Oxy In Acid Moiety Patents (Class 560/39)
  • Patent number: 4147873
    Abstract: Novel vinyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; Z is R.sub.1 OCCH.dbd.CH-- or R.sub.1 OC(CH.sub.2).sub.n -- wherein n is an integer of from 1 to 3; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when Z is R.sub.1 OC(CH.sub.2).sub.
    Type: Grant
    Filed: July 1, 1977
    Date of Patent: April 3, 1979
    Assignee: Merrell Toraude et Compagnie
    Inventors: Brian W. Metcalf, Michel Jung
  • Patent number: 4134991
    Abstract: A compound having the general formula ##STR1## in which R represents a hydrogen atom or a hydroxyl radical, R.sub.1 represents a hydrogen atom or a methyl radical, and R.sub.2 represents a phenylethyl radical, a C.sub.1 -C.sub.16 alkyl radical, or a C.sub.6 -C.sub.16 monocyclic, polycyclic or alicyclic radical optionally bonded through a methylene radical, and its pharmaceutically acceptable acid addition salts, the formula (I) having the L-configuration when R is OH and when R and R.sub.1 are both hydrogen, and having the DL-configuration when R is hydrogen and R.sub.1 is methyl.These compounds and salts are useful as medicaments in human and veterinary medicine for cardiovascular and/or neurological treatment.
    Type: Grant
    Filed: September 26, 1977
    Date of Patent: January 16, 1979
    Assignee: Synthelabo
    Inventor: Camille G. Wermuth
  • 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: 4113959
    Abstract: Chiral, hinged, asymmetric host binaphthyl-based multiheteromacrocycles of oxygen covalently bonded to styrene/divinylbenzene copolymers are provided. These new compounds have specific chiral recognition properties, which properties make these new compounds useful for separating or resolving racemic and other mixtures of amino acids, amino acid esters and salts thereof for either or both of analytical purposes or large scale manufacturing procedures.
    Type: Grant
    Filed: June 13, 1977
    Date of Patent: September 12, 1978
    Assignee: The Regents of the University of California
    Inventor: Donald J. Gram
  • Patent number: 4105789
    Abstract: New carboxyalkylacylamino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
    Type: Grant
    Filed: May 10, 1976
    Date of Patent: August 8, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Miguel Angel Ondetti, David W. Cushman
  • Patent number: 4098789
    Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkoxycarbonyl, amido or substituted amido; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; have antiinflammatory activity.
    Type: Grant
    Filed: March 2, 1977
    Date of Patent: July 4, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Chester F. Turk
  • Patent number: 4094978
    Abstract: 3-(3-hydroxyprop-1-(t)-enyl)-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids; 3-(3-carbamoyloxyprop-1-(t)-enyl)-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids; and 3-[3-(N-substituted carbamoyloxy)prop-1-(t)-enyl]-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids and derivatives and salts thereof and process for preparing such compounds. The compounds are useful as antibacterials and are active against a wide variety of gram positive and gram negative bacteria.
    Type: Grant
    Filed: July 29, 1976
    Date of Patent: June 13, 1978
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Philip J. Beeby
  • Patent number: 4094857
    Abstract: An antioxidant useful for stabilizing polyesters having the formula ##STR1## where R.sub.1 is hydrogen or a lower alkyl radical; R.sub.2 is a monovalent radical containing carbon, hydrogen, and oxygen, free of ethylenic or acetylenic unsaturation, and having a molecular weight between about 99-300 and, further, containing two carboxyl groups or their ester forming equivalents; R.sub.3 and R.sub.4 are tertiary alkyl radicals each containing not more than 8 carbon atoms; and x is an integer of from 0-4.
    Type: Grant
    Filed: September 1, 1977
    Date of Patent: June 13, 1978
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: James Richard Wolfe, Jr.
  • Patent number: 4076947
    Abstract: This disclosure describes novel 15-hydroxy prostanoic acids and derivatives thereof useful as bronchodilators, hypotensive agents and gastric acid secretion inhibitors (anti-ulcer).
    Type: Grant
    Filed: January 12, 1977
    Date of Patent: February 28, 1978
    Assignee: American Cyanamid Company
    Inventors: Robert Eugene Schaub, Martin Joseph Weiss
  • Patent number: 4075241
    Abstract: The compounds 2-Aryl-3-amino-1-butanol derivatives of the formula ##STR1## wherein R represents hydrogen or acyl; R.sup.1 and R.sup.2 each independently represents hydrogen, phenyl lower alkyl, or lower alkoxy substituted phenyl lower alkyl, or both R.sup.1 and R.sup.2 are lower alkyl; and their pharmaceutically acceptable acid salts.The compounds are crystalline solids or liquids which, having two asymmetry centers, can be obtained in their stereoisomeric forms as racemic mixtures or in their optically active forms. The compounds have cardiovascular activity as coronary dilators.The compounds can be prepared by reacting an .alpha.-arylcrotonate with ammonia or with an amine followed by hydrogenation of the carbalkoxy group to give the corresponding butanol. The butanols are acylated in usual ways to give the compounds of formula (I) wherein R represents an acyl group.
    Type: Grant
    Filed: May 8, 1972
    Date of Patent: February 21, 1978
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Elvio Bellasio, Franco Cristiani
  • Patent number: 4075219
    Abstract: A process for preparing the compound represented by the formula ##STR1## wherein the indicated carbon has the D-configuration which comprises dissolution of the compound in the L-configuration or as a mixture of the D and L-configurations in aqueous pyridine from which the compound having the D-configuration selectively crystallizes.
    Type: Grant
    Filed: March 31, 1977
    Date of Patent: February 21, 1978
    Assignee: Eli Lilly and Company
    Inventor: Lawrence J. McShane
  • Patent number: 4072760
    Abstract: Phenylethanolamines of the formula I ##STR1## wherein R is substituted phenyl or optionally substituted furyl, thienyl, or pyridyl, R.sub.5 is hydrogen, lower alkyl, or optionally substituted benzyl, R.sub.4, R.sub.6, R.sub.8, and R.sub.9 each are hydrogen or lower alkyl, R.sub.7 is hydrogen, halogen, or lower alkyl, Q is --CO--or --CH.sub.2 --, and L is hydrogen or lower alkylcarbonyl, and enantiomers, diastereoisomers and salts thereof; also, process for preparing the compounds. Compounds of the invention possess bronchosposmolytic activity.
    Type: Grant
    Filed: November 17, 1975
    Date of Patent: February 7, 1978
    Assignee: Pharmacia AS
    Inventor: Kurt Hedegaard
  • Patent number: 4070478
    Abstract: Benzimidazol-5-yl alanine derivatives useful as antihypertensive agents are disclosed as well as methods for their preparation.
    Type: Grant
    Filed: February 17, 1977
    Date of Patent: January 24, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Chandravadan Nanalal Talaty, Jeremy Wright, Nicolas Zenker
  • Patent number: 4061631
    Abstract: New 1-aza-4-thiacyclohexane-4,4-dioxide derivatives are used alone or in combination with other stabilizers for stabilizing organic materials. The new compounds are prepared by reacting substituted diallylsulfides with ammonia, amines or hydrazines.
    Type: Grant
    Filed: January 22, 1976
    Date of Patent: December 6, 1977
    Assignee: Ciba-Geigy Corporation
    Inventor: Jean Rody
  • Patent number: 4058642
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, chlorine, hydroxyl, trifluoromethyl, methyl or methoxy, andR.sub.2 is hydrogen, alkyl of 1 to 2 carbon atoms or benzyl;And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as hypertensives.
    Type: Grant
    Filed: November 30, 1976
    Date of Patent: November 15, 1977
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Ernst-Otto Renth, Anton Mentrup, Kurt Schromm, Alexander Walland
  • Patent number: 4057556
    Abstract: Tropone derivatives characterized by having a derivative of oxamic acid at positions 2 and/or 5 are disclosed. In addition, the tropone nucleus can be optionally further substituted. The foregoing compounds are useful for preventing or treating allergic conditions in a mammal. Methods for the preparation and use of said compounds are disclosed.
    Type: Grant
    Filed: June 17, 1976
    Date of Patent: November 8, 1977
    Assignee: Ayerst, McKenna & Harrison Ltd.
    Inventors: Jehan F. Bagli, Tibor Bogri
  • Patent number: 4055414
    Abstract: The disclosure herein relates to 2-halo-N-(N.sup.1 -hydrocarbyloxyoxalyl-N.sup.1 -acylaminomethyl)-2',6'-dialkylacetanilides, to a process for preparing these compounds, herbicidal compositions containing same and method of use to selectively control undesired vegetation in agricultural crops, e.g., monocotyledons such as wheat, sorghum and rice and dicotyledons such as sugarbeets and soybeans.
    Type: Grant
    Filed: March 11, 1976
    Date of Patent: October 25, 1977
    Assignee: Monsanto Company
    Inventor: John P. Chupp