Abstract: Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for their preparation, and methods for reducing intraocular pressure utilizing the compounds or compositions are disclosed.
Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.
Type:
Grant
Filed:
March 11, 1988
Date of Patent:
September 19, 1989
Assignee:
Warner-Lambert Company
Inventors:
Mary E. Carethers, Wiaczeslaw A. Cetenko, David T. Connor, Elizabeth A. Johnson, John S. Kiely, Charles F. Schwender, Jagadish C. Sircar, Roderick J. Sorenson, Paul C. Unangst, Robert F. Bruns
Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.
Abstract: Novel flavone carboxylic acid derivatives, intermediates therefor, and method for the preparation thereof, and their use in the differentiation of certain types of malignant cells, are all disclosed, certain of the novel compounds disclosed to be superior to retinoic acid in their activity.
Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
Type:
Grant
Filed:
March 16, 1987
Date of Patent:
September 13, 1988
Assignee:
Hoechst-Roussel Pharmaceuticals
Inventors:
Raymond W. Kosley, Jr., Robert J. Cherill
Abstract: Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
Abstract: A new widely-applicable method has been found for synthesis of 9,10-anthraquinones and similar chemical compounds of wide use in industry and pharmacology, by reacting suitable aromatic substrates with activated dicarboxylic acids (more particularly dichlorides) in the presence of metal halides. The special characteristics of the reaction are the good yields, high selectivity, the possibility of operating in a single reactor and the use of starting compounds which are cheap and easily available on the market.
Type:
Grant
Filed:
June 27, 1986
Date of Patent:
April 19, 1988
Assignee:
Consiglio Nazionale Delle Ricerche
Inventors:
Franca Bigi, Giovanni Casiraghi, Giuseppe Casnati, Giovanni Sartori
Abstract: A method of regioselectively and stereoselectively synthesizing forskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-on e) from 9-deoxyforskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one) with a good yield is described. In a preferred embodiment, it comprises an enol ether formation from 8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one-6,7-carbon ate, oxidation of the enol ether with a suitable peroxy acid to obtain 11,12-dehydro-8,13-epoxy-11-methoxy-1.alpha.,6.beta.,7.beta.,9.beta.-tetra hydrolabd-14-ene-6,7-carbonate and hydrolysis of the latter under an acidic condition to obtain 8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-one -6,7-carbonate. As an alternative way of protecting the two hydroxy groups at carbon-6 and carbon-7, they may also be converted to dimethyl acetal during the synthetic sequence. Four compounds produced in the synthetic scheme as intermediates, namely, 9,11-dehydro-8,13-epoxy-11-methoxy-1.
Abstract: The present invention relates to a process for the isolation of labdan derivatives from the plant Coleus forskohlii, and their use as medicaments having anti-inflammatory and analgesic activity.
Type:
Grant
Filed:
April 3, 1986
Date of Patent:
February 9, 1988
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Alihussein N. Dohadwalla, Sadashiv S. Mandrekar, Nandkumar K. Dadkar, Yatendra Khandelwal, Richard H. Rupp, Noel J. de Souza
Abstract: Novel chroman compounds which have excellent antioxidant activity and/or analgesic activity or serve as precursors for such active compounds are provided. There are also provided uses of these active compounds as an antioxidant and/or analgesic.
Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
Type:
Grant
Filed:
October 20, 1986
Date of Patent:
June 16, 1987
Assignee:
Hoechst-Roussel Pharmaceuticals Inc.
Inventors:
Raymond W. Kosley, Jr., Robert J. Cherill
Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
Type:
Grant
Filed:
October 17, 1986
Date of Patent:
June 9, 1987
Assignee:
Hoechst-Roussel Pharmaceuticals Inc.
Inventors:
Raymond W. Kosley, Jr., Robert J. Cherill
Abstract: Derivatives of 2,2'-iminobisethanol having useful properties in the treatment and/or the prevention of disorders of the coronary-vascular system.
Type:
Grant
Filed:
October 12, 1984
Date of Patent:
March 31, 1987
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Guy R. E. Van Lommen, Marcel F. L. De Bruyn, Marc F. J. Schroven
Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
Type:
Grant
Filed:
December 4, 1985
Date of Patent:
January 27, 1987
Assignee:
Hoechst-Roussel Pharmaceuticals Inc.
Inventors:
Raymond W. Kosley, Jr., Robert J. Cherill
Abstract: The invention relates to substituted 4-aminomethylene-chromans and chromens of Formula (I) infra, as well as methods for making of said chromans and chromens, compositions containing said chromans and chromens and methods for the use of said chromans, chromens and compositions containing said chromans and chromens. The compounds and compositions of the invention are useful for their circulation influencing activity.
Type:
Grant
Filed:
December 13, 1983
Date of Patent:
January 7, 1986
Assignee:
Bayer Aktiengesellschaft
Inventors:
Arno Widdig, Hans-Joachim Kabbe, Andreas Knorr, Ulrich Benz
Abstract: There are described novel dyes of the formulae ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, unsubstituted or substituted alkyl, cycloalkyl, aralkyl or aryl, and R.sub.1 and R.sub.2 together with the nitrogen atom, and optionally with the inclusion of further hetero atoms, can also form a 5- to 7-membered heterocycle, or one of the radicals R.sub.1 or R.sub.2 can be linked with the carbon atoms, in the o-position with respect to the amino group, of the ring A to form a fused-on, saturated, unsubstituted or substituted 5- or 6- membered ring,X is .dbd.NR.sub.3, .dbd.NCOR.sub.4, ##STR2## .dbd.NH or .dbd.O, wherein R.sub.3 is alkyl or unsubstituted or substituted phenyl,R.sub.4 is unsubstituted or substituted alkyl, aralkyl, aryl, vinyl, alkoxy, phenoxy or amino, andR.sub.5 is cyano, carbalkoxy, or unsubstituted or substituted carbonamide, andR.sub.
Abstract: Potential insect control compounds which are chromenes, as well as their method of preparation and use, are disclosed. Compounds have been found which are effective in the control of insects by inhibiting the actions of juvenile hormone. An example of a useful compound is 5-methyl-7-ethoxy-2,2-dimethyl-3-chromene. Such compounds act to induce precocious maturation of immature insects, resulting in death either during or within a short time before or after the molting to an incompetant precocious adult. Additional effects which have been obtained include sterilization of mature insects.
Abstract: There is provided a class of novel 3,4-dihydro-2H-benzopyran derivatives which either have excellent inhibitory activity against unfavorable effects of heat, light and oxidative factors or are of use as precursors of compounds having such activity, and methods for producing these derivatives. Also provided are methods of using such 3,4-dihydro-2H-benzopyran derivatives as stabilizers for organic materials sensitive to heat, light or/and oxidative factors, and organic compositions containing such stabilizers.
Abstract: A process for the preparation of an isochromane of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and denote hydrogen, lower alkyl or lower alkoxy, or together form a cyclopentane or cyclohexane ring which is optionally substituted by lower alkyl andR.sup.3 denotes hydrogen or lower alkyl,comprising reacting an alcohol of the formula ##STR2## with formaldehyde and a carboxylic acid anhydride of the formula ##STR3## or with a methylene diester of the formula ##STR4## in which R.sup.4 represents a lower alkyl radical, in the presence of an acid catalyst. The products are known, having a musk-like odor.