Patents Represented by Attorney Steven R. Lammert

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  • Azetidinone mercury sulfides and process therefor
    Patent number: 4175076
    Abstract: Novel azetidinone mercury sulfides are prepared by the reaction of penicillin derived thiazolineazetidinones with a mercuric halide in the presence of an alcohol or glycol. They are useful intermediates in the preparation of cephalosporin compounds.
    Type: Grant
    Filed: November 21, 1977
    Date of Patent: November 20, 1979
    Assignee: Eli Lilly and Company
    Inventor: Lowell D. Hatfield
  • Process for preparation of 3-halo-3-methylcephams
    Patent number: 4160091
    Abstract: 3-Halo-3-methylcephams and 2-halomethylpenams are prepared by the reaction of novel azetidinone mercuric sulfides with positive halogenating agents. 3-Halo-3-methylcephams are useful as intermediates to known desacetoxy cephalosporin antibiotics.
    Type: Grant
    Filed: November 21, 1977
    Date of Patent: July 3, 1979
    Assignee: Eli Lilly and Company
    Inventor: David K. Herron
  • Method of preparation of 3-methylenecephams
    Patent number: 4159266
    Abstract: Penicillin sulfoxide derived azetidinone sulfinyl chlorides and related sulfinic acid derivatives are cyclized to 3-methylenecephams by reaction with Friedel-Crafts catalysts or metathetic cation forming agents.
    Type: Grant
    Filed: May 13, 1977
    Date of Patent: June 26, 1979
    Assignee: Eli Lilly and Company
    Inventor: Stjepan Kukolja
  • Cephalosporin displacement reaction
    Patent number: 4144391
    Abstract: The present invention is directed to a process for the displacement of the acetoxy group of a cephalosporanic acid by a sulfur nucleophile, in an organic solvent and under essentially anhydrous conditions.
    Type: Grant
    Filed: December 27, 1977
    Date of Patent: March 13, 1979
    Assignee: Eli Lilly and Company
    Inventor: Lowell D. Hatfield
  • Cephalexin tablets
    Patent number: 4143129
    Abstract: A small tablet containing over 90% by weight of an orally active cephalosporin such as cephalexin and which utilizes as a binder polyvinyl pyrrolidone having a number average molecular weight of from 500,000 to 1,500,000.
    Type: Grant
    Filed: January 16, 1978
    Date of Patent: March 6, 1979
    Assignee: Lilly Industries Limited
    Inventor: Richard Marsden
  • 3-Substituted propanoic acid derivatives
    Patent number: 4100350
    Abstract: The invention provides 3-(2-formyl-3-hydroxy-5-oxocyclopent-1-enyl)-p ropanoic acid and derivatives thereof having anti-thrombotic activity coupled with low toxicity. Also provided is a method for preparing such compounds by subjecting a 3-[3-hydroxy-5-oxo-2-(.beta.-styryl)cyclopent-1-enyl]-propanoic acid or derivative thereof to oxidative cleavage.
    Type: Grant
    Filed: March 2, 1977
    Date of Patent: July 11, 1978
    Assignee: Lilly Industries Ltd.
    Inventors: William Dawson, Michael John Foulis, Norman James Albert Gutteridge, Colin William Smith
  • Methylenedioxybenzene -- improved method of preparation
    Patent number: 4082774
    Abstract: Methylenation of catechol by reaction with a methylene dihalide under alkaline conditions is improved by adding the pre-formed catechol dianion in a heated protic alkaline medium to a solution of methylene dihalide in dimethyl sulfoxide.
    Type: Grant
    Filed: July 11, 1974
    Date of Patent: April 4, 1978
    Assignee: Eli Lilly and Company
    Inventor: John A. Kirby
  • Method of preparation of 3-methylenecephams
    Patent number: 4052387
    Abstract: Penicillin sulfoxide derived azetidinone sulfinyl chlorides and related sulfinic acid derivatives are cyclized to 3-methylenecephams by reaction with Friedel-Crafts catalysts or metathetic cation forming agents.
    Type: Grant
    Filed: April 2, 1976
    Date of Patent: October 4, 1977
    Assignee: Eli Lilly and Company
    Inventor: Stjepan Kukolja
  • Process for preparation of 7-alkoxy-3-chloromethylcephems
    Patent number: 4048163
    Abstract: 7-Alkoxy-3-chloromethyl-3-cephems are provided by reacting a 3-methylenecepham with an alkali metal salt of a lower primary alcohol in the presence of tert-butyl hypochlorite at a temperature ranging from about -80.degree. to about 0.degree. C. The 3-chloromethylcephems provided by this invention are useful intermediates for the preparation of known cephalosporin antibiotics.
    Type: Grant
    Filed: March 22, 1976
    Date of Patent: September 13, 1977
    Assignee: Eli Lilly and Company
    Inventor: Gary A. Koppel
  • Process for preparation of 7-alkoxy-3-bromomethylcephems
    Patent number: 4048160
    Abstract: 7-Alkoxy-3-bromomethyl-3-cephems are provided by reacting a 3-methylenecepham with an alkali metal salt of a lower primary alcohol in the presence of a positive brominating agent at a temperature ranging from about -80.degree. to about 0.degree. C. The 3-bromomethylcephems provided by this invention are useful intermediates for the preparation of known cephalosporin antibiotics.
    Type: Grant
    Filed: March 22, 1976
    Date of Patent: September 13, 1977
    Assignee: Eli Lilly and Company
    Inventor: Gary A. Koppel
  • Process for preparation of 3-halomethylcephems
    Patent number: 4042585
    Abstract: 3-Halomethyl-3-cephems are provided by reacting a 3-methylenecepham with an alkali metal salt of a lower alcohol or a bicyclic amidine base in the presence of a positive halogenating agent at a temperature ranging from -80.degree. to about 20.degree. C. The 3-halomethylcephems provided by this invention are useful intermediates for the preparation of known cephalosporin antibiotics.
    Type: Grant
    Filed: March 22, 1976
    Date of Patent: August 16, 1977
    Assignee: Eli Lilly and Company
    Inventor: Gary A. Koppel
  • Process for preparation of 3-hydroxymethylcephems
    Patent number: 4038275
    Abstract: 3-Hydroxymethyl-2-cephems are provided by (1) reacting a 2-halomethylcephem compound with a .gamma.-hydroxycarboxylic acid salt or a .delta.-hydroxycarboxylic acid salt and (2) reacting the novel .gamma. or .delta.-hydroxy esters thereby obtained with a protic acid. The 3-hydroxymethylcephems provided by the process of this invention are useful intermediates for the preparation of known cephalosporin antibiotics.
    Type: Grant
    Filed: April 19, 1976
    Date of Patent: July 26, 1977
    Assignee: Eli Lilly and Company
    Inventors: Gary A. Koppel, Laurence J. Nummy
  • 3-Substituted propanoic acid derivatives and pharmaceutical composition
    Patent number: 4027036
    Abstract: The invention provides 3-(2-formyl-3-hydroxy-5-oxocyclopent-1-enyl)-propanoic acid and derivatives thereof having anti-thrombotic activity coupled with low toxicity. Also provided is a method for preparing such compounds by subjecting a 3-[3-hydroxy-5-oxo-2-(.beta.-styryl)cyclopent-1-enyl]-propanoic acid or derivative thereof to oxidative cleavage.
    Type: Grant
    Filed: April 10, 1974
    Date of Patent: May 31, 1977
    Assignee: Lilly Industries, Ltd.
    Inventors: William Dawson, Michael John Foulis, Norman James Albert Gutteridge, Colin William Smith
  • 7-Acylamino-3-acyl-2(or 3)cephems
    Patent number: 4012380
    Abstract: Intermediate C-3 1-hydroxyalkyl or 1-hydroxyarylalkyl cephems, prepared by reacting Grignard reagents at low temperature with 3-formyl-2-cephem compounds, are oxidized to the corresponding 7-acylamino-3-acyl-2(or 3)cephem-4-carboxylic acids and esters thereof, which are useful as antibiotics or as intermediates in preparing antibiotic substances.
    Type: Grant
    Filed: December 10, 1974
    Date of Patent: March 15, 1977
    Assignee: Eli Lilly and Company
    Inventor: Douglas O. Spry
  • 3-(Substituted)carbonylamino cephem derivatives
    Patent number: 4001226
    Abstract: 7-Acylamino and 7-amino-3-(substituted)carbonylamino-3(or 2)-cephem-4-carboxylic acids and esters thereof, which are useful as antibiotics or as intermediates in preparing antibiotic substances respectively, are prepared from 7-acylamino-3-azidocarbonyl-2(or 3)-cephem-4-carboxylic acid esters via the corresponding thermally derived 3-isocyanatocephem derivatives.
    Type: Grant
    Filed: December 4, 1974
    Date of Patent: January 4, 1977
    Assignee: Eli Lilly and Company
    Inventor: Douglas O. Spry
  • Preparation of 6-acylamino-2-methyl-2-halomethyl penams
    Patent number: 3960844
    Abstract: A 7-acylamino-3-hydroxy-3-methylcepham-4-carboxylic acid ester is reacted with a mixture of a halogenating agent and a tertiary carboxamide to produce a 2-halomethylpenam compound, a useful intermediate for the preparation of desacetoxycephalosporins.
    Type: Grant
    Filed: February 11, 1975
    Date of Patent: June 1, 1976
    Assignee: Eli Lilly and Company
    Inventors: Stjepan Kukolja, Steven R. Lammert
  • 3,4-Dicarboxycephalosporins and derivatives
    Patent number: 3953436
    Abstract: 7-Acylamino and 7-amino-3-carboxy-3-cephem-4-carboxylic acids and derivatives thereof, which are useful as antibiotics or as intermediates in preparing antibiotic substances, are prepared by an NBS oxidation of acetal derivatives of 3-formyl cephalosporins.
    Type: Grant
    Filed: April 19, 1974
    Date of Patent: April 27, 1976
    Assignee: Eli Lilly and Company
    Inventor: Douglas O. Spry