Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 514/313)
  • Patent number: 10342868
    Abstract: Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
    Type: Grant
    Filed: January 17, 2017
    Date of Patent: July 9, 2019
    Assignee: Augusta University Research Institute, Inc.
    Inventors: Samir N. Khleif, Mikayel Mkrtichyan
  • Patent number: 10322111
    Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
    Type: Grant
    Filed: February 8, 2016
    Date of Patent: June 18, 2019
    Assignee: GENZYME CORPORATION
    Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
  • Patent number: 10308923
    Abstract: The present invention relates to a medium composition for production of botulinum toxin and, more particularly, to a medium composition for culture of Clostridium sp. capable of producing botulinum toxin. The medium composition of the present invention comprises a porcine peptone and at least one plant-derived peptone selected from the group consisting of a garden pea hydrolysate, a cotton seed hydrolysate and a wheat gluten hydrolysate. When the medium according to the present invention, which contains plant-derived peptones, porcine peptones and minerals, is used for culture of Clostridium botulinum, the growth rate of the bacterium in the medium is higher than that in each of the medium that is in current use and the medium comprising plant-derived peptones alone. In addition, when the medium of the present invention is used, a high concentration of botulinum toxin can be produced by culturing the bacterium in a safe manner.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: June 4, 2019
    Assignee: DAEWOONG CO., LTD.
    Inventors: Kyoung-Yun Kim, Hye-Young Sul, Kyoung-Min Min
  • Patent number: 10292978
    Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.
    Type: Grant
    Filed: January 17, 2017
    Date of Patent: May 21, 2019
    Assignee: Augusta University Research Institute, Inc.
    Inventors: Samir N. Khleif, Mikayel Mkrtichyan, Iryna Lebedyeva
  • Patent number: 10246444
    Abstract: Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.
    Type: Grant
    Filed: January 17, 2018
    Date of Patent: April 2, 2019
    Assignee: SABILA BIOSCIENCES LLC
    Inventor: Tarek Suhayl Mansour
  • Patent number: 10227343
    Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: March 12, 2019
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Colleen M. Niswender, Corey R. Hopkins, Joanne Bronson, Yong-Jin Wu, Kyle Emmitte, Joe Panarese, Darren W. Engers, Julie Engers
  • Patent number: 10219516
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: August 17, 2017
    Date of Patent: March 5, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: Ronald J. Heemstra, Ronald Ross, Jr., Kyle A. DeKorver, Kaitlyn Gray, Daniel I. Knueppel, Peter Vednor, Timothy P. Martin, Joseph D. Eckelbarger, John F. Daeuble, Sr., Ricky Hunter, David A. Demeter, Tony K. Trullinger, Erich W. Baum, Zoltan L. Benko, Nakyen Choy, Gary D. Crouse, Fangzheng Li, Jeffrey Nissen, Monica B. Olson, Michelle Riener, Thomas C. Sparks, Frank J. Wessels, Maurice C. Yap
  • Patent number: 10159678
    Abstract: Methods and compositions are described for reducing airway reactivity and the susceptibility to asthmatic bronchoconstriction that involve increasing sphingolipid content in airways and lungs of a mammalian subject.
    Type: Grant
    Filed: May 16, 2013
    Date of Patent: December 25, 2018
    Assignees: Cornell University, Columbia University
    Inventors: Stefan Worgall, Tilla S. Worgall
  • Patent number: 10112905
    Abstract: Aminoquinoline compounds useful for treating chronic pain, addiction, and other conditions are provided. The aminoquinoline compound is represented by Formula (I) which is defined in the specification.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: October 30, 2018
    Assignee: LOHOCLA RESEARCH CORPORATION
    Inventor: Boris Tabakoff
  • Patent number: 10052317
    Abstract: The invention provides a neurokinin 3 receptor (NKR3) antagonist for use in the treatment, prevention or amelioration of hot flushes in a human subject, for example a menopausal woman or a patient undergoing cancer therapy which affects secretion of sex steroids. The invention also provides a NKR3 antagonist together with a further active agent, and a composition and a kit comprising a NKR3 antagonist and a further active agent. The invention further provides a NKR3 agonist or exogenous NKB for the induction of hot flushes in a human subject.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: August 21, 2018
    Assignee: Imperial Innovations Limited
    Inventors: Waljit Dhillo, Channa Jayasena
  • Patent number: 10005721
    Abstract: The present invention provides a compound of the Formula I: wherein A is: and W, Y, X, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, for use as an inhibitor of the EP4 receptor.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: June 26, 2018
    Assignee: Eli Lilly and Company
    Inventors: Maria Jesus Blanco-Pillado, Peter Rudolph Manninen, Matthew Allen Schiffler, Tatiana Natali Vetman, Alan M Warshawsky, Jeremy Schulenburg York
  • Patent number: 9814701
    Abstract: The present invention is directed to topical ophthalmic compositions of a lipophilic compound and an oligomeric or polymeric carrier wherein the compositions are useful in the treatment and prevention of macular degeneration. The invention also includes methods of treating macular degeneration by using a topical ophthalmic composition of a lipophilic compound and an oligomeric or polymeric carrier.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: November 14, 2017
    Assignee: Aldeyra Therapeutics, Inc.
    Inventors: Thomas A. Jordan, John Clifford Chabala, Gerald D. Cagle
  • Patent number: 9809599
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
    Type: Grant
    Filed: November 11, 2015
    Date of Patent: November 7, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Simona M. Ceccarelli, Aurelia Conte, Holger Kuehne, Bernd Kuhn, Werner Neidhart, Ulrike Obst Sander, Markus Rudolph
  • Patent number: 9801870
    Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:
    Type: Grant
    Filed: June 28, 2016
    Date of Patent: October 31, 2017
    Assignee: AROG PHARMACEUTICALS, INC.
    Inventor: Vinay K. Jain
  • Patent number: 9783500
    Abstract: Various 2-aminoquinoline compounds as can be used, in vivo or in vitro, for selective inhibition of neuronal nitric oxide synthase.
    Type: Grant
    Filed: August 31, 2016
    Date of Patent: October 10, 2017
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Maris A. Cinelli, Anthony V. Pensa
  • Patent number: 9781935
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: October 10, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Ronald J. Heemstra, Ronald Ross, Jr., Kyle DeKorver, Kaitlyn Gray, Daniel I. Knueppel, Peter Vednor, Timothy P. Martin, Joseph D. Eckelbarger, John F. Daeuble, Sr., Ricky Hunter, David A. Demeter, Tony K. Trullinger, Erich Baum, Zoltan L. Benko, Nakyen Choy, Gary Crouse, Fangzheng Li, Jeff Nissen, Monica B. Olson, Michelle Riener, Thomas C. Sparks, Frank J. Wessels, Maurice C. Yap
  • Patent number: 9770448
    Abstract: Compositions and methods for the treatment of Bowen's disease, an orphan disease, are described. In addition, compositions and methods for the treatment of recurrent respiratory papillomatosis (RRP), an orphan disease, are described. Compositions and methods for the treatment of stage 1 melanoma are also described. The compositions comprise one or more active ingredients selected from the group consisting of: chloroquine, amodiaquine, and an antibiotic such as metronidazole. The methods comprise administering a therapeutically effective amount of such compositions to a subject in need thereof.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: September 26, 2017
    Inventors: Justice E. Obi, James K. Bashkin
  • Patent number: 9687481
    Abstract: The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: June 27, 2017
    Assignee: ALDEYRA THERAPEUTICS, INC.
    Inventors: Todd Brady, Scott Young, William A. Kinney, Kenneth J. Mandell
  • Patent number: 9475773
    Abstract: A method for treating polycystic ovarian syndrome and related conditions with a compound (I): or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 14, 2014
    Date of Patent: October 25, 2016
    Assignee: ASTRAZENECA AB
    Inventors: Peter Stewart Gilmour, Tony Ho, Rahul Kakkar, Lorraine Webber
  • Patent number: 9393240
    Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:
    Type: Grant
    Filed: May 4, 2015
    Date of Patent: July 19, 2016
    Assignee: AROG PHARMACEUTICALS, INC.
    Inventor: Vinay K. Jain
  • Patent number: 9376393
    Abstract: A new medical therapy, and more particularly certain quinoline compounds which are anti-angiogenic integrin aplha5beta1 inhibitors, for use in the treatment of fibrosis, or a fibrosis-related disease, such as a fibrotic disease affecting the lung, liver, kidney, skin, epidermis, endodermis, muscle, tendon, cartilage, heart, stomach, large intestine, small intestine, colon, uterus, nervous system, testis, adrenal gland, artery, vein, biliary tract, or eye.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: June 28, 2016
    Assignee: Clanotech AB
    Inventor: Yihai Cao
  • Patent number: 9364469
    Abstract: The present invention discloses a method of treating gefitinib-resistant non-small-cell lung cancer, comprising administering an effective amount of D561-0775. A pharmaceutical composition comprising D561-0775 admixed with a pharmaceutical carrier for treating Gefitinib-resistant non-small-cell lung cancer is also disclosed therein.
    Type: Grant
    Filed: October 29, 2015
    Date of Patent: June 14, 2016
    Assignee: Macau University of Science and Technology
    Inventors: Lai-Han Leung, Xiao-Jun Yao, Kam Wai Wong, Liang Liu, Xi Chen
  • Patent number: 9309307
    Abstract: An advantage of some aspects of the invention is to provide an antibody against an amyloid precursor protein signal peptide. The invention provides an amyloid precursor protein signal peptide.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: April 12, 2016
    Assignees: SEIKO EPSON CORPORATION, TOAGOSEI CO., LTD.
    Inventors: Hitoshi Fukushima, Masato Hanamura, Mikio Niwa, Masaji Okamoto, Tomoko Naoe, Tetsuhiko Yoshida
  • Patent number: 9278089
    Abstract: A method of treating an Hepatitis C Virus infection in a patient, comprising providing a therapeutically effective amount, to a patient in need thereof, of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: G1 is a group of the formula or where n is 0, 1, 2, 3, or 4 and Het is a 5- or 6-membered heteroaryl group containing 1 to 4 heteroatoms independently chosen from N, O, and S, which Het is optionally substituted.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: March 8, 2016
    Assignee: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: David Waugh, Christopher Self, Guangtao Zhang, Yves Pommier, Robert H. Shoemaker, Michael Currens, John Cardellina, Andrew Jobson, George Lountos, Dominic Scudiero
  • Patent number: 9260384
    Abstract: A compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, is provided. Also, a composition containing a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents, is provided. Further, use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof for anti-apoptosis is provided, preventing or treating a disease or disorder associated with apoptosis; especially for protecting cardiomyocyte, preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: February 16, 2016
    Assignee: Chinese PLA General Hospital
    Inventors: Kunlun He, Song Li, Wu Zhong, Juan Liu, Lili Wang, Xin Li, Guoliang Hu, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Ruijun Li, Chunlei Liu, Jie Bai
  • Patent number: 9249103
    Abstract: Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.
    Type: Grant
    Filed: January 14, 2013
    Date of Patent: February 2, 2016
    Assignees: Oregon Health & Science University, The United States of America as Represented by the Department of Veterans Affairs
    Inventors: Michael K. Riscoe, Rolf W. Winter, Sovitj Pou, David J. Hinrichs, Jane Xu Kelly, Yuexin Li, Aaron Nilsen
  • Patent number: 9212144
    Abstract: Various 2-aminoquinoline compounds as can be used, in vivo or in vitro, for selective inhibition of neuronal nitric oxide synthase.
    Type: Grant
    Filed: January 12, 2015
    Date of Patent: December 15, 2015
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Maris A. Cinelli
  • Patent number: 9199938
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
    Type: Grant
    Filed: November 1, 2012
    Date of Patent: December 1, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Simona M. Ceccarelli, Aurelia Conte, Holger Kuehne, Bernd Kuhn, Werner Neidhart, Ulrike Obst Sander, Markus Rudolph
  • Patent number: 9199967
    Abstract: The present application relates to cycloalkylpyridin-2-amines derivates of formula (1) or stereoisomers thereof or pharmaceutically acceptable salts thereof. The present application also relates to the process for the preparation of compounds of formula (I). The present application further describes the compounds of formula (1) as cholesteryl ester-transfer protein (CETP) inhibitors. The present application further relates to pharmaceutical compositions comprising compounds of formula (1) or stereoisomers thereof or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 17, 2012
    Date of Patent: December 1, 2015
    Assignee: Dr. Reddy's Laboratories Ltd.
    Inventors: Anima Boruah, Shanavas Alikunju
  • Patent number: 9173850
    Abstract: Provided herein are 4-methylpyrazole (4-MP) formulations, stable under storage conditions of up to about 55° C.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: November 3, 2015
    Assignee: RAPTOR PHARMACEUTICALS INC.
    Inventors: Thomas E. Daley, Kathy Powell, Olga Jarzebinski
  • Patent number: 9126952
    Abstract: The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in Claim 1, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: September 8, 2015
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Thomas Fuchss, Frank Zenke
  • Patent number: 9128079
    Abstract: Provided herein are cell lines and assays that can be utilized to identify taste receptor modulators.
    Type: Grant
    Filed: August 8, 2012
    Date of Patent: September 8, 2015
    Assignees: The Coca-Cola Company, The University of North Carolina
    Inventors: Harish Radhakrishna, Michael D. Brown, David Peter Siderovski, Adam Kimple, Staci Padove Cohen
  • Patent number: 9101624
    Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: August 11, 2015
    Assignee: AROG PHARMACEUTICALS, INC.
    Inventor: Vinay K. Jain
  • Patent number: 9066954
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: June 30, 2015
    Assignee: Amgen Inc.
    Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia W. Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie K. Springer, Markian Stec, Ning Xi, Kevin Yang
  • Patent number: 9056105
    Abstract: Described herein are compounds, compositions, and methods useful for treating bone diseases or defects. Also described herein are compounds, compositions and methods for treating bone diseases or defects by inhibiting phosphatase complexes.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: June 16, 2015
    Assignee: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Hiroki Yokota, Ping Zhang
  • Patent number: 9045423
    Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: June 2, 2015
    Assignee: KOWA COMPANY, LTD.
    Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Patent number: 9040560
    Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: May 26, 2015
    Assignee: Merck Patent GmbH
    Inventors: Amanda E. Sutton, Thomas E. Richardson, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Yufang Xiao, Andreas Goutopoulos, Ruoxi Lan, David Perrey, Harold George Vandeveer, Lesley Liu-Bujalski, Frank Stieber, Brian L. Hodous, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
  • Publication number: 20150133441
    Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
    Type: Application
    Filed: June 6, 2014
    Publication date: May 14, 2015
    Inventor: Gerard M. Housey
  • Publication number: 20150133436
    Abstract: The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 14, 2015
    Inventors: Chun-Wa CHUNG, Edwige NICODEME
  • Patent number: 9029395
    Abstract: Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: May 12, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Robert J. Watson
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Patent number: 9029396
    Abstract: The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: May 12, 2015
    Assignee: Novartis AG
    Inventors: Nigel Graham Cooke, Rita Ramos, Karen Kammertoens, Maurice Van Eis
  • Publication number: 20150126550
    Abstract: Pharmaceutical uses of 6-amino quinazoline or 3-cyano quinoline derivatives are disclosed. Specifically, the 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (I), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, are protein kinase inhibitors, in which each substitutent group of general formula (I) is as defined in the specification.
    Type: Application
    Filed: December 1, 2014
    Publication date: May 7, 2015
    Inventors: Xin LI, Bin WANG
  • Publication number: 20150119421
    Abstract: The present invention includes a method of inhibiting or reducing deregulated FLT3 tyrosine kinase activity or FLT3 tyrosine kinase expression in a subject with a proliferative disease by administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound (CP-673,451) of Formula I: or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: July 30, 2014
    Publication date: April 30, 2015
    Inventor: Vinay K. Jain
  • Publication number: 20150105404
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Publication number: 20150105366
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
  • Publication number: 20150094334
    Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 2, 2015
    Applicant: PRANA BIOTECHNOLOGY LIMITED
    Inventors: Kevin Jeffrey BARNHAM, Elisabeth Colette Louise GAUTIER, Gaik Beng KOK, Guy KRIPPNER
  • Publication number: 20150094310
    Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventor: Florian Holsboer