Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
Abstract: The invention relates to hydroxamic and carboxylic acid derivatives. Compounds of the formula:
are disclosed. These compounds are useful for the treatment of diseases mediated by inhibitors of matrix metalloproteinase, ADAM, ADAM-TS enzymes, and/or TNF&agr;-mediated diseases including degenerative diseases and certain cancers.
Type:
Grant
Filed:
September 6, 2002
Date of Patent:
May 11, 2004
Assignee:
Darwin Discovery, Ltd.
Inventors:
Duncan Batty, Verity Margaret Sabin, Robert John Watson, Hazel Joan Dyke, Andrew Sharpe, Richard John Davenport, David Alan Owen, Andrew Douglas Baxter
Abstract: An electroluminescent element is disclosed, comprising an electroluminescent material and a fluorescent substance emitting light having an emission maximum at the wavelength different from that of light emitted from the electroluminescent material upon absorption of the light emitted from the electroluminescent material. A color conversion filter is also disclosed, comprising a fluorescent substance emitting light having an emission maximum at the wavelengths of 400 to 700 nm upon absorption of the light emitted from the electroluminescent material.
Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.
Type:
Application
Filed:
June 11, 2003
Publication date:
April 8, 2004
Applicant:
SUGEN, INC.
Inventors:
Peng Cho Tang, Li Sun, Ngoc My Tran, Anh Thi Nguyen, Asaad Nematalla
Abstract: This invention relates to the use of the combined action of a compound with neurotrophic activity and a compound enhancing the dopamine activity for the treatment of Parkinson's disease.
Type:
Application
Filed:
October 23, 2003
Publication date:
April 1, 2004
Inventors:
Dan Peters, Lars Christian Ronn, Gunnar M. Olsen, Arne Moller
Abstract: The present invention is a novel pharmaceutical agent, (5R)-5-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione 1
Type:
Application
Filed:
August 5, 2003
Publication date:
February 12, 2004
Inventors:
Brad A. Acker, Richard Frederick Heier, Alan Q. Jin, Malcolm Wilson Moon
Abstract: The present invention concerns an improved optical method and optical sensing device for determining the levels of polyhydroxyl-substituted organic molecules in vitro and/or in vivo in aqueous media. In particular, a sensory devise is implemented in a mammal to determine sugar levels. Specifically, a dye is combined with a conjugated nitrogen-containing heterocyclic aromatic boronic acid-substituted bis-onium compound in the presence of a sugar, such as fructose or glucose. The viologens are preferred as the aromatic conjugated nitrogen-containing boronic acid substituted compounds. The method is useful to determine sugar levels in a human being.
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Abstract: Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed. Compounds useful as cannabinoid receptor modulators for treating respiratory and non-respiratory leukocyte-activation associated diseases comprise compounds of formula (I),
in which A and B are nitrogen or carbon, provided only one of A and B is nitrogen; and R1-R6 are as defined in the specification, wherein R2 with R5 may form a ring, and/or two R4 groups may form a six-membered aryl or heteroaryl ring, optionally having a substituent R6 forming a ring with R3.
Type:
Grant
Filed:
February 8, 2001
Date of Patent:
November 25, 2003
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Katerina Leftheris, Hong Wu, Stephen Wrobleski, Ping Chen, John Hynes, John Tokarski
Abstract:
The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.
Type:
Grant
Filed:
May 3, 2000
Date of Patent:
November 4, 2003
Assignee:
Abbott Laboratories
Inventors:
William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
Abstract: Pyridone-fused azabicyclic compounds of the formula
and their pharmaceutically acceptable salts and prodrugs, wherein R1, R2 and R3 are defined below, intermediates and methods for their preparation. Compositions and methods for using compounds of the formula I in the treatment of neurological and mental disorders related to a decrease in cholinergic function such as nicotine addiction, Huntington's Chorea, tardive dyskinesia, hyperkinesia, mania, dyslexia, schizophrenia, analgesia, attention deficit disorder (ADD), multi-infarct demetia, age related cognitive decline, epilepsy, neurological and mental disorders related to a decrease in cholinergic function, senile dementia of the Alzheimer's type, Parkinson's disease, attention deficit hyperactivity disorder (ADHD), anxiety, obesity, Tourette's Syndrome and ulcerative colitis.
Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.
Type:
Application
Filed:
November 25, 2002
Publication date:
October 2, 2003
Inventors:
Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
Abstract: The subject matter of the present invention is directed to novel substituted beta-carbolines, and specifically compounds of the formula I,
which are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of I&kgr;B kinase is involved.
Type:
Grant
Filed:
March 15, 2001
Date of Patent:
September 30, 2003
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Olaf Ritzeler, Alfredo Castro, Louis Grenier, Francois Soucy, Wayne W. Hancock, Hormoz Mazdiyashi, Vito Palombella, Julian Adams
Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis
and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is
n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.
Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.
Abstract: Methods of preparing amino-substituted-tetrahydroisoquinoline ring compounds include the steps of providing a support-bound amino-substituted-tetrahydroisoquinoline compound; forming an intermediate by reacting the support-bound amino-substituted-tetrahydroisoquinoline compound with a reagent; and cyclizatively cleaving the support-bound amino-substituted-tetrahydroisoquinoline compound to form the amino-substituted-tetrahydroisoquinoline ring compound.
Abstract: Non-steroidal compounds and compositions which are agonists, partial agonists, and antagonists for androgen receptors and methods of preparation for the non-steroidal compounds and compositions.
Type:
Application
Filed:
December 23, 2002
Publication date:
August 7, 2003
Inventors:
Lawrence G. Hamann, James Kong, James P. Edwards
Abstract: The present invention relates to tricyclic 2-pyridone compounds of formula (I):
or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Type:
Grant
Filed:
July 19, 2001
Date of Patent:
July 22, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
James D. Rodgers, Haisheng Wang, Mona Patel, Argyrios Arvanitis, Anthony J. Cocuzza
Abstract: The present invention relates to tricyclic compounds of formula (I):
or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Type:
Grant
Filed:
October 18, 2000
Date of Patent:
July 15, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Barry L. Johnson, Mona Patel, James D. Rodgers, Christine M. Tarby, Rajagopal Bakthavatchalam
Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is 0 or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.
Type:
Application
Filed:
June 20, 2002
Publication date:
July 10, 2003
Inventors:
Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
Abstract: 1-substituted, 2-substituted 1H-imidazo[4,5-c]-quinolin-4-amines are disclosed. These compounds function as antiviral agents, they induce biosynthesis of interferon, and they inhibit tumor formation in animal models. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.
Type:
Application
Filed:
September 10, 2002
Publication date:
June 26, 2003
Applicant:
3M Innovative Properties Company
Inventors:
John F. Gerster, Stephen L. Crooks, Kyle J. Lindstrom
Abstract: Novel compounds of formula (I):
wherein X1, X2, X3 and X4, n, R1, R2 and R3 are defined in the specification, and pharmaceutically acceptable salts and prodrugs of the compounds of formula (I) have therapeutic uses. These compounds are useful for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea. They are particularly useful for the treatment of obesity.
Type:
Grant
Filed:
February 27, 2001
Date of Patent:
June 24, 2003
Assignees:
Hoffman-La Roche Inc., Vernalis Research Limited
Inventors:
Jonathan Mark Bentley, Paul Hebeisen, Sven Taylor
Abstract: A pharmaceutical composition comprising an efficient amount of a compound selected among the compounds of formulae (I) and (II). The compounds have useful cytotoxic properties providing therapeutic application as antitumoral medicine.
Type:
Grant
Filed:
September 18, 2001
Date of Patent:
June 24, 2003
Assignee:
Laboratorie L. Lafon
Inventors:
Evelyne Delfourne, Nathalie Bontemps-Subielos, Francis Darro, Jean Bastide, Robert Kiss, Armand Frydman
Abstract: The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).
Type:
Application
Filed:
May 21, 2002
Publication date:
May 29, 2003
Inventors:
Rosanne Bonjouklian, Jeffrey Daniel Cohen, Joseph Michael Gruber, Douglas Webb Johnson, Louis Nickolaus Jungheim, Julian Stanley Kroin, Peter Ambrose Lander, Ho-Shen Lin, Mark Christopher Lohman, Brian Stephen Muehl, Bryan Hurst Norman, Vinod Francis Patel, Michael Enrico Richett, Kenneth Jeff Thrasher, Sreenivasarao Vepachedu, Wesley Todd White, Yongping Xie, Jeremy Schulenburg York, Brandon Lee Parkhurst
Abstract: Compounds of the formula (1), in which the substituents have the meanings mentioned in the description, are suitable for the prevention and treatment of gastrointestinal diseases.
Abstract: Sensing elements, sensor systems and methods for determining the concentration of oxygen and oxygen-related analytes in a medium are provided. The sensing element comprises a solid polymeric matrix material that is permeable to oxygen or an oxygen related analyte and an indicator that is covalently bonded to the solid polymeric matrix material. The indicator is a luminescent platinum group metal polyaromatic chelate complex capable of having its luminescence quenched by the presence of oxygen The polyaromatic complex comprises three ligands, at least one of which is a bidentate diphenylphenanthroline. The polyaromatic complex is distributed substantially homogenously throughout the matrix material and is covalently bonded to the matrix material via a linker arm. The linker arm is attached to a phenyl group of a diphenylphenanthroline ligand and to the backbone of the polymeric matrix material.
Type:
Application
Filed:
August 22, 2001
Publication date:
May 29, 2003
Inventors:
James G. Bentsen, Ralph R. Roberts, Orlin B. Knudson, Daniel Alvarez, Michael J. Rude
Abstract: Benzo[f]naphthyridine derivatives of formula (I):
benzo[f]naphthyridine derivatives and benzo[f]naphthyridine esters of formula (IVa):
aminoquinoline derivatives of formula (X):
processes for preparing such compounds; and compositions comprising them.
Type:
Grant
Filed:
December 31, 2001
Date of Patent:
May 20, 2003
Assignee:
Aventis Pharma S.A.
Inventors:
Jean-François Desconclois, Arielle Genevois-Borella, Philippe Girard, Michel Kryvenko, Marc Pierre Lavergne, Jean-Luc Malleron, Guy Picaut, Michel Tabart, Sylvie Wentzler
Abstract: The present invention relates to compounds of the general formula (I)
The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
Type:
Grant
Filed:
June 11, 2001
Date of Patent:
March 18, 2003
Assignee:
Novo Nordisk A/S
Inventors:
Lone Jeppesen, Per Sauerberg, Anthony Murray, Paul Stanley Bury
Abstract: Bis-o-aminophenols and o-aminophenolcarboxylic acids have the following structures:
A1 to A7 are, independently of each other, H, F, CH3, CF3, OCH3 or OCF3. T is an aromatic or heterocyclic residue. A method for preparing bis-o-aminophenols and o-aminophenolcarboxylic acids is also provided.
Type:
Grant
Filed:
March 12, 2001
Date of Patent:
March 11, 2003
Assignee:
Infineon Technologies AG
Inventors:
Jörg Haussmann, Gerhard Maier, Recai Sezi
Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.
Type:
Grant
Filed:
September 18, 2001
Date of Patent:
March 4, 2003
Assignee:
Schering Corporation
Inventors:
Neng-Yang Shih, Robert G. Aslanian, John J. Piwinski, Andrew T. Lupo, Jr., Adriano Afonso
Abstract: Compounds having formula (I) wherein R3, R4, R7 and R8 are independently selected from the group consisting of hydrogen, lower alkyl, halogen, amine, mono(lower)alkylamine, di(lower)alkylamine, phenyl, or substituted phenyl possess antitumor activity and are new with the exception of the compound in which R3, R4, R7, R8 are all hydrogen and the compound in which R3 and R7 are hydrogen, R4 is chlorine, and R8 is a 2-nitrophenyl group.
Type:
Grant
Filed:
July 11, 2001
Date of Patent:
February 25, 2003
Assignee:
Universidad Complutense de Madrid
Inventors:
Carmen Avendano, José María Perez, Maria del Mar Blanco, José Carlos Menendez, Dolores Garcia Gravalos, Jesús Angel de la Fuente, María Jesús Martin
Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.
Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by:
and physiologically acceptable salts thereof.
Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure:
including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, A, X, Y and Z are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
Type:
Grant
Filed:
May 18, 2001
Date of Patent:
December 31, 2002
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Mustapha Haddach, John Patrick Williams, Michael K. Schwaebe