著者

野副 重男 草野 源次郎

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.17, no.8, pp.723-730, 1981-08-01 (Released:2018-08-26)

著者

竹下 隆三

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.19, no.2, 1983

著者

日髙 淳 花木 秀明

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.55, no.2, pp.121-125, 2019 (Released:2019-02-01)

参考文献数

21

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抗菌薬に対する耐性菌の出現と蔓延は世界的な問題であり、WHOをはじめ各国が国主導の対策を講じつつあるが、様々な要因により薬剤耐性(AMR)菌感染症治療薬の開発は停滞している。本稿では、新薬開発の代表例としてβ-ラクタマーゼ阻害薬およびその合剤の開発状況について概説し、新規抗菌薬の創薬促進のための考えや課題などについて述べる。

著者

長井 長義

出版者

公益社団法人 日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.1909, no.329, pp.739-751, 1909

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エフェドリン」ハ著者カ始メテ麻黄中ヨリ發見シタル鹽基ニシテ著者ハ明治十八年以來之カ研究ニ從事シ其構造ヲ殆ント完全ニ解明スルヲ得タリシヲ以テ更ニ之カ合成ヲ企畫シ實驗漸ク其緒ニ就カントスルニ當リ助手ノ他ニ轉職スルニ會/之ヲ中止スルノ已ムヲ得サルニ至リシカ今回獨逸ノ藥化學者シュミット氏ハ「エフェドリン鹽基ノ合成ニ著手シ其方針ノ著者カ十餘年前既ニ案出セシモノニ接近セルヲ知リ著者ハ同研究ヲ再興シ昨冬以來收メ得タル業蹟ヲ報告セリ

著者

土釜 恭直

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.139, no.2, pp.209-219, 2019-02-01 (Released:2019-02-01)

参考文献数

41

被引用文献数

3

---

Antibody-drug conjugates (ADCs), monoclonal antibodies conjugated with highly potent drugs (payloads) through chemical linkers, are an emerging class of therapeutic agents for cancer chemotherapy. Their clinical success has been demonstrated by the 4 ADCs already approved by the U.S. Food and Drug Administration (FDA), and more than 60 promising ADCs now in clinical trials. Further advancement of this novel molecular platform could potentially revolutionize current strategies and regimens for treating cancers. The linker structure and antibody-linker conjugation modality critically contribute to ADC homogeneity, circulation stability, pharmacokinetic profiles, tolerability, and overall treatment efficacy. Despite extensive efforts to improve these parameters, most ADC linkers used to date possess linear structures, and therefore accommodate only single payloads. The clinical potential of branched ADC linkers, enabling the installation of two payload molecules, remains unexplored because of the lack of efficient conjugation methods. In addition, according to a recent report, the stability of enzymatically cleavable linkers in mouse circulation is another crucial factor for the successful evaluation of ADCs in preclinical studies. In this review, I present my research group's effort to develop both branched linkers and efficient conjugation methods for constructing dual-loading ADCs with high homogeneity and enhanced potency. I also present a novel tripeptide ADC linker with enhanced stability in mouse circulation. Multidisciplinary experience, approaches, and collaboration are key to successfully advancing our ADC research programs. I herein describe how my experience in the U.S. has helped to develop and manage complex biomedical research projects in a small academic laboratory setting.

著者

川口 実希 木村 美智男 宇佐美 英績 川地 志緒里 郷 真貴子 池田 義明 吉村 知哲

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.139, no.3, pp.483-490, 2019-03-01 (Released:2019-03-01)

参考文献数

22

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This study aimed to clarify the situation of use of health foods by patients and the level of satisfaction of patients in order to make use of information on cases where patients undergoing cancer medication therapy use health foods. Between May 7, 2018 and June 29, 2018, we conducted a questionnaire survey of patients with progressive cancer who were undergoing cancer chemotherapy at Ogaki Municipal Hospital. In addition, we conducted a multivariate analysis of patients who were using health foods and those who were not. The questionnaire items included the objectives of use, product effectiveness and satisfaction, and QOL. The rate of health food use was 81/281 (29.5%). The primary objectives of use were, “to maintain health” (29.8%) and “to alleviate symptoms” (24.0%). The primary sources of information about health foods were “a friend” (50.6%) and “TV” (13.5%). The satisfaction level was 0-3 points in 8.3% of patients, 4-6 points in 38.1% of patients, and 7-10 points in 53.6% of patients. For “stage of illness (recurrence),” the odds ratio was 1.810 (95% CI, 1.040-3.150; p=0.035), and for “QOL value,” the odds ratio was 2.210 (95% CI, 1.220-4.020; p=0.009), indicating that these factors had a significant influence on health food use. Health foods tended to be used in patients who had recurring cancer with low QOL and various symptoms, and friends and other people close to the patient had a large influence on the patient's decision. It was clear that the patients' satisfaction level was high.

著者

小林 力

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.50, no.4, pp.330_1, 2014 (Released:2016-06-01)

著者

萩庭 丈寿 坂井 進一郎 相見 則郎 山中 悦二 新間 信夫

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.93, no.4, pp.448-452, 1973-04-25 (Released:2008-05-30)

参考文献数

12

被引用文献数

21 33

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In the reinvestigation of the constituents of Uncaria rhynchophylla MIQ. (Japanese name "kagikazura"), the presence of two oxindole alkaloids, corynoxeine and isocorynoxeine, was demonstrated, besides the reported rhynchophylline and isorhynchophylline.3) Furthermore, four indole alkaloids were newly isolated ; hirsutine, hirsuteine, dihydrocorynantheine, and corynantheine. A chemical structural evidence of hirsutine was obtained from its epimerization to dihydrocorynantheine with acetic acid catalysis.

著者

山中 悦二 君塚 ゆみ子 相見 則郎 坂井 進一郎 萩庭 丈寿

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.103, no.10, pp.1028-1033, 1983-10-25 (Released:2008-05-30)

参考文献数

8

被引用文献数

12 27

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Quantitative analysis of the tertiary alkaloids in various parts of Uncaria rhynchophylla MIQ. was made by use of high performance liquid chromatography (HPLC). The best result was obtained in the following conditions : column ; Radial Pak C8 and mobile phase ; CH3CN-0.05M AcONH4 buffer (pH 4.0) [90 : 10]. The result revealed that the constitution of the alkaloids varied markedly depending on the botanical parts examined. While oxindole alkaloids (1, 2, 3 and 6) occupy ca. 97% of total alkaloids in hook, small stem and leaf, respectively, content of indole alkaloids (mainly 8 and 10) is almost exclusive (ca. 96%) in the bark of underground part. In the bark of aerial part both oxindole and indole alkaloids were found to be contained in nearly equal amounts. The alkaloidal content is very low in the wood (aerial or underground part) but the content ratios of rare alkaloids (4 and 7) to the total alkaloids are higher than the other parts.

著者

小林 義郎

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.100, no.8, pp.779-791, 1980-08-25 (Released:2008-05-30)

参考文献数

18

被引用文献数

1

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Studies on organic fluorine compounds in our laboratory are summarized. New methods for the synthesis of fluorine compound are as follows ; 1) fluorination of alcohols with fluorophosphoranes, 2) trifluoromethylation of aromatic and aliphatic halides with trifluoromethyl halides and copper powder, and 3) cycloaddition reaction with novel fluorine reagents like hexafluorobutyne. Reactions of trifluoromethyl aromatic compounds were investigated thoroughly, and some interesting characters of fluorine compounds were revealed. Trifluoromethylated valence bond isomers of aromatic compounds were synthesized, and some novel reactions of these highly strained compounds were shown. The characteristics that a fluorine atom is a small substituent and that a carbon-fluorine bond is very strong were used to study the metabolism of vitamin D3. Some interesting reactions by use of fluorine compounds as synthetic reagents are also discussed.

著者

太田 美里

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.53, no.10, pp.1010-1011, 2017

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2013年から2年間,中国北京大学薬学院に博士研究員として在籍した時の体験談である。中国では博士研究員修了は博士号取得後の一つの経歴として重要視されており,登録から修了までの過程を述べた。滞在時には苦労した点が多く,実体験をそのまま記した。一方,中国の実験室は様々な機器が揃っており,実験環境が素晴らしい。また,中国の病院の生薬を用いた処方の調剤の様子を見学できたのでその実情について紹介した。

著者

熊懐 稜丸

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.105, no.8, pp.713-723, 1985-08-25 (Released:2008-05-30)

参考文献数

26

被引用文献数

4 3

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New reactions developed for the synthesis of medicinally useful trifluoromethyl compounds are discussed. First, the trifluoromethylation of aromatic halogen compounds with CF3I and Cu powder is presented. This method is applicable to a wide range of aromatic halides, while aliphatic halides cannot be converted to trifluoromethyl compounds. This difficulty was removed by two-step procedure. CF3I and Cu powder were shaken in a stainless steel tube, and the excess of Cu powder was removed by filtration. The solution of [CF3-Cu] was treated with halogen compounds to give trifluoromethyl compounds. Next, the Friedel-Crafts reaction of trifluoropropene was presented, which gave trifluoropropyl compounds. It was very difficult to obtain these products by other routes. Attempted application of the trifluoropropyl compounds are included. Finally, some reactions useful for the synthesis of special types of trifluoromethyl compounds were summarized, where photoreaction, 1, 3-dipolar reaction, and ene reaction of trifluoromethyl compounds are included.

著者

熊懐 稜丸

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.126, no.11, pp.1059-1085, 2006-11-01 (Released:2006-11-01)

参考文献数

66

被引用文献数

2 2

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This review describes new syntheses of organofluorine compounds taking advantage of the special properties of fluorine compounds as synthones. The main reactions presented are as follows: 1) Trifluoromethylation of aryl or alkyl halides. Application of this reaction for the synthesis of fluorine analogues of nucleic acid bases is discussed. 2) Some syntheses of trifluoromethyl compounds using the Diels-Alder or the 1,3-dipolar reaction, trifluoromethylated carbene, and photoreaction. 3) The Friedel-Crafts reaction of 3,3,3-trifluoropropene, where linear alkylation occurs due to electronic effect of the trifluoromethyl group in good contrast with the Friedel-Crafts reaction of propene. 4) The ene reaction of trifluoromethylated carbonyl compounds, which work as good enophiles. Application of this reaction to the synthesis of trifluoro analogues of terpenes is discussed. 5) The ene reaction of trifluoromethylated imines. 6) Reaction of halothane, which has a highly acidic hydrogen and two halogens adjacent to the trifluoromethyl group and shows interesting reactivities with various bases and metals to give products with unexpected structures. 7) Reaction of 2-bromo-2,2-difluoroacetate with Cu, where the cross-coupling reaction, Michael-type reaction, and radical reaction for different types of difluoroacetates are presented. 8) Reaction of 2-bromo-2,2-difluoroacetate in the presence of Rh catalyst. This reaction provided a new methodology for the introduction of fluoroalkyl substituents to the α-position of α,β-unsaturated ketones. The Rh catalyst solved some difficulties in the introduction of difluoroacetate to carbonyl compounds (Reformatsky reaction). Application of this reaction to imines provided easy access to β,β-difluoro-β-lactams.

著者

佐藤 和之

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.126, no.8, pp.597-605, 2006-08-01 (Released:2006-08-01)

参考文献数

30

被引用文献数

2 2

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Novel fluoroalkylated products where a CF2COOEt group was introduced at the α-position of α,β-unsaturated ketones or the Reformatsky-type products have been obtained selectively by the reaction of BrCF2COOEt and α,β-unsaturated ketones with Et2Zn in the presence of RhCl(PPh3)3 depending on the solvents. Furthermore, the novel α-fluoroalkylated products could synthesize by using various halofluoroalkyl compounds (Rf-X) instead of BrCF2COOEt. On the other hand, this Reformatsky-type reaction by imines gave difluoro-β-lactams or 3-amino-2,2-difluorocalboxylic esters without or with MgSO4•7H2O, selectively.

著者

小林 和弘 織田 範一 伊藤 磯雄

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.101, no.9, pp.806-813, 1981-09-25 (Released:2008-05-30)

参考文献数

14

被引用文献数

1 1

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As the initial study of variations of skeletons of antitumor antibiotics, simple synthesis of naphtho [2, 3-g] quinolines (IIIa, b, VIII) and naphtho [2, 3-g] quinoxalines (XIIIa, b), which are novel heterocyclic ring systems, was carried out by Diels-Alder reaction of 1, 2-dimethylenecyclohexane with quinoline-5, 8-diones (Ia-c) or quinoxaline-5, 8-diones (IIa, b). Air oxidation of these Diels-Alder adducts gave tetrahydro naphtho [2, 3-g] quinolines (IVa, b, IX) and tetrahydronaphtho [2, 3-g] quinoxalines (XVa, b). The Diels-Alder adducts and aromatized compounds were converted into the corresponding diacetoxynaphtho [2, 3-g] quinolines (VI, VII, X) and diacetoxynaphtho [2, 3-g] quinoxalines (XVII, XVIII).

著者

小林 和弘 織田 範一 榊原 仁作

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.103, no.2, pp.165-172, 1983-02-25 (Released:2008-05-30)

参考文献数

16

被引用文献数

1 1

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Ethyl 5-hydroxybenzo [α] phenazine-6-carboxylates (IIa, b) were prepared by the condensation of ethyl 1, 4-dihydro-1, 4-dioxo-3-methoxy-2-naphthoate (I) with o-phenylene-diamines. Acylations and alkylations of IIa, b gave the corresponding o-acyl and alkyl compounds (IIIa-k). The reaction of IIa, b with ethanolamine gave β-hydroxyethyl-carboxamides (Va, b). Compound Va was converted into β-chlorinated compound (VIa), whose chlorine was substituted by dialkylamines to give ethylenediamine-type amides (VIIa, b, c). Compounds VIId and VIIe were obtained by the reaction of IIb with dialkylalkylenediamines. Oxidation of IIa, b afforded N-oxides (IXa, b). The antimicrobial activities of all synthetic compounds were tested by paper discagar diffusion assay. Compounds IIId, e, g, VIIa and IXa showed inhibitory activities to T. interdigitale and IXa to C. albicans.

著者

小林 和弘 織田 範一 榊原 仁作

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.103, no.4, pp.473-479, 1983-04-25 (Released:2008-05-30)

参考文献数

8

被引用文献数

1 1

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Ethyl 1, 4-dihydro-1, 4-dioxo-3-methoxy-2-naphthoate (I) is condensed with amidines, 2-aminopyridines and 3-aminopyrazole, to give new tetracyclic quinones (IIIa-c and VI) containing nitrogen atom and hydrogenation of IIIa and IIIb over Pd-C or Raney-Ni afforded 1, 2, 3, 4-tetrahydro (IXa, b) or 1, 2, 3, 4, 7, 8, 9, 10-octahydrobenzo[g]pyrido[2, 1-b]quinazoline (Xa), respectively. Benzo[g]pyrido[2, 1-b]quinazoline derivatives except for Xa showed inhibitory activities to S. aureus and T. interdigitale.

著者

小松 俊哉 矢野 雅士 稲田 治明 岩本 光男 岡田 一男 鈴木 健一

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.115, no.12, pp.1016-1021, 1995-12-25 (Released:2008-05-30)

参考文献数

9

被引用文献数

3 3

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The two mono-hydroxylated metabolites of 9-amino-2, 3, 5, 6, 7, 8-hexahydro-1H-cyclopenta [b] quinoline monohydrochloride monohydrate (NIK-247), which is a new drug for the treatment of dementia, were synthesized to determine their chemical structures. Reduction of two tricyclic ketones, 9-amino-1, 2, 3, 5, 6, 7-hexahydro-8H-cyclopenta [b] quinolin-8-one and 9-amino-2, 3, 5, 6, 7, 8-hexahydro-1H-cyclopenta [b]-quinolin-1-one, with NaBH4 afforded the corresponding racemic alcohols. The optically active mono-hydroxylated metabolites, (+)-9-amino-2, 3, 5, 6, 7, 8-hexahydro-1H-cyclopenta [b] quinolin-8-ol and (+)-9-amino-2, 3, 5, 6, 7, 8-hexahydro-1H-cyclopenta [b] quinolin-1-ol, were obtained by optical resolution of each racemic alcohol using (+)-di-p-toluoyl-D-tartaric acid.

著者

阿部 誠治

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.54, no.4, pp.346-347, 2018

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2014年6月より2年間、米国ニューヨーク州に留学してきた。研究は統合失調症や自閉症に関する基礎研究でマウスを使った動物実験が主な内容であった。初めての海外生活、実験内容もほとんど初めてということもあり、なかなか上手くいかなかったが、徐々に慣れてきて何とかこなすことができた。留学を通して得られた物は多くあり、多くの方に海外での挑戦をして欲しいと思う。

著者

岸本 堅太郎

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.55, no.1, pp.53_3, 2019 (Released:2019-01-01)

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米国で民間保険会社から委託を受けたPBM(薬剤給付管理会社)が作成する医薬品の推奨リストのこと.通常は,①競合のない医薬品,②競合のある中で推奨される医薬品(臨床上の有用性,リベートなど),③競合のある他の医薬品,④後発医薬品に4分類されることが多い.また,全ての医薬品が収載されているわけではない.日本の薬価基準と違い,価格は載っていない.