Abstract: A process is described for preparing optically active alpha-halogenated carbonyl compounds.This process consists of transforming the carbonyl compound into the corresponding acetal with tartaric acid or a derivative thereof, halogenating this acetal and releasing the carbonyl compound.
Type:
Grant
Filed:
October 6, 1986
Date of Patent:
August 16, 1988
Assignee:
Zambon SpA
Inventors:
Graziano Castaldi, Silvia Cavicchioli, Claudio Giordano, Carlo Restelli
Abstract: A process is described for preparing alpha-haloalkyl-aryl-ketones, comprising reacting a substantially anhydrous strong acid with a ketal of formula ##STR1## in which Ar, R, R.sub.1, R.sub.2 and X have the meanings given in the description.
Abstract: 1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.
Type:
Grant
Filed:
April 1, 1987
Date of Patent:
August 16, 1988
Assignee:
Ciba-Geigy Corporation
Inventors:
Alex Alder, Jaroslaw Stanek, Daniel Bellus
Abstract: The invention relates to 2,6-exo-configured tricyclo-5.2.1.0.sup.2,6 decane derivatives that correspond to general formula A wherein ##STR1## R.sup.a, R.sup.b, R.sup.c, R.sup.d are hydrogen or R.sup.d is a methyl group and R.sup.a, R.sup.b, R.sup.c are hydrogen or methyl groups, one of the substituents being a methyl group and both the others being hydrogen,the broken line represents a C-C double bond optionally at (-3) or (-4),the wavy line represents geometric isomers,R.sup.1 and R.sup.2 are hydrogen, or lower alkyl groups with a total of 1-6 carbon atoms, andX represents a carbonyl or hydroxyl function, as well as a process for their synthesis and their use as scents.
Abstract: This invention relates to pharmaceutical compositions containing a class of 5-phenyl-1,3-dioxoalkenyl compounds useful as inhibitors of leukotriene biosynthesis and thus useful in the treatment of conditions associated with leukotrienes. This invention also relates to the use of the 5-phenyl-1,3-dioxoalkenyl compounds in the inhibition of leukotriene biosynthesis and thus in the treatment of conditions associated with leukotrienes. This invention further relates to a novel process for the preparation of the 5-phenyl-1,3-dioxoalkenyl compounds.
Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, acyl, alkylsulfonyl, benzenesulfonyl, substituted benzenesulfonyl, and an inorganic or organic cation;R.sup.2 is selected from alkyl, alkenyl, alkynyl, substituted alkyl, haloalkenyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl and phenyl; andn is an integer chosen from 2 to 5.The compounds are cereal selective herbicides and in further embodiments the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of compounds of formula I, herbicidal compositions containing as active ingredient a compound of formula I, and processes for severely damaging or killing unwanted plants by applying to the plants or to the growth medium of the plants an effective amount of a compound of formula I.
Type:
Grant
Filed:
December 29, 1986
Date of Patent:
July 26, 1988
Assignee:
Imperial Chemical Industries plc
Inventors:
Richard B. Warner, Alexander Serban, Keith G. Watson, Graham J. Bird, Lindsay E. Cross, Graeme Farquharson
Abstract: 1-Isopropyl-3-methyl-2-(but-2'-enoyl)cyclohexane derivatives having the general formula ##STR1## in which the dotted lines represent no double bond, one double bond at position 4 or two double bonds at positions 1 and 5, 2 and 4 or 4 and 6 are valuable fragrances with fruity flowery and green odors, in some cases accompanied by woody and/or herbal notes. Above defined compounds can be used as a perfume component in perfume compositions or in products to be perfumed.
Type:
Grant
Filed:
January 9, 1987
Date of Patent:
July 26, 1988
Assignee:
Naarden Intl. N.V.
Inventors:
Antonius J. A. Van Der Weerdt, Nicolaas L. J. Broekhof, Jan G. Witteveen
Abstract: There are provided NMR contrast agents comprising water-soluble paramagnetic metal chelates, preferably of Cr(III), Fe(III) or Gd(III), wherein the chelating entity is an anilide group containing organic moiety, preferably a compound of formula I ##STR1## wherein R.sup.1 to R.sup.5 may represent hydrogen or halogen atoms, optionally halogenated alkyl or alkoxy groups or carboxyl groups. The agents are especially suitable for use in NMR imaging of the hepatobiliary system.
Abstract: The present invention relates to new synthetic compounds of the cannabinoid class, specifically carenadiol and its derivatives. This compound and its derivatives have been shown to have biological activity which indicates their usefulness in the treatment of patients with various neurological disorders.
Type:
Grant
Filed:
May 15, 1987
Date of Patent:
July 19, 1988
Assignee:
University Patents, Inc.
Inventors:
Arnold R. Martin, Paul F. Consroe, Vibhakar J. Shah
Abstract: 3,10-Diacetyl-11-isopropylidene-7,7-dimethyl-tricyclo[6.2.1.0.sup.2,6 ]undeca-2,5,9-triene is a flavoring ingredient useful for the aromatization of smoking articles. It develops upon smoking green, slightly floral, metallic, astringent, fatty, slightly bitter and earthy notes.It is prepared by a two-step process from 1-(4-isopropylidene-1-cyclopent-1-enyl)-1-ethanone.
Abstract: The invention relates to a process for preparing aromatic or hetero-aromatic aldehydes by the Reimer-Tiemann formylation reaction. The process comprises employing a solid alkaline hydroxide in order to carry out the reaction in a solid/liquid medium and by adjusting the initial hydration rate of the medium to be higher than 0.05 moles of water per mole of initial compound and less than 1.5 moles of water per mole of alkaline hydroxide initially in the medium. Such a process makes it possible to substantially increase the yield of the Reimer-Tiemann reaction and to avoid tar formation entirely or in large part.
Type:
Grant
Filed:
April 10, 1987
Date of Patent:
July 5, 1988
Assignee:
Institut National Polytechnique
Inventors:
Annick Thoer, Ghislain Denis, Michel Delmas, Antoine Gaset
Abstract: Method for the preparation of ketones, by means of oxydation of the corresponding secondary alcohols, characterized in that said alcohols are catalytically oxidized by H.sub.2 O.sub.2 inside a two-phase system comprising:(a) an aqueous phase, containing hydrogen peroxide as the oxidizing agent;(b) an organic phase, containing a secondary alcohol and optionally a solvent immiscible with said aqueous phase, as well as a peroxidic catalyst having the general formula Q.sub.3 XW.sub.4 O.sub.24, wherein X represents an atom of phosphorus or of arsenic and wherein Q represents a quaternary cation, containing hydrocarbon groups having a total of from 20 to 70 C atoms.
Type:
Grant
Filed:
January 8, 1987
Date of Patent:
June 28, 1988
Assignees:
Instituto Guido Donegani S.p.A., Consiglio Nazionale Delle Ricerche
Inventors:
Carlo Venturello, Mario Gambaro, Marco Ricci
Abstract: There is disclosed a method for the preparation of a dialkyl ketone from an aliphatic carboxylic acid in the presence of a catalyst comprising manganese dioxide on a support of catalytically active alumina. This method is a convenient way of making diethyl ketone from propionic acid.
Abstract: 4,4,7-trimethyl-3,4,7,8-tetrahydro-2(6H)-naphthalen-one is obtained by an elimination reaction from 3-oxo-.alpha.-ionol by way of direct addition thereof to a solution of a protonic acid in an inert solvent at an elevated temperature, or following its conversion into a low-carbon alkyl ester, particularly acetate, by way of the treatment of the latter, preferably with sodium acetate, in a polar non-protonic solvent at 150.degree.14 300.degree. C., wherein the output can be increased by raising the temperature of reaction. The product of the process is suitable, in pure form or as mixed with simultaneously produced 3,5,5-trimethyl-4-butenylidene-cyclo-hex-2-en-1-one, as an odiferous substance or as a fragrant substance for foods and tobacco.
Abstract: A process for making a 2,6-di-hydrocarbyl-4-alkoxyalkylphenol, e.g. 2,6-di-tert-butyl-4-methoxymethylphenol, by reacting a 2,6-dihydrocarbylphenol with formaldehyde in a stoichiometric excess of alcohol and in the presence of a Mannich base catalyst preferably formed in situ by adding a catalyst-forming amount of a secondary amine, e.g. dimethylamine, to the mixture of 2,6-di-hydrocarbylphenol, formaldehyde and alcohol. Unreacted alcohol and amine are distilled out and the 2,6-di-hydrocarbyl-4-alkoxyalkylphenol is reacted with a benzene-type compound, e.g. mesitylene, to make a hindered phenolic antioxidant, e.g. 1,3,5-trimethyl-2,4,6-tri-(3,5-di-tert-butyl-4-hydroxybenzyl)benzene.
Abstract: The invention is insecticidal diaminoguanidine hydrazone compounds which are also effective antifeeding agents for insects and methods for their preparation.
Type:
Grant
Filed:
December 8, 1986
Date of Patent:
June 28, 1988
Assignee:
American Cyanamid Company
Inventors:
Roger W. Addor, Donald P. Wright, Jr., Jack K. Siddens, John J. Hand
Abstract: Compounds with anthropodicidal activities having the general formula (1) ##STR1## and their isomeric forms wherein R represents F, Cl, Br, ethoxy, methoxy or propxy and n is an integer between 1 and 5; or R represents 3,4-methylenedioxyl; and R.sup.40 represents di- or trichloromethyl, fluorodichloromethyl or trifluoromethyl.
Type:
Grant
Filed:
March 10, 1986
Date of Patent:
June 28, 1988
Assignee:
Dunlena Pty. Ltd.
Inventors:
George Holan, Kurt Rihs, Wynona M. P. Johnson
Abstract: The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or anti-hyperglycaemic activity.
Abstract: Benzoyl alanines having the formula: ##STR1## in which the symbols R.sup.1 and R.sup.2 (a) both represent hydrogen or(b) both represent a straight-chain or branched chain alkyl residue having from 1 to about 6 carbon atoms, or(c) R.sup.1 represents hydrogen and R.sup.2 represents a straight-chain or branched chain alkyl residue having from 1 to about 6 carbon atoms and in which the symbol R.sup.3 represents a C(CH.sub.3).sub.m (CH.sub.2 OH).sub.3-m moiety wherein the symbol m represents an integer of from 0 to 3and alkali metal and ammonium salts thereof, are disclosed.The compounds are useful as corrosion-inhibitors for metals in aqueous systems.
Type:
Grant
Filed:
June 13, 1986
Date of Patent:
June 14, 1988
Assignee:
Henkel Kommanditgesellschaft auf Aktien
Inventors:
Josef Penninger, Karl H. Schmid, Juergen Geke
Abstract: The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sup.1 =HO or HOOC(CH.sub.2).sub.x CHR.sup.2 NH--;R.sup.2 =H, lower alkyl, benzyl or --CH.sub.2 OH;x=0 or 1;A=--(CH.sub.2).sub.n -- or ##STR2## n=1 to 5; and Y=H, Cl or OCH.sub.3Z=H or Clm=0 or 1R=lower alkyl;with the proviso that where R.sup.1 =OH, Y is H or Cl and m is 1, n is 4 or 5.The present invention is also directed to an antisickling pharmaceutical carrier and an antisickling agent of the general formula (I) (without the proviso) and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
April 30, 1987
Date of Patent:
June 14, 1988
Assignees:
Merck & Co., Inc., The University of Pittsburgh
Inventors:
Donald J. Abraham, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.