Patents Represented by Attorney Stephen B. Coan
  • Patent number: 4110439
    Abstract: In the fermentation production of gentamicin C a plurality of additional antibiotic compounds are obtained. Four of these compounds, gentamicin A, gentamicin B, gentamicin B.sub.1 and gentamicin X exhibit significant anti-protozoal and anthelmintic activity while gentamicin B and B.sub.1 have significant antibacterial properties with markedly reduced side effects.
    Type: Grant
    Filed: December 20, 1976
    Date of Patent: August 29, 1978
    Assignee: Schering Corporation
    Inventors: David J. Cooper, Jay A. Waitz, Mae Counelis, Jay Weinstein
  • Patent number: 4107166
    Abstract: This invention relates to 1-amino naphthyridines prepared by a base-catalyzed condensation while in an aprotic solvent. In this condensation an o-alkyl aryl nitrile may be reacted either with the same or different o-alkyl aryl nitrile or with another nitrile. The 1-amino naphthyridines are useful as antifungal and antibacterial agents.
    Type: Grant
    Filed: April 11, 1977
    Date of Patent: August 15, 1978
    Assignee: Schering Corporation
    Inventors: Joseph Mayer, Margaret H. Sherlock
  • Patent number: 4103018
    Abstract: 2-[4-(Polyhalo-2-hydroxy-2-propyl)anilino]-2-oxazolin-4-ones and the thiazolin-4-ones corresponding thereto, having useful anti-hypertensive properties, are disclosed herein. The compounds are prepared by reaction of the appropriate 4-(polyhalo-2-hydroxy-2-propyl)aniline with a .beta.-chloroethanoyl isocyanate or isothiocyanate and then cyclization of the resultant intermediate.
    Type: Grant
    Filed: October 12, 1976
    Date of Patent: July 25, 1978
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Nicola Zampaglione
  • Patent number: 4093742
    Abstract: Novel polyhaloisopropyl-substituted arylureas having potent antihypertensive properties are disclosed herein.
    Type: Grant
    Filed: May 4, 1976
    Date of Patent: June 6, 1978
    Assignee: Schering Corporation
    Inventor: Bernard R. Neustadt
  • Patent number: 4093731
    Abstract: The title compound is a novel substance which effectively treats helminthiasis.
    Type: Grant
    Filed: March 7, 1977
    Date of Patent: June 6, 1978
    Assignee: Schering Corporation
    Inventor: Mohammed Mehdi Nafissi-Varchei
  • Patent number: 4092359
    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 155OF-1G NRRL 5742) for the elaboration of a novel antibacterial agent designated Mutamicin 2.
    Type: Grant
    Filed: February 15, 1974
    Date of Patent: May 30, 1978
    Assignee: Schering Corporation
    Inventors: Peter J. L. Daniels, Mohammad Mehdi Nafissi Varchei
  • Patent number: 4088644
    Abstract: Disclosed herein are novel N-acyl-3-aryl-3-azetidinols useful as intermediates. A method is provided for their direct preparation from acyclic starting materials. These N-acyl-3-aryl-azetidinols provide a convenient route to the 3-azetidinol series.
    Type: Grant
    Filed: March 20, 1974
    Date of Patent: May 9, 1978
    Assignee: Schering-Corporation
    Inventor: Elijah H. Gold
  • Patent number: 4087184
    Abstract: A method and apparatus for automatically inspecting liquid filled containers for particulate contaminants in relative size. The method comprising the steps of illuminating the liquid with a constant intensity light source, imaging the entire illuminated liquid volume, including the meniscus, into a plurality of image planes with fiber optic bundles, and monitoring the fiber optic bundles with an array of constant sensitivity photo transducers. Each photo transducer continually translates the illumination value of the vial image of an assigned and separate unit volume of the liquid-filled container into a voltage signal and each signal is monitored for a signal change indicative of particulate movement. The interfering output signal due to the meniscus decay is corrected, and the accept/reject decision is based upon a composite signal representative of all the differentiated signals received from the array of photo transducers.
    Type: Grant
    Filed: April 16, 1976
    Date of Patent: May 2, 1978
    Assignee: Schering Corporation
    Inventors: Julius Z. Knapp, John C. Zeiss
  • Patent number: 4081547
    Abstract: Novel para-polyfluoroisopropyl-anilino-2-oxazolines and thiazolines are provided which exhibit potent antihypertensive properties without significant CNS depression.
    Type: Grant
    Filed: March 19, 1976
    Date of Patent: March 28, 1978
    Assignee: Schering Corporation
    Inventor: Bernard R. Neustadt
  • Patent number: 4081451
    Abstract: This invention relates to a novel process for preparing 2-halogeno-nicotinic acids. The compounds, especially 2-chloro-nicotinic acid, are intermediates in the preparation of anilino nicotinic acid derivatives. The latter compounds are useful as analgesic anti-diarrheal and anti-inflammatory agents.
    Type: Grant
    Filed: April 4, 1977
    Date of Patent: March 28, 1978
    Assignee: Schering Corporation
    Inventor: Joseph Mayer
  • Patent number: 4081544
    Abstract: The present 2-substituted imidazolines and 2-substituted-3,4,5,6-tetrahydropyrimidines possess valuable anti-depressant and anti-inflammatory properties. The compounds are prepared by the condensation of an appropriately substituted nitrile with a diamine. For example, condensation of 2-pyridylbenzyl cyanide with 1,2-ethylene diamine or with 1,3-propylene diamine produces a 2-(2-pyridylbenzyl) imidazoline or a 2-(2-pyridylbenzyl)-3,4,5,6-tetrahydropyrimidine.
    Type: Grant
    Filed: December 27, 1976
    Date of Patent: March 28, 1978
    Assignee: Schering Corporation
    Inventor: Lewis A. Walter
  • Patent number: 4081549
    Abstract: Disclosed herein are 2-aminoalkyl-3-aryl-benzothiophenes and benzofurans useful as antimicrobial agents.
    Type: Grant
    Filed: January 12, 1977
    Date of Patent: March 28, 1978
    Assignee: Schering Corporation
    Inventor: Martin Steinman
  • Patent number: 4079054
    Abstract: Described are 3-oxo-7.alpha.-halogeno-17.alpha.-1,4-pregnadiene-21,17.beta.-carbolactone s and compounds related thereto, i.e. 2',3'.alpha.-tetrahydrofuran-2'-spiro-17(7.alpha.-halogeno-1,4-androstadie ne-3-ones) and (17R)-spiro-[7.alpha.-halogeno-1,4-androstadiene-17,1'-cyclobutane]-3,2'-d iones, all of which are valuable as aldosterone antagonists. Also described are the corresponding 7.beta.-hydroxy derivatives useful as intermediates.
    Type: Grant
    Filed: December 22, 1976
    Date of Patent: March 14, 1978
    Assignee: Schering Corporation
    Inventors: Michael J. Green, Ho-Jane Shue
  • Patent number: 4078139
    Abstract: The process for removing a secondary hydroxyl group from an organic compound having at least one secondary hydroxyl group and having any amino groups protected, comprises the reaction of a reactive ester of said secondary hydroxyl group selected from the group consisting of an O-alkylthioester and an O-alkylselenoester with at least one mole of an organotin hydride, preferably tri-n-butylstannane, in an inert, aprotic solvent at a temperature of at least about 100.degree. C and under an inert atmosphere.The process is particularly useful in removing secondary alcohols in aminoglycoside antibiotics to produce deoxy derivatives thereof having antibacterial activity.Also described are novel O-sec.-alkylthiobenzoate, O-sec.-alkyl-S-methylxanthate, N-(sec.-alkoxythiocarbonyl)-imidazole esters, and di-O-alkylthiocarbonates having at least one secondary O-alkyl group, useful intermediates of the claimed process.
    Type: Grant
    Filed: July 12, 1976
    Date of Patent: March 7, 1978
    Assignee: Schering Corporation
    Inventors: Derek H. R. Barton, Stuart W. McCombie
  • Patent number: 4078056
    Abstract: Micromonospora arborensis produces a plurality of antibiotics named herein antibiotic 68-1147 complex, when cultivated under controlled aerobic conditions. Two of the antibiotics, antibiotic 68-1147 I and antibiotic 68-1147 II are described and shown to be effective antibacterial agents, especially against gram positive bacteria.
    Type: Grant
    Filed: February 2, 1976
    Date of Patent: March 7, 1978
    Assignee: Schering Corporation
    Inventors: Marvin J. Weinstein, Gerald H. Wagman, Joseph A. Marquez, Raymond T. Testa
  • Patent number: 4076711
    Abstract: This disclosure relates to the method for the treatment of psoriasis which comprises the topical administration to a mammal suffering from psoriasis of an effective dose for treating psoriasis of a 7X-5Q-3Y-3H-.gamma.-triazolo[4,5-d]-pyrimidine wherein X is halogeno, alkoxy, or --NRR.sub.1, R and R.sub.1 being lower alkyl, Y is cycloalkyl, hydroxycycloalkyl, phenyl, bicycloalkyl, or A--R.sub.2 with A being methylene or ethylene and R.sub.2 being phenyl or bicycloalkyl, and Q is hydrogen or Y.
    Type: Grant
    Filed: December 22, 1976
    Date of Patent: February 28, 1978
    Assignee: Schering Corporation
    Inventors: Ashit K. Ganguly, Edwin A. Peets, Anil K. Saksena
  • Patent number: 4076589
    Abstract: Glycerol is efficiently converted to dihydroxyacetone by Acetobacter suboxydans at an acid pH under aerobic conditions in a medium consisting of yeast hydrolysate or fish hydrolysate, glycerol and water.
    Type: Grant
    Filed: July 17, 1975
    Date of Patent: February 28, 1978
    Assignee: Schering Corporation
    Inventor: William Charney
  • Patent number: 4076708
    Abstract: 3-Oxo-6-unsubstituted-7.alpha.-halogeno-4-dehydro steroids, wherein said halogen is chlorine, bromine or iodine, are prepared by reaction of a 3-oxo-6,7-di-unsubstituted-4,6-bis-dehydro steroid with at least an equimolar quantity of the corresponding hydrogen halide in a non-reactive organic solvent at temperatures no higher than about 30.degree. C, and then are isolated by removal of said solvent and any excess acid at temperatures no higher than about 25.degree. C without subjecting said 3-oxo-6-unsubstituted-7.alpha.-halogeno-4-dehydro steroid to a basic medium.A preferred species of this process is that wherein the starting steroid is a 3,20-dioxo-9-unsubstituted-11-oxygenated-1,4,6-pregnatriene-17,21-diol or ester thereof, preferably a 17,21-di-lower alkanoate or a 17-benzoate 21-lower alkanoate ester thereof, whereby is prepared in good yields a 3,20-dioxo-7.alpha.-halogeno-1,4-pregnadiene-17.alpha.,21-diol or ester thereof, useful as topical anti-inflammatory agents.
    Type: Grant
    Filed: December 22, 1976
    Date of Patent: February 28, 1978
    Assignee: Schering Corporation
    Inventors: Michael J. Green, Ho-Jane Shue, Elliot L. Shapiro, Margaret A. Gentles
  • Patent number: 4075331
    Abstract: Described herein are novel monoesters of rosamicin, also known as Antibiotic 67-694. Also described is a process for the preparation of such esters by the selective solvolysis of diester precursors. The monoesters are broad spectrum antibacterial agents but are generally more effective against gram-positive bacteria.
    Type: Grant
    Filed: January 13, 1977
    Date of Patent: February 21, 1978
    Assignee: Schering Corporation
    Inventor: Hans Reimann
  • Patent number: D254415
    Type: Grant
    Filed: August 1, 1977
    Date of Patent: March 11, 1980
    Assignee: Plough, Inc.
    Inventor: Ted I. Kingsford