Sulfonamides (i.e., Q-(o=)s(=o)-n, Wherein Q Is A Substituent And Wherein Any Substituent Attached To The Nitrogen Will Be Referred To As E) Patents (Class 514/601)
-
Publication number: 20080261970Abstract: Compounds of formula (I), including methods of making and methods of using are described in formula (I).Type: ApplicationFiled: September 27, 2005Publication date: October 23, 2008Applicant: ELIXIR PHARMACEUTICALS, INC.Inventors: Jeffrey O. Saunders, Andrew D. Napper
-
Publication number: 20080255091Abstract: The invention discloses aromatic amides and sulfonates to treat or prevent type 2 diabetes mellitus (T2DM), the pathological consequences of T2DM, to inhibit amyloidosis or to prevent death of ?-cells of the pancreas.Type: ApplicationFiled: June 20, 2008Publication date: October 16, 2008Applicant: ASTRUM THERAPEUTICS PTY LTD.Inventors: Alexander B. Zolotoy, Eric S. Hayes
-
Patent number: 7427633Abstract: A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam lysinate delivered as an aerosol or dry powder formulation.Type: GrantFiled: April 2, 2007Date of Patent: September 23, 2008Assignee: Gilead Sciences, Inc.Inventor: Alan Bruce Montgomery
-
Publication number: 20080214672Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating asthma.Type: ApplicationFiled: December 18, 2007Publication date: September 4, 2008Inventor: John Jessen Wright
-
Patent number: 7414076Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: GrantFiled: June 18, 2004Date of Patent: August 19, 2008Assignee: Neurochem (INTERNATIONAL) LimitedInventors: Xianqi Kong, David Migneault, Isabelle Valade, Xinfu Wu, Francine Gervais
-
Patent number: 7411002Abstract: Certain lipophilic polycationic sulfonamides are provided and are useful for treating various diseases or conditions and particularly sepsis.Type: GrantFiled: June 7, 2006Date of Patent: August 12, 2008Assignees: The University of Kansas, Mediquest Therapeutics, Inc.Inventors: Mark R. Burns, Sunil A. David, Scott A. Jenkins
-
Publication number: 20080176939Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.Type: ApplicationFiled: August 1, 2007Publication date: July 24, 2008Applicants: CoMentis, Inc., The Board of Trustees of the University of Illinois, Oklahoma Medical Research Foundation, Purdue Research FoundationInventors: Arun K. Ghosh, Nagaswamy Kumaragurubaran, Chunfeng Liu, Thippeswamy Devasamudram, Hui Lei, Lisa Swanson, Sudha Ankala, Jordan Tang, Geoffrey Bilcer
-
Patent number: 7399776Abstract: This invention relates to a method for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, or tissue injuries. The method includes administering to a subject in need thereof an effective amount of one or more compounds of the following formula. Each variable in this formula is defined in the specification.Type: GrantFiled: March 30, 2004Date of Patent: July 15, 2008Assignee: Taigen BiotechnologyInventors: Kak-Shan Shia, Gholam Hossein Hakimelahi, Jia-Liang Zhu, Chi-Feng Yen, Ying-Huey Huang, Yibin Xiang, Hua-Chien Chen, Ching-Cheng Wang
-
Publication number: 20080167331Abstract: The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.Type: ApplicationFiled: March 14, 2008Publication date: July 10, 2008Inventor: Robert M. Burk
-
Patent number: 7393873Abstract: N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: June 30, 2004Date of Patent: July 1, 2008Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, John Jin Lim, Dai-shi Su, Michael R. Wood
-
Publication number: 20080146618Abstract: Therapeutic methods for inhibiting the growth of preneoplastic/neoplastic vertebrate cells that abnormally express MN protein are disclosed. Screening assays are provided for identifying compounds, preferably organic compounds, preferably aromatic and heterocylic sulfonamides, which inhibit the enzymatic activity of MN/CA IX and that are useful for treating patients with preneoplastic/neoplastic disease. Further, the CA IX-specific inhibitors when labeled or linked to an appropriate visualizing means can also be used diagnostically/prognostically for preneoplastic/neoplastic disease, and for imaging use, for example, to detect hypoxic precancerous cells, tumors and/or metastases, by selectively binding to activated CA IX, preferably CA IX activated under hypoxic conditions, and not to inactive CA IX. Such detection of hypoxic conditions can be helpful in determining effective treatment options, and in predicting treatment outcome and the prognosis of disease development.Type: ApplicationFiled: October 30, 2007Publication date: June 19, 2008Inventors: Claudiu Supuran, Andrea Scozzafava, Silvia Pastorekova, Jaromir Pastorek
-
Patent number: 7381749Abstract: Disclosed herein are carbonyl compounds of having the structural formula: or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof, Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.Type: GrantFiled: June 9, 2005Date of Patent: June 3, 2008Assignee: Kalypsys, Inc.Inventors: James William Malecha, Stewart Alwyn Noble, Christian Andreus Hassig, Paul L. Wash, Brandon M. Wiley, Charles Maxwell Lawrence, Timothy Z. Hoffman
-
Patent number: 7375120Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: April 16, 2003Date of Patent: May 20, 2008Assignee: Smithkline Beecham CorporationInventors: Siegfried B. Christensen, IV, Maxwell D. Cummings, Jinhwa Lee, Jia-ning Xiang
-
Publication number: 20080096922Abstract: A compound of the formula (1): wherein m, n and p is independently an integer of 0 to 4 with the proviso that 3?m+n?8; X is the formula: NR4, etc.; R1, R3 and R4 are a substituted or unsubstituted aryl group, etc.; R2 is a hydrogen atom, etc.; a, b, c, d, e and f are a hydrogen atom or a substituted or unsubstituted alkyl group, etc.; Y is the formula: —SO2—, etc.; and Z is an oxygen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt of the same has an activity of potentiating an expression of a low density lipoprotein receptor and thus is useful as an agent for treating hyperlipidemia or arteriosclerosis.Type: ApplicationFiled: April 4, 2005Publication date: April 24, 2008Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Hitoshi Ban, Shigehiro Asano
-
Patent number: 7348353Abstract: The invention provides compounds of formula (I) wherein m, n, A, R, R?, R?, R0, X and Y are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals in the treatment of e.g.Type: GrantFiled: December 3, 2002Date of Patent: March 25, 2008Assignee: Novartis AGInventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner
-
Publication number: 20080058290Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.Type: ApplicationFiled: March 15, 2005Publication date: March 6, 2008Applicants: TEMPLE UNIVERSITY - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION, ONCONOVA THERAPEUTICS INC.Inventors: E. Premkumar Reddy, M. V. Ramana Reddy, Stanley C. Bell
-
Patent number: 7288571Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR?R?) or an acylsulphonamide (CONHSO2R?) derivative, or a pharmaceutically acceptable salt thereof, and all stereolsom thereof; or when n is equal to or greater than one, R4 may be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR?R?). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5—H).Type: GrantFiled: July 26, 2005Date of Patent: October 30, 2007Assignee: Karo Bio ABInventors: Jon Hangeland, Minsheng Zhang, Yolanda Caringal, Denis Ryono, Yi-Lin Li, Johan Malm, Ye Liu, Neeraj Garg, Chris Litten, Ana Maria Garcia Collazo, Konrad Koehler
-
Patent number: 7265220Abstract: Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.Type: GrantFiled: February 17, 2003Date of Patent: September 4, 2007Assignee: Les Laboratories ServierInventors: Guillaume De Nanteuil, Philippe Gloanec, Tony Verbeuren, Alain Rupin
-
Patent number: 7259187Abstract: Tropolone derivatives represented by the formula (I), which have retinoid actions and are useful as active ingredients of medicaments [R1 to R4 represent hydrogen atom, an alkyl group, or an alkoxyl group; the ring represented by Ar represents an aryl ring or a heteroaryl ring; X represents a single bond, —N?N—, —CON(R5)—, —(C?C)nCON(R6)—, —N(R7)CON(R8)—, —SO2N(R9)—, —N(R10)— (R5 to R9 represent hydrogen atom or an alkyl group, n represents 1 to 3, R10 represents hydrogen atom, an alkyl group, or an acyl group), an alkylene group, an aryldiyl group, or a heterocyclic diyl group; Y represents hydrogen atom, —OR11 (R11 represents hydrogen atom, an alkyl group, or an acyl group), —NHR12 (R12 represents hydrogen atom, an alkyl group, an acyl group, or amino group), or a halogen atomType: GrantFiled: December 18, 2001Date of Patent: August 21, 2007Assignee: Research Foundation Itsuu LaboratoryInventor: Hiroyuki Kagechika
-
Patent number: 7253282Abstract: The invention is concerned with novel hexafluoroisopropanol substituted cyclohexane derivatives of formula (I) wherein R1 to R4, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: December 16, 2005Date of Patent: August 7, 2007Assignee: Hoffman-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
-
Patent number: 7250446Abstract: Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.Type: GrantFiled: March 26, 2004Date of Patent: July 31, 2007Assignee: Council of Scientific and Industrial ResearchInventors: Sangita, Atul Kumar, Man Mohan Singh, Girish Kumar Jain, Puvvada Sri Ramanchandra Murthy, Suprabhat Ray
-
Patent number: 7205434Abstract: There is disclosed a novel class of sulphonamido-substituted bridged bicycloalkyl derivatives comprising a substitute on the bridgehead position. The compounds modulate the production of the ?-amyloid precursor protein, and hence are useful in the treatment of Alzheimer's Disease.Type: GrantFiled: July 31, 2002Date of Patent: April 17, 2007Assignee: Merck Sharp & Dohme Ltd.Inventors: Joanne Clare Hannam, Timothy Harrison, Andrew Madin, Timothy Jason Sparey
-
Patent number: 7161031Abstract: Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: Ar, X, X1, g, R and R3 are as defined herein.Type: GrantFiled: February 28, 2003Date of Patent: January 9, 2007Assignees: Temple University - Of The Commonwealth System of Higher Education, Onconova Therapeutics, Inc.Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
-
Patent number: 7115632Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.Type: GrantFiled: May 11, 2000Date of Patent: October 3, 2006Assignee: G. D. Searle & Co.Inventors: Louis J Bedell, Joseph J McDonald, Thomas E Barta, Daniel P Becker, Rao N Shashidhar, John N Freskos, Brent V Mischke, Daniel P Getman, Gary A DeCrescenzo, Clara I Villamil
-
Patent number: 7105569Abstract: New active compound combinations of valinamide derivatives of the formula (I) in which R1 and R2 has the meaning given in the description, with known fungicidal active substances, and their use for combating phytopathogenic fungi are described.Type: GrantFiled: May 6, 2002Date of Patent: September 12, 2006Assignee: Bayer AktiengesellsachftInventors: Heinz-Wilhelm Dehne, Wilhelm Brandes, Karl-Heinz Kuck, Thomas Seitz
-
Patent number: 7094431Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.Type: GrantFiled: September 30, 2003Date of Patent: August 22, 2006Inventor: Mickey L. Peshoff
-
Patent number: 7034057Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.Type: GrantFiled: November 19, 2003Date of Patent: April 25, 2006Assignee: Schering CorporationInventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
-
Patent number: 6963010Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.Type: GrantFiled: January 8, 2002Date of Patent: November 8, 2005Assignee: MediQuest Therapeutics, Inc.Inventors: Mark R. Burns, Gerard F. Graminski
-
Patent number: 6960574Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), X= R3= Y= Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl. Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R?=H or O(?) as well as pharmaceuticals compositions and methods for the treatment of opiate addiction, opiate dependence, opiate tolerance, opiate related abstinence syndrome, nicotine addition and obesity based thereon.Type: GrantFiled: March 17, 2004Date of Patent: November 1, 2005Assignee: University of FloridaInventor: Laszlo Prokai
-
Patent number: 6958416Abstract: The invention relates to derivatives of valproyltaurinamide of formula (I) in which R1 and R2 are independently hydrogen, a C1-C6-alkyl group, an arylalkyl group or an aryl group. The derivatives are especially useful for the treatment of epilepsy, affective illness, cognitive disorders, neurodegenerative disease, neuropathic pain syndrome, migraine, stroke, brain ischemia, or head trauma injury.Type: GrantFiled: March 5, 2002Date of Patent: October 25, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Meir Bialer, Boris Yagen, Nina Isoherranen
-
Patent number: 6946492Abstract: Embodiments of the invention relate to methods of reducing weight in mammals and for the prophylaxis or treatment of obesity comprising administration of C2-substituted indan-1-one systems and their physiologically acceptable salts and physiologically functional derivatives. Compounds for use in methods of embodiments of the invention may include compounds of the formula in which the radicals are as defined, and their physiologically acceptable salts.Type: GrantFiled: August 30, 2002Date of Patent: September 20, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
-
Patent number: 6943170Abstract: This invention relates generally to N-cycloalkylglycines of the Formula (I): or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits including the same, methods for using the same for treating viral infection or an assay standards or reagents, and intermediates and processes for making the same.Type: GrantFiled: October 30, 2003Date of Patent: September 13, 2005Assignee: Bristol-Myers Squibb CompanyInventor: David J. Carini
-
Patent number: 6924311Abstract: The present invention relates to methods for elevating high density lipoprotein (HDL) plasma levels, decreasing the absorption of dietary cholesterol in the intestine, decreasing the plasma level of low density lipoprotein (LDL), and increasing the conversion of cholesterol to bile acids, utilizing LXR? selective agonists, usually without elevating the plasma levels of triglycerides. Also provided are methods of using such agonists to treat metabolic diseases alone or in combination with other active agents. Also provided are methods for decreasing hyperglycemia and insulin resistance methods for treating type II diabetes, and methods for treating type II diabetes and reducing the cardiovascular complications of type II diabetes, utilizing an LXR agonist. Further provided are methods for treating obesity and methods for treating the complications of obesity including type II diabetes, cardiovascular disease, hyperlipidemia, and hypertension, administering an LXR?-selective antagonist.Type: GrantFiled: October 17, 2001Date of Patent: August 2, 2005Assignee: X-Ceptor Therapeutics, Inc.Inventors: Ira G. Schulman, Eric D. Bischoff, Rajendra K. Tangirala
-
Patent number: 6924286Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: August 4, 2003Date of Patent: August 2, 2005Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
-
Patent number: 6919376Abstract: Compositions and methods of using an MT103 family member, wherein MT103 is the chemical N,N-dicyclohexyl-(1S)-isoborneol-10-sulfonamide. Uses of the compositions include cancer therapy, antibacterials, antifungals, induction of apoptosis, and hormonal antagonists.Type: GrantFiled: September 20, 2002Date of Patent: July 19, 2005Assignee: Medisyn Technologies, Inc.Inventors: Javier Llompart, Jorge Galvez
-
Patent number: 6919369Abstract: Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: August 19, 2002Date of Patent: July 19, 2005Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
-
Patent number: 6908947Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: October 25, 2001Date of Patent: June 21, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
-
Patent number: 6906092Abstract: The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: June 25, 2003Date of Patent: June 14, 2005Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic, Andrew David White
-
Patent number: 6906099Abstract: The present invention relates to the use of a composition that increases central nervous system GABA levels in a mammal, for the treatment of addiction to drugs of abuse and modification of behavior associated with addiction to drugs of abuse in said mammal.Type: GrantFiled: February 2, 2001Date of Patent: June 14, 2005Assignee: Brookhaven Science Associates, LLCInventors: Stephen L. Dewey, Jonathan D. Brodie, Charles R. Ashby, Jr.
-
Patent number: 6890942Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.Type: GrantFiled: May 5, 2004Date of Patent: May 10, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Hatice Belgin Gulgeze, Jacques Banville, Roger Remillard, Donald Corson
-
Patent number: 6884784Abstract: The present invention provides a unique approach for the diagnosis and management of infections by Chlamydia species, particularly C. pneumoniae. The invention is based, in part, upon the discovery that a combination of agents directed toward the various stages of the chlamydial life cycle is effective in substantially reducing infection. Products comprising combination of antichlamydial agents, novel compositions and pharmaceutical packs are also described.Type: GrantFiled: March 19, 2002Date of Patent: April 26, 2005Assignee: Vanderbilt UniversityInventors: William M. Mitchell, Charles W. Stratton
-
Patent number: 6852484Abstract: The present inventors have discovered that Asparagine Synthase is essential for fungal pathogenicity. Specifically, the inhibition of Asparagine Synthase gene expression in fungi results in no signs of successful infection or lesions. Thus, Asparagine Synthase can be used as a target for the identification of antibiotics, preferably antifungals. Accordingly, the present invention provides methods for the identification of compounds that inhibit Asparagine Synthase expression or activity. The methods of the invention are useful for the identification of antibiotics, preferably antifungals.Type: GrantFiled: December 10, 2001Date of Patent: February 8, 2005Assignee: Icoria, Inc.Inventors: Sze-Chung Lo, Maria Victoria Montenegro-Chamorro, Sheryl Frank, Blaise Darveaux, Sanjoy Mahanty, Ryan Heiniger, Amy Skalchunes, Huaqin Pan, Rex Tarper, Jeffrey Shuster, Matthew M. Tanzer, Lisbeth Hamer, Kiichi Adachi, Todd M. DeZwaan
-
Patent number: 6849634Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: December 7, 2001Date of Patent: February 1, 2005Assignee: ICAgenInventors: Serge Beaudoin, Aimee D. Reed, Michael F. Gross
-
Publication number: 20040254150Abstract: Certain ethanolamine analogs and related compounds useful in the control nematodes that infest plants or the situs of plants are described.Type: ApplicationFiled: May 12, 2004Publication date: December 16, 2004Inventors: Michelle Coutu Hresko, Deryck J. Williams, Merry B. McLaird, John D. Bradley, Barry J. Shortt, Ronald E. Worthington
-
Patent number: 6822001Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.Type: GrantFiled: November 2, 2001Date of Patent: November 23, 2004Assignee: Tularik Inc.Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
-
Publication number: 20040229922Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: ApplicationFiled: March 30, 2004Publication date: November 18, 2004Applicant: G.D. Searle & Co.Inventors: Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
-
Patent number: 6818671Abstract: This invention relates to compositions of nimesulide for topical application.Type: GrantFiled: April 10, 2001Date of Patent: November 16, 2004Inventors: Koral Embil, Ray Figueroa
-
Publication number: 20040220236Abstract: The present invention pertains to compounds of the formula (I) which are, inter alia, antiprolilferative agents, anticancer agents, anitimycohacterial agents, antituberculosis agents, and/or thioredoxin/thioredoxin reductase inhibitor: wherein: Q is ═O or ═N—S(═O)2—RQ; RQ is -II or optionally substituted C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; Ar is optionally substituted C5-20aryl; RO is an oxy substituent; the bond marked &agr; is a single bond or a double bond; the bond marked &bgr; is a single bond or a double bond; R3 and R5 are each independently ring substituents; R2 and R6 are each independently ring substituents; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for example, in the treatment of proliferative conditions, (e.g.Type: ApplicationFiled: April 27, 2004Publication date: November 4, 2004Inventors: Malcolm Francis Graham Stevens, Geoffrey Wells, Andrew David Westwell, Tracey Dawn Poole
-
Patent number: 6812251Abstract: The invention provides a method of inhibiting tumor growth by contacting the tumor with a composition containing a taurine compound. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death.Type: GrantFiled: March 15, 2002Date of Patent: November 2, 2004Assignee: Rhode Island HospitalInventors: Paul Calabresi, Bai-Chuan Pan, James Darnowski
-
Patent number: 6800631Abstract: A palatable antimicrobial drug concentrate comprising: (a) a sulfonamide and/or sulfonamide salt in aqueous solution; (b) a 2,4-diaminopyrimidine in stable suspension within said solution; and (c) a suspending agent. The invention has a long room temperature shelf life and is sufficiently stable to be administered via the drinking water of animals.Type: GrantFiled: June 24, 2002Date of Patent: October 5, 2004Inventors: Michael A. Strobel, William A. Soderlund, Jr.