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.
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
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.
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.
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.
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.
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.
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
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
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.
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.
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.
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.
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.