Nitrogen Attached Directed Or Indirectly To Morpholine Ring By Nonionic Bonding Patents (Class 544/162)
  • Patent number: 10816552
    Abstract: A compound of formula (I): as described herein and methods and uses thereof as for mass tagging a biosensor or biologically active material.
    Type: Grant
    Filed: January 11, 2019
    Date of Patent: October 27, 2020
    Assignees: The Governing Council of the University of Toronto, University Health Network
    Inventors: Mark Nitz, Landon J. Edgar, Bradly G. Wouters, David Hedley, Lisa M. Willis, Matthew A. Lumba, Hanuel Park, Ravi N. Vellanki
  • Patent number: 10280237
    Abstract: The present invention relates to salts of etheramines and polymeric acid, and in particular to salts of etheramines and polycarboxylic acid and their manufacturing process.
    Type: Grant
    Filed: August 11, 2015
    Date of Patent: May 7, 2019
    Assignee: BASF SE
    Inventors: Bernhard Ulrich von Vacano, Sophia Ebert, Bjoern Ludolph, Christof Wilhelm Wigbers, Christian Eidamshaus, Brian J. Loughnane, Frank Huelskoetter, Stefano Scialla
  • Patent number: 10222380
    Abstract: A compound of formula (I) as described herein and methods and uses thereof as probes in the mass tagging of biosensors or biologically active materials for use in mass cytometry analysis of tissue samples such as in the detection, labelling and quantification of oxygen-deprived cells by using, for example, tellurophene-tagged 2-nitroimidazole.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: March 5, 2019
    Assignees: The Governing Council of the University of Toronto, University Health Network
    Inventors: Mark Nitz, Landon J. Edgar, Bradley G. Wouters, David Hedley, Lisa M. Willis, Matthew A. Lumba, Hanuel Park, Ravi N. Vellanki
  • Patent number: 10004674
    Abstract: Compounds, and agents for oxidatively changing the color of keratinic fibers that include such compounds, in particular human hair, in a cosmetic carrier. The compounds are at least one oxidation dye precursor product of formula (I) and/or physiologically acceptable salt thereof, in which R1, R2, R3, R4 independently of one another, stand for a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, a hydroxy-(C1-C6)-alkyl group, a polyhydroxy-(C2-C6)-alkyl group, or a C1-C6-alkoxy-C2-C6-alkyl group, n stands for an integer from 2 to 6, and Z stands for an aromatic or aliphatic heterocycle or for an aromatic or aliphatic carbocycle.
    Type: Grant
    Filed: December 14, 2016
    Date of Patent: June 26, 2018
    Assignee: Henkel AG & Co. KGaA
    Inventors: Antje Gebert-Schwarzwaelder, Helmut Giesa, Jan-Michael Schoenebeck
  • Patent number: 9108936
    Abstract: Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: April 18, 2013
    Date of Patent: August 18, 2015
    Assignee: GRUENENTHAL GMBH
    Inventors: Gregor Bahrenberg, Sven Kuehnert, Simon Lucas, Wolfgang Schroeder
  • Publication number: 20150133431
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 14, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventor: Gary C. Look
  • Patent number: 8993568
    Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof, methods of treating hypertriglyceridemia using the compounds; and a process for preparing the compounds.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: March 31, 2015
    Assignee: Eli Lilly and Company
    Inventors: Maria Rosario Gonzalez-Garcia, Maria Carmen Fernandez
  • 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: 20150038512
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, or reduce biofilms, or to inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: October 6, 2014
    Publication date: February 5, 2015
    Inventors: Ryan Looper, Dustin Williams, Sujeevini Jeyapalina, Travis Haussener, Paul R. Sebahar, Hariprasada R. Kanna Reddy
  • Publication number: 20150038705
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: October 6, 2014
    Publication date: February 5, 2015
    Inventors: DUSTIN WILLIAMS, RYAN LOOPER, SUJEEVINI JEYAPALINA, TRAVIS HAUSSENER, PAUL R. SEBAHAR, HARI KANNA REDDY
  • Publication number: 20150038498
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 5, 2015
    Inventors: Timothy Allen Blizzard, Tesfaye Biftu
  • Patent number: 8946478
    Abstract: Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: February 3, 2015
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hua Bai, Xuyang Zhao, Yongxiang Gong, Jinqing Zhong, Qifeng Zhu, Xiaoyu Liu, Lifei Liu, Qixian Zhou
  • Patent number: 8940890
    Abstract: Disclosed is a synthesis method of a compound of formula 1,5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxyl]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (i.e. aprepitant), which comprises cyclizing a compound of formula 4 in a solvent, wherein R is C1-C5 alkyl. The intermediate for preparing aprepitant is also disclosed. The present method is especially suitable for industrial production of aprepitant.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: January 27, 2015
    Assignee: Chengdu DI'AO Pharmaceutical Group Co., Ltd.
    Inventors: Jianxin Ji, Qiang Zhang, Fengtian Du, Yi Jin, Tao Zhang, Na Guo, Xiaowei Yan, Yongrongn Yang, Bogang Li
  • Publication number: 20140371176
    Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 18, 2014
    Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
  • Patent number: 8802673
    Abstract: The present invention relates to compounds of formula I wherein A, B, X, Y, Ar, R1, R2, R?, m and n are as defined herein and to pharmaceutical active acid addition salts thereof, which have a good affinity to the trace amine associated receptors TAAR1, so that they can be used for the treatment of depression, anxiety disorders and bipolar disorder.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: August 12, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: Guido Galley, Roger David Norcross, Philippe Pflieger
  • Patent number: 8785208
    Abstract: The present invention provides fluorogenic compounds for the detection of target metal ions wherein the compounds exhibit a Stokes shift greater than 50 nm and the detectable signal is modulated by photoinduced electron transfer (PET). The present compounds consist of three functional elements, the ion sensing moiety (chelating moiety), the reporter moiety (fluorophore or fluorescent protein) and spacer or linker between the sensing and reporter moieties of the present compound that allows for PET upon binding of a metal ion and excitation by an appropriate wavelength.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: July 22, 2014
    Assignee: Life Technologies Corporation
    Inventors: Kyle Gee, Vladimir Martin
  • Patent number: 8785440
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: July 22, 2014
    Assignees: Biogen Idec MA, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Publication number: 20140171403
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
    Type: Application
    Filed: March 15, 2013
    Publication date: June 19, 2014
    Applicant: Novartis AG
    Inventors: Darren Mark Legrand, Vikki Furminger, Christopher Thomson, Owen Rhys Hughes, Emily Stanley
  • Publication number: 20140142303
    Abstract: The invention relates to a process for the preparation of 5-chloro-N-({(5-S)-2-oxo3-[4-(3-oxo-morj)holine-4-yl)-phenyl]-1,3-oxazolidine-5-yl}-methyl) thiophen-2-carboxamide having the INN rivaroxaban. The process is characterized by the reactions according to claim 1. The invention also relates to intermediates formed in the above process.
    Type: Application
    Filed: May 4, 2012
    Publication date: May 22, 2014
    Applicant: EGIS Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
    Inventors: Eva Sipos, Gyorgyi Kovanyine Lax, Balazs Havasi, Balazs Volk, Gyorgy Krasznai, Gyorgy Ruzsics, Jozsef Barkoczy, Maria Tothne Lauritz, Gyula Lukacs, Andras Boza, Laszlo Jozsef Hegedus, Maria Julia Taborine Toth, Eva Pecsi
  • Publication number: 20140128335
    Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.
    Type: Application
    Filed: February 23, 2012
    Publication date: May 8, 2014
    Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE CORSE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jean-Michel Bolla, Jean Michel Brunel, Joseph Pierre Felix Casanova, Vannina Lorenzi, Liliane Berti
  • Patent number: 8642596
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: February 4, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yuanming Zhang, Sylvie Laquerre
  • Publication number: 20130345213
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: LUPIN LIMITED
    Inventors: Manojkumar Ramprasad Shukla, Vinod Dinkar Chaudhari, Majid Bashir Sayyed, Ramesh Dattatraya Phadtare, Navnath Bajirao Walke, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8592419
    Abstract: The invention provides the compounds of formula (): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, A, X, Y, a, b and n are as defined herein. Also disclosed are methods for making the compounds of formula (I) and their use in treating or preventing diseases associated with cell overproliferation and dysfunctional sphingolipid signal transduction. The invention also encompasses the use of the compounds in combination with an apoptosis-signaling ligand, such as Fas ligand. Preferably, the Fas ligand is administered in the form of a gene therapy agent.
    Type: Grant
    Filed: October 31, 2005
    Date of Patent: November 26, 2013
    Assignee: MUSC Foundation for Research Development
    Inventors: Alicja Bielawska, Yusuf A. Hannun, James Norris, Zdzislaw M. Szulc, Jian-yun Dong, Jacek Bielawski, David A. Schwartz, David H. Holman, Ahmed M. El-Zawahry, John McKillop
  • Publication number: 20130310383
    Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.
    Type: Application
    Filed: July 24, 2013
    Publication date: November 21, 2013
    Applicant: Allergan, Inc.
    Inventors: Bertrand Leblond, Eric Beusoleil, Thierry Taverne, John E. Donello
  • Patent number: 8524898
    Abstract: Novel iminium-type coupling agents containing proton acceptors in their iminium moiety, which can be used beneficially as coupling agents in various chemical polypeptide and/or polynucleotide syntheses, and are particularly useful as yield enhancing and racemization suppressing coupling agents for use in peptide syntheses, are disclosed. Further disclosed are a process of preparing such iminium-type coupling agents and their use in the preparation of polypeptides and/or polynucleotides.
    Type: Grant
    Filed: May 15, 2008
    Date of Patent: September 3, 2013
    Assignee: Luxembourg Bio Technologies Ltd.
    Inventors: Fernando Albericio, Ayman El-Faham, Yoav Luxembourg, Ariel Ewenson
  • Publication number: 20130225810
    Abstract: Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.
    Type: Application
    Filed: November 3, 2011
    Publication date: August 29, 2013
    Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hua Bai, Xuyang Zhao, Yongxiang Gong, Jinqing Zhong, Qifeng Zhu, Xiaoyu Liu, Lifei Liu, Qixian Zhou
  • Publication number: 20130158021
    Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.
    Type: Application
    Filed: October 26, 2012
    Publication date: June 20, 2013
    Applicant: Massachusetts Institute of Technology
    Inventor: Massachusetts Institute of Technology
  • Patent number: 8426587
    Abstract: The present invention is related to the preparation and pharmaceutical use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification: (I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: April 23, 2013
    Assignee: Pharmaxis Ltd.
    Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
  • Publication number: 20130072488
    Abstract: Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
    Type: Application
    Filed: May 13, 2011
    Publication date: March 21, 2013
    Applicant: Shanghai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Yongyong Zheng, Yunfeng Liao, Yali Li
  • Publication number: 20120301552
    Abstract: A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
    Type: Application
    Filed: December 23, 2011
    Publication date: November 29, 2012
    Applicant: JAPAN TOBACCO INC.
    Inventors: Yuko Shinagawa, Teruhiko Inoue, Toshihiro Kiguchi, Taku Ikenogami, Naoki Ogawa, Kenji Fukuda, Takashi Nakagawa, Masanori Shindo, Yuki Soejima
  • Patent number: 8283383
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: October 9, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Publication number: 20120190816
    Abstract: The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR8, where R8 is C1-6 alkyl, C6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC (O)— occurs without racemisation. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.
    Type: Application
    Filed: July 20, 2011
    Publication date: July 26, 2012
    Inventors: Laurence M. Harwood, Ran Yan
  • Patent number: 8202866
    Abstract: The present invention is directed to a compound of formula I, and processes for the manufacture of said compounds as well as medicaments containing said compound. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: June 19, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu
  • Publication number: 20120149707
    Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.
    Type: Application
    Filed: April 21, 2011
    Publication date: June 14, 2012
    Applicant: OSCOTEC INC.
    Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
  • Publication number: 20120101039
    Abstract: A compound of general formula I their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, methods of treating diseases with said compounds, and the use of said compounds in the manufacture of medicaments.
    Type: Application
    Filed: May 26, 2010
    Publication date: April 26, 2012
    Applicant: LEO PHARMA A/S
    Inventors: Jef Fenscholdt, Thomas Høyer, Xifu Liang, Sophie Elisabeth Havez
  • Publication number: 20120046272
    Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.
    Type: Application
    Filed: August 19, 2011
    Publication date: February 23, 2012
    Applicant: GRUNENTHAL GMBH
    Inventor: Ramesh SESHA
  • Publication number: 20120004206
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Application
    Filed: August 25, 2011
    Publication date: January 5, 2012
    Inventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
  • Publication number: 20110313158
    Abstract: The invention describes the development of highly efficient, recyclable two component system, CuAl-hydrotalcite/rac 1,1?-Binaphthalene-2,2?-diol catalytic system for the N-alkylation of electron deficient aryl chlorides in presence of potassium carbonate as a base at room temperature in 3-6 h, wherein the process is provided for the preparation of various secondary amines via C—N coupling reaction of aliphatic amines(aliphatic open chain, acyclic, benzyl amines and heterocyclic amines) with various aryl chlorides.
    Type: Application
    Filed: February 26, 2010
    Publication date: December 22, 2011
    Inventors: Pravin R. Likhar, R. Arundhati, M. Lakshmi Kantam
  • Publication number: 20110306600
    Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.
    Type: Application
    Filed: June 10, 2011
    Publication date: December 15, 2011
    Applicant: Grunenthal GmbH
    Inventor: Ramesh SESHA
  • Publication number: 20110306542
    Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.
    Type: Application
    Filed: June 9, 2011
    Publication date: December 15, 2011
    Applicant: Receptos, Inc.
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
  • Publication number: 20110275784
    Abstract: The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR8, where R8 is C1-6 alkyl, C6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC (O)— occurs without racemisation. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.
    Type: Application
    Filed: July 20, 2011
    Publication date: November 10, 2011
    Inventors: Laurence M. Harwood, Ran Yan
  • Publication number: 20110230428
    Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Application
    Filed: July 22, 2009
    Publication date: September 22, 2011
    Inventors: John Wityak, Leticia M. Toledo-sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
  • Publication number: 20110207926
    Abstract: A compound represented by formula (1), a tautomer thereof, or a salt of the compound or tautomer, which is useful as a bactericide/disinfectant. In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like, R2 represents a hydrogen atom or an optionally substituted alkyl group, or alternatively R1 and R2 may combine together with an adjacent nitrogen atom to form an optionally substituted nitrogen-containing heterocyclic group; R4 represents a hydrogen atom or an optionally substituted alkyl group; R3 represents an optionally substituted alkyl group; and R5 and R6 each represents a hydrogen atom or a methyl group, excluding a compound wherein both R2 and R4 represent a hydrogen atom and a compound wherein both R1 and R4 represent a hydrogen atom are excluded.
    Type: Application
    Filed: August 24, 2009
    Publication date: August 25, 2011
    Applicant: HAMARI CHEMICALS, LTD.
    Inventors: Shirou Maeda, Akihisa Maeda
  • Patent number: 7956185
    Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 7, 2011
    Assignee: Abbott Laboratories
    Inventors: Robert B. Diebold, Stevan W. Djuric, Vincent L. Giranda, Laura A. Hexamer, Nan-Horng Lin, Julie M. Miyashiro, Thomas D. Penning, Magdalena Przytulinska, Thomas J. Sowin, Gerard M. Sullivan, Zhi-Fu Tao, Yunsong Tong, Anil Vasudevan, Le Wang, Keith W. Woods, Zhiren Xia, Henry Q. Zhang
  • Patent number: 7951803
    Abstract: Compounds of the formula wherein R1 represents optionally substituted C1-C10 alkyl, aryl or heteroaryl, and R3 represents alkoxy-substituted aryl or optionally substituted heteroaryl, are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.
    Type: Grant
    Filed: March 9, 2007
    Date of Patent: May 31, 2011
    Assignee: Pharmacopeia, LLC
    Inventors: Andrew G. Cole, Marc-Raleigh Brescia, Joan J. Zhang, Zahid Hussain, David J. Diller, Axel Metzger, Gulzar Ahmed, Ian Henderson
  • Publication number: 20110046128
    Abstract: A series of novel compounds showing anticonvulsant, chemical countermeasure(s), and analgesic activities is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.
    Type: Application
    Filed: September 13, 2010
    Publication date: February 24, 2011
    Applicant: AURIMMED PHARMA, INC.
    Inventors: Amir Pesyan, Manuel F. Balandrin
  • Publication number: 20110046129
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
    Type: Application
    Filed: September 9, 2010
    Publication date: February 24, 2011
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
  • Publication number: 20110039852
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: January 29, 2009
    Publication date: February 17, 2011
    Applicant: AMIRA PHARMACEUTICALS, INC.
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
  • Publication number: 20100331234
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Application
    Filed: March 3, 2010
    Publication date: December 30, 2010
    Applicant: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher Gerard Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel G. Anderson
  • Publication number: 20100317582
    Abstract: The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Application
    Filed: November 20, 2008
    Publication date: December 16, 2010
    Applicant: LEO Pharma A/S
    Inventors: Jef Fensholdt, Sophie Elisabeth Havez, Bjarne Nørremark