Acyclic C-n=n-n Containing Patents (Class 514/151)
  • Patent number: 12110263
    Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
    Type: Grant
    Filed: May 9, 2022
    Date of Patent: October 8, 2024
    Assignee: Lighthouse Pharmaceuticals, Inc.
    Inventors: Andrei W. Konradi, Robert A. Galemmo, Jr., Stephen S. Dominy, Casey C. Lynch, Leslie J. Holsinger
  • Patent number: 11325884
    Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
    Type: Grant
    Filed: June 11, 2020
    Date of Patent: May 10, 2022
    Assignee: CORTEXYME, INC.
    Inventors: Andrei W. Konradi, Robert A. Galemmo, Jr., Stephen S. Dominy, Casey C. Lynch, Leslie J. Holsinger
  • Patent number: 11035848
    Abstract: The present invention relates to a system and method for identifying malignant cancer cells that produce anti-cancer compounds.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: June 15, 2021
    Inventor: Philip J. Weintraub
  • Patent number: 10730826
    Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: August 4, 2020
    Assignee: CORTEXYME, INC.
    Inventors: Andrei W. Konradi, Robert A. Galemmo, Jr., Stephen S. Dominy, Casey C. Lynch, Leslie J. Holsinger
  • Patent number: 10022449
    Abstract: The present invention relates to iota- and/or kappa-carrageenan in combination with a neuraminidase inhibitor for use as a medicament in the prophylactic or therapeutic treatment of a symptom, condition or disease caused by or associated with an infection by an influenza virus.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 17, 2018
    Assignee: MARINOMED BIOTECHNOLOGIE GmbH
    Inventors: Andreas Grassauer, Eva Prieschl-Grassauer, Christiane Meier, Marielle Konig-Schuster
  • Patent number: 9994586
    Abstract: The present invention provides a compound of Formula XXVIII: werein R1is H or CH3, and optionally including a salt or a hydrate of said compound.
    Type: Grant
    Filed: August 17, 2016
    Date of Patent: June 12, 2018
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9850221
    Abstract: Sulfated and unsulfated flavonoid oligomers as inhibitors of cancer stem cells (CSCs) are provided. In particular, sulfated flavonoid dimers are shown to selectively inhibit CSCs growth and self-renewal both in vitro and in vivo.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: December 26, 2017
    Assignee: VIRGINIA COMMONWEALTH UNIVERSITY
    Inventors: Umesh R. Desai, Rajesh Karuturi, Bhaumik B. Patel, Nirmita J. Patel
  • Patent number: 9187420
    Abstract: Disclosed is a compound of formula (I) wherein ‘a’ and R1-R5 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogs, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogs. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: November 17, 2015
    Assignee: Lupin Limited
    Inventors: Neelima Sinha, Gourhari Jana, Ajay Ramchandra Tilekar, Navnath Popat Karche, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150141378
    Abstract: Described herein are nitroxyl progenitor compounds, and compositions including, and methods or generating, the compounds thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions.
    Type: Application
    Filed: September 22, 2014
    Publication date: May 21, 2015
    Inventors: John P. Toscano, Christopher M. Pavlos, Preeya Kapur Boppana
  • Publication number: 20150105354
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20150105351
    Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 16, 2015
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Patent number: 8975280
    Abstract: A compound of Formula I are provided: wherein R is: R1 is a substituted or unsubstituted alkyl group; W1-4 are independently selected from hydrogen, substituted or unsubstituted alkyl groups, substituted or unsubstituted haloalkyl groups, substituted or unsubstituted alkanoyl groups, substituted or unsubstituted aroyl groups, or substituted or unsubstituted haloalkanoyl groups; X1-5 are independently selected from H, NO2, N3, and NH2; Y is absent or is a substituted or unsubstituted C1-alkyl group, other than carbonyl; Z is selected from a bond or NH, provided that when Z is a bond, Y is absent, and provided that when Z is NH, Y is a substituted or unsubstituted C1-alkyl group, other than carbonyl. Also provided are D-arabinitol compounds, methods for preparing such compounds and compositions of such compounds, and methods of using such compounds.
    Type: Grant
    Filed: May 22, 2007
    Date of Patent: March 10, 2015
    Assignee: The Chancellor, Masters and Scholars of The University of Oxford
    Inventors: Terry D. Butters, Raymond A. Dwek, George W. J. Fleet
  • Patent number: 8968733
    Abstract: A bioadherent composition includes a first mixture containing a plurality of reactive members of a specific binding pair, said reactive members being bound to a ligand capable of binding a receptor on biological tissue, and a second mixture containing a plurality of complementary reactive members of the specific binding pair, said complementary reactive members being bound to a ligand capable of binding a receptor on biological tissue, said reactive members capable of forming covalent bonds with said complementary reactive members via a reaction selected from Huisgen cycloaddition reactions, Diels-Alder reactions, and/or thiol-alkene reactions. A method for bonding biological tissue involves utilizing the bioadherent composition.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: March 3, 2015
    Assignee: Sofradim Production
    Inventor: Sebastien Ladet
  • Patent number: 8946302
    Abstract: The invention provides compounds of the formulas described herein and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: February 3, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Arnold E. Ruoho, Abdol R. Hajipour, Uyen B. Chu, Dominique A. Fontanilla
  • Publication number: 20150025045
    Abstract: The present invention relates to gene regulation. In particular, the present invention provides small compounds capable of modulating p300 and/or CBP-mediated transcription and related methods of therapeutic and research use. In addition, the present invention provides methods for treating conditions associated with aberrant p300 and/or CBP-mediated transcription with p300 and/or CBP-mediated transcription modulators (e.g., p300 and/or CBP-mediated transcription inhibitors).
    Type: Application
    Filed: September 14, 2012
    Publication date: January 22, 2015
    Applicants: THE OHIO STATE UNIVERSITY, THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Anna Mapp, Quintin Pan
  • Publication number: 20150018318
    Abstract: Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 15, 2015
    Inventors: Marianne Donnelly, Hui Qiu, Henry Yu, Lesley Liu-Bujalski, Andreas Goutopoulos
  • Publication number: 20150011513
    Abstract: A triazole bridged flavonoid dimer compound library was efficiently constructed via the cycloaddition reaction of a series of flavonoid-containing azides (Az 1-15) and alkynes (Ac 1-17). These triazole bridged flavonoid dimers and their precursor alkyne- and azide-containing flavonoids were screened for their ability to modulate multidrug resistance (MDR) in P-gp-overexpressed cell line (LCC6MDR), MRP1-overexpressed cell line (2008/MRP1) and BCRP-overexpressed cell line (HEK293/R2 and MCF7-MX100). Generally, they displayed very promising MDR reversal activity against P-gp-, MRP1- and BCRP-mediated drug resistance. Moreover, they showed different levels of selectivity for various transporters. Overall, they can be divided into mono-selective, dual-selective and multi-selective modulators for the P-gp, MRP1 and BCRP transporters.
    Type: Application
    Filed: March 1, 2013
    Publication date: January 8, 2015
    Inventors: Larry Ming Cheung Chow, Tak Hang Chan, Kin Fai Chan, Iris Lai King Wong, Man Chun Law
  • Patent number: 8921344
    Abstract: A method of increasing the bioavailability of 5-aminosalicylate compound by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of 5-aminosalicylate compound in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food.
    Type: Grant
    Filed: November 3, 2006
    Date of Patent: December 30, 2014
    Assignee: Salix Pharmaceuticals, Inc.
    Inventor: Lorin Johnson
  • Publication number: 20140309197
    Abstract: The present invention relates to stabilized pharmaceutical formulations prepared from solutions comprising an antineoplastic compound having a cyclic or non-cyclic hydrazine, triazine, or tetrazine group, or a pharmaceutically acceptable salt thereof, and a stabilizer, wherein the stabilizer is an antioxidant and/or more susceptible to nucleophilic attack than the antineoplastic compound.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Mahmoud S. AlSwisi, Mahmoud A.A. Ghannam
  • Publication number: 20140303123
    Abstract: The present invention relates to compositions (e.g., dendrimer scaffolds) capable of click chemistry for use in synthesis of functionalized dendrimers within biological settings, and methods of use of the same.
    Type: Application
    Filed: November 15, 2012
    Publication date: October 9, 2014
    Inventors: James R. Baker, JR., Sascha Nilu Goonewardena, Hong Zong
  • Publication number: 20140303074
    Abstract: The present disclosure provides methods of reducing immunodeficiency virus transcription, involving use of diflunisal or an active ester thereof. The disclosure also provides methods of treating an immunodeficiency virus infection in an individual, the method generally involving administering to the individual an effective amount of diflunisal or an active ester thereof.
    Type: Application
    Filed: December 12, 2012
    Publication date: October 9, 2014
    Inventors: Eric M. Verdin, Kotaro Shirakawa
  • Publication number: 20140294964
    Abstract: A uniform microfluidized nanoemulsion is disclosed containing an anti-cancer agent, such as dacarbazine. The microfluidized nanoemulsion improves the combination's cell membrane permeability by at least four-fold over conventional nanoemulsion compositions, which significantly increases the intracellular concentration of anticancer agents. As a nanoemulsion, dacarbazine has a greater anti-cancer efficacy than when applied as a free solution.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 2, 2014
    Inventors: Robert J. Nicolosi, Jean-Bosco Tagne
  • Publication number: 20140242190
    Abstract: Methods for preventing and/or reducing side effects of an anti-cancer agent in a subject in need thereof are disclosed. The method comprises administering to the subject, who is under an anti-cancer agent treatment, a composition comprising a therapeutically effective amount of isolated deoxyelephantopin and/or an analogue thereof; and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: May 2, 2014
    Publication date: August 28, 2014
    Applicant: Academia Sinica
    Inventors: Lie-Fen SHYUR, Wen-Wan CHAO, Ya-Wen CHENG
  • Publication number: 20140227260
    Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 21, 2014
    Publication date: August 14, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventor: Chengzhi Zhang
  • Publication number: 20140212509
    Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.
    Type: Application
    Filed: May 24, 2013
    Publication date: July 31, 2014
    Applicant: ABBVIE INC.
    Inventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
  • Publication number: 20140200200
    Abstract: The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.
    Type: Application
    Filed: May 18, 2012
    Publication date: July 17, 2014
    Applicants: UNIVERSITE DE BORDEAUX I, INSERM (Institut National de la Sante et de la Recherche Medicale), UNIV DE BORDEAUX II VICTOR SEGALEN
    Inventors: Pier Vincenzo Piazza, Monique Vallee, Giovanni Marsicano, Francois-Xavier Felpin, Luigi Bellocchio, Daniela Cota, Jean-Michel Revest, Sergio Vitiello, Umberto Spampinato, Rafael Maldonado
  • Patent number: 8772269
    Abstract: The present invention relates to pharmaceutical compositions comprising a sulfonamide-including compound in combination with an angiogenesis inhibitor.
    Type: Grant
    Filed: September 13, 2005
    Date of Patent: July 8, 2014
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Takashi Owa, Yoichi Ozawa, Taro Semba
  • Publication number: 20140161908
    Abstract: Novel chroman derivatives and intermediate compounds, compostions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotheraputic selective agents are described.
    Type: Application
    Filed: May 10, 2013
    Publication date: June 12, 2014
    Applicant: MEI Pharma, Inc.
    Inventors: Andrew HEATON, Alan HUSBAND
  • Publication number: 20140135295
    Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt of the compound. Also described are pharmaceutical formulations thereof and methods of using the same.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: IRONWOOD PHARMACEUTICALS
    Inventors: Jeffrey Segal, Nisha Perez, Timothy Claude Barden
  • Patent number: 8648058
    Abstract: A compound of formula I, wherein R1-R7 are defined herein, or stereoisomers therof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using these compounds for treating hypertension.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: February 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lin Yan
  • Publication number: 20140005149
    Abstract: Triazene-substituted diphenyl derivatives are suitable as chemotherapeutic agents for treating carcinomas in humans and animals.
    Type: Application
    Filed: July 15, 2011
    Publication date: January 2, 2014
    Inventor: Heinz Förster
  • Publication number: 20130296278
    Abstract: A compound having the structure (I) useful for treating hypertension, pulmonary arterial hypertension, congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
    Type: Application
    Filed: January 12, 2012
    Publication date: November 7, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Shrenik K. Shah, James Dellureficio
  • Patent number: 8551963
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
    Type: Grant
    Filed: November 5, 2009
    Date of Patent: October 8, 2013
    Assignee: Ambit Biosciences Corporation
    Inventors: Julius L. Apuy, Darren E. Insko, Joyce J. James
  • Publication number: 20130259800
    Abstract: The invention described herein pertains to the use of oxazolidinone antibiotics, alone or in combination, in the treatment of cancer. In particular, the invention pertains to the treatment of malignant gliomas, thyroid cancer or melanoma, or borderline forms of malignant glioma, thyroid cancer or melanoma.
    Type: Application
    Filed: December 15, 2011
    Publication date: October 3, 2013
    Applicant: BIOVISTA, INC.
    Inventors: Andreas Persidis, Spyros Deftereos
  • Patent number: 8506989
    Abstract: The invention relates to a preparation comprising a creatine component, which has excellent bio-availability and leads to improved creatine retention in the human and animal body. The present invention further relates to a method for the production of said preparation, and to the use thereof as a nutritional supplement, functional food, animal feed additive, pharmaceutical, and as an additive for cosmetic and dermatologic formulations.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: August 13, 2013
    Assignee: AlzChem Trostberg GmbH
    Inventors: Thomas Gastner, Frauke Warrikoff, Barbara Nieβ, Josef Fuest
  • Patent number: 8497256
    Abstract: The instant application provides methods and compositions for the treatment of male subjects having ulcerative colitis.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: July 30, 2013
    Assignee: Salix Pharmaceuticals, Ltd
    Inventors: William Forbes, Enoch Bortey, Lorin Johnson
  • Publication number: 20130165417
    Abstract: The invention relates to methods of treating cardiovascular and cardiopulmonary diseases and associated conditions, including hypertension. The invention further relates to pharmaceutical compositions for treating cardiovascular and cardiopulmonary diseases, especially hypertension, and lung injury.
    Type: Application
    Filed: April 23, 2011
    Publication date: June 27, 2013
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION
    Inventors: Mohan K. Raizada, David A. Ostrov, Michael J. Katovich
  • Patent number: 8450345
    Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: May 28, 2013
    Assignees: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics Corporation
    Inventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
  • Patent number: 8445466
    Abstract: The present invention provides amide-protected creatine molecules and compositions, containing one or more bioactive forms of creatine in aqueous compositions, wherein bioactive forms of creatine do not appreciably degrade into creatinine. Also provided are various beneficial effects of administering aqueous compositions having at least one amide-protected creatine molecule.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: May 21, 2013
    Inventor: John H. Owoc
  • Publication number: 20130116215
    Abstract: The invention features novel pharmaceutical combinations useful for the treatment of neurological diseases, specifically neurodegenerative diseases. The novel pharmaceutical combinations of the invention demonstrate additive or synergistic effect in silico and in vivo. The invention also relates to methods of treatment of neurological and neurodegenerative diseases including the pharmaceutical combinations of the invention.
    Type: Application
    Filed: October 25, 2012
    Publication date: May 9, 2013
    Inventors: Mireia Coma, Patrick Aloy, Albert Pujol, Xavier Gomis, Baldomero Oliva, Alberto Lleó, José Manuel Mas
  • Publication number: 20130102571
    Abstract: The invention provides compounds of the formulas described herein and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.
    Type: Application
    Filed: December 6, 2012
    Publication date: April 25, 2013
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventor: WISCONSIN ALUMNI RESEARCH FOUNDATION
  • Patent number: 8426390
    Abstract: The present invention relates to novel triazene compounds, to a process for their preparation, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans. The novel triazene compounds are distinguished, as compared with the known triazene compounds, by improved activity while at the same time having reduced toxicity, that is to say by fewer side-effects.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: April 23, 2013
    Assignee: Trin Therapeutics GmbH
    Inventors: Rudolf Reiter, Jochen Kalbe, Heinz Forster
  • Publication number: 20130028989
    Abstract: Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.
    Type: Application
    Filed: February 5, 2011
    Publication date: January 31, 2013
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: John J. Turchi, Sarah Shuck
  • Publication number: 20130004481
    Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.
    Type: Application
    Filed: January 5, 2012
    Publication date: January 3, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Flavio Solca, Ulrich Guertler, Michael Sanderson, Ulrike Tontsch-Grunt, Irene Waizenegger
  • Publication number: 20120309698
    Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
    Type: Application
    Filed: December 6, 2011
    Publication date: December 6, 2012
    Inventors: Yasutsugu Ueda, Timothy P. Connolly, Barry L. Johnson, Chen Li, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Margaret E. Sorenson, Michael A. Walker, Michael S. Bowsher, Rongti Li
  • Publication number: 20120276093
    Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase 11 inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
    Type: Application
    Filed: November 17, 2010
    Publication date: November 1, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Dario Ballinari, Antonella Ciavolella, Enrico Pesenti, Alessia Montagnoli
  • Publication number: 20120237592
    Abstract: Provided are compositions that include lipid particles, such as liposomes, that can fuse with the ER membrane of a cell. The lipid particles can also deliver a cargo, such as a therapeutic or an imaging agent, encapsulated inside the particles inside the ER lumen of the cell. The compositions can be useful for treating and/or preventing diseases or conditions caused by or associated with a virus, such as viral infections, including HIV and HCV infections.
    Type: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Inventors: Stephanie Pollock, Raymond Allen Dwek, Nicole Zitzmann
  • Patent number: 8258119
    Abstract: The present invention discloses triazene analogs of the general formula (I) and formula (II), their tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts thereof for the metastatic malignant melanoma and other cancers including but not limited to lymphomas, sarcomas, carcinomas, and gliomas. The invention further discloses a process for the preparation of the above said triazene analogs of formula (I) and formula (II), and their pharmaceutically acceptable compositions.
    Type: Grant
    Filed: September 15, 2009
    Date of Patent: September 4, 2012
    Assignee: Kasina Laila Innova Pharmaceuticals
    Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Rama Raju Gokaraju, Trimurtulu Golakoti, Venkateswarlu Somepalli, Sengupta Krishanu, Kiran Bhupathiraju
  • Publication number: 20120207856
    Abstract: Methods for treating a patient at risk for or diagnosed with colorectal cancer are disclosed herein. The method of the present invention determines the overall expression of MSH3 in cells suspected of being colorectal cancer cells from the patient and predicting the efficacy of therapy with a genotoxic anti-neoplastic agent for treating the patient, wherein a decrease in the overall expression of MSH3 in the patient cells when compared to the expression of MSH3 in normal colorectal cells indicates a predisposition to responsiveness to genotoxic anti-neoplastic agent therapy, wherein the therapy comprises administering an effective amount of the genotoxic anti-neoplastic agent therapy to patients.
    Type: Application
    Filed: February 10, 2012
    Publication date: August 16, 2012
    Applicant: Baylor Research Institute
    Inventors: Ajay Goel, C. Richard Boland, Minoru Koi, Masanobu Takahashi
  • Patent number: 8217022
    Abstract: The present invention refers to analogues of 1,3-bis(4-nitrophenyl)triazenes, their pharmaceutically acceptable salts and N-acyl derivatives for the treatment of different types of tumors. Said compounds show cytotoxicity at very low concentrations (IC50 0.22 to 12.8 ?M), and good solubility. These compounds can be used in the treatment of tumor patients as single drugs or in combination with other cytostatics.
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: July 10, 2012
    Assignee: Rudjer Boskovic Institute
    Inventors: Maja Osmak, Slovenko Polanc, Tamara Cimbora Zovko, Anamaria Brozovic, Marijan Kocevar, Vita Majce, Branko Alic