Patents Examined by Gerald A. Schwartz
  • 6-Sulfur analogs of penicillins and cephalosporins
    Patent number: 4093625
    Abstract: Sulfur analogs of 6-aminopenicillanic acid and biologically active derivatives thereof are formed in a photochemical reaction of the esters of 6-diazopenicillanic acid with thiol compounds. Sulfur analogs of 7-aminocephalosporanic acid and biologically active derivatives thereof may be analogously formed in a photochemical reaction of the esters of 7-diazocephalosporanic acid with thiol compounds, or preferably, are formed from the corresponding sulfur analogs of 6-aminopenicillanic acid and derivatives thereof, through sulfoxide rearrangement of the thiazolidine ring of penicillins to the dihydrothiazine ring system of cephalosporins. These sulfur analogs of penicillins and cephalosporins are new antibacterial agents and display antibacterial activity against a wide variety of organisms.
    Type: Grant
    Filed: August 9, 1976
    Date of Patent: June 6, 1978
    Assignee: Massachusetts Institute of Technology
    Inventors: Thomas J. Commons, John C. Sheehan, Young-Sek Lo
  • Derivatives of amoxicillin
    Patent number: 4092309
    Abstract: Derivatives of amoxicillin having broad spectrum antibacterial activity are disclosed. In addition, the following methods for preparing the compounds are provided (a) reacting the free amino acid amoxicillin or the acid salt or silylated derivative thereof with a reactive derivative of 6-(4-pyridyl)-1,2-dihydro-2-oxonicotinic acid and (b) reacting the free amino acid 6-aminopenicillanic acid or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-(+)-N-(1,2-dihydro-2-oxonicotinyl)-2-(p-hydroyphenyl)glycine.
    Type: Grant
    Filed: April 27, 1977
    Date of Patent: May 30, 1978
    Assignee: Warner-Lambert Company
    Inventor: Thomas Frederick Mich
  • Mixtures having antimicrobial or pesticidal effect
    Patent number: 4092432
    Abstract: The present invention relates to mixtures of guanidated aliphatic polyamines, or their acid addition salts, having antimicrobial or pesticidal effect. More particularly the invention relates to such mixtures which have a total degree of guanidation exceeding 30%. The mixtures are suitable for agricultural and industrial use.
    Type: Grant
    Filed: October 22, 1976
    Date of Patent: May 30, 1978
    Assignee: KemaNord AB
    Inventors: Christer James Axel Bjorklund, Alf Ragnar Reuterhall
  • Esters of amidinopenicillanic acids, pharmaceutical preparations and method for treating infectious diseases
    Patent number: 4089963
    Abstract: New esters of amidinopenicillanic acids of the formula ##STR1## wherein each of R.sup.1 and R.sup.2, which are the same or different, is a saturated or unsaturated alkyl group, a cycloalkyl, or cycloalkyl-alkyl group, or wherein R.sup.1 and R.sup.2, together with the adjacent nitrogen atom, form a heterocyclic ring system; R.sup.3 is the radical ##STR2## in which radicals R.sup.4 is an alkyl, phenyl, or substituted phenyl; and R.sup.5 is hydrogen or methyl, useful as active ingredients in pharmaceutical preparation and methods for the treatment of infectious diseases.
    Type: Grant
    Filed: June 10, 1975
    Date of Patent: May 16, 1978
    Assignee: Astra Pharmaceutical Products, Inc.
    Inventors: Peter Bamberg, Bertil Ake Ekstrom, Berndt Olof Harald Sjoberg
  • 2-Decarboxy-2-hydroxymethyl-cis-4,5-didehydro-11-deoxy-PGE.sub.1, compounds
    Patent number: 4088691
    Abstract: This invention comprises certain analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.
    Type: Grant
    Filed: March 17, 1977
    Date of Patent: May 9, 1978
    Assignee: The Upjohn Company
    Inventor: Norman A. Nelson
  • 2-Decarboxy-2-hydroxy methyl-cis-4,5-didehydro-9-deoxy-9,10-didehydro-PGD.sub.1 compounds
    Patent number: 4088690
    Abstract: This invention comprises certain analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.
    Type: Grant
    Filed: March 17, 1977
    Date of Patent: May 9, 1978
    Assignee: The Upjohn Company
    Inventor: Norman A. Nelson
  • 2-Decarboxy-2-hydroxymethyl-9-deoxy-9,10-didehydro-PGD.sub.1 analogs
    Patent number: 4088693
    Abstract: This invention comprises certain analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.
    Type: Grant
    Filed: April 6, 1977
    Date of Patent: May 9, 1978
    Assignee: The Upjohn Company
    Inventor: Norman A. Nelson
  • 2-Decarboxy-2-hydroxymethyl-5-oxa-11-deoxy-PGE.sub.1 compounds
    Patent number: 4088692
    Abstract: This invention comprises certain analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmocological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.
    Type: Grant
    Filed: March 17, 1977
    Date of Patent: May 9, 1978
    Assignee: The Upjohn Company
    Inventor: Norman A. Nelson
  • 2-Decarboxy-2-hydroxymethyl-11-deoxy-PGE.sub.2 analogs
    Patent number: 4088694
    Abstract: This invention comprises certain analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.
    Type: Grant
    Filed: April 6, 1977
    Date of Patent: May 9, 1978
    Assignee: The Upjohn Company
    Inventor: Norman A. Nelson
  • Anti-androgenic steroids
    Patent number: 4087461
    Abstract: 6 (H)-5,10-seco-4,5-dieneketo steroids are disclosed which exhibit anti-ardrogenic properties.
    Type: Grant
    Filed: August 22, 1977
    Date of Patent: May 2, 1978
    Assignee: The Johns Hopkins University
    Inventor: Cecil H. Robinson
  • Carbodiimides
    Patent number: 4085140
    Abstract: A process for the conversion of isocyanate groups to carbodiimide groups which comprises contacting the compound containing the isocyanate groups with a cyclic phosphorus compound which catalyses said conversion in the presence of a nitrogeneous base and the use of the products thereof in the manufacture of isocyanate-based polymers.
    Type: Grant
    Filed: August 23, 1977
    Date of Patent: April 18, 1978
    Assignee: Imperial Chemical Industries Limited
    Inventor: Arthur Ibbotson
  • Process for producing imine compounds
    Patent number: 4083869
    Abstract: An imine compound is produced in high yield by reacting a benzophenone with ammonia in the presence of 0.01 to 100% by weight of an oxide of at least one of metals selected from the group consisting of metals of the second to fifth periods of Group III to V of the periodic Table, and iron as a catalyst at a reaction temperature of 150.degree. to 250.degree. C on the basis of benzophenone. Ammonia is fed to the reaction system continuously under a pressure of 2 to 15 atmospheres. A solvent may be used for the reaction. The catalyst metal oxide can be readily recovered and reused without any influence of water formed by the reaction.
    Type: Grant
    Filed: September 7, 1977
    Date of Patent: April 11, 1978
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Tomiya Isshiki, Tetsuo Tomita, Mitsuo Abe, Norio Takeda, Mitsuo Miura
  • Antibacterial agents
    Patent number: 4081441
    Abstract: The penicillanic acids of the formula ##STR1## wherein Z is an oxygen or sulfur atom and their pharmaceutically acceptable salts and physiologically hydrolyzed esters possess antibacterial activity and are particularly valuable in treating Pseudomonas infections.
    Type: Grant
    Filed: April 6, 1977
    Date of Patent: March 28, 1978
    Assignee: Bristol-Myers Company
    Inventors: Stephen Richard Baker, Charles Truman Holdrege
  • 6-Amino-2,2-dimethyl-3-cyanopenams
    Patent number: 4081455
    Abstract: 6-AMINO AND 6-(N-protected amino)-2,2-dimethyl-3-cyanopenams, intermediates therefor, and a process for the conversion of the 3-cyano penams, by reaction with a source of azide ion in a reaction inert solvent, to 6-amino-and 6-(N-protected amino)-2,2-dimethyl-3(5-tetrazolyl)penams, intermediates for the preparation of antibacterial agents.
    Type: Grant
    Filed: February 25, 1977
    Date of Patent: March 28, 1978
    Assignee: Pfizer Inc.
    Inventor: Donald E. Kuhla
  • 3-Substituted aminocycloalkyl esters of penicillin antibiotics
    Patent number: 4081546
    Abstract: A class of substituted aminocycloalkyl esters of penicillins have improved pharmacokinetic properties and are hydrolysed to the antibacterially active penicillin.
    Type: Grant
    Filed: June 20, 1977
    Date of Patent: March 28, 1978
    Assignee: Beecham Group Limited
    Inventor: Harry Ferres
  • Penicillins
    Patent number: 4081545
    Abstract: A class of .alpha.-(heterocyclic carbonylamino) penicillins in which the heterocyclic group of the acyl moiety is a fused bicyclic ring having a nitrogen atom at the bridge position, shows good antibacterial activity.
    Type: Grant
    Filed: October 29, 1976
    Date of Patent: March 28, 1978
    Assignee: Beecham Group Limited
    Inventor: John Peter Clayton
  • Penicillin oxides
    Patent number: 4081443
    Abstract: Compounds of the formula: ##STR1## (where COB is carboxy or protected carboxy and X is hydrogen or nucleophilic group)preparable by oxidation of the corresponding N-nitrosopenicillin derivatives are useful as starting materials for synthesizing known and useful cephalosporins.
    Type: Grant
    Filed: June 15, 1977
    Date of Patent: March 28, 1978
    Assignee: Shionogi & Co., Ltd.
    Inventors: Shoichiro Uyeo, Hikaru Itani, Tsutomu Aoki, Teruji Tsuji, Wataru Nagata
  • Benzyl oxime ethers
    Patent number: 4079149
    Abstract: Insecticidal benzyl oxime ethers of the formula: ##STR1## wherein the symbols have meanings defined in the specification.
    Type: Grant
    Filed: June 30, 1977
    Date of Patent: March 14, 1978
    Assignee: Shell Oil Company
    Inventor: Arthur C. Henry
  • Fungicidally active derivatives of carbamic acid oxime-esters of isonitrosocyanoacetic acid
    Patent number: 4079147
    Abstract: Derivatives of carbamic acid oxime-esters of isonitrosocyanoacetic acid of the formula ##STR1## in which Q represents a straight or branched hydrocarbon chain with 1 to 11 carbon atoms,R.sup.1 represents the --NHR.sup.3 or --NH--CO--NH.sub.2 group or a straight or branched alkoxy group with 1 to 5 carbon atoms,R.sup.2 represents an alkoxycarbonyl, alkenoxycarbonyl or alkynoxycarbonyl group, in each case with a total of up to 5 carbon atoms, or represents the CN group, andR.sup.3 represents hydrogen or alkyl with up to 4 carbon atomsWhich possess fungicidal properties.
    Type: Grant
    Filed: June 3, 1977
    Date of Patent: March 14, 1978
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Brandes, Werner Daum
  • Phthalide penicillin ester intermediates
    Patent number: RE29650
    Abstract: .[.The.]. Phthalide ester of 6-[(D(-).alpha.-aminophenylacetamido] penicillanic acid and intermediates therefor .[.are described.].. The phthalide penicillin ester is orally administrable to provide high serum concentrations of the .Iadd.free acid form of the .Iaddend..[.parent.]. penicillin..[.This application is a division of application Ser. No. 259,560 filed June 5, 1972, now U.S. Pat. No. 3,860,579..]. .Iadd.
    Type: Grant
    Filed: August 18, 1977
    Date of Patent: May 30, 1978
    Assignee: Beecham Group Limited
    Inventor: Harry Ferres