The Additional Ring Is A Six-membered Hetero Ring Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/318)
  • Patent number: 11026936
    Abstract: Compounds of the formula I in which X, Q, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.
    Type: Grant
    Filed: March 27, 2017
    Date of Patent: June 8, 2021
    Assignee: Merck Patent GmbH
    Inventor: Hans-Peter Buchstaller
  • Patent number: 10759791
    Abstract: Disclosed are compounds that are shown to inhibit the biological activity of nitric oxide synthases (NOSs). Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject in need thereof. Because the disclosed compounds are shown to inhibit the activity of nitric oxide synthases (NOSs), the disclosed compounds and pharmaceutical compositions may be utilized in methods for treating a subject having or at risk for developing a disease or disorder that is associated with NOS activity.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: September 1, 2020
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Heng-Yen Wang, Yajuan Qin, Fengwei Zou, Soo Sung Kang, Qing Jing
  • Patent number: 10736841
    Abstract: Novel compositions including bepotastine besilate and a corticosteroid are provided, compositions including at least about 0.008% w/v benzalkonium chloride, and compositions including hydroxypropylmethyl cellulose E15 LV.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: August 11, 2020
    Assignee: BAUSCH & LOMB INCORPORATED
    Inventors: Angel Padilla, George Baklayan
  • Patent number: 10730863
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: August 4, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: David S. Yoon, Rushith Kumar Anumula, Srinivas Cheruku, Yanting Huang, Elizabeth Anne Jurica, Wei Meng, Susheel Jethanand Nara, Rishikesh Narayan, Ramesh Kumar Sistla, Ximao Wu, Guohua Zhao
  • Patent number: 10669256
    Abstract: The present invention relates to the crystalline forms of a 5-HT1F receptor agonist 2,4,6-trifluoro-N-[6-[(1-methyl-piperidine-4-yl)carbonyl]pyridin-2-yl]-benzene formamide (lasmiditan) and its hydrochloride. The crystalline forms of the present invention have advantages in crystallinity, hygroscopicity, morphology, crystal form stability, and chemical stability as compared with the known forms of lasmiditan and lasmiditan hydrochloride. The present invention also relates to processes for the preparation of the crystalline forms of lasmiditan and lasmiditan hydrochloride, pharmaceutical compositions thereof and their use in treating and/or preventing a patient's migraine and other diseases or conditions associated with 5-HT1F receptor dysfunction.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: June 2, 2020
    Assignee: Hangzhou SoliPharma Co., Ltd.
    Inventors: Xiaohong Sheng, Xiaoxia Sheng, Xiawei Jiang
  • Patent number: 10632116
    Abstract: The present invention relates to the use of 5-HT1 agonists in pharmaceutical compositions, compounds and methods for treatment of movement disorders related to neurological dysfunctions. The invention is particularly relevant for treatment of patients suffering from tardive dyskinesia, Parkinson's disease and associated disorders thereof. Kits of parts comprising the 5-HT1 agonist compounds or pharmaceutical compositions according to the present invention, as well as methods of preparation are also provided by the present invention.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: April 28, 2020
    Assignee: Contera Pharma A/S
    Inventors: John Bondo Hansen, Mikael S. Thomsen
  • Patent number: 10562853
    Abstract: The invention concerns compounds that possess a high affinity at 5-HT1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: February 18, 2020
    Assignees: NEUROLIXIS, UNIVERSITE JAGELLONE
    Inventors: Joanna Sniecikowska, Adam Bucki, Adrian Newman-Tancredi, Mark Andrew Varney
  • Patent number: 10499641
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: September 25, 2017
    Date of Patent: December 10, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Pierre Cristau, Thomas Seitz, Joachim Kluth, Stefan Hillebrand, Juergen Benting, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 10479765
    Abstract: The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: November 19, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Hartmut Beck, Tobias Thaler, Raimund Kast, Daniel Meibom, Mark Meininghaus, Carsten Terjung, Martina Delbeck, Klemens Lustig, Uwe Muenster, Britta Olenik
  • Patent number: 10377739
    Abstract: A compound having the following formula: or a pharmaceutically acceptable salt thereof. A medicament or pharmaceutical composition contains the compound. A method of treating a respiratory tract disease includes administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: August 13, 2019
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Patent number: 10301271
    Abstract: The disclosure relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzoate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: May 28, 2019
    Assignee: Purdue Pharma L.P.
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 10253039
    Abstract: The present invention provides N-benzyl-3-sulfonamidopyrrolidines and related compounds, as well as pharmaceutical compositions and sanitizing compositions containing the same. The compounds and compositions are useful as antibiotic agents. Methods for making and using the compounds and compositions are also described.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: April 9, 2019
    Assignees: Wisconsin Alumni Research Foundation, The Regents of the University of California
    Inventors: Jared T. Shaw, Jared T. Moore, Molly R. Fensterwald, Douglas B. Weibel, Katherine A. Hurley
  • Patent number: 10214540
    Abstract: Provision of orally-available and low-toxic somatostatin receptor subtype 2 agonist. Since the compound represented by the general formula (I): wherein all symbols represent the same meanings as those described in the description, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof is non-peptidic low-molecular compound which has strong somatostatin receptor subtype 2 agonist activity, the compound is orally-available. Additionally, since the compound is low-toxic, the compound is useful for the prevention and/or treatment of the somatostatin related diseases such as acromegaly or gastrointestinal obstruction.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: February 26, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Akiharu Ishida, Takeshi Matsushita, Tetsuya Sekiguchi, Tatsuya Komagata, Takuya Nishio
  • Patent number: 10196377
    Abstract: A compound having the following formula: or a pharmaceutically acceptable salt thereof. A medicament or pharmaceutical composition contains the compound. A method of treating a respiratory tract disease includes administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: February 5, 2019
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Patent number: 10179764
    Abstract: The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.
    Type: Grant
    Filed: July 23, 2016
    Date of Patent: January 15, 2019
    Assignees: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION
    Inventors: Yongseok Choi, Jae-Hong Kim, Kyeong Lee, Hyo-Kyung Han, Jun Dong Wei, Jinsun Kwon, Ja-Il Goo
  • Patent number: 10167265
    Abstract: Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: X1-L-X2 wherein L is a linking moiety comprising an enone; and X1 and X2 are each independently an optionally-substituted N-heterocycle. Also disclosed are method for treating pulmonary conditions and other organ or system conditions with the compounds.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: January 1, 2019
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America as represented by the Department of Veterans Affairs
    Inventor: Raju Reddy
  • Patent number: 10155744
    Abstract: A medicament or pharmaceutical composition for the treatment of a respiratory tract disease, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating a respiratory tract disease includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: December 18, 2018
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Patent number: 10155746
    Abstract: A medicament or pharmaceutical composition for the treatment of respiratory syncytial virus, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating respiratory syncytial virus includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: December 18, 2018
    Assignee: OBSCHESTVO S OGRANICHENNOT OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Patent number: 10155745
    Abstract: A medicament or pharmaceutical composition for the treatment of exacerbations of asthma and chronic obstructive pulmonary disease, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating exacerbations of asthma and chronic obstructive pulmonary disease includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: December 18, 2018
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Patent number: 10155743
    Abstract: Biologically active glutarimide derivatives of the following formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: December 18, 2018
    Assignee: Obschestvo S Ogranichennoi Otvetstvennostiyu “Pharmaenterprises”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Patent number: 10155747
    Abstract: A method for preparing a compound of formula I: or a pharmaceutically acceptable salt thereof, by heating of dicarboxylic acid monoamide of formula II with a dehydrating agent in an organic solvent.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: December 18, 2018
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Patent number: 10100018
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: August 20, 2014
    Date of Patent: October 16, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: William Buffham, Hannah Canning, Richard Davenport, William Farnaby, Stephen Mack, Alka Parmar, Susanne Wright
  • Patent number: 10023565
    Abstract: The present invention relates to a compound of formula (I), a stereomeride, pharmaceutically acceptable salt, a solvate or an N-oxide thereof, a medicine composition comprising the compound, a method for preparing the compound, and a usage of the compound in treating diseases related to Hsp70. The diseases are preferably selected from tumors, neurodegenerative diseases, and allogeneic transplantation rejection and infection.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: July 17, 2018
    Assignee: INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A. CHINA
    Inventors: Wu Zhong, Song Li, Yanqun Zeng, Junhai Xiao, Xinbo Zhou, Zhibing Zheng, Xingzhou Li, Xiaokui Wang, Lili Wang
  • Patent number: 9938279
    Abstract: The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: April 10, 2018
    Assignee: ENERGENESIS BIOMEDICAL CO., LTD
    Inventors: Han-Min Chen, Cheng-Yi Kuo, Chun-Fang Huang, Jiun-Tsai Lin
  • Patent number: 9930890
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: July 5, 2016
    Date of Patent: April 3, 2018
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Pierre Cristau, Thomas Seitz, Joachim Kluth, Stefan Hillebrand, Juergen Benting, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 9879006
    Abstract: The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Grant
    Filed: March 16, 2015
    Date of Patent: January 30, 2018
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Hamed Aissaoui, Christoph Boss, Patrick Bouis, Julien Hazemann, Romain Siegrist
  • Patent number: 9862690
    Abstract: Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: X1-L-X2 wherein L is a linking moiety comprising an enone; and X1 and X2 are each independently an optionally-substituted N-heterocycle. Also disclosed are method for treating pulmonary conditions and other organ or system conditions with the compounds.
    Type: Grant
    Filed: May 9, 2014
    Date of Patent: January 9, 2018
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America as Represented by the Department of Veterans Affairs
    Inventor: Raju Reddy
  • Patent number: 9707218
    Abstract: This invention relates to novel pyrazole-substituted amino-heteroaryl compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of anaplastic lymphoma kinase (ALK).
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: July 18, 2017
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Bhaumik A. Pandya, Craig E. Masse, Ian Robert Silverman, Roger D. Tung
  • Patent number: 9637501
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: May 2, 2017
    Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITED
    Inventor: B. Narasimhulu Naidu
  • Patent number: 9573897
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: February 21, 2017
    Assignee: CHEMOCENTRYX, INC.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Patent number: 9555023
    Abstract: The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: January 31, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Craig Grant, James P. Kanter, Graeme Langlands
  • Patent number: 9522115
    Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: December 20, 2016
    Assignees: Purdue Pharma L.P., The P.F. Laboratories, Inc., Purdue Pharmaceuticals L.P.
    Inventors: Curtis Wright, Benjamin Oshlack, Christopher Breder
  • Patent number: 9457093
    Abstract: A solid dispersion of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and processes for preparing the solid dispersion are provided herein. Also, a pharmaceutical composition comprising a solid dispersion of N4-(4-([1,2,4]triazolo[1,5-?]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and uses thereof are provided herein.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: October 4, 2016
    Assignee: Array BioPharma Inc.
    Inventors: David Shank Fry, Christopher M. Lindemann, Michael Preigh, Corey Jay Bloom, Christopher Donovan Craig, Devon Brevard Dubose, Jeff Gautschi, Dan Smithey
  • Patent number: 9458142
    Abstract: The invention relates to protein-adhesive dyes, to the preparation thereof and to preparations comprising same, and to a method for coloring keratin-containing fibers, in particular for coloring human hair.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: October 4, 2016
    Assignee: Merck Patent GmbH
    Inventors: Thomas Rudolph, Rene Peter Scheurich
  • Patent number: 9422244
    Abstract: This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: August 23, 2016
    Assignee: Abbvie Bahamas Ltd.
    Inventors: Arnold van Loevezijn, Josephus H. M. Lange, Gerrit A. Barf, Arnold P. den Hartog
  • Patent number: 9421165
    Abstract: The present invention relates to oral controlled release pharmaceutical compositions comprising Bepotastine. The oral controlled release pharmaceutical composition comprises Bepotastine or pharmaceutically acceptable salts thereof and at least one release controlling agent. The present invention also provides the use of oral controlled release pharmaceutical compositions of Bepotastine for the treatment of allergic rhinitis and for the treatment of pruritus caused by urticaria.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: August 23, 2016
    Assignee: LUPIN LIMITED
    Inventors: Ashish Ashokrao Deshmukh, Pravin Meghrajji Bhutada, Sajeev Chandran, Shirishkumar Kulkarni
  • Patent number: 9409882
    Abstract: The invention relates to a compound of formula (I) wherein A1, A2 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: August 9, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lilli Anselm, David Banner, Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Beat Spinnler
  • Patent number: 9387173
    Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.
    Type: Grant
    Filed: March 16, 2015
    Date of Patent: July 12, 2016
    Assignees: Purdue Pharma L.P., The P.F. Laboratories, Inc., Purdue Pharmaceuticals L.P.
    Inventors: Curtis Wright, Benjamin Oshlack, Christopher Breder
  • Patent number: 9353051
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: May 31, 2016
    Assignee: SIGA Technologies, Inc.
    Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
  • Patent number: 9278961
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: March 8, 2016
    Assignees: GENENTECH, INC., CURIS, INC.
    Inventors: Janet L. Gunzner, Daniel Sutherlin, Mark S. Stanley, Liang Bao, Georgette M. Castanedo, Rebecca L. Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F. T. Koehler
  • Patent number: 9266856
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: February 23, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Patent number: 9249147
    Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
    Type: Grant
    Filed: July 3, 2014
    Date of Patent: February 2, 2016
    Assignee: CHEMBRIDGE CORPORATION
    Inventor: Vlad Edward Gregor
  • Patent number: 9221797
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: January 30, 2014
    Date of Patent: December 29, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Patent number: 9173883
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: November 3, 2015
    Assignee: NOVARTIS AG
    Inventors: Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Patent number: 9150929
    Abstract: The present invention relates to diagnostic, therapeutic and prognostic methods for thyroid cancers. In one embodiment, the present invention provides a method for treating a an anaplastic thyroid cancer (ATC) patient comprising the step of administering to the patient an effective amount of an anaplastic lymphoma kinase (ALK) inhibitor. In another embodiment, a method for diagnosing ATC in patient comprises the step of performing an assay on a biological sample from the patient to identify the presence or absence of a C3592T and/or a G3602A mutation in exon 23 of the ALK gene according to SEQ ID NO:6, wherein the presence of either of both of the mutations correlates with a diagnosis of ATC in the patient.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: October 6, 2015
    Assignee: The Johns Hopkins University
    Inventors: Michael Mingzhao Xing, Murugan Avaniyapuram Kannan
  • Patent number: 9108922
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: August 18, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Wenrong Huang
  • Patent number: 9090601
    Abstract: The present invention relates to a compound represented by the formula (I) or (I?): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: July 28, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Hiroshi Banno, Masaaki Hirose, Osamu Kurasawa
  • Patent number: 9078886
    Abstract: The present invention features, inter alia, pharmaceutically acceptable compositions that include metyrapol as the sole pharmaceutically active agent; compositions that include metyrapol and at least one additional pharmaceutically active agent; compositions in which the agent targeting the HPA axis is, itself, new or modified (e.g., a bi-specific antibody designed to traverse the blood-brain barrier or a known compound redesigned by, for example, conjugation to a substance that traverses the blood-brain barrier); and compositions in which the agent targeting the HPA axis is newly formulated in such a way that it fails to significantly inhibit cortisol production in the adrenal gland. For example, the composition can be formulated to include a dosage that is too low to reduce plasma cortisol levels or formulated to preferentially affect the skin.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: July 14, 2015
    Assignees: Embera Neurotherapeutics, Inc., Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: Nicholas E. Goeders, Barbara S. Fox, Glenn Guerin
  • Patent number: 9061019
    Abstract: The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.
    Type: Grant
    Filed: February 17, 2014
    Date of Patent: June 23, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Craig Grant, James P. Kanter, Graeme Langlands
  • Patent number: 9062002
    Abstract: The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particularly FabI inhibitors. Formula (I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: June 23, 2015
    Assignees: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn. BHD
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof