Abstract: There is presented peptide derivatives comprising polypeptides to which are bound via its functional side-chains penicilloyl residues of the formula ##STR1## wherein R signifies 2-pentenyl, n-pentyl, n-heptyl, allylthiomethyl, 5-amino-5-carboxypentyl, benzyl, .alpha.-carboxy benzyl, .alpha.-aminobenzyl, phenoxy benzyl, phenoxymethyl, .alpha.-phenoxy ethyl, .alpha.-phenoxypropyl, 2,6-dimethoxyphenyl, 2-ethoxy-1-naphthyl, 3-carboxy-2-quinoxazinyl, 5-methyl-3-phenyl-4-isoxazolyl, .alpha.-amino-p-hydroxy benzyl, 3-(2-chlorophenyl)-5-methyl-4-isoxazolyl, 3-(2,6-dichlorophenyl)-5-methyl-4-isoxazolyl, 3-(2-chloro-6-fluoro-phenyl)-5-methyl-4-isoxazolyl, .alpha.-carboxy-3-thienylmethyl or .alpha.-sulphonylbenzyl.The peptide derivatives exhibit antiallergic activity.
Abstract: Homologs of antibiotic Lasalocid A and their pharmaceutically acceptable salts are produced by a known species of Streptomyces. The homologs exhibit coccidiostatic and antibacterial activity and thus are useful as coccidiostats and antibacterial agents.
Abstract: The invention relates to a new and useful antibiotic substance which is of the formula ##STR1## and to processes for its production and recovery. The antibiotic which exhibits ionophoric properties, is classified as a polyether group antibiotic. The antibiotic of formula I is effective in inhibiting the growth of gram positive bacteria and exhibits utility as an antihypertensive agent and as a compound to improve ruminant feed utilization. The antibiotic of Formula I is prepared by cultivating a strain of Streptomyces sp. X-14547 in an aqueous carbohydrate solution containing nitrogenous nutrients and mineral salts and thereafter isolating the antibiotic from the fermentation broth.
Abstract: Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is selected from the group consisting of lower alkylthio together with the sulfoxide and sulfone thereof, halo, lower alkylamino or lower alkoxy; Y is oxo or thio; R.sub.3 is selected from the group consisting of hydrogen, --COOR.sub.4 wherein R.sub.4 is hydrogen or lower alkyl, --CONR.sub.6 R.sub.5 wherein R.sub.5 and R.sub.6 are hydrogen or lower alkyl; X is hydrogen or halogen; and R.sub.7 is lower alkyl or hydrogen and the pharmaceutically acceptable salts and N-oxides thereof.Also presented are processes to produce the above compounds and intermediates therefor and derivatives thereof.
Type:
Grant
Filed:
July 27, 1978
Date of Patent:
August 28, 1979
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Armin Walser, Rodney I. Fryer, Louis Benjamin
Abstract: The invention relates to a compound, 1-methyl-9.beta.-D-ribofuranosyl-isoguanine, and to a process for the preparation thereof by isolation from natural sources. The compound has muscle relaxing, central nervous system, anti-inflammatory, anti-allergy and hypotensive activity.
Abstract: A method is disclosed for treating hypertension in warm-blooded animals by the oral administration, to an animal in need of such treatment, of a therapeutically effective dose for example, from about, 0.1 to 5 mg/kg/day as chronic administration or 5 to 10 mg/kg/day, of a polyether compound such as bromolasalocid or bromoisolasalocid. Also disclosed are examples of such polyether compounds and methods for their preparation.
Abstract: Compounds are presented of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, amino, halogen and nitro; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, carboxylic acids, esters and primary, secondary or tertiary amides thereof, alkylhydroxy, acylhydroxy-lower alkyl, amino-lower alkyl, alkylamino-lower alkyl, acylamino-lower alkyl and carboxaldehyde; and X is hydrogen or halogen and the pharmaceutically acceptable salts thereof.Also presented are processes to produce the above compounds and intermediates thereof.
Abstract: Novel thienotriazolodiazepine derivatives and processes for their preparation are described. These compounds are useful as anticonvulsants, muscle-relaxants and sedatives.
Type:
Grant
Filed:
October 14, 1977
Date of Patent:
May 22, 1979
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Joseph Hellerbach, Paul Zeller, Dieter Binder, Otto Hromatka
Abstract: Compounds are presented of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, amino, halogen and nitro; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, carboxylic acids, esters and primary, secondary or tertiary amides thereof, alkylhydroxy, acylhydroxy-lower alkyl, amino-lower alkyl, alkylamino-lower alkyl, acylamino-lower alkyl and carboxaldehyde; and X is hydrogen or halogen and the pharmaceutically acceptable salts thereof.Also presented are processes to produce the above compounds and intermediates thereof. These compounds exhibit pharmacological activity as anxiolytics, sedatives, muscle relaxants and anticonvulsants.
Abstract: A new antibiotic, designated as antibiotic 1745A/X, is produced by the fermentation of the known microorganism Streptomyces antibioticus, ATCC 11891, using the novel compound erythronolide A oxime as the substrate. This new antibiotic is useful an an antibacterial agent.
Type:
Grant
Filed:
March 16, 1978
Date of Patent:
May 1, 1979
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Richard W. Kierstead, Ronald A. LeMahieu, David Pruess
Abstract: The invention relates to synthetic processes to produce the known pharmacologically active 9-methoxypsoralen. Also disclosed are various novel intermediates utilized in these processes.
Abstract: A process to produce 1-methyl isoquanosine, a compound of the formula ##STR1## is disclosed. Also disclosed is a novel intermediate in said process. The 1-methyl isoguanosine has been found to have pharmacological activity, e.g. anti-inflammatory activity and muscle relaxant activity.
Abstract: Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is selected from the group consisting of lower alkylthio together with the sulfoxide and sulfone thereof, halo, lower alkylamino or lowe alkoxy; Y is oxo or thio; R.sub.3 is selected from the group consisting of hydrogen, --COOR.sub.4 wherein R.sub.4 is hydrogen or lower alkyl, --CONR.sub.6 R.sub.5 wherein R.sub.5 and R.sub.6 are hydrogen or lower alkyl; X is hydrogen or halogen; and R.sub.7 is lower alkyl or hydrogenAnd the pharmaceutically acceptable salts and N-oxides thereof.Also presented are processes to produce the above compounds and intermediates therefor and derivatives thereof.
Type:
Grant
Filed:
July 27, 1978
Date of Patent:
April 3, 1979
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Armin Walser, Rodney I. Fryer, Louis Benjamin
Abstract: The invention relates to synthetic processes to produce the known pharmacologically active 9-methoxypsoralen. Also disclosed are various novel intermediates utilized in these processes.
Abstract: Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is selected from the group consisting of lower alkylthio together with the sulfoxide and sulfone thereof, halo, lower alkylamino or lower alkoxy; Y is oxo or thio; R.sub.3 is selected from the group consisting of hydrogen, --COOR.sub.4 wherein R.sub.4 is hydrogen or lower alkyl, --CONR.sub.6 R.sub.5 wherein R.sub.5 and R.sub.6 are hydrogen or lower alkyl; X is hydrogen or halogen; and R.sub.7 is lower alkyl or hydrogen and the pharmaceutically acceptable salts and N-oxides thereof.Also presented are processes to produce the above compounds and intermediates therefor and derivatives thereof.
Type:
Grant
Filed:
July 27, 1978
Date of Patent:
March 27, 1979
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Armin Walser, Rodney I. Fryer, Louis Benjamin
Abstract: The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.4 is lower alkyl or hydrogen and may be different,And the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.
Abstract: The temperature of the reflux fed to a fractionating tower is increased after the reflux enters the tower and before it passes onto the reflux return tray by passing the reflux through an atomizer in the fractionating tower above the reflux return tray to produce a downfalling spray of liquid droplets; collecting the droplets on a reflux pan located between the atomizer and the reflux return tray, the reflux pan being designed to allow the passage of hot vapors rising from the reflux return tray; and passing the collected liquid from the reflux pan onto the reflux return tray. The distance between the reflux pan and the atomizer is such as to allow the downfalling droplets to absorb sufficient heat from the hot rising vapors so that the temperature of the reflux fluid collected on the reflux pan is increased to the desired value.
Type:
Grant
Filed:
February 1, 1978
Date of Patent:
February 20, 1979
Assignee:
Exxon Research and Engineering Co.
Inventors:
Dennis G. Alexion, Fredrick P. Storm, Jr.
Abstract: A compound which is the C-17 epimer of deoxy-(0-8)-epi-17-salinomycin is produced by the fermentation of a strain of Streptomyces albus 80,614 (ATCC 21,838). The compound exhibits activity as an antimicrobial and antihypertensive agent.
Abstract: The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.4 is lower alkyl or hydrogen and may be different and the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.