Takeda Chemical Industries, Inc.

Susumu Tsushima

Kohei Nishikawa

Hiroaki Nomura

Mitsuru Shiraishi

Michiyuki Sendai

Norichika Matsumoto

Mitsuo Numata

Muneo Takatani

Isao Minamida

Yoshio Yoshioka

Motoo Hozumi

Shoshichi Nojima

Minoru Hirata

Masayasu Kato

Yoshio Kozai

Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.

Lipid derivatives, their production and use

Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.

Substituted amine derivatives, their production and use

Novel compound of the formula: ##STR1## is useful as a platelet activating factor antagonist and is so stable that it is advantageously used as drugs.

Pyridinium nitrate, composition containing same and their use for

Disclosed 2-(syn)-hydroxyimino-acetamide derivatives of the formula: ##STR1## wherein Y is hydrogen, hydroxyl, an acyloxy, carbamoyloxy, a quaternary ammonium or a nitrogen-containing heterocyclic ring-substituted thio group; or pharmaceutically acceptable salts or esters thereof are useful as antibacterial agents. Also disclosed are processes for producing them.

Cephalosporin derivatives

Novel pyridinium derivatives represented by the formula (I): ##STR1## wherein ##STR2## is an optionally substituted pyridinium ring; R.sup.1 is a lower alkyl group or aralkyl group;

Pyridinium derivatives, their production and use

Novel phospholipids, inclusive of salts thereof, of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently an aliphatic hydrocarbon residue containing 1 to 20 carbon atoms, with the numbers of the carbon atoms for both totalling 8 to 30, and

Phospholipids

A novel phospholipid of the formula: ##STR1## wherein R.sup.1 is an alkyl group of 10 to 24 carbon atoms, R.sup.2 is a cyclic imide group and A.sup.+ is a cyclic ammonio group and a salt thereof have platelet activating factor inhibiting activity and are useful for prevention and treatment of circulatory disorders and allergic bronchial asthma.

Certain 3-alkoxy-2-cyclic-imido-propyl-phosphate-ethyl-cyclic ammonium

Novel ketoalkylphospholipids, inclusive of salts thereof, of the formula ##STR1## wherein R.sup.1 is an aliphatic hydrocarbon residue containing 10 to 20 carbon atoms,

Ketoalkylphospholipids

Method for inhibiting activities of platelet activating factor

Glycerol derivatives, inclusive of salts thereof, of the formula ##STR1## wherein R.sup.1 is alkyl or alkylcarbamoyl containing 10 to 30 carbon atoms, R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1-6 alkyl or, taken together with the adjacent nitrogen atom, form cyclic amino, and ##STR2## represents cyclic ammonio, and of the formula ##STR3## wherein R.sup.1 is as defined above, R.sup.2' and R.sup.3' are C.sub.1-6 alkyl or, taken together with the adjacent nitrogen atom, form cyclic amino and R.sup.4', R.sup.5' and R.sup.6' are independently hydrogen or C.sub.1-6 alkyl, are useful as antihypertensive agents.

Method of use of 1-(alkyl for alkylcarbanoyl)-2-carbamoylglycerol

Tridecyloxy- or tetradecyloxy-propane derivatives of the formula: ##STR1## wherein R.sup.1 is tridecyl or tetradecyl, R.sup.2 is hydrogen or --OCH.sub.3, and R.sup.3, R.sup.4 and R.sup.5 independently represent hydrogen or C.sub.1-3 alkyl, or ##STR2## represents cyclic ammonio, and their salts, have inhibitory activity to multiplication of tumor cells and antimicrobial activity.

Tridecyloxy- or tetradecyloxy-propane derivatives

Certain phosphoric acid ester derivatives of 1,3-dioxy propane

Novel 3-acyloxymethyl-cephem compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen or an acyl group; W is acetonyl, or a group represented by --X--COOH or --X--OH (X is an organic residue) or salts thereof were found to be useful as starting materials for preparing cephalosporins of the formula: ##STR2## wherein R.sup.3 stands for a residue nucleophilic compound and R.sup.1 has the same meaning as above.

Process for preparing cephalosporins

Novel 3-acyloxymethyl-cephem compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen or an acyl group; W is acetonyl, or a group represented by --X--COOH or --X--OH (X is an organic residue) or salts thereof were found to be useful as starting materials for preparing cephalosporins of the formula: ##STR2## wherein R.sup.3 stands for a residue of a nucleophilic compound and R.sup.1 has the same meaning as above.

Growing community of inventors

Suita, Japan

Susumu Tsushima