Abstract: Antibiotic TM-531 having the formula: ##STR1## TM-531 is effective against gram-positive bacteria, plant pathogenic microorganisms and protozoa.
Abstract: A stable suppository useful as an antiasthmatic agent containing 3-formylamino-4-hydroxy-.alpha.-[N-(1-methyl-2-p-methoxyphenylethyl)aminom ethyl]benzyl alcohol.1/2fumarate monohydrate, polyvinyl pyrrolidone, and at least one of cyclodextrin, dextran and magnesium metasilicate aluminate together with a suppository base.
Abstract: This invention relates to new 7-substituted-3-cephem-4-carboxylic acids and pharmaceutically acceptable salts thereof, which have antimicrobial activities, and processes for preparation thereof, to intermediates for preparing the same and processes for preparation thereof, and to pharmeceutical compositions comprising the same and methods of using the same prophylactically and therapeutically for treatment of infectious diseases in human beings and animals.
Abstract: The invention relates to novel amino or acylamino-substituted pyrimidinyl cephalosporanic acid derivatives and pharmaceutically acceptable salts thereof, of antibacterial activity, to processes for the preparation thereof, and to pharmaceutical compositions comprising the novel cephalosporanic acid derivatives.
Abstract: An oxoazetidine derivative compound of the formula: ##STR1## wherein R.sub.1 represents a substituted or unsubstituted amino radical and R.sub.3 represents a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, and --SR.sub.2 is a residue of a thiophilic sulphur nucleophile.
Abstract: A new type of plasminogen-activating substance is extracted from the bile of hogs, which substance is characterized by;(A) a molecular weight of 80,000 .+-.10,000;(B) an isoelectric point of 7.1;(C) an ultraviolet absorption spectrum showing a peak (.lambda. max) at a wave length of about 278 nm;(D) a fibrinolysis activity such that a Ca-added standard fibrin plate is lysed but a heated fibrin plate is not lysed;(E) such a high thermal stability that heating at a temperature of 80.degree. C. for 10 minutes causes the plasminogen-activating activity to be decreased to an extent corresponding to 50% of the original activity and heating at a temperature of 60.degree. C.
Abstract: A process for preparing an azetidinone of the formula: ##STR1## which comprises reacting a C-unsubstituted methyleneamine of the formula: ##STR2## with R.sup.2 --CH.sub.2 COOH, its acid halide or anhydride, in the presence of boron trihalide and an organic base, wherein R.sup.1 is an organic residue bearing a carboxy group or its derivative and R.sup.2 is azido, substituted amino, halogen, acyloxy, alkoxy, aryloxy or aralkoxy.
Abstract: Derivatives of 5-substituted 2-pyrrolidinecarboxylic acid which have the general formula ##STR1## are useful in compositions as antihypertensive agents.
Abstract: The invention relates to novel 7.alpha.-methoxycephalosporin derivatives having at the 7.beta.-position an amido group acylated by a 1,3-dithietane carboxylic acid residue and to 7.beta.-isothiazolylthioacetamido-7.alpha.-methoxycephalosporins having antibacterial activity by themselves and, as the case may be, capable of being converted into the aforesaid 7.alpha.-methoxycaphalosporin derivatives. The compounds of this invention exhibit excellent antibacterial activity and are particularly effective against gram negative bacteria.
Abstract: 3,7-Disubstituted-3-cephem-4-carboxylic acid compounds having bacteriostatic properties and the following formula: ##STR1## in which R.sup.1 is thiadiazolyl or isothiazolyl, each of which may have suitable substituent(s), or thiazolyl; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is carboxy or protected carboxy; R.sup.4 is hydrogen, acyloxy or a heterocyclicthio group which may have suitable substituent(s); and R.sup.5 is hydrogen or lower alkoxy, process for making same and treating infectious diseases therewith.
Abstract: 7.alpha.-Methoxy-3-p-sulfooxy or p-hydroxycinnamoyloxymethyl cephalosporin derivatives which are useful as antibiotics and as intermediates for the production of other 7.alpha.-methoxycephalosporin derivatives.
Abstract: Hyaluronidase obtained from Streptomyces koganeiensis has the following characteristics:(a) Acts as an endo B-hexosaminidase(b) Degrades hyaluronic acid but not chondroitin sulfate A, C, or chondroitin(c) Optimum pH around 4.0(d) Stable pH range 4.0-11.3(e) Optimum temperature around 60.degree. C.(f) Stable a temperature below 60.degree. C.
Abstract: A novel coating agent for solid medicaments containing a hydrogel-like substance of a water-insoluble hydroxypropyl cellulose having 5-16% by weight of a hydroxypropoxy group or the dry powder of a hydrogel-like substance. By coating solid medicaments with the coating agent, solid medicaments having high impact resistance and showing very less aging can be provided advantageously in industry.
Abstract: Novel 4-(2'-pyridylamino)phenylacetic acid derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen, a halogen, a lower alkyl having 1 to 3 carbon atoms, or nitro, R.sub.2 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R.sub.3 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R.sub.4 is hydrogen or a lower alkyl having 1 to 3 carbon atoms, R.sub.5 is hydrogen or --CH.sub.2 CH.sub.2 OR.sub.6 wherein R.sub.6 is a lower alkyl having 2 or 3 carbon atoms and being substituted with 1 or 2 hydroxy groups, provided that R.sub.1 or R.sub.2 is not 4-halogen, or pharmaceutically acceptable salts thereof, and a process for the preparation thereof, pharmaceutical composition of said compounds, and a method of using said compounds as anti-inflammatory and analgesic agents. They have excellent anti-inflammatory and analgesic activities with an extremely weak ulcerogenicity in the gastrointestinal tract.
Abstract: The imidazole derivatives of the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, the symbol .dbd. represents a double bond that bond is E or Z, or a triple bond, and m and n, which may be the same or different, each represent zero, or an integer of 1 to 10, and non-toxic acid addition salts thereof, and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof are new compounds. These compounds have a strong inhibitory effect on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents for inflammation, hypertension, thrombus, cerebral apoplexy and asthma.
Type:
Grant
Filed:
May 2, 1979
Date of Patent:
March 17, 1981
Assignees:
Ono Pharmaceutical Co., Ltd., Kissei Pharmaceutical Co., Ltd.
Abstract: S-Substituted derivatives of N-(2-mercapto-2-methylpropanoyl)-cysteine which have the formula ##STR1## are useful as a medicine for suppressing liver disorders.
Abstract: 3-Substituted-7-substituted alkanamido-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities, processes for the preparation thereof, pharmaceutical compositions comprising the same, and methods of using the same therapeutically in the treatment of infections.
Abstract: 7-(2-Hydroxyimino-2-hydroxyphenyl-acetamido)-3-substituted-3-cephem-4-carbo xylic acids are disclosed which possess an antibacterial activity.
Abstract: A 2-aminomethyl phenol derivative of the formula (I): ##STR1## wherein X is a halogen atom; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different are each a hydrogen atom or a straight or branched chain alkyl group having 1 to 4 carbon atoms; n is 2, 3, 4 or 5 and a pharmaceutically acceptable acid addition salt thereof are disclosed. Also disclosed is a process for preparing such derivative or a pharmaceutically acceptable acid addition salt thereof.