Patents Examined by Deepak Rao
  • 2-imidazolyl-pyrimidine scaffolds as potent and selective inhibitors of neuronal nitric oxide synthase
    Patent number: 9701661
    Abstract: Imidazolyl-pyrimidine and related compounds, as can utilize heme-iron coordination in the selective inhibition of neuronal nitric oxide synthase.
    Type: Grant
    Filed: July 13, 2015
    Date of Patent: July 11, 2017
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Paramita Mukherjee, Hien M. Nguyen
  • Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
    Patent number: 9701643
    Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: July 11, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Brydon L. Bennett, Mercedes Delgado, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mehran F. Moghaddam, Mark A. Nagy, Stephen Norris, David A. Paisner, William J. Romanow, Yoshitaka Satoh, Marianne Sloss, Jayashree Tikhe, Won Hyung Yoon
  • Salt of nitrogen-containing heterocyclic compound or crystal thereof, pharmaceutical composition, and FLT3 inhibitor
    Patent number: 9701644
    Abstract: An object of the present invention is to provide a compound and pharmaceutical composition showing superior stability and/or solubility, etc. and having superior FLT3 inhibitory activity. The present invention provides a salt of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide, or a crystal thereof. Since the salt or a crystal thereof has superior FLT3 inhibitory activity and shows superior physicochemical properties as drugs, such as storage stability, solubility, and so forth, it is useful for treatments of diseases or conditions relating to FLT3. The present invention also provides a pharmaceutical composition and FLT3 inhibitor containing the salt or a crystal thereof.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: July 11, 2017
    Assignee: FUJIFILM Corporation
    Inventors: Shinsuke Mizumoto, Takuya Matsumoto
  • Heteroaryl inhibitors of sumo activating enzyme
    Patent number: 9695154
    Abstract: Disclosed are compounds of formula (I); or a pharmaceutically acceptable salt thereof; wherein Y, Ra, Ra?, Rc, Rf, X2, Rd, Rd?, Re, Re?, m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders.
    Type: Grant
    Filed: July 1, 2014
    Date of Patent: July 4, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Matthew O. Duffey, Dylan B. England, Zhigen Hu, Mitsuhiro Ito, Steven P. Langston, Charles McIntyre, Hirotake Mizutani, He Xu
  • 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
    Patent number: 9688672
    Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
    Type: Grant
    Filed: July 13, 2016
    Date of Patent: June 27, 2017
    Assignee: NOVARTIS AG
    Inventors: Thomas Raymond Caferro, Zhuoliang Chen, Young Shin Cho, Abran Q. Costales, Julian Roy Levell, Gang Liu, James R. Manning, Martin Sendzik, Cynthia Shafer, Michael David Shultz, James Clifford Sutton, Yaping Wang, Qian Zhao
  • Pyrimidine compounds and pyrimido indole compounds and methods of use
    Patent number: 9688690
    Abstract: The present invention discloses a compound comprising the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2, and optionally comprising a pharmaceutically acceptable salt, hydrate, or solvate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: June 27, 2017
    Assignee: Duquesne University of the Holy Ghost
    Inventor: Aleem Gangjee
  • Tyrosine kinase inhibitors
    Patent number: 9688676
    Abstract: The present disclosure provides compounds that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase (“BTK”) inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: June 27, 2017
    Assignee: PRINCIPIA BIOPHARMA INC.
    Inventor: Timothy D. Owens
  • Heteroaryl compounds useful as inhibitors of SUMO activating enzyme
    Patent number: 9683003
    Abstract: Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, Ra, Ra?, Rb, Rc, X1, X2, X3, Rd, Z1, and Z2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: June 20, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Matthew O. Duffey, Dylan England, Scott Freeze, Zhigen Hu, Steven Langston, Charles McIntyre, Hirotake Mizutani, Koji Ono, He Xu
  • Pyrazolyl pyrimidinamine compound and application thereof
    Patent number: 9682962
    Abstract: Disclosed are pyrazolyl pyrimidinamine compounds with structures as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a broad spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, anthracnosis of cucumber and the like, and especially have better control effect on downy mildew of cucumber, powdery mildew of wheat and anthracnosis of cucumber. The compounds of present invention also show good insecticidal activity, part of the compounds, at very low doses, have excellent control effect on diseases caused by Plutella xylostella, armyworm, Myzus persicae, Tetranychus cinnabarinus etc.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: June 20, 2017
    Assignee: Shenyang Sinochem Agrochemicals R&D CO., LTD.
    Inventors: Changling Liu, Xufeng Sun, Jie Zhao, Lizeng Wang, Keke Li, Jinbo Zhang, Xuanming Chen, Aiying Guan, Yuquan Song, Jie Lan, Sen Ma, Lijun Ru
  • Substituted biphenyl analogues as dual inhibitors of aromatase and sulfatase
    Patent number: 9682941
    Abstract: The present invention relates to new biphenyl derivatives of formula These compounds acting as aromatase and sulfatase inhibitors, they are particularly useful for treating pathological conditions or diseases in which aromatase and sulfatase are involved. Moreover, the present invention provides processes for the preparation of these compounds. The invention also relates to pharmaceutical compositions containing said products and their use for the preparation of a medicament, in particular for the treatment of diseases characterized by aromatase and sulfatase activity such as hormone-dependent cancers.
    Type: Grant
    Filed: December 31, 2013
    Date of Patent: June 20, 2017
    Assignee: ESTRYX PHARMA LIMITED
    Inventors: Serge Auvin, Olivier Lavergne, Qi Chao, Yufeng Chen
  • Heteroaryl substituted pyrazoles
    Patent number: 9682974
    Abstract: Compounds of formula (I), processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: October 27, 2014
    Date of Patent: June 20, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Anne Mengel, Anja Richter, Marion Hitchcock, Hans Briem, Gerhard Siemeister, Wilhelm Bone, Amaury Ernesto Fernandez-Montalvan, Jens Schröder, Simon Holton, Cornelia Preuβe, Ursula Mönning
  • SIK inhibitor for use in a method of treating an inflammatory and/or immune disorder
    Patent number: 9670165
    Abstract: The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 6, 2017
    Assignees: Dana-Farber Cancer Institute, Inc., University Court of the University of Dundee
    Inventors: Philip Cohen, Kristopher Clark, Hwan Geun Choi, Nathanael Gray
  • Metalloenzyme inhibitor compounds as fungicides
    Patent number: 9663491
    Abstract: The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: May 30, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Michael R. Loso, Gary D. Gustafson, Asako Kubota, Maurice C. Yap, Zachary A. Buchan, Kimberly M. Steward, Michael T. Sullenberger, William J. Hoekstra, Christopher M. Yates
  • 5-(trifluoromethyl)pyrimidine derivatives and method for producing same
    Patent number: 9656970
    Abstract: Provided are 5-(trifluoromethyl)pyrimidine derivatives useful as intermediates for pharmaceuticals and agrochemicals and as intermediates for electronic materials and methods for producing the same. 2,4-dichloro-5-(trifluoromethyl)pyrimidine is reacted with 2,2,2-trifluoroethanol, benzyl alcohol, or benzenethiol to obtain the intended 2-(2,2,2-trifluoroethoxy)-4-chloro-5-(trifluoromethyl)pyrimidine, 2-benzyloxy-4-chloro-5-(trifluoromethyl)pyrimidine, 2,4-bis(2,2,2-trifluoroethoxy)-5-(trifluoromethyl)pyrimidine, or 2-chloro-4-phenylthio-5-(trifluoromethyl)pyrimidine.
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: May 23, 2017
    Assignee: TOSOH F-TECH, INC.
    Inventors: Takumi Kagawa, Daiki Shigehiro, Kosuke Kawada
  • N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfoximine group
    Patent number: 9650361
    Abstract: The present invention relates to disubstituted N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: May 16, 2017
    Assignee: BAYER PHARAM AKTIENGESELLSCHAFT
    Inventors: Ulrich Lücking, Niels Böhnke, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Dirk Kosemund, Rolf Bohlmann, Ludwig Zorn
  • Voriconazole sodium phosphate hydrates and polymorphs thereof
    Patent number: 9650400
    Abstract: The present invention relates to a voriconazole sodium phosphate hydrate, polymorphs thereof, a preparation method thereof, and use thereof, wherein the voriconazole phosphate salt hydrate prepared by using an isopropanol-water system, ethanol-water system, or an ethanol system comprises different crystal forms. And these kinds of crystal forms have favorable water solubility and stability and feature a simple manufacturing process. The voriconazole phosphate salt hydrate is principally used for treatment of fungal infections.
    Type: Grant
    Filed: September 23, 2014
    Date of Patent: May 16, 2017
    Assignee: SHAANXI SYNTHETIC PHARMACEUTICAL Co., LTD.
    Inventor: Qiyuan Zhang
  • Substituted benzylpyrazoles
    Patent number: 9643953
    Abstract: Compounds of formula (I) and their use as pharmaceutical.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: May 9, 2017
    Assignees: BAYER INTELLECTUAL PROPERTY GMBH, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Knut Eis, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Simon Holton, Mark Jean Gnoth, Cornelia Preuβe
  • Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase
    Patent number: 9636341
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: May 2, 2017
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marc Gustaaf Celine Verdonck, Patrick Rene Angibaud, Bruno Roux, Isabelle Noelle Constance Pilatte, Peter Ten Holte, Janine Arts, Kristof Van Emelen
  • Methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds
    Patent number: 9636333
    Abstract: The present disclosure provides methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, including rheumatoid arthritis, having the structure of Formula (I): wherein R1, R2, R3, R4, R5 and X are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: May 2, 2017
    Assignee: CONFLUENCE LIFE SCIENCES, INC.
    Inventors: Susan L. Hockerman, Joseph B. Monahan, Shaun R. Selness
  • Double donor functionalisation of the peri-positions of perylene and naphthalene monoimide via versatile building blocks
    Patent number: 9630973
    Abstract: The present invention provides the compounds of formulae (3) and (1) wherein n is 0 or 1, R13 and R14 are the same or different and are selected from the group consisting of NHR310, NR311R312, OR313, SR314 and R315, or R13 and R14 together are selected from the group consisting of (a), (b) and (c), and X is CI, Br of I, and a process for the preparation of compounds of formula (3) comprising the compounds of formula (1) as key intermediates.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: April 25, 2017
    Assignees: BASF SE, Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
    Inventors: Henrike Wonneberger, Helmut Reichelt, Yulian Zagranyarski, Chen Li, Klaus Muellen, Long Chen