Plural Hetero Atoms In The Tetracyclo Ring System (e.g., Acronycines, Etc.) Patents (Class 514/285)
  • Publication number: 20130216520
    Abstract: Biomass (e.g., plant biomass, animal biomass, microbial, and municipal waste biomass) is processed to produce useful products, such as food products and amino acids.
    Type: Application
    Filed: November 9, 2010
    Publication date: August 22, 2013
    Applicant: XYLECO, INC.
    Inventor: Marshall Medoff
  • Publication number: 20130217675
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 22, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130190294
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: March 7, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc
  • Publication number: 20130190293
    Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: July 25, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130190308
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130184303
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130184304
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Applicant: Medivation Technologies, Inc.
    Inventor: Medivation Technologies, Inc.
  • Patent number: 8481572
    Abstract: Provided is a pharmaceutical composition including as an active component a compound of formula (I): wherein X and (R1)n are as defined, and a physiological acceptable carrier. Also provided is a method for treating cancer including administering to an individual in need of such treatment an effective amount of the presently described pharmaceutical composition.
    Type: Grant
    Filed: August 10, 2008
    Date of Patent: July 9, 2013
    Assignee: Urifer Ltd.
    Inventors: Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen
  • Publication number: 20130172320
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: July 4, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130158063
    Abstract: Disclosed are compounds, compositions and methods related PPAR antagonists. Certain compounds are effective at inhibiting PPARs. The compositions can be used to inhibit PPARs, treat cancer and treat metabolic disorders.
    Type: Application
    Filed: August 24, 2011
    Publication date: June 20, 2013
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Milton Lang Brown, Yali Kong, Yong Liu, Robert Glazer, York Tomita
  • Publication number: 20130143878
    Abstract: The invention described herein pertains to substituted dibenzonaphthyridine compounds, pharmaceutical compositions, and formulations comprising the dibenzonaphthyridine compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.
    Type: Application
    Filed: August 17, 2011
    Publication date: June 6, 2013
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Mark S. Cushman, Evgeny A. Kiselev
  • Publication number: 20130137635
    Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.
    Type: Application
    Filed: February 9, 2011
    Publication date: May 30, 2013
    Applicant: LEXICON PHARMACEUTICALS, INC.
    Inventor: Arthur Thomas Sands
  • Publication number: 20130131091
    Abstract: The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. wherein Het represents pyridyl; X represents an oxygen atom; R1, R2, R3, R7, R10a, R10b, R11, and R12 represent a hydrogen atom; R4, R5, and R6 represent a hydrogen atom, hydroxyl, optionally substituted C1-18 alkylcarbonyloxy, optionally substituted C1-18 alkylsulfonyloxy, optionally substituted arylcarbonyloxy, C1-6 alkyloxy-C1-6 alkyloxy, C1-6 alkyloxy-C1-6 alkyloxy-C1-6 alkyloxy; R8 represents a hydrogen atom; and R13a, R13b, and R13c represent methyl.
    Type: Application
    Filed: May 23, 2011
    Publication date: May 23, 2013
    Inventors: Kimihiko Goto, Ryo Horikoshi, Kazuhiko Oyama, Yoshimasa Fukuda, Nozomu Nakanishi, Masato Tani, Nobuto Minowa, Masaaki Mitomi, Satoshi Omura, Toshiaki Sunazuka, Hiroshi Tomoda
  • Publication number: 20130122081
    Abstract: The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provides methods of making the liposome compositions provided by the present invention.
    Type: Application
    Filed: October 17, 2012
    Publication date: May 16, 2013
    Inventors: Keelung Hong, Daryl C. Drummond, Dmitri Kirpotin
  • Patent number: 8431564
    Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: April 30, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
  • Publication number: 20130071353
    Abstract: Inhibitors of retroviral propagation, methods of treatment and prevention of retroviral infections using the inhibitors, and pharmaceutical compositions including the inhibitors, are disclosed.
    Type: Application
    Filed: March 14, 2011
    Publication date: March 21, 2013
    Applicant: TRANA DISCOVERY, INC
    Inventors: Richard H. Guenther, Jerzy R. Szewczyk
  • Publication number: 20130053367
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: February 28, 2013
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain, Michael John Green
  • Publication number: 20130053363
    Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Publication number: 20130039904
    Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.
    Type: Application
    Filed: August 2, 2010
    Publication date: February 14, 2013
    Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.
    Inventor: Lifeng Xu
  • Publication number: 20120316192
    Abstract: The present invention relates to novel substituted indolo[2,3-a]quinolizines and stereoisomeric forms thereof and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these substituted indolo[2,3-a]quinolizines together with pharmaceutically acceptable carrier, excipient and/or diluents. Said novel substituted indolo[2,3-a]quinolizines have been identified as useful for the prophylaxis and treatment of cancer by the induction of strong mitotic delays, chromosomal misalignments and mitotic tri- and multipolarization leading to cell cycle stop and apoptosis. Furthermore a synthesis for preparation of the substituted indolo[2,3-a]quinolizines is disclosed in the present invention.
    Type: Application
    Filed: February 29, 2012
    Publication date: December 13, 2012
    Inventors: Herbert Waldmann, Kamal Kumar, Katja Hübel, Verena Pries, Heiko Dückert, Sascha Menninger, Slava Ziegler, Hanna Bruss, Vivek Khedkar, Vincent Eschenbrenner
  • Publication number: 20120308608
    Abstract: Provided herein are Compounds that induce interferon production and methods for identifying such Compounds. Also provided herein are compositions comprising such Compounds and methods of using such Compounds to treat interferon-sensitive diseases such as viral infections, cancer, and multiple sclerosis.
    Type: Application
    Filed: January 31, 2011
    Publication date: December 6, 2012
    Inventors: Megan Shaw, Mila Ortigoza, Adolfo Garcia-Sastre, Peter Palese
  • Patent number: 8324237
    Abstract: The invention includes processes mainly for the treatment of a inflammatory diseases, such as inflammatory bowel disease, arthritis, atherosclerosis, asthma, allergy, inflammatory kidney disease, circulatory shock, multiple sclerosis, chronic obstructive pulmonary disease, skin inflammation, periodontal disease, psoriasis and T cell-mediated diseases of immunity, including allergic encephalomyelitis, allergic neuritis, transplant allograft rejection, graft versus host disease, myocarditis, thyroiditis, nephritis, systemic lupus erthematosus, and insulin-dependent diabetes mellitus. The processes involve treating a patient with a pharmaceutical composition containing an active ingredient that inhibits the activity of sphingosine kinase.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: December 4, 2012
    Inventors: Charles D. Smith, Kevin J. French, Lynn W. Maines
  • Patent number: 8318766
    Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: November 27, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Zhihua Sui, Xuqing Zhang, Xiaojie Li
  • Publication number: 20120283215
    Abstract: Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.
    Type: Application
    Filed: September 14, 2010
    Publication date: November 8, 2012
    Applicants: The Regents of the University of California, a California Corporation, University of Texas at El Paso, Health and Human Services
    Inventors: Leonard M. Neckers, Marc B. Cox, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Tonos de Leon, Heather Balsiger, Robert Fletterick
  • Patent number: 8293762
    Abstract: Heteroarylpyridinone derivatives represented by formula (I) wherein R1, R2, R3, R4, R5, and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions including them and their use as therapeutic agents in the treatment of cancer and cell proliferation disorders.
    Type: Grant
    Filed: February 18, 2008
    Date of Patent: October 23, 2012
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Ermes Vanotti, Maria Menichincheri, Alessandra Scolaro
  • Publication number: 20120263659
    Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 18, 2012
    Applicants: BASF SE, SYMRISE AG
    Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
  • Patent number: 8273760
    Abstract: Disclosed herein are indolo[3,2-c]quinoline compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R and m are given the definitions as set forth in the Specification and Claims. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: September 25, 2012
    Assignee: Kaohsiung Medical University
    Inventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Jing-Jer Lin, Chih-Ming Lu
  • Publication number: 20120220610
    Abstract: The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed.
    Type: Application
    Filed: March 25, 2010
    Publication date: August 30, 2012
    Applicant: CORNELL UNIVERSITY
    Inventors: Richard A. Cerione, Jon W. Erickson, Kristin Wilson Cerione, Jianbin Wang
  • Patent number: 8247428
    Abstract: Indole alkaloid derivatives having an opioid receptor agonistic effect, their synthesis, and therapeutic compositions containing these derivatives, and methods of treating conditions with these compounds and therapeutic compositions, are provided.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: August 21, 2012
    Assignees: National University Corporation Chiba University, Josai University Corporation
    Inventors: Hiromitsu Takayama, Mariko Kitajima, Kenjiro Matsumoto, Syunji Horie
  • Publication number: 20120178759
    Abstract: The invention relates to the use of specific compounds of formula (I) and their pharmaceutically-acceptable salts: (Formula 1) (I) as a new family of protein kinase CK2 inhibitors; the invention also relates to the use of compounds of formula (I) for the preparation of pharmaceutical compositions for the prevention and/or treatment of disorders and/or diseases chosen Camongst cancers; autoimmune and inflammatory diseases; infectious diseases; diabetes angiogenesis related disorders; retinopathies and cardiac hypertrophy.
    Type: Application
    Filed: July 28, 2010
    Publication date: July 12, 2012
    Applicants: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENE ALT, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, INSTITUT NAT DE LA SAN ET DE LA RECH MED (INSERM)
    Inventors: Claude Cochet, Renaud Prudent, Virginie Moucadel, Chi-Hung N'guyen
  • Publication number: 20120165362
    Abstract: Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors, and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
    Type: Application
    Filed: March 6, 2012
    Publication date: June 28, 2012
    Inventors: Bijan Pedram, Cornelis Arjan Van Oeveren, Lin Zhi, Shuo Zhao, Yixing Shen
  • Patent number: 8198293
    Abstract: Compositions and methods for treating chronic infectious diseases using substantially pure oxymatrine or pharmaceutically acceptable salts or esters thereof are disclosed. In one embodiment described herein, the chronic infectious disease is chronic fatigue syndrome. Further described are compositions having an anti-infective amount of substantially pure oxymatrine or pharmaceutically acceptable salts or esters thereof.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: June 12, 2012
    Inventor: John K. S. Chia
  • Publication number: 20120129882
    Abstract: A synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds wherein said procedures provides an increment in the compounds biological activity. The compounds are further used for intra cellular binding, cytotoxicity on malignant cells through apoptosis activation mediated by mitochondrial damage, cellular organelles binding and damage, DNA fragmentation, marker of bacterial growth, antibacterial activity, cell cycle disruption, and a marker due to the auto-fluorescent properties.
    Type: Application
    Filed: February 1, 2012
    Publication date: May 24, 2012
    Inventors: Beatriz Zayas, Osvaldo Cox
  • Publication number: 20120108623
    Abstract: This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs.
    Type: Application
    Filed: October 4, 2011
    Publication date: May 3, 2012
    Applicant: Adolor Corporation
    Inventors: Bertrand Le Bourdonnec, Roland E. Dolle
  • Publication number: 20120107269
    Abstract: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the present application.
    Type: Application
    Filed: May 14, 2010
    Publication date: May 3, 2012
    Applicant: Tianjin Hemay Biotech Co., Ltd
    Inventors: Hesheng Zhang, Guanghuai Zeng, Yifei Gao
  • Patent number: 8158646
    Abstract: An indoloquinoline wherein the quarternary N-5 atom is a straight C(1-5) chain, a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring; the 10 position is N—R10, O, S, S?O, CH2, or C?O, where R10 is a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring. In one embodiment the quarternary N-5 atom is —CH3 and the 10 position is N—(CH2)5—Ph.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: April 17, 2012
    Assignee: Florida Agricultural and Mechanical University
    Inventor: Seth Y. Ablordeppey
  • Publication number: 20120083488
    Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).
    Type: Application
    Filed: June 9, 2010
    Publication date: April 5, 2012
    Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
  • Publication number: 20120058940
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 1, 2010
    Publication date: March 8, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG
  • Patent number: 8129530
    Abstract: The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: March 6, 2012
    Assignee: H. Lundbeck A/S
    Inventors: Morten Jorgensen, Benny Bang-Andersen, Ask Puschl, Niels Mork, Jennifer Larsen
  • Publication number: 20120041017
    Abstract: Pyridocarbazole-type compounds of formula (I): are provided as a medicament, and more particularly for application in anticancer chemotherapy. Also provided is a pharmaceutical composition with the compound and methods for preventing and/or treating neurodegenerative-type pathologies, such as Alzheimer's disease and schizophrenia, parasitoses, such as malaria, or glaucomas.
    Type: Application
    Filed: February 19, 2010
    Publication date: February 16, 2012
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, COMMISSARIAT A L ' ENERGIE ATOMIQUE ET AUX ENE ALT, INSTITUT CURIE
    Inventors: Laurence Lafanechere, Emilie Vassal, Caroline Barette, ChiHung Nguyen, Christian Rivalle, Renaud Prudent
  • Publication number: 20120035198
    Abstract: Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections.
    Type: Application
    Filed: July 8, 2011
    Publication date: February 9, 2012
    Inventors: Mohammad Javad Aman, Sina Bavari, James C. Burnett, Kelly Lyn Warfield
  • Publication number: 20120028908
    Abstract: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.
    Type: Application
    Filed: October 1, 2011
    Publication date: February 2, 2012
    Applicant: Abbott Laboratories
    Inventors: Shekhar VISWANATH, Larry Bartelt, Robert Leanna, Michael Rasmussen, Madhup Dhaon, Rodger Henry, Thomas Borchardt, Shuang Chen, Geoff Zhang
  • Publication number: 20120021036
    Abstract: The invention provides nanostructures or products of manufacture for use as ex vivo or in vivo composition (e.g., a drug, or a therapeutic, diagnostic or imaging reagent) delivery vehicles. In one aspect, the invention provides nanoparticles comprising several compartments which in unison function as a composite nanostructure. In one embodiment, the nanoparticles of the invention comprise a combination of polymer core/lipid bilayer interface which incorporate covalently attached lipid-vascular targeting ligands. These composite nanoparticles can deliver highly effective and selective payloads for diagnostic, prophylactic or therapeutic applications.
    Type: Application
    Filed: January 14, 2010
    Publication date: January 26, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Bharat Majeti, Eric Murphy, Wolfgang Wrasidlo, David Cheresh
  • Patent number: 8093390
    Abstract: Fused [1,2]imidazo[4,5-c] ring compounds, e.g., fused [1,2]imidazo[4,5-c]quinolines and [1,2]imidazo[4,5-c]naphthyridines, with a substituent, e.g., a substituted alkoxy substituent, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: January 10, 2012
    Assignee: 3M Innovative Properties Company
    Inventors: Michael J. Rice, Bryon A. Merrill, Philip D. Heppner
  • Publication number: 20110306603
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: August 23, 2011
    Publication date: December 15, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Patent number: 8067401
    Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: November 29, 2011
    Assignee: International Patent Holdings LLC
    Inventors: Paul Kiprono Chepkwony, Maria Medina, Mitchell Medina
  • Patent number: 8067432
    Abstract: A method for preparing a stable dispersion of a camptothecin, camptothecin prodrug, or analog thereof for administration to a patient in need thereof includes preparing a solution of the camptothecin, wherein the solution has a pH which places substantially an entirety of that camptothecin in a carboxylate form. The camptothecin may be a neutral camptothecin. The solution is next loaded into a liposome including at least one lipid, which may be a phospholipid. An intraliposomal pH is maintained which preserves substantially an entirety of the camptothecin in the carboxylate form. The liposomal dispersion is administered to an individual in need thereof, whereby the liposomes accumulate at and permeate into tumor tissue and an active, lactone form camptothecin is released in situ at the tumor site. Compositions formulated in accordance with the described method for treatment of a cancer in an animal in need thereof are provided also.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: November 29, 2011
    Assignee: University of Kentucky Research Foundation
    Inventors: Bradley D. Anderson, Vijay Joguparthi, Tian-Xiang Xiang
  • Publication number: 20110269790
    Abstract: The present invention provides compounds and pharmaceutically acceptable salts thereof methods for synthesizing thienopyridines and methods for inhibiting TNF-? activity for the treatment of cancer, asthma, arthritis, diabetes and inflammation. Provided are compounds of formula (I).
    Type: Application
    Filed: January 5, 2010
    Publication date: November 3, 2011
    Inventors: Shireesha Boyapati, Akkinepally Raghuram Rao, Banda Narsaiah, Prakash V. Diwan, Sistla Ramakrishna, Madhusudhana, Tallapally Yakaiah
  • Patent number: 8048862
    Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: November 1, 2011
    Assignee: InterMune, Inc.
    Inventors: Scott D. Seiwert, Leonid Beigelman, Brad Buckman, Antitsa Dimitrova Stoycheva, Steven B. Porter, Williamson Ziegler Bradford, Vladimir Serebryany
  • Publication number: 20110245272
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: September 23, 2010
    Publication date: October 6, 2011
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty