Patents Examined by Brian McDowell
  • 17?-hydroxylase/C-lyase inhibitors
    Patent number: 9029399
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: May 12, 2015
    Assignee: Novartis AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Saumitra Sengupta
  • Quinazoline based EGFR inhibitors containing a zinc binding moiety
    Patent number: 9024024
    Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: May 5, 2015
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
  • Substituted chromenes as kinase modulators
    Patent number: 9018375
    Abstract: The present invention provides PI3K protein kinase modulators of formula (I): wherein R, R1, R2, L1, Cy1, Cy2 and n are as described herein, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: April 28, 2015
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V. S. Vakkalanka
  • Hydroxygallium porphyrazine derivative mixture and electrophotographic photoconductor
    Patent number: 9005856
    Abstract: A hydroxygallium porphyrazine derivative mixture including: a plurality of different hydroxygallium porphyrazine derivatives each represented by the following General Formula (A-2): where A1, A2, A3, A4, B1, B2, B3 and B4 each independently represent a nitrogen atom or a carbon atom bonded to hydrogen, with the proviso that both of A1 and B1 are carbon atoms each bonded to hydrogen or only one of A1 and B1 is a nitrogen atom, both of A2 and B2 are carbon atoms each bonded to hydrogen or only one of A2 and B2 is a nitrogen atom, both of A3 and B3 are carbon atoms each bonded to hydrogen or only one of A3 and B3 is a nitrogen atom, and both of A4 and B4 are carbon atoms each bonded to hydrogen or only one of A4 and B4 is a nitrogen atom.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Ricoh Company, Ltd.
    Inventors: Tomoyuki Shimada, Ryota Arai
  • 5,8-difluoro-4-(2-(4-(heteroaryloxy)-phenyl)ethylamino)quinazolines and their use as agrochemicals
    Patent number: 9000162
    Abstract: The present disclosure relates to compounds of Formula 1,5,8-difluoro-4-(2-(4-(heteroaryloxy)phenyl)ethylamino)quinazolines, and their use as agrochemicals and animal health products.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: April 7, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: William K. Brewster, Carla J. R. Klittich, Chenglin Yao, Yuanming Zhu, Brent J. Rieder
  • Compound having activity of blocking NMDA receptor channel, and pharmaceutical agent using the same
    Patent number: 8987253
    Abstract: [PROBLEMS] To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. [MEANS FOR SOLVING PROBLEMS] A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: March 24, 2015
    Assignee: National University Corporation Chiba University
    Inventors: Kazuei Igarashi, Hiromitsu Takayama
  • Three-dimensional structure and method of producing the same
    Patent number: 8987439
    Abstract: The three-dimensional structure of the present invention is a three-dimensional structure formed on a base. This three-dimensional structure contains a plurality of porphyrins, a plurality of first metal ions, and a plurality of specific organic molecules. The porphyrin contains two or more functional groups. The first metal ion is a metal ion for linking the functional group of one porphyrin to the functional group of another porphyrin. The above specific organic molecule is an organic molecule that forms a coordinate bond with a metal ion contained in the two-dimensional structure and that has only one site to coordinate to the metal ion.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: March 24, 2015
    Assignee: Japan Science and Technology Agency
    Inventors: Rie Makiura, Hiroshi Kitagawa
  • Medicine for treating ischemic brain injury and its sequelae, and preparation method thereof
    Patent number: 8987449
    Abstract: Disclosed in the present invention are a compound of the general structure formula LQC-T as shown below, wherein R represents an aromatic organic acid or phenol or the structural analog thereof, such as protocatechuic acid, protocatechuic aldehyde, vanillic acid, gallic acid, caffeic acid, ferulic acid etc., and the synthesis and use of the compound. The compounds promote new blood vessel growth in the chick embryo chorioallantoic membrane, wherein LQC-T4 can be used to prepare a medicine for treating ischemic brain injury (stroke) and its sequelae.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: March 24, 2015
    Assignee: Haimin Lei
    Inventors: Haimin Lei, Ying Hong
  • Quinazoline based EGFR inhibitors containing a zinc binding moiety
    Patent number: 8975401
    Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (I) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: March 10, 2015
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai, Stephen Gould
  • Compounds useful as inhibitors of ATR kinase
    Patent number: 8969356
    Abstract: The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: March 3, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Joanne Pinder, Stephen Young, Philip Michael Reaper
  • Compounds useful as inhibitors of ATR kinase
    Patent number: 8962631
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula II: wherein the variables are as defined herein.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: February 24, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Michael O'Donnell, Philip Michael Reaper
  • Tricyclic tetrahydroquinoline antibacterial agents
    Patent number: 8952149
    Abstract: Described herein are antibacterial compounds of formula I, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: February 10, 2015
    Assignee: Zoetis LLC
    Inventors: Michael Curtis, Timothy Allan Johnson, Manjinder S. Lall, Peter Laurence Toogood, Joseph S. Warmus
  • Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents
    Patent number: 8946233
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: February 3, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Aryl- and heteroaryl- nitrogen-heterocyclic compounds as PDE10 inhibitors
    Patent number: 8946230
    Abstract: Aryl- and heteroaryl-nitrogen heterocyclic compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, p, q, R1, R2, R3, X1, X2, X3, Y1 and Y2 are defined herein; and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: February 3, 2015
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Kristin L. Andrews, Michael J. Frohn, Paul E. Harrington, Alexander J. Pickrell, Robert M. Rzasa
  • Pheophorbide-? conjugates and their uses
    Patent number: 8940783
    Abstract: The present invention relates to a pheophorbide-? conjugate or its salt, solvate or hydrate. The pheophorbide-? conjugate of the present invention exhibiting fluorescence upon its introduction into cells and degradation inhibits the survival of various cancer cells. Especially, the conjugate of pheophorbide-? (1) and doxorubicin shows higher fluorescence intensity at lower pH (cancer environment). Therefore, the present composition for photodynamic therapy (PDT) of cancers is also very useful in detecting cancers. Interestingly, the anticancer effects of the present composition are dually exerted with help of both the photosensitizer and the anticancer drug of the present conjugates.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: January 27, 2015
    Assignee: Gwangju Institute of Science and Technology
    Inventors: Yong-Chul Kim, Hyo Jin Ko, Hyun You, Jung-Hoon Yoon, Hyo-Eun Yoon
  • Pyridopyrazine derivatives and their use
    Patent number: 8937068
    Abstract: Pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: January 20, 2015
    Assignee: Zentaris GmbH
    Inventors: Irene Seipelt, Eckhard Claus, Eckhard Guenther, Tilmann Schuster, Michael Czech, Emmanuel Polymeropoulos
  • Quinazolinones as prolyl hydroxylase inhibitors
    Patent number: 8937078
    Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: February 10, 2010
    Date of Patent: January 20, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, Jr., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Pyridone and pyridazinone derivatives as anti-obesity agents
    Patent number: 8933079
    Abstract: Pyridone and pyridazinone derivatives that are active against the melanin-concentrating hormone (MCH) and useful as anti-obesity pharmaceuticals.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: January 13, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Oost, Ralf Lotz, Dirk Stenkamp
  • JAK kinase modulating compounds and methods of use thereof
    Patent number: 8927711
    Abstract: Provided herein are quinazoline compounds of formula (I): The compounds are useful for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: January 6, 2015
    Assignee: Ambit Biosciences Corp.
    Inventors: Sunny Abraham, Qi Chao, Michael J. Hadd, Mark W. Holladay, Gang Liu, Eduardo Setti
  • Heterocyclic compound and use thereof
    Patent number: 8916551
    Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda