Acridines (including Hydrogenated) Patents (Class 514/297)
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Patent number: 7205311Abstract: This invention pertains to certain acridone and acridine compounds of the formula which inhibit telomerase, regulate cell proliferation, etc., and/or treat cancer, proliferative conditions, etc.Type: GrantFiled: January 14, 2003Date of Patent: April 17, 2007Assignee: Cancer Research Technology LimitedInventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
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Patent number: 7160896Abstract: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ?O, L is —H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula —N(RN)Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable salType: GrantFiled: July 6, 2001Date of Patent: January 9, 2007Assignee: Cancer Research Technology LimitedInventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reskza
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Patent number: 7141581Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: August 12, 2003Date of Patent: November 28, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven Bender, Dana Hu-Lowe, David Ray Shalinsky
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Patent number: 7094378Abstract: Methods and apparatuses for treating fluids to inactivate microorganisms which may be present therein, said fluid containing one or more components selected from the group consisting of protein, blood and blood constituents are provided. The methods comprise adjusting the percentage of plasma in said fluid to a desired value; mixing an inactivation-effective, substantially non-toxic amount of an endogenous photosensitizer or endogenously-based derivative photosensitizer to said fluid; exposing said fluid to photoradiation of sufficient wavelength and energy to activate the photosensitizer, whereby said microorganisms are inactivated.Type: GrantFiled: June 15, 2000Date of Patent: August 22, 2006Assignee: Gambro, Inc.Inventors: Raymond Paul Goodrich, Jr., Dennis Hlavinka
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Patent number: 7084106Abstract: The present invention provides a novel treatment for senile dementia (Alzheimer's Type), comprising administering an anti-complement protein to a patient in need of such treatment in an amount sufficient to inhibit the complement cascade and thereby inhibit the production or enlargement of amyloid plaques in the brain of the patient. The present invention further provides pharmaceutical compositions comprising anti-complement protein, or derivatives thereof, and/or pharmaceutically acceptable salts thereof in a variety of unique pharmaceutical dosage forms.Type: GrantFiled: January 19, 2000Date of Patent: August 1, 2006Assignee: University of Louisville Research Foundation, Inc.Inventors: Girish J. Kotwal, James Daly, IV
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Patent number: 7060711Abstract: The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament and for the manufacture of a medicament for treatment of a disease state which can be alleviated by treatment with a 5-HT2B antagonist.Type: GrantFiled: October 25, 2002Date of Patent: June 13, 2006Assignee: Biofrontera Bioscience GmbHInventors: Hermann Lubbert, Christoph Ullmer, Emile Bellott, Mark Froimowitz, Douglas Gordon
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Patent number: 7041674Abstract: A compound of formula 1 wherein X?, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in pharmaceutical compositions, and methods of treating patients using them.Type: GrantFiled: November 20, 2003Date of Patent: May 9, 2006Assignee: Boehringer Ingelhiem Pharma GmbH & Co. KGInventors: Steffen Breitfelder, Matthias Hoffmann, Matthias Grauert, Michael P. Pieper, Georg Speck
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Patent number: 7030132Abstract: A method for increasing the systemic exposure of cells selected from tumor cells and normal cells to an orally administered pharmaceutically active compound, wherein a bioenhancer comprising an inhibitor of BCRP is orally administered concomitantly with said orally administered pharmaceutically active compound, and in which method the inhibitor is administered simultaneously with the pharmaceutical compound.Type: GrantFiled: November 19, 2001Date of Patent: April 18, 2006Assignee: Cancer Research Ventures LimitedInventors: Johannes Henricus Matthias Schellens, Alfred Hermanus Schinkel
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Patent number: 7030133Abstract: The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become disturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.Type: GrantFiled: February 5, 2003Date of Patent: April 18, 2006Assignee: City of HopeInventors: Samuel Rahbar, Iraj Lalezari
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Patent number: 7019015Abstract: A fungicidal composition and method of treating plant diseases using a compound of the formula I.Type: GrantFiled: September 2, 2004Date of Patent: March 28, 2006Assignee: Valent BioSciences, Inc.Inventors: Daniel F. Heiman, Peter D. Petracek, Judith A. Fugiel, Prem Warrior
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Patent number: 7012145Abstract: Process for preparing 3-[(4S)-5-oxo-2-(trifluoromethyl)-1,4,5,6,7,8-hexahydroquinolin-4-yl]benzonitrile, pharmaceutical compositions containing the compound and methods of treatment using the same.Type: GrantFiled: January 23, 2003Date of Patent: March 14, 2006Assignee: Astrazeneca ABInventors: Andrew Jones, Jonathan Moseley, Ian Patel, Evan Snape, Maureen Young
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Patent number: 6998405Abstract: Compounds of the general formula I wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/heteroaromatic, and wherein X is —(CH2)m—, in which m is an integer 1–3, to form a ring E or, when E is absent, a group R1 bound to the nitrogen atom, wherein R1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e.Type: GrantFiled: December 18, 2003Date of Patent: February 14, 2006Assignee: H. Lundbeck A/SInventors: Håkan Wikström, Durk Dijkstra, Bastiaan Johan Venhuis
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Patent number: 6974821Abstract: The invention provides methods for treating neuropsychiatric disorders such as schizophrenia, Alzheimer's Disease, autism, depression, benign forgetfulness, childhood learning disorders, closed head injury, and attention deficit disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) a therapeutically effective amount of D-alanine (or a modified form thereof), provided that the composition is substantially free of D-cycloserine, and/or (ii) D-serine (or a modified form thereof), and/or (iii) 105 to 500 mg of D-cycloserine (or a modified form thereof), and/or (iv) N-methylglycine (or a modified form thereof).Type: GrantFiled: September 23, 2003Date of Patent: December 13, 2005Assignee: The General Hospital CorporationInventors: Guochuan Tsai, Joseph Coyle
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Patent number: 6956043Abstract: A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.Type: GrantFiled: June 4, 2003Date of Patent: October 18, 2005Assignee: Novartis AGInventors: Patrice Guitard, Barbara Haeberlin, Rainer Link, Friedrich Richter
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Patent number: 6906081Abstract: This invention relates to a method of treating cognition deficit disorders comprising administering to a mammal in need of such treatment an effective amount of a dual histamine H3 receptor antagonist/m2 muscarinic antagonist, or a combination of a histamine H3 receptor antagonist and a m2 muscarinic antagonist.Type: GrantFiled: February 6, 2002Date of Patent: June 14, 2005Assignee: Schering CorporationInventors: John A. Hey, Robert G. Aslanian
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Patent number: 6884802Abstract: Compounds of formula 1, in which Het is an unsubstituted or R6- and/or R7-substituted pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrimidinyl, pyrazinyl or pyradazinyl radical, or an unsubstituted or R6- and/or R7-substituted fused bi- or tricyclic ring system comprising at least one aromatic ring and up to 4 heteroatoms-selected from the group consisting of O (oxygen), S (sulfur), N (nitrogen)- which is bonded to the phenanthridinyl radical via one of the rings comprising one or more heteroatoms, are active PDE4 inhibitors.Type: GrantFiled: July 7, 2001Date of Patent: April 26, 2005Assignee: ALTANA Pharma AGInventor: Beate Schmidt
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Patent number: 6869974Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.Type: GrantFiled: April 11, 2000Date of Patent: March 22, 2005Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6867197Abstract: The present invention relates to genetic mutations in mitochondrial cytochrome c oxidase genes that segregate with Alzheimer's disease (AD). The invention provides methods for detecting such mutations, as a diagnostic for Alzheimer's Disease, either before or after the onset of clinical symptoms. The invention further provides treatment of cytochrome c oxidase dysfunction.Type: GrantFiled: November 23, 1999Date of Patent: March 15, 2005Assignee: MitokorInventors: Robert E. Davis, Soumitra S. Ghosh, John S. Kiely
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Patent number: 6831086Abstract: The invention relates to the use of acridine or acridine derivatives, preferably in combination with benzalkonium chloride, for the inactivation of enveloped or nonenveloped viruses. The process according to the invention is preferably carried out in the presence of proteins whose biological activity is substantially retained.Type: GrantFiled: December 7, 1995Date of Patent: December 14, 2004Assignee: ZLB Behring GmbHInventor: Dieter Bernhardt
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Publication number: 20040235884Abstract: An agent for prophylaxis or therapy of cholinergic nerve disorder, which contains, as an active ingredient, a pharmaceutical agent capable of increasing the choline transporter number on the cell membrane surface of cholinergic nerve terminal or a pharmaceutical agent capable of increasing the choline transporter number on the cell membrane surface by acting on intracellular localized changes of the choline transporters.Type: ApplicationFiled: March 2, 2004Publication date: November 25, 2004Inventors: Ken Takashina, Tomoko Bessho
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Patent number: 6821983Abstract: This invention relates to 9-anilinoacridine compounds, and more particularly to their synthesis and their use in pharmaceutical compositions for treating diseases.Type: GrantFiled: July 30, 2003Date of Patent: November 23, 2004Assignee: Academia SinicaInventors: Tsann-Long Su, Jang-Yang Chang, Ting-Chao Chou
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Publication number: 20040229899Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: January 6, 2004Publication date: November 18, 2004Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20040229898Abstract: The invention is drawn to compositions and methods for inhibiting and treating malformed forms of proteins causing neurodegenerative disease, such as protease resistant prion proteins (PrPSc) and those associated with transmissible spongiform encephalopathies (TSEs). Bis-acridines are characterized by a dimeric motif, comprising two acridine heterocycles tethered by a linker. A library of bis-(6-chloro-2-methoxy-acridin-9-yl) and bis-(7-chloro-2-methoxy-benzo[b][1,5]naphthyridin-10-yl) analogs were synthesized to explore the effect of structurally diverse linkers on PrPSc replication in ScN2a cells. Structure-activity analysis revealed that linker length and structure effect inhibition of prion replication in cultured, scrapied cells.Type: ApplicationFiled: November 25, 2003Publication date: November 18, 2004Applicant: The Regents of the University of CaliforniaInventors: Stanley B. Prusiner, Carsten Korth, Barnaby C.H. May
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Patent number: 6803373Abstract: A combination of 9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7,-dimethoxy-2-isoquinolinyl)ethyl]pheny]-4-acridinecarboxamide or a salt thereof and paclitaxel and its analogs or derivatives.Type: GrantFiled: September 3, 2002Date of Patent: October 12, 2004Assignee: SmithKline Beecham CorporationInventor: Jan H. M. Schellens
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Publication number: 20040198765Abstract: This invention relates to 9-anilinoacridine compounds, and more particularly to their synthesis and their use in pharmaceutical compositions for treating diseases.Type: ApplicationFiled: July 30, 2003Publication date: October 7, 2004Inventors: Tsann-Long Su, Jang-Yang Chang, Ting-Chao Chou
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Publication number: 20040192717Abstract: This invention relates to salts of guanidine derivatives of formula R—X—C(═NH)NH3+Z−, wherein X represents a valence bond, —CH2—NH—, —CH2—NH—NH— or —CH═N—NH—; R represents a linear or branched C1-C30 alkyl, C3-C20 cycloalkyl, adamantyl, norbornyl, tricyclodecyl, benzyl, furyl, pyridyl, anthracyl, naphthyl, phenanthryl, perinaphthyl or quinuclidinyl residue, which can be substituted by one or more hydroxyl groups, C1-C4 alkoxy groups, C1-C4 alkyl groups and/or one or more halogen atoms or one or more amino groups; Z represents O—CO—Y, O—S(O)2—Y, or O—P(O)(OH)—Y; and Y represents a linear or branched C1-C12 alkyl, C3-C8 cycloalkyl, benzyl, furyl or pyridyl residue, which can be substituted by one or more hydroxyl groups, carboxylic acid groups, C1-C4 alkoxy groups, C1-C4 alkyl groups and/or one or more halogen atoms or one or more amino groups.Type: ApplicationFiled: April 8, 2004Publication date: September 30, 2004Inventor: Eberhard Amtmann
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Publication number: 20040138220Abstract: The present invention relates to compounds of the formula I, 1Type: ApplicationFiled: December 23, 2003Publication date: July 15, 2004Applicants: Pfizer, Inc., Pfizer Products, Inc.Inventor: Spiros Liras
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Publication number: 20040132747Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: ApplicationFiled: December 19, 2003Publication date: July 8, 2004Inventors: Peter Emig, Eckhard Gunther, Jurgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Publication number: 20040116457Abstract: Agents for improving excretory potency of the urinary bladder which comprises an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action.Type: ApplicationFiled: December 4, 2003Publication date: June 17, 2004Inventors: Yuji Ishihara, Takayuki Doi, Hiroshi Nagabukuro, Yuji Ishichi
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Publication number: 20040116407Abstract: The invention features a method for treating a patient having a cancer or other neoplasm by administering to the patient two compounds simultaneously or within 14 days of each other in amounts sufficient to treat the patient.Type: ApplicationFiled: July 11, 2003Publication date: June 17, 2004Inventors: Alexis Borisy, Curtis Keith, Michael A. Foley, Brent R. Stockwell, Debra A. Gaw, M. James Nichols, Margaret S. Lee
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Publication number: 20040110784Abstract: The present invention provides a therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia comprising, as an active ingredient, a tricyclic compound represented by formula (I): 1Type: ApplicationFiled: September 22, 2003Publication date: June 10, 2004Inventors: Tsuyoshi Yamagata, Kaoru Atsuki, Tetsuji Ohno, Shiro Sirakura, Akira Karasawa
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Publication number: 20040082601Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: October 21, 2003Publication date: April 29, 2004Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Publication number: 20040053955Abstract: Compounds having the formula (I), 1Type: ApplicationFiled: December 20, 2002Publication date: March 18, 2004Inventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
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Patent number: 6706722Abstract: The invention relates to novel acridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: July 20, 2001Date of Patent: March 16, 2004Assignee: Zentaris AGInventors: Peter Emig, Eckhard Günther, Bernd Nickel, Gerhard Bacher, Silke Baasner, Thomas Beckers, Beate Aue
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Publication number: 20040044023Abstract: The present invention relates to pharmaceutical compositions for treatment or prevention of memory impairment which comprise a cholinesterase inhibitor and at least one other pharmacologically active agent selected from HMG-CoA reductase inhibitors, cholesterol absorption inhibitors, gamma or beta secretase inhibitors, NMDA antagonists, muscarinic receptor agonists and nicotinic receptor agonists. Additionally, the present invention relates to the use of these pharmaceutical compositions to treat or prevent memory impairment in a mammal, such as a human.Type: ApplicationFiled: August 30, 2002Publication date: March 4, 2004Inventor: Marc Cantillon
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Publication number: 20040039005Abstract: This invention concerns the use of compounds of formula 1Type: ApplicationFiled: August 5, 2003Publication date: February 26, 2004Inventors: Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6683087Abstract: Compounds of the general formula I and salts thereof with pharmaceutically acceptable acids or bases are disclosed as well as the use of such compounds for the manufacturing of pharmaceutical compositions for the treatment of Parkinson's disease, psychoses, Huntington's disease, impotence, renal failure, heart failure or hypertension. Pharmaceutical compositions and methods of treating Parkinson's disease and schizophrenia are also disclosed.Type: GrantFiled: October 18, 2002Date of Patent: January 27, 2004Assignee: Axon Biochemicals B.V.Inventors: Håkan Wikström, Durk Dijkstra, Bastiaan Johan Venhuis
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4-Quinolinol derivatives and agrohorticultural bactericides containing the same as active ingredient
Patent number: 6680282Abstract: A new agricultural and horticultural fungicide having an excellent control effect is provided. 4-Quinolinol derivatives represented by the following formula: or agriculturally and horticulturally acceptable acid addition salts thereof.Type: GrantFiled: March 21, 2000Date of Patent: January 20, 2004Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kazumi Yamamoto, Takeshi Teraoka, Michiaki Iwata, Keiichi Imamura, Hiroshi Kurihara, Norio Sasaki, Yoshihiro Usui, Nobumitsu Sawai -
Publication number: 20040006074Abstract: Certain derivatives of acridones and benzothiadiazines have been found to have anti-cancer properties by virtue of their specific inhibition of the cyclin D dependent kinase CDK4. These molecules inhibit CDK4 activity more than they inhibit the activity of other such kinases (e.g. CDC2 and CDK2). This specificity results in an improved therapeutic index when used as drugs to treat susceptible cancers.Type: ApplicationFiled: December 2, 2002Publication date: January 8, 2004Applicant: The Government of the United States of AmericaInventors: Michael J. Kelley, Kazuhiko Nakagawa, Barry Roy Dent
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Publication number: 20030235609Abstract: There is provided a method of reducing insulin resistance in a mammalian subject comprising administering a suitable acetylcholine esterase antagonistType: ApplicationFiled: January 24, 2003Publication date: December 25, 2003Inventor: Wilfred Wayne Lautt
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Publication number: 20030229073Abstract: The present invention provides a compound of the formula (I) and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. In said formula, X=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Y=O, (CH2)m, S, SO, SO2, NH, NR8; Z=NH, O, NR8, S, SO, SO2. The remaining substituents are described in the specification.Type: ApplicationFiled: July 5, 2002Publication date: December 11, 2003Inventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
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Publication number: 20030225031Abstract: Methods and compositions are disclosed that provide acetylcholinesterase inhibitors for the prevention and treatment of diseases and disorders of the central nervous system, including dementia such as Alzheimer's disease, to the central nervous system via intranasal delivery. The methods and compositions of the present invention provide therapeutic concentrations of the acetylcholinesterase inhibitor in the cerebrospinal fluid of a mammal without the attendant disadvantages, risks and side effects of oral or injection delivery.Type: ApplicationFiled: May 15, 2003Publication date: December 4, 2003Inventor: Steven C. Quay
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Publication number: 20030220362Abstract: The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become disturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.Type: ApplicationFiled: February 5, 2003Publication date: November 27, 2003Inventors: Samuel Rahbar, Iraj Lalezari
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Publication number: 20030207909Abstract: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent.Type: ApplicationFiled: April 4, 2003Publication date: November 6, 2003Inventors: Stephen Neidle, Richard John Harrison, Llyod Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
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Patent number: 6642222Abstract: 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: GrantFiled: May 3, 2000Date of Patent: November 4, 2003Assignee: Abbott LaboratoriesInventors: William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
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Publication number: 20030199489Abstract: The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.Type: ApplicationFiled: November 1, 2002Publication date: October 23, 2003Applicant: The Regents of the University of MichiganInventor: Shaomeng Wang
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Publication number: 20030199473Abstract: This invention concerns the compounds of formula 1Type: ApplicationFiled: March 26, 2003Publication date: October 23, 2003Applicant: Janssen Pharmaceutica N.V.Inventors: Paul A.J. Janssen, Jan Heeres, Henri E.L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
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Publication number: 20030194433Abstract: Antimicrobial compositions containing a singlet oxygen-generating agent and a lubricant exhibit very effective antimicrobial activity against a variety of organisms, including Gram-positive bacteria, Gram-negative bacteria, fungi and yeast. The compositions have particular utility as beverage container lubricants. The passage of a container along a conveyor is antimicrobially lubricated by applying a lubricant to at least a portion of the container-contacting surface of the conveyor or to at least a portion of the conveyor-contacting surface of the container and generating singlet oxygen in situ. This method provides effective control of microbes on a beverage conveyor line, at rates comparable to purely chemical biocidal systems.Type: ApplicationFiled: March 12, 2002Publication date: October 16, 2003Applicant: EcolabInventors: Robert D.P. Hei, Stephan M. Hubig, Matthew J. Finley
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Publication number: 20030195200Abstract: The present invention relates to compounds of the general formula (I) 1Type: ApplicationFiled: February 20, 2003Publication date: October 16, 2003Inventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson