Mochida Pharmaceutical Co., Ltd.

Mochida Seiyaku Kabushiki Kaisha

Hiroshi Kosuzume

Ei Mochida

Yasuo Suzuki

Haruo Ohnishi

Masahiro Mizota

Kazuo Yamaguchi

Haruo Onishi

The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof. The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton. The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

Intermediates cephalosporin derivatives

The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof. The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton. The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

Cephalosporin compounds and pharmaceutical compositions thereof

Intermediates of cephalosporin compounds

Cephalosporin derivatives

Process for removing immune complex in blood by use of the immobilized

This invention provides a human leucocyte pepsin-like enzyme and a therapeutic agent and method for treating allergic disorders, immune complex diseases and tumors, the agent containing the enzyme as an effective ingredient. The human leucocyte pepsin-like enzyme of this invention is a protein of human origin and, therefore, a therapeutic agent containing said enzyme as an effective ingredient shows extremely little adverse reactions such as anaphylaxis and thus is highly safe.

Human leucocyte pepsin-like enzyme as a therapeutic agent for treating

Therapeutic agent for the treatment of allergic disorders, immune complex diseases and tumors, which contains a human urinary acid protease as an active ingredient, and a method for treating allergic disorders, immune complex diseases and tumors by administering the said acid protease, which has never been used as a therapeutic agent for allergic disorders, immune complex diseases and tumors. Since the acid protease is a protein of human origin, the probability of adverse reactions such as anaphylactic shock due to the antigenicity of the acid protease is believed to be extremely small.

Method for treatment of allergic disorders and immune complex diseases

There are provided a pharmaceutical composition having an effect to control phagocytic function, which comprises a pharmaceutically effective amount of human pepsin and/or a human leukocyte pepsin-like enzyme and a pharmaceutically acceptable carrier, and a therapeutic method using said composition. The pharmaceutical composition is useful for treatment of infectious diseases, gout and arteriosclerosis.

Composition for treating infectious diseases, gout or arteriosclerosis

7-Diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine and pharmaceutical

A pharmaceutical composition having diuretic, hypotensive and antiedemic effects which contains a 6-halo-4-oximino-1,2,3,4-tetrahydroquinoline derivative or a salt thereof, and a method to use the above-described derivative or a salt thereof as a diuretic, hypotensive and antiedemic agent.

Diuretic, hypotensive and antiedemic quinoline oximes

A method of producing .gamma.-globulin which can be administered intravenously without adverse reactions and loss of opsonic activity is provided. The method comprises treating .gamma.-globulin with pepsin or uropepsin in a neutral pH range of 6.0 to 7.5. The aggregates in .gamma.-globulin are selectively decomposed by the method of the present invention, while any decomposition of monomer .gamma.-globulin molecule is substantially prevented. A therapeutic agent for intravenous injection which is reduced its anticomplementary activity and is stabilized by adding uropepsin which serves simultaneously as a proteolytic enzyme and a stabilizer, to human .gamma.-globulin. Uropepsinogen can be also as a stabilizer.

Method of producing .gamma.-globulin for intravenous injection and

The compositions for therapeutic treatment contain as an active ingredient a 2-[(2-methoxyphenyl)-axo]-1H-imidazole derivative of the formula: ##STR1## wherein X is hydrogen or halogen, or a pharmaceutically acceptable salt thereof. This compound is effective for the therapeutic treatment of edema, hypotension, cardiac insufficiency and mucosa hyperemia.

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Yokohama, Japan

Hiroshi Kosuzume