Patents Represented by Attorney Raymond A. McDonald
  • Patent number: 4267374
    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
  • Patent number: 4260823
    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
  • Patent number: 4260626
    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
  • Patent number: 4205073
    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.
    Type: Grant
    Filed: April 30, 1975
    Date of Patent: May 27, 1980
    Assignee: Schering Corporation
    Inventors: Margaret H. Sherlock, James F. Long
  • Patent number: 4178453
    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
  • Patent number: 4172095
    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.
    Type: Grant
    Filed: June 10, 1977
    Date of Patent: October 23, 1979
    Assignee: Schering Corporation
    Inventors: Martin Steinman, Yee S. Wong
  • Patent number: 4169141
    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.
    Type: Grant
    Filed: January 30, 1978
    Date of Patent: September 25, 1979
    Assignee: Shering Corporation
    Inventors: John G. Topliss, Adriano Afonso
  • Patent number: 4161540
    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.
    Type: Grant
    Filed: October 3, 1977
    Date of Patent: July 17, 1979
    Assignee: Schering Corporation
    Inventors: Rudolph O. Neri, John G. Topliss
  • Patent number: 4161523
    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
  • Patent number: 4155904
    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.
    Type: Grant
    Filed: July 23, 1976
    Date of Patent: May 22, 1979
    Assignee: Schering Corporation
    Inventor: Walter Schlesinger
  • Patent number: 4144270
    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.
    Type: Grant
    Filed: June 26, 1974
    Date of Patent: March 13, 1979
    Assignee: Schering Corporation
    Inventors: Rudolph O. Neri, John G. Topliss
  • Patent number: 4139625
    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.
    Type: Grant
    Filed: August 12, 1977
    Date of Patent: February 13, 1979
    Assignee: Schering Corporation
    Inventor: Margaret H. Sherlock
  • Patent number: 4139638
    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.
    Type: Grant
    Filed: October 3, 1977
    Date of Patent: February 13, 1979
    Assignee: Schering Corporation
    Inventors: Rudolph O. Neri, John G. Topliss
  • Patent number: 4138488
    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.
    Type: Grant
    Filed: January 10, 1977
    Date of Patent: February 6, 1979
    Assignee: Schering Corporation
    Inventors: Margaret H. Sherlock, Heide Roebke
  • Patent number: 4137224
    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
  • Patent number: 4133887
    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.
    Type: Grant
    Filed: August 12, 1977
    Date of Patent: January 9, 1979
    Assignee: Schering Corporation
    Inventor: Margaret H. Sherlock
  • Patent number: 4129720
    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
  • Patent number: 4127662
    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.
    Type: Grant
    Filed: August 12, 1977
    Date of Patent: November 28, 1978
    Assignee: Schering Corporation
    Inventor: Margaret H. Sherlock
  • Patent number: 4125612
    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.
    Type: Grant
    Filed: June 20, 1977
    Date of Patent: November 14, 1978
    Assignee: Schering Corporation
    Inventor: Margaret H. Sherlock
  • Patent number: 4123433
    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.
    Type: Grant
    Filed: August 12, 1977
    Date of Patent: October 31, 1978
    Assignee: Schering Corporation
    Inventor: Margaret H. Sherlock