Patents Examined by Deepak Rao
  • Substituted phenyl-Spleen Tyrosine Kinase (Syk) inhibitors
    Patent number: 9353066
    Abstract: The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: May 31, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Andrew M. Haidle, Jason Burch, Daniel Guay, Jacques Yves Gauthier, Joel Robichaud, Jean Francois Fournier, John Michael Ellis, Matthew Christopher, Solomon D. Kattar, Graham F. Smith, Alan B. Northrup
  • Solid state forms of a quinazoline derivative and its use as a BRAF inhibitor
    Patent number: 9353097
    Abstract: This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: May 31, 2016
    Assignee: Ignyta, Inc.
    Inventors: Stephen J. Bierlmaier, Ralph C. Haltiwanger, Martin J. Jacobs
  • Multicomponent crystals comprising dasatinib and selected co-crystal formers
    Patent number: 9340536
    Abstract: Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (1R,2S,5R)-(?)-menthol.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: May 17, 2016
    Assignee: BASF SE
    Inventors: Tiziana Chiodo, Andreas Hafner, Tobias Hintermann, Beate Salvador, Martin Szelagiewicz, Fritz Blatter, Bernd Siebenhaar, Marcus Vossen
  • Pyrrolo[2,3-B]pyrazines as SYK inhibitors
    Patent number: 9334278
    Abstract: The present invention relates to the use of novel pyrrolo[2,3-b]]pyrazines wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: May 10, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Cornelius Hermann, Joshua Kennedy-Smith, Matthew C. Lucas, Fernando Padilla, Ryan Craig Schoenfeld, Peter Michael Wovkulich
  • N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidine-1(2H)-carboxamide derivatives
    Patent number: 9321734
    Abstract: This present disclosure is related to the field of to N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidine-1(2H)-carboxamide compounds and their derivatives and to the use of these compounds as fungicides. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/746,837 filed Dec. 28, 2012, which is expressly incorporated by reference herein. Background and Summary of the Invention Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: April 26, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Beth Lorsbach, W. John Owen, Lindsay Stelzer, Chenglin Yao
  • 5-alkynyl-pyrimidines
    Patent number: 9321771
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: April 26, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Siegfried Schneider, Dirk Kessler, Lars van der Veen, Tobias Wunberg
  • Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1
    Patent number: 9315489
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: April 19, 2016
    Assignee: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Malignant and non-malignant disease treatment with Ras antagonists
    Patent number: 9309203
    Abstract: The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: April 12, 2016
    Assignee: Pisces Therapeutics, LLC
    Inventors: James H. Wikel, Michael J. Brownstein
  • Polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyrdazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof
    Patent number: 9308205
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: April 12, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz-Hermann Bokel, Frank Stieber, Cristina Donini
  • Process for making hydroxylated cyclopentylpyrimidine compounds
    Patent number: 9309204
    Abstract: The invention provides new processes for making and purifying hydroxylated cyclopenta[d]pyrimidine compounds, which are useful for the treatment of diseases such as cancer as AKT protein kinase inhibitors, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: April 12, 2016
    Assignees: ARRAY BIOPHARMA INC., GENENTECH, INC.
    Inventors: Jonathan W. Lane, Travis Remarchuk, Sagar Shakya, Keith L. Spencer, Peter J. Stengel
  • Pyrimidinyl-diazospiro compounds
    Patent number: 9309254
    Abstract: The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: April 12, 2016
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Gerard M. P. Giblin, David T. MacPherson, David R. Witty, Steven J. Stanway
  • Substituted benzothienopyrimidines
    Patent number: 9296757
    Abstract: The present invention relates to substituted benzothienopyrimidine compounds of general formula I: in which R1a, R1b, R2a, R2b, and R2c are 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: Grant
    Filed: May 17, 2013
    Date of Patent: March 29, 2016
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Klar, Georg Kettschau, Dirk Kosemund, Florian Pühler, Knut Eis, Philip Lienau, Ulf Bömer, Detlev Sülzle, Lars Wortmann
  • Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
    Patent number: 9296727
    Abstract: The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: March 29, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell
  • Polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-hydrochloride salt and processes of manufacturing thereof
    Patent number: 9289427
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: March 22, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz-Hermann Bokel, Frank Stieber, Cristina Donini
  • Cyclobutyl benzimidazoles as PDE 10 inhibitors
    Patent number: 9284302
    Abstract: The present invention is directed to substituted cyclobutyl benzimidazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: March 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
  • Solid forms of an ion channel modulator
    Patent number: 9273038
    Abstract: Crystalline solid forms of the selective late sodium current inhibitor 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: March 1, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Anna Chiu, Olga V. Lapina, Petinka I. Vlahova
  • Substituted pyridone derivatives as PDE10 inhibitors
    Patent number: 9273033
    Abstract: The present invention is directed to substituted pyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: March 1, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
  • VEGFR3 inhibitors
    Patent number: 9266864
    Abstract: This invention relates to compounds of the formula (I): The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer, as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphangiogenesis.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: February 23, 2016
    Assignee: CANCER THERAPEUTICS CRC PTY LIMITED
    Inventors: Richard Charles Foitzik, Neil Choi, Benjamin Joseph Morrow, Catherine Fae Hemley, Gillian Elizabeth Lunniss, Michelle Ang Camerino, Danny Ganame, Paul Anthony Stupple, Romina Lessene, Wilhelmus Johannes Antonius Kersten, Andrew John Harvey, Ian Peter Holmes
  • Substituted benzylindazoles for use as Bub1 kinase inhibitors in the treatment of hyperproliferative diseases
    Patent number: 9265763
    Abstract: Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: February 23, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marion Hitchcock, Anne Mengel, Vera Pütter, Gerhard Siemeister, Antje Margret Wengner, Hans Briem, Knut Eis, Volker Schulze, Amaury Ernesto Fernandez-Montalvan, Stefan Prechtl, Simon Holton, Jörg Fanghänel, Philip Lienau, Cornelia Preusse, Mark Jean Gnoth
  • 2-hydroxyarylamide derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating cancer containing same as active ingredient
    Patent number: 9266872
    Abstract: The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.
    Type: Grant
    Filed: April 18, 2014
    Date of Patent: February 23, 2016
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Semi Kim, Ill Young Lee, Hye-Jin Min, Eun-Hee Nam, Pilho Kim, Chang Soo Yun, Dong Joon Ko