Takeda Chemical Industries, Inc.

Hitachi, Ltd.

Tatsuo Chemical Ind., Ltd.

Yoshinobu Yoshimura

Akio Miyake

Mitsuo Numata

Tatsuo Nishimura

Shoji Kishimoto

Takatsuka Yashiki

Naoto Hashimoto

Nobuharu Kakeya

Yoshiaki Kato

Kiminori Tomimatsu

Naoru Hamaguchi

Kunio Takanohashi

Yoko Nishida

Norio Tada

Kouzi Onishi

Nobuhide Morikawa

An apparatus for directly connecting an analytical column and a mass spectrometer comprising a fixed member having at least four holes which respectively introduce washing solution, eluate containing a component eluted from the analytical column, desalting solution and eluent for eluting the component, and a movable member rotated with respect to an axis having at least four tubes around the axis and mounting the four trapping columns, whereby the trapping columns are respectively washed, trapped, desalted and eluted in parallel. Furthermore, a common trapping column may be used instead of the four trapping columns by controlling the apparatus with four analytical modes.

Apparatus for directly coupling analytical column with mass spectrometer

A compound of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl group; R.sub.2 is an unsubstituted or lower alkyl-substituted alicyclic alkyl group of 3 to 12 carbon atoms or a C.sub.3-6 alicyclic alkyl-substituted lower alkyl group or a pharmaceutically acceptable salt thereof, processes for preparing the same, a pharmaceutical composition thereof are provided. The compound has an improved absorbability and can be orally applied as antibiotics.

Cephalosporin ester derivatives

This invention relates to a compound of the formula: ##STR1## wherein Q is nitrogen or CH; R.sup.1 is hydrogen or a lower alkyl group which may be substituted; and ring A is a pyridine or pyridazine ring which is substituted at the ring-constituting carbon atom by a group of the formula:

Cephem compounds, their production and use

A compound of the general formula: ##STR1## wherein R.sup.0 is hydrogen, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; A is S, S.fwdarw.O, O or CH.sub.2 ; R.sup.4 is hydrogen, methoxy group or formamido group; R.sup.13 is hydrogen, methyl, hydroxyl or a halogen; and A is an optionally substituted condensed cyclic group formed by combining an imidazole or pyrazole ring with 5- or 6-membered nitrogen-containing aromatic heterocyclic ring to share a C-N bond with each other, or a salt or ester thereof. and a process for preparing the same and a pharmaceutical composition thereof are disclosed.

Antibacterial compounds, and use

A compound having the general formula ##STR1## wherein, R.sup.0 is a hydrogen atom, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; Z is S, S.fwdarw.O,O or CH.sub.2 ; R.sup.4 is a hydrogen atom, a methoxy group, or a formamide group; R.sup.13 is a hydrogen atom, a methyl group, a hydroxyl group, or a halogen atom; A.sym. is a condensed triazolio group which may be substituted, or a pharmaceutically acceptable salt or ester thereof is novel and has an excellent antibacterial activity.

Cephem compounds

A compound of the formula ##STR1## wherein (1) R.sub.1 is a lower alkyl group of 2 to 6 carbon atoms or a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a cycloalkyl group of 5 to 7 carbon atoms or a lower alkyl group of 1 to 3 carbon atoms which is substituted by a cycloalkyl group of 5 to 7 carbon atoms or by a phenyl group, or (2) R.sub.1 is a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a lower alkyl group of 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.

1-Acyloxyalkyl esters of cephalosporin

A compound of the formula: ##STR1## or a pharmaceutical acceptable salt thereof, processes for preparing the same and a pharmaceutical composition containing the compound or the salt thereof mentioned above are provided. The compound has antibiotic activity and has improved absorbability.

Cephalosporin esters, their production and use

A novel steroid compound of the formula ##STR1## wherein A is a lower alkylene group; ##STR2## is an acyl group; and  is a single bond or a double bond, and methods of producing the compound (I) as follows: ##STR3## and a pharmaceutical composition containing the compound (I). The compound (I) exhibits excellent antiandrogenic activity on oral administration and can be used for the treatment of prostatic hypertrophy.

Double ester of 16.beta.-ethylestran-17.beta.-ol derivatives

Cephalosporin derivatives of the formula: ##STR1## wherein R.sub.1 is methyl or ethyl and R.sub.2 is a straight-chain or branched alkyl group of 5 to 7 carbon atoms, and their pharmaceutically acceptable salts, which are effective as orally administrable antibiotic agents against both gram-positive- and negative-bacteria, and the production and compositions thereof, are proposed.

Cephalosporin derivatives

Crystallized cephalosporin salts, particularly crystalline addition salt of pivaloyloxymethyl 7.beta.-[2-(2-aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl)-1 H-tetrazol-5-yl]thio]methyl]ceph-3-em-4-carboxylate with hydrochloric acid, tartaric acid or citric acid, which is very stable and is readily adsorbable through intestinal tract, with little individual differences, when the salt is applied orally.

Crystallized cephalosporin salts

A cephalosporin derivative of the formula: ##STR1## wherein R represents ##STR2## or its pharmaceutically acceptable acid addition salt is found to be useful as orally administrable antibiotics having broad anti-microbial activities against both Gram-positive and Gram-negative bacteria.

Cephalosporin esters

Novel cephalosporin derivatives, namely pivaloyloxymethyl 7.beta.-[2-(2-aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl)-1 H-tetrazol-5-yl]thio]methyl]-ceph-3-em-4-carboxylate and its pharmaceutically acceptable acid addition salts are found to be useful as orally administrable antibiotics having broad antimicrobial activities against both gram-positive and gram-negative bacteria.

Growing community of inventors

Ibaraki, Japan

Yoshinobu Yoshimura