Abstract: This invention relates to novel resveratrol analogs of the formula given below; wherein R, R1, R2 and R3 are: 1. R=OH, R1=R2=R3=H; 2. R=OH, R1=Br, R2=R3=H; 3. R=R1=OH, R2=R3=H; 4. R=R1=R3=H, R2=3,4,5-trihydroxybenzoyl; 5. R=R1=H, R2=R3=3,4,5-trihydroxybenzoyl; 6. R=R1=R3=H, R2=3,4-dihydroxycinnamoyl; 7. R=R1=R3=H, R2=3,4,5-trihydroxycinnamoyl; 8. R=R1=R3=H, R2=—CH2CH2N(CH3)2; 9. R=R1=R3=H, R2=—COCH2NH2.HCl. These compounds exhibited high antioxidant properties and are useful in food industry and in cosmetics. The compounds may be used in pharmaceutical composition as an antioxidant or free radical scavenger.
Abstract: This invention relates to novel {overscore (&ohgr;)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.
Type:
Application
Filed:
October 27, 2003
Publication date:
September 30, 2004
Applicant:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Abstract: New aromatic diamine derivatives and the preparation thereof are disclosed. The diamine derivatives of the present invention can be added to conventional polymerization reactions of tetracarboxylic acids or dianhydrides thereof and diamines to form new polyamic acids. After high-temperature baking, the polyamic acids are cyclized to form polyimides. These polyimides can be used as alignment film materials for liquid crystal display cell and have good alignment property and stability, and are effective in promoting pre-tilt angles.
Abstract: Described are cyclobexylamine derivatives of Formula I, Formula II, or Formula III and their pharmaceutically acceptable salts thereof:
The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are described in the specification.
Type:
Grant
Filed:
December 2, 2002
Date of Patent:
July 20, 2004
Assignee:
Warner-Lambert Company
Inventors:
Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
Abstract: Compounds of formula I:
wherein A, B, D, and R are as defined herein and their agriculturally acceptable salts are disclosed as effective insecticides. In addition, compositions comprising an insecticidally effective amount of a compound of Formula I in admixture with at least one agriculturally acceptable extender or adjuvant and methods of controlling insects comprising applying said compositions to locus on crops where control is desired are disclosed. It is emphasized that this abstract is provided to comply with the rules requiring an abstract that will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the claims (see 37 C.F.R. 1.72(b)).
Type:
Grant
Filed:
August 29, 2001
Date of Patent:
June 22, 2004
Assignee:
FMC Corporation
Inventors:
George Theodoridis, Edward Barron, Daniel H. Cohen, Ellen M. Crawford, Thomas G. Cullen, Hongyan Qi, Elizabeth Rowley, Syed F. Ali, Walter H. Yeager, Christina B. Duggan
Abstract: The present invention relates to the use of a compound having the formula I, wherein R1 are independently hydrogen or a C1-C4 straight or branched alkyl group, which may be substituted with one or more halogen and/or C1-C4 alkyloxy groups, R2 is a C1-C3 hydrocarbyl group, R3 is a C1-C4 straight or branched alkyl group, which may be substituted by one or more C1-C4 alkyloxy groups and/or halogen groups, or R3 is a phenyl group, or a benzyl group, which may be substituted with one or more C1-C4 straight or branched alkyl group, (ethyl, propyl, trimethyl) and/or C1-C4 alkyloxy groups and/or halogen groups, or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical composition for treating tinnitus. The invention also relates to a pharmaceutical composition comprising the compounds and a method for treating tinnitus by administrating the compounds.
Abstract: Disclosed are multibinding compounds which are &bgr;2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
Abstract: An improved and industrially advantageous process for the preparation of the antidepressant fluoxetine and its pharmaceutically acceptable salts, preferably hydrochloride.
Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).
Type:
Grant
Filed:
January 15, 2002
Date of Patent:
November 11, 2003
Assignee:
Theravance, Inc.
Inventors:
Seok-Ki Choi, Paul R. Fatheree, David C. Green, Daniel Marquess
Abstract: The present invention relates to an improved process for preparing 4-(6-bromohexyloxy)-butylbenzene by reacting 4-phenylbutanol with 1,6-dibromohexane in the presence of a base and a phase transfer catalyst, wherein 4-phenylbutanol in a diluent is metered into a mixture consisting of 1,6-dibromohexane, a base, a phase transfer catalyst and a diluent, and the use of the 4-(6-bromohexyloxy)-butylbenzene thus prepared for producing salmeterol in a method known per se.
Type:
Application
Filed:
March 4, 2003
Publication date:
September 11, 2003
Applicant:
Boehringer Ingelheim Pharma GmbH & Co. KG
Abstract: The invention relates to novel diaryl naphthyl methane compounds having general formula I as shown herein below, and said compounds useful in the treatment of esterogen related disease or syndrome,
Pharmaceutical compositions comprising said novel methane derivatives, process for the preparation of the novel methane derivatives and methods for the treatment of esterogen related diseases or syndrome.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
August 26, 2003
Assignee:
Council of Scientific and Industrial Research
Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides naphthalene compounds, intermediates, formulations, and methods.
Type:
Grant
Filed:
August 26, 1997
Date of Patent:
July 29, 2003
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.
Abstract: Compounds of formula (Ia) as potent, &bgr;1-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3′,4′-dimethoxyphenyl.
Type:
Application
Filed:
September 21, 1999
Publication date:
May 29, 2003
Inventors:
WILLIAM JOHN LOUIS, GRAHAM PAUL JACKMAN, DIMITRIOS IAKOVIDIS, SIMON NICHOLAS STEWART LOUIS, OLAF HEINO DRUMMER
Abstract: An improved light attenuating compound for use in the production of microdevices is provided. Broadly, the light attenuating compound is difunctional and can be directly incorporated (either physically or chemically) into photolithographic compositions such as anti-reflective coatings (ARC) and contact or via hole fill materials. The preferred light attenuating compound comprises functional groups electronically isolated from the light absorbing moieties of the compound. As a result, the spectral properties of the compound are not negatively affected when the functional groups form bonds with other compounds during polymerization or crosslinking.
Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
Abstract: The present invention provides processes for the preparation of 3-aryloxy-3-arylpropylamines and intermediates thereof using an nucleophilic aromatic displacement in 1,3-dimethyl-2-imidazolidinone or N-methylpyrrolidinone.
Type:
Grant
Filed:
September 12, 2001
Date of Patent:
April 1, 2003
Assignee:
Eli Lilly and Company
Inventors:
Douglas Patton Kjell, Kurt Thomas Lorenz
Abstract: 1,4-diaminonaphthalene and/or 1,5-diaminonaphthalene are produced by (a) reacting naphthalene with a halogen, (b) optionally, separating 1,4-dihalogen naphthalene or 1,5-dihalogen naphthalene from the mixture from step (a), and (c) reacting the mixture from step (a) or the 1,4-dihalogen naphthalene or the 1,5-dihalogen naphthalene from step (b) with ammonia and/or an organic amine in the presence of a catalyst.
Type:
Grant
Filed:
May 3, 2002
Date of Patent:
March 25, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Joachim Zechlin, Lothar Duda, Gerhard Wegener, Andreas Hoffmann, Bodo Temme
Abstract: Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst, wherein the catalytically active mass of the catalyst contains, after its preparation and before the treatment with hydrogen,
22 to 45% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2,
1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO,
5 to 50% by weight of oxygen-containing compounds of nickel, calculated as NiO, where the molar ratio of nickel to copper is greater than 1,
5 to 50% by weight of oxygen-containing compounds of cobalt, calculated as CoO,
0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and 0 to 10% by weight of oxygen-containing compounds of aluminum and/or manganese, calculated as Al2O3 or MnO2.
Type:
Grant
Filed:
December 5, 2000
Date of Patent:
February 25, 2003
Assignee:
BASF Aktiengesellschaft
Inventors:
Jan Nouwen, Arthur Höhn, Horst Neuhauser, Frank Funke, Stephan Andreas Schunk, Johann-Peter Melder, Knut Eger, Michael Hesse, Joachim Wulff-Döring
Abstract: Molecules demonstrating anti-proliferative effects against epithelial cancer cell lines, human estrogen-dependent cancer cells and endothelial cells are disclosed. The molecules are intended for use in therapeutic preparations for the treatment of various cancers. The compounds specified are 1,2-diphenyl-1-naphthyl ethene derivatives.
Type:
Application
Filed:
August 21, 2001
Publication date:
October 10, 2002
Inventors:
Jonathan Martin Schmidt, Julie Mercure, Shuguang Zhu, John Whelan, Natalie Lazarowych
Abstract: Improved processes for preparation of high enantiomeric purity compounds center on resolution using simulated moving bed chromatography of a racemic precursor early in the synthesis. Resolution is effected with high enantiomeric purity, and subsequent reactions of the desired enantiomer performed with high optical specificity to maintain enantiomeric purity. The undesired enantiomer is racemized and recycled to the resolution phase to avoid loss.
Abstract: The present patent application relates to new substituted 3-phenoxy- or 3-phenylalkyloxy-2-phenyl-propylamines of general formula 1, processes for preparing them and their use as pharmaceutical compositions.
Type:
Grant
Filed:
February 18, 2000
Date of Patent:
August 27, 2002
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Werner Stransky, Matthias Grauert, Adrian Carter, Thomas Weiser, Wolf-Dietrich Bechtel, Helmut Ensinger, Ralf Richard H. Lotz, Rainer Palluk, Uwe Pschorn
Abstract: The present invention relates to novel 3-alkoxybenzylamine derivatives of general formula (1):
which are useful as medicinal products and in particular as antipsychotic agents.
Abstract: It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
Type:
Application
Filed:
April 11, 2001
Publication date:
February 7, 2002
Inventors:
Jayraz Luchoomun, Charles Q. Meng, Uday Saxena
Abstract: Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided.
[in the formula (1, R1 represents a C1-5 alkyl group which may be halogenated, R2 represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3 represents oxygen atom or a methylene group which may be substituted by a C1-4 alkyl group; and R4 represents 1-or 2 naphthyl group or a phenyl group which may be substituted.
Abstract: The present invention provides novel amorphous fluoxetine hydrochloride as a useful intermediate for the preparation of Form A of fluoxetine hydrochloride.
Type:
Grant
Filed:
January 31, 2001
Date of Patent:
October 30, 2001
Inventors:
Grayson Walker Stowell, Robert R. Whittle
Abstract: Fluorine-containing phenethylamines are obtained in an advantageous manner by reacting fluorine-containing bromobenzenes with acrylamide in the presence of a palladium catalyst, hydrogenating the resulting arylacrylamides catalytically and then rearranging the arylamides obtained. The invention also embraces novel arylacrylamides and novel arylamides.
Abstract: Compounds of formula (I)
wherein R, R′, R″, R1, R2, R3, R4, R5, R6, X, Y, m, n, and p have the meanings reported in the description; and their pharmaceutically acceptable salts are described.
Type:
Grant
Filed:
August 12, 1999
Date of Patent:
May 15, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Stefania Montanari, Paolo Cavalleri, Francesco Santangelo, Cristina Fraire, Giancarlo Grancini, Napoletano Mauro, Francesco Marchini, Lorenzo Pradella, Claudio Semeraro
Abstract: Improved processes for preparation of the (S)-oxetines in high enantiomeric purity centers on resolution using simulated moving bed chromatography of a racemic precursor early in the oxetine synthesis. Resolution is effected with high enantiomeric purity, and subsequent reactions of the desired enantiomer performed with high optical specificity to maintain enantiomeric purity. The undesired enantiomer may be racemized and recycled to the resolution phase to avoid loss.
Abstract: The invention relates to novel bis-o-aminophenols, and bis-o-aminothiophenols of the following structure: ##STR1## where A.sup.1 to A.sup.6 are--independently of one another--H, F, CH.sub.3, CF.sub.3, OCH.sub.3, OCF.sub.3, CH.sub.2 CH.sub.3, CF.sub.2 CF.sub.3, OCH.sub.2 CH.sub.3 or OCF.sub.2 CF.sub.3, where at least one of the radicals A.sup.1 to A.sup.6 must be F or an F-containing group; T is O or S, and m is 0 or 1; and Z is a carbocyclic or heterocyclic aromatic radical.
Abstract: This invention relates to compounds represented by the following formula (1): ##STR1## wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a substituted or unsubstituted phenylene group, R.sup.3 represents a substituted or unsubstituted phenyl group or an aliphatic hydrocarbon group containing at least four .pi. electrons, R.sup.4 represents an alkyl group having 1 to 4 carbon atoms, and m and n individually represent integers of from 1 to 4, or salts thereof, and also to compositions containing the same. These compounds have antifungal activities and are useful as drugs.
Abstract: The present invention relates to new phenylethylamine derivatives, processes for preparing them and their use as pharmaceutical compositions.
Type:
Grant
Filed:
July 29, 1999
Date of Patent:
October 17, 2000
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Ralf Anderskewitz, Franz Birke, Hans M. Jennewein
Abstract: This invention concerns a fuel additive comprising an etheramine alkoxylate, and fuel compositions and additive concentrates made therefrom. The etheramine alkoxylate may be of formula: ##STR1## where R.sup.1 is a straight or branched alkyl, or alkylaryl; R.sup.2 is independently in each occurrence hydrogen or alkyl from 1 to 6 carbons; R.sup.3 is independently in each occurrence hydrogen or alkyl of from 1 to 6 carbons; m averages from about 2 to about 20; and x and y each independently average from about 0 to 2, where x+y averages from about 1 to about 4.
Type:
Grant
Filed:
June 26, 1998
Date of Patent:
May 16, 2000
Assignee:
Huntsman Petrochemical Corporation
Inventors:
John M. Larkin, Wei-Yang Su, Terry L. Renken
Abstract: Amines are prepared from primary or secondary alcohols and nitrogen compounds selected from the group of ammonia, primary and secondary amines, at from 80 to 250.degree. C. under pressures from 0.1 to 40 MPa with hydrogen in the presence of a catalyst comprising zirconium, copper and nickel, wherein the catalytically active composition comprises20-85% by weight of oxygen-containing zirconium compounds, calculated as ZrO.sub.2,1-30% by weight of oxygen-containing copper compounds, calculated as CuO,14-70% by weight of oxygen-containing nickel compounds, calculated as NiO, where the molar ratio of nickel to copper is greater than 1,0-10% by weight of oxygen-containing aluminum and/or manganese compounds, calculated as Al.sub.2 O.sub.3 and/or MnO.sub.2,and no oxygen-containing cobalt or molybdenum compounds.
Type:
Grant
Filed:
September 23, 1998
Date of Patent:
May 2, 2000
Assignee:
BASF Aktiengesellschaft
Inventors:
Joachim Wulff-Doring, Michael Hesse, Johann-Peter Melder, Philipp Buskens, Guido Voit, Frank Funke
Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.
Abstract: A synthesis of fluoxetine is disclosed. The process begins with a lower alkyl ester of 3-benzoylpropionic acid, which is reduced in the presence of a chiral ligand to produce the corresponding .gamma.-hydroxy ester, and the ester is cleaved. The free acid is then condensed with the alcohol to form a .gamma.-lactone, which is treated with ammonia to provide the .gamma.-hydroxy amide. The amide undergoes a Hoffman rearrangement to provide a 2-oxo-1,3 oxazine, which is reduced to 3-(methylamino)-1-phenyl-1-propanol. The alcohol is deprotonated and reacted with a 4-chloro- or 4-fluoro benzotrifluoride to provide fluoxetine free base.
Type:
Grant
Filed:
May 24, 1999
Date of Patent:
February 22, 2000
Assignee:
Sepracor Inc.
Inventors:
James Wallace Hilborn, Alex Roger Jurgens, Chris Hugh Senanayake
Abstract: A simple and inexpensive process is described for reducing the concentration of N-nitroso-containing compounds in compositions comprising N-nitroso-containing compounds and other desired compounds wherein the N-nitroso-containing compounds thermally decompose at a temperature below the decomposition temperature of the desired compounds. For compositions comprising dinitroaniline herbicides wherein the N-nitroso compound is a N-nitroso derivative of a precursor in the manufacture of the herbicide, for example Flumetralin, N-ethyl-N-(2-chloro-6-fluorobenzyl)-2,6-dinitro-4-trifluoromethylaniline, the process requires heating the mixture to a temperature greater than about 120.degree. C., and holding the composition at that temperature for a time effective to decompose the N-nitroso compound present in the mixture. Volatile decomposition products are advantageously removed from the composition.
Type:
Grant
Filed:
May 10, 1999
Date of Patent:
January 25, 2000
Assignee:
SRM Chemical, Ltd, Co.
Inventors:
Lowell J. Lawrence, Stephan Kwiatkowski