 receptor拮抗剂

在研机构

北京嘉林药业股份有限公司 [+2]

原研机构

Nisshin Flour Milling Co Ltd

在研适应症

恶心和呕吐 [+2]

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

日本

首次获批日期2004-01-29

N-5849

靶点

APOE

作用机制

APOE激动剂

在研机构-

原研机构

Nisshin Flour Milling Co Ltd [+1]

在研适应症-

非在研适应症

肝癌

最高研发阶段无进展

首次获批国家/地区-

首次获批日期-

100 项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的临床结果

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0 项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的专利（医药）

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11

项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的文献（医药）

2006-11-01·YAKUGAKU ZASSHI4区 · 医学

ステロールを用いる生物活性化合物の合成と構造活性相関

4区 · 医学

Review

作者: TACHIBANA, Yoji

Sterols are widely and abundantly distributed in nature. It is convenient to utilize them for the preparation of useful compounds such as pharmaceuticals with steroid and secosteroid skeletons. This paper describes the synthesis and structure-activity relationships of naturally occurring active forms of vitamin D analogues, sterols having neurite outgrowth activity, and liver X receptor agonist. The active form of vitamin D(4) showed similar biological activities but had higher affinity to the vitamin D-binding protein compared with the corresponding vitamins D(2) and D(3). This shows that the active form of vitamin D(4) is a good candidate for an agent to replace the active forms of vitamins D(2) and D(3). In the course of screening for low molecular-weight compounds that exhibit neurite outgrowth activity in the culture broth, we found that the natural product dictyosterol showed strong activity. From screening of the analogues, it was found that the double bond between C22 and C23 in the side chain of the sterol is essential for its activity. Ergost-22-ene-1alpha,3beta-diol was found to serve as a stronger liver X receptor agonist than 24(S), 25-epoxycholesterol, which regulates the expression of genes involved in lipid metabolism. Structure-function study showed that the 1alpha-hydroxyl group, the saturated steroid structure, and the double bond between C22 and C23 are needed to function as a liver X receptor agonist.

2006-01-01·Journal of Nutritional Science and Vitaminology4区 · 医学

Comparative Oral Toxicity of Coenzyme Q10 and Its (2Z)-Isomer in Rats: Single and Four-Week Repeated Dose Toxicity Studies

4区 · 医学

Article

作者: Hatakeyama, Shigeki ; Kawase, Shigeo ; Yoshimura, Ikuo

It has been reported that coenzyme Q10 (CoQ10) functions as an electron transfer carrier in mitochondria, and can produce an improvement in heart diseases such as congestive heart failure. Its (2Z)-isomer contains a cis-double bond at the 2-position of the decaprenyl side chain. As the original organic industrial synthesis of CoQ10 resulted in a product that contained a small amount of this isomer, the efficacy and safety of CoQ10 was determined using CoQ10 containing this isomer; however, no toxicity data have been reported for the (2Z)-isomer itself. Thus, we conducted single (2,000 mg/kg) and 4-wk repeated (1,000 mg/kg) oral dose toxicity studies in rats to compare the toxicological profiles of CoQ10 and its (2Z)-isomer. The two compounds displayed similar toxicological profiles, and it was concluded that neither CoQ10 nor its (2Z)-isomer produce toxic effects in rats in single or repeated doses.

Tennen Yuki Kagobutsu Toronkai Koen Yoshishu

Study on the stereoselective synthesis of cell cycle inhibitor, FR901464

作者: Horigome, Masato ; Watanabe, Hidenori ; Kitahara, Takeshi

FR901464 (I; R = Q), FR901463, i.e. I (R = Q¹), and FR901465, i.e. I (R = Q²), are new antitumor substances which were isolated from a culture broth of a bacterium of Pseudomonas sp. Number2663.These compounds show transcriptional regulating activity and induce characteristic G1 and G2/M phase arrest in the cell cycle.Related to these activities, they show potent antitumor effect.Especially, FR901464 I (R = Q) exhibits the most prominent antitumor activity among the three compoundsThe unique structure as well as the significant biol. activities prompted the authors to undertake the synthesis of this class of compoundHerein, the authors describe a stereoselective synthetic approach to FR901464 I (R = Q).The retrosynthetic anal. divided FR901464 I (R = Q) into three segments, the carboxylic acid II, the sulfone III, and the aldehyde IV.The authors thought that II, III, and IV would be obtained from com. available compounds resp., and the target mol. FR901464 I (R = Q) should be synthesized via convergent route by condensations of these segments.According to this synthetic plan, the authors carried out their study.The acid II was prepared from Et (S)-(-)-lactate using the reported method.N-Boc-L-threonine was used as the starting material to synthesize III.The Garner aldehyde V was prepared from N-Boc-L-threonine.Its side chain was elongated by the Wittig reaction, and was led to a lactone VI (Z = O) by acid catalyzed ring closure.Treatment with Lawesson's reagent and the following Wittig reaction gave the olefin isomers, (E)- and (Z)-VI (Z = :CH₂CO₂Me).After the base catalyzed deconjugation of olefin, catalytic hydrogenation gave the tetrahydropyran with the desired all-cis stereochem. as a sole product, and the successive DIBAL reduction afforded the aldehyde (VII), which was converted into the sulfone III through 4 steps.The aldehyde IV was synthesized from 2-deoxy-D-glucose.First, 4,6-dihydroxyl groups of 2-deoxy-D-glucose were protected as benzylidene acetal.Selective oxidation of hemiacetal with bromine, followed by the protection of the remaining free hydroxyl group gave the lactone VIII.Methylation and acetalization followed by deprotection of benzylidene group afforded diol IX.It was converted into aldehyde IV via protection-deprotection process and Dess-Martin oxidationHaving completed the synthesis of the three segments II, III and IV, the authors next examined the coupling processes.Condensation of II with III was achieved by using HBTU to give the amide X.Using Julia olefination method, coupling of X and the aldehyde IV afforded the diene I (R = Q³, R¹ = tert-BuMe₂Si).The successive selective desilylation and oxidation afforded the diene I (R = Q⁴, R¹ = tert-BuMe₂Si).The diene I (R = Q⁴, R¹ = tert-BuMe₂Si) possesses most of the carbon framework with the requisite asym. carbons involved of FR901464, I (R = Q, R¹ = Ac).Since XI (R = Q⁴, R¹ = tert-BuMe₂Si) is considered as a potential key intermediate in the authors' our synthetic strategy, conversion of XI (R = Q⁴) to the target mol. FR901464, I (R = Q, R¹ = Ac) is now under investigation.

100 项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的药物交易

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100 项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的转化医学

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