Wako Pure Chemical Industries, Inc.

Kabushiki Kaisha Yakult Honsha

Satoru Okajima

Tadashi Miyasaka

Seigo Sawada

Toshiro Hanada

Kazuhiko Yamanishi

Takashi Yaegashi

Kenichi Tezuka

Kenichiro Nokata

Akinori Shintani

Teruo Yokokura

Hiroshi Nagata

Hisako Nagai

New campotothecin derivatives and a process for preparing same are disclosed, which are represented by the general formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R.sup.4 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R.sup.5 represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 substituents should not be a hydrogen atom and also that if any one of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is a hydroxyl or lower alkoxy group, all of the other three substituents should not be a hydrogen atom.

Camptothecin derivatives

New camptothecin derivatives, useful as antitumor agents or intermediates therefor, of the general formula (I) ##STR1## wherein X is a lower alkyl group, and R is a hydrogen atom or the grouping -COY where Y is a linear or branched unsubstituted C.sub.1 -C.sub.18 alkyl group; a lower alkyl group substituted by a halogen atom or a lower alkylthio, amino, acylamino, hydroxyl, lower alkoxy, aryloxy or lower alkoxycarbonyl group; a C.sub.3 -C.sub.19 alkenyl, C.sub.3 -C.sub.19 alkynyl or C.sub.3 -C.sub.8 cycloalkyl group; a C.sub.3 -C.sub.8 cycloalkyl group substituted by an acylamino-lower alkyl group; an N-acylpyrrolidyl group; a phenyl group; a phenyl group substituted by a halogen atom or a trifluoromethyl, nitro, amino, lower alkoxycarbonyl, lower alkyl, phenyl or lower alkoxy; a cinnamyl group; a benzyl group; a naphthyl group; a pyridyl group; a furyl group; or a thienyl group, as well as acid addition salts and quaternary ammonium salts thereof, and a process for preparing the new camptothecin derivatives by subjecting 7-ethylcamptothecin to the treatment with an N-di-X-ethylenediamine followed by acylation.

Disclosed herein is a novel compound which is excellent in solubility to water around a neutral range, stable in an aqueous solution state for a long period of time, and high in coloring sensitivity with a stable coloring development, and is represented by the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same as or different from one another, represent lower alkyl groups, and X.sub.1 and X.sub.2 both represent --O(CH.sub.2).sub.n SO.sub.3 M in which M is a hydrogen atom, an alkali metal ion or NH.sub.4.sup.+, and n is an integer of 2-4, or either of X.sub.1 and X.sub.2 represents --O(CH.sub.2).sub.n SO.sub.3 M in which M and n are the same meanings as given above and the other represents a hydrogen atom. This reagent is hardly susceptible of the influence of the serum components such as hemoglobin, bilirubin and so on due to its color having absorption on a longer wavelength side. Disclosed is also a method of quantitatively measuring an oxidative substance, particularly, hydrogen peroxide, by using this color test reagent.

Triphenyl methane derivatives and method of quantitatively measuring an

Disclosed herein is a novel compound which is excellent in solubility to water around a neutral range, stable in an aqueous solution state for a long period of time, and high in coloring sensitivity with a stable coloring development, and is represented by the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same as or different from one another, represent lower alkyl groups, and X.sub.1 and X.sub.2 both represent --O(CH.sub.2).sub.n SO.sub.3 M in which M is a hydrogen atom, an alkali metal ion or NH.sub.4.sup.+, and n is an integer of 2-4, or either of X.sub.1 and X.sub.2 represents --O(CH.sub.2).sub.n SO.sub.3 M in whch M and n are the same meanings as given above and the other represents a hydrogen atom. This reagent is hardly susceptible of the influence of the serum components such as hemoglobin, bilirubin and so on due to its color having absorption on a longer wavelength side. Disclosed is also a method of quantitatively measuring an oxidative substance, particularly, hydrogen peroxide, by using this color test reagent.

Growing community of inventors

Tokyo, Japan

Satoru Okajima