The Effect of Compaction Force on the Transition to Hydrate of Anhydrous Aripiprazole.

abstract：:The hypoglycemic component, elatoside E, was isolated from the root cortex of Aralia elata SEEM. (Araliaceae) together with elatoside F and eight known oleanolic acid glycosides, elatosides A and C, oleanolic acid 3-O-[alpha-L-arabinofuranosyl (1-->4)]-beta-D-glucopyranosiduronic acid, oleanolic acid 3-O-beta-D-glucop...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Murakami T,Harada E,Murakami N,Yamahara J,Matsuda H

更新日期：1996-10-01 00:00:00

abstract：:A novel time-controlled system based on elementary osmotic pump tablet containing a drug-resin complexes (DRCs) core is presented. In the traditional osmotic pump tablets (OPTs), the lag time was always minimized. On the contrary, in the DRCs osmotic pump tablet (DRCOPT), the lag time was increased to achieve time-con...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang C,Chen F,Heng PW,Li JZ,Li X,Ye GH,Nie SF,Pan WS

更新日期：2008-04-01 00:00:00

abstract：:A series of optically active substituted 1,2-dihydro-6-oxo-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acids was prepared via optically active 2-methyl-4,5-difluoroindoline (10) and tested for antibacterial activities. Among them, (2S)-9-[(3R,1'S)-3-(1'-amino)ethyl-1-pyrrolidinyl]-8-fluoro-1,2-dihydro- 2- methyl-6-oxo-6H-...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsuji K,Tsubouchi H,Ishikawa H

更新日期：1995-10-01 00:00:00

abstract：:From the water-soluble portion of the methanolic extract of the fruit of anise (Pimpinella anisum L.), which has been used as a spice and medicine since antiquity, twelve new and five known glucosides of phenylpropanoids, including four stereoisomers of anethole glycol 2'-O-beta-D-glucopyranoside and four stereoisomer...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishikawa T,Fujimatu E,Kitajima J

更新日期：2002-11-01 00:00:00

abstract：:Anti-tauro 1 beta-hydroxycholic acid antisera were prepared by immunizing rabbits with N-(1 beta,3 alpha, 7 alpha, 12 alpha-tetrahydroxy-5 beta-cholan-24-oyl)-2- aminopropionic acid-bovine serum albumin (BSA) conjugate. The antisera raised had high affinity (1.25-1.46 x 10(9) M-1) and specificity for conjugated 1 beta...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikegawa S,Murai T,Yoshimura T,Tohma M

更新日期：1992-07-01 00:00:00

abstract：:Infection with Helicobacter pylori (H. pylori) plays an important role in the pathogenesis of gastritis, peptic ulcer and gastric cancer, and the 13C-urea breath test (13C-UBT) is a convenient and non-invasive method for the detection of H. pylori in the stomach. We have examined the sensitivity, specificity and accur...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajiwara M,Iida K,Takatori K,Taniguchi Y,Kimura K

更新日期：1997-04-01 00:00:00

abstract：:The fluorometric thiobarbituric acid (TBA) assay of blood plasma was performed under various conditions in order to assess whether the assay reflects lipid peroxidation. The TBA-reactivity of malonaldehyde was not dependent on the pH values of the reaction and was little affected by tert-butyl hydroperoxide (tert-BuOO...

journal_title：Chemical & pharmaceutical bulletin

authors： Kojima T,Kikugawa K,Kosugi H

更新日期：1990-12-01 00:00:00

abstract：:To develop non-prodrugs of taxoids with satisfactory stability in vivo, high water-solubility, and potent antitumor activity, we prepared several 10-O-sec-aminoethyl docetaxel analogs (3) and evaluated their cytotoxicity against mouse leukemia and human tumor cell lines, microtubule disassembly-inhibitory activity, an...

journal_title：Chemical & pharmaceutical bulletin

authors： Uoto K,Takenoshita H,Yoshino T,Hirota Y,Ando S,Mitsui I,Terasawa H,Soga T

更新日期：1998-05-01 00:00:00

abstract：:Alkylidenemalonates were readily dimerized in the presence of SmI2 to give 2,3-disubstituted 1,1,4,4-butanetetracarboxylates as mixtures of meso and racemic isomers in moderate to good yields. The structure of the less polar isomer of tetraethyl 2,3-diphenyl-1,1,4,4-butanetetracarboxylate was determined by X-ray cryst...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamashita M,Okuyama K,Kawasaki I,Nakamura S,Nagamine R,Tsujita T,Ohta S

更新日期：2000-11-01 00:00:00

abstract：:From the air-dried root of Glycyrrhiza uralensis, collected in the northeastern part of China, ten new oleanane-type triterpene oligoglycosides were isolated together with glycyrrhizin (1) and several known flavonoids. Among the newly isolated triterpene oligoglycosides, the chemical structures of licorice-saponin A3 ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa I,Hori K,Taniyama T,Zhou JL,Yoshikawa M

更新日期：1993-01-01 00:00:00

abstract：:This paper describes practical and selective hydrogenation methodologies using heterogeneous palladium catalysts. Chemoselectivity develops dependent on the catalyst activity based on the characteristic of the supports, derived from structural components, functional groups, and/or morphologies. We especially focus on ...

journal_title：Chemical & pharmaceutical bulletin

authors： Monguchi Y,Ichikawa T,Sajiki H

更新日期：2017-01-01 00:00:00

abstract：:A series of 43 stilbene derivatives that showed cytotoxicity against human lung carcinoma (A549) was analyzed using comparative molecular field analysis (CoMFA) for defining the hypothetic pharmacophore model. The polyoxylated stilbenes were found to be active inhibitors of tubulin polymerization. Several cis-stilbene...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim S,Min SY,Lee SK,Cho WJ

更新日期：2003-05-01 00:00:00

abstract：:The interaction of a newly developed Helicobacter pylori eradicating agent (TG44, 4-methylbenzyl-4'-[trans-4-(guanidinomethyl)cyclohexylcarbonyloxy]biphenyl-4-carboxlylate monohydrochloride) with beta-cyclodextrin (beta-CyD) in aqueous solution and in solid state was studied to gain insight into the high in-vivo H. py...

journal_title：Chemical & pharmaceutical bulletin

authors： Anzai K,Mizoguchi J,Yanagi T,Hirayama F,Arima H,Uekama K

更新日期：2007-10-01 00:00:00

abstract：:The object of this study was to develop hydroxypropyl methylcellulose (HPMC) based cephalexin extended release tablet, which can release the drug for six hours in predetermined rate. Twenty-one batches of cephalexin tablets were prepared by changing various physical and chemical parameters, in order to get required th...

journal_title：Chemical & pharmaceutical bulletin

authors： Saravanan M,Sri Nataraj K,Ganesh KS

更新日期：2003-08-01 00:00:00

abstract：:Chlorpheniramine (CPM) maleate was prepared as a series of resinates by the batch method. The several resinates were investigated by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and infrared (IR) spectrometry. The results from DSC and XRPD showed that the molecular state of the entrapped dr...

journal_title：Chemical & pharmaceutical bulletin

authors： Akkaramongkolporn P,Yonemochi E,Terada K

更新日期：2000-02-01 00:00:00

abstract：:A vaginal suppository containing ulinastatin (UTI) was developed as a hospital pharmacy product from UTI injection solution and Witepsol® S-55. After mixing at 50°C for 0-8 h, UTI suppositories were prepared, which had good UTI content uniformity. Because 2% surfactant was contained in S-55, the UTI injection solution...

journal_title：Chemical & pharmaceutical bulletin

authors： Kishino T,Inoue Y,Inoue K,Saito K,Kondo M,Otsuka K,Terukina T,Hattori Y,Otsuka M

更新日期：2018-01-01 00:00:00

abstract：:beta-Cyclododecyl aspartate was prepared and its application to peptide synthesis was examined. Derivatives of beta-cyclododecyl aspartate are more likely to crystallize and should be useful for peptide synthesis. The cyclododecyl ester was much stable to bases than the benzyl ester and rather more stable than the cyc...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawasaki K,Murakami T,Koshino K,Namikawa M,Maeda M,Hama T,Mayumi T

更新日期：1994-04-01 00:00:00

abstract：:The microbial transformation of five flavans (1-5) by endophytic fungi isolated from the tea plant Camellia sinensis was investigated. It was found that the endophytic filamentous fungus Diaporthe sp. oxidized stereoselectively at C-4 position of (+)-catechin (1) and (-)-epicatechin (2) to give the correspondent 3,4-c...

journal_title：Chemical & pharmaceutical bulletin

authors： Agusta A,Maehara S,Ohashi K,Simanjuntak P,Shibuya H

更新日期：2005-12-01 00:00:00

abstract：:Two major and two minor forms of dihydrodiol dehydrogenase with similar molecular weights of around 36000 were purified from monkey liver cytosol. All the forms oxidized trans-dihydrodiols of benzene and naphthalene and reduced aromatic aldehydes, but showed differences in charge, specificity for other substrates and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakagawa M,Harada T,Hara A,Nakayama T,Sawada H

更新日期：1989-10-01 00:00:00

abstract：:In the pharmaceutical preparation of a controlled release drug, it is very important and necessary to understand the entire release properties. As the first step, the dissolution test under various conditions is selected for the in vitro test, and usually the results are analyzed following Drug Approval and Licensing ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukui A,Fujii R,Yonezawa Y,Sunada H

更新日期：2006-08-01 00:00:00

abstract：:New gamma-pyrones, 9'-oxopodopyrone (3) and 8-methyl-9'-oxopodopyrone (4) were isolated from the leaves of Gonystylus keithii, along with known gamma-pyrones, 10'-oxopodopyrone (1) and 8-methyl-10'-oxopodopyrone (2). These gamma-pyrones markedly inhibited the bovine parathyroid hormone (PTH)-induced Ca release from ne...

journal_title：Chemical & pharmaceutical bulletin

authors： Kanazawa T,Ohkawa Y,Kuda T,Minobe Y,Tani T,Nishizawa M

更新日期：1997-06-01 00:00:00

abstract：:The Michael reaction of malonates with maleates afforded the corresponding adducts in high yields with high enantioselectivities (up to 98% enantiomeric excess (ee)) by using dilithium 3,3'-dichlorobinaphtholate as a catalyst. The obtained Michael adducts could be converted to optically active tricarboxylic acid (TCA)...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakamoto M,Kaneko T,Orito Y,Shimoda Y,Nakajima M

更新日期：2019-01-01 00:00:00

abstract：:Two new friedelane-type triterpenes named 12alpha-hydroxyfriedelane-3,15-dione and 3beta-hydroxyfriedelan-25-al, together with six known compounds were isolated from the stems of Drypetes paxii Hutch. (Euphorbiaceae). Their structures were established on the basis of conventional 1 dimensional (1D) NMR methods, 2D shi...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiozem DD,Trinh-Van-Dufat H,Wansi JD,Mbazoa Djama C,Fannang VS,Seguin E,Tillequin F,Wandji J

更新日期：2009-10-01 00:00:00

abstract：:Fourteen flavonol glycosides including two new compounds were isolated from the leaves of two Diospyros plants (D. cathayensis and D. rhombifolia). The structures of isolated compounds were determined by spectroscopic analysis. The scavenging activity of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical of the isolated com...

journal_title：Chemical & pharmaceutical bulletin

authors： Furusawa M,Tanaka T,Ito T,Nakaya K,Iliya I,Ohyama M,Iinuma M,Murata H,Inatomi Y,Inada A,Nakanishi T,Matsushita S,Kubota Y,Sawa R,Takahashi Y

更新日期：2005-05-01 00:00:00

abstract：:Stereoisomers of thiol proteinase inhibitor (TPI) were synthesized by a conventional solution method. Among them, iNoc-D-Gln-Val-Val-Ala-Ala-pNA weakly inhibited the amidolytic activity of papain, although iNoc-Gln-Val-Val-Ala-Ala-pNA inhibited papain activity fairly potently. However, the other five D-amino acid-cont...

journal_title：Chemical & pharmaceutical bulletin

authors： Iguchi S,Hirano K,Okamoto H,Okamoto Y,Okada Y

更新日期：1996-08-01 00:00:00

abstract：:The purpose of this study was to elucidate the effect of high-temperature storage on the stability of ranitidine, specifically with respect to the potential formation of N-nitrosodimethylamine (NDMA), which is classified as a probable human carcinogen. Commercially available ranitidine reagent powders and formulations...

journal_title：Chemical & pharmaceutical bulletin

authors： Abe Y,Yamamoto E,Yoshida H,Usui A,Tomita N,Kanno H,Masada S,Yokoo H,Tsuji G,Uchiyama N,Hakamatsuka T,Demizu Y,Izutsu KI,Goda Y,Okuda H

更新日期：2020-10-01 00:00:00

abstract：:Four vitamin D3 analogues (7a, 7b, 7c and 7d) bearing a hydroxyalkoxy group at the 2 beta-position were synthesized from the alpha-epoxide (5). The C-3 analogue (7b) showed the highest potency for elevating plasma calcium levels in rats. Furthermore, the 25-hydroxylated C-3 analogue (ED-71) (3), prepared from the 25-h...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyamoto K,Murayama E,Ochi K,Watanabe H,Kubodera N

更新日期：1993-06-01 00:00:00

abstract：:In the course of our research on spiro-compounds as neurokinin receptor antagonists, N-[2-aryl-4-(spiro-substituted piperidin-1'-yl)butyl]carboxamides were designed, based on YM-35375 (3) as a lead compound, and evaluated for NK2 receptor-antagonistic activities. Some derivatives inhibited the binding of radio-labeled...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Kakefuda A,Nagaoka H,Yamamoto O,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:A synthetic platform for chlorpromazine (CPZ) oligomers, which could be generated via photo-reaction of CPZ, is essential to promote their biological and structural studies. In this paper, the first synthetic platform for CPZ oligomers is described. A photo-irradiation experiment of CPZ to confirm whether the structur...

journal_title：Chemical & pharmaceutical bulletin

authors： Kohiki T,Nishikawa Y,Inokuma T,Shigenaga A,Otaka A

更新日期：2017-01-01 00:00:00

abstract：:Pyrrole-2,5-dicarboxylates were rapidly and selectively reduced to the corresponding mono-alcohol using 3 eq of diisobutylaluminum hydride at 0°C. Pyrrole-2,4-dicarboxylate showed the same reactivity; however, the selectivity decreased with pyrrole-3,4-dicarboxylate. When the nitrogen atom of the pyrrole-2,5-dicarboxy...

journal_title：Chemical & pharmaceutical bulletin

authors： Yasui E,Tsuda J,Ohnuki S,Nagumo S

更新日期：2016-01-01 00:00:00