Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
  • Patent number: 10357508
    Abstract: In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid prodrug (e.g., galangin prodrug).
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 23, 2019
    Assignee: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen
  • Patent number: 10253044
    Abstract: The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: April 9, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Yujun Zhao, Bing Zhou, Angelo Aguilar, Liu Liu, Longchuan Bai, Donna McEachern, Duxin Sun, Bo Wen, Ruijuan Luo, Ting Zhao, Arul Chinnaiyan, Irfan A. Asangani, Jeanne Stuckey, Jennifer Lynn Meagher, Xu Ran, Yang Hu
  • Patent number: 10226464
    Abstract: The present invention provides, inter alia, compounds capable of inhibiting NF-?B. Pharmaceutical compositions containing and methods of using the compounds are also provided herein.
    Type: Grant
    Filed: December 29, 2016
    Date of Patent: March 12, 2019
    Assignee: ImmuneTarget, Inc.
    Inventors: Samedy Ouk, Hsiou-Chi Liou
  • Patent number: 10179790
    Abstract: A compound of formula I, (I) or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: January 15, 2019
    Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNING
    Inventors: Martin Scobie, Olov Wallner, Tobias Koolmeister, Karl Sven Axel Vallin, Carl Martin Henriksson, Sylvain Jacques, Evert Homan, Thomas Helleday
  • Patent number: 10166271
    Abstract: This disclosure reveals that cyclic corticotrophin releasing factor (CRF) antagonist peptides (such as astressin B, its functional fragments, and their derivatives) induce hair growth and prevent hair loss in vivo. This important discovery enables, for instance, methods of promoting hair growth, and methods of treating hair loss (such as the hair loss that occurs normally in some individuals or that is the result of a health disorder or therapeutic treatment). Exemplary cyclic CRF antagonist peptides useful in the disclosed methods are provided throughout the disclosure.
    Type: Grant
    Filed: June 20, 2007
    Date of Patent: January 1, 2019
    Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, SALK INSTITUTE FOR BIOLOGICAL STUDIES
    Inventors: Million Mulugeta, Lixin Wang, Yvette Taché, Jean Rivier
  • Patent number: 10149852
    Abstract: The present disclosure describes the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogs/derivatives as well as their acceptable salts, for treating neuropathic pain resulting from chemotherapy. Methods, compositions, dose units and dose forms of tetrodotoxin related to the use are described.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: December 11, 2018
    Assignee: WEX PHARMACEUTICALS INC.
    Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Jose Manuel Baeyens, Susan Lu, Donald Wong, Walter Korz
  • Patent number: 10085991
    Abstract: The present invention is directed to formulations comprising PVP polymer, a dispersion of a compound of Formula I (API), and citric acid, which formulations mitigate the effects of coadministering the compound of Formula I with a proton pump inhibitor compound.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 2, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lei Zhu, Yvonne Cegielnik, Qun Lu
  • Patent number: 10005789
    Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), according to Formula I, below, wherein R1, R2, R3 and R4 are as defined herein, useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: June 26, 2018
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
  • Patent number: 9981921
    Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: May 29, 2018
    Assignee: ArQule, Inc.
    Inventors: Craig Bates, David P. Reed
  • Patent number: 9968574
    Abstract: The present invention provides, among other things, therapeutic compositions and methods that can effectively treat, slow or prevent a neurological disease (e.g., a neurodegenerative disease, e.g., mild cognitive impairment (MCI) or Alzheimer's disease (AD)), in particular, based on therapeutically effective amount of nifedipine, oxidized or nitroso nifedipine derivatives, lactam (e.g., a compound of formula (Ic) or (Ic-i), e.g., NFD-L1), thyroxine (T4), triiodothyronine (T3) and combinations thereof.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: May 15, 2018
    Assignee: The University of Kentucky Research Foundation
    Inventors: Mark Lovell, Bert Lynn
  • Patent number: 9896455
    Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
    Type: Grant
    Filed: August 22, 2016
    Date of Patent: February 20, 2018
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9802955
    Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: October 3, 2016
    Date of Patent: October 31, 2017
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9790234
    Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: October 17, 2017
    Assignee: NIMBUS IRIS, INC.
    Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
  • Patent number: 9717903
    Abstract: Methods to restore and/or improve the libido, the sex drive, in males and females, without introducing any external unnatural drugs. The process utilizes a TENS/EMS (Transcutaneous Electrical Nerve Stimulation/Electronic Muscle Stimulation) machine to naturally generate the increased production by the human body's nerve fiber's neurotransmitters.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: August 1, 2017
    Inventor: Gary Barrett
  • Patent number: 9708332
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4 and n are defined herein, are useful as inhibitors of RSV.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: July 18, 2017
    Assignee: MEDIVIR AB
    Inventors: Claudio Sturino, Teddy Halmos, Anne Decor, Martin Duplessis, Patrick Deroy, Araz Jakalian, Louis Morency, Cyrille Kuhn, Chantal Grand-Maitre, Martin Tremblay, Christian Brochu
  • Patent number: 9695135
    Abstract: The invention provides compounds of formula I: and salts thereof wherein R1-R4 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts, and methods for their use in therapy. The compounds have useful antiviral properties.
    Type: Grant
    Filed: May 11, 2015
    Date of Patent: July 4, 2017
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Eddy Arnold, Joseph D. Bauman, John E. Kerrigan, Ajit K. Parhi, Kalyan Das, Cody Kelley, Dishaben V. Patel
  • Patent number: 9649302
    Abstract: The present disclosure relates to pharmaceutical compositions useful for (and to a method of) treating autoimmune, respiratory and/or inflammatory diseases and conditions. The method involves administering to a subject in need thereof roflumilast N-oxide by inhalation. The present disclosure particularly relates to the treatment of asthma and chronic obstructive pulmonary disease (COPD) by administering roflumilast N-oxide by inhalation.
    Type: Grant
    Filed: January 28, 2014
    Date of Patent: May 16, 2017
    Assignee: INCOZEN THERAPEUTICS PVT. LTD.
    Inventor: Swaroop K. Vakkalanka
  • Patent number: 9636342
    Abstract: The invention provides a method for treating prostate cancer in a subject comprising administering to the subject an effective amount of a selective inhibitor of one or more of CDK8 and CDK19. In some embodiments the inhibitor inhibits CDK19. In some embodiments, the inhibitor inhibits CDK8 at a Kd of lower than 200 nM and/or inhibits CDK19 at a Kd of lower than 100 nM. In some embodiments, the prostate cancer is androgen independent. In some embodiments, the prostate cancer is androgen independent due to one or more of androgen receptor gene amplification, androgen receptor gene mutation, ligand-independent transactivation of androgen receptor and activation of intracellular androgen synthesis. In some embodiments, the inhibitor inhibits increased activity of NF-?B. In some embodiments, the inhibitor does not inhibit increased basal levels of NF-?B. In some embodiments, inhibition of one or more genes by AR is not inhibited.
    Type: Grant
    Filed: November 1, 2013
    Date of Patent: May 2, 2017
    Assignee: University of South Carolina
    Inventors: Mengqian Chen, Igor Roninson
  • Patent number: 9604937
    Abstract: A compound of formula (I), or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: March 28, 2017
    Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNING
    Inventors: Martin Scobie, Thomas Helleday, Tobias Koolmeister, Sylvain Jacques
  • Patent number: 9585885
    Abstract: [Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D2 receptors. [Solution] The present invention provides a compound represented by the general formula (I): in which R1 is C1-6 alkyl or the like; R2 is hydrogen or the like; R3 and R4 are each hydrogen, C1-6 alkyl, R10R11N—C1-6 alkyl, aralkyl, or the like; R5 and R6 are hydrogen or the like; and R7 is hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine D2 receptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 7, 2017
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Toshihiro Nishimura, Yasunori Ueno, Kiyoshi Kasai, Masako Yoshida
  • Patent number: 9556187
    Abstract: This disclosure relates to novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities. A tricyclic heterocyclic compound represented by the formula (Ib), wherein the rings Ab and Bb, Xb, Yb, R1b, R2b, R3b, L1b, L2b, L3b and nb are as defined in the specification.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: January 31, 2017
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
  • Patent number: 9504688
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: November 29, 2016
    Assignees: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, THE CURATORS OF THE UNIVERSITY OF MISSOURI
    Inventors: David Ginsburg, Scott D. Larsen, Bryan Yestrepsky, Hongmin Sun
  • Patent number: 9505756
    Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: November 29, 2016
    Assignee: HYDRA BIOSCIENCES, INC.
    Inventors: Xinyuan Wu, Spencer David Kimball, Ping Chen, Ding Zhou, Shaoping Peng
  • Patent number: 9422297
    Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: August 23, 2016
    Assignee: Duquesne University of the Holy Ghost
    Inventor: Aleem Gangjee
  • Patent number: 9415005
    Abstract: This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: August 16, 2016
    Assignee: VeroScience LLC
    Inventor: Anthony H. Cincotta
  • Patent number: 9403778
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides dermatological compositions comprising a compound of formula I or mixtures of one or more compounds of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for protecting skin or DNA from photodamage or repairing photodamaged skin or DNA.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: August 2, 2016
    Assignee: Regents of the University of Minnesota
    Inventors: Robert Vince, Abbas Raza, Christine Dreis
  • Patent number: 9402830
    Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: August 2, 2016
    Assignee: Melior Discovery, Inc.
    Inventors: John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
  • Patent number: 9382287
    Abstract: Methods are provided for using methotrexate (MTX) active agents in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of an MTX active agent in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2?-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions and kits that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: July 5, 2016
    Assignee: Tosk, Inc.
    Inventors: William A. Garland, Brian D. Frenzel, Travis Karg
  • Patent number: 9365575
    Abstract: The present invention relates to compounds of Formula I or a pharmaceutically acceptable salt thereof, wherein variables R, Ar, X, and Ar1 and n are as defined herein. The compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: June 14, 2016
    Assignee: Allergan, Inc.
    Inventors: Thomas C. Malone, Julie A. Wurster, Clarence Eugene Hull, III
  • Patent number: 9359370
    Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: June 7, 2016
    Assignee: Beta Pharma, Inc.
    Inventors: Yinxiang Wang, Guojian Xie, Lieming Ding, Fenlai Tan, Yunyan Hu, Wei He, Bin Han, Wei Long, Yong Liu, Haima Ai, Charles Davis, Don Zhang
  • Patent number: 9301958
    Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: April 5, 2016
    Assignee: Phytotox Limited
    Inventor: Nestor Antonio Lagos Wilson
  • Patent number: 9303035
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: April 5, 2016
    Assignee: Novartis AG
    Inventors: Mahbub Ahmed, Alexander Ashall-Kelly, Graham Charles Bloomfield, Louisa Gueritz, Jeffrey McKenna, Joseph McKenna, Simon Mutton, Rakesh Parmar, Jon Sheperd, Paul Wright
  • Patent number: 9284335
    Abstract: Described herein are compounds and chemical entities of Formula (I), methods of their synthesis, compositions comprising them, and their use in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: March 15, 2016
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Amy Allan, Bryan Branstetter, Brian Dyck, Laurent Gomez, Tami Jo Marrone, Marco Peters, Michael I. Weinhouse
  • Patent number: 9284318
    Abstract: The present invention relates to novel kinase inhibitors. Compounds of this class have been found to be effective inhibitors of protein kinases, including members of PDGFR and VEGFR families.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: March 15, 2016
    Assignee: Pharmascience, Inc.
    Inventors: Alain Laurent, Yannick Rose, Stephen Morris, James Jaquith
  • Patent number: 9260452
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: February 16, 2016
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Patent number: 9227979
    Abstract: Disclosed are compounds of the formula (I) which are fluorescently labeled antagonists of the A3 adenosine receptor: wherein A, R1, R2, and Y are as described herein. Also disclosed are diagnostic compositions and a method of diagnosis of a patient for a possible treatment by an antagonist of the A3 adenosine receptor, involving the use of one or more of these compounds as diagnostic agents.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: January 5, 2016
    Assignees: The United States of America, as represented by The Secretary, Department of Health and Human Services, Universita Degli Studi Di Trieste, Universita Degli Studi Di Padova
    Inventors: Kenneth A. Jacobson, Santhosh Kumar Thatikonda, Eszter Erika Kozma, Giampiero Spalluto, Stefano Moro, Stephanie Federico
  • Patent number: 9181269
    Abstract: The present invention discloses novel enantiomeric antifungal compounds of Formula (1a) and Formula (1b) containing thieno-[2,3-d]Jpyrimidin-4(3H)-one moiety and pharmaceutically acceptable salts thereof, method of preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these compounds.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: November 10, 2015
    Assignees: FDC Limited, Council for Scientific & Industrial Research
    Inventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmeshwer Prabhkara Sawargave, Subhash Prataprao Chavan, Mohan Anand Chandavarkar, Ramkrishnan Ramachandran Iyer, Vikas Vasant Nawathye, Gajanan Jalindar Chavan, Amit Chandrakant Tawte, Deepali Damodar Rao
  • Patent number: 9173846
    Abstract: This invention provides novel solid pharmaceutical compositions and processes for the bulk production of said compositions. This invention also provides methods of using the pharmaceutical compositions in the treatment of cancer.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: November 3, 2015
    Assignee: MILLENNIUM PHARMACEUTICALS, INC.
    Inventor: Bhavishya Mittal
  • Patent number: 9163022
    Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to rheumatoid arthritis.
    Type: Grant
    Filed: September 4, 2014
    Date of Patent: October 20, 2015
    Assignee: vTv Therapeutics LLC
    Inventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
  • Patent number: 9107925
    Abstract: The invention concerns a sodium channel blocker for the treatment of a reduction or loss of superficial sensitivity or sense of touch of a human being or another mammal.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: August 18, 2015
    Assignee: PHYTOTOX LIMITED
    Inventors: Max Rutman, Jean J. Pilorget, Constanza Sigala, Pablo Valenzuela
  • Patent number: 9085586
    Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: July 21, 2015
    Assignee: Nimbus Iris, Inc.
    Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
  • Patent number: 9085588
    Abstract: The present invention relates to the technical field of medicine, and specifically provides methods for preparing Icotinib, Icotinib hydrochloride, and intermediates thereof. These methods avoid the use of phosphorus oxychloride, thereby greatly reducing the emission of pollutants, which is of major benefits to the economy and environment.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: July 21, 2015
    Assignee: Betta Pharmaceuticals Co., Ltd.
    Inventors: Shaojing Hu, Wei Long, Fei Wang, Zongquan Li
  • Patent number: 9073936
    Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: July 7, 2015
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
  • Patent number: 9045489
    Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: October 9, 2012
    Date of Patent: June 2, 2015
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Publication number: 20150141445
    Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
    Type: Application
    Filed: September 25, 2014
    Publication date: May 21, 2015
    Inventor: Aleem Gangjee
  • Publication number: 20150141444
    Abstract: The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: May 21, 2015
    Inventors: Scott D. Kuduk, Christina Ng DiMarco, Thomas J. Greshock
  • Publication number: 20150141408
    Abstract: The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Publication number: 20150141415
    Abstract: The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 21, 2015
    Inventors: Omonike Arike Olaleye, Sarah Finney John, Adaugo Chimzurum Isichei, Jun O Liu, Rosa Maldonado, Janice Endsley
  • Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and 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 a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Publication number: 20150132352
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).
    Type: Application
    Filed: May 2, 2013
    Publication date: May 14, 2015
    Inventors: Hongmin Sun, Bryan Yestrepsky, David Ginsburg, Scott D. Larsen