Oxy Patents (Class 562/444)
  • Patent number: 4182899
    Abstract: The present application relates to the optical resolution into optical antipodes of compounds of the formula ##STR1## as well as to salts consisting of an optical isomer of a compound of the above formula and an optical isomer of 2-aminobutanol. The optically active compounds of the above formula are employed as starting materials for the production of semisynthetic antibiotics of the cephalosporin or penicillin type.
    Type: Grant
    Filed: August 7, 1978
    Date of Patent: January 8, 1980
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Yung B. Chae, Dae W. Kim
  • Patent number: 4179573
    Abstract: This invention provides the amino acid (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid which is prepared by hydrolysis of bestatin. Bestatin is a chemical which inhibits aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase, enhances the antitumor effect of bleomycin, has the chemical name [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine, has the following structure ##STR1## and is prepared by cultivating a strain of streptomyces which produces bestatin in a nutrient medium under aerobic conditions until substantial activity inhibitory to aminopeptidase B is imparted to said cultured medium and then recovering said bestatin from said cultured medium. A preferred strain is Streptomyces olivoreticuli FERM-P No. 2590 (A.T.C.C. 31159).
    Type: Grant
    Filed: August 19, 1977
    Date of Patent: December 18, 1979
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada, Yoshiro Okami
  • Patent number: 4175206
    Abstract: Glyoxylic acid or a salt of glyoxylic, an ammonium salt of an organic or inorganic acid and a phenol compound of the formula: ##STR1## wherein n is an integer of one to three, are condensed together to prepare hydroxyphenylglycine compounds of the formula: ##STR2## wherein n is the same as defined above. The hydroxyphenylglycine compounds thus obtained are useful as intermediates in the synthesis of penicillins and cephalosporins.
    Type: Grant
    Filed: May 8, 1978
    Date of Patent: November 20, 1979
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Masaru Senuma, Nobuhiko Ishihara, Shigeru Nishimoto, Eisaku Yamato, Noboru Shigematsu
  • Patent number: 4172846
    Abstract: A process is disclosed for the separation of a mixture of an optically active .alpha.-phenylglycine amide and the corresponding optically active .alpha.-phenylglycine acid, through the formation of a novel Schiff base of at least the amide, and achieving the separation with the resulting solubility differences while substantially completely avoiding racemization.
    Type: Grant
    Filed: October 19, 1977
    Date of Patent: October 30, 1979
    Assignee: Stamicarbon, B.V.
    Inventor: Wilhelmus H. J. Boesten
  • Patent number: 4169108
    Abstract: Aminoalkylnaphthols and esters thereof, useful as cardiotonic agents, prepared from the corresponding RO-naphthalenealkylamines, certain of which are also useful as cardiotonic agents, are disclosed.
    Type: Grant
    Filed: August 16, 1973
    Date of Patent: September 25, 1979
    Assignee: Sterling Drug Inc.
    Inventor: Denis M. Bailey
  • Patent number: 4163060
    Abstract: Novel substituted aromatic aliphatic amino carboxylic acids containing a tertiary nitrogen atom such as 3-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)] ethylamino] -1-propane carboxylic acid ethyl ester or 7-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)] ethylamino] -1-heptane carboxylic acid ethyl ester have been found to be useful spasmolytic agents.
    Type: Grant
    Filed: January 17, 1977
    Date of Patent: July 31, 1979
    Assignee: U.S. Philips Corporation
    Inventors: Jan Hartog, Johannes M. A. Zwagemakers
  • Patent number: 4140863
    Abstract: The present invention relates to certain 9,11-dideoxy-PGF-type compounds wherein the C-9 and C-11 carbon atoms are substituted by halogen. In particular, 9,11-chloro-, 9,11-bromo-, and 9,11-iodo-9,11-dideoxy-PGF compounds are disclosed.These compounds are particularly useful for numerous pharmacological purposes, based on their ability to stimulate mammalian smooth muscle tissue.
    Type: Grant
    Filed: June 17, 1977
    Date of Patent: February 20, 1979
    Assignee: The Upjohn Company
    Inventor: Roy A. Johnson
  • Patent number: 4134994
    Abstract: Amine salts of tertiary amino acids have been found to be effective as catalysts for polyurethane synthesis and they have been found to exhibit delayed action, in many instances, in the polymerization of urethanes. Typically, the amine salts of tertiary amino acids are formed by initially reacting a primary or secondary amine with an aldehyde and disubstituted acid to form a Mannich adduct and then reacting the resulting Mannich acid adduct with an amine.
    Type: Grant
    Filed: December 1, 1976
    Date of Patent: January 16, 1979
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Ibrahim S. Bechara, Philip J. Zaluska, Rocco L. Mascioli
  • Patent number: 4128573
    Abstract: 2-[4-(2-Fluorophenoxy)phenyl]propionic acid and salts, esters, the amide and the alcohol derived therefrom, useful as anti-inflammatory agents, and their preparation.
    Type: Grant
    Filed: September 22, 1976
    Date of Patent: December 5, 1978
    Assignee: Boots Pure Drug Company Limited
    Inventors: Stewart S. Adams, Bernard J. Armitage, John S. Nicholson, James G. Tantum
  • Patent number: 4123538
    Abstract: Novel (2-amino-2-oxoethoxy)acetic acid compounds and antisecretory compositions and methods employing (2-amino-2-oxoethoxy)acetic acid compounds are disclosed. The (2-amino-2-oxoethoxy)acetic acid compounds are also useful as cardiotonic agents and as calcium binding agents; certain of the compounds are also useful for their calcium transport properties. Novel 4-substituted 3,5-morpholinediones intermediates in the preparation of certain of the (2-amino-2-oxoethoxy)acetic acid compounds and further useful as antisecretory agents are also disclosed.
    Type: Grant
    Filed: August 30, 1977
    Date of Patent: October 31, 1978
    Assignee: McNeil Laboratories, Incorporated
    Inventor: Michael J. Umen
  • Patent number: 4123611
    Abstract: 6-Aminoacylamidopenicillanic acid or 7-amino-acylamidocephalosporanic acids are produced in high yields by acylating 6-aminopenicillanic acid or 7-aminocephalosporanic acid with an amino acid, or a functional equivalent thereof, having its amino group protected with N,N-disubstituted .beta.-keto acid amide, and then removing the protecting group from the resulting protected 6-aminoacylamidopenicillanic acid or protected 7-aminoacylamidocephalosporanic acid by hydrolysis.
    Type: Grant
    Filed: January 6, 1975
    Date of Patent: October 31, 1978
    Assignee: President of Osaka University
    Inventors: Toshiyasu Ishimaru, Yasutsugu Shimonishi, Hisayuki Sakurai, Minoru Hatanaka
  • Patent number: 4120867
    Abstract: Monoradioiodinated derivatives of compounds employed in a radioassay prepared from precursors which are either active esters, amino acids, or amines, including a phenolic or imidazole substituent group in which one of the possible two sites on the group for radioiodination is substituted to permit production of a monoradioiodinated derivative. A preferred precursor is an active ester of 3-fluoro-5-radioidotyrosine which can be coupled to a compound including an amino group to produce a monoradioiodinated derivative of the compound.
    Type: Grant
    Filed: September 29, 1976
    Date of Patent: October 17, 1978
    Assignee: Becton, Dickinson & Company
    Inventors: Anandrao S. Akerkar, Herman Rutner
  • Patent number: 4120870
    Abstract: Group IB and IIB metal phosphine complexes are disclosed. These complexes are reacted with rhodium complex precursors to form useful enantioselective hydrogenation catalysts. Also disclosed is a method of preparing useful compounds having optical activity such as natural products and compounds useful as flavors and fragrances.
    Type: Grant
    Filed: July 18, 1977
    Date of Patent: October 17, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John Melvin Townsend, Donald Herman Valentine, Jr.
  • Patent number: 4111981
    Abstract: Cephalosporin compounds having a substituted phenylglycyl substituent at the 7-position and any of a variety of groups at the 3-position are prepared by acylation of a 7-aminocephalosporanic acid. The compounds have antibacterial activity.
    Type: Grant
    Filed: April 28, 1977
    Date of Patent: September 5, 1978
    Assignee: SmithKline Corporation
    Inventor: John Gerald Gleason