Plural Ring Oxygens In The Hetero Ring Patents (Class 514/452)
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Publication number: 20120283267Abstract: Methods of treating exposure to Giardia lamblia and/or giardiasis and methods of antagonizing Giardia lamblia attachment to the intestinal wall of a subject are described herein.Type: ApplicationFiled: December 2, 2010Publication date: November 8, 2012Applicant: GEORGETOWN UNIVERSITYInventors: Heidi G. Elmendorf, Colleen D. Walls, Christian Wolf
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Patent number: 8304451Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes—“isotubacin” class and “isoisotubacin” class—all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.Type: GrantFiled: May 2, 2007Date of Patent: November 6, 2012Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.Inventors: Ralph Mazitschek, Nicholas Paul Kwiatkowski, James Elliot Bradner
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Patent number: 8304440Abstract: The present invention relates to a combination of antimalarial active ingredients, namely a bisthiazolium salt or a precursor thereof and artemisinin or derivatives thereof. The invention also relates to a pharmaceutical composition comprising such a combination and use thereof in the treatment and/or prevention of malaria.Type: GrantFiled: August 6, 2010Date of Patent: November 6, 2012Assignee: SanofiInventors: Laurent Fraisse, Henri Vial, Sharon Aurore Wein
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Publication number: 20120269901Abstract: The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.Type: ApplicationFiled: December 19, 2011Publication date: October 25, 2012Applicant: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTEInventors: John C. Reed, Maurizio Pellecchia
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Publication number: 20120270902Abstract: The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3?, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).Type: ApplicationFiled: February 13, 2012Publication date: October 25, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Martin Neitzel, Jennifer Marugg
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Publication number: 20120252836Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Phillippe Meyer, Peteris Alberts, Mainkar Prathama
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Publication number: 20120244134Abstract: The present invention provides a process for preparing an aqueous dispersion containing a high concentration of nano/submicron, hydrophobic, functional compounds. The process is carried out by using a complex stabilizer having an HLB value of about 10 to about 17, comprising lecithin and at least one non-phospholipid selected from polysorbate, sucrose ester, and polyglycerol fatty acid ester; selecting a specific weight ratio of the hydrophobic functional compounds and the stabilizer; and using homogenization technique, media milling technique, and/or centrifugal technique. The aqueous dispersion containing a high concentration of nano/submicron, hydrophobic, functional compound produced by the process of the invention has stable dispersibility and improved bioavailability, and can be applied to the fields of foods and pharmaceuticals.Type: ApplicationFiled: July 19, 2011Publication date: September 27, 2012Inventors: Ru-Yin CHEN, Chung-Jen CHEN, Yi-Jie TSAI, Jia-Jiu WU, Chih-Ping HUANG, Chung-Liang CHU
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Publication number: 20120245166Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.Type: ApplicationFiled: October 14, 2010Publication date: September 27, 2012Applicant: Southern Research InstituteInventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
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Publication number: 20120245141Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,Type: ApplicationFiled: March 29, 2012Publication date: September 27, 2012Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
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Patent number: 8263642Abstract: In one aspect, the invention relates to compounds and methods useful for activating heme sensor systems; for decreasing virulence of bacteria, for example, Staphylococcus aureus; pharmaceutical compositions comprising the compounds; and methods of treating microbial-related disorders. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: June 25, 2009Date of Patent: September 11, 2012Assignee: Vanderbilt UniversityInventors: Eric Skaar, Devin Stauff, Olusegun O. Aranmolate
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Publication number: 20120225892Abstract: The present invention relates to compounds of formula (I) compositions, in particular pharmaceutical compositions, and medicaments comprising at least one compound of formula (I). The invention also relates to the use of such a compound for manufacturing a medicament. In particular the medicament and the pharmaceutical composition are intended to treat diseases linked with insulin regulation problems, such as diabetes. This invention aims also to methods for treating or preventing such diseases.Type: ApplicationFiled: November 16, 2010Publication date: September 6, 2012Applicant: MELLITECHInventors: Didier Roche, Fabrice Chimienti, Martin Ohsten
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Patent number: 8258183Abstract: By using a composition for preventing onset and/or recurrence of stroke which contains ethyl icosapentate as its effective component, onset and/or recurrence of stroke is prevented, or in particular, the onset and/or recurrence of stroke in a hyperlipidemia patient who has been treated with HMG-CoA RI, or in particular the recurrence of stroke in a patient who is beyond six months after the onset of stroke, is prevented.Type: GrantFiled: August 9, 2010Date of Patent: September 4, 2012Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Mitsuhiro Yokoyama, Hideki Origasa, Masunori Matsuzaki, Yuji Matsuzawa, Yasushi Saito
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Patent number: 8258177Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: August 11, 2011Date of Patent: September 4, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Publication number: 20120220545Abstract: Provided are coumarin compounds of formula I, for example, robustic acid methyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.Type: ApplicationFiled: January 27, 2012Publication date: August 30, 2012Inventors: Seth J. ORLOW, Li Ni Komatsu
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Publication number: 20120208767Abstract: A method includes obtaining a biological sample from a subject that does not display a symptom of Painful Bladder Syndrome (PBS). The method also includes analyzing the biological sample for a mutated form of NAD(P)H dehydrogenase [quinone], also known as Quinone Oxidoreductase 1, abbreviated NQO1, or a mutation of a NQO1 gene. The method also includes determining a risk of PBS for the subject based on analyzing the biological sample. In some methods, the mutation determined to present an increased risk is a cytosine to thymine nucleotide substitution at a position that leads to a proline to serine amino acid substitution at amino acid position 187 to produce a protein NQO1P187S. Another method includes selecting a subject that has above normal risk of Painful Bladder Syndrome (PBS) or is expressing a symptom of PBS, and treating the subject with a therapeutically effective amount of an antioxidant.Type: ApplicationFiled: February 14, 2012Publication date: August 16, 2012Applicant: University of Maryland, BaltimoreInventor: Anil K. Jaiswal
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Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
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Publication number: 20120196926Abstract: Provided are benzopyran compounds of formula I, for example, pomiferin-3?,4?-dimethyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Inventor: Seth J. ORLOW
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Publication number: 20120178799Abstract: The present invention is an energy drink that included both creatine and caffeine, which provides superior energy, concentration and performance over other energy beverages/liquids. The invention can include other vitamins and beneficial additives, but is intended to be unflavored and unsweetened.Type: ApplicationFiled: January 6, 2012Publication date: July 12, 2012Inventor: Terence O'Neil
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Publication number: 20120178800Abstract: A synergistic antimicrobial composition having two components. The first component is glutaraldehyde. The second component is 2,6-dimethyl-1,3-dioxan-4-yl acetate.Type: ApplicationFiled: September 15, 2010Publication date: July 12, 2012Inventor: Bei Yin
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Publication number: 20120157519Abstract: Tellurium-containing compounds identified for use in a method of treating, or prophylaxis against, a viral infection caused by an influenza virus, uses thereof and pharmaceutical kits and pharmaceutical corn positions comprising the same, are disclosed. The tellurium-containing compounds disclosed herein are suitable for co-administration with an antiviral agent.Type: ApplicationFiled: June 16, 2010Publication date: June 21, 2012Applicant: Biomas Ltd.Inventors: Benjamin Sredni, Michael Albeck
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Publication number: 20120157520Abstract: The present invention relates to compounds with a dioxane nucleus derived from carbohydrates and C-glucosides, process for obtaining same, to the use of such compounds as cytotoxic and antiproliferative agents and to the use thereof for producing a cancer treatment drug.Type: ApplicationFiled: June 25, 2010Publication date: June 21, 2012Applicants: Universidad De La Laguna, Consejo Superior De Investigaciones Cientificas (CSIC)Inventors: Alicia Boto Castro, Rosendo Hernández González, Dácil Hernádez Mesa, Eleuterio Álvarez González, Raquel Marín Cruzado, Mario Diaz González
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Publication number: 20120142766Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: January 18, 2008Publication date: June 7, 2012Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Publication number: 20120129856Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.Type: ApplicationFiled: October 18, 2011Publication date: May 24, 2012Applicant: Cerenis Therapeutics SAInventors: Daniela Carmen Oniciu, Jean-Louis Henri Dasseux, Ronald Barbaras, Valery Kochubey, Dmitry Kovalsky, Oleg Gennadievich Rodin, Otto Geoffroy, Anna Rzepiela
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Publication number: 20120129818Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.Type: ApplicationFiled: April 23, 2010Publication date: May 24, 2012Inventor: Desikan Rajagopal
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Patent number: 8183213Abstract: Combination therapy comprising RXR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.Type: GrantFiled: October 24, 2007Date of Patent: May 22, 2012Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Jacqueline C. Bussolari, Xiaoli Chen, Bruce R. Conway, Keith T. Demarest, Hamish N. M. Ross, Rafael Severino
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Publication number: 20120122784Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: May 17, 2012Applicant: LEO PHARMA A/SInventors: Bjarne Nørremark, Lars Kristian Albert Blæhr, Anne Eeg Knapp, Kristoffer Månsson
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Publication number: 20120122965Abstract: The present invention relates to compositions for skin protection and improvement that contain dibenzo-p-dioxine derivatives as effective components. Since the compositions for skin protection and improvement that contain the dibenzo-p-dioxine derivative according to the present invention have excellent functions such as moisturizing and/or wrinkle prevention which are useful in prevention and improvement of various skin diseases, they can be extensively used as cosmetic ingredients or pharmaceutical agents for prevention and improvement of skin diseases.Type: ApplicationFiled: November 16, 2011Publication date: May 17, 2012Applicant: LIVECHEM, INC.Inventors: Hyeon-Cheol Shin, Hye-Jeong Hwang
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Publication number: 20120122822Abstract: Disclosed are a composition for reducing beta amyloid-induced neurotoxicity by inhibiting ?-secretase activity, comprising a dibenzofuran derivative, and a method for preparing the same. Further disclosed is that the combination of the dibenzofuran derivative with a ?-secretase inhibitor or an anti-inflammatory agent shows higher activity with respect to reducing beta amyloid-induced neurotoxicity.Type: ApplicationFiled: November 17, 2010Publication date: May 17, 2012Applicant: Phloronol, Inc.Inventors: Bong-Ho LEE, Seongho KIM, Hyeon-Cheol SHIN, Haengwoo LEE
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Publication number: 20120122918Abstract: Compounds of formula (1) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)-Q.Type: ApplicationFiled: November 28, 2011Publication date: May 17, 2012Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: David Ryall BROWN, Ian COLLINS, Lloyd George CZAPLEWSKI, David John HAYDON
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Publication number: 20120121696Abstract: Several terpene glycosides (e.g., mogroside V, paenoiflorin, geniposide, rubusoside, rebaudioside A, steviol mono-side and stevioside) were discovered to enhance the solubility of a number of pharmaceutically and medicinally important compounds, including but not limited to, paclitaxel, camptothecin, curcumin, tanshinone HA, capsaicin, cyclosporine, erythromycin, nystatin, itraconazole, celecoxib, clofazimine, digoxin, oleandrin, nifedipine, and amiodarone. The use of the diterpene glycoside rubusoside and monoterpene glycoside paenoiflorin increased solubility in all tested compounds. The terpene glycosides are a naturally occurring class of water solubility-enhancing compounds that are non-toxic and that will be useful as new complexing agents or excipients in the pharmaceutical, agricultural (e.g., solubilizing pesticides), cosmetic and food industries.Type: ApplicationFiled: June 24, 2010Publication date: May 17, 2012Inventor: Zhijun Liu
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Publication number: 20120121536Abstract: Glucose deprivation is an attractive strategy in cancer research and treatment. Cancer cells upregulate glucose uptake and metabolism for maintaining accelerated growth and proliferation rates. Specifically blocking these processes is likely to provide new insights to the role of glucose transport and metabolism in tumorigenesis, as well as in apoptosis. As solid tumors outgrow the surrounding vasculature, they encounter microenvironments with a limited supply of nutrients leading to a glucose deprived environment in some regions of the tumor. Cancer cells living in the glucose deprived environment undergo changes to prevent glucose deprivation-induced apoptosis. Knowing how cancer cells evade apoptosis induction is also likely to yield valuable information and knowledge of how to overcome the resistance to apoptosis induction in cancer cells.Type: ApplicationFiled: March 24, 2011Publication date: May 17, 2012Applicant: OHIO UNIVERSITYInventors: Xiaozhuo Chen, Stephen Bergmeier
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Patent number: 8178579Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.Type: GrantFiled: July 17, 2007Date of Patent: May 15, 2012Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Scott M. Sternson, Jason C. Wong, Christina M. Grozinger, Stephen J. Haggarty, Kathryn M. Koeller
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Publication number: 20120115850Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.Type: ApplicationFiled: May 10, 2011Publication date: May 10, 2012Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
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Publication number: 20120108631Abstract: The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.Type: ApplicationFiled: October 26, 2011Publication date: May 3, 2012Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Tzofit Kehat, Sima Mirilashvili, Alex Aizikovich, Daniel Sherman, Vered Behar, Osnat Kashtan
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PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF SALICYLANILIDES FOR TREATMENT OF HEPATITIS VIRUSES
Publication number: 20120108592Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol -
Publication number: 20120101143Abstract: The invention provides compositions, pharmaceutical preparations and methods for increasing activity (e.g., ion transport) of the mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR), e.g., DF508 CFTR, G551D-CFTR, G1349D-CFTR, or D1152H-CFTR, that are useful for the treatment of cystic fibrosis (CF). The compositions and pharmaceutical preparations of the invention may comprise one or more phenylglycine-containing compounds or sulfonamide-containing compounds of the invention, or an analog or derivative thereof.Type: ApplicationFiled: April 15, 2011Publication date: April 26, 2012Inventors: Alan Verkman, R. Kiplin Guy, Nicoletta Pedemonte, Luis J.V. Galietta
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Publication number: 20120093753Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.Type: ApplicationFiled: December 20, 2011Publication date: April 19, 2012Inventors: Michael J. Fevola, Frank C. Sun, Stacey E. York
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Publication number: 20120088783Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: September 26, 2011Publication date: April 12, 2012Applicant: Ampere Life Sciences, Inc.Inventors: Bing WANG, Gail Walkinshaw, Donald R. James
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Publication number: 20120087882Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.Type: ApplicationFiled: December 20, 2011Publication date: April 12, 2012Inventors: Michael J. Fevola, Frank C. Sun, Stacey E. York
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Publication number: 20120088823Abstract: Provided is a composition for scalp and hair treatment, comprising a menthol derivative and a prostaglandin compound having two hetero atoms at the 15 position. The composition of the present invention is effective not only for preventing dandruff and itchy scalp but also for preventing or treating hair loss, baldness, or hair thinness.Type: ApplicationFiled: December 19, 2011Publication date: April 12, 2012Applicant: R-TECH UENO, LTD.Inventors: Masato IINO, Satoshi YAMAKI, Satoshi NAKANISHI, Masahiro TAJIMA, Ryuji UENO
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Publication number: 20120077871Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.Type: ApplicationFiled: November 24, 2010Publication date: March 29, 2012Applicant: TAPESTRY PHARMACEUTICALS, INC.Inventors: Jan ZYGMUNT, James FERRARA, James D. MCCHESNEY
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Publication number: 20120070476Abstract: The present disclosure includes compositions and methods of inactivating pathogens of a genital tract of a female. The compositions include L-lactic acid substantially free of D-lactic acid. In particular, an intravaginal ring for sustained release of L-lactic acid out of a reservoir containing multi-gram quantities of L-lactic acid, with minimal osmotically induced swelling or pressurization of the reservoir during prolonged use is provided.Type: ApplicationFiled: May 28, 2010Publication date: March 22, 2012Inventors: Thomas R. Moench, Deirdre E. O'Hanlon, Richard A. Cone
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Publication number: 20120071539Abstract: Methods and compositions comprising chemical compounds that modulate the silencing of a polynucleotide of interest in a cell are provided. Such chemical compounds when used in combination with an appropriate silencing element can be used to modulate (increase or decrease) the level of the polynucleotide targeted by the silencing element. Methods of using such compositions both in therapies involving RNAi-mediated suppression of gene expression, as well as, in vitro methods that allow for the targeted modulation of expression of a polynucleotide of interest are provided. Pharmaceutical or cosmetic compositions comprising such compounds and silencing elements also are disclosed. Methods for screening a compound of interest for the ability to modulate the activity of a heterologous silencing element also are provided.Type: ApplicationFiled: December 12, 2007Publication date: March 22, 2012Applicant: Emory UniversityInventor: Peng Jin
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Publication number: 20120071523Abstract: The instant invention provides novel benzofuran-4,5-diones and pharmaceutical compositions thereof useful for inhibiting PDF and for treating proliferative and infectious diseases. Compounds may be selective for eukaryotic (e.g., human) PDF or prokaryotic PDF.Type: ApplicationFiled: May 5, 2010Publication date: March 22, 2012Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: Hakim Djaballah, Christophe Antczak
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Publication number: 20120065257Abstract: The present invention is a method for the treatment or prevention of migraine comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment and/or prevention of migraine, which includes mono-therapy and alternatively, co-therapy with at least anti-migraine agent.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Inventor: Virginia L. Smith-Swintosky
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Publication number: 20120064062Abstract: Organic compounds showing the ability to inhibit bacterial omptin proteases, specifically Yersinia pestis plasminogen activator (Pla) are disclosed. The disclosed Y. pestis plasminogen activator inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by Y. pestis.Type: ApplicationFiled: September 13, 2011Publication date: March 15, 2012Inventors: Jon D. Goguen, Daniel Aiello, Donald T. Moir, Bing Li
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Publication number: 20120059012Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five- to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.Type: ApplicationFiled: May 12, 2010Publication date: March 8, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Akihito Fujii, Kazumi Niidome, Chiaki Migihashi, Toshiyuki Kamei, Takafumi Matsumoto, Tomoyuki Hirata
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Patent number: 8124651Abstract: Embodiments of the present invention relate to inhibitors of thioredoxin. Certain embodiments relate to palmarumycin based compounds and methods of using the same. Such compounds may be useful in inhibiting the overexpression of thioredoxin, inhibiting tumor growth and treating cancer.Type: GrantFiled: September 15, 2006Date of Patent: February 28, 2012Assignees: The University of Pittsburgh Office of Technology Transfer, Arizona Board of RegentsInventors: Garth Powis, Peter Wipf
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Publication number: 20120046238Abstract: A method for treating an infection with a virus. The method includes administering to a subject in need thereof an effective amount of one or more coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a pharmaceutical composition including a coumarin compound.Type: ApplicationFiled: November 10, 2011Publication date: February 23, 2012Applicant: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Tsu-An Hsu, Jiann-Yih Yeh, Jim-Tong Horng, Shin-Ru Shih, Sui-yuan Chang, Yu-Sheng Chao
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Publication number: 20120046320Abstract: The present invention discloses ?-diketones, ?-diketones or ?-hydroxyketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.Type: ApplicationFiled: August 17, 2011Publication date: February 23, 2012Applicant: WINTHERIX, LLCInventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga