scispace - formally typeset
Search or ask a question
Author

Hisao Yamaguchi

Bio: Hisao Yamaguchi is an academic researcher from Teijin. The author has contributed to research in topics: Suppository & Alkyl. The author has an hindex of 9, co-authored 36 publications receiving 399 citations.

Papers
More filters
Patent
29 Nov 1991
TL;DR: In this paper, a pharmaceutical composition for treating gout, hyperuricemia and so forth, which contains an efficacious compound of a new category, i.e., a 2-arylthiazole derivative represented by general formula (I), wherein Ar represents (un)substituted pyridyl, thienyl, furyl, naphthyl or phenyl; X represents hydrogen, alkyl or optionally protected carboxyl; and Y represents hydrogen or carbonyl.
Abstract: A pharmaceutical composition for treating gout, hyperuricemia and so forth, which contains an efficacious compound of a new category, i.e., a 2-arylthiazole derivative represented by general formula (I), wherein Ar represents (un)substituted pyridyl, thienyl, furyl, naphthyl or phenyl; X represents hydrogen, alkyl or optionally protected carboxyl; and Y represents hydrogen, alkyl, or optionally protected hydroxy or carbonyl. The invention also provides novel 2-arylthiazole derivatives included in these derivatives and pharmaceutically acceptable salts thereof.

89 citations

Patent
29 Nov 1991
TL;DR: The 2-arylthiazole derivatives are represented by the following formula (I): ##STR1## wherein Ar is an unsubstituted or substituted pyridyl, thienyl, furyl, naphthyl or phenyl group; X is a hydrogen atom, alkyl group or carboxyl group which may be protected, and Y is a hydroxyl or carbonyl group as discussed by the authors.
Abstract: Pharmaceutical compositions for treating gout or hyperuricemia and containing a new categorized compound, i.e. 2-arylthiazole derivatives, as an active ingredient, are provided. The 2-arylthiazole derivatives in the present invention are represented by the following formula (I): ##STR1## wherein Ar is an unsubstituted or substituted pyridyl, thienyl, furyl, naphthyl or phenyl group; X is a hydrogen atom, alkyl group or carboxyl group which may be protected, and Y is a hydrogen atom, alkyl group, or a hydroxyl or carbonyl group which may be protected. Furthermore, novel compounds included in the 2-arylthiazole derivatives and pharmaceutically acceptable salts thereof are provided.

59 citations

Journal ArticleDOI
Tohru Hashimoto, Koji Hasegawa, Hisao Yamaguchi1, Masahiko Saito1, Ishimoto Sachio1 
TL;DR: Batatasin, which occurs in dormant bulbils of yams and induces dormancy in this organ has been shown by spectrometric analysis and synthesis to be 3,3′-dihydroxy-5-methoxy-bibenzyl.

52 citations

Journal ArticleDOI
TL;DR: In this article, N-(2,2,4,6-tetramethyl-2,3-dihydrobenzofuran-7-yl)amide derivatives were synthesized and tested for their ability to inhibit rabbit small intestinal ACAT and lower serum total cholesterol in cholesterol-fed rats.
Abstract: Novel N-(2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)amide derivatives 1 were synthesized and tested for their ability to inhibit rabbit small intestinal ACAT (acyl-CoA:cholesterol acyltransferase) and lower serum total cholesterol in cholesterol-fed rats. Among the synthesized compounds, N-(2,2,4,6-tetramethyl-2,3-dihydrobenzofuran-7-yl)amide derivatives showed potent ACAT inhibitory activity. The synthesis and structure−activity relationships of these compounds are described. A methyl group at position 6 of the 2,3-dihydrobenzofuran moiety was important for potent ACAT inhibitory activity. In the series of N-(2,2,4,6-tetramethyl-2,3-dihydrobenzofuran-7-yl)amides, lipophilicity of the acyl moiety was necessary for the potent ACAT inhibitory activity. The highly lipophilic acid amides N-(2,2,4,6-tetramethyl-2,3-dihydrobenzofuran-7-yl)-2,2-dimethyldodecanamide (10) and 6-(4-chlorophenoxy)-N-(2,2,4,6-tetramethyl-2,3-dihydrobenzofuran-7-yl)-2,2-dimethyloctanamide (50) showed potent activity. Introduction of a di...

39 citations

Patent
27 Mar 1981
TL;DR: A pharmaceutical composition for intrarectal administration comprising a pharmaceutically effective amount of an active ingredient which when administered alone to the rectum, is substantially unabsorbable into the living body through the mucous membrane of the rectal fluid.
Abstract: A pharmaceutical composition for intrarectal administration comprising a pharmaceutically effective amount of an active ingredient which when administered alone to the rectum, is substantially unabsorbable into the living body through the mucous membrane of the rectum, said composition further containing an absorption aid acting within the rectum in such a way as to induce absorption of said active ingredient through the rectal mucous membrane, said absorption aid being characterized by (1) being substantially nontoxic to living organisms, (2) containing in the molecule at least two hydrophilic groups selected from the class consisting of carboxyl groups, acidic hydroxyl groups, carboxyl groups in the form of pharmaceutically acceptable salts, acidic hydroxyl groups in the form of pharmaceutically acceptable salts, carboxyl groups in the form of amides and acidic hydroxyl groups in the form of esters, (3) containing in the molecule at least two lipophilic groups selected from the class consisting of groups of the formulae ##STR1## and -CH2 -, the number of the lipophilic groups being not less than that of the hydrophilic groups, and (4) having a molecular weight of from about 100 to about 300; and a suppository prepared therefrom in unit dosage form.

32 citations


Cited by
More filters
Journal ArticleDOI
TL;DR: The scope of this novel method for the preparation of polycyclic arenes is illustrated by thetotal synthesis of a series of polyoxygenated phenanthrenes that are close relatives of the anticancer agent combretastatin A-4, as well as by the total synthesis of the aporphine alkaloid O-methyl-dehydroisopiline and its naturally occurring symmetrical dimer.
Abstract: Readily available biphenyl derivatives containing an alkyne unit at one of their ortho-positions are converted into substituted phenanthrenes on exposure to catalytic amounts of either PtCl2, AuCl, AuCl3, GaCl3 or InCl3 in toluene. This 6-endo-dig cyclization likely proceeds through initial pi-complexation of the alkyne unit followed by interception of the resulting eta2-metal species by the adjacent arene ring. The reaction is inherently modular, allowing for substantial structural variations and for the incorporation of substituents at any site of the phenanthrene product. Moreover, it is readily extended to the heterocyclic series as exemplified by the preparation of benzoindoles, benzocarbazoles, naphthothiophenes, as well as bridgehead nitrogen heterocycles such as pyrrolo[1,2-a]quinolines. Depending on the chosen catalyst, biaryls bearing halo-alkyne units can either be converted into the corresponding 10-halo-phenanthrenes or into the isomeric 9-halo-phenanthrenes; in the latter case, the concomitant 1,2-halide shift is best explained by assuming a metal vinylidene species as the reactive intermediate. The scope of this novel method for the preparation of polycyclic arenes is illustrated by the total synthesis of a series of polyoxygenated phenanthrenes that are close relatives of the anticancer agent combretastatin A-4, as well as by the total synthesis of the aporphine alkaloid O-methyl-dehydroisopiline and its naturally occurring symmetrical dimer.

521 citations

Journal ArticleDOI
TL;DR: Mechanistic and computational studies point to the involvement of a concerted, inner-sphere palladation-deprotonation pathway that is enabled by the presence of three-center agostic interactions at the transition state.
Abstract: Palladium-catalyzed alkane arylation reactions with aryl halides are described for the preparation of 2,2-dialkyl-dihydrobenzofuran substrates. These reactions occur in excellent yield and very high selectivity for the formation of one sole product arising from a reaction at nearby methyl groups. Mechanistic and computational studies point to the involvement of a concerted, inner-sphere palladation-deprotonation pathway that is enabled by the presence of three-center agostic interactions at the transition state. This mechanism accurately predicts the experimentally observed kinetic isotope effect as well as the site selectivity and should be useful in the design of new reactions and catalysts.

326 citations

Patent
07 Feb 1995
TL;DR: In this article, it was found that dry insulin powders are rapidly absorbed through the alveolar regions of the lungs, and that they can be inhaled by a mammalian host.
Abstract: Systemic delivery of insulin to a mammalian host is accomplished by inhalation of a dry powder of insulin. It has been found that dry insulin powders are rapidly absorbed through the alveolar regions of the lungs.

292 citations

Journal ArticleDOI
TL;DR: No extra functionalization step is required for palladium(II)-catalyzed oxidative carbocyclizations like that shown, which provide highly substituted benzofuran and dihydrobenzofuran derivatives by net dehydrogenation.
Abstract: No extra functionalization step is required for palladium(II)-catalyzed oxidative carbocyclizations like that shown, which provide highly substituted benzofuran and dihydrobenzofuran derivatives by net dehydrogenation. The mechanism is similar to that of Heck cyclizations. Products containing quaternary carbon stereocenters can be obtained in diastereomerically pure form.

198 citations