Ring Oxygen In The Additional Hetero Ring Patents (Class 514/254.1)
  • Patent number: 10828289
    Abstract: There are provided, inter alia, methods and compounds and method for inducing hair growth in a subject in need thereof.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: November 10, 2020
    Assignee: The Regents of the University of California
    Inventor: William Lowry
  • Patent number: 10479781
    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: March 4, 2016
    Date of Patent: November 19, 2019
    Assignee: Neuprozyme Therapeutics APS
    Inventors: Conni Lauritzen, John Pedersen
  • Patent number: 10364253
    Abstract: The invention relates to salinomycin derivatives such as compounds having the structure of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a therapeutically effective amount of compounds of formula (I), and the use of compounds of formula (I) for treating or inhibiting progression of cancer. The cancer is selected from the group consisting of breast cancer, pancreatic cancer, and prostate cancer.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: July 30, 2019
    Assignee: Channel Therapeutics, Inc.
    Inventors: Sireesh Appajosyula, Kandalam V. Ramanujachary, Subash C. Jonnalagadda
  • Patent number: 9814706
    Abstract: This invention relates to a new salt of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides the pharmaceutically acceptable hydrobromide salt, pharmaceutical compositions comprising this salt, and uses of this salt as a drug substance.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: November 14, 2017
    Assignee: TEVA PHARMACEUTICALS INTERNATIONAL GMBH
    Inventors: Anne Zimmermann, Brian Frøstrup
  • Patent number: 9649297
    Abstract: A method is described for treating attention deficit hyperactivity disorder (ADHD), by administering to the individual an anti-epileptic mood stabilizer at a dose which is sub-therapeutic for mood stabilization, optionally in combination with a psychostimulant. Also described is a method of improving reading comprehension and/or fluency in an individual suffering from learning difficulties which method comprises administering to the individual an anti-epileptic mood stabilizer.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: May 16, 2017
    Assignee: Gosforth Centre (Holdings) Pty Ltd.
    Inventor: Philip Bird
  • Publication number: 20150126494
    Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 30, 2013
    Publication date: May 7, 2015
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Janet R. Sparrow, Rando Allikmets
  • Publication number: 20150094520
    Abstract: A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
    Type: Application
    Filed: December 8, 2014
    Publication date: April 2, 2015
    Inventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Sanath K. MEEGALLA, M. Jonathan RUDOLPH, Mark J. WALL, Kenneth J. WILSON, Renee Louise DESJARLAIS, Carl M. MANTHEY, Christopher J. MOLLOY
  • Publication number: 20150087629
    Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Publication number: 20150051220
    Abstract: A compound of formula (I) for use in the treatment of a condition or disorder associated with nicotinamide adenine dinucleotide phosphate oxidase.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 19, 2015
    Applicant: GLUCOX BIOTECH AB
    Inventors: Mona Wilcke, Erik Walum, Per Wikstrom
  • Publication number: 20150025069
    Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Inventors: Timothy Scott Daynard, Geoffrey C. Winters, David W.C. Hunt
  • Patent number: 8937056
    Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: January 20, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
  • Patent number: 8933102
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: January 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson
  • Publication number: 20150011562
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R10 and X have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 8, 2015
    Inventors: Henry Yu, Thomas E. Richardson, Pandi Bharathi, Brian H. Heasley, Matthew G. Jenks, Robert J. Foglesong
  • Patent number: 8912196
    Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: December 16, 2014
    Assignee: ATIR Holding S.A.
    Inventors: Vladimir Kogan, Lev Tabachnik
  • Publication number: 20140364439
    Abstract: The present invention provides methods and devices related to markers (or biomarkers) associated with chronic lymphocytic leukemia (CLL). Examples of these markers include drivers of CLL progression. The invention contemplates, inter alia, detecting the clonal, including subclonal, profile of CLL in a subject and the presence (or absence) of subclonal driver mutations, and utilizing this information in predicting disease progression, need, timing and/or nature of treatment regimen, and likelihood and frequency of relapse.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Applicants: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Catherine J Wu, Gad Getz
  • Publication number: 20140343000
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 20, 2014
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Publication number: 20140296254
    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: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Publication number: 20140275112
    Abstract: Disclosed herein are methods and compositions comprising compounds capable of normalizing neuronal calcium dyshomeostasis. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, Pick's disease, chronic traumatic encepholopathy, traumatic brain injury, stroke, cerebellar ataxia, multiple sclerosis, Down syndrome, and aging-related CNS disorders.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Rosalind Franklin University of Medicine and Science
    Inventors: Grace E. Stutzmann, Russell Dahl
  • Publication number: 20140275010
    Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
  • Patent number: 8835419
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: September 16, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. MacMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20140235650
    Abstract: The invention relates to a compound of formula (I), where R1, R2, R7, m, n, and L1 are as defined in claim 1, and to the methods for preparing same, to the pharmaceutical compositions containing same, and to the uses thereof in the treatment of diseases associated with insulin resistance syndrome.
    Type: Application
    Filed: June 22, 2012
    Publication date: August 21, 2014
    Applicant: Metabolys
    Inventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier
  • Publication number: 20140194422
    Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.
    Type: Application
    Filed: June 12, 2012
    Publication date: July 10, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Thota Ganesh, Aiming Sun, Susane M. Smith, John David Lambeth
  • Publication number: 20140194349
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: AbbVie Inc.
    Inventors: David A. DeGoey, Charles A. Flentge, William J. Flosi, David J. Grampovnik, Dale J. Kempf, Larry L. Klein, Ming C. Yeung, John T. Randolph, Xiu C. Wang, Su Yu
  • Patent number: 8759352
    Abstract: The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholester
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: June 24, 2014
    Assignees: Merck Sharp & Dohme B.V., Pharmacopeia LLC.
    Inventors: Andrew John Cooke, David Jonathan Bennett, Andrew Stanley Edwards, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Koc-Kan Ho, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer
  • Publication number: 20140171439
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 19, 2014
    Applicant: Janssen Pharmaceutica, N.V.
    Inventors: Kristof VAN EMELEN, Marc Gustaaf Celine VERDONCK, Sven Franciscus Anna VAN BRANDT, Patrick Rene ANGIBAUD, Lieven MEERPOEL, Alexey Borisovich DYATKIN
  • Patent number: 8716294
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising tenilsetam or pharmaceutically acceptable salts thereof that are useful in modulating inflammation. In particular, the compounds or pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder involving inflammation, including, but not limited to, delayed type hypersensitivity and contact hypersensitivity.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: May 6, 2014
    Assignee: Melior Discovery, Inc.
    Inventors: Andrew Reaume, Heather Hain, Michael Saporito
  • Publication number: 20140107119
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: November 15, 2013
    Publication date: April 17, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
  • Patent number: 8691184
    Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: April 8, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
  • Publication number: 20140094455
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: August 19, 2013
    Publication date: April 3, 2014
    Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Publication number: 20140088077
    Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.
    Type: Application
    Filed: December 3, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
  • Publication number: 20140088095
    Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.
    Type: Application
    Filed: September 16, 2013
    Publication date: March 27, 2014
    Applicant: SK Biopharmaceuticals Co., Ltd.
    Inventors: Byong Sung KWAK, Hong Sik MOON, Han-Ju YI, Young Soon KANG, Dae Joong IM, Eun Hee CHAE, Sang Mi CHAE, Ki Ho LEE
  • Publication number: 20140088106
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 14, 2013
    Publication date: March 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
  • Patent number: 8674100
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are as set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. The compounds of formula I are useful for treating a variety of disorders including autoimmune diseases such as rheumatoid arthritis, multiple sclerosis and psoriasis.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: March 18, 2014
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJariais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Patent number: 8673904
    Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: March 18, 2014
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • Publication number: 20140073609
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
    Type: Application
    Filed: May 14, 2013
    Publication date: March 13, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. HERGENROTHER, Karson S. PUTT, Quinn P. PETERSON, Valerie FAKO
  • Patent number: 8669260
    Abstract: The application discloses ketoconazole derivatives that are antagonists of the human pregnane X receptor (PXR), methods of preparing the derivatives, uses of the derivatives with drug therapy, and methods of inhibiting tumor cell proliferation and multidrug resistance using inhibitors of PXR.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: March 11, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Sridhar Mani, Bhaskar C. Das
  • Publication number: 20140057889
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20140057890
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20140005181
    Abstract: The present disclosure relates to compounds and methods for treating a disease mediated by apelin.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 2, 2014
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Layton Smith, Anthony B. Pinkerton
  • Patent number: 8614211
    Abstract: Chemical entities that are arctigenin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 24, 2013
    Assignee: NeuPharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Patent number: 8609640
    Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: December 17, 2013
    Assignee: Eisai, Inc.
    Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang, Jiayi Wu
  • Publication number: 20130296295
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: March 15, 2013
    Publication date: November 7, 2013
    Inventor: ABBVIE INC.
  • Publication number: 20130190288
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130172315
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: July 4, 2013
    Applicant: ChemoCentryx, Inc.
    Inventor: ChemoCentryx, Inc.
  • Publication number: 20130158046
    Abstract: Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 20, 2013
    Applicant: Mersana Therapeutics, Inc
    Inventors: Laura C. Akullian, Russell C. Petter, John J. Kane, Charles E. Hammond, Mao Yin, Aleksandr Yurkovetskiy, Cheri A. Stevenson
  • Patent number: 8450317
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: May 28, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jennifer A. Kowalski, Daniel Richard Marshall, Anthony S. Prokopowicz, III, Sabine Schlyer, Robert Sibley, Ronald John Sorcek, Di Wu, Frank Wu, Erick Richard Roush Young
  • Patent number: 8431563
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: April 30, 2013
    Assignee: Amgen Inc.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • Publication number: 20130072497
    Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.
    Type: Application
    Filed: November 14, 2012
    Publication date: March 21, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Publication number: 20130023522
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: July 17, 2012
    Publication date: January 24, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Henry YU, Jiezhen LI, Thomas E. RICHARDSON, Pandi BHARATHI, Brian H. HEASLEY, Andreas GOUTOPOULOS
  • Patent number: 8343963
    Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: January 1, 2013
    Assignee: 4SC AG
    Inventor: Stefano Pegoraro