1,4 Diazines Patents (Class 514/252.1)
  • Patent number: 10745387
    Abstract: The present disclosure provides a novel solid state form of pladienolide pyridine compounds having Formula I, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: August 18, 2020
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Gregg F. Keaney, John Wang, Baudouin Gerard, Kenzo Arai, Xiang Liu, Guo Zhu Zheng, Kazunobu Kira, Parcharee Tivitmahaisoon, Sudeep Prajapati, Nicholas C. Gearhart, Yoshihiko Kotake, Satoshi Nagao, Regina Mikie Kanada Sonobe, Masayuki Miyano, Norio Murai, Silvia Buonamici, Lihua Yu, Eunice Sun Park, Betty Chan, Peter G. Smith, Michael P. Thomas, Ermira Pazolli, Kian Huat Lim, Atsushi Endo, Arani Chanda
  • Patent number: 10604511
    Abstract: This invention relates to compounds of formula I a process for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions having an association with the orexin sub-type 1 receptor. Ar, R1, R2 and R3 have meanings given in the description.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: March 31, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec
  • Patent number: 10583087
    Abstract: Disclosed is a pharmaceutical composition for oral administration, comprising 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid, which is a compound having pH-dependent solubility, or a pharmaceutically acceptable salt thereof, and a cellulose derivative. In the pharmaceutical composition for oral administration, the solubility and absorbability of the drug are improved.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: March 10, 2020
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Yumiko Suda, Toshiro Sakai, Ryo Kojima, Dal Oyama, Koji Nishimura, Kumi Naiki
  • Patent number: 10548845
    Abstract: Disclosed is a pharmaceutical composition for oral administration, comprising 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid, which is a compound having pH-dependent solubility, or a pharmaceutically acceptable salt thereof, and a cellulose derivative. In the pharmaceutical composition for oral administration, the solubility and absorbability of the drug are improved.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: February 4, 2020
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Yumiko Suda, Toshiro Sakai, Ryo Kojima, Dal Oyama, Koji Nishimura, Kumi Naiki
  • Patent number: 10258617
    Abstract: A dose regimes comprising the simultaneous administration of two pharmaceutical compositions, wherein the first pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof for once daily oral administration, and the second pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof which together with said first composition quickly achieves a steady-state plasma level of vortioxetine in said patient which steady-state plasma level is the same as the steady-state vortioxetine plasma level achieved by the administration to said patient of said first composition alone.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: April 16, 2019
    Assignee: H. Lundbeck A/S
    Inventors: Connie Sanchez Morillo, Karina Krøjer Søby, Benny Bang-Andersen
  • Patent number: 10188737
    Abstract: Provided is a pharmaceutical composition, which comprises 5-{[(3R)-1-acryloylpyrrolidin-3-yl]oxy}-6-ethyl-3-({4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-pyrazine-2-carboxamide (hereinafter referred to as “compound A”) or a pharmaceutically acceptable salt thereof, and is stabilized. The pharmaceutical composition comprises compound A or a pharmaceutically acceptable salt thereof, and a pharmaceutical additive having a difference in water activity value of 0.1 or more, and is stabilized.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: January 29, 2019
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Hiroaki Tasaki, Mitsuru Yoshida, Daisuke Tsunashima, Ryota Azuma
  • Patent number: 9914702
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: December 1, 2016
    Date of Patent: March 13, 2018
    Assignees: Bionomics Limited, Merck Patent GmbH
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Patent number: 9913839
    Abstract: A dose regimes comprising the simultaneous administration of two pharmaceutical compositions, wherein the first pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof for once daily oral administration, and the second pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof which together with said first composition quickly achieves a steady-state plasma level of vortioxetine in said patient which steady-state plasma level is the same as the steady-state vortioxetine plasma level achieved by the administration to said patient of said first composition alone.
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: March 13, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Connie Sanchez Morillo, Karina Krøjer Søby, Benny Bang-Andersen
  • Patent number: 9889135
    Abstract: The present invention relates to the use of one or more biomarkers to evaluate the likelihood that a CDK4 inhibitor would produce an anti-cancer effect in a subject. It is based, at least in part, on the discovery that cancer treatment with a CDK4 inhibitor is more effective where treated cancer cells undergo cellular senescence rather than a transient cell cycle arrest, where cellular senescence is associated with decreased MDM2 protein level. Accordingly, in non-limiting embodiments, the present invention provides for methods, compositions, and kits for a companion diagnostic for CDK4 inhibitors, and in particular, to the use of MDM2 expression as a biomarker for the likelihood that a cancer can be successfully treated by CDK4 inhibition.
    Type: Grant
    Filed: October 15, 2015
    Date of Patent: February 13, 2018
    Assignee: Memorial Sloan-Kettering Cancer Center
    Inventors: Andrew Koff, Aimee Crago, David Liu, Marta Kovatcheva, Samuel Singer, Gary K. Schwartz, Mark A. Dickson, Mary Elizabeth Klein
  • Patent number: 9890177
    Abstract: Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: February 13, 2018
    Assignee: ANGUS CHEMICAL COMPANY
    Inventors: Daniel M. Trauth, George D. Green, Raymond J. Swedo, Richard L. James, Ian A. Tomlinson
  • Patent number: 9872861
    Abstract: This invention pertains to methods of treating systemic lupus erythematosus and Sjogren's Syndrome with compounds that selectively inhibit the activity of Bcl-2 anti-apoptotic proteins. Specifically, the current invention is directed to treatment with compounds that selectively inhibit the activity of Bcl-2 proteins, with a lesser affinity for inhibiting the activity of other BCL-2 family proteins, including Bcl-XL.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: January 23, 2018
    Assignee: AbbVie Inc.
    Inventors: Steven Elmore, Andrew Souers, Lichun Wang, Tariq Ghayur, Stuart J. Perper
  • Patent number: 9856228
    Abstract: The invention relates to compounds of Formula (I) and their use as selective dipeptidyl peptidase I inhibitors, as well as pharmaceutical compositions comprising said compounds, and methods of treatment involving said compounds.
    Type: Grant
    Filed: September 8, 2014
    Date of Patent: January 2, 2018
    Assignee: PROZYMEX A/S
    Inventors: Conni Lauritzen, John Pedersen
  • Patent number: 9820984
    Abstract: A dose regimes comprising the simultaneous administration of two pharmaceutical compositions, wherein the first pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof for once daily oral administration, and the second pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof which together with said first composition quickly achieves a steady-state plasma level of vortioxetine in said patient which steady-state plasma level is the same as the steady-state vortioxetine plasma level achieved by the administration to said patient of said first composition alone.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: November 21, 2017
    Assignee: H. Lundbeck A/S
    Inventors: Connie Sanchez Morillo, Karina Krøjer Søby, Benny Bang-Andersen
  • Patent number: 9815772
    Abstract: The present disclosure relates to processes for the preparation of 2-amino-1,3-propane diol compounds and their hydrochloride salts. Particularly, the present disclosure relates to processes for synthesizing 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol and its hydrochloride salt 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride respectively. The said process is safe, commercially feasible for large-scale synthesis and has improved efficacy along with many other advantages. The present disclosure also relates to the novel polymorphs of 2-amino-1,3-propane diol compound and its hydrochloride salt, where in 2-amino-1,3-propane diol compound is 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol, and its hydrochloride salt is 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride.
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: November 14, 2017
    Assignee: Biocon Limited
    Inventors: Kothakonda Kiran Kumar, Chandrashekar Aswathanarayanappa, Dharshan Jakkali Chandregowda, Chandrasekhar Duvva, Venkata Srinivas Pullela
  • Patent number: 9770025
    Abstract: The present invention relates to novel fungicidal compositions for the treatment of phytopathogenic diseases of useful plants, especially phytopathogenic fungi, and to a method of controlling such phytopathogenic diseases on useful plants. In particular compositions suitable for control of diseases caused by phytopathogens comprise a mixture of a compound of formula (I), with a compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants using such compositions.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: September 26, 2017
    Assignee: Syngenta Participations AG
    Inventors: Gina Mercia Swart, Michael Oostendorp
  • Patent number: 9757374
    Abstract: The present invention discloses compositions of liquid and gel formulation containing aripiprazole in the form of a patch for transdermal delivery.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: September 12, 2017
    Assignee: Aequus Pharmaceuticals Inc.
    Inventors: Fotios M. Plakogiannis, Muhammed Anwar Hossain
  • Patent number: 9580412
    Abstract: Methods for preparing disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds that correspond to general formula (I) are described. Also described are pharmaceutical compositions that include the compounds, and methods of using the compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: February 28, 2017
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteau, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Patent number: 9493451
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: November 15, 2016
    Assignees: Bionomics Limited, Merck Patent GmbH
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Patent number: 9388149
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: July 12, 2016
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marléne Schuppli-Nollet
  • Patent number: 9314446
    Abstract: The present invention relates to a formulation made from a chitosan, a gelatin, and a phosphate salt can provide a sustained release/maintenance of a therapeutic agent, wherein the phosphate salt is selected from the group consisting of disodium phosphate and ammonium hydrogen phosphate.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: April 19, 2016
    Inventors: Shih-Hwa Chiou, Catherine Jui-Ling Liu, Yung-Hsin Cheng
  • Patent number: 9296720
    Abstract: This invention relates to new carboxamide-substituted heteroaryl-pyrazoles, method for their production, their use for the treatment and/or prophylaxis of diseases, as well as their use for the production of pharmaceutical agents for the treatment and/or prophylaxis of diseases, in particular retroviral diseases, in humans and/or animals.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: March 29, 2016
    Assignee: AICURIS GMBH & CO. KG
    Inventors: Steffen Wildum, Burkhard Klenke, Astrid Wendt
  • Patent number: 9173881
    Abstract: The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination of at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: November 3, 2015
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventor: Martine Clozel
  • Patent number: 9149459
    Abstract: The use of an S1P receptor modulator of the formula (Ia) or (Ib) wherein the meaning of the different residues is that indicated in claim 14, in the preparation of a medicament for preventing, inhibiting or treating an inflammatory condition selected from polymyositis, dermatomyositis and nerve-muscle diseases e.g. muscular dystrophies and inclusion body myositis.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: October 6, 2015
    Assignee: Novartis AG
    Inventors: Syed Sohail Ahmed, Marco Londei, Timothy Wright, Peter Gergely
  • Patent number: 9079900
    Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: July 14, 2015
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Gingsee Lee, Garrick Packard, Jingjing Zhao, Patrick Anthony Jokiel, Deborah Mortensen, Jennifer Riggs, Juan Antonio Gamboa, Marie Georges Beauchamps, Matthew Michael Kreilein, Mohit Atul Kothare, Sophie Perrin-Ninkovic, Philip Pye, William Wei-Hwa Leong, Jan Elsner, Anusuya Choudhury
  • Patent number: 9056813
    Abstract: The present invention provides a process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA.
    Type: Grant
    Filed: January 17, 2013
    Date of Patent: June 16, 2015
    Assignee: Glenmark Generics Limited
    Inventors: Milind Gharpure, Krishna Narawade, Prem Chand, Shekhar Bhaskar Bhirud
  • Publication number: 20150141427
    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: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: 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
  • Patent number: 9028876
    Abstract: Rate-controlled particles, comprising compounds of the formula as a solid dispersion.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: May 12, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Thomas Hantke, Bettina Rehbock, Jörg Rosenberg, Jörg Breitenbach
  • Publication number: 20150126437
    Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.
    Type: Application
    Filed: October 17, 2012
    Publication date: May 7, 2015
    Applicant: The Regents of the University of California
    Inventors: Anandasankar Ray, Sean Michael Boyle
  • Patent number: 9012449
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: April 21, 2015
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Patent number: 9006238
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: April 14, 2015
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Patent number: 9006454
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 14, 2015
    Assignee: Merck Serono S.A.
    Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
  • Publication number: 20150098992
    Abstract: Provided is a composite formulation comprising multi-unit spheroidal tablets (MUSTs) encapsulated in a hard capsule and a method for preparing same. The inventive hard capsule composite formulation can effectively charge the MUSTs in the limited space of the capsule, which allows charging a high dose of different pharmaceutically active ingredients in a capsule with a relatively small size, to thereby increase the productivity and render it readily administered to patients. Also, the capsule has a good dissolution rate because the pharmaceutically active ingredients contained in the capsule are separated from one another; therefore, the dissolution rates of the ingredients are less affected by one another. It may also be possible to maximize the therapeutic effects of the pharmaceutically active ingredients since the composite formulation has good stability.
    Type: Application
    Filed: April 12, 2013
    Publication date: April 9, 2015
    Applicant: HANMI PHARM. CO., LTD
    Inventors: Kyeong Soo Kim, Dong Ho Kim, Taek Kwan Kwon, Yong Il Kim, Jae Hyun Park, Jong Soo Woo
  • Patent number: 8987304
    Abstract: The present invention provides antituberculous therapeutic drugs with a higher potency. The present invention provides also antituberculous therapeutic drugs containing oxazole compounds represented by (I) general formula (1): [wherein R1 represents a hydrogen atom or C1-6 alkyl group, n represents an integer of 0-6, and R2 represents general formula (A) or the like, wherein R3 represents a phenoxy group (at least one group selected from the group consisting of a halogen atom, an optionally halogen-substituted C1-6 alkyl group and an optionally halogen-substituted C1-6 alkoxy group may be substituted on the phenyl ring) or the like], optically active forms thereof or salts thereof, and drugs (II) such as primary antituberculous drugs.
    Type: Grant
    Filed: October 4, 2006
    Date of Patent: March 24, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Yoshihiko Shimokawa
  • Publication number: 20150080408
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 19, 2015
    Applicant: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Patent number: 8969350
    Abstract: The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclopropyl-3-fluoro-4-methyl-5[3-[[1-[2-[2-(methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-benzamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a ?2 adrenoceptor agonist; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DPI antagonist; an Histone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a MABA compound; an MPO inhibitor; a muscarinic antagonist; a PDE4 inhibitor; a PPAR? agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: March 3, 2015
    Assignee: Astrazeneca AB
    Inventors: Anne Elizabeth Cooper, Timothy Jon Luker, Jerzy Andrzej Schmidt
  • Patent number: 8969351
    Abstract: A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively.
    Type: Grant
    Filed: November 17, 2011
    Date of Patent: March 3, 2015
    Assignee: Novartis AG
    Inventors: Joerg Berghausen, Haixia Ren
  • Patent number: 8969347
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: March 3, 2015
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Publication number: 20150045312
    Abstract: Methods of treating autism, autistic spectrum disorders or Fragile X syndrome comprised of administering molecules that engage the cystine-glutamate exchange (System xc?) and/or elevate the extracellular levels of glutathione in the CNS. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.
    Type: Application
    Filed: August 11, 2014
    Publication date: February 12, 2015
    Inventors: Michael Neary, Chad Beyer
  • Patent number: 8952013
    Abstract: A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.
    Type: Grant
    Filed: December 28, 2011
    Date of Patent: February 10, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Janusz W. Kostanski, Takakuni Matsuda, Manoj Nerurkar, Vijay H. Naringrekar
  • Patent number: 8946413
    Abstract: There is provided a compound of Formula I(a) or I(b): or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 3, 2015
    Assignee: Pfizer Inc.
    Inventors: Robert O. Hughes, Rajesh V. Devraj, Donald J. Rogier, John I. Trujillo, Steve R. Turner, Wei Huang
  • Publication number: 20150004207
    Abstract: An interventional medical device and manufacturing method thereof, the interventional medical device comprising a stent body (1); the stent body (1) is provided with a drug releasing structure on the surface, the drug in the drug releasing structure being a drug for inhibiting adventitial fibroblast proliferation. When the interventional medical device is implanted into a human body, the drug for inhibiting the adventitial fibroblast proliferation can be slowly released into vessel wall cells in contact with the stent body (1), thus inhibiting the proliferation of the adventitial fibroblasts, promoting vascular compensatory expansion, and reducing the incidence rate of instent restenosis.
    Type: Application
    Filed: January 17, 2012
    Publication date: January 1, 2015
    Applicant: SHANGHAI MICROPORT MEDICAL (GROUP) CO., LTD.
    Inventors: Xu Cai, Dadong Zhang, Yan Hu, Peng Huang, Junfei Li, Chengyun Yue, Zhirong Tang, Qiyi Luo
  • Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Publication number: 20140350030
    Abstract: The present invention provides compounds of formula (I): where R1, R2, X, Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.
    Type: Application
    Filed: September 17, 2012
    Publication date: November 27, 2014
    Inventors: Dario Doller, Guiying Li
  • Publication number: 20140336198
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 13, 2014
    Applicants: MERCK PATENT GMBH, BIONOMICS LIMITED
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Patent number: 8883786
    Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch
  • Publication number: 20140329837
    Abstract: Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Application
    Filed: July 22, 2014
    Publication date: November 6, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Gerard BOTTON, Eric VALEUR, Christine CHARON, Micheline KERGOAT, Samer ELBAWAB
  • Publication number: 20140329824
    Abstract: The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination of at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof
    Type: Application
    Filed: July 18, 2014
    Publication date: November 6, 2014
    Inventor: MARTINE CLOZEL
  • Publication number: 20140315898
    Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
    Type: Application
    Filed: December 12, 2012
    Publication date: October 23, 2014
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo
  • Publication number: 20140315913
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Patent number: RE46364
    Abstract: [Object] The main object of the present invention is to provide a fibrosis inhibitor. [Solving Means] The present invention relates to a fibrosis inhibitor containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient; In the formula (1), R1 and R2 are the same or different and each represents an optionally substituted aryl; R3 and R4 are the same or different and each represents hydrogen atom or alkyl; R5 represents hydrogen atom, alkyl or halogen atom; Y represents N or N?O; A represents NR6, and R6 represents hydrogen atom, alkyl, etc.; D represents alkylene or alkenylene which is optionally substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, etc.; and Q represents carboxy, alkoxycarbonyl, etc.
    Type: Grant
    Filed: May 16, 2016
    Date of Patent: April 11, 2017
    Assignee: NIPPON SHINYAKU CO., LTD.
    Inventors: Koji Murakami, Takuya Toramoto