Hetero Ring Attached Directly Or Indirectly To The Phenothiazine Ring Nitrogen By Acyclic Nonionic Bonding Patents (Class 514/225.2)
  • Patent number: 11266651
    Abstract: Provided herein is a pharmaceutical composition comprising two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a ?2-adrenoreceptor agonist. Also provided herein is a method of treating, preventing, or ameliorating a cardiovascular disease in a subject, comprising administering to the subject in need thereof two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a ?2-adrenoreceptor agonist.
    Type: Grant
    Filed: May 7, 2018
    Date of Patent: March 8, 2022
    Assignee: CARDIX Therapeutics, LLC
    Inventors: Jin Jean Wang, Gerald J. Yakatan, Ting N. Lin, Jing H. Gao
  • Patent number: 11260029
    Abstract: The present disclosure relates to methods of preventing or treating parasite infection in a plurality of fish in need thereof, comprising administering to the fish an effective amount of a medicated fish feed. The medicated fish feed comprises fish feed granules or pellets coated with a composition comprising a neonicotinoid such as imidacloprid and a carrier having a high apparent digestibility coefficient such as a processed/cooked corn protein concentrate.
    Type: Grant
    Filed: June 24, 2015
    Date of Patent: March 1, 2022
    Inventors: John O'Halloran, John Terence Drost
  • Patent number: 10456388
    Abstract: Disclosed herein is desloratadine or ebastin for use in treatment of a patient diagnosed with breast cancer. Also disclosed is desloratadine or ebastin for use in treatment of a patient diagnosed with a cancer type susceptible to immunotherapy.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: October 29, 2019
    Assignee: Belina Pharma AB
    Inventors: Hakan Olsson, Rickard Einefors
  • Patent number: 9884948
    Abstract: A porous material includes a polyhexahydrotriazine material. Pores in the porous material can be of various sizes including nanoscale sizes. The porous material may be used in a variety of applications, such as those requiring materials with a high strength-to-weight ratio. The porous material can include a filler material dispersed therein. The filler material can be, for example, a particle, a fiber, a fabric, or the like. In some examples, the filler material can be a carbon fiber or a carbon nanotube. A method of making a porous material includes forming a resin including a polyhemiaminal or polyhexahydrotriazine component and a polythioaminal component. The resin can be heated to promote segregation of the components into different phases with predominately one or the other component in each phase. Processing of the resin after phase segregation to decompose the polythioaminal component can form pores in the resin.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: February 6, 2018
    Assignee: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Dylan J. Boday, Mareva B. Fevre, Jeannette M. Garcia, James L. Hedrick, Rudy J. Wojtecki
  • Patent number: 9301955
    Abstract: This invention relates to tritoqualine for use in the treatment of cystic fibrosis or any one of its complications. The invention also relates to the method for the treatment of cystic fibrosis or any one of its complications by administering tritoqualine. The invention can be used to improve the condition of individuals with cystic fibrosis.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: April 5, 2016
    Assignee: ORPHAN SYNERGY EUROPE-PHARMA
    Inventor: Dominique Costantini
  • Patent number: 8962574
    Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Paul Anthony Reilly
  • Publication number: 20150037377
    Abstract: The present invention relates to substituted cellulose acetates and methods of use thereof. One embodiment of the present invention provides a coating having a substituted cellulose acetate having a polar substituent that has an oxygen atom covalently bonded to a nonmetal selected from the group of sulfur, phosphorus, and boron; wherein the nonmetal is present in at least about 0.01% by weight of the substituted cellulose acetate.
    Type: Application
    Filed: October 16, 2014
    Publication date: February 5, 2015
    Applicant: Celanese Acetate LLC
    Inventors: Michael T. Combs, Thomas S. Garrett
  • Publication number: 20150031686
    Abstract: Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 29, 2015
    Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
  • Publication number: 20140315897
    Abstract: Novel methods and compounds for treating Alzheimer's Disease are provided. In one aspect, the invention provides methods for treating Alzheimer's Disease by administering certain phenothiazine derivatives. In one embodiment, the methods include administering an effective amount of a 3-oxo-7-dialkyl-amino-phenothiazine derivative, or 3-oxo-7-dialkyl-amino-phenothiazine. In another embodiment, the invention provides methods for treating Alzheimer's Disease by administering an effective amount of a 3,7-diazetidin-1-yl-phenothiazine or a derivative thereof. In another aspect, the invention provides novel azetidinyl phenothiazine compounds.
    Type: Application
    Filed: July 3, 2014
    Publication date: October 23, 2014
    Inventors: Vishwanath Lingappa, Clarence R. Hurt
  • Patent number: 8865197
    Abstract: An encapsulated formulation for food and bioactive agent delivery to aquatic animals includes various combinations of nutrients, a digestion enhancer, bioactive agents, and a local absorption enhancer. The bioactive agents and absorption enhancer may be encapsulated within a delay layer for targeted release at an area of the digestive tract distinct from the region of nutrient release. The bioactive agents and absorption enhancer may be coated with a sticky coating so that they tend to adhere to the inner surfaces of the wall of the digestive tract, thereby localizing their release and enhancing their effect. Instead of bioactive agents themselves, precursors may be delivered so as to generate the bioactive agents locally. The encapsulated precursors of a specific bioactive agent are separately contained in capsules which themselves can be adhesive to one another.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: October 21, 2014
    Assignee: Israel Oceanographic and Limnological Research Ltd.
    Inventors: Amos Tandler, William Koven, Shalom Zemach
  • Patent number: 8846667
    Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: September 30, 2014
    Assignee: The General Hospital Corporation
    Inventors: Vineet Gupta, M. Amin Arnaout
  • Patent number: 8828986
    Abstract: 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: Grant
    Filed: April 20, 2012
    Date of Patent: September 9, 2014
    Assignee: Prosetta Antiviral Inc.
    Inventors: Clarence Hurt, Andy Atuegbu, Anatoliy Kitaygorodskyy, Beverly Freeman, Vishwanath Lingappa
  • Publication number: 20140243313
    Abstract: The invention disclosed herein is direct to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in treating neurodegenerative diseases and promoting the generation or survival of neurons in the mammalian brain. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to a method of promoting the generation or survival of neurons in a patient in need thereof in neurodegenerative and related diseases.
    Type: Application
    Filed: September 19, 2012
    Publication date: August 28, 2014
    Inventors: Austin Chih-Yu Chen, Jill Melissa Baccei, Brian Andrew Stearns, Nicholas Simon Stock, Yen Pham Truong
  • Patent number: 8809317
    Abstract: 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: Grant
    Filed: March 29, 2012
    Date of Patent: August 19, 2014
    Assignee: Prosetta Antiviral Inc.
    Inventors: Clarence R. Hurt, Vishwanath Lingappa, Beverly Freeman, Andy Atuegbu, Anatoliy Kitaygorodskyy
  • Publication number: 20140221286
    Abstract: It is discovered that sodium-channel blockers inhibit the secretion of glucagon from pancreatic alpha cells. The present disclosure, based on such discoveries, provides compositions and methods for the treatment of hyperglycemia and related diseases and conditions with Na-channel blockers.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 7, 2014
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Patent number: 8796448
    Abstract: Novel methods and compounds for treating Alzheimer's Disease are provided. In one aspect, the invention provides methods for treating Alzheimer's Disease by administering certain phenothiazine derivatives. In one embodiment, the methods include administering an effective amount of a 3-oxo-7-dialkyl-amino-phenothiazine derivative, or 3-oxo-7-dialkyl-amino-phenothiazine. In another embodiment, the invention provides methods for treating Alzheimer's Disease by administering an effective amount of a 3,7-diazetidin-1-yl-phenothiazine or a derivative thereof. In another aspect, the invention provides novel azetidinyl phenothiazine compounds.
    Type: Grant
    Filed: December 9, 2011
    Date of Patent: August 5, 2014
    Assignee: Prosetta Antiviral Inc.
    Inventors: Vishwanath Lingappa, Clarence R. Hurt
  • Patent number: 8795630
    Abstract: Compounds useful for the early diagnosis of malignant tumors, multiple sclerosis, and especially Alzheimer's Disease and related dementias; especially compounds of Formula (I) wherein R1 is selected from the group consisting of hydrogen, cyano, fluoro, iodo, alkyl, and aryl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; X is selected from the group consisting of CH2, CH2O, oxygen, OCH2, CH2S, SCH2, NH, N-alkyl, and N-aryl; Y is an optional spacer group, absent or selected from the group consisting of oxygen, sulfur, NH, N-alkyl, and N-aryl; and Z is selected from the group consisting of alkyl substituted with cyano, fluoro, or iodo and aryl substituted with cyano, fluoro, or iodo. In a preferred embodiment, R1 and R2 are hydrogen, X is CH2O, Y is absent, and Z is phenyl substituted with fluoro, cyano, or iodo. In some embodiments, Z is more specifically 18F-phenyl or 123I-phenyl or 131I-phenyl. Other compounds are also provided.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: August 5, 2014
    Assignee: Treventis Corporation
    Inventors: Sultan Darvesh, Eric Joy, Earl Martin, Ian Macdonald, Ian Pottie
  • Patent number: 8765742
    Abstract: Three dihydrate forms B, C and D and a monohydrate form E of methylthioninium chloride are described. Forms B, C, D and E can be prepared under controlled humidity and temperature from methylthioninium chloride with higher water content or conversion of a hydrate. The hydrates can be incorporated in pharmaceutical compositions.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: July 1, 2014
    Assignee: Wista Laboratories Ltd.
    Inventors: Rolf Hilfiker, Timo Rager
  • Patent number: 8759336
    Abstract: Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: June 24, 2014
    Assignee: Prosetta Antiviral Inc.
    Inventors: Clarence R. Hurt, Vishwanath Lingappa, Beverly Freeman, Andy Atuegbu, Anatoliy Kitaygorodorskyy
  • Patent number: 8758822
    Abstract: The present invention relates to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, and more particularly, to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, including a first step of dissolving a biodegradable polymer in a non-volatile polar organic solvent, a second step of adding poorly soluble drugs to water and the biodegradable polymer solution to produce a dispersion, and a third step of adding the dispersion to emulsifier solutions in a batch under the condition of low mechanical energy level stirring.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: June 24, 2014
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Bong Hyun Chung, Yong Taik Lim, Jung Hyun Han
  • Patent number: 8754074
    Abstract: The present invention relates to the use of the vinyl quinuclidine enantiomer (R) of the following formula 2 as a synthesis intermediate in the preparation of (R)-mequitazine.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: June 17, 2014
    Assignees: Pierre Fabre Medicament, Commissariat a l'Energie Atomique et aux Energies Alternatives
    Inventors: Marc Nicolas, Laurent Larquetoux, Sébastien Leroux, Eric Doris
  • Publication number: 20140113890
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
  • Patent number: 8642591
    Abstract: The present invention relates to a composition containing at least one amidine derivative or carboxamide derivative of general formula (I) or (A) in combination with at least one compound chosen from steroids, corticoids or corticosteroids, wherein said composition is suitable for the preparation of a medicament.
    Type: Grant
    Filed: March 6, 2007
    Date of Patent: February 4, 2014
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Bernadette Pignol, Serge Auvin, Dennis Bigg, Pierre-Etienne Chabrier de Lassauniere
  • Publication number: 20130310348
    Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).
    Type: Application
    Filed: July 25, 2013
    Publication date: November 21, 2013
    Applicants: State University
    Inventors: David H. Peyton, Steven Burgess
  • Patent number: 8440821
    Abstract: Described is a method for the synthesis and/or purification of a high purity diaminophenothiazinium compound of the following formula: characterized by a purity of greater than 98% and less than 1% Azure B, 0.15% Azure A, 0.15% Azure C and 0.05% Methylene Violet Bernthsen (MVB), as impurities. Also described are related high purity compounds, compositions, and methods of using such compounds and compositions. The compounds and compositions are useful in the treatment of diseases caused by tau aggregation, such as Alzheimer's disease and other dementias, and infection.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: May 14, 2013
    Assignee: Wista Laboratories Ltd.
    Inventors: Claude Michel Wischik, John Mervyn David Storey, Colin Marshall, James Peter Sinclair, Thomas Craven Baddeley
  • Publication number: 20130045967
    Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.
    Type: Application
    Filed: September 13, 2012
    Publication date: February 21, 2013
    Inventors: Vineet Gupta, M. Amin Arnaout
  • Publication number: 20120301402
    Abstract: A method for assessing if a subject has or is at risk of developing cardiac arrhythmia is described. The method includes determining the activity of Rap1A protein in a bodily sample of the subject and comparing the activity of Rap1A protein from the bodily sample of the subject to at least one Rap1A control. A decreased level of Rap1A activity in the bodily sample of the subject as compared to the at least one Rap1A control indicates that the subject is at risk of developing or has cardiac arrhythmia. Methods for evaluating the efficacy of treatment of a subject having decreased Rap1A activity with an antiarrhythmic agent are also described.
    Type: Application
    Filed: April 27, 2012
    Publication date: November 29, 2012
    Applicant: NATIONWIDE CHILDREN'S HOSPITAL, INC.
    Inventors: Maqsood Ahmed Chotani, John Anthony Bauer, Mandar Shankar Joshi, Selvi Chrysolyte Jeyaraj
  • Publication number: 20120302556
    Abstract: 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: Application
    Filed: March 29, 2012
    Publication date: November 29, 2012
    Applicant: PROSETTA ANTIVIRAL INC.
    Inventors: Clarence R. Hurt, Vishwanath Lingappa, Beverly Freeman, Andy Atuegbu, Anatoliy Kitaygorodskyy
  • Publication number: 20120270854
    Abstract: 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: Application
    Filed: April 20, 2012
    Publication date: October 25, 2012
    Applicant: PROSETTA ANTIVIRAL INC.
    Inventors: Clarence Hurt, Vishwanath Lingappa, Beverly Freeman, Anatolly Kitaygorodskyy, Andy Atuegbu
  • Publication number: 20120238543
    Abstract: Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV.
    Type: Application
    Filed: March 16, 2012
    Publication date: September 20, 2012
    Applicant: Prosetta Antiviral, Inc.
    Inventors: Clarence Hurt, Beverly Freeman, Vishwanath Lingappa, Andy Atuegbu, Anatoliy Kitaygorodskyy
  • Patent number: 8268816
    Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. For example, one such compound useful as an agonist of integrin CD11b/CD18 is the compound of Formula (I): Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: September 18, 2012
    Inventors: Vineet Gupta, M. Amin Arnaout
  • Patent number: 8207146
    Abstract: The present invention relates to substituted phenothiazines with a double bond and physiologically acceptable salts thereof, and their use as a medicament.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: June 26, 2012
    Assignee: Sanofi-Aventis
    Inventors: Stefanie Keil, Elisabeth Defossa, Dieter Schmoll, Axel Dietrich, Johanna Kuhlmann-Gottke, Karl-Christian Engel
  • Patent number: 8143245
    Abstract: This invention relates to the use of 10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine as well as its pharmaceutically acceptable salts for the preparation of a drug having the particularity of treating or preventing urinary incontinence, by local and/or oral route.
    Type: Grant
    Filed: December 26, 2007
    Date of Patent: March 27, 2012
    Assignee: Pierre Fabre Medicament
    Inventors: Thierry Clerc, Jacky Tisne-Versailles, Christophe Przybylski
  • Publication number: 20120065187
    Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
    Type: Application
    Filed: November 21, 2011
    Publication date: March 15, 2012
    Applicants: ALCON RESEARCH, LTD, KALYPSYS, INC.
    Inventors: Allen J. Borchardt, Clay Beauregard, Travis Cook, Robert L. Davis, Daniel A. Gamache, John M. Yanni
  • Publication number: 20110306576
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: December 15, 2011
    Applicant: PHARMALUCIA LIMITED
    Inventor: Mark Wainwright
  • Publication number: 20110269703
    Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 10, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Paul Anthony Reilly
  • Publication number: 20110269815
    Abstract: The present invention is directed to methods of reducing cancer cell proliferation and/or treating cancer by administering a therapeutically effective amount of a compound that inhibits the activity of ACSVL3.
    Type: Application
    Filed: June 25, 2009
    Publication date: November 3, 2011
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Paul A. Watkins, John Laterra
  • Publication number: 20110165259
    Abstract: [Problem to be Solved] The purpose of present invention is to provide a medicine which has low contamination with a fine-pulverizing medium, is safe and has improved bioavailability. [Solution] A method for producing a composite organic compound powder for medical use is used which comprises: mixing a poorly water-soluble and crystalline organic compound powder, a physiologically acceptable salt, a physiologically acceptable polyol, and a carboxyvinyl polymer and fine-pulverizing the organic compound powder; and removing at least the salt and the polyol during or after fine-pulverizing.
    Type: Application
    Filed: September 15, 2009
    Publication date: July 7, 2011
    Applicant: ACTIVUS PHARMA CO., LTD.
    Inventors: Takashi Hirokawa, Takahiro Tada, Jun Nihira
  • Publication number: 20110144043
    Abstract: The present invention is directed to methods, kits and compositions for modulating the activity of Stat molecules (e.g., Stat1, Stat3 and Stat5). The compounds of the invention are useful for treating and/or preventing disorders characterized by Stat dysregulation, such as hyperproliferative disorders. Further, the compounds of the present invention are also useful in culturing stem cells and treating ischemic disorders.
    Type: Application
    Filed: December 11, 2009
    Publication date: June 16, 2011
    Applicant: Dana-Farber Cancer Institute
    Inventor: David A. Frank
  • Patent number: 7956183
    Abstract: 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: Grant
    Filed: July 10, 2007
    Date of Patent: June 7, 2011
    Assignee: WisTa Laboratories Ltd.
    Inventors: Claude Michel Wischik, John Mervyn David Storey, Colin Marshall, James Peter Sinclair, Thomas Craven Baddeley
  • Publication number: 20110086023
    Abstract: The invention provides a topical pharmaceutical composition for application to the nasal or ocular mucosa which comprises (1) a pharmaceutical excipient suitable for topical administration, (2) a mucosal adjuvant, (3) an antihistamine drug and (4) a mast cell stabilizer, a non-steroidal anti-inflammatory drug, a phosphodiesterase inhibitor, an anti-IgE agent, heparin, a topical steroid or a leukotriene blocker.
    Type: Application
    Filed: December 20, 2010
    Publication date: April 14, 2011
    Applicant: Fairfield Clinical Trials LLC
    Inventor: Edward M. Lane
  • Publication number: 20110014127
    Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.
    Type: Application
    Filed: January 5, 2009
    Publication date: January 20, 2011
    Inventor: Bernard P. Schachtel
  • Publication number: 20100273752
    Abstract: The present application relates to the use of 10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine, 10-[(3S)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine or 10-[(3R,3S)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine, or a pharmaceutically acceptable salt thereof, to prepare a drug to prevent or treat pathologies involving histamine H4 receptor.
    Type: Application
    Filed: December 4, 2008
    Publication date: October 28, 2010
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Thierry Clerc, Christophe Przybylski, Jacky Tisne-Versailles, Didier Cussac
  • Publication number: 20100273765
    Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, 4?- and/or 6? halo and/or alkoxy analogs, and various 5? substituents that incorporate a cyclic amine moiety.
    Type: Application
    Filed: June 21, 2007
    Publication date: October 28, 2010
    Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Joseph Raker, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
  • Publication number: 20100260669
    Abstract: Multi-dose active agent packages and methods for using the same for treating a subject for a condition are provided. Aspects of the invention include a multi-dose active agent package containing a plurality of unit dosage forms of an active agent configured to modulate at least a portion of a subject's autonomic nervous system during at least one season of the year. The active agent is present in an amount sufficient to alter the parasympathetic activity/sympathetic activity ratio of the subject in a manner effective to treat the subject for the condition. The subject active agent packages and methods find use in the treatment of a variety of different conditions, including disease conditions that increase in severity and/or occurrence during one or more seasons of the year. Also provided are kits for use in practicing the subject methods.
    Type: Application
    Filed: April 15, 2010
    Publication date: October 14, 2010
    Inventors: Anthony Joonkyoo Yun, Patrick Yuarn-Bor Lee
  • Publication number: 20100254910
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Application
    Filed: June 11, 2010
    Publication date: October 7, 2010
    Applicant: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Publication number: 20100222257
    Abstract: Disclosed herein are substituted phenethylamine alpha adrenergic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: May 17, 2010
    Publication date: September 2, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20100173891
    Abstract: The compounds of the present invention are of formula I: wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.
    Type: Application
    Filed: March 16, 2010
    Publication date: July 8, 2010
    Inventors: Brian Herbert, Wenge Xie, Truc Minh Nguyen, Allen T. Hopper, Ashok Tehim
  • Patent number: 7749982
    Abstract: The present invention relates to a complex that includes mequitazine, a cyclodextrin, and an interaction agent wherein the rate of solubilization in water of complexed mequitazine, measured for a 2 g/l mixture of mequitazine in water at 35° C. after 15 minutes of stirring, is greater than 50% at pH 9. The present invention also relates to a method of preparing the aforementioned complex and a pharmaceutical composition of which the complex is a part.
    Type: Grant
    Filed: October 19, 2005
    Date of Patent: July 6, 2010
    Assignee: Pierre Fabre Medicament
    Inventors: Bernard Freiss, Hubert Lochard
  • Publication number: 20100160298
    Abstract: The topical use of 5,6,7-trihydroxyheptanoic acid and analogs alone or in combination with histamine antagonists and/or mast cell stabilizers is disclosed for the treatment of ocular allergy.
    Type: Application
    Filed: February 8, 2010
    Publication date: June 24, 2010
    Applicant: Alcon Research, Ltd.
    Inventors: Peter G. Klimko, Clay Beauregard