Abstract: This invention is a novel methods of manufacturing chalcones that includes reacting a carbon-linked heteroaryl or heterocyclic substituted benzaldehyde with an acetophenone in a solvent or mixture of solvents in the presence of LiOMe. Also provided are new chalcones for the treatment of medical conditions.
Type:
Application
Filed:
December 19, 2003
Publication date:
September 16, 2004
Inventors:
M. David Weingarten, Liming Ni, Charles Q. Meng, Kimberly J. Worsencroft, James A. Sikorski
Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
Type:
Application
Filed:
February 18, 2004
Publication date:
September 16, 2004
Applicant:
Encysive Pharmaceuticals Inc.
Inventors:
Chengde Wu, C. Eric Anderson, Huong Bui, Daxin Gao, Jamal Kassir, Wen Li, Junmei Wang, Robert V. Market
Abstract: Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.
Type:
Application
Filed:
November 10, 2003
Publication date:
August 19, 2004
Applicant:
GRUENENTHAL GmbH
Inventors:
Bernd Sundermann, Hagen-Heinrich Hennies, Werner Englberger, Babette-Yvonne Koegel
Abstract: The present invention relates to a process for preparing perfluoroalkylanilines and to their use for preparing active ingredients, in particular for agrochemicals.
Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.
Abstract: The invention provides Zn-chelating compounds that are molecularly engineered to bind to a specific target sequence in a protein of interest. The Zn2+0 ion is far less toxic and promiscuous than nickel and therefore provides an attractive alternative to Ni-based labeling systems. Invention Zn-chelating compounds also do not require oxidizable thiols and therefore can be used in non-reducing environments such as the surface of living cells. In addition, the target sequence is genetically encodable and requires incorporation of only a few amino acids, unlike fusions to fluorescent proteins such as GFP.
Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: 1
Type:
Application
Filed:
December 12, 2003
Publication date:
July 15, 2004
Applicant:
Pharmacia Corporation
Inventors:
David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
Abstract: A method of manufacturing a new N-carboxyamino acid anhydride and polyamino acid using a simple process operation.
The method for manufacturing N-carboxyamino acid anhydride comprising reacting &agr;-amino acid with di-tert-butyltricarbonate. The method for manufacturing polyamino acid comprising decarboxylating the N-carboxyamino acid anhydride obtained by reacting &agr;-amino acid with di-tert-butyltricarbonate.
Abstract: Bis-aryl diamidoxime compounds, such as 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.
Type:
Application
Filed:
November 25, 2003
Publication date:
July 1, 2004
Applicants:
University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
Inventors:
David W. Boykin, Mariappan Anbazhagan, Richard R. Tidwell
Abstract: This invention discloses a process for synthesizing an amine functionalized monomer that comprises (1) reacting a secondary amine with a 2,3-dihalopropene to produce a vinyl halide containing secondary amine having a structural formula selected from the group consisting of 1
Type:
Application
Filed:
December 9, 2003
Publication date:
June 24, 2004
Applicant:
The Goodyear Tire & Rubber Company
Inventors:
Adel Farhan Halasa, Wein-Liang Hsu, Jin-Ping Zhou, Chad Aaron Jasiunas, Corey Stanton Yon
Abstract: The present invention is directed to benzophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.
Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aminoalkyl-substituted aryl compounds of Formula I: 1
Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1):
wherein X is selected from halogen and R5SO4 where the halogen is preferably Cl, Br or I; R, R1 and R2 are each individually selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl, or two of R, R1 and R2 together with the nitrogen atom to which they are attached form a C3 to C6 saturated or unsaturated ring optionally containing in the ring one or more additional hetero atoms selected from O, S and N atoms; R3 and R 4 are each individually selected from C1 to C6 alkyl, C1 to C6 hydroxyalkyl, C1 to C6 alkoxy, C1 to C6 aminoalkyl or R3 and R4 together form a C1 to C5 alkylene group; and R5 is selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl.
Type:
Grant
Filed:
January 18, 2002
Date of Patent:
June 15, 2004
Assignee:
The Procter & Gamble Company
Inventors:
Mu-Ill Lim, Yuh-Guo Pan, Gottfried Wenke
Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
Type:
Application
Filed:
September 5, 2003
Publication date:
June 10, 2004
Inventors:
John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more 2-fluorobenzenesulfonyl compounds corresponding to Formula (I) wherein A, R1, R2, and R3 are as described in the specification, and novel 2-fluorobenzenesulfonyl compounds within Formula (I).
Type:
Application
Filed:
July 11, 2003
Publication date:
May 13, 2004
Inventors:
David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John J. Talley
Abstract: This invention provides a compound of the formula:
or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 o
Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.
Type:
Application
Filed:
October 10, 2003
Publication date:
April 22, 2004
Inventors:
Yuan-Ching P. Chiang, Gary E. Aspnes, Kimberly G. Estep
Abstract: An improved process for preparing arylethanoldiamines is described. Compounds of this type are known to be useful as agonists at a typical beta-adrenoceptors (also known as beta-3-adrenoceptors).
Type:
Application
Filed:
July 31, 2003
Publication date:
April 22, 2004
Inventors:
Jason William Beames Cooke, Bobby Neal Glover, Ronnie Maxwell Lawrence, Matthew Jude Sharp, Maria Fumiko Tymoschenko
Abstract: The invention relates to a process for carrying out a homogeneously catalyzed C—C coupling reaction between an optionally substituted (hetero)aromatic bromide compound and a second reactant, which is chosen from the group of olefins in which at least one of the substituents on the olefinic sp2 carbon atoms is a hydrogen atom, and the group of organoboron compounds with the formula Ar—B(OR1)—OR2, where Ar stands for an optionally substituted (hetero)aryl group and R1 and R2 each independently represent H or an alkyl group or, together with the O-atoms to which they are bound and the B-atom, form a ring with 2-5 C-atoms, in the presence of an aprotic dipolar solvent and a base, a palladium salt without a ligand being used as palladium catalyst and the reaction being carried out at a ratio between the quantity of palladium present in the palladium salt and the optionally substituted (hetero)aromatic bromine compound of between 0.00001 and 0.1 mol %, preferably between 0.01 and 0.1 mol %.
Type:
Application
Filed:
December 8, 2003
Publication date:
April 22, 2004
Inventors:
Andreas Hendrikus Maria De Vries, Johannes Gerardus De Vries
Abstract: The invention relates to novel pyrrolidyl-substituted para-phenylenediamine derivatives, to dye compositions containing them and to the process for dyeing keratin fibers using these compositions.
Abstract: A pyrrolidine derivative, which is an intermediate for a quinuclidine derivate side chain useful as a squalene synthase inhibitor, and producing method thereof are disclosed.
Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes.
Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: 1
Type:
Application
Filed:
June 30, 2003
Publication date:
April 1, 2004
Inventors:
Stephan Rodewald, Steven Kristofer Henning, Brian Earl Burkhart
Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Type:
Application
Filed:
March 27, 2003
Publication date:
March 11, 2004
Inventors:
Yang Gao, Alan J. Hutchison, John M. Peterson, Wallace C. Pringle, Andrew Thurkauf, Taeyoung Yoon, He Zhao
Abstract: The present invention provides a novel class of RXR modulator compounds that exhibit an improved pharmacologic profile relative to the profile of previously studied RXR modulators, including those that share common structural features with the presently claimed modulators. The present invention also provides synthetic methods for preparing these compounds as well as pharmaceutical compositions incorporating these novel compounds and methods for the therapeutic use of such compounds and pharmaceutical compositions.
Type:
Application
Filed:
May 9, 2003
Publication date:
March 11, 2004
Inventors:
Robert J. Ardecky, Marcus F. Boehm, Amy L. Faulkner, Lawrence G. Hamann, Todd K. Jones, Christopher M. Mapes, Pierre-Yves Michellys, John S. Tyhonas
Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.
Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I:
wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.
Type:
Grant
Filed:
December 13, 2002
Date of Patent:
March 2, 2004
Assignee:
Pharmacia Corporation
Inventors:
David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, 1
Type:
Application
Filed:
December 10, 2002
Publication date:
February 26, 2004
Inventors:
Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrence G. Hamann, David Green, Francis N. Ferrara
Abstract: The present invention relates to a process for the preparation of N-arylanthranilic acids, and a process for the preparation of N-aryl anthranilic esters, amides, and hydroxamic esters.
Type:
Application
Filed:
February 7, 2003
Publication date:
February 26, 2004
Inventors:
Michael Huai Gu Chen, Edward Mark Davis, Javier Magano, Thomas Norman Nanninga, Derick Dale Winkle
Abstract: A process for obtaining (nitroxymethyl)phenyl esters of salicylic acid derivatives of formula (I) wherein R1 is the OCOR3 group characterized in that it comprises the following steps: a) reaction of a halide of a salicylic acid derivative with hydroxybenzylacohol in the presence of a base: b) nutration of the obtained product in anhydrous conditions by a mixture of nitric acid with a different inorganic acid, or an organic acid, or an anhydride of one or two organic acids: c) recovery of the final product.
Abstract: The subject invention provides useful and novel calcium channel blockers based upon mibefradil. The subject invention also provides methods for synthesizing the compounds of the invention. The invention also provides methods for the control or prevention of hypertension, angina pectoris, ischemia, arrhythmias, and cardiac insufficiency in a patient by administering a compound, or composition, of the invention to an individual in need of such treatment.
Type:
Application
Filed:
August 18, 2003
Publication date:
February 19, 2004
Inventors:
Pascal Druzgala, Peter G. Milner, Jurg Pfister, Xiaoming Zhang