Hetero Ring Containing Patents (Class 514/156)
  • Patent number: 9290490
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Kaleen Konrad Childers, Maria Emilia Di Francesco, John Michael Ellis, Christian Fischer, Jonathan Grimm, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Ryan D. Otte, Alessia Petrocchi, Adam J. Schell, Hua Zhou
  • Publication number: 20150080350
    Abstract: The present invention provides bumetanide, analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, analogs and methods for their use. These analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma. Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 19, 2015
    Inventors: John J. PARTRIDGE, Daryl W. HOCHMAN
  • Publication number: 20150080351
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
  • Patent number: 8883766
    Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: November 11, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
  • Publication number: 20140221321
    Abstract: In one embodiment, the present application discloses methods of treating diseases and disorders with sulfasalazine and pharmaceutical formulations of sulfasalazine where the bioavailability of the sulfasalazine is increased. In another embodiment, the present application also provides dosing regimens for treating neurodegenerative diseases and disorders with compositions comprising sulfasalazine.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: Glialogix, Inc.
    Inventors: Thaddeus Cromwell Reeder, Mark Wade Moore, Douglas Alan Lorenz, David Keith Lyon
  • Publication number: 20140162986
    Abstract: Methods for therapy of cystic fibrosis and other conditions are provided. The methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e. ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments include the use of agents to modulate transport of thiol-containing compounds within the cell. Therapeutic methods involve the administration of such agents to a patient afflicted with cystic fibrosis and/or another condition responsive to stimulation of thiol-containing compound transport.
    Type: Application
    Filed: February 13, 2014
    Publication date: June 12, 2014
    Applicant: NATIONAL JEWISH MEDICAL AND RESEARCH CENTER
    Inventors: Brian J. Day, Leonard W. Velsor
  • Patent number: 8628751
    Abstract: The invention provides compounds, including compositions, preparations and formulations, and methods of using and making such compounds. Compounds of the present invention include pyrazine derivatives having a pyrazine core and a plurality of substituents. In some embodiments, pyrazine derivatives of the invention are pyrazine core compounds having one or more electron donating groups and one or more electron withdrawing groups optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: January 14, 2014
    Assignee: Medi Beacon Development, LLC
    Inventors: William L. Neumann, John N. Freskos
  • Patent number: 8604229
    Abstract: This invention provides new lipoxin analogs, compositions containing analogs, and methods of using these compounds and compositions for treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease. The invention also provides for methods of treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease with compositions containing COX-2 inhibitors. Further, the invention provides methods for preventing systemic diseases beyond the oral cavity that are related to periodontal disease using the composition containing lipoxin analogs, COX-2 inhibitors, or both.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: December 10, 2013
    Assignees: University of Southern California, Trustees of Boston University, Brigham and Women's Hospital, Inc.
    Inventors: Thomas E. Van Dyke, Nicos A. Petasis, Charles N. Serhan
  • Patent number: 8598084
    Abstract: An herbicide/insecticide composition containing (a) a pyridine carboxylic acid component and (b) an insecticide component provides synergistic control of selected weeds.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: December 3, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: Norbert M. Satchivi, Paul R. Schmitzer
  • Publication number: 20130310344
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Application
    Filed: August 5, 2011
    Publication date: November 21, 2013
    Applicant: ASTRAZENECA AB
    Inventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh, Jeffrey Gilbert Varnes
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130303491
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 14, 2013
    Applicant: Siga Technologies Inc.
    Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
  • Publication number: 20130303493
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 14, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 8518715
    Abstract: A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q1, X, Y, Z, Z1, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion of 90Y, 111In or 177Lu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: August 27, 2013
    Assignee: Nordion (Canada) Inc.
    Inventors: Zoltan Kovacs, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso, Cara Ferreira
  • Publication number: 20130116216
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: November 12, 2010
    Publication date: May 9, 2013
    Inventors: Celia Dominguez, John Wityak, Michael Prime, Stephen Martin Courtney, Christopher Yarnold, Frederick Brookfield, Richard Marston, Douglas Macdonald
  • Publication number: 20130101615
    Abstract: This invention is a method for immunizing, preventing or treating a Mycobacterium avium subspecies paratuberculosis-associated disease or condition by screening subjects for markers indicative of predisposition or susceptibility to a Mycobacterium avium subspecies paratuberculosis-associated disease or condition and administering a Mycobacterium avium subspecies paratuberculosis vaccine or prophylactic or therapeutic agent.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Inventor: Robert J. Greenstein
  • Patent number: 8278354
    Abstract: Methods for reducing the likelihood of embryonic death in a female ruminant by feeding the ruminant for at least 30 days after conception an effective amount of free-flowing fatty acid calcium salt product comprising from about 1 to 10% by weight of eicosapentaenoic acid (EPA) and from about 1 to about 10% by weight of decosahexaenoic acid (DHA).
    Type: Grant
    Filed: August 10, 2004
    Date of Patent: October 2, 2012
    Assignee: Virtus Nutrition LLC
    Inventors: George K. Strohmaier, Eiler D. Frederiksen, Nestor Daniel Luchini
  • Publication number: 20120208790
    Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 16, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
  • Patent number: 8198101
    Abstract: A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q1, X, Y, Z, Z1, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion of 90Y, 111Li or 177Lu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.
    Type: Grant
    Filed: March 6, 2007
    Date of Patent: June 12, 2012
    Assignee: Nordion (Canada) Inc.
    Inventors: Zoltan Kovacs, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso
  • Publication number: 20120094964
    Abstract: The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.
    Type: Application
    Filed: May 6, 2010
    Publication date: April 19, 2012
    Inventors: Tadashi Inoue, Masashi Ohmi, Kiyoshi Kawamura, Kazuo Ando, Yuji Shishido
  • Publication number: 20120022028
    Abstract: The present invention relates to soluble guanylate cyclase (sGC) and to phosphodiesterases (PDEs) and the pharmacology of sGC stimulators, sGC activators and PDE inhibitors. More particularly, the invention relates to the use of sGC stimulators and sGC activators in combination with PDE5 inhibitors for preparation of medicaments for the treatment of male erectile dysfunction (MED) in particular for the MED treatment of difficult to treat patients and patients not or not fully responding to PDE5 inhibitors.
    Type: Application
    Filed: January 7, 2010
    Publication date: January 26, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Peter Sandner, Johannes-Peter Stasch, Michael-Friedrich Böttcher
  • Publication number: 20110256129
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: April 25, 2011
    Publication date: October 20, 2011
    Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt, Alexander Shoemaker, Michael Mitten
  • Publication number: 20110237553
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: March 16, 2011
    Publication date: September 29, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Patent number: 7985771
    Abstract: The invention relates to a method of treating with furanone derivatives and the pharmaceutically acceptable salts thereof, one or more conditions of the skin, in particular regulating skin condition, regulating signs of skin aging, treating a number of conditions such as contact dermatitis, skin irritation, rosacea, acne, psoriasis, and preventing and protecting skin tissue against age-related damage or damage resulting from insults such as harmful (UV) radiation or environmental pollution, stress and fatigue.
    Type: Grant
    Filed: July 30, 2003
    Date of Patent: July 26, 2011
    Assignee: Monsanto Technology LLC
    Inventors: Sekhar Boddupalli, Gail Walkinshaw, Bing Wang
  • Publication number: 20110144067
    Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 16, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Patent number: 7935688
    Abstract: The present invention provides a compound represented by the following general formula (I): or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing such a compound, and the like. The compound or a pharmaceutically acceptable salt thereof, the pharmaceutical composition containing such a compound, or the like is useful as a medicine or the like for therapy of benign prostatic hyperplasia, cancer, osteoporosis, psoriasis, secondary hyperparathyroidism, chronic glomerulonephritis, lupus nephritis and/or diabetic nephropathy and the like.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: May 3, 2011
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Tadakatsu Takahashi, Yoshiyuki Ono, Hirotaka Kashiwagi, Tsuyoshi Haneishi, Kazuki Shimizu
  • Publication number: 20110053897
    Abstract: Provided herein area novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.
    Type: Application
    Filed: July 26, 2010
    Publication date: March 3, 2011
    Applicant: IRM LLC
    Inventors: Jianwei CHE, Bei Chen, Qiang Ding, Xueshi Hao, Xiaohui He, Songchun Jiang, Qihui Jin, Yunho Jin, Hong Liu, Yahua Liu, Barun Okram, Tetsuo Uno, Xu Wu, Kunyong Yang, Xuefeng Zhu
  • Patent number: 7858569
    Abstract: Antibacterial solution useful as a cleaning agent suitable for cutaneous use by humans or otherwise which is aqueous based, free of alcohol and surfactants and having a quaternary ammonium compound as its principal antimicrobial agent, a number of moisturizing agents and DMDM Hydantoin serving at least as a preservative.
    Type: Grant
    Filed: March 30, 2005
    Date of Patent: December 28, 2010
    Assignee: Water Journey Ltd.
    Inventors: Francine Glick, Eugene Puchalski, Jr., Annette Joubert
  • Publication number: 20100292306
    Abstract: Compositions and methods for treatment of individuals diagnosed with a dystrophin deficiency are disclosed. In particular, inhibitors of NF?B transactivation and/or inhibitors that suppress p65 expression are used to prevent and/or reverse muscle damage in animals or humans lacking dystrophin. Such compositions and methods are useful in the treatment of individuals with muscular dystrophy.
    Type: Application
    Filed: July 28, 2010
    Publication date: November 18, 2010
    Inventors: C. George Carlson, Rajvir Singh
  • Publication number: 20100249077
    Abstract: The present invention relates to novel pyridylmethyl-sulfonamide compounds of formula (I) where: n is 0 to 4; m is 0 to 4; R1 is halogen, CN, NO2, OH, SH, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, etc.; and/or two radicals R1 together form a fused ring; R2 is H, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl, C3-C8-cycloalkyl, C1-C4-alkyl-C3-C8-cycloalkyl or benzyl; R3 is halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; Y is —O—, C1-C4-alkanediyl, —O—CH2—, —CH2—O—, —C(NORn)—, —S—, —S(?O)—, —S(?O)2— or —N(Rn)—; and the N-oxides, and salts thereof and their use for combating phytopathogenic harmful fungi, and also to compositions and seed comprising at least one such compound.
    Type: Application
    Filed: November 21, 2008
    Publication date: September 30, 2010
    Applicant: BASF SE
    Inventors: Wassilios Grammenos, Jan Klaas Lohmann, Thomas Grote, Jochen Dietz, Bernd Mueller, Michael Puhl, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Joachim Rheinheimer
  • Publication number: 20100210603
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Application
    Filed: September 11, 2009
    Publication date: August 19, 2010
    Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
  • Publication number: 20100197640
    Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
    Type: Application
    Filed: January 29, 2010
    Publication date: August 5, 2010
    Applicant: 4SC AG
    Inventor: Stefano PEGORARO
  • Patent number: 7723389
    Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.
    Type: Grant
    Filed: November 4, 2002
    Date of Patent: May 25, 2010
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
  • Patent number: 7608244
    Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
    Type: Grant
    Filed: July 16, 2007
    Date of Patent: October 27, 2009
    Assignee: Mallinckrodt Inc.
    Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
  • Patent number: 7435408
    Abstract: Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear a-hydroxy-acid polyester backbone having at least one amino acid group incorporated therein and at least one poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, porous particles having a relatively large mean diameter, for example greater than 5 ?m, can be used for enhanced delivery of a therapeutic agent to the alveolar region of the lung.
    Type: Grant
    Filed: April 6, 2004
    Date of Patent: October 14, 2008
    Assignees: Massachusetts Institute of Technology, The Penn State Research Foundation
    Inventors: David A. Edwards, Giovanni Caponetti, Jeffrey S. Hrkach, Noah Lotan, Justin Hanes, Robert S. Langer, Abdellaziz Ben-Jebria
  • Patent number: 7208629
    Abstract: Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1–6alkyl and —(CH2)n-C3–7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1–6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: April 24, 2007
    Assignee: Glaxo Group Limited
    Inventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, George Stuart Cockerill, Suzanne Joy Merrick, Kathryn Jane Smith, Ann Louise Walker
  • Patent number: 6927197
    Abstract: Antibacterial solution useful as a cleaning agent suitable for cutaneous use by humans or otherwise which is aqueous based, free of alcohol and surfactants and having a quaternary ammonium compound as its principal antimicrobial agent, a number of moisturizing agents and DMDM Hydantoin serving at least as a preservative.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: August 9, 2005
    Assignee: Water Journey Ltd.
    Inventors: Francine Glick, Eugene Puchalski, Jr.
  • Patent number: 6867229
    Abstract: Composition which is useful in particular for the treatment and protection of domestic animals which are infested with parasites or are likely to be infested with them, these compositions comprising, in the form of a ready-to-use solution: a) an insecticidal active substance of formula (I), b) a crystallization inhibitor, c) an organic solvent having a dielectric constant of between 10 and 35, preferably of between 20 and 30, d) an organic co-solvent having a boiling point below 100° C., preferably below 80° C., and a dielectric constant of between 10 and 40, preferably of between 20 and 30.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: March 15, 2005
    Assignee: Merial
    Inventor: Jean Pierre Etchegaray
  • Patent number: 6670456
    Abstract: Actinium-225 complexes comprising functionalized polyazamacrocyclic chelant compounds are disclosed. Such complexes show improved stability and can be conjugated to a biological carrier.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: December 30, 2003
    Assignee: Dow Global Technologies Inc.
    Inventors: R. Keith Frank, Garry E. Kiefer, Jaime Simon
  • Patent number: 6479456
    Abstract: An antimicrobial perfume compositions that contain a perfume ingredient having antimicrobial activity of at least 80% as measured by the “agar surface coating test,” the “vapor phase test,” or by the “direct spray method.” The active ingredient is grapefruit-pip, a fumitory extract, a fumaric acid or an ester of fumaric acid or lactic acid.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: November 12, 2002
    Assignee: Firmenich SA
    Inventor: Günter Holzner
  • Patent number: 6395765
    Abstract: Composition which is useful in particular for the treatment and protection of domestic animals which are infested with parasites or are likely to be infested with them, these compositions comprising, in the form of a ready-to-use solution: a) an insecticidal active substance of formula (I), b) a crystallization inhibitor, c) an organic solvent having a dielectric constant of between 10 and 35, preferably of between 20 and 30, d) an organic co-solvent having a boiling point below 100° C., preferably below 80° C., and a dielectric constant of between 10 and 40, preferably of between 20 and 30.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: May 28, 2002
    Assignee: Merial
    Inventor: Jean Pierre Etchegaray
  • Patent number: 6294186
    Abstract: The present invention relates to antimicrobial compositions which provide enhanced immediate as well as residual anti-viral and antibacterial efficacy. The antimicrobial compositions of the present invention provide previously unseen residual effectiveness against Gram negative bacteria, Gram positive bacteria, and viruses, fungi, and improved immediate germ reduction upon use. These compositions comprise: a) a safe and effective amount of a benzoic acid analog; b) a safe and effective amount of a metal salt; and c) a dermatologically acceptable carrier for the acid and salt wherein said composition has a pH of from about 1 to about 7. The invention further relates to methods of use for the present compositions as well as antimicrobial products which incorporate the compositions.
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: September 25, 2001
    Inventors: Peter William Beerse, Kimberly Ann Biedermann, Steven Hardy Page, Michael Joseph Mobley, Jeffrey Michael Morgan
  • Patent number: 6117858
    Abstract: The invention relates to a new and improved pharmaceutical composition and method for delivery of therapeutic agents. The methods and composition of the invention can be used with several therapeutic agents and can achieve site specific delivery of a therapeutic or diagnostic substance. This can allow for lower doses and for improved efficacy with drugs which traditionally reach targeted sites and can result in improved utility for agents such as oligonucleotides and polynucleotides which are plagued with problems with biodistribution.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: September 12, 2000
    Assignee: The Board of Regents of the University of Nebraska
    Inventors: Thomas R. Porter, Patrick L. Iversen
  • Patent number: 6100245
    Abstract: The present invention provides compositions and methods for treating ulcerative colitis by providing an effective amount of simethicone and in a preferred embodiment in combination with sulfasalazine.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: August 8, 2000
    Assignee: McNeil-PPC, Inc.
    Inventor: Thomas Sox
  • Patent number: 6004948
    Abstract: Compounds of the formula (I) in which A is oxygen, sulphur or NH; B is a group of the formula (IIa) or (IIb); and the other variables have the meaning given in claim 1, may be used as inhibitors of the enzyme cyclooxygenase II ##STR1##
    Type: Grant
    Filed: September 3, 1998
    Date of Patent: December 21, 1999
    Assignee: Nycomed Austria GmbH
    Inventors: Heinz Blaschke, Peter Kremminger, Michael Hartmann, Harald Fellier, Jorg Berg, Thomas Christoph, Franz Rovenszky, Dagmar Stimmeder
  • Patent number: 5849727
    Abstract: This invention relates to a new and improved pharmaceutical composition and method for delivery of therapeutic or bioactive agents. The methods and composition of the invention can be used with several therapeutic or bioactive agents and can achieve site-specific delivery of a therapeutic or biologically-active substance. This can allow for lower doses and for improved efficacy with drugs, particularly agents such as oligonucleotides which are plagued with problems in achieving therapeutic levels at targeted sites.
    Type: Grant
    Filed: June 28, 1996
    Date of Patent: December 15, 1998
    Assignee: Board of Regents of the University of Nebraska
    Inventors: Thomas R. Porter, Patrick L. Iversen
  • Patent number: 5110808
    Abstract: The invention concerns novel (oxamido- and ureido-phenylsulfonyl)nitromethane derivatives and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.
    Type: Grant
    Filed: July 31, 1991
    Date of Patent: May 5, 1992
    Assignee: Imperial Chemical Industries, PLC
    Inventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
  • Patent number: 4818753
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is H, methyl, ethyl, or chloro and R.sup.2 is hydrocarbyl of 1-12 C are useful as antifungal agents. Compounds of this series wherein R.sup.2 is 7-12 C are novel. A new synthetic method for the compounds is also described.
    Type: Grant
    Filed: September 18, 1987
    Date of Patent: April 4, 1989
    Assignee: SRI International
    Inventors: William T. Colwell, Joseph I. DeGraw
  • Patent number: 4769447
    Abstract: The present invention provides gamma-glutamyl-4-azoanilides, processes for their preparation and their use as substrates for gamma-glutamyl transferase determination, of the formula ##STR1## wherein X is alkyl, --(CH.sub.2).sub.m --COOH or --O--(CH.sub.2).sub.n --COOH wherein m is 0-4 and n is 1-4; R is optionally substituted p-nitrophenyl; an optionally substituted thiophene residue; an optionally substituted thiazole residue; an optionally substituted benzothiazole residue; an optionally substituted benzoisothiazole residue; an N-alkylthiazole residue; or an optionally substituted 1,3,5-thiodiazole residue; as well as the alkali metal, alkaline earth metal and ammonium salts thereof.
    Type: Grant
    Filed: January 27, 1987
    Date of Patent: September 6, 1988
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elli Rauscher, John Griffiths, Leonard F. Dixon
  • Patent number: 4742069
    Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols A, R and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as described herein.Compounds of formula I have a pronounced calcium-antagonistic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: May 3, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jaunin, Henri Ramuz