Abstract: Certain aminomethyl-benzodioxanes and benzopyrans are useful serotonergic agents. They possess anxiolytic properties with few of the side effects often associated with dopaminergic agents.
Abstract: Processes for the preparation of 4-substituted analogues of 5-acetylamino-2,3,5- trideoxy-D-glycero-D-galacto-non-2-enopyranosinic acid are described.
Abstract: A phenol, a formaldehyde and an unsaturated compound having carbon-carbon double bond are reacted in the presence of a secondary amine and an acid at a temperature of 100.degree. to 250.degree. C., to give a chroman.
Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 55080. This novel antibiotic is useful as an anticoccidial in poultry, in the prevention and treatment of swine dysentery and as a growth promotant in cattle and swine.
Type:
Grant
Filed:
December 6, 1994
Date of Patent:
February 27, 1996
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, John P. Dirlam, Hiroshi Maeda, Junsuke Tone
Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
Type:
Grant
Filed:
April 29, 1994
Date of Patent:
February 20, 1996
Assignee:
Polaroid Corporation
Inventors:
Richard M. Allen, Peter K. Chu, John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
Abstract: The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromarase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.
Type:
Grant
Filed:
March 18, 1994
Date of Patent:
February 13, 1996
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Norton P. Peet, J. O'Neal Johnston, Joseph P. Burkhart
Abstract: The present invention provides a compound which has a fluoroalkyl group, a lipophilic group (an alkyl group) and a hydrophilic group in the same molecule.
Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof where A is phenyl, naphthyl or dihydro- or tetrahydronaphthyl optionally substituted on the aromatic ring by one to three substituents independently selected from halogen, cyano, trifluoromethyl, nitro, alkoxy, alkylsulfonyl, alkyl, cycloalkyl, aryl or a hydrogen bond donor; B is a bond or an oxygen atom and R.sup.1 to R.sup.4 are as defined herein. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
Abstract: This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.
Abstract: This invention relates to alkylated sulfonium alkylene derivatives of certain 2H-1-benzopyrans, to the intermediates and processes useful for their preparation, to their free-radical scavenger and cardioprotective properties and to their end-use application as therapeutic agents.
Type:
Grant
Filed:
February 28, 1995
Date of Patent:
January 16, 1996
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.
Abstract: Methods of producing carboxylic acid ester derivatives of formulae (I) and (II), which are useful, for instance, as intermediates for producing an anti-hypercholesterolemic agent having an inhibitory effect on HMG-CoA Reductase: ##STR1## wherein R.sup.1 and R.sup.2 are independently a protective group for hydroxyl group, or R.sup.1 and R.sup.2 integrally constitute a protective group for hydroxyl groups; R.sup.3 is an alkyl group, or an aryl group; and R.sup.4 is a substituted aryl group, a substituted heterocyclic group, a substituted vinyl group, or a substituted cycloalkenyl group; and ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are respectively the same as defined in the above formula (I), are disclosed. In addition, intermediates for use in these methods of producing the carboxylic acid ester derivatives are disclosed.
Abstract: This invention relates to a novel 7-deacetoxy baccatine IV derivative having formula (I): ##STR1## the preparation thereof from taxine B, and its use in preparing biologically active products. In said formula (I), R is a hydrogen atom or acetyl radical and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydroxy-function protective groupings (preferably acetonides).
Type:
Grant
Filed:
January 14, 1994
Date of Patent:
January 2, 1996
Assignee:
Centre National de la Recherche Scientifique
Inventors:
Alain Ahond, Laurent Ettouati, Pierre Potier, Christiane Poupat
Abstract: Sulfonated diphosphines of the formula ##STR1## in which Ar is m-C.sub.6 H.sub.4 -SO.sub.3 M, M is hydrogen, ammonium, a monovalent metal, or the chemical equivalent of a polyvalent metal; Ph is phenyl; the m's are individually 1 or 2, and the n's are individually 0, 1, or 2. A method of their preparation and the hydroformylation of olefins and olefinically unsaturated compounds using these compounds as a constituent of water-soluble catalyst systems are also disclosed.
Type:
Grant
Filed:
May 11, 1994
Date of Patent:
January 2, 1996
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Wolfgang A. Herrmann, Rainer Manetsberger, Helmut Bahrmann, Christian Kohlpaintner, Peter Lappe
Abstract: The novel 2R,4S-2-ethyl-4-[(4-phenoxyphenoxy)methyl]dioxolan of formula I ##STR1## can be used as a pesticide. It is used to control especially insects in fruit and citrus crops.
Type:
Grant
Filed:
September 29, 1994
Date of Patent:
December 26, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Friedrich Karrer, Hans-Peter Buser, Gerardo Ramos, Alfred Rindlisbacher, Luigi M. Venanzi, Thomas R. Ward
Abstract: Cytotoxic metabolites are isolated by extraction and chromatography from a marine sponge of the same species as that deposited in the Zoological Museum of the University of Amsterdam under reg. no. ZMA POR. 10883. The isolated compounds belong to the genus of compounds having the structure: ##STR1## wherein R is C.sub.6 -C.sub.12 alkyl or C.sub.6 -C.sub.12 alkenyl having 1 or 2 double bonds, which may be interrupted with one or more imino groups and which may be substituted with one or more substituents selected from the group consisting of amino, carboxyl, hydroxy, imino and oxo.
Abstract: A new benzodioxole derivative has a substituent in the phenyl ring which is a carboxyalkylthioalkyl or the like and is effective to treat a liver disease.
Abstract: A pattern can be formed on a substrated using a pattern forming material comprising (a) a medium, e.g. a polymer or compound, having reactivity for changing solubility in an alkali aqueous solution by a reaction using an acid as a catalyst, and (b) as an acid precursor an alkylsulfonic acid ester obtained from a compound having at least two phenolic hydroxyl groups.
Type:
Grant
Filed:
September 13, 1993
Date of Patent:
November 28, 1995
Assignees:
Hitachi, Ltd., Hitachi Chemical Company, Ltd.
Abstract: Compounds of formula I ##STR1## in which R.sub.1 is isooctyl, nonyl or dodecyl, R.sub.2 is H or --SO.sub.3 R.sub.6, R.sub.3 (A--O).sub.m R.sub.5 where each A, independently, is --C.sub.2 H.sub.4 --, --C.sub.3 H.sub.6 -- or --C.sub.4 H.sub.8 --, R.sub.4 is (B--O).sub.n R.sub.5 where each B, independently, is --C.sub.2 H.sub.4 --, --C.sub.3 H.sub.6 -- or --C.sub.4 H.sub.8 --, R.sub.5 is H or --SO.sub.3 R.sub.6, provided that at least one R.sub.5 is --SO.sub.3 R.sub.6, R.sub.6 is H, an alkali metal, an equivalent of an alkaline earth metal or optionally substituted ammonium, m is 1, 2 or 3 and n is 0, 1 or 2, provided that m+n is at most 4, when n=0 then R.sub.5 is H and m=1, when only one group R.sub.5 is --SO.sub.3 R.sub.6 and n=1 or 2 then both R.sub.2 's are H,are useful as emulsifying and dispersing agents, especially as dyeing or printing assistants for dyeing or printing a substrate dyeable with anionic or disperse dyes.