Patents Represented by Attorney Paul C. Steinhardt
  • Patent number: 4468513
    Abstract: Nickel salts are used to effect the regio-selective acylation and alkylation of the 2'-amino group of 4-O-substituted-2-deoxystreptamine containing aminoglycosides. The 2'-N-substituted derivatives of apramycin, certain .alpha. or .beta.-(lower alkyl)aprosaminides and certain .alpha. or .beta.-(substituted lower alkyl)aprosaminides are new. The 2'-N-substituted-4-O-substituted-2-deoxystreptamine aminoglycosides produced by the process of this invention are antibacterial agents.
    Type: Grant
    Filed: September 7, 1982
    Date of Patent: August 28, 1984
    Assignee: Eli Lilly and Company
    Inventors: Herbert A. Kirst, Brenda A. Truedell
  • Patent number: 4468512
    Abstract: Zinc salts are used to effect the regio-selective acylation and alkylation of the 1-amino group of 4-O-substituted-2-deoxystreptamine-containing aminoglycosides. The 1-N-substituted derivatives of apramycin, 3'-hydroxyapramycin, certain .alpha. or .beta.-(lower alkyl)aprosaminides and certain .alpha. or .beta.-(substituted lower alkyl)-aprosaminides are new. The 1-N-substituted-4-O-substituted-2-deoxystreptamine aminoglycosides produced by the process of this invention are antibacterial agents.
    Type: Grant
    Filed: September 7, 1982
    Date of Patent: August 28, 1984
    Assignee: Eli Lilly and Company
    Inventors: Herbert A. Kirst, Brenda A. Truedell
  • Patent number: 4462942
    Abstract: Antibiotic A47934 is produced by submerged, aerobic fermentation of new Streptomyces toyocaensis NRRL 15009. The antibiotic is active against gram-positive bacteria in vitro and in vivo. It promotes growth in poultry and swine and serves to enhance feed efficiency in ruminant animals having a developed rumen.
    Type: Grant
    Filed: July 30, 1982
    Date of Patent: July 31, 1984
    Assignee: Eli Lilly and Company
    Inventors: Robert L. Hamill, Ralph E. Kastner
  • Patent number: 4459405
    Abstract: 7-(S)-Acylamino-3-hydroxymethyl-3-cephem sulfones are disclosed. These compounds are intermediates in the synthesis of 1-oxa .beta.-lactam antibiotics.
    Type: Grant
    Filed: November 16, 1982
    Date of Patent: July 10, 1984
    Assignee: Eli Lilly and Company
    Inventor: David A. Hall
  • Patent number: 4458065
    Abstract: Apramycin derivatives substituted at the 7'-amino group with a methyl, ethyl, n-propyl or n-butyl substituent are broad spectrum antibiotics. Also claimed are intermediates in the synthesis of these 7'-N-alkylapramycin derivatives.
    Type: Grant
    Filed: February 17, 1983
    Date of Patent: July 3, 1984
    Assignee: Eli Lilly and Company
    Inventor: Herbert A. Kirst
  • Patent number: 4436596
    Abstract: N-substituted-2-(R)-(sulfinic acid)-3-(S)-(acylamino)-4-oxo-azetidines, which are useful as intermediates in 1-oxa .beta.-lactam antibiotics, are synthesized by electrolytic reduction of 7-(S)-acylamino-3-hydroxymethyl-3-cephem-4-carboxylic acid compounds.
    Type: Grant
    Filed: November 16, 1982
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: David A. Hall
  • Patent number: 4436912
    Abstract: Cephalosporin broad spectrum antibiotics possessing a 7.beta.-[2-[(2-aminooxazol)-4-yl]-2-(substituted oximino)]acetamido side chain and a variety of substituents at the 3-position of the cephalosporins are claimed. Also claimed are intermediates in the synthesis of the above cephalosporin antibiotics.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: March 13, 1984
    Assignee: Eli Lilly and Company
    Inventor: William J. Wheeler
  • Patent number: 4431809
    Abstract: Antibiotic A-33853 is produced by submerged, aerobic fermentation of a new Streptomyces sp. NRRL 12068. The antibiotic and the diacetyl and triacetyl derivatives thereof disclosed herein have shown antibacterial activity against Staphylococcus and Streptococcus species which are penicillin resistant. In addition, the antibiotic and its tetraacetyl derivative have shown antiviral and antitrichomonal activity in vitro.
    Type: Grant
    Filed: May 7, 1982
    Date of Patent: February 14, 1984
    Assignee: Eli Lilly and Company
    Inventors: Marvin M. Hoehn, Karl H. Michel
  • Patent number: 4430499
    Abstract: Cephalosporin broad spectrum antibiotics possessing a 7.beta.-[2-[(2-aminooxazol)-4-yl]-2-(substituted oximino)acetamido side chain and a variety of substituents at the 3-position of the cephalosporins are claimed. Also claimed are intermediates in the synthesis of the above cephalosporin antibiotics.
    Type: Grant
    Filed: September 8, 1981
    Date of Patent: February 7, 1984
    Assignee: Eli Lilly and Company
    Inventor: William J. Wheeler
  • Patent number: 4424344
    Abstract: Nickel salts are used to effect the regio-selective acylation and alkylation of the 2'-amino group of 4-O-substituted-2-deoxystreptamine containing aminoglycosides. The 2'-N-substituted derivatives of apramycin, certain .alpha. or .beta.-(lower alkyl)aprosaminides and certain .alpha. or .beta.-(substituted lower alkyl)aprosaminides are new. The 2'-N-substituted-4-O-substituted-2-deoxystreptamine aminoglycosides produced by the process of this invention are antibacterial agents.
    Type: Grant
    Filed: September 21, 1981
    Date of Patent: January 3, 1984
    Assignee: Eli Lilly and Company
    Inventors: Herbert A. Kirst, Brenda A. Truedell
  • Patent number: 4424345
    Abstract: Zinc salts are used to effect the regio-selective acylation and alkylation of the 1-amino group of 4-O-substituted-2-deoxystreptamine-containing aminoglycosides. The 1-N-substituted derivatives of apramycin, 3'-hydroxyapramycin, certain .alpha. or .beta.-(lower alkyl)aprosaminides and certain .alpha. or .beta.-(substituted lower alkyl)-aprosaminides are new. The 1-N-substituted-4-O-substituted-2-deoxystreptamine aminoglycosides produced by the process of this invention are antibacterial agents.
    Type: Grant
    Filed: September 21, 1981
    Date of Patent: January 3, 1984
    Assignee: Eli Lilly and Company
    Inventors: Herbert A. Kirst, Brenda A. Truedell
  • Patent number: 4407750
    Abstract: Aryl 4R[1-(2-N-3-methyl-4-al-Z-but-2-ene-oate)-2-oxo-3s-acylamino azetidinone]disulfides are prepared by reacting the corresponding 7.alpha.-acylamino-2.alpha.-alkoxy-3-methyl-3-cephem-4-carboxylates first with either phenylsulfenyl chloride or a monosubstituted-phenylsulfenyl chloride where the substituent is either chloro, methoxy, methyl or acetoxy. The disulfide compounds produced in this invention are intermediates in the synthesis of the 7.beta.-acylamino-7.alpha.-alkoxy-3-methyl 1-oxa .beta.-lactam acids, a class of antibiotic compounds.
    Type: Grant
    Filed: August 7, 1981
    Date of Patent: October 4, 1983
    Assignee: Eli Lilly and Company
    Inventors: Stjepan Kukolja, Janice L. Pfeil
  • Patent number: 4394313
    Abstract: 4R, 4'R bis [1-(2-N-3-methyl-4-al-Z-but-2-ene-oate)-2-oxo-3S-acylamino azetidine]disulfide compounds are prepared by reacting the corresponding 7.alpha.-acylamino-2.alpha.-alkoxy-3-methyl-3-cephem-4-carboxylates first with an N-chloro halogenating agent, e.g., N-chlorosuccinimide, then with an aqueous suspension of mercury dichloride and cadmium carbonate. The disulfide compounds produced in this invention are intermediates in the synthesis of the biologically active 7.beta.-acyl-amino-7.alpha.-alkoxy-3-methyl 1-oxa .beta.-lactam antibiotic compounds.
    Type: Grant
    Filed: May 18, 1981
    Date of Patent: July 19, 1983
    Assignee: Eli Lilly and Company
    Inventors: Stjepan Kukolja, Janice L. Pfeil
  • Patent number: 4379917
    Abstract: Apramycin derivatives substituted at the 6"-position with a variety of substituents are claimed as broad spectrum antibiotics. Also claimed are starting materials and intermediates in the synthesis of the above apramycin derivatives.
    Type: Grant
    Filed: December 24, 1981
    Date of Patent: April 12, 1983
    Assignee: Eli Lilly and Company
    Inventor: Herbert A. Kirst