The Hetero Ring Contains Plural Ring Nitrogens Patents (Class 514/225.8)
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Patent number: 8383617Abstract: A method of treatment for the prevention or therapy of a protein aggregation disease includes the administration in combination of a first active medicament and a second active medicament, wherein the first active medicament is active to impede aggregation of amyloid protein and the second active medicament is active to disaggregate previously formed aggregates of amyloid protein.Type: GrantFiled: January 30, 2008Date of Patent: February 26, 2013Assignee: PAD Pharma LimitedInventors: Stuart Mark Wilson, Christopher John Stanley
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Patent number: 8377929Abstract: Novel crystalline form of perphenazine 4-aminobutyrate trimesylate and a process of producing the same are disclosed. The novel crystalline form is characterized by a unique XRPD pattern and a DSC that exhibits an endothermic peak at a relatively high temperature (e.g., higher than 209° C.). Also disclosed are a process of preparing perphenazine 4-aminobutyrate trimesylate by in situ deprotection and salification, in a single-step synthesis, and a highly pure perphenazine 4-aminobutyrate trimesylate obtained thereby. Uses of any of the described perphenazine 4-aminobutyrate trimesylate are also disclosed.Type: GrantFiled: February 24, 2011Date of Patent: February 19, 2013Assignees: Ramot at Tel-Aviv University Ltd., Bar-Ilan University, BioLineRX Ltd.Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman, Mazal Shaul, Efrat Halbfinger
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Publication number: 20130035304Abstract: This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: January 31, 2011Publication date: February 7, 2013Inventors: Loren D. Walensky, Michelle L. Stewart, Nicole Cohen
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Publication number: 20130024953Abstract: The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.Type: ApplicationFiled: May 3, 2012Publication date: January 24, 2013Applicant: University of Pittsburgh - of the Commonwealth System of Higher EducationInventors: Stephen C. Pak, David Hirsch Perlmutter, Gary A. Silverman
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Publication number: 20120322753Abstract: The production method prepares a solid preparation by dissolving water-insoluble and/or water indissolvable alkaline active pharmaceutical ingredient in an acidifier-containing acid solution to obtain medicated acid liquid; homogeneously mixing alkalizer, adjuvants and the medicated acid liquid, and carrying out wet granulation. The alkalizer is a reagent to reduce the acidity of the mixture of the alkalizer and the medicated acid liquid relative to the acidity of the medicated acid liquid. The preparation method avoids the problems in mechanical pulverization, such as environmental pollution, great loss and serious security risks. This method is simply operated, has high safety coefficient and is convenient for industrialized production. Also disclosed is the solid preparation produced by the method. The solid preparation produced by the method has better dissolution performance than that produced by prior art, and has better or at least equivalent stability and content uniformity with prior art.Type: ApplicationFiled: December 28, 2010Publication date: December 20, 2012Applicants: SHANGHAI ZHONGXI SUNVE PHARMACEUTICAL CO., LTD., SHANGHAI ZHONGXI PHARMACEUTICAL COMPANYInventors: Siji Zheng, Bo Tan
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Publication number: 20120321575Abstract: The present invention relates to novel pharmaceutical or cosmetic compositions comprising at least one inhibitor of a sub-unit of AP-1 adaptor complex, of a kinesin interacting with AP-1, in particular Kif13A, or of the interaction between a sub-unit of AP-1 adaptor complex and said kinesin, as well as the use of same to manufacture a drug intended for the treatment of pigmentary disorders and as a depigmentation agent.Type: ApplicationFiled: August 8, 2012Publication date: December 20, 2012Applicants: INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Graca Raposo, Cédric Delevoye, Danièle Tenza, Ilse Hurbain
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Publication number: 20120309748Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.Type: ApplicationFiled: August 16, 2012Publication date: December 6, 2012Applicants: Bar-Ilan University, Ramot at Tel-Aviv University Ltd.Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-ad, Abraham Weizman
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Publication number: 20120302556Abstract: Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.Type: ApplicationFiled: March 29, 2012Publication date: November 29, 2012Applicant: PROSETTA ANTIVIRAL INC.Inventors: Clarence R. Hurt, Vishwanath Lingappa, Beverly Freeman, Andy Atuegbu, Anatoliy Kitaygorodskyy
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Publication number: 20120302557Abstract: The present invention relates to a method of photodynamic therapy and to a method of inducing a photocytoxic effect which comprises applying to an area to be treated an effective amount of a compound of formula in which R1, R2, R3 and R4 each independently is an optionally-substituted linear, branched or cyclic hydrocarbon group, or R1 and R2 together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring or R3 and R4 together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP? is a counteranion and P is 1, 2 or 3; except for the compounds in which —NR1R2 and —NR3R4 are the same and are selected from —N(CH3)2 or —N(CH2CH3)2; and exposing the area to light to activate the compound.Type: ApplicationFiled: April 23, 2012Publication date: November 29, 2012Applicant: Photopharmica LimitedInventors: Stanley Beames BROWN, Cassandra Claire O'Grady, John Griffiths, Kirste Joanne Mellish, Richard George Tunstall, David John Howard Roberts, David Ian Vernon
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Patent number: 8309543Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 23, 2012Date of Patent: November 13, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Hilgraf
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Publication number: 20120282307Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.Type: ApplicationFiled: July 19, 2012Publication date: November 8, 2012Applicant: Depomed, Inc.Inventors: Bret Berner, Sui Yuen Eddie Hou, Gloria M. Gusler
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Publication number: 20120277211Abstract: Methods and compositions that relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a SULT4A1-1 haplotype are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the haplotype status.Type: ApplicationFiled: November 4, 2010Publication date: November 1, 2012Applicant: SUREGENE LLCInventors: Timothy L. Ramsey, Mark D. Brennan
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Publication number: 20120270854Abstract: Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.Type: ApplicationFiled: April 20, 2012Publication date: October 25, 2012Applicant: PROSETTA ANTIVIRAL INC.Inventors: Clarence Hurt, Vishwanath Lingappa, Beverly Freeman, Anatolly Kitaygorodskyy, Andy Atuegbu
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Publication number: 20120245145Abstract: In the broadest aspect, the invention provides a composition for and a method of prophylactic and/or therapeutic treatment of a animal/mammal for any viral disease, mixed bacterial and viral infections, bacterial infections, bacterial endotoxins, bacterial exotoxins, autoimmune diseases, and cellular or humoral mediated allergic conditions that is caused by any virus that relies on the maintenance of specific calcium ion concentrations for the post ribosomal RNA synthesis processing of viral protein translation, transportation and processing of viral structural components by utilizing a therapeutic amount of a blocker selected from the group consisting of a calcium channel blocker, a metabolite thereof, a calmodulin blocker and a metabolite thereof, and a pharmaceutical acceptable diluent or carrier; and/or is caused by damage to the animal/mammal by a pathological immune response to antigens.Type: ApplicationFiled: December 3, 2010Publication date: September 27, 2012Inventor: Kenneth W. Adams
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Patent number: 8273341Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 8, 2011Date of Patent: September 25, 2012Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Michael Graupe, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard Mackman, Hyung-Jun Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Publication number: 20120208773Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.Type: ApplicationFiled: August 12, 2010Publication date: August 16, 2012Applicant: Valeant International (Barbados) SRLInventors: Andrew John Duffield, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
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Publication number: 20120201888Abstract: Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.Type: ApplicationFiled: January 10, 2012Publication date: August 9, 2012Applicant: CHARLESTON LABORATORIES, INC.Inventors: Paul Bosse, John Ameling, Bernard Schachtel, Ray Takigiku
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Patent number: 8236791Abstract: Provided are methods of determining whether a compound is an inhibitor of an S100 protein. The methods utilize a biosensor that comprises the S100 protein that has a covalently bound fluorescent dye at an amino acid residue of the S100 protein that becomes less exposed to the aqueous solution upon activation of the S100 protein, where the fluorescent dye has decreased fluorescence when exposed to the aqueous solution than when protected from exposure to the aqueous solution. Also provided are methods of treating a subject having metastatic cancer.Type: GrantFiled: August 10, 2006Date of Patent: August 7, 2012Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anne Reba Bresnick, Sarah Claire Garrett
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Publication number: 20120172292Abstract: This invention discloses a method for enhancing the efficacy of antimicrobial, anti-protozoa and anti-cancer treatments by co-administering an inhibitor of endogenous NO production and/or NO scavenger.Type: ApplicationFiled: September 10, 2010Publication date: July 5, 2012Applicant: NEW YORK UNIVERSITYInventors: Evgeny A. Nudler, Ivan Gusarov
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Patent number: 8202861Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 9, 2004Date of Patent: June 19, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E Gonzales, III, Andreas P Termin, Esther Martinborough, Nicole Zimmerman
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Publication number: 20120148604Abstract: The present invention, relates to methods including compounds, derivatives, antibodies, interfering RNA, biologies, polypeptides, dominant negative effectors, and their use in the treatment of neuropathic pain by inhibition of transient receptor potential (TRP) channels. In another embodiment, this invention relates to inhibitors, antagonists, and agonists of TRPC4. TRPC4 therapeutic agents and modulators include but are not limited to small molecule inhibitors, compounds, amino acid derivatives, polypeptides, RNA interference agents, natural chemicals, ligand derivatives, and ions. TRPC4 therapeutic agents and modulators are developed for the treatment of neuropathic pain, including but not limited to pain sensations such as nociception, hyperalgesia, allodynia, and loss of sensory function.Type: ApplicationFiled: August 20, 2010Publication date: June 14, 2012Applicant: TRANSPOSAGEN BIOPHARMACEUTICALS, INC.Inventors: Eric M. Ostertag, John Stuart Crawford
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Publication number: 20120128735Abstract: A method of treatment for epilepsy and other disease states is described, which comprises delivery of gabapentin in a gastric retained dosage form.Type: ApplicationFiled: November 21, 2011Publication date: May 24, 2012Applicant: DEPOMED, INC.Inventors: Bret BERNER, Sui Yuen Eddie HOU
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Publication number: 20120122792Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: PROMENTIS PHARMACEUTICALS, INC.Inventors: Edward M. Johnson, II, Daniel G. Lawton
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Publication number: 20120114767Abstract: An assay for a GCH1 allele and associated genotype for the screening, prediction, diagnosis, prognosis, treatment and treatment response of psychiatric, neuropsychiatric, and neurological disorders, such as schizophrenia, schizoaffective disorder and bipolar disorder, and for defining treatments of such disorders. The presence of a variant in the GCH1 gene, alone or in conjunction with a measurement of low or altered biopterin, or altered BH4 system measures, is used to screen or diagnose subjects at risk for developing a psychiatric, neuropsychiatric, or neurological disorder. The genetic assay, with or without a biopterin or BH4 system assay, may also be used to determine treatment regimens. For subjects with an impaired BH4 system, treatments to increase or normalize biopterin, BH4, or the BH4 system can also be used, such as BH4 supplementation, lithium treatment, phenylalanine treatment, or other treatments and therapies.Type: ApplicationFiled: December 12, 2011Publication date: May 10, 2012Applicant: THE RESEARCH FOUNDATION FOR MENTAL HYGIENEInventors: James D. Clelland, Catherine L. Clelland
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Publication number: 20120108545Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.Type: ApplicationFiled: May 19, 2010Publication date: May 3, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
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Patent number: 8168628Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.Type: GrantFiled: April 21, 2010Date of Patent: May 1, 2012Assignees: Ramot at Tel-Aviv University Ltd., Bar-Ilan UniversityInventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman
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Publication number: 20120064168Abstract: A method of treatment for epilepsy and other disease states is described, which comprises delivery of gabapentin in a gastric retained dosage form.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Applicant: DEPOMED, INC.Inventors: BRET BERNER, SUI YUEN EDDIE HOU
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Publication number: 20120064129Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Applicant: DEPOMED, INC.Inventors: Bret Berner, Sui Yuen Eddie Hou, Gloria M. Gusler
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Publication number: 20120035161Abstract: The invention includes compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, treating diseases associated with activated lymphocytes, or treating PAH.Type: ApplicationFiled: July 18, 2011Publication date: February 9, 2012Inventors: Stephen Roth, Bruce Tomczuk
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Patent number: 8088368Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: May 12, 2010Date of Patent: January 3, 2012Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Scott E. Lazerwith, Richard L. Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, William J. Watkins, Lianhong Xu
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Publication number: 20110319382Abstract: A composition, use of and a method of removing a hyperplastic skin lesion on a mammal comprising administering to the lesion or locus thereof a therapeutically effective amount of a composition comprising a blocker selected from the group consisting of a calcium channel blocker, a metabolite thereof, a calmodulin blocker and a metabolite thereof and a pharmaceutically acceptable diluent or carrier.Type: ApplicationFiled: October 29, 2009Publication date: December 29, 2011Inventor: Kenneth W. Adams
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Publication number: 20110312948Abstract: Novel crystalline form of perphenazine 4-aminobutyrate trimesylate and a process of producing the same are disclosed. The novel crystalline form is characterized by a unique XRPD pattern and a DSC that exhibits an endothermic peak at a relatively high temperature (e.g., higher than 209° C.). Also disclosed are a process of preparing perphenazine 4-aminobutyrate trimesylate by in situ deprotection and salification, in a single-step synthesis, and a highly pure perphenazine 4-aminobutyrate trimesylate obtained thereby. Uses of any of the described perphenazine 4-aminobutyrate trimesylate are also disclosed.Type: ApplicationFiled: February 24, 2011Publication date: December 22, 2011Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman, Mazal Shaul, Efrat Halbfinger
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Publication number: 20110306576Abstract: A compound of formula (II) or a pharmaceutically acceptable derivative thereof for use in a method of combating and/or detecting a pathogen; wherein X is selected from O, S and Se; each of R1, R2, R4, R6, R8, R9, R11, R12, R13 and R14 is independently selected from hydrogen, halogen, sulfo, sulfoxy, mercapto, acyl, nitro, amino or an optionally substituted alkyl, alkenyl, alkynyl, aryl, amine or alkoxy group; provided that at least one of R11, R12, R13 and R14 is an optionally substituted amine group.Type: ApplicationFiled: February 25, 2010Publication date: December 15, 2011Applicant: PHARMALUCIA LIMITEDInventor: Mark Wainwright
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Publication number: 20110281855Abstract: The present invention provides a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol. The present invention further provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol.Type: ApplicationFiled: April 21, 2011Publication date: November 17, 2011Applicant: GRUENENTHAL GMBHInventor: RAMESH SESHA
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Publication number: 20110274655Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.Type: ApplicationFiled: May 5, 2011Publication date: November 10, 2011Applicant: Infinity PharmaceuticalsInventors: Adilah BAHADOOR, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20110244020Abstract: The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1-3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 ?m, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided. The device contained in the kit typically, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Also disclosed, are methods for using these aerosols and kits.Type: ApplicationFiled: April 1, 2011Publication date: October 6, 2011Applicant: Alexza Pharmaceuticals, Inc.Inventors: Ron L. HALE, Craig C. Hodges, Peter M. Lloyd, Amy T. Lu, Daniel J. Myers, Joshua D. Rabinowitz, Martin J. Wensley, Jeffrey A. McKinney, Alejandro C. Zaffaroni
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Publication number: 20110223221Abstract: The present invention relates to processes of stabilization of cation radicals from one or more phenothiazinic compounds or derivatived compounds thereof. Another embodiment of the present invention relates to cosmeceutical formulations comprising one or more phenothiazinic compounds or derivatived compounds thereof, in combination with cosmeceutically acceptable excipients. The invention also relates to uses of one or more phenothiazinic compounds or derivatived compounds thereof, i the preparation of cosmeceutical formulations for the prevention of skin diseases and disturbances. Methods for prevention of skin diseases and disturbances are also disclosed by the present invention. Particularly, the embodiments of the present invention employ the cited one or more phenothiazinic compounds o derivatived compounds thereof in the form of their stabilized cation radicals.Type: ApplicationFiled: May 12, 2009Publication date: September 15, 2011Inventors: Iseli Lourenco Nantes, Tiago Rodrigues, Carolina Gregorutti Dos Santos
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Publication number: 20110218155Abstract: The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an ?1 helix, ?2 helix, a loop between ?1-?2, ?.6 helix, and select residues of ?4, ?.5, and ?.8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.Type: ApplicationFiled: October 9, 2009Publication date: September 8, 2011Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Loren D. Walensky, Evripidis Gavathiotis
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Publication number: 20110177999Abstract: The present invention relates to therapeutic combinations and kits useful in treating CFTR-related diseases, such as cystic fibrosis.Type: ApplicationFiled: August 7, 2008Publication date: July 21, 2011Inventors: Ashvani Singh, Jennings Franklin Worley, Gregor Zlokamik
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Publication number: 20110178073Abstract: Methods and articles of manufacture for use in improving a cognitive function, utilizing a conjugate comprising a first moiety having GABA agonist activity and a second moiety having CNS activity being covalently linked to the first moiety, are disclosed. Also disclosed are methods and articles of manufacture of preventing onset or inhibiting progression of a cognitive impairment or dysfunction utilizing the disclosed conjugate.Type: ApplicationFiled: December 9, 2010Publication date: July 21, 2011Inventors: Yona GEFFEN, Kinneret Savitsky, Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman
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Patent number: 7981885Abstract: The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.Type: GrantFiled: August 31, 2007Date of Patent: July 19, 2011Assignee: Immune Control Inc.Inventors: Stephen Roth, Clayton Buck, Christopher Self, Gary Olson
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Publication number: 20110151001Abstract: Disclosed is a novel pharmaceutical composition for external application for increasing the permeation of prochlorperazine or a pharmaceutically acceptable salt thereof through the skin to allow prochlorperazine or the pharmaceutically acceptable salt thereof to exhibit its excellent pharmacological activity. Specifically disclosed is a novel pharmaceutical composition for external application, which contains prochlorperazine or a pharmaceutically acceptable salt thereof as an active ingredient and further contains menthol. The composition contains, as an active ingredient, prochlorperazine which has been widely used clinically as the first-line drug of a therapeutic agent for nausea or vomiting before or after a surgery or the like, and is extremely highly useful as a transdermally absorbable antiemetic agent that has excellent efficacy and can be used safely over a long period.Type: ApplicationFiled: March 3, 2009Publication date: June 23, 2011Applicant: NIPPON ZOKI PHARMACEUTICAL CO., LTD.Inventors: Yasuko Obata, Yuki Otake, Kozo Takayama
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Publication number: 20110150775Abstract: The present invention provides systems for developing and/or testing therapies for prenatal diseases and conditions including Down Syndrome. The present invention also provides diagnostic methods for Down Syndrome involving, in some embodiments, gene expression analyses of fetal RNA and/or detection of expression of particular genes involved in Down Syndrome. Also provided are microarrays and kits useful in prenatal diagnostic applications.Type: ApplicationFiled: June 1, 2009Publication date: June 23, 2011Inventors: Donna Slonim, Kirby Johnson, Diana Bianchi
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Patent number: 7956183Abstract: A method for the synthesis of a diaminophenothiazinium compound of the following formula: comprising (a) purifying a corresponding reduced compound which is N-acylated at the heterocyclic nitrogen; (b) deacylating the purified compound to provide the corresponding reduced compound; and (c) oxidizing the reduced compound to provide the diaminophenothiazinium compound. Optional purification may performed, for example, after deacylating and after oxidizing. The method provides high purity diaminophenothiazinium compounds which are suitable for pharmaceutical and related therapeutic uses. Such uses include inactivating pathogens, the treatment of the infectious diseases, and for the treatment of diseases of protein aggregation, such as tauopathies, including Alzheimer's disease.Type: GrantFiled: July 10, 2007Date of Patent: June 7, 2011Assignee: WisTa Laboratories Ltd.Inventors: Claude Michel Wischik, John Mervyn David Storey, Colin Marshall, James Peter Sinclair, Thomas Craven Baddeley
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Publication number: 20110118189Abstract: Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.Type: ApplicationFiled: April 24, 2009Publication date: May 19, 2011Inventors: Stephen J. Farr, John Turanin, Roger Hawley, Jeffrey A. Schuster
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Publication number: 20110117214Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 15, 2010Publication date: May 19, 2011Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Ronald C. Newbold, Chengzhi Zhang
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Publication number: 20110105469Abstract: Methods and compositions that relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a SULT4A1-1 haplotype are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the haplotype status.Type: ApplicationFiled: November 3, 2010Publication date: May 5, 2011Applicant: Suregene, LLCInventors: Timothy L. Ramsey, Mark D. Brennan
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Publication number: 20110105467Abstract: Methods and compositions relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a SULT4A1-1 haplotype are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the haplotype status.Type: ApplicationFiled: August 18, 2010Publication date: May 5, 2011Inventors: TIMOTHY L. RAMSEY, MARK D. BRENNAN
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Publication number: 20110105468Abstract: Methods and compositions relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a SULT4A1-1 haplotype are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the haplotype status.Type: ApplicationFiled: August 18, 2010Publication date: May 5, 2011Inventors: Timothy L. Ramsey, Mark D. Brennan
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Publication number: 20110053866Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.Type: ApplicationFiled: August 12, 2010Publication date: March 3, 2011Applicant: Biovail Laboratories International (Barbados) S.R.L.Inventors: Andrew John Duffield, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai