Abstract: Photoiniferters for controlled radical polymerizations are described. The photoiniferters have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.
Type:
Application
Filed:
April 12, 2004
Publication date:
October 7, 2004
Applicant:
3M Innovative Properties Company
Inventors:
Michael S. Wendland, Kevin M. Lewandowski, Duane D. Fansler, Babu N. Gaddam, Steven M. Heilmann
Abstract: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.
Abstract: Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula:
wherein Y is a radical of Formulae II or III:
in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.
Type:
Grant
Filed:
June 6, 2003
Date of Patent:
July 6, 2004
Assignee:
University of Virginia Patent Foundation
Inventors:
Timothy L. Macdonald, Thomas A. Miller, Charles D. Thompson, Christine M. Dieckhaus
Abstract: Photoiniferters for controlled radical polymerizations are described. The photoiniferters have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.
Type:
Grant
Filed:
March 21, 2003
Date of Patent:
June 8, 2004
Assignee:
3M Innovative Properties Company
Inventors:
Michael S. Wendland, Kevin M. Lewandowski, Duane D. Fansler, Babu N. Gaddam, Steven M. Heilmann
Abstract: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.
Abstract: The present invention relates to certain substituted heterocycles, including 2-substituted thiazolidinone and 2-substituted oxazolidinone compounds. These compounds are useful in the treatment of diseases related to uncontrolled cellular proliferation, such as cancer or precancerous conditions. The compounds are also useful for modulating lipid and/or carbohydrate metabolism, and treating Type II diabetes, hyperglycemia or obesity, and for treating inflammatory diseases such as arthritis.
Type:
Application
Filed:
December 6, 2002
Publication date:
May 20, 2004
Inventors:
Magnus Pfahl, Hussien A. Al-Shamma, Andrea Fanjul Giachino, David P. M. Pleynet, Haifeng Bao, Lyle W. Spruce, Christopher N. Cow, Catherine Tachdjian, James W. Zapf, Torsten R. Wiemann
Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.
Type:
Application
Filed:
December 2, 2002
Publication date:
February 19, 2004
Inventors:
Michael J. Ricks, William H. Dent, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesei, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
Abstract: Compounds of Formula (IA) and Formula (IB) 1
Type:
Application
Filed:
March 21, 2003
Publication date:
February 5, 2004
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Younes Bekkali, Rajashehar Betageri, Mario G. Cardozo, Thomas A. Gilmore, Christian Hanke Justus Joachim Harcken, Thomas M. Kirrane, Daniel Kuzmich, John Robert Proudfoot, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell, Hossein Razavi
Abstract: The invention relates to novel compounds of formula (I) in which A, B, W, G and Het have the same designation cited in the description. The invention also relates to several methods for the production of said new compounds and the use thereof as pesticides and herbicides.
Type:
Application
Filed:
December 10, 2002
Publication date:
January 15, 2004
Inventors:
Reiner Fischer, Thomas Bretschneider, Axel Trautwein, Astrid Ullmann, Mark Wilhelm Drewes, Christoph Erdelen, Peter Dahmen, Dieter Feucht, Rolf Pontzen
Inventors:
Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
Abstract: Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.
Type:
Application
Filed:
December 20, 2002
Publication date:
November 13, 2003
Inventors:
Richard Martin, Brenton Todd Flatt, Jeffrey Dean Kahl, Tie-Lin Wang
Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.
Type:
Application
Filed:
April 1, 2003
Publication date:
October 30, 2003
Applicant:
Merck & Co., Inc.
Inventors:
Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Application
Filed:
February 26, 2002
Publication date:
October 9, 2003
Applicant:
G.D. Searle & Co.
Inventors:
Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, Joseph J. McDonald
Abstract: A description is given of substituted 3-heteroaryl(amino- or oxy)pyrrolidin-2-ones of the formula (I), processes for preparing them, and their use as herbicides or as plant growth regulators.
Type:
Application
Filed:
July 9, 2002
Publication date:
September 11, 2003
Inventors:
Guido Bojack, Lothar Willms, Alfred Angermann, Hermann Bieringer, Hubert Menne, Thomas Auler
Abstract: Disclosed are substituted heteroarylalkanoic acids acids of the following formula D-A-C(O)R′, where D, A, and R′ are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.
Type:
Application
Filed:
November 14, 2002
Publication date:
September 4, 2003
Applicant:
The Institutes for Pharmaceutical Discovery, Inc. A Corporation of the State of Delaware
Abstract: Compounds of the general formula I
where the index and the substituents have the following meanings:
n is 0 or 1 to 4;
X is O or S;
Y is a five-membered heteroaromatic ring;
R1 is nitro; cyano; halogen;
alkyl; haloalkyl; alkoxy; haloalkoxy; alkylthio;
phenyl or phenoxy;
R2 is hydrogen;
alkyl, alkenyl or alkynyl;
or a saturatedy,or unsaturated ring which, in addition to carbon atoms, can also contain hetero atoms as ring members are described.
Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.
Type:
Application
Filed:
May 13, 2002
Publication date:
August 7, 2003
Inventors:
Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Andrew Mott, Lori Sutin, Jan Tejbrant
Abstract: A peroxisome proliferator activated receptor regulator containing a compound of formula (I)
(wherein all symbols are as defined in the specification), or a salt thereof as active ingredient.
Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.
Abstract: The present invention relates to a process for preparing 5-alkoxy-substituted oxazoles, in particular for preparing 4-methyl-5-alkoxy-substituted oxazoles and also a process for preparing pyridoxine derivatives.
Type:
Application
Filed:
January 23, 2003
Publication date:
July 3, 2003
Inventors:
Harald Rust, Kirsten Burkart, Tillmann Faust, Jochem Henkelmann, Alois Kindler, Christian Knoll, Michael Becker
Abstract: An imaging member, such as a negative-working printing plate or on-press cylinder, can be prepared with a hydrophilic imaging layer comprised of a heat-sensitive hydrophilic charged polymer (ionomer) and an infrared radiation sensitive negatively-charged oxonol dye that has a &lgr;max of greater than 700 nm. The heat-sensitive polymer and IR dye can be formulated in water or water-miscible solvents to provide highly thermal sensitive imaging compositions. In the imaging member, the polymer reacts to provide increased hydrophobicity in areas exposed to energy that provides or generates heat. For example, heat can be supplied by laser irradiation in the IR region of the electromagnetic spectrum. The heat-sensitive polymer is considered “switchable” in response to heat, and provides a lithographic image without conventional alkaline processing.
Abstract: The invention provides compounds of Formula I: compounds of the Formula I:
wherein R1, R2, R4, R6, X, and W are defined herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which &agr;7 is known to be involved.
Type:
Grant
Filed:
August 14, 2002
Date of Patent:
May 13, 2003
Assignee:
Pharmacia & Upjohn Company
Inventors:
Donn G. Wishka, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, David W. Piotrowski, Jeffrey W. Corbett, Alice L. Bodnar, Vincent E. Groppi, Jr.
Abstract: Zwitterionic imide compounds are provided according to the formula: R1—SO2—N−—SO2—R2+, where R1 and R2+are any suitable groups. Typically R1 is a highly fluorinated alkane and R2+contains a quaternary ammonium group or a heteroatomic aromatic group having an cationic nitrogen, such as: pyridiniumyl, pyridaziniumyl, pyrimidiniumyl, pyraziniumyl, imidazoliumyl, pyrazoliumyl, thiazoliumyl, oxazoliumyl, or triazoliumyl. Zwitterionic liquids are provided, typically having melting points of less than 100 ° C. and typically having a solubility in water of less than 5% by weight.
Abstract: The invention relates to a process for preparing N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides in which, in a first step, 2-amino-4,5-difluoro-benzonitrile is reacted with sulphonyl halides in the presence of an acid acceptor and in the presence of a diluent at temperatures between 0° C. and 150° C. and, in a second step, the N-(2-cyano-4,5-difluoro-phenyl)-sulphonamides and/or N-(2-cyano-4,5-difluoro-phenyl)-sulphonimides obtained in the first step are as pure substances or as mixtures with ammonia in the presence of a diluent reacted at a temperature between 100° C. and 200° C. The invention furthermore relates to novel intermediates of the process.
Type:
Grant
Filed:
September 5, 2001
Date of Patent:
April 8, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Achim Hupperts, Mark Wilhelm Drewes, David Erdman, Reinhard Lantzsch
Abstract: A process for the preparation of 5-(3,5-dimethylphenoxymethyl)-2-oxazolidinone, which includes:
a) reacting 3,5-dimethylphonel with epichlorohydrin to obtain a mixture of 1-(3,5-dimethylphenoxy)2,3-epoxy propane (1) and 1-(3,5-dimethylphenoxy)-3-chloro-2-propanol (2);
b) reacting the mixture of (1) and (2) obtained from step (a) with benzylamine to obtain a first compound;
c) reducing the first compound with hydrogen in presence of ammonia, to obtain a second compound; and
d) reacting the second compound with dimethylcarbonate in the presence of a strong base to obtain 5-(3,5-dimethlphenoxymethyl)-2-oxazolidinone.
Abstract: The present invention provide compounds of Formula I
The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.
Type:
Grant
Filed:
July 23, 2001
Date of Patent:
March 4, 2003
Assignee:
Warner-Lambert Company
Inventors:
Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
Abstract: Compounds, compositions and methods are provided that are useful in the treatment of chemokine receptor-mediated conditions and diseases. In particular, the invention provides compounds which modulate CCR4 function or a CCR4-mediated response. The subject compounds and compositions are useful for the treatment or prevention of inflammatory conditions and diseases.
Type:
Application
Filed:
May 22, 2002
Publication date:
January 23, 2003
Applicant:
Tularik Inc.
Inventors:
Tassie Collins, Hossen Mahmud, Jonathan Houze, Alan Xi Huang, Julio C. Medina, Xuemei Wang, Feng Xu, Qingge Xu, Liusheng Zhu
Abstract: 3-(alk-2-ynyloxy)carbonyl-5-oxazolidine carboxylic acid and its analogs having a formula
and wherein R1 is hydrogen, aryl, heteroaryl, alkyl, alkenyl, alkynyl, R2 and R3 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, R4 is hydrogen, alkyl, alkenyl, alkynyl, aryl, substituted aryl, heteroaryl, R5 and R6 independently selected from hydrogen, alkyl, alkenyl,alkynyl, arly, heteroaryl, alkoxy, alkeyloxy, alkynyloxy, aryloxy, heteroaryloxy.
Abstract: Lactams, libraries of lactams, and an efficient method of synthesizing a lactam, including a &ggr;-lactam, in which an a-diazoacetamide of the general structure (I) is reacted under conditions promoting intramolecular C-H insertion, for example in the presence of a rhodium salt such as Rh2(OAc)4, 1
Abstract: Compounds of formula (I) in which the substituents and symbols have the meanings indicated in the description, are suitable for the control of Helicobacter bacteria.
Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like.
Type:
Application
Filed:
April 19, 2002
Publication date:
November 7, 2002
Inventors:
Lone Jeppesen, Henrik Sune Andersen, Ole Hvilsted Olsen, Luke Milburn Judge, Daniel Dale Holsworth, Farid Bakir, Frank Urban Axe, Yu Ge
Abstract: Disclosed is a 5-acylamino-2-arylazo, nitro, or nitroso-4-substituted-phenol having the structural formula I:
wherein:
R* is an arylazo, nitro, or nitroso group,
Y is a coupling-off group, and
R′ is a substituent group.
Also disclosed is a method of using the compound in a simplified process for making a photographic coupler.
Abstract: This invention relates to a process for the Heck coupling reaction where heterogeneous palladium catalysts are used to activate aryl halides for a carbon-carbon coupling with olefins in the presence a base and an aprotic solvent to produce aryl-olefin compounds. The process, in particular, provides for the use of aryl chlorides substituted with electron-withdrawing or electron-donating group for the cross coupling with olefins.
Type:
Application
Filed:
March 4, 2002
Publication date:
September 12, 2002
Inventors:
Shane W. Krska, Thorsten S. Rosner, Yongkui Sun
Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
Type:
Grant
Filed:
July 28, 1998
Date of Patent:
September 10, 2002
Assignee:
G.D. Searle & Co.
Inventors:
Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
Abstract: The present invention relates to sulphonylexazolamines of general formula (I), wherein R1, R2 represent independently from each other H, A, —(CH2)n—Ar or alkenyl with 2-6 C atoms, R1 and R2 together also represent a mononuclear saturated heterocycle with 1-2 N, O and/or S atoms, Z is H, A, CF3, NO2, Hal, OH, OA, NH2, NHA or NH2. A represents alkyl with 1-6 C atoms, Ar is Z-monosubstituted or Z-disubstituted phenyl, Hal is F, Cl, Br, or L n is 1 or 2 of the physiologically acceptable salts or solvates thereof. Said sulphonyloxazolamines are used as therapeutic active ingredients. The invention also relates to the use of sulphonyloxazolamines as therapeutic active ingredients and/or to the production of pharmaceutical preparations to combat diseases of the central nervous system. The invention further relates to a pharmaceutical preparation and the production thereof.
Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2.
The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.
Type:
Grant
Filed:
September 14, 2000
Date of Patent:
August 20, 2002
Assignee:
Pharmacia Corporation
Inventors:
John J Talley, James W Malecha, Stephen Bertenshaw, Matthew J Graneto, Jeffery Carter, Jinglin Li, Srinivasan Nagarajan, David L Brown, Donald J Rogier, Jr., Thomas D Penning, Ish K Khanna, Xiangdong Xu, Richard M Weier
Abstract: A method of preparing a reduced product by efficiently reducing an unsaturated organic compound by using, as a reducing agent, a trichlorosilane which is industrially cheaply available and is easy to handle, and a reducing agent therefor. A reduced product of an unsaturated organic compound is obtained by mixing the unsaturated organic compound and a trichlorosilane together to reduce the unsaturated organic compound in the presence of a compound that forms a silicon complex having five coordinations upon acting on the trichlorosilane such as an N-formylated product of a secondary amine having not less than 3 carbon atoms. The invention further provides a reducing agent comprising a particular silicon complex.
Abstract: Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
Type:
Grant
Filed:
April 9, 2001
Date of Patent:
June 4, 2002
Assignee:
Allergen Sales, Inc.
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.
Type:
Grant
Filed:
June 7, 1999
Date of Patent:
May 28, 2002
Assignee:
Advanced Medicine, Inc.
Inventors:
J. Kevin Judice, Deborah L. Higgins, John H. Griffin
Abstract: The present invention provides an efficient stereoselective method for manufacturing (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amine-3-yl]methyl]pyrrolidine-4-thiol or a salt thereof which is useful as an intermediate for the manufacture of carbapenem and also provides the intermediate.
A method for manufacturing which comprises the step of reacting a compound of the formula (I):
(wherein, R1 is a lower alkylsulfonyl group, an optionally substituted arylsulfonyl group or an alkylsilyl group; and R2 is a protecting group for an amino group) with a compound of the formula (II):
(wherein, R3 is a substituted or unsubstituted lower alkyl group or aryl group; X is an oxygen atom or a sulfur atom; Y is an azide group or a nitro group; and m is an integer of 2 to 5).
Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
Type:
Grant
Filed:
August 29, 2000
Date of Patent:
April 9, 2002
Assignee:
Allergan Sales, Inc.
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna