Benzo Fused At 4,5-positions Of The Diazole Ring Patents (Class 514/394)
  • Patent number: 10669263
    Abstract: 2-(5-{1-[2-(Difluoromethoxy)-6-fluorobenzyl]-2-methyl-1H-benzimidazol-6-yl}pyrimidin-2-yl)propan-2-ol, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: June 2, 2020
    Assignee: UCB Biopharma SRL
    Inventor: Jag Paul Heer
  • Patent number: 10588880
    Abstract: In one aspect, methods of treating non-alcoholic steatohepatitis (NASH) or preventing or delaying the progression of non-alcoholic fatty liver disease (NAFLD) to NASH are provided. In some embodiments, the method comprises administering a therapeutically effective amount of ubenimex.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: March 17, 2020
    Assignee: Eiger BioPharmaceuticals, Inc.
    Inventors: Xiaofeng Xiong, David A. Cory
  • Patent number: 10584115
    Abstract: Amine substituted pyridine and pyrazine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: March 10, 2020
    Assignee: PTC THERAPEUTICS, INC.
    Inventors: Ramil Baiazitov, Soongyu Choi, Wu Du, Seongwoo Hwang, Chang-Sun Lee, Ronggang Liu, Young-Choon Moon, Steven D. Paget, Hongyu Ren, Nadiya Sydorenko, Richard Gerald Wilde
  • Patent number: 10570262
    Abstract: The present disclosure provides an edible gelatin base film and preparation method thereof, relating to material fields. The preparation method can improve the mechanical property of the film. The films prepared by the method have antibacterial properties, low-temperature stability and high-temperature dissolution, environmental-friendly components. The method includes the following steps: a) preparing gel nanoparticles; b) preparing bacterial cellulose nanoparticles; c) preparing the gelatin base film: mixing pullulan, glycerin, nisin, antibacterial peptide, the gel nanoparticles obtained from step a) and the bacterial cellulose nanoparticles obtained from step b), ultrasonically degassing, then being subjected to coating and drying to obtain the gelatin base film. The preparation method is used to prepare an edible gelatin base film.
    Type: Grant
    Filed: April 24, 2019
    Date of Patent: February 25, 2020
    Assignee: NINGXIA JINBOLE FOOD TECHNOLOGY CO., LTD.
    Inventors: Yuzhu Wu, Zheng Li, Yimin Lu
  • Patent number: 10568891
    Abstract: Disclosed herein is, among other things, a soft gel vaginal pharmaceutical composition and dosage form containing solubilized estradiol for the treatment of vulvovaginal atrophy (VVA) and female sexual dysfunction (FSD).
    Type: Grant
    Filed: December 7, 2016
    Date of Patent: February 25, 2020
    Assignee: TherapeuticsMD, Inc.
    Inventors: Sebastian Mirkin, Julia M. Amadio, Brian A. Bernick
  • Patent number: 10561680
    Abstract: Topical composition for the treatment of mucosal lesions It relates to a topical composition comprising specific amounts of: a) a hyaluronic acid or a pharmaceutically or veterinary acceptable salt thereof, b) one or more adhesive agents, and c) a non-absorbable antibiotic; to delivery devices comprising it; and to its uses in medicine, in particular, in the treatment and/or prevention of mucosal lesions; in the prevention of postpolypectomy syndrome; as adjuvant therapy to mechanical treatments in gastrointestinal perforations, and as sealant treatment in surgical anastomoses and leaks or fistulas in gastrointestinal tract.
    Type: Grant
    Filed: February 25, 2016
    Date of Patent: February 18, 2020
    Assignees: FUNDACIÓ INSTITUT D'INVESTIGACIÓ EN CIÈNCIES DE LA SALUT GERMANS TRIAS I PUJOL, CENTRO DE INVESTIGACIÓN BIOMÉDICA EN RED
    Inventors: Vicente María Lorenzo-Zúñiga García, Ramon Bartolí Solé, Jaume Boix Valverde
  • Patent number: 10537581
    Abstract: According to various embodiments of this disclosure, pharmaceutical compositions comprising solubilized estradiol are provided. In various embodiments, such compositions are encapsulated in soft capsules which may be vaginally inserted for the treatment of vulvovaginal atrophy.
    Type: Grant
    Filed: October 22, 2014
    Date of Patent: January 21, 2020
    Assignee: TherapeuticsMD, Inc.
    Inventors: Brian A. Bernick, Thorsteinn Thorsteinsson, Peter H. R. Persicaner, Janice Louise Cacace, Frederick D. Sancilio, Neda Irani, Julia Amadio
  • Patent number: 10532986
    Abstract: Provided are a phosphodiesterase-4 (PDE4) inhibitor and application thereof in preparation of a medication for treating a disease related to PDE4. Specifically disclosed is a compound as shown in formula (I) and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 22, 2017
    Date of Patent: January 14, 2020
    Assignee: Medshine Discovery Inc.
    Inventors: Yunfu Luo, Chundao Yang, Maoyi Lei, Lanbao Sun, Guoping Hu, Jian Li, Shuhui Chen
  • Patent number: 10435386
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: October 8, 2019
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
  • Patent number: 10406138
    Abstract: The present invention is directed to a combination comprising a proteasome inhibitor and a compound of formula I or a pharmaceutically acceptable salt thereof: to a pharmaceutical composition and to a kit both comprising said combination, to the combination, composition or kit for use in the treatment of cancer, and to a method of treatment of cancer in a patient in need thereof comprising administering to said patient an effective amount of said combination, composition or kit.
    Type: Grant
    Filed: May 21, 2018
    Date of Patent: September 10, 2019
    Assignee: Purdue Pharmaceutical Products L.P.
    Inventors: Thomas Jorg Mehrling, Enrique Maria Ocio
  • Patent number: 10183010
    Abstract: The present invention relates to the technical field of medicinal chemistry, and in particular discloses a 2-oxo-1,2-dihydrobenzo[cd]indole compound and use thereof. The compound and pharmaceutically acceptable salt, isomer, racemate, prodrug, co-crystallized complex, hydrate, and solvate thereof can effectively inhibit the BET bromodomain receptor, and can be used for preparing a medicine for treating cancers, cell proliferative disorders, inflammatory diseases, and autoimmune disorders, sepsis, and viral infections.
    Type: Grant
    Filed: January 27, 2016
    Date of Patent: January 22, 2019
    Assignee: GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES
    Inventors: Yong Xu, Xiaoqian Xue, Yan Zhang, Ming Song
  • Patent number: 10179123
    Abstract: The present invention relates to 2-Aryl- and 2-Arylalkyl-benzimidazoles of general formula (I): in which A, R1, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: July 4, 2016
    Date of Patent: January 15, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Olaf Panknin, Katja Zimmermann, Roland Neuhaus
  • Patent number: 10067120
    Abstract: Use of acetylated tubulin as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject to said compound, wherein the compound is a furazanobenzimidazoles compound of general formula (I).
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: September 4, 2018
    Assignee: BASILEA PHARMACEUTICA AG
    Inventors: Heidi Alexandra Lane, Felix Bachmann
  • Patent number: 9914721
    Abstract: The present invention relates to compounds of the formula (I) wherein Ar1 and Ar2 are as described in the description and to their use as pharmaceuticals for the treatment of sundown syndrome. The invention also relates to the preparation of such compounds and of pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: March 13, 2018
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Christoph Boss, Catherine Roch, Christine Brotschi, Markus Gude, Bibia Heidmann, Francois Jenck, Thierry Sifferlen, Michel Steiner, Jodi T. Williams
  • Patent number: 9909012
    Abstract: Antimicrobial inks, sealants, coatings or varnishes that are manufactured in three distinct phases: Phase 1, which is an oil phase comprising Ethoxylate Alcohol Laureth 7, Didecyldimethylammonium chloride, Glutaric acid dialdehyde, Pinus sylvestris, Alkyldimemylberizylammonium chloride, Parachlorometaxylenol, Ethylenediaminetetraacetic acid, 2-Hydroxypropanoic acid, Hydroxy-9-cis-octadecenoic acid, Cetyl alcohol wax, Octadecenoic acid, Palmityl alcohol, and Epoxy-cis-9-octadecenoic acid; Phase 2, which is a micro-emulsion phase comprising Ethoxylate Alcohol Laureth-7, Cetyl alcohol wax, Pinus sylvestris, and Propan-2-ol and Phase 3, which combines the products of Phases 1 and 2 with a base to produce the ink, sealant, coating or varnish.
    Type: Grant
    Filed: June 5, 2014
    Date of Patent: March 6, 2018
    Inventor: Robert Timothy Gros
  • Patent number: 9845296
    Abstract: The present invention relates to novel 2,5,6-benzimidazole derivatives and pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating a patient infected by Mycobacterium tuberculosis by administering to the patient a 2,5,6-benzimidazole derivative or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: December 19, 2017
    Assignee: The Research Foundation for The State University of New York
    Inventors: Iwao Ojima, Divya Awasthi
  • Patent number: 9775832
    Abstract: Provided is a pharmaceutical composition for oral administration enabling improved solubility, improved dissolution properties, and improved oral absorbability of (2R)—N-({5-[3-(2,5-difluorophenyl)-2-(1,3-dihydro-2H-benzimidazole-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl}sulfonyl)-2-hydroxypropane imide amide (hereinafter referred to as compound A) or a pharmaceutically acceptable salt thereof, as well as size reduction. The pharmaceutical composition for oral administration contains an amorphous form of compound A or its pharmaceutically acceptable salt, and a polymer.
    Type: Grant
    Filed: June 24, 2015
    Date of Patent: October 3, 2017
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Hiroyuki Kojima, Masakazu Miyazaki, Mare Nishiura, Takashi Nishizato
  • Patent number: 9708311
    Abstract: The present invention relates to novel benzimidazole derivatives of the general formula processes for their preparation and their use for the production of pharmaceutical compositions for the treatment of diseases and indications that are connected with the receptor EP4.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: July 18, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Olaf Peters, Nico Bräuer, Thorsten Blume, Antonius Ter Laak, Ludwig Zorn, Jens Nagel, Stefan Kaulfuss, Gernot Langer, Joachim Kuhnke
  • Patent number: 9688657
    Abstract: The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-1-methyl-1H-benzimidazole-5-yl)carbonyl]-(2-pyridinyl) amino}propanoate and Ethyl-3-{[(2-dichloromethyl-1-methyl-1H-benzimidazole-5-yl)carbonyl]-(2-pyridinyl)amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 25, 2014
    Date of Patent: June 27, 2017
    Assignee: USV Private Limited
    Inventors: Laxmikant Narhari Patkar, Harish Kashinath Mondkar, Nitin Dnyaneshwar Arote, Sachin Shivaji Patil, Tanaji Shamrao Jadhav, Nitin Nivrutti Hagavane, Rajesh Ganpat Bhopalkar
  • Patent number: 9642821
    Abstract: The present disclosure provides methods of determining the levels of BRCA1 in a cell, altering the levels of BRCA1 in a cell, determining the likelihood of developing cancer, and determining the prognosis of a patient with cancer using miR-182 and analogs thereof. Importantly, the invention also provides methods of determining whether a patient should be treated with PARP inhibitors, improving PARP therapy in cancer, as well as methods for selecting and improving genotoxic therapies. Also featured are methods of treating patients with cancers based on the expression levels of miR-182. The invention also features compositions comprising miR-182 and analogs thereof, antagomirs of mIR-182 and analogs thereof, in combination with PARP inhibitors and genotoxic agents.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: May 9, 2017
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventor: Dipanjan Chowdhury
  • Patent number: 9623008
    Abstract: In one embodiment, the invention provides a method of treating a subject suffering from a breast cancer tumor which is non-responsive or intrinsically resistant to anti-estrogen therapy comprising administering a therapeutically effective amount of an inhibitor of alternative (ALT) non-homologous end joining (NHEJ) factor to the subject. In another embodiment the invention provides a method of treating a subject who suffers from a pancreatic cancer which is non-responsive to chemotherapy and/or radiation comprising co-administering a therapeutically effective amount of PARP1 inhibitor and a DNA ligase III? inhibitor to the subject. Related diagnostic methods, nucleic acid arrays, devices and kits are also provided.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: April 18, 2017
    Assignees: STC.UNM, UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Alan Edward Tomkinson, Feyruz Rassool
  • Patent number: 9603930
    Abstract: The present invention provides stable bendamustine-containing pharmaceutical compositions suitable for long term storage. The compositions include bendamustine, a pharmaceutically acceptable salt, and/or a hydrate form thereof, a solvent mixture of N,N-dimethylacetamide and glycerin, and an antioxidant. The bendamustine-containing compositions have less than about 2% of total impurities after two month storage at 25° C./60% RH. The pharmaceutical compositions may be used for treating neoplastic diseases.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: March 28, 2017
    Assignee: Navinta, LLC
    Inventor: Mahendra R. Patel
  • Patent number: 9598377
    Abstract: The present invention is directed to particles prepared via the polymerization of at least one surfactant and an isocyanate-containing compound. Pharmaceutical compositions prepared using these particles are also described.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 21, 2017
    Assignee: Cephalon, Inc.
    Inventors: Peter D. Brown, Anthony S. Drager
  • Patent number: 9592407
    Abstract: Pharmaceutical compositions containing a combination of NPM inhibitor and anti-cancer agent are disclosed. Methods of inhibiting or reducing the growth of cancer cells in a subject, by administering an effective amount of nucleophosmin (NPM) inhibitor and one or more anticancer agents, whereby the symptoms and signs of cancer in the subject are reduced are also provided.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: March 14, 2017
    Assignees: CHANG GUNG MEMORIAL HOSPITAL, LINKOU & HSIEH, THOMAS
    Inventor: Sen-yung Hsieh
  • Patent number: 9579384
    Abstract: Methods of treating bendamustine responsive conditions in patients having fluid and/or sodium intake restrictions are disclosed. The methods include identifying patients having such restrictions and in need of bendamustine, and then administering thereto a bendamustine-containing composition in a volume of about 120 ml or less intravenously over a period of about 15 minutes or less. The smaller volumes and reduced sodium load as compared to currently known methods of treatment minimize cardiac and/or renal stress in patients having diseases such as congestive heart failure or renal disease.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: February 28, 2017
    Assignee: EAGLE PHARMACEUTICALS, INC.
    Inventors: Srikanth Sundaram, Scott L. Tarriff
  • Patent number: 9562017
    Abstract: The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation.
    Type: Grant
    Filed: April 28, 2015
    Date of Patent: February 7, 2017
    Assignees: AsrtaZeneca AB, Array BioPharma Inc.
    Inventors: John DeMattei, Tsung-Hsun Chuang, Gorkhn Sharma-Singh, Paul Alfred Dickinson, Mohammed Pervez, Richard Anthony Storey, Christopher John Squire, James Gair Ford, Ronald John Roberts
  • Patent number: 9522907
    Abstract: The present invention provides a compound of general formula A for use as a potential anticancer agent against human cancer cell lines and a process for the preparation thereof wherein R is selected from the group consisting of H, F, Cl, Br, OMe, Me and CF3, R1 is selected from the group consisting of H, 4-F, 4-Cl, 4-Br, 4-CF3, 4-OMe, 3,4-OMe, 3,5-OMe and 3,4,5-OMe, and n is an integer ranging from 1-3.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: December 20, 2016
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kamal Ahmed, Srinivasa Reddy Telukutla, Srinivasulu Vunnam, Venkata Subbarao Ayinampudi, Shankaraiah Nagula, Venkata Phani Surya Vishnu Vardhan Madugulla
  • Patent number: 9476889
    Abstract: Use of acetylated tubulin as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject to said compound, wherein the compound is a furazanobenzimidazoles compound of general formula (I).
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: October 25, 2016
    Assignee: BASILEA PHARMACEUTICA AG
    Inventors: Heidi Alexandra Lane, Felix Bachmann
  • Patent number: 9457027
    Abstract: The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.
    Type: Grant
    Filed: August 26, 2015
    Date of Patent: October 4, 2016
    Assignee: Cellceutix Corporation
    Inventors: Richard W. Scott, Bozena Korczak
  • Patent number: 9458119
    Abstract: A process for the production of a compound of formula (III) which comprises a step of reacting a compound of formula (I) with an excess amount of a compound of formula (II) in absence of aromatic solvent, wherein n is 0, 1, 2, 3 or 4; X is NH, O or S; each R1 group may be the same or different, and is independently selected from the group consisting of hydrogen, hydroxyl, alkoxy, alkyl, carbonyl, carboxyl, carboxylic acid ester, amido, cyano, halogenated aliphatic, nitro, and amino; and R2 group is selected from the group consisting of hydroxyl, Cl, F, Br, amino, and alkoxy.
    Type: Grant
    Filed: February 20, 2012
    Date of Patent: October 4, 2016
    Assignee: RHODIA OPERATIONS
    Inventors: Tao Zhang, Claude Mercier, Olivier Buisine
  • Patent number: 9439889
    Abstract: Compositions and Methods are described in which Albendazole sulfone binds to Wolbachia FtsZ providing anti filarial activity.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: September 13, 2016
    Assignee: The Regents of the University of California
    Inventors: Laura Serbus, Fredric Landmann, Catharina Lindley, Pamela White, William Sullivan
  • Patent number: 9433609
    Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, solvates thereof, wherein R and R? are, each independently, —CR1R2R3, aryl, heteroaryl or heteroC4-6cycloalkyl, whereby aryl and heteroaryl may optionally be substituted with 1 or 2 substituents selected from halo and methyl. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: September 6, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: Koen Vandyck, Stefaan Julien Last, Ioannis Nicolaos Houpis, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 9428515
    Abstract: The present invention encompasses compounds of the general formula I wherein the groups A, R1 to R2 and X have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Grant
    Filed: May 7, 2015
    Date of Patent: August 30, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Harald Engelhardt
  • Patent number: 9427428
    Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, solvates thereof, wherein R and R? are, each independently, —CR1R2R3, aryl, heteroaryl or heteroC4-6cycloalkyl, whereby aryl and heteroaryl may optionally be substituted with 1 or 2 substituents selected from halo and methyl. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: August 30, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: Koen Vandyck, Stefaan Julien Last, Ioannis Nicolaos Houpis, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 9399037
    Abstract: The present invention relates to the use of triazinones such as triazinediones and triazinetriones for triazinetriones for the preparation of compositions for treating animals, in particular treating animals prophylactically, against parasitic protozoans, and to these compositions.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: July 26, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventor: Gisela Greif
  • Patent number: 9376395
    Abstract: The present invention is directed to pharmaceutical compositions comprising: (a) a cyclopolysaccharide and (b) a compound of Formula (I) or its pharmaceutical acceptable salt: wherein X1, X2, Q, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compositions.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: June 28, 2016
    Assignee: Purdue Pharmaceuticals Products L.P.
    Inventors: Yu Chen, Lan Yang, Feiyu Feng, Qiufu Ge, Dianwu Guo, Yi Chen
  • Patent number: 9320730
    Abstract: Provided herein are pharmaceutical compositions comprising nitrogen mustard, for example bendamustine hydrochloride, solid dispersions substantially free of degradants. Also provided are methods of producing and administering nitrogen mustards and in particular bendamustine hydrochloride solid dispersions substantially free of degradants. The pharmaceutical compositions can be used for any disease that is sensitive to treatment with bendamustine hydrochloride, such as neoplastic diseases.
    Type: Grant
    Filed: March 4, 2015
    Date of Patent: April 26, 2016
    Inventor: Vasilios Voudouris
  • Patent number: 9308174
    Abstract: New formulations of bendamustine hydrochloride having HPLC purity higher than 99% obtained through the lyophilization of aqueous solutions without organic solvents, are described.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: April 12, 2016
    Assignee: CHEMI S.P.A.
    Inventors: Stefano Turchetta, Maurizio Zenoni, Paolo Brandi
  • Patent number: 9273010
    Abstract: The present invention provides a process for the preparation of 1H-benzimidazol-1-methyl-5-N,N-di(2-hydroxyethyl)-2-butanoic acid ethyl ester. The present invention also provides a process for the preparation of bendamustine hydrochloride. The present invention further provides a process for the purification of bendamustine hydrochloride.
    Type: Grant
    Filed: May 24, 2012
    Date of Patent: March 1, 2016
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Bandi Vamsi Krishna
  • Patent number: 9266892
    Abstract: The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: February 23, 2016
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Jincong Zhuo, Meizhong Xu, Ding-Quan Qian
  • Patent number: 9238070
    Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R? is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: January 19, 2016
    Assignee: Gilead Calistoga LLC
    Inventors: W. Michael Gallatin, Roger G. Ulrich, Neill A. Giese
  • Patent number: 9233949
    Abstract: One aspect of the invention relates to compounds, compositions and methods for treating oxidative stress and/or hypertension. In certain embodiments, the invention relates to a mixture of tempol and an angiotensin receptor blocker (ARB) and the use of said mixture to treat oxidative stress and/or hypertension. In certain embodiments, the invention relates to a tempol/ARB adduct and the use of said adduct to treat oxidative stress and/or hypertension.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: January 12, 2016
    Assignee: Georgetown University
    Inventors: Milton L. Brown, Yali Kong, Christopher Stuart Wilcox
  • Patent number: 9174986
    Abstract: Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).
    Type: Grant
    Filed: February 23, 2015
    Date of Patent: November 3, 2015
    Assignee: GENZYME CORPORATION
    Inventors: John L. Kane, Jr., Gloria Matthews, Markus Metz, Michael Kothe, Jinyu Liu, Andrew Scholte
  • Patent number: 9162986
    Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: October 20, 2015
    Assignee: PHARMACYCLICS LLC
    Inventors: Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, Steven M. Torkelson, Kieron E. Wesson, Wendy B. Young
  • Patent number: 9149474
    Abstract: The present invention relates to compositions containing stimulant and anti-histamine compounds, to methods for treating symptoms related to inflammation using the combination compounds, and to a method for preparing the compositions.
    Type: Grant
    Filed: May 6, 2012
    Date of Patent: October 6, 2015
    Inventor: Michael Leighton
  • Patent number: 9132120
    Abstract: In one embodiment, the invention provides a method of treating a subject suffering from a breast cancer tumor which is non-responsive or intrinsically resistant to anti-estrogen therapy comprising administering a therapeutically effective amount of an inhibitor of alternative (ALT) non-homologous end joining (NHEJ) factor to the subject. In another embodiment the invention provides a method of treating a subject who suffers from a pancreatic cancer which is non-responsive to chemotherapy and/or radiation comprising co-administering a therapeutically effective amount of PARP1 inhibitor and a DNA ligase III? inhibitor to the subject. Related diagnostic methods, nucleic acid arrays, devices and kits are also provided.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: September 15, 2015
    Assignees: STC.UNM, UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Alan Edward Tomkinson, Feyruz Rassool
  • Patent number: 9101573
    Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: August 11, 2015
    Assignee: VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.
    Inventors: Josep Bassaganya-Riera, Pinyi Lu, Raquel Hontecillas
  • Patent number: 9102692
    Abstract: A method for treating cancer that includes administering a pharmaceutically effective amount of a composition containing a compound represented by formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: August 11, 2015
    Assignees: Chugai Seiyaku Kabushiki Kaisha, F. Hoffmann-La Roche AG
    Inventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
  • Patent number: 9060971
    Abstract: The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a flaviviridae viral infection, for example, hepatitis C virus (HCV), wherein treatment comprises administering a compound effective to inhibit the function of the HCV NS5A protein and an additional compound or combinations of compounds having anti-HCV activity.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: June 23, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Christopher M. Owens, Bradley B. Brasher, Yao-Ling Qiu, Lijuan Jiang
  • Patent number: 9051265
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Grant
    Filed: June 6, 2012
    Date of Patent: June 9, 2015
    Assignee: The Scripps Research Institute
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin