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.
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.
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: 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
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.
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.
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.
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.
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.
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.
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.
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
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.
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.