Indole Ring System (including Hydrogenated) Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/254.09)
  • Patent number: 10273243
    Abstract: The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is H, OH, or halogen; B is a substituted or unsubstituted heterobicycle, pyridazine, pyrazole, pyrazine, thiadiazole, or triazole, wherein the heterobicycle is other than chloro substituted indole; and the pyrazole, when substituted, is substituted with other than trifluoromethyl, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: April 30, 2019
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Nicoleta Dobri, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
  • Patent number: 10011590
    Abstract: The present application relates to crystalline and amorphous Vilazodone hydrochloride. The present application further relates to amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carriers. The present application also relates to a process for the preparation of form I of vilazodone free base.
    Type: Grant
    Filed: April 13, 2017
    Date of Patent: July 3, 2018
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Javed Iqbal, Srinivas Oruganti, Rajesh Kumar Rapolu, Vishweshwar Peddy, Rajesham Boge, Deepika Pathivada, Dharma Jagannadha Rao Velaga, Sesha Reddy Yarraguntla, Sudhakar Reddy Baddam, Anitha Naredla, Kiran Kumar Doniparthi, Srividya Ramakrishnan
  • Patent number: 9969721
    Abstract: The present invention relates to an improved process for the preparation of vilazodone Hydrochloride and a process for preparation of novel pure amorphous form of vilazodone hydrochloride.
    Type: Grant
    Filed: April 5, 2013
    Date of Patent: May 15, 2018
    Assignee: Alembic Pharmaceuticals Limited
    Inventors: Venkat Raman Jayaraman, Dhiraj Rathod, Irfan Vohra, Vinayak Bhujade, Viral Modi, Mayur Budh, Ojas Gandhi
  • Patent number: 9931347
    Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X2, X4, X10, and X11 may be the same or different and each is independently selected from C and N; X1, X3, X5, X6, X7, X8, and X9 may be the same or different and each is independently selected from C, N and O; each bond having a dotted line may independently be a double bond or a single bond, provided that valencies at each atom are maintained; the dotted lines joining X4 with the carbon atoms either side of X2 are single bonds, and are only present when X2 is absent, X3 is absent and X4 is C, and when these bonds are present the ring carbons on each side of X2 are not directly bonded to each other; each R1 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of R1 groups present is such that the valency of X1 is maintaine
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: April 3, 2018
    Assignee: IOmet Pharma Ltd.
    Inventors: Phillip Martin Cowley, Alan Wise, Margaret Huggett
  • Patent number: 9822109
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: November 21, 2017
    Assignee: Plexxikon Inc.
    Inventors: Jiazhong Zhang, Wayne Spevak
  • Patent number: 9505744
    Abstract: The present invention provides solid state forms of Vilazodone and Vilazodone hydrochloride, processes for preparing these solid state forms, and pharmaceutical compositions comprising one or more of these solid state forms.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: November 29, 2016
    Assignee: Assia Chemical Industries LTD.
    Inventors: Edislav Leksic, Dubravka Pavlicic, Dijana Skalec Samec, Jasna Dogan
  • Publication number: 20150126525
    Abstract: Provided are crystalline and amorphous vilazodone hydrochloride. Further provided are amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carries. Also provided is a process for the preparation of form I of vilazodone free base.
    Type: Application
    Filed: May 10, 2013
    Publication date: May 7, 2015
    Inventors: Javed Iqbal, Srinivas Oruganti, Rajesh Kumar Rapolu, Vishweshwar Peddy, Rajesham Boge, Deepika Pathivada, Dharma Jagannadha Rao Velaga, Sesha Reddy Yarraguntla, Sudhakar Reddy Baddam, Anitha Naredla, Kiran Kumar Doniparthi, Ramesh Kumar Nadgoud, Narasimha Rao Pagadala, Syam Kumar Unniaran, Srividya Ramakrishnan
  • Publication number: 20150126526
    Abstract: Co-crystal of a serotonin reuptake inhibitor, in stable form.
    Type: Application
    Filed: November 4, 2014
    Publication date: May 7, 2015
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Nicolas TESSON, Jordi de Mier VINUÉ
  • Patent number: 9018214
    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: Grant
    Filed: April 20, 2012
    Date of Patent: April 28, 2015
    Assignee: 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: 20150099746
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 9, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Patent number: 8999994
    Abstract: The present invention relates to a compound of formula (I): wherein: R1 and R2 are selected from among H and C1-C10 alkyl; R3 is selected from among H, —OR4, N, —CN, —C(O)R4, —C(O)OR4, —C(O)NR4R5, —C?NR4, —OC(O)R4, —NR4R5, —NR4C(O)R5, —NO2, —N?CR4R5, halogen and C1-C10 alkyl, wherein R4 and R5 are selected from among H, alkyl, alkenyl, cycloalkyl and aryl; X, Y, Z1, Z2 and Z3 are selected independently from among CH and N; A is selected from among (CH2)n, NH, O and CO, wherein n is an integer between 1 and 6, to the procedure for the obtainment of said compounds, to a pharmaceutical composition comprising said compound, and to the use thereof in the treatment of a neurodegenerative disease, more particularly treatment of Alzheimer's or Parkinson's disease.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: April 7, 2015
    Assignees: Consejo Superior de Investigaciones Cientificas, Universitat Autonoma de Barcelona, Universidad de Barcelona
    Inventors: Abdelouahid Samadi, José Luis Marco Contelles, Irene Bolea Tomás, Francisco Javier Luque Garriga, Mercedes Unzeta López
  • Publication number: 20150080316
    Abstract: The invention relates to new functionalized thieno-indole derivatives of formula (I) or (II) which have cytotoxic activity and are useful in treating diseases such as cancer and cellular proliferation disorders. The invention also relates to the use of these functionalized thieno-indole derivatives in the preparation of conjugates.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 19, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa
  • Publication number: 20150080381
    Abstract: Method of treating alopecia and acne with are disclosed.
    Type: Application
    Filed: April 12, 2013
    Publication date: March 19, 2015
    Inventors: Mark G. Currie, Yueh-tyng Chien
  • Publication number: 20150080411
    Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
    Type: Application
    Filed: November 21, 2014
    Publication date: March 19, 2015
    Applicant: MERCK PATENTGESELLSCHAFT
    Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Bottcher
  • Patent number: 8980897
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: March 17, 2015
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlene Schuppli-Nollet
  • Publication number: 20150057248
    Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.
    Type: Application
    Filed: September 1, 2014
    Publication date: February 26, 2015
    Applicant: The Board of Regents of The University of Texas System
    Inventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
  • Publication number: 20150051219
    Abstract: A method of treating exposure to organophosphate agents through the use of compounds comprising tetrahydroindolone and arylpiperazine moieties.
    Type: Application
    Filed: July 28, 2014
    Publication date: February 19, 2015
    Inventors: David Reed HELTON, David Brian FICK
  • Publication number: 20150051154
    Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
    Type: Application
    Filed: March 28, 2013
    Publication date: February 19, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
  • Publication number: 20150051144
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: September 26, 2012
    Publication date: February 19, 2015
    Inventors: Harikishore Pingali, Vrajesh Pandya
  • Publication number: 20150038484
    Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: PFIZER INC.
    Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
  • Publication number: 20150018370
    Abstract: The invention relates to a new solvate, Vilazodone hydrochloride monoethanol monohydrate solvate, and to a process for the preparation of polymorphic form III of Vilazodone hydrochloride via the Vilazodone hydrochloride monoethanol monohydrate solvate.
    Type: Application
    Filed: July 9, 2014
    Publication date: January 15, 2015
    Inventors: Marijan Stefinovic, Clemens Haefele, Ulrich J. Griesser
  • Publication number: 20150018310
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: September 29, 2014
    Publication date: January 15, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
  • Publication number: 20150018339
    Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Application
    Filed: February 21, 2014
    Publication date: January 15, 2015
    Inventors: Christopher R. MCCURDY, Christophe Mesangeau, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem, Frederick T. Chin, Jacques Henri Poupaert
  • Patent number: 8927552
    Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: January 6, 2015
    Assignee: Merck Patentgesellschaft
    Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
  • Patent number: 8927546
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: January 6, 2015
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • Patent number: 8921375
    Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: December 30, 2014
    Assignee: Merck Patentgesellschaft
    Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Bottcher
  • Publication number: 20140378472
    Abstract: The present invention relates to amorphous vilazodone hydrochloride, its process of preparation and pharmaceutical composition thereof.
    Type: Application
    Filed: December 12, 2012
    Publication date: December 25, 2014
    Inventors: Poonam Kaushik, Ram Thaimattam, Mohan Prasad, Sudershan Kumar Arora
  • Publication number: 20140350022
    Abstract: The present invention relates to a beneficial treatment of tumours in patients suffering from NSCLC, and to a clinical marker useful as as predictive variable of the responsiveness of tumours in patients suffering from NSCLC. The present invention further relates to a method for selecting patients likely to respond to a given therapy, wherein said method optionally comprises the use of a specific clinical marker. The present invention further relates to a method for delaying disease progression and/or prolonging patient survival of NSCLC patients, wherein said method comprises the use of a specific clinical marker.
    Type: Application
    Filed: May 2, 2014
    Publication date: November 27, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Birgit GASCHLER-MARKEFSKI, Ralf KAISER
  • Publication number: 20140336200
    Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: ADAMED SP. Z O.O.
    Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
  • Publication number: 20140323498
    Abstract: The present invention provides solid state forms of Vilazodone and Vilazodone hydrochloride, processes for preparing these solid state forms, and pharmaceutical compositions comprising one or more of these solid state forms
    Type: Application
    Filed: November 21, 2012
    Publication date: October 30, 2014
    Inventors: Edislav Leksic, Dubravka Pavlicic, Dijana Skalec Samec, Jasna Dogan
  • Patent number: 8865682
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: October 21, 2014
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
  • Publication number: 20140303138
    Abstract: The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.
    Type: Application
    Filed: December 3, 2013
    Publication date: October 9, 2014
    Inventors: Wilfried Braje, Astrid Netz, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
  • Publication number: 20140303185
    Abstract: The present invention relates to novel crystalline polymorphic forms of Vilazodone hydrochloride of formula (I). This present invention further provides the process for the preparation of novel polymorphic forms of Vilazodone hydrochloride.
    Type: Application
    Filed: April 9, 2014
    Publication date: October 9, 2014
    Inventors: Buchi Reddy REGURI, Venkateshwar Goud THIRUMANI, Srinivasa Rao MANNAVA, Suresh DEVINENI
  • Publication number: 20140296217
    Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
    Type: Application
    Filed: February 20, 2014
    Publication date: October 2, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: John Edward PARK, Gerald Juergen ROTH, Armin HECKEL, Nveed CHAUDHARY, Trixi BRANDL, Georg DAHMANN, Matthias GRAUERT
  • Publication number: 20140296249
    Abstract: Dopamine D3 receptor antagonists and partial agonists are known to modulate the reinforcing and drug-seeking effects induced by cocaine and other abused substances. By introducing functionality into the butylamide linking chain of the 4-phenylpiperazine class of ligands, improved D3 receptor affinity and selectivity, as well as water solubility, is achieved. A series of linking-chain derivatives are disclosed wherein functionality such as OH, OAc, and cis or trans-cyclopropyl groups have been introduced into the linking chain. In general, these modifications are well tolerated at D3 receptors and achieve high selectivity over D2 and D4 receptors.
    Type: Application
    Filed: April 30, 2014
    Publication date: October 2, 2014
    Applicants: The United States of America, as Represented by the Secretary, Department of Health and Human Serv, THE UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE AT FORT WORTH
    Inventors: Amy Hauck Newman, Peter Grundt, George C. Cyriac, Robert Luedtke, Jianjing Cao
  • Patent number: 8846684
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: September 30, 2014
    Assignee: The Regents of The University of Michigan
    Inventors: Scott Larsen, Janice Sindac, Scott Barraza, David J. Miller
  • Publication number: 20140275076
    Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Katsunori Tsuboi, Yosuke Takanashi, Shingo Tojo, Tomohiro Kodama, Katsumi Kubota, Toshio Kanai
  • Publication number: 20140275033
    Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
  • Publication number: 20140275108
    Abstract: Provided herein are novel benzenesulfonamide compounds having a structure of formula (I) below: as well as to the method for synthesizing same and to the use thereof in pharmaceutical compositions to be used in human or veterinary medicine, as well as to the use thereof. Also provided herein are methods of using the disclosed pharmaceutical compositions for the treatment of neuroinflammatory skin diseases such as acne.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Carine MOUNIER, Isabelle Carlavan, Jerome Aubert, André Jomard, Patricia Rossio
  • Publication number: 20140275115
    Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
    Type: Application
    Filed: May 30, 2014
    Publication date: September 18, 2014
    Applicant: MERCK PATENTGESELLSCHAFT
    Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Bottcher
  • Patent number: 8835635
    Abstract: Disclosed herein is a stable amorphous form of vilazodone hydrochloride substantially free of crystalline forms, a process for the preparation, pharmaceutical compositions, and methods of treating thereof. Disclosed also herein are stable amorphous co-precipitates of vilazodone hydrochloride and a pharmaceutically acceptable excipient, methods for the preparation, pharmaceutical compositions, and method of treating thereof.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: September 16, 2014
    Assignee: Symed Labs Limited
    Inventors: Dodda Mohan Rao, Aadepu Jithender
  • Patent number: 8815870
    Abstract: The present teachings provide a compound of Formula (I-B): wherein R1-R10 are as described herein; a pharmaceutically acceptable salt of the compound, a geometric isomer of the compound, or a pharmaceutically acceptable salt of the geometric isomer. Also described are methods of preparing the same, as well as methods for preparing vilazodone using the same.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: August 26, 2014
    Inventors: Henning Böttcher, Timo Heinrich
  • Publication number: 20140228359
    Abstract: The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
    Type: Application
    Filed: July 20, 2012
    Publication date: August 14, 2014
    Applicant: UNIVERSITE JOSEPH FOURIER
    Inventors: Jean-Noël Denis, Marcelle Claude Jolivalt, Louis Max Maurin, Nikolaevna Olga Burchak
  • Publication number: 20140200226
    Abstract: Novel compositions and methods for the treatment and prevention of malaria are disclosed herein.
    Type: Application
    Filed: December 12, 2013
    Publication date: July 17, 2014
    Applicants: Florida Atlantic University, University of Central Florida Research Foundation, Inc.
    Inventors: Debopam Chakrabarti, Amy Wright
  • Patent number: 8779132
    Abstract: The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C?O, (C?O)O, (C?O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C?O or (C?O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: July 15, 2014
    Assignee: Astex Therapeutics Limited
    Inventors: Miles Stuart Congreve, Lynsey Helen Fazal, Martyn Frederickson, Christopher William Murray, Michael Alistair O'Brien, Andrew James Woodhead, John Francis Lyons, Neil Thomas Thompson
  • Patent number: 8778948
    Abstract: The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein C1 and C2 represent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R1, R2, R3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: July 15, 2014
    Assignee: NHWA Pharma, Corporation
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang
  • Publication number: 20140194442
    Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.
    Type: Application
    Filed: January 12, 2012
    Publication date: July 10, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Flavio Solca, Ulrich Guertler, Michael Sanderson, Ulrike Tontsch-Grunt, Irene Waizenegger
  • 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: 20140187563
    Abstract: The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of an inhibitor of vascular endothelial growth factor receptors (VEGFRs) in conjunction with a thrombin inhibitor.
    Type: Application
    Filed: March 6, 2014
    Publication date: July 3, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Joanne VAN RYN, Frank HILBERG, Pilar GARIN-CHESA
  • Patent number: RE46815
    Abstract: To provide a novel furanone derivative, and a medicine including the same.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: May 1, 2018
    Assignee: Carna Biosciences, Inc.
    Inventors: Takayuki Irie, Ayako Sawa, Masaaki Sawa, Tokiko Asami, Yoko Funakoshi, Chika Tanaka