Ss Pharmaceutical Co., Ltd.

Other

Bausch-lomb Incorporated

Akihiro Shibata

Takemitsu Asaoka

Hideaki Matsuda

Tadayuki Kuraishi

Tatsuhiko Katori

Sunao Takeda

Naokata Taido

Fujiko Konno

Ryuichi Kawahara

Susumu Sato

Lyle M Bowman

Masaru Matsumoto

Katsumi Imamori

Santosh K Chandrasekaran

Mari Ohtsuka

Teruo Komoto

Masami Takahashi

Fumio Ishii

Koichi Tachibana

Yoshihiko Kanamaru

Hiroyuki Hirota

Samir Roy

Hiroyuki Naito

Hidehiko Kohya

Terumitsu Kaihoh

Kenichi Kukita

Yoshihiro Nishikawa

Tasdayuki Kuraishi

Kimihiro Kanemitsu

Santosh Kumar Chandrasekaran

The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.

Quinolone carboxylic acid compositions and related methods of treatment

Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Substituted benzylurea derivatives and medicine containing the same

Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Substituted vinylurea derivatives and medicine containing the same

A quinolone carboxylic acid derivative having the following formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH.sub.2, O, S, SO, SO.sub.2, or N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms; or a salt thereof; and an antimicrobial agent comprising the same. The compound exhibits a superior antimicrobial activity, especially against gram positive microorganisms, and is thus useful for the treatments and prevention of various infectious diseases in clinics.

Quinolone carboxylic acid derivatives

5-aminoquinolone carboxylic acid derivative and antibacterial agent

Quinoline carboxylic acid derivatives

Derivatives of .alpha.,.alpha.-trehalose-6,6'-fatty acid diester having phosphoric ester groups in the molecule which are useful as a carcinostatic agent. One of the derivatives may be prepared by reacting diphenylphosphoryl chloridate with a derivative of 2,3,2',3'-tetra-O-benzyl-.alpha.,.alpha.-trehalose-6,6'-fatty acid diester. Another derivative may be obtained by substituting benzyl groups at 2,3,2',3' positions of trehalose with hydrogen atoms.

Derivative of .alpha., .alpha.-trehalose and a process for preparing the

Disclosed herein are novel .alpha.,.alpha.-trehalose fatty acid diester derivatives useful as carcinostatic substances and surface-activating materials and represented by the general formula (I): ##STR1## wherein R.sup.1 means an alkyl group having 1-21 carbon atoms, R.sup.2 denotes a hydrogen atom or carbobenzoxy group, and R.sup.3 stands for a hydrogen atom or benzyl group. Their preparation processes are also disclosed.

.alpha.,.alpha.-trehalose fatty acid diester derivative

Growing community of inventors

Yachiyo, Japan

Akihiro Shibata