Toyo Jozo Kabushiki Kaisha

Kokusan Chemical Works Limited

Susumu Watanabe

Nobuaki Nakagawa

Toshiharu Noda

Tetsuo Matsuda

Hideo Sakakibara

Tatsuro Fujiwara

Shigeo Katsuragi

Kunio Matsumoto

Kunio Ohyama

Osamu Okegawa

Tadashiro Fujii

Kaoru Morita

Toshiyuki Watanabe

Sadami Kobari

Tsutomu Hirata

Kiyoharu Takahashi

Akira Ohtsuka

Yoshitaka Kagimoto

Satoshi Omura

Masaru Otani

Eiichi Honda

Kikuo Kotani

Masahiko Taniuchi

Eisuke Munekata

Tadanori Morikawa

Hirose Yamauchi

Tosio Meguro

Shunpei Sakakibara

Kazuhiko Matsumoto

Shuichi Kitazawa

A method for assay of enzyme activity which comprises treating an amide compound of the formula ##STR1## with peptidase; treating thus-liberated amine of the formula ##STR2## with an oxidase which consume oxygen and forms pigment by oxidative condensation of said amine with a coupler of the formula ##STR3## and quantitatively measuring the detectable changes. Also disclosed is an assay method which comprises treating an amide compound of the formula ##STR4## or a salt thereof, with peptidase to liberate an aniline derivative of the formula ##STR5## oxidizing said aniline derivative; and quantitatively measuring detectable change.

Assaying peptidase enzyme activity

A compound of the formula ##STR1## wherein R is L-leucyl or .gamma.-L-glutamyl and X and Y are halogen and are the same or different, or a salt thereof. These compounds are useful as synthetic substrates for assaying peptidase activity.

Novel synthetic substrate and assay method using the same

Apparatus for performing an immunoassay, comprises in combination a reaction tube closed at its bottom, and in the reaction tube a molded element having on its surface material having specific binding ability for a component in a liquid specimen to be assayed. The shape of the surface of the element adjacent the interior surface of the tube is the complement of the shape of the interior surface of the tube. A spacer rib is provided on the element, in contact with the interior surface of the tube. This rib holds the element in such position in the tube that the surfaces of complementary shape of the element and tube are shaped from each other a small but constant distance. A thin layer of constant thickness of a liquid specimen for immunoassay is thus receivable between the complementary surfaces. This arrangement increases the contact surface of the liquid medium in the reaction tube by the element, by establishing a homogeneous uniform layer of liquid medium. This avoids the need for stirring and shaking and reduces the required volume of the specimen to be assayed.

Element for immunoassay

Peptides for assaying human parathyroid hormone

C-Terminal fragment of human chorionic gonadotropin

Novel amine compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl and R.sub.2 is substituted methyl amino or D-amino acid residue, or a salt thereof. R.sub.1 can typically be isobutyl or methyl; and R.sub.2 can be methylamino of the formula

Assay method of enzyme activity

Deformyltylosin derivatives of the formula ##STR1## wherein A is ##STR2## --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R.sub.1 is hydrogen, lower alkanoyl or aryl-lower alkanoyl, X.sub.1 and X.sub.2 are hydrogen or are connected to form a valence bond, Y.sub.1 and Y.sub.2 are hydrogen or are connected to form a valence bond, Q.sub.1 is hydrogen or methyl, Q.sub.2 is hydrogen or ##STR3## R.sub.2 is hydrogen or lower alkanoyl, R is hydrogen or ##STR4## R.sub.3 is hydrogen or C.sub.2-5 alkanoyl, and R.sub.4 is hydrogen or C.sub.2-6 alkanoyl, and when R.sub.3 is not hydrogen, then R.sub.4 is not hydrogen, or a pharmaceutically acceptable salt thereof, have strong antibacterial activities as compared to the known antibiotic tylosin, and also have enhanced antibacterial activities against all macrolide antibiotic-resistant strains such as A, B and C group strains, and have higher blood levels as compared with tylosin.

Deformyltylosin derivatives

A polyfunctional disulfide compound, useful as a cross-linking reagent having S--S exchange reactivity, of the formula ##STR1## wherein R is 2-benzothiazolyl or 2-pyridyl-N-oxide and X is a spacer group having an alkylene group directly bonded to each S--S group.

Polyfunctional disulfide compounds having S--S exchange reactivity

Derivatives of antibiotic tylosin of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkanoyl, A.sub.1 and A.sub.2 are groups of which one is R.sub.2 and the other is R.sub.3, and R.sub.2 and R.sub.3 are C.sub.2-6 alkanoyl, or a physiologically acceptable salt thereof, have enhanced antibacterial activity against macrolide antibiotic-resistant strains.

Derivatives of antibiotic tylosin

3'-acylated macrolide antibiotics of the formula ##STR1## wherein R.sub.1 is hydrogen or C.sub.2-3 alkanoyl, R.sub.2 is hydrogen or C.sub.2-4 alkanoyl, at least one of R.sub.1 and R.sub.2 being hydrogen, and one of R' and R' being R.sub.3 and the other R.sub.4, R.sub.3 being C.sub.2-6 alkanoyl and R.sub.4 being C.sub.2-5 alkanoyl, or a pharmaceutically acceptable salt thereof.

3'-Acylated macrolide antibiotics

A polypeptide having calcitonin activity of the formula ##EQU1## and the salts thereof with pharmaceutically acceptable acids.

EEL calcitonin

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Shizuoka, Japan

Susumu Watanabe