Abstract: Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.
Type:
Grant
Filed:
June 25, 1979
Date of Patent:
May 12, 1981
Assignee:
Merrell Toraude et Compagnie
Inventors:
Brian W. Metcalf, Michel Jung, Charles Danzin
Abstract: Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## is hydrogen, a straight or branched lower alkyl group of 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; and pharmaceutically acceptable salts and individual optical isomers thereof.
Type:
Grant
Filed:
July 2, 1979
Date of Patent:
April 7, 1981
Assignee:
Merrell Toruade et Compagnie
Inventors:
Patrick J. Casara, Michel Jung, Brian W. Metcalf
Abstract: Novel antisecretory compounds of the formula: ##STR1## wherein R is ##STR2## and pharmaceutically acceptable salts, diasteriomers and individual optical isomers thereof.
Type:
Grant
Filed:
March 26, 1979
Date of Patent:
April 7, 1981
Assignee:
Richardson-Merrell Inc.
Inventors:
Albert A. Carr, Hsien C. Cheng, Stephen W. Horgan, James K. Woodward
Abstract: This invention relates to compositions of matter useful as anti-diarrheal agents and to the method of controlling and treating diarrhea in warm blooded animals. The active anti-diarrheal agents are substituted anilino nicotinic acids, and salts thereof and ester and hydrazine derivatives of said acids.
Abstract: The aminocyclitol 2,5-dideoxystreptamine may be prepared by a novel two-step synthesis from cis-4,8-dioxatricyclo [5.1.0.0.sup.3,5 ]octane. The aminocyclitol and a novel intermediate in the synthesis thereof are utilized by a Micromonospora inyoensis (M. inoyensis strain 1550F-1G NRRL 5742) for the elaboration of a novel antibacterial agent designated Mutamicin 2.
Type:
Grant
Filed:
January 13, 1978
Date of Patent:
December 11, 1979
Assignee:
Schering Corporation
Inventors:
Peter J. L. Daniels, Mohammed M. N. Varchei
Abstract: This invention relates to a novel process for preparing 3-amino-2-methylbenzotrifluoride from 4-X-substituted-2-methylthiomethylbenzotrifluorides. The former compounds are useful in the preparation of anilino-nicotinic and anilino-anthranilic acids exhibiting analgesic, anti-inflammatory or anti-diarrheal properties. Some of the intermediates are novel per se.
Abstract: Disclosed herein are di-O-(aminoglycosyl)-1,3-diaminocyclitol antibacterial agents having on the 1-N-position of the 1,3-diaminocyclitol moiety a dipeptidyl or a tripeptidyl substituent. The compounds are useful antibacterial agents, as are their non-toxic pharmaceutically acceptable acid addition salts. Also disclosed are methods for preparing such agents from di-O-(aminoglycosyl)-1,3-diaminocyclitol antibacterial agents which are unsubstituted at the 1-N-position.
Abstract: This application relates to certain 4'-substituted and to 3',4'-disubstituted anilides, to methods for their preparation and to methods for their use as antiandrogens. These substituted anilides are useful in the treatment of androgen dependent disease states, such as benign prostatic hypertrophy, hirsutism, acne and the like.
Abstract: Antibiotic 67-694, (also known as rosamicin) a new broad spectrum antibiotic is described together with methods for its production via the cultivation under controlled conditions of Micromonospora rosaria, a new species of Micromonospora, and to methods for purifying and using the same. Its 2'-monoesters and its 3,2'-diesters and their acid addition salts also possess antibiotic activity.
Type:
Grant
Filed:
October 21, 1974
Date of Patent:
July 17, 1979
Assignee:
Schering Corporation
Inventors:
Marvin J. Weinstein, Gerald H. Wagman, Joseph A. Marquez
Abstract: This invention relates to an improved process for the preparation of 1,3-dihydro-2H-1,4-benzodiazepin-2-ones and 2,3-dihydro-1H-1,4-benzodiazepines by the condensation of a 2-(2-haloacylamido)-benzophenone or a 2-(2-haloethylamino)-benzophenone, respectively, in the presence of hexamethylenetetramine, a water miscible alcohol containing 5 to 50 volume percent water, and an ammonium salt.
Abstract: This application relates to certain 4'-substituted and to 3',4'-disubstituted anilides, to methods for their preparation and to methods for their use as anti-androgens.
Abstract: Disclosed herein are novel 5-tritylpicolinic acids, amides, esters and pharmaceutically acceptable salts thereof. Also disclosed are methods for the use of said novel compounds as anti-acne agents.
Abstract: This application relates to certain 4'-substituted and to 3', 4'-disubstituted anilides, to methods for their preparation and to methods for their use as antiandrogens. These substituted anilides are useful in the treatment of androgen dependent disease states, such as benign prostatic hypertrophy, hirsutism, acne and the like.
Abstract: Disclosed herein are substituted diphenylmethyl picolinic acids, pharmaceutically acceptable salts, amides and esters thereof. The compounds disclosed are useful as topical anti-acne agents.
Abstract: A novel antibiotic complex exhibiting antifungal activity is produced by fermenting a novel species of bacteria from the genus Aeromonas, the bacterium being herein designated Aeromonas sp. W-10. The antibiotic complex is comprised of at least three and possibly as many as six components and has been designated Antibiotic W-10 Complex. Two members of the complex have been isolated in substantially pure form and are designated Antibiotic 20561 and Antibiotic 20562, the antibiotics exhibiting substantial antifungal activity.
Type:
Grant
Filed:
February 9, 1977
Date of Patent:
January 30, 1979
Assignee:
Schering Corporation
Inventors:
David Taplin, Marvin J. Weinstein, Raymond T. Testa, Joseph A. Marquez, Mahesh G. Patel
Abstract: Disclosed herein are novel 5-tritylpicolinic acids, amides, esters and pharmaceutically acceptable salts thereof. Also disclosed are methods for the use of said novel compounds as anti-acne agents.
Abstract: Everninomicin B, C or D may be converted to amino derivatives by reductive means. The amino derivatives may, subsequently, be converted to novel N-acyl, N-alkyl or N,N-dialkyl derivatives. Alternatively, everninomicins B, C or D may be converted to N-acyl-N-hydroxylamino derivatives also by reductive means. The derivatives so-produced and the non-toxic pharmaceutically acceptable cationic salts thereof are novel and are antibacterial agents.
Type:
Grant
Filed:
September 16, 1977
Date of Patent:
December 12, 1978
Assignee:
Schering Corporation
Inventors:
Ashit K. Ganguly, Viyyoor M. Girijavallabhan, Olga Sarre, Hans Reimann
Abstract: Disclosed herein are novel 5-tritylpicolinic acids, amides, esters and pharmaceutically acceptable salts thereof. Also disclosed are methods for the use of said novel compounds as anti-acne agents.
Abstract: This invention relates to N-1(p-biphenylalkyl) piperazines, to the processes for making such compounds and to the use of such compounds as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis.
Abstract: Disclosed herein are novel 5-tritylpicolinic acids, amides, esters and pharmaceutically acceptable salts thereof. Also disclosed are methods for the use of said novel compounds as anti-acne agents.