Para-n-benzene - Sulfoxy-n Containing Doai, And Said Benzene Ring Is Not Part Of A Polycyclo Ring System Patents (Class 514/155)
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Patent number: 10626081Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.Type: GrantFiled: September 16, 2016Date of Patent: April 21, 2020Assignee: METACRINE, INC.Inventors: Nicholas D. Smith, Steven P. Govek, Johnny Y. Nagasawa
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Patent number: 10603298Abstract: The invention relates to a succinate dehydrogenase inhibitor or a prodrug and/or a pharmaceutically acceptable salt thereof for use in the treatment or prevention of reperfusion injury, such as ischemia-reperfusion injury, by inhibiting the accumulation of succinate, wherein the inhibitor or prodrug and/or pharmaceutically acceptable salt thereof is a cell-permeable reversible inhibitor of succinate dehydrogenase.Type: GrantFiled: July 3, 2015Date of Patent: March 31, 2020Inventors: Edward Chouchani, Thomas Krieg, Michael Patrick Murphy, Lorraine Work, Christian Frezza, Kourosh Saeb-Parsy
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Patent number: 10442779Abstract: The invention provides compositions and methods useful for the treatment of Friedreich's ataxia. In some embodiments, the invention provides compositions and methods useful for inhibiting the ubiquitination of frataxin.Type: GrantFiled: September 22, 2015Date of Patent: October 15, 2019Assignee: FRATAGENE THERAPEUTICS S.R.L.Inventors: Roberto Testi, Ottaviano Incani, Alessandra Rufini, Gabriella DeMartino
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Patent number: 9884039Abstract: The present teachings relate to liquid pharmaceutical formulations of furosemide, where the pharmaceutical formulations include a molar excess of tris(hydroxymethyl)aminomethane to furosemide, have a pH in the range of 7 to 8.5, and a concentration of tris(hydroxymethyl)aminomethane greater than or equal to about 50 mM. The present teachings can improve the stability of liquid pharmaceutical formulations including furosemide and the suitability of such pharmaceutical formulations for subcutaneous administration or delivery.Type: GrantFiled: April 3, 2014Date of Patent: February 6, 2018Assignee: scPharmaceuticals Inc.Inventors: Scott A. Michaels, Pieter Muntendam, Glenn R. Larsen
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Patent number: 9493423Abstract: Disclosed herein are an N-(pyrazolylmethyl)arylsulfonamide derivative useful as a calcium ion channel blocker, a pharmaceutically acceptable salt thereof, and the medicinal use thereof as a therapeutic agent using its calcium ion channel blocking effect.Type: GrantFiled: February 26, 2015Date of Patent: November 15, 2016Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Ghil Soo Nam, Kyung Il Choi, Jung Hyun Kim, Ae Nim Pae, Jin Ri Hong, Jae Kyun Lee
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Patent number: 9427398Abstract: Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in N,N-dimethylacetamide, polyethylene glycol and D5W useful in the treatment of hypertension, heart failure and renal disease leading to edematous states. Also disclosed are methods for preparing such solutions.Type: GrantFiled: December 17, 2012Date of Patent: August 30, 2016Assignee: Academic Pharmaceuticals IncorporatedInventors: John Somberg, Vasant Ranade
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Patent number: 9217019Abstract: Described herein are compositions and methods for treating Friedreich's Ataxia (FRDA). In some aspects, mutant forms of frataxin which are resistant to ubiquitination are provided. In some aspects, pharmaceutical compositions comprising mutant frataxin are provided. In further aspects, methods of using mutant frataxin are provided.Type: GrantFiled: July 27, 2011Date of Patent: December 22, 2015Assignee: Fratagene Therapeutics Ltd.Inventor: Roberto Testi
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Patent number: 8940301Abstract: The present invention provides methods of treating cancer by administering an IL8-CXCR1 pathway inhibitor (e.g., an anti-CXCR1 antibody or Repertaxin) alone or in combination with an additional chemotherapeutic agent such that non-tumorigenic and tumorigenic cancer cells in a subject are killed. The present invention also provides compositions and methods for detecting the presence of and isolating solid tumor stem cells in a patient (e.g., based on the presence of CXCR1 or FBXO21).Type: GrantFiled: November 11, 2009Date of Patent: January 27, 2015Assignee: The Regents of The University of MichiganInventors: Max S. Wicha, Christophe Ginestier
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Patent number: 8883766Abstract: 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: GrantFiled: April 27, 2012Date of Patent: November 11, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
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Publication number: 20140329778Abstract: The present invention relates to a compound according to formula I in particular as anti-ulcer agent and/or anti-Helicobacter pylori agent, wherein R1 is selected from linear or branched C1-C6 alkyl, H, thioether and benzyl, and R2 is selected from linear or branched C1-C10 alkanediyl and pharmaceutical compositions thereofType: ApplicationFiled: March 13, 2014Publication date: November 6, 2014Applicant: King Saud UniversityInventors: Amani S. AWAAD, Reham Moustafa EL-MELIGY, Ahmed M. ALAFEEFY
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Publication number: 20140329777Abstract: Methods to treat infectious diseases are disclosed herein. Some embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) to treat infectious diseases. Other embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) and administration of one or more antibiotics to treat infectious diseases.Type: ApplicationFiled: April 22, 2014Publication date: November 6, 2014Inventors: Lisa Ann Morici, Saja Asakrah
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Publication number: 20140303103Abstract: The present disclosure provides methods for detecting the presence of a cancer stem cell and their use in cancer prognosis, evaluating risk of cancer metastasis, identifying or validating drug candidates, and determining treatment efficacy. It also provides kits useful for detecting the presence of cancer stem cells as well as methods of treating cancer using CAIX inhibitors.Type: ApplicationFiled: October 24, 2012Publication date: October 9, 2014Inventors: Paul C. McDonald, Frances E. Lock, Shoukat Dedhar
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COMPOUNDS AND METHODS FOR MODULATING MITOCHONDRIAL METABOLISM AND REACTIVE OXYGEN SPECIES PRODUCTION
Publication number: 20140128352Abstract: Compounds that modulate mitochondrial reactive oxygen species (ROS) production are provided. The compounds may modulate ROS production at defined sites without also altering energy production. Methods of using and identifying such compounds are also provided.Type: ApplicationFiled: September 20, 2013Publication date: May 8, 2014Applicant: Buck Institute for Research on AgingInventors: Martin D. Brand, Adam Orr -
Patent number: 8703749Abstract: A method of treating Friedreich's Ataxia with compounds of formula I including pharmaceutically acceptable salts, tautomers or stereoisomers of compounds of formula Lp.Type: GrantFiled: December 7, 2010Date of Patent: April 22, 2014Inventors: Roberto Testi, Ottaviano Incani
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Patent number: 8637493Abstract: Described are methods for treating cancers, e.g., glioblastoma, including administering an inhibitor of Notch signalling, e.g., a gamma secretase inhibitor, in combination with a chemotherapeutic agent.Type: GrantFiled: November 10, 2010Date of Patent: January 28, 2014Assignee: University of MassachusettsInventors: Alonzo H. Ross, Candace Gilbert, Richard Moser
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Publication number: 20140018326Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 27, 2011Publication date: January 16, 2014Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
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Publication number: 20140018325Abstract: Compounds of Formula I are disclosed wherein R1, R2, R3A, R3B, R4A, R4B, R5A, R5B, R6A, R6B, R8 and R9 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 27, 2011Publication date: January 16, 2014Inventors: Michael John Boyd, Carmela Molinaro, Amelia Roy, Vouy Linh Truong
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Patent number: 8629126Abstract: Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. The quinolone derivatives have excellent platelet aggregation inhibitory activity. A method of using the compounds is also disclosed.Type: GrantFiled: February 2, 2012Date of Patent: January 14, 2014Assignee: Astellas Pharma Inc.Inventors: Yuji Koga, Takao Okuda, Susumu Watanuki, Takashi Kamikubo, Fukushi Hirayama, Hiroyuki Moritomo, Jiro Fujiyasu, Michihito Kageyama, Toshio Uemura, Jun Takasaki
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Publication number: 20130310347Abstract: 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: ApplicationFiled: May 21, 2013Publication date: November 21, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
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Publication number: 20130303491Abstract: 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: ApplicationFiled: July 22, 2013Publication date: November 14, 2013Applicant: Siga Technologies Inc.Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
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Publication number: 20130225404Abstract: The present invention relates to the composition comprising a neonicotinoid insecticide selected from: imidacloprid, clothianidin and thiamethoxam and a metabolic herbicide safener. The composition is of particular use in the treatment of plant propagation material (preferably seeds) and improves the growing characteristics of a plant and/or prevents from unwanted plant damage caused by herbicides.Type: ApplicationFiled: October 19, 2011Publication date: August 29, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Christoph Grimm, Michael Schade, Andreas Zoschke, Beat Reber
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Publication number: 20130203692Abstract: This invention relates to oral veterinary compositions for combating ectoparasites and endoparasites in animals, comprising at least one systemically-acting active agent in combination with a pharmaceutically acceptable carrier. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof.Type: ApplicationFiled: January 31, 2013Publication date: August 8, 2013Applicant: MERIAL LIMITEDInventors: Mark David Soll, Diane Larsen, Susan Mancini Cady, Peter Cheifetz, Izabela Galeska
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Publication number: 20130150333Abstract: Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor ? (ROR?) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR? results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).Type: ApplicationFiled: February 13, 2013Publication date: June 13, 2013Applicant: ORPHAGEN PHARMACEUTICALSInventor: Orphagen Pharmaceuticals
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Publication number: 20130116216Abstract: 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: ApplicationFiled: November 12, 2010Publication date: May 9, 2013Inventors: Celia Dominguez, John Wityak, Michael Prime, Stephen Martin Courtney, Christopher Yarnold, Frederick Brookfield, Richard Marston, Douglas Macdonald
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Publication number: 20130109658Abstract: A method of treating Friedreich's Ataxia with compounds of formula I including pharmaceutically acceptable salts, tautomers or stereoisomers of compounds of formula Lp.Type: ApplicationFiled: December 7, 2010Publication date: May 2, 2013Inventors: Roberto Testi, Ottaviano Incani
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Publication number: 20130045952Abstract: The present invention relates to ABA agonist compounds which increase plant stress resistance. The invention also relates to methods of using these compounds. The invention further relates to compositions and formulations comprising the ABA agonist compounds, and uses thereof.Type: ApplicationFiled: August 17, 2012Publication date: February 21, 2013Applicant: Van Andel Research InstituteInventors: Yong Xu, Xiaoyin Edward Zhou, Karsten Melcher, Huaqiang Eric Xu
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Patent number: 8263097Abstract: A method for treating acne on the skin. The method has the steps of (a) providing an drapeable or flexible porous article impregnated with an aqueous cleansing composition having a carrier, benzoyl peroxide, and one or more cleansing agents; (b) contacting an area of the skin affected by acne with the porous article such that the skin is contacted by the composition; and (c) removing the composition from the skin wherein residual benzoyl peroxide remains on the skin in an anti-acne effective amount. There are also anti-acne compositions.Type: GrantFiled: December 22, 2011Date of Patent: September 11, 2012Assignee: Medicis Pharmaceutical CorporationInventors: Waranush Jitpraphai, Eugene Gans
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Publication number: 20120208790Abstract: 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: ApplicationFiled: April 27, 2012Publication date: August 16, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
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Publication number: 20120129817Abstract: The subject matter of this application is directed to combinations of (2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydrophenanthridin-2-ol with other active compounds for the treatment of diabetes mellitus type 2 and/or type 1.Type: ApplicationFiled: February 1, 2012Publication date: May 24, 2012Applicant: NYCOMED GMBHInventors: Thomas KLEIN, Anja BLASER, Bettina RUDOLPH, Ulrich KAUTZ, Jens SELIGE, Wolfgang KROMER
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Publication number: 20120022027Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related 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 hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: October 28, 2010Publication date: January 26, 2012Applicant: Siga Technologies Inc.Inventors: Dongcheng Dai, Tove Bolken, Sean M. Amberg, Dennis E. Hruby, Thomas R. Bailey, Jack H. Nunberg, Celestine Johnson Thomas
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Publication number: 20110256129Abstract: 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: ApplicationFiled: April 25, 2011Publication date: October 20, 2011Inventors: 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
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Publication number: 20110237553Abstract: 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: ApplicationFiled: March 16, 2011Publication date: September 29, 2011Applicant: ABBOTT LABORATORIESInventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
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Publication number: 20110178046Abstract: Described are methods for treating cancers, e.g., glioblastoma, including administering an inhibitor of Notch signalling, e.g., a gamma secretase inhibitor, in combination with a chemotherapeutic agent.Type: ApplicationFiled: November 10, 2010Publication date: July 21, 2011Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Alonzo H. Ross, Candace Gilbert, Richard Moser
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Patent number: 7964585Abstract: A method of treating diabetic neuropathy in a subject includes administering to a subject having diabetes or at risk of diabetes a therapeutically effective amount of a pharmaceutical composition comprising at least one of sulfasalazine or a composition including 5-aminosalicyclic acid and sulfapyridine.Type: GrantFiled: March 13, 2007Date of Patent: June 21, 2011Assignee: Case Western Reserve UniversityInventors: Liliana Berti-Mattera, Timothy S. Kern
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Publication number: 20110144067Abstract: 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: ApplicationFiled: December 7, 2010Publication date: June 16, 2011Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Publication number: 20110129546Abstract: The invention relates to a dermatological pharmaceutical composition for the treatment of skin inflammation diseases, such as dermatitis, atopic dermatitis, vitiligo, alopecia areata, acne, psoriasis and pruritus. The invention comprises a base anti-inflammatory agent, such as indometacin; one or more optional active ingredients selected alternatively from among at least a corticoid and an antibiotic; and a combination of topical antioxidants used to potentiate the anti-inflammatory effect, selected from among green tea, lipoic acid, curcumin, ascorbyl palmitate, Coenzyme Q10, resveratrol, Pycnogenol™, L-camosine, taurine, vitamin E, vitamin C, papaya extract, isoflavones, manganese, lycopene and quercetin. At least one of the topical antioxidants is a peroxisome proliferator-activated receptor-gamma (PPAR-?) activator. The invention also includes at least one antioxidant substance with an antiproliferative effect on keratonocytes, e.g.Type: ApplicationFiled: June 19, 2009Publication date: June 2, 2011Inventor: Ignacio Umbert Mill
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Publication number: 20110003777Abstract: The present invention relates generally to the treatment of diseases and disorders that are mediated by histone deacetylase (HDAC), for example, cancer, with Belinostat™ (also known as (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide; PXD101; and PX 105684), and more particularly, to improvement treatments of such diseases (for example, cancers, for example, leukemias), which employ prolonged continuous infusion (e.g., prolonged continuous intravenous infusion) of Belinostat™.Type: ApplicationFiled: March 6, 2009Publication date: January 6, 2011Applicant: TOPOTARGET A/SInventors: Maxwell Sehested, Peter Buhl Jensen, Nis Nissen
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Publication number: 20100331284Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.Type: ApplicationFiled: May 24, 2010Publication date: December 30, 2010Applicant: NEUROTECH PHARMACEUTICALS CO., LTD.Inventors: Byoung Joo GWAG, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
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Publication number: 20100310680Abstract: This invention relates to a novel composition and method useful for the treatment of acne, and more particularly, to a composition and method for reducing an appearance of post acne marks and scars without skin irritation in a short amount of time.Type: ApplicationFiled: June 9, 2009Publication date: December 9, 2010Inventors: Theresa Chen, Geraldine Watson, I-Ting Wu
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Patent number: 7842681Abstract: Methods of reducing the number of platelets in mammals and preventing or treating pro-thrombotic conditions and diseases that are characterized by an excess of, or undesired activation of, platelets using inhibitors of anti-apoptotic Bcl-2 family protein members is disclosed.Type: GrantFiled: September 5, 2007Date of Patent: November 30, 2010Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Saul Rosenberg, Gary Gordon
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Publication number: 20100210603Abstract: 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: ApplicationFiled: September 11, 2009Publication date: August 19, 2010Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
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Publication number: 20100196280Abstract: The present invention describes polymer nanoparticles with a cationic surface potential, in which both hydrophobic and hydrophilic pharmaceutically active substances can be encapsulated. The hydrophilic and thus water-soluble substances are encapsulated in the particle core by co-precipitation through ionic complexing with a charged polymer. Both therapeutic agents and diagnostic agents can be used as pharmaceutically active substances for encapsulation. The cationic particle surface permits stable, electrostatic surface modification with partially oppositely charged compounds, which can contain target-specific ligands for improving passive and active targeting.Type: ApplicationFiled: June 7, 2007Publication date: August 5, 2010Inventors: Katrin Claudia Fischer, Sascha General
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Patent number: 7723389Abstract: 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: GrantFiled: November 4, 2002Date of Patent: May 25, 2010Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
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Patent number: 7576101Abstract: The application provides for methods and compositions for inhibiting demyelination, promoting remyelination and/or treating paralysis in a subject in need thereof. Preferably, such compositions include immunoglobulins (e.g., antibodies, antibody fragments, and recombinantly produced antibodies or fragments), polypeptides (e.g., soluble forms of the ligand proteins for integrins) and small molecules, which when administered in an effective amount inhibits demyelination and/or promotes remyelination in a patient. The compositions and methods described herein can also utilize other anti-inflammatory agents used to palliate conditions and diseases associated with demyelination.Type: GrantFiled: January 26, 2004Date of Patent: August 18, 2009Assignee: Elan Pharmaceuticals, Inc.Inventors: Stephen J. Karlik, Michael A. Pleiss, Andrei W. Konradi, Francine S. Farouz, Christopher M. Semko, Darren B. Dressen, Elizabeth Messersmith, Stephen Freedman, Ted Yednock
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Patent number: 7435408Abstract: 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: GrantFiled: April 6, 2004Date of Patent: October 14, 2008Assignees: Massachusetts Institute of Technology, The Penn State Research FoundationInventors: David A. Edwards, Giovanni Caponetti, Jeffrey S. Hrkach, Noah Lotan, Justin Hanes, Robert S. Langer, Abdellaziz Ben-Jebria
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Patent number: 7071177Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: April 26, 2001Date of Patent: July 4, 2006Assignee: Syntex (U.S.A.) LLCInventors: Nancy Elisabeth Krauss, Taraneh Mirzadegan, David Bernard Smith, Keith Adrian Walker
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Patent number: 6753298Abstract: Compositions for controlling diseases caused by protozoans of the genus Neospora, which are characterized in that they comprise one or more active compounds which inhibit the microtubulin system of plants.Type: GrantFiled: December 2, 2002Date of Patent: June 22, 2004Assignee: Bayer AGInventors: Gisela Greif, Folker Lieb, Carl Fedtke
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Publication number: 20040062817Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprise 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 and (b) fat-soluble vitamins. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products. This invention also relates to methods for preparing and using the antibacterial/antifungal-wound healing compositions and the pharmaceutical products in which the therapeutic compositions may be used.Type: ApplicationFiled: September 30, 2003Publication date: April 1, 2004Inventor: Mickey L. Peshoff
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Publication number: 20030171341Abstract: Compounds of formula 1 modulate the activity of Rho C: 1Type: ApplicationFiled: November 19, 2002Publication date: September 11, 2003Inventors: Dongxu Sun, Edward L. Perkins, Stuart Tugendreich
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Publication number: 20030165577Abstract: Topical compositions which include urea and an antimicrobial agent, particularly sulfacetamide or metronidazole, are described. Sulfacetamide compositions further including sulfur are also described. Methods for treating dermatological disorders using the compositions are also described.Type: ApplicationFiled: February 11, 2003Publication date: September 4, 2003Applicant: Bradley Pharmaceuticals, Inc.Inventors: Dileep Bhagwat, Bradley P. Glassman, Daniel Glassman