Pyrimidines (including Hydrogenated) (e.g., Cytosine, Etc.) Patents (Class 514/49)
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Patent number: 9833515Abstract: The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same.Type: GrantFiled: March 1, 2016Date of Patent: December 5, 2017Assignee: Redwood Bioscience, Inc.Inventors: Romas Alvydas Kudirka, Aaron Edward Albers, Robyn M. Barfield, David Rabuka
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Patent number: 9834576Abstract: The present invention relates to methods and intermediates for synthesizing 2?-deoxy-2?,2?-difluorotetrahydrouridine compounds.Type: GrantFiled: October 29, 2014Date of Patent: December 5, 2017Assignee: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hyeong-wook Choi, Steven Mathieu, Frank Fang, Bryan Matthew Lewis
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Patent number: 9820998Abstract: The present invention relates to use of bisphosphonate formulations for the treatment and management of HIV/AIDS. The method of the invention comprises administering a formulation comprising an effective amount of a bisphosphonate that specifically inhibits the activity and/or decreases the number of monocytes and/or macrophages, thereby reducing or eliminating HIV reservoirs. The invention also provides a method of complementing an HIV antiviral therapy, such as the highly active antiretroviral therapy (HAART), with a bisphosphonate formulation to improve clinical outcome.Type: GrantFiled: May 15, 2015Date of Patent: November 21, 2017Assignees: BIOREST LTD., OREGON HEALTH & SCIENCE UNIVERSITYInventors: Yoram Richter, Gershon Golomb, Jonah B. Sacha
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Patent number: 9808460Abstract: Disclosed herein are auris acceptable gel compositions containing a multiparticulate glutamate receptor antagonist, and methods for the treatment of otic diseases or conditions through intratympanic administration of the composition to an individual afflicted with an otic disease or condition.Type: GrantFiled: May 15, 2015Date of Patent: November 7, 2017Assignees: OTONOMY, INC., THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Jay Lichter, Andrew M. Trammel, Fabrice Piu, Qiang Ye, Benedikt Vollrath, Luis A. Dellamary, Carl Lebel, Jeffrey P. Harris
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Patent number: 9802957Abstract: This invention relates to processes for preparing a JAK1 inhibitor having Formula Ia: as well as new forms of the inhibitor.Type: GrantFiled: April 29, 2015Date of Patent: October 31, 2017Assignee: Incyte CorporationInventors: Jiacheng Zhou, Shili Chen, Yongzhong Wu, Zhongjiang Jia, Yingrui Dai
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Patent number: 9744186Abstract: In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to substituted gemcitabine aryl amide analogs, methods of making the same, pharmaceutical compositions comprising same, methods of treating viral disorders and disorders of uncontrolled cellular proliferation using same.Type: GrantFiled: August 8, 2016Date of Patent: August 29, 2017Assignee: NUCORION PHARMACEUTICALS, INC.Inventor: Zucai Suo
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Patent number: 9655905Abstract: The present invention includes embodiments for treatment and/or prevention of sickle cell disease that employ Hydroxyfasudil or Isocoronarin D alone or either in conjunction with each other or an inducer of HbF production. The compounds may act synergistically, and the compounds employed circumvent the side effects seen with Hydroxyurea.Type: GrantFiled: September 13, 2012Date of Patent: May 23, 2017Assignee: KING ABDULLAH UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Magbubah Essack, Vladimir Bajic, Aleksandar Radovanovic
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Patent number: 9616098Abstract: Vancomycin-containing compositions substantially free of precipitation after at least about 12 months of storage at refrigerated or ambient conditions are disclosed. The compositions include vancomycin or a pharmaceutically acceptable salt thereof; a polar solvent including propylene glycol, polyethylene glycol and mixtures thereof; lactic acid, a lactate salt, or mixtures thereof; and optionally, a pH adjuster in an amount sufficient to maintain a pH of the compositions at from about 3 to about 8.Type: GrantFiled: May 30, 2014Date of Patent: April 11, 2017Assignee: SciDose, LLCInventor: Nagesh R. Palepu
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Patent number: 9605031Abstract: The invention provides compositions of matter comprising a cowpea chlorotic mottle virus capsid protein (CCMV CP) and a ribonucleic acid, as well as methods for using such compositions. In such compositions, the cowpea chlorotic mottle virus capsid protein envelops the ribonucleic acid so as to for a capsid that can inhibit the degradation of the ribonucleic acid (e.g. by RNAses). A method of delivering a ribonucleic acid into the cytoplasm of a mammalian cell is also provided. Typically, the method comprises the steps of combining the mammalian cell with a composition of matter described herein under conditions selected to allow the cowpea chlorotic mottle virus capsid to contact the mammalian cell and deliver the ribonucleic acid into the cytoplasm of a mammalian cell.Type: GrantFiled: November 13, 2014Date of Patent: March 28, 2017Assignee: The Regents of the University of CaliforniaInventors: William M. Gelbart, Charles M. Knobler, Rees F. Garmann, Odisse Azizgolshani, Ruben D. Cadena-Nava
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Patent number: 9597344Abstract: Provided is a liposome comprising a lipid bilayer and a sonosensitizer that is disposed in and/or on the lipid bilayer, wherein the sonosensitizer self-assembles to form aggregates when exposed to ultrasound; and a method of efficiently delivering an active agent to a target site in the body of a subject using the sonosensitive liposome.Type: GrantFiled: August 19, 2015Date of Patent: March 21, 2017Assignee: SAMSUNG ELECTRONICS CO., LTD.Inventors: Sun Min Park, Jungyong Nam, Kitae Park, Hyun Ryoung Kim, Eun Sung Park
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Patent number: 9573971Abstract: The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The antiviral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection.Type: GrantFiled: January 8, 2016Date of Patent: February 21, 2017Assignee: ContraVir Pharmaceuticals, Inc.Inventors: Yanling Wang, Yuan Wang, Xungui He, Chuanjun Liu, Jirang Zhu, Jie Li, Qingzhong Cheng, Mingyong Yuan
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Patent number: 9567363Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.Type: GrantFiled: December 29, 2014Date of Patent: February 14, 2017Assignee: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
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Patent number: 9480752Abstract: The present invention refers to a conjugate comprising at least one polyunsaturated fatty acid residue, particularly an arachidonic acid residue, more particularly an anandamide (arachidonoyl ethanol amide) residue and covalently bound thereto at least one nucleosidic component selected from nucleic acids, nucleosides and nucleotides. This conjugate is suitable for the transfection of cells such as mammalian cells including human cells with high efficacy. Thus, a new delivery vehicle for therapeutic molecules including antisense molecules, siRNA molecules, miRNA molecules, antagomirs or precursors of such molecules, as well as the therapeutic nucleosides or nucleotides, is provided.Type: GrantFiled: July 10, 2013Date of Patent: November 1, 2016Assignee: Baseclick GmbHInventor: Thomas Carell
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Patent number: 9476099Abstract: The present invention is a gene expression panel of chemotherapeutic drug-resistant cancer stem cells comprising RIN1, SOX15 and TLR4. In one embodiment the cancer stem cells are testicular cancer germ cells. The present invention provides for a kit and method for determining response to treatment with decitabine at low doses.Type: GrantFiled: July 31, 2013Date of Patent: October 25, 2016Assignee: Trustees of Dartmouth CollegeInventors: Michael Spinella, Maroun J. Beyrouthy
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Patent number: 9457089Abstract: In an aqueous solution, a composition includes at least one protein, including at least one antibody fragment, and at least one water-soluble viscosity-reducing agent chosen from the group consisting of cytidine, 2?-deoxycytidine, uridine, 2?-deoxyuridine, thymidine and ribothymidine, alone or as a mixture. The protein includes at least one antibody fragment being at a concentration greater than or equal to 50 mg/ml.Type: GrantFiled: September 10, 2013Date of Patent: October 4, 2016Assignee: ADOCIAInventor: Olivier Soula
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Patent number: 9370567Abstract: A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.Type: GrantFiled: November 16, 2011Date of Patent: June 21, 2016Assignee: ARRAY BIOPHARMA INC.Inventors: Kurtis D. Davies, Stefan Gross
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Patent number: 9359451Abstract: Disclosed are methods and materials for treating or preventing complications due to traumatic injuries using estrogen or derivatives thereof.Type: GrantFiled: March 15, 2013Date of Patent: June 7, 2016Assignee: THE UAB RESEARCH FOUNDATIONInventors: Irshad H. Chaudry, William J. Hubbard, Zheng Feng Ba
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Patent number: 9351989Abstract: This invention is directed to phosphoroamidate and phosphorodiamidate derivatives including the compounds of formula (I) having the structure wherein U, V, W, Z, R1, X1, X2, and Y are defined herein. These compounds and pharmaceutical compositions containing these compounds are useful in the treatment of viral infections in mammals infected by a virus in the Flaviviridae family of viruses, in particular hepatitis C virus (HCV). The compounds of this invention may be prepared by various methods known in the art of organic chemistry in general and nucleoside and nucleotide analog synthesis in particular.Type: GrantFiled: December 29, 2011Date of Patent: May 31, 2016Assignees: INHIBITEX, INC., UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITEDInventors: Chris McGuigan, Karolina Madela, Claire Bourdin, John Vernachio, Stanley Chamberlain
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Patent number: 9296741Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: GrantFiled: March 14, 2013Date of Patent: March 29, 2016Assignee: AbbVie Inc.Inventors: Le Wang, John K Pratt, Keith F McDaniel, Yujia Dai, Steven D Fidanze, Lisa Hasvold, James H Holms, Warren M Kati, Dachun Liu, Robert A Mantei, William J McClellan, George S Sheppard, Carol K Wada
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Patent number: 9265785Abstract: Embodiments of compositions and methods for the treatment of blood disorders and malignancies in a subject are described herein. In one embodiment, a composition for the treatment of a blood disorder or a malignancy in a subject comprises decitabine, tetrahydrouridine, and an excipient. In another embodiment, a method for the treatment of a blood disorder or a malignancy in a subject comprises the oral administration of a composition comprising decitabine and tetrahydrouridine. In some examples, the composition may be administered 1-3 times weekly.Type: GrantFiled: March 7, 2012Date of Patent: February 23, 2016Assignee: The Board of Trustees of the University of IllinoisInventors: Joseph Desimone, Yogen Saunthararajah
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Patent number: 9259469Abstract: Compositions comprising decitabine and tetrahydrouridine for the treatment of blood disorders and hematological and solid malignancies are described.Type: GrantFiled: December 21, 2009Date of Patent: February 16, 2016Assignee: The Board of Trustees of the University of IllinoisInventors: Joseph Desimone, Yogen Saunthararajah
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Patent number: 9145444Abstract: The invention relates to compounds and methods useful in detection and therapy of HPV-associated diseases. The invention is based on the elucidation of a mechanism by which replication of HPVs occurs in naturally infected tissues and cells. Moreover it is based on the identification of distinct epigenetic changes of the viral genome in infected cells that allows promotion of the affected cells to precancerous and cancerous cells. The invention therefore provides methods of diagnosing neoplasias and their precursor lesions as well as methods of preventing the development of malignancies or inhibiting tumor growth.Type: GrantFiled: October 31, 2008Date of Patent: September 29, 2015Assignee: Ruprecht-Karls-Universität HeidelbergInventors: Magnus Von Knebel Doeberitz, Svetlana Vinokurova
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Patent number: 9133232Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: GrantFiled: December 16, 2013Date of Patent: September 15, 2015Assignee: University of North Carolina at WilmingtonInventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Patent number: 9126971Abstract: The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: wherein B is nucleoside base according to the structure: and the remaining variables as defined in the specification, and pharmaceutical compositions comprising the compounds. The compounds are useful interalia as anti-viral agents in viral therapy.Type: GrantFiled: May 7, 2012Date of Patent: September 8, 2015Assignee: YALE UNIVERSITYInventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
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Patent number: 9125884Abstract: Provided herein are methods for treating subjects having a cancer, such as a relapsed or refractory solid tumor, wherein the method comprises administering to the subject a cytidine analog. In certain of the methods, the cytidine analog is administered alone or in combination with one or more anti-cancer agents. Also provided are methods for using a cytidine analog, to treat diseases and disorders including disorders related to abnormal cell proliferation, hematologic disorders, and immune disorders, among others. In certain of the methods, the cytidine analog is formulated in an oral dosage form and administered orally.Type: GrantFiled: October 31, 2012Date of Patent: September 8, 2015Assignee: Celgene CorporationInventors: Kyle J. MacBeth, Aaron N. Nguyen, Jorge DiMartino
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Patent number: 9102714Abstract: A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.Type: GrantFiled: October 11, 2012Date of Patent: August 11, 2015Assignee: Lipoxen Technologies LimitedInventors: Dale Howard Hreczuk-Hirst, Sanjay Jain, Peter Laing, Gregory Gregoriadis, Ioannis Papaioannou
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Pharmacological modulation of telomere length in cancer cells for prevention and treatment of cancer
Patent number: 9078901Abstract: Acyclic nucleoside analogs such as acyclovir, ganciclovir, penciclovir and the corresponding pro-drugs, i.e., valacyclovir, valganciclovir and famciclovir, respectively have been identified as inhibitors or antagonists of both telomerase (encoded by TERT) and reverse transcriptase encoded by L-1 (LINE-1) RT, and as useful for treating or preventing cancers induced or mediated by the two enzymes. Method of treating or preventing such cancers in patients involves administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases in cells of the patients. The inhibitor or antagonist blocks lengthening of telomeres in telomerase positive and telomerase negative cells. Methods and kits for detecting pathologically proliferating cells expressing TERT and L1RT are also disclosed.Type: GrantFiled: December 12, 2013Date of Patent: July 14, 2015Assignee: ALT Solutions Inc.Inventor: Igor E. Bondarev -
Patent number: 9073960Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.Type: GrantFiled: December 20, 2012Date of Patent: July 7, 2015Assignee: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Jerome Deval, Marija Prhavc
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Publication number: 20150148307Abstract: The present invention is directed to methods of prognosing relapsed leukemia in a subject. These methods are based on the detection of one or more relapse-specific gene mutations in a patient sample. The present invention further relates to methods of preventing and treating relapse leukemia in a subject based on the determined prognosis of the subject.Type: ApplicationFiled: May 7, 2013Publication date: May 28, 2015Applicant: NEW YORK UNIVERSITYInventors: William L. Carroll, Julia A. Meyer
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Publication number: 20150148301Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.Type: ApplicationFiled: May 23, 2013Publication date: May 28, 2015Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
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Patent number: 9040501Abstract: Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them.Type: GrantFiled: November 14, 2013Date of Patent: May 26, 2015Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Sergel Belyakov, Bridget Duvall, Dana Ferraris, Gregory Hamilton, Mark Vaal
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Patent number: 9040490Abstract: A cytosine analog, a method of preparation of a cytosine analog, a DNA methyltransferase 1 inhibitor, and a method for DNA methylation inhibition, is provided for the treatment of diseases associated with deviations from normal DNA methylation. The analog of cytosine may be comprised of 1, N4, 5 and 6-substituted derivatives of cytosine or 5,6-dihydrocytosine, wherein the analog can be described by the chemical formula where R1 is H, R3, R4, 2?-deoxyribosyl, R4 is alkyl or aryl, X is N or C, wherein if X in the analog of formula I is N, then R5 is no substituent and if X in the analog of formula I and/or II is C or if X in the analog of formula II is N, then R5 and R6 are independently alkyl, aryl, hydroxyalkyl, aminoalkyl, hydroxyl, carboxyl, amino group, alkoxyl, aryloxyl, aminoalkyl, aminoaryl, thio group, sulfonyl, sulfinyl or halogen.Type: GrantFiled: March 17, 2011Date of Patent: May 26, 2015Assignee: INSTYTUT CHEMII BIOORGANICZNEJ PANInventors: Jan Barciszewski, Wojciech T. Markiewicz, Ewelina Adamska, Beata Plitta, Malgorzata Giel-Pietraszuk, Eliza Wyszko, Maria Markiewicz, Agnieszka Fedoruk-Wyszomirska, Tadeusz Kulinski, Marcin Chmielewski
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Patent number: 9040500Abstract: This invention relates to methods for treating a hematopoietic neoplasm comprising administering a therapeutically effective amount of a combretastatin compound, or a pharmaceutically acceptable salt thereof, to a subject having a hematological malignancy, wherein the combretastatin compound comprises a catechol or quinone moiety and is capable of forming a reactive oxygen species (ROS) in vivo. The method may further comprise co-administering a second chemotherapeutic agent.Type: GrantFiled: November 28, 2011Date of Patent: May 26, 2015Assignee: OXiGENE, Inc.Inventors: David Chaplin, Bronwyn G. Siim
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Publication number: 20150141364Abstract: This application relates to combination therapies including triciribine compounds and epidermal growth factor receptor inhibitor compounds, particularly erlotinib-like compounds and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.Type: ApplicationFiled: November 27, 2013Publication date: May 21, 2015Applicant: University of South FloridaInventors: Jin Q. CHENG, Said M. Sebti
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Publication number: 20150140127Abstract: Provided is a method for detecting injury to the brain comprising: a) determining the level of a tight junction (TJ) protein in exosomes isolated from a test sample from a subject, wherein the TJ protein is occludin, claudin-3, claudin-5, claudin-12, ZO-1, ZO-2, ZO-3, JAM-A, JAM-B or JAM-C, or any combination thereof; b) comparing the level of the TJ protein in the test sample to the level of the TJ protein in a control sample, wherein an elevated level of the TJ protein in the test sample relative to the level of the TJ protein in the control sample indicates that the subject has an injury to the brain.Type: ApplicationFiled: June 25, 2013Publication date: May 21, 2015Applicant: TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATIONInventors: Servio H. Ramirez, Slava Rom, Yuri Persidsky
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Publication number: 20150140124Abstract: The present invention relates to the BAD pathway's influence on development, progression, chemo-sensitivity, and overall survival for multiple human cancers and its potential as a therapeutic target to increase chemo-sensitivity. BAD pathway expression was associated with the development and/or progression of breast, colon, and endometrial cancers, relapse-free survival from breast cancer, and overall survival from ovarian, colon, and brain cancers. Expression was also associated with in vitro sensitivity to a range of cytotoxic agents. pBAD levels were higher in cancer versus immortalized normal cells and chemo-resistant versus—sensitive cancer cells and associated with increased cell proliferation.Type: ApplicationFiled: November 10, 2014Publication date: May 21, 2015Inventors: Johnathan M. Lancaster, Douglas C. Marchion, Yin Xiong
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Publication number: 20150141342Abstract: The differential expression of select miRNA in plasma and bile among patients with PDAC, chronic pancreatitis (CP), and controls were measured. Patients (n=215) with treatment-naïve PDAC (n=77), CP with bile or pancreatic duct pathology (n=67), and controls (n=71) that had been prospectively enrolled in a Pancreatobiliary Disease Biorepository at the time of endoscopic retrograde cholangiopancreatography (ERCP) or endoscopic ultrasound (EUS) were identified. Controls were patients with choledocholithiasis but normal pancreata. The sample was separated into training (n=95) and validation (n=120) cohorts to establish and then test the performance of PDAC Signature Panels in diagnosing PDAC. The training cohort (n=95) included age-matched patients with CP and controls. Panels were derived from the differential expression of 10-candidate miRNA in plasma or bile.Type: ApplicationFiled: November 14, 2014Publication date: May 21, 2015Inventors: Murray Korc, A. Jesse Gore, Gregory A. Cote, Stuart Sherman
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Publication number: 20150132258Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventor: George D. Hartman
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Publication number: 20150132298Abstract: The present invention provides compounds according to formula I: and pharmaceutically acceptable salts thereof. For compounds of formula I, R1 and R2 are independently selected from the group consisting of H, —C(?O)—(CH2)2-aryl, and —C(?O)—(CH2)n—C(?O)—NH-aryl. The subscript n is from 2 to 6. R3 is selected from the group consisting of H and —C(?O)—O—R4; and R4 is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, arylalkyl, substituted arylalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl and substituted heteroalkyl. Compounds are provided wherein at least one of R1 and R2 is other than H. Pharmaceutical compositions, methods for inhibiting the growth of cancer cells, and methods for the treatment of cancer are also provided.Type: ApplicationFiled: January 16, 2015Publication date: May 14, 2015Inventor: Laurence I. Wu
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Publication number: 20150132280Abstract: A human dietary supplement comprises theacrine and optionally other compounds that modulate the effects of theacrine. Uses for the theacrine-containing supplement include improvement of at least one of mood, energy, focus, concentration or sexual desire or a reduction of at least one of anxiety or fatigue.Type: ApplicationFiled: November 12, 2014Publication date: May 14, 2015Applicant: ORTHO-NUTRA, LLCInventors: Hector L Lopez, Shawn Wells, Tim N. Ziegenfuss
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Patent number: 9029335Abstract: Provided herein are novel bicyclic nucleosides, oligomeric compounds that include such bicyclic nucleosides and methods of using the oligomeric compounds. More particularly, the novel bicyclic nucleosides comprise a furanose ring system having a bridge comprising a 4?-methylene group attached to a 2?-sulfoxide or sulfone group and optionally including one or more substituent groups attached to the 4?-methylene and or the 5?-position. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: GrantFiled: October 9, 2013Date of Patent: May 12, 2015Assignee: Isis Pharmaceuticals, Inc.Inventors: Thazha P. Prakash, Eric E. Swayze
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Patent number: 9029346Abstract: Methods and compounds are disclosed for irreversibly inhibiting a DNA repair enzyme that possesses lyase activity.Type: GrantFiled: December 13, 2013Date of Patent: May 12, 2015Assignee: The Johns Hopkins UniversityInventors: Marc M. Greenberg, Dumitru Arian, Theodore L. Deweese, Mohammad Hedayati
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Publication number: 20150126471Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as “TFM compounds”) which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: May 14, 2013Publication date: May 7, 2015Inventors: Ian Collins, Thomas Peter Matthews, Tatiana Faria Da Fonseca Mchardy, James Osborne, Michael Lainchbury, Michael Ian Walton, Michelle Dawn Garrett
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Patent number: 9023839Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: GrantFiled: April 22, 2014Date of Patent: May 5, 2015Assignee: IRM LLCInventors: Valentina Molteni, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
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Publication number: 20150111847Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.Type: ApplicationFiled: January 6, 2015Publication date: April 23, 2015Applicant: GENERICS [UK] LIMITEDInventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
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Publication number: 20150110773Abstract: Methods and kits for GPP-targeting, e.g., for the treatment of oncogenic Kras-associated cancers, and methods for determining the efficacy of those methods are provided.Type: ApplicationFiled: May 23, 2013Publication date: April 23, 2015Inventors: Alec C. Kimmelman, Jaekyoung Son, Lewis Cantley, Costas A. Lyssiotis
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Patent number: 9012427Abstract: Disclosed herein are pharmaceutical compositions that can include a thionucleotide analog for use in combination therapy with other agents. Also disclosed herein are methods of treating diseases and/or conditions with a pharmaceutical composition that can include a thionucleotide analog in combination therapy with other agents.Type: GrantFiled: March 12, 2013Date of Patent: April 21, 2015Assignee: Alios BioPharma, Inc.Inventors: Lawrence M Blatt, Leonid Beigelman, Hua Tan, Julian Alexander Symons, David Bernard Smith, Min Jiang, Tara Lynn Kieffer, Cornelis Arie Rijnbrand
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Patent number: 9012428Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).Type: GrantFiled: November 10, 2011Date of Patent: April 21, 2015Assignees: Janssen Products, LP, Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
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Publication number: 20150104384Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.Type: ApplicationFiled: March 1, 2013Publication date: April 16, 2015Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
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Publication number: 20150105341Abstract: Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.Type: ApplicationFiled: October 9, 2014Publication date: April 16, 2015Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Marija Prhavc, Christian Andreas Jekle, Jerome Deval