Abstract: A novel biphenyl derivative of the formula: ##STR1## wherein Ring A is a substituted or unsubstituted sulfur-containing or oxygen-containing heteromonocyclic ring; Ring B is a ring of the formula: ##STR2## each of R.sup.1 and R.sup.3 is hydrogen atom, a halogen atom or a lower alkoxy group, or R.sup.1 is hydrogen atom, and R.sup.2 and R.sub.3 are combined together to form a lower alkylenedioxy group; R.sup.4 is a lower alkyl group which may have a substituent selected from a lower alkoxy group and a lower alkoxycarbonyl group; Y is methylene group or carbonyl group, and a pharmaceutically acceptable salt thereof are disclosed. Said derivative and a pharmaceutically acceptable salt thereof are useful as a therapeutic or prophylactic agent for hepatic diseases.
Abstract: Methods and compositions for blocking various channels and receptors within an organism are provided. For example, a toxin was isolated from the Argiope aurantia spider. This toxin was found to have a reversible effect on excitatory amino acid receptors. Another toxin having a molecular weight of from approximately 5,000 to approximately 7,000 daltons was isolated from the Hololena curta spider. This toxin was found to have an irreversible effect on excitatory amino acid receptors.The present invention further relates to methods of treating heart and neurological diseases by applying the toxins isolated and identified. In particular, the low molecular weight toxin from Agelenopsis aperta may provide a treatment of certain heart conditions such as arrhythmia, angina, hypertension, and congestive heart failure. In addition, the toxins may provide beneficial effects on certain neuological conditions including seizures.
Abstract: Disclosed are novel substituted 4-thiazolidinone derivatives having cyclooxygenase and 5-lipoxygenase inhibiting properties and which are topical antiinflammatory agents for inflammed conditions of the skin having the formula: ##STR1## wherein R is hydrogen or loweralkyl; R.sup.1 is loweralkyl or aryl; X is --(CH.sub.2)-aryl, --O--(CH.sub.2).sub.0-3 -aryl, --C(O)(CH.sub.2).sub.0-3 -aryl, --CH(OH)--(CH.sub.2).sub.0-3 -aryl or 3,4 ##STR2## (to form naphthyl ring); aryl is phenyl, substituted phenyl, or 2,3 or 4 pyridyl; W is oxygen; Q is -(alk.sup.1).sub.0-1 --(O).sub.0-1 --(B).sub.0-1 --(alk.sup.2).sub.0-1 --[C(O)Z].sub.0-1 ; B is ##STR3## Z is OR.sup.3 or NR.sup.4 R.sup.5 where R.sup.3 is hydrogen, loweralkyl, or a pharmaceutically acceptable metal cation, R.sup.4 and R.sup.5 are hydrogen or loweralkyl; alk.sup.1 and alk.sup.
Abstract: A radiation-sensitive material comprising a polyacid composed of tungsten and niobium, titanium and/or tantalum. A uniform film can be formed by an easy spin coating method. The polyacid has a radiation sensitivity higher than that of a polyacid comprising only tungsten.
Abstract: The stereochemical structure necessary for preparation of perpendicularly arranged cores is provided by a compound of the formula ##STR1## wherein X is a reactive group through which polymeric subunits can be bonded to the compound. In particular, X is advantageously Br. This compound can be synthesized by the reaction of tetrakis(3'-trimethylsilyl-2'-propynyl)silane with zirconocene dichloride and n-butyllithium and adding sulfur monochloride to the reaction product. This produces an adduct in which X is SiMe.sub.3. This adduct may be converted to the bromo compound by reaction with bromine. The tetrakis(3'-trimethylsilyl-2-propynyl)silane may be prepared by forming a magnesium Grignard reagent from 3-bromo-1-trimethylsilylpropyne and reacting the Grignard reagent with silicon tetrachloride.
Type:
Grant
Filed:
March 12, 1990
Date of Patent:
October 22, 1991
Assignee:
The University of South Carolina
Inventors:
James M. Tour, Ruilian Wu, Jeffry S. Schumm
Abstract: Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl.Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position.Furthermore, the compounds having remarkable antitumor activities and therefore can provide novel antitumor agents.
Type:
Grant
Filed:
February 28, 1989
Date of Patent:
October 22, 1991
Assignees:
Yamasa Shoyu Kabushiki Kaisha, Sumitomo Pharmaceuticals Company Limited
Abstract: A process for the preparation of a stable emulsion of at least one water-immiscible liquid phase L in an aqueous phase D is described which comprises mixing the liquid phase or phases L with a dispersion of spheres in an aqueous phase D, the spheres having an average diameter of 0.025 to 5 microns and consisting of substantially concentric lipid laminae encapsulating an aqueous phase E between them, the lipid or lipids constituting the laminae being ionic or nonionic amphiphilic substances capable of forming a lamellar phase in water, and subjecting the whole to mechanical agitation so as to disperse the phase (or phases) L in the phase D in the form of droplets having an average diameter of 0.1 micron to a few microns.
Type:
Grant
Filed:
March 14, 1988
Date of Patent:
October 8, 1991
Assignee:
L'Oreal
Inventors:
Arlette Zabotto, Jacqueline Griat, Rose-Marie J. Handjani, Guy G. Vanlerberghe, Alain J. Ribier
Abstract: A durable, effective foam suppressant composition produced through free-radical polymerization of mixtures of polydiorganosiloxanes, silica and a free radical polymerization initiator, and optionally, vinyl monomer(s) and pendant vinyl modified silicone oil, followed by dilution of the resulting reaction product with a low viscosity polysiloxane is disclosed. Also disclosed are methods for its production and use in suppressing foams in liquid mediums.
Type:
Grant
Filed:
January 3, 1989
Date of Patent:
October 8, 1991
Assignee:
Union Carbide Chemicals and Plastics Technology Corporation
Abstract: The invention relates to photoinitiators having a combined structure ##STR1## and their use as photoinitiators in the photopolymerization of ethylenically unsaturated compounds or binder systems containing them.
Type:
Grant
Filed:
August 8, 1989
Date of Patent:
September 10, 1991
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: Novel 8-azabicyclo[3.2.1]octylalkylthiazolidinones of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, m, x and y are defined herein, process for the preparation thereof, and methods of treating psychoses and alleviating pain employing compounds and compositions thereof are disclosed.
Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.
Abstract: Furan sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
Type:
Grant
Filed:
April 12, 1990
Date of Patent:
September 3, 1991
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Gerald S. Ponticello, Harold G. Selnick
Abstract: The present invention relates to emulsion compositions and methods for preparing these emulsion compositions which employ amphipathic emulsifying agents and high shear polymeric emulsion techniques and which may be used for the preparation of a great variety of emulsion compositions. In particular, the method provides for the preparation of hybrid products which effectively cleanse and also leave a highly protective substantive residue on the skin.
Type:
Grant
Filed:
May 31, 1990
Date of Patent:
August 27, 1991
Assignee:
Richardson-Vicks Inc.
Inventors:
Eugene Puchalski, George Deckner, Emil F. Schneider
Abstract: 1-Chloro-3,5-difluorobenzene is chlorinated to give 4,6-difluoro-1,2,3-trichlorobenzene which in turn is nitrated and reduced to the corresponding novel aniline, 2,6-difluoro-3,4,5-trichloroaniline. Further reduction of this aniline provides 2,6-difluoroaniline with high selectivity.
Abstract: This invention relates to the process for preparing partially brominated non-condensed ring polyaromatic product. The process comprises forming a reaction mass by adding a substantially stoichiometric amount of Br.sub.2 to a mixture comprising a non-condensed ring polyaromatic, a solvent selected from a group consisting of methylene dibromide, methylene dichloride and mixtures thereof, and a catalyst selected from the group consisting of zirconium halide, iron, ferric chloride and mixtures thereof, the reaction mass being maintained at a temperature within the range of from about 10.degree. to about 50.degree. C. during at least substantially all of the addition; refluxing the reaction mass after the addition is completed or at least nearly completed; and recovering from the reaction mass the partially brominated non-condensed ring polyaromatic product.
Type:
Grant
Filed:
May 26, 1988
Date of Patent:
August 20, 1991
Assignee:
Ethyl Corporation
Inventors:
Bonnie G. McKinnie, David R. Brackenridge
Abstract: Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.
Type:
Grant
Filed:
March 19, 1990
Date of Patent:
August 13, 1991
Assignee:
Sanofi
Inventors:
Jean Gubin, Pierre Chatelain, Marcel Descamps, Dino Nisato, Henri Inion, Jean Lucchetti, Jean-Marie Mahaux, Jean-Noel Vallat
Abstract: A material for an optical component comprising polytungstic acid having peroxo groups, and an optical component, at least part of which is constituted of a thin film of the above-mentioned material. By using this material, a thin film of an inorganic material having an excellent stability is formed by the inexpensive wet painting method. An optical component using the above-mentioned thin film can be formed on an arbitrary substrate with high accuracy at a low temperature of about 100.degree. C. or below. The polytungstic acid may contain carbon as a heteroatom and/or may have Nb, Ti, V, Ta and/or Mo substituted for part of W.
Abstract: The invention concerns a 1,2-dihydro-3H-indazol-3-one derivative of formula I ##STR1## wherein Ra is hydrogen, halogeno, hydroxy, cyano, trifluoromethyl, 1-6C)alkyl or (1-6C)alkoxy;Rb is hydrogen or (1-6C)alkyl;Rc is hydrogen, (1-8C)alkyl or (3-8C)alkenyl; andY is (1-8C)alkyl, (3-8C)alkenyl or (3-8C)alkynyl, or Y is a group of the formula --A--Q in which A is (1-6C)alkylene or (3-6C)alkenylene, and Q is phenyl, naphthyl, pyridyl, thienyl, isoxazolyl, thiazolyl or thiadiazolyl, which may optionally bear one or two substituents;or a pharmaceutically-acceptable salt thereof;or a (12-4C)alkoxycarbonyl derivative thereof.The invention also concerns processes for the manufacture of an indazol-3-one of the formula I and pharmaceutical compositions containing said indazol-3-one. Also included in the invention is a method of treating various inflammatory or allergic diseases using an indazol-3-one of the formula I and the use of such a compound in the production of a new medicament for such use.
Type:
Grant
Filed:
June 30, 1989
Date of Patent:
July 30, 1991
Assignees:
ICI Pharma, Imperial Chemical Industries PLC
Abstract: Methods for treating damaged corneal, uterine or cartilage tissue comprising applying a therapeutically effective amount of a composition comprising:(a) a sterile extracellular connective tissue matrix composition comprising collagens, proteoglycans, glycosaminoglycans and glycoproteins wherein said collagens, said proteoglycans, said glycosamino glycans, and said glycoproteins have each been extracted from an extracellular connective tissue matrix and are in their native structural form and(b) a pharmaceutically acceptable carrier.
Abstract: This invention relates to (R)-.alpha.-methyl-4-halobenzenemethanamine salts of epimers of acids of the formula ##STR1## and the use of these salts to separate these epimers. These acids are leukotriene antagonists.