Nonshared Hetero Atoms In At Least Two Rings Of The Polycyclo Ring System Patents (Class 514/81)
  • Patent number: 11104678
    Abstract: The present invention relates to purine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: May 6, 2019
    Date of Patent: August 31, 2021
    Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
    Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig McGowan, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 11014950
    Abstract: Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.
    Type: Grant
    Filed: August 8, 2019
    Date of Patent: May 25, 2021
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Patent number: 11008333
    Abstract: A crystalline form of an alkyl benzene sulfonyl urea compound that is useful as an oral antidiabetics is disclosed. Specifically, the compound is a hydrochloride salt of N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide of the following formula I.
    Type: Grant
    Filed: December 30, 2016
    Date of Patent: May 18, 2021
    Assignee: HANMI PHARM. CO., LTD.
    Inventors: Jong Ouk Baek, Ji Young Jeon, Hee Sook Oh, Hee Cheol Kim, Sun Young Jang, Tae Hee Ha
  • Patent number: 10813933
    Abstract: A drug containing, as an active ingredient, a compound represented by ALK inhibitors such as brigatinib, AP26113-analog, and AZD3463 has been found to be effective against a non-small cell lung cancer having a point mutation at C797S in EGFR which has acquired a resistance to chemotherapy agents. Further, the drug used in combination with an anti-EGFR antibody demonstrates a notable suppression effect on the tumor growth. The drug has a potential to be a therapeutic agent effective against a non-small cell lung cancer which is resistant to gefitinib, a first generation therapeutic agent and osimertinib, a third generation therapeutic agent.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: October 27, 2020
    Assignee: JAPANESE FOUNDATION FOR CANCER RESEARCH
    Inventors: Ryohei Katayama, Ken Uchibori, Naoya Fujita
  • Patent number: 10780062
    Abstract: A tobacco product includes a dry powder composition comprising an amount of myo-inositol effective for treating and/or delaying onset of dysplastic lesions in the bronchial airway of an individual. A method for administering myo-inositol to an individual comprises the individual consuming the tobacco product.
    Type: Grant
    Filed: March 22, 2019
    Date of Patent: September 22, 2020
    Assignee: COLORADO CAN LLC
    Inventor: Robert E. Sievers
  • Patent number: 10751351
    Abstract: The present invention provides means and methods for treating diabetic foot infections. In particular, drug compounds are provided that combine a high therapeutic activity against Staphylococcus Spp. bacteria with a high degree of bone penetration and vasodilatory effects. This unique combination of properties allows to accomplish high local concentrations of the drug at the site of infection even in diabetic foot patients typically having poor blood perfusion at the site of infection.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: August 25, 2020
    Assignee: Debiopharm International S.A.
    Inventors: Grégoire Vuagniaux, Linda Kadi, Frederick Wittke
  • Patent number: 10745428
    Abstract: Compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: December 5, 2016
    Date of Patent: August 18, 2020
    Assignees: IDENIX PHARMACEUTICALS LLC, MERCK SHARP & DOHME CORP.
    Inventors: Izzat Tiedje Raheem, Timothy J. Hartingh, John Schreier, Jean-Laurent Paparin
  • Patent number: 10702532
    Abstract: Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.
    Type: Grant
    Filed: January 8, 2019
    Date of Patent: July 7, 2020
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Patent number: 10688196
    Abstract: It is described a complex of riboflavin into hydroxypropylated ?-cyclodextrins as photosensitizer in the riboflavin-UV mediated cross-linking of corneal collage fibers and the relative ophthalmic compositions comprising it.
    Type: Grant
    Filed: April 29, 2015
    Date of Patent: June 23, 2020
    Assignee: SOOFT ITALIA SPA
    Inventors: Giovanni Cavallo, Edoardo Stagni, Marco Biondi, Piero Biondi
  • Patent number: 10596103
    Abstract: Described herein is a vaginal ring drug delivery system comprising (i) a core comprising a first thermoplastic polymer and a first therapeutic agent, wherein the first therapeutic agent is dissolved in the first thermoplastic polymer, and (ii) a skin surrounding the core comprising a second thermoplastic polymer and a second therapeutic agent, wherein the second therapeutic agent is in solid form.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: March 24, 2020
    Assignee: Merek Sharp & Dohme B.V.
    Inventors: Dennis Aarts, Wouter de Graaff, Johannes Antonius Hendrikus van Laarhoven
  • Patent number: 10561665
    Abstract: Autistic Spectrum Disorders (ASD) are a group of developmental disorders including autistic disorder, Asperger disorder and pervasive developmental disorder not otherwise specified which may be treated by use of a galanthamine analog wherein the hydroxy group of galantamine is replaced by a carbamate, carbonate or ester group and the methoxy group may be replaced by another alkoxy group of from two to six carbon atoms, a hydroxy group, hydrogen, an alkanoyloxy group or 2 to 10 carbon atoms, a benzoyloxy or substituted benzoyloxy group, a carbonate group of 1 to 10 carbon atoms or a carbamate group such as a mono alkyl or dialkyl or an aryl carbamate wherein the alkyl groups or aryl groups contain from 1 to 10 carbons; and the N-methyl group may be replaced by hydrogen, alkyl of 1 to 10 carbon atoms, benzyl, cyclopropylmethyl group or a substituted or unsubstituted benzoyloxy group. Galantamine mon-alkylcarbamates are particularly useful.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: February 18, 2020
    Assignee: Synaptec Development LLC
    Inventor: Bonnie M. Davis
  • Patent number: 10377782
    Abstract: Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.
    Type: Grant
    Filed: September 15, 2016
    Date of Patent: August 13, 2019
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Patent number: 10335423
    Abstract: A process is provided for protecting a primate host from a self-replicating infection by an immunodeficiency retrovirus. Protection is achieved by administering to the primate host a combination of a pharmaceutically effective amount of a nucleoside reverse transcriptase inhibitor and a pharmaceutically effective amount of a nucleotide reverse transcriptase inhibitor prior to exposure to the immunodeficiency retrovirus. The administration is effective if provided in a single dose within 24 hours of the exposure. A regime of regular daily doses is also effective in providing protection against an immunodeficiency retrovirus becoming self-replicating after infecting a primate host.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: July 2, 2019
    Assignee: THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human Services
    Inventors: Walid Heneine, Thomas M. Folks, Robert Janssen, Ronald A. Otten, Jose Gerardo Garcia Lerma
  • Patent number: 10233202
    Abstract: The present invention relates to a tenofovir monobenzyl ester phosphamide prodrug, preparation method and pharmaceutical use thereof. Specifically, the present invention relates to a compound of general formula (X), or isomer, pharmaceutically-acceptable salt, hydrate or solvate thereof, preparation method and use thereof in the preparation of drugs for treating viral infectious diseases, preferably AIDS infection, hepatitis B or diseases caused by hepatitis B virus.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: March 19, 2019
    Assignee: Jiangsu Tasly Diyi Pharmaceutical Co., LTD.
    Inventors: Guocheng Wang, Huimin Wu
  • Patent number: 10213430
    Abstract: Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: February 26, 2019
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Patent number: 10167302
    Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, and their use in medicine particular as anti-viral agents; wherein: X is selected from O and NR11; Y is selected from O, S and NR12; A is selected from —(CR1R2)n-, —(CR9R10)—, —(CR9R10)—(CR1R2)n-, —(CR1R3)—(CR2R4)—(CR1R2)n-, —CR3?CR4—(CR1R2)n- and —C?C—(CR1R2)n-; R1 and R2 are independently selected from H, alkyl, hydroxyl, hydroxymethyl and halogen; R3 and R4 are independently selected from H and alkyl, or R3 and R4 together with the carbon atoms to which they are attached form a mono or bicyclic ring system selected from cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl and heteroaryl; R5 is selected from H, P(?O)(OH)2 and P(?O)(OH)—O—P(?O)(OH)2; R6 is selected from H and alkyl; R7 and R8 are independently selected from H, alkyl, halogen and hydroxymethyl R9 and R19 together with the carbon atoms to which they are attached form a mono or bicyclic ring system selected
    Type: Grant
    Filed: May 20, 2015
    Date of Patent: January 1, 2019
    Assignees: UNIVERSITY COLLEGE CORK, KATHOLIEKE UNIVERSITEIT LEUVEN
    Inventors: Anita Maguire, Alan Ford, Jan Balzarini, Wim Dehaen
  • Patent number: 10071110
    Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: September 11, 2018
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Patent number: 9968686
    Abstract: The invention relates to an antisense or siRNA oligonucleotide or conjugate with improved pharmacokinetic properties, methods of producing the same as well as the use of such compounds and conjugates, e.g. as pharmaceutical composition, a pharmaceutical kit, a medicament or a tool in biomedical research. The conjugates of the invention have the formula I being P-(L-S—S—Y—X)n, wherein P represents a natural, artificial and/or modified oligonucleotide, L represents a linker group attached to one or more nucleosides at any position within the oligonucleotides sequence; S represents sulfur; X represents a ligand; Y represents a spacer and n is an integer ranging from 1 to the oligonucleotide length of P.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: May 15, 2018
    Assignee: UNIVERSITY OF VIENNA
    Inventors: Christian R. Noe, Mehrdad Dirin, Johannes Winkler, Bodo Lachmann, Ernst Urban
  • Patent number: 9956239
    Abstract: The present invention relates to compounds and methods for treating retroviral infections and/or Hepatitis B viral infections. Some compounds of the invention are described by Formula I: or a stereoisomer, a diastereomer, an enantiomer or racemate thereof.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: May 1, 2018
    Assignee: Chimerix, Inc.
    Inventor: Ernest Randall Lanier
  • Patent number: 9937191
    Abstract: A process is provided for protecting a primate host from a self-replicating infection by an immunodeficiency retrovirus. Protection is achieved by administering to the primate host a combination of a pharmaceutically effective amount of a nucleoside reverse transcriptase inhibitor and a pharmaceutically effective amount of a nucleotide reverse transcriptase inhibitor prior to exposure to the immunodeficiency retrovirus. The administration is effective if provided in a single dose within 24 hours of the exposure. A regime of regular daily doses is also effective in providing protection against an immunodeficiency retrovirus becoming self-replicating after infecting a primate host.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: April 10, 2018
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Walid Heneine, Thomas M. Folks, Robert Janssen, Ronald A. Otten, Jose Gerardo Garcia Lerma
  • Patent number: 9926320
    Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
    Type: Grant
    Filed: May 19, 2014
    Date of Patent: March 27, 2018
    Assignee: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
    Inventors: Soo Yei Ho, Stephanie Eliane Blanchard, Athisayamani Jeyaraj Duraiswamy, Jenefer Alam, Vikrant Arun Adsool
  • Patent number: 9907761
    Abstract: Compositions of and methods for using synthetic retinoids as retinoid replacements and opsin agonists are provided.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: March 6, 2018
    Assignee: University of Washington
    Inventors: Krzysztof Palczewski, David A. Saperstein
  • Patent number: 9896446
    Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative diseases.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: February 20, 2018
    Assignee: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Robert L. Hudkins, Eugen F. Mesaros, Gregory R. Ott, Craig A. Zificsak, Allison L. Zulli, Ming Tao, Katherine M. Fowler, Emma L. Morris, Gregoire A. Pave, Jonathan R. A. Roffey, Nathaniel J. T. Monck, Christelle N. Soudy, Ikeoluwa Olowoye
  • Patent number: 9862722
    Abstract: Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: January 9, 2018
    Assignee: Pharmacyclics LLC
    Inventors: Wei Chen, David J. Loury, Tarak D. Mody, Longcheng Wang
  • Patent number: 9834571
    Abstract: The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: February 16, 2016
    Date of Patent: December 5, 2017
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Xiaotian Zhu, Yihan Wang, William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno
  • Patent number: 9801884
    Abstract: Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: October 31, 2017
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Patent number: 9777028
    Abstract: The present invention relates to co-crystals, salts and crystalline forms of tenofovir alafenamide and methods for preparation, use and isolation of such compounds.
    Type: Grant
    Filed: June 13, 2016
    Date of Patent: October 3, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Bing Shi, Zhuoyi Su, Fang Wang
  • Patent number: 9771363
    Abstract: Provided herein are heterocyclic compounds of Formula (I), pharmaceutical compositions containing such a compound and their therapeutic uses, methods for their preparation, intermediate compounds, pharmaceutical compositions containing such a compound, and their therapeutic uses.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: September 26, 2017
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Jiazhong Zhang, Songyuan Shi, Ben Powell, Yan Ma
  • Patent number: 9757361
    Abstract: This invention concerns the use of cyclopamine, a naturally occurring steroidal alkaloid known for over thirty years, for the treatment of psoriasis and achievement of rapid clearance of the psoriatic skin lesions together with the reversion of the histopathological signs of disease to normalcy with no detectable side effects. The cyclopamine-induced clearance of psoriatic lesions from the skin of patients is associated with the causation of cellular differentiation in lesional epidermis and with the rapid disappearance of CD4(+) lymphocytes and other inflammatory cells from lesional skin. Therapeutic compositions comprising of cyclopamine and a corticosteroid and/or the pre-treatment of lesions with a corticosteroid provide significantly further increased therapeutic effectiveness over the use of cyclopamine alone or a corticosteroid alone.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: September 12, 2017
    Inventors: Sinan Tas, Oktay Avci
  • Patent number: 9757354
    Abstract: The invention provides compositions and methods for treating cyanide poisoning.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: September 12, 2017
    Assignee: REGENTS OF THE UNIVERSITY OF MINNESOTA
    Inventors: Steven Earl Patterson, Herbert Tsukasa Nagasawa, Robert Vince, Alexandre Monteil
  • Patent number: 9744181
    Abstract: The present invention relates to therapeutic combinations of [2-(6-amino-purin-9 yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S,cis)-4-amino-5-fluoro-1-(2 hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (?)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: August 29, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Terrence C. Dahl, Mark M. Menning, Reza Oliyai
  • Patent number: 9556163
    Abstract: The invention relates to a process for the preparation of 5-chloro-N-({(5-S)-2-oxo3-[4-(3-oxo-morj)holine-4-yl)-phenyl]-1,3-oxazolidine-5-yl}-methyl) thiophen-2-carboxamide having the INN rivaroxaban. The invention also relates to intermediates formed in the above process.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: January 31, 2017
    Assignee: EGIS Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
    Inventors: Eva Sipos, Gyorgyi Kovanyine Lax, Balazs Havasi, Balazs Volk, Gyorgy Krasznai, Gyorgy Ruzsics, Jozsef Barkoczy, Maria Tothne Lauritz, Gyula Lukacs, Andras Boza, Laszlo Jozsef Hegedus, Maria Julia Taborine Toth, Eva Pecsi
  • Patent number: 9550803
    Abstract: An amino acid conjugate of a cyclic or acyclic nucleoside phosphonate is provided. In some cases, the amino acid conjugate is a tyrosine alkyl amide phosphonate ester conjugate of a cyclic or acyclic nucleoside phosphonate, and is useful as an antiviral compound. In certain cases, the tyrosine conjugate includes a long chain alkyl group on the carboxamide group of the tyrosine residue. In a method of preparing an acyclic tyrosine conjugate, a tert-butyloxycarbonyl (Boc) protected tyrosine residue containing a long chain alkyl group is reacted with an acyclic nucleoside phosphonate mono-ethyl ester in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate to produce a Boc-protected nucleoside phosphonate di-ester, and the di-ester is deethylated and deprotected to produce the tyrosine conjugate. Methods of inhibiting viral replication and methods of treating a viral infection using the amino acid conjugate are also provided.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: January 24, 2017
    Assignee: University of Southern California
    Inventors: Charles E. McKenna, Boris A Kashemirov, Ivan S Krylov, Valeria M. Zakharova
  • Patent number: 9532997
    Abstract: Disclosed herein are novel methods and compositions useful for promoting intestinal stem cell function. The methods and compositions are particularly useful for stimulating the proliferation of and/or self-renewal of intestinal stem cells, as well as for minimizing, preventing, or ameliorating cellular damage resulting from incidental or accidental exposure to radiation (e.g., cancer radiation therapy).
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: January 3, 2017
    Assignee: Whitehead Institute for Biomedical Research
    Inventors: Pekka Katajisto, Michael Pacold, David M. Sabatini, Omer Yilmaz
  • Patent number: 9493493
    Abstract: Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.
    Type: Grant
    Filed: September 15, 2015
    Date of Patent: November 15, 2016
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Patent number: 9457035
    Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: February 11, 2014
    Date of Patent: October 4, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
  • Patent number: 9394258
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: July 19, 2016
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
  • Patent number: 9387209
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions comprising the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit are also disclosed. In one aspect, the invention relates to a compound having the structure or a pharmaceutically acceptable salt, a solvate or hydrate, a prodrug, or a metabolite thereof. In one embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is fluoro; R5 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; and R6 is hydrogen, or a salt thereof. In another embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; R5 is chloro or fluoro; and R6 is hydrogen, or a salt thereof.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: July 12, 2016
    Assignee: ANNJI PHARMACEUTICAL CO., LTD.
    Inventors: Ji-Wang Chern, Chao-Wu Yu, Pei-Teh Chang
  • Patent number: 9334272
    Abstract: Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.
    Type: Grant
    Filed: July 24, 2014
    Date of Patent: May 10, 2016
    Assignees: Ramot at Tel-Aviv University Ltd., Bar-Ilan University
    Inventors: Abraham Nudelman, Ada Rephaeli
  • Patent number: 9283238
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: March 15, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
  • Patent number: 9206208
    Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolizm, cancer, viral infections, and the like.
    Type: Grant
    Filed: October 29, 2014
    Date of Patent: December 8, 2015
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Patent number: 9206209
    Abstract: An exemplary emboidment is related to a pharmaceutical composition of the class of nucleotide analogues and antiviral pro-nucleotides useful in partial or complete inhibition of human immunodeficiency virus (HIV). An exemplary embodiment is expressed in the formula (XVI): where X stands for N3 and B stands for thymidine-1-yl, or X stands for H and B stands for uracil-1-yl or adenin-1-yl or hypoxanthin-1-yl.A method of synthesis of the nucleotide analogue using a phosphorylating agent for synthesis of the nucleotide analogue is provided.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: December 8, 2015
    Assignees: INSTYTUT CHEMII BIOORGANICZNEJ PAN, NARODOWY INSTYTUT LEKOW
    Inventors: Adam Kraszewski, Joanna Romanowska, Michal Sobkowski, Agnieszka Szymanska-Michalak, Jacek Stawinski, Jerzy Boryski, Andrzej Lipniacki, Andrzej Piasek
  • Patent number: 9096624
    Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: August 4, 2015
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: Andrew P. Crew, Dan Sherman, Rama Devi Appari, Xin Chen, Ramesh Chilukuri, Hanqing Dong, Caterina Ferraro, Kenneth Foreman, Ramesh C. Gupta, An-Hu Li, Kathryn M. Stolz, Brian Volk, Robert Zahler
  • Patent number: 9090639
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Grant
    Filed: December 5, 2013
    Date of Patent: July 28, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond W Colburn, Scott L Dax, Christopher M Flores, Jay M Matthews, Ning Qin, Laura W. Andraka, Christopher Teleha, Mark A Youngman
  • Patent number: 9056882
    Abstract: The present invention provides a process for preparation of tenofovir by dealkylation of its phosphonate ester using Ionic complexes. The present invention also provides a process for preparation of tenofovir disoproxil or a salt thereof using the tenofovir of the present invention.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: June 16, 2015
    Assignee: Laurus Labs Private Ltd.
    Inventors: Venkata Sunil Kumar Indukuri, Sree Rambabu Joga, Seeta Ramanjaneyulu Gorantla, Satyanarayana Chava
  • Publication number: 20150141375
    Abstract: The present invention provides methods of treating diseases associated with at least one virus. The methods include administering a compound described in the invention in a therapeutically effective amount. According to some aspects of the present invention, the methods may further comprise at least one immunosuppressant agent to treat diseases associated with at least one virus of a subject in need of immunosuppressant agents.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: George R. Painter, Ernest Randall Lanier, Gwendolyn Painter
  • Publication number: 20150141376
    Abstract: Pharmaceutical compositions of anti-viral compounds, process for preparation and method of using the same are provided. Particularly, the present invention relates to chemically stable pharmaceutical compositions of efavirenz, emtricitabine and tenofovir disoproxil fumarate with optionally one or more pharmaceutically acceptable excipients, process for preparation and method for the treatment or prevention of the symptoms or effects of an HIV infection in an infected patient.
    Type: Application
    Filed: November 18, 2014
    Publication date: May 21, 2015
    Inventors: Chandrashekhar Kandi, Nagaprasad Vishnubhotla, Asif Anwar, Krishna Kumar Chegonda, Sivakumaran Meenakshisunderam
  • Publication number: 20150133400
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 14, 2015
    Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
  • Publication number: 20150133404
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
  • Publication number: 20150132258
    Abstract: 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: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman