Plural Diazine Rings Patents (Class 544/357)
  • Publication number: 20140336190
    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 R1a, R1b, R2, R2b, R3, R4a, R4b, and R5 are described herein.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Patent number: 8883789
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Annekatrin Heimann, Georg Dahmann, Marc Grundl, Stephan Georg Mueller, Bernd Wellenzohn
  • Publication number: 20140323463
    Abstract: [Problem] A compound which is useful as an inhibitor on EGFR T790M mutation kinase activity is provided. [Means for Solution] The present inventors have investigated a compound having an inhibitory action on an EGFR T790M mutation kinase, and have found that a pyrazinecarboxamide compound has an inhibitory action on an EGFR T790M mutation kinase, thereby completing the present invention.
    Type: Application
    Filed: January 15, 2013
    Publication date: October 30, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Takahiro Matsuya, Yutaka Kondoh, Itsuro Shimada, Shigetoshi Kikuchi, Maiko Iida, Kenichi Onda, Hiroki Fukudome, Yukihiro Takemoto, Nobuaki Shindou, Hideki Sakagami, Hisao Hamaguchi
  • Publication number: 20140323467
    Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Application
    Filed: May 23, 2014
    Publication date: October 30, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
  • Publication number: 20140323484
    Abstract: The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer. The compounds have the general formula (1): and salts, N-oxides and tautomers thereof, wherein m is 2, 3 or 4; n is 0 or 1; Q1 is selected from a bond; C(?O); S(O); SO2; and an alkylene chain of 1 to 4 carbon atoms in length between the moiety R4 and the nitrogen atom.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 30, 2014
    Inventors: Robert George Boyle, Richard Justin Boyce
  • Publication number: 20140323458
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Publication number: 20140315914
    Abstract: The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.
    Type: Application
    Filed: April 14, 2014
    Publication date: October 23, 2014
    Inventors: Astrid Netz, Thorsten Oost, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
  • Publication number: 20140315893
    Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
    Type: Application
    Filed: November 22, 2012
    Publication date: October 23, 2014
    Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
  • Patent number: 8865720
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, 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: Grant
    Filed: October 14, 2013
    Date of Patent: October 21, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviane Van Heusden
  • Publication number: 20140309211
    Abstract: Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.
    Type: Application
    Filed: May 29, 2014
    Publication date: October 16, 2014
    Applicant: ARRIEN PHARMACEUTICALS LLC
    Inventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
  • Publication number: 20140308317
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 9, 2013
    Publication date: October 16, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventors: Xiaodong Fan, Yongjiang Xu, Dahui Liu, Michael J. Costanzo
  • Publication number: 20140309193
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 16, 2014
    Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
  • Publication number: 20140309192
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complication(s) resulting from elevated blood pressure and/or reduced tissue perfusion.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: Thuy-Anh Tran, Anthony C. Blackburn, Bryan A. Kramer, Maiko Nagura, Carleton R. Sage, Young-Jun Shin, Ning Zou
  • Publication number: 20140309209
    Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: November 23, 2012
    Publication date: October 16, 2014
    Inventors: Yonghong Song, Qing Xu, Zhaozhong J. Jia, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Publication number: 20140299851
    Abstract: An organic electroluminescence element that uses a compound expressed by the following general formula has low inter-molecular interaction and high orientation during vapor deposition, and by using compounds that are resistant to aggregation, luminous efficiency is high, and there is little change in chromaticity accompanying drive deterioration (either V1 or W1 and either V2 or W2 form rings, the rings formed by V1 and V2 are six-membered rings, and the rings formed by W1 and W2 are five-membered rings; A2 to A4 and A6 to A8 represent CRZ or N, and RZ represents a hydrogen atom or a substituent; and R2, R3, R7, and R8 represent a hydrogen atom, an alkyl group, an aryl group, a heteroaryl group, a fluorine atom, a hydrogen atom [sic], or a deuterium atom.).
    Type: Application
    Filed: April 11, 2012
    Publication date: October 9, 2014
    Applicant: UDC Ireland Limited
    Inventors: Koji Takaku, Tetsu Kitamura, Toru Watanabe, Yasunori Yonekuta
  • Publication number: 20140303176
    Abstract: The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 9, 2014
    Inventors: Andreas HAUPT, Jürgen DINGES, Liliane UNGER, Karsten WICKE, Robert VAN WATERSCHOOT, Karla DRESCHER, Ana RELO
  • Publication number: 20140288086
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Applicants: PFIZER INC., AGOURON PHARMACEUTICALS, INC.
    Inventors: Jingrong Jean CUI, Lee Andrew FUNK, Lei JIA, Pei-Pei KUNG, Jerry Jialun MENG, Mitchell David NAMBU, Mason Alan PAIRISH, Hong SHEN, Michelle TRAN-DUBE
  • Publication number: 20140287916
    Abstract: A compound of formula (I), wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, an unsubstituted aromatic 6-membered heterocycle; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: September 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch
  • Publication number: 20140275062
    Abstract: The invention relates to novel compounds which are naphthalene diimides of general formula (I): The compounds are used in therapy, particularly in cancer treatment.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Inventors: Stephen NEIDLE, Stephan A. OHNMACHT, Mekala GUNARATNAM, Aaron Grainger DALE, Marialuisa MICCO, Gavin William COLLIE
  • Publication number: 20140256939
    Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 11, 2014
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Nobuyuki AE, Yuji FUJIWARA
  • Publication number: 20140256658
    Abstract: The present invention describes antibiotic conjugates. These single drug entities are formed connecting one antibiotic with another antibiotic. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
  • Publication number: 20140248654
    Abstract: Provided is a compound represented by formula (I), which can be used as a fluorescent probe that becomes highly fluorescent only in an intracellular acidic environment and can be adapted to the fluorescent imaging of an intracellular vesicle that is a microstructure. In the formula, R1 and R2 independently represent a hydrogen atom, or an alkyl group which may be substituted (wherein R1 and/or R2 represents an alkyl group which may be substituted); R3, R4, R5, R6, R7 and R8 independently represent a hydrogen atom, a halogen atom, or the like; X represents a functional group to which a labeling site or a target-accumulating site can be introduced, or the like; Y represents a halogen atom, an alkyl group which may be substituted, or the like; m represents an integer of 0 to 5; and n represents an integer of 0 to 5.
    Type: Application
    Filed: September 6, 2012
    Publication date: September 4, 2014
    Applicant: THE UNIVERSITY OF TOKYO
    Inventors: Yasuteru Urano, Tetsuo Nagano, Daisuke Asanuma, Kenzo Hirose, Shigeyuki Namiki, Yousuke Takaoka
  • Patent number: 8822464
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: September 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
  • Patent number: 8822448
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
  • Publication number: 20140243322
    Abstract: Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Coferon, Inc.
    Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
  • Publication number: 20140243257
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, JR., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingcan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
  • Publication number: 20140242121
    Abstract: The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Application
    Filed: October 3, 2012
    Publication date: August 28, 2014
    Applicant: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. Lipford, Charles M. Zepp
  • Patent number: 8816079
    Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: August 26, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
  • Patent number: 8815852
    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: Grant
    Filed: April 30, 2008
    Date of Patent: August 26, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Ki Ho Lee, Han Ju Yi, Hyeon Cho, Dae Joong Im, Eun Hee Chae, Yeon Jung Choi
  • Publication number: 20140235609
    Abstract: The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for treating diseases connected to tehinhibition of H3 receptor.
    Type: Application
    Filed: October 8, 2012
    Publication date: August 21, 2014
    Inventors: Tie-Lin Wang, Xuechun Zhang
  • 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
  • Patent number: 8809313
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Grant
    Filed: May 29, 2012
    Date of Patent: August 19, 2014
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Publication number: 20140221311
    Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3?, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I).
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Genesis M. Bacani, Wendy Eccles, Anne E. Fitzgerald, Steven D. Goldberg, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Alice Lee-Dutra, Jing Liu, Kelly J. McClure, Steven P. Meduna, Daniel J. Pippel, Mark D. Rosen, Zachary S. Sales
  • Publication number: 20140221310
    Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, L and R2 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Wendy Eccles, Anne E. Fitzgerald, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Jing Liu, Neelakandha S. Mani, Kelly J. McClure, Steven P. Meduna, Mark D. Rosen
  • Publication number: 20140221384
    Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: ERIMOS PHARMACEUTICALS LLC
    Inventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris
  • Patent number: 8796275
    Abstract: The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal.
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: August 5, 2014
    Assignees: The Trustees of the University of Pennsylvania, Cellceutix Corporation
    Inventors: Richard W. Scott, Doron Greenbaum, Dahui Liu, Xiaodong Fan, Yongjiang Xu, Haizhong Tang, Ehab Khalil
  • Patent number: 8796272
    Abstract: The present invention relates to novel compounds of formula [I] or pharmaceutically acceptable salts thereof: The compounds of the present invention are useful in the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, spasm, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder, or sleep disorders, which is based on the glycine uptake-inhibiting action.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: August 5, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Minoru Moriya, Hiroshi Ohta, Shuji Yamamoto, Kumi Abe, Yuko Araki, Xiang-Min Sun, Daisuke Wakasugi
  • Publication number: 20140213580
    Abstract: Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.
    Type: Application
    Filed: June 18, 2012
    Publication date: July 31, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
  • Patent number: 8791121
    Abstract: The present invention relates to oligooxopiperazines and their use. Methods for preparing oligooxopiperazines are also disclosed.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: July 29, 2014
    Assignee: New York University
    Inventors: Paramjit S. Arora, Petra Tosovska, Danielle Guarracino, Brooke Bullock
  • Publication number: 20140206865
    Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: SYMPHONY EVOLUTION, INC.
    Inventors: Lynne Canne Bannen, Erick Wang Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, Zhaoyang Wen, Wei Xu, Richard George Khoury
  • Publication number: 20140200346
    Abstract: The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.
    Type: Application
    Filed: June 5, 2012
    Publication date: July 17, 2014
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.p.A.
    Inventors: Walter Cabri, Roberto Castagnani, Silvia Armaroli, Gianandrea Quattrociocchi, Vincenzo Colangeli
  • Publication number: 20140199601
    Abstract: The present invention aims to provide an additive for a non-aqueous electrolyte solution with excellent storage stability capable of forming a stable SEI on the surface of an electrode to improve cell performance such as a cycle performance, a discharge/charge capacity, and internal resistance, when the additive is used for electrical storage devices such as non-aqueous electrolyte solution secondary cells and electric double layer capacitors. The present invention also aims to provide a non-aqueous electrolyte solution containing the additive for a non-aqueous electrolyte solution and to provide an electrical storage device using the non-aqueous electrolyte solution.
    Type: Application
    Filed: July 6, 2012
    Publication date: July 17, 2014
    Applicant: SUMITOMO SEIKA CHEMICALS CO., LTD.
    Inventors: Tomohiro Onozuka, Shohei Fujimoto, Koji Fujita
  • 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: 20140187556
    Abstract: Anti-amyloid compounds are provided along with methods of use thereof.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 3, 2014
    Applicant: Treventis Corporation
    Inventors: Mark A. Reed, Arun Yadav, Scott C. Banfield, Christopher J. Barden
  • Publication number: 20140187546
    Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 3, 2014
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Longqin Hu, Amrik Sahota
  • Publication number: 20140187529
    Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.
    Type: Application
    Filed: February 29, 2012
    Publication date: July 3, 2014
    Applicant: LOCUS PHARMACEUTICALS, INC.
    Inventors: Rupa S. Shetty, Martha J. Kelly, Bin Liu, Jinming Zou, Kristopher K. Moffett, Younghee Lee
  • Publication number: 20140187553
    Abstract: The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 3, 2014
    Applicant: AMGEM INC.
    Inventors: Hui-Ling Wang, Victor J. Cee, Bradley J. Herberich, Claire L.M. Jackson, Brian Alan Lanman, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Bin Wu, Ryan Wurz, Andrew Tasker
  • Publication number: 20140179666
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 26, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • Publication number: 20140171438
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 19, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventors: Wenxi Pan, Haizhong Tang
  • Publication number: 20140155409
    Abstract: The invention relates to a compound of formula (I), where R1, R2, R3, m, n, and L1 are as defined in claim 1, 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: June 5, 2014
    Applicant: Metabolys
    Inventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier