Hetero Ring In The Polycyclo Ring System Patents (Class 514/320)
  • Publication number: 20130225530
    Abstract: The present invention relates to a pharmaceutical composition for use as a medicament for the treatment or prophylaxis of cardiac hypertrophy, comprising at least one compound of formula (I), wherein: R1 is e.g. hydrogen, —CH3, R2 is e.g. hydrogen, —CH3, R4 is hydrogen, —OH, —NH2; R5 is hydrogen, —OH; R6 is hydrogen, —OH; R3 is e.g. —OCH3 or a pharmaceutically acceptable salt, and at least one pharmaceutical excipient.
    Type: Application
    Filed: July 6, 2011
    Publication date: August 29, 2013
    Applicant: DKFZ DEUTSCHES KREBSFORSCHUNGSZENTRUM
    Inventors: Min Li-Weber, H. Peter Krammer, Gernot Polier
  • Patent number: 8501774
    Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: August 6, 2013
    Assignee: Morphochem Aktiengesellschaft für Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Muller, Michael W. Cappi
  • Publication number: 20130196987
    Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.
    Type: Application
    Filed: October 30, 2012
    Publication date: August 1, 2013
    Applicant: EISAI CO., LTD.
    Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
  • Publication number: 20130197033
    Abstract: A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: wherein R1 is a hydrogen atom or C1-6 alkyl group.
    Type: Application
    Filed: January 29, 2013
    Publication date: August 1, 2013
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventor: EISAI R&D MANAGEMENT CO., LTD.
  • Patent number: 8466200
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: February 7, 2012
    Date of Patent: June 18, 2013
    Assignee: Merck Patent GmbH
    Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
  • Publication number: 20130150401
    Abstract: The present invention relates to compounds of formula I, wherein R1, LP, LQ, X, A, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 13, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Boehringer Ingelheim International GmbH
  • Publication number: 20130143921
    Abstract: This invention provides the methods of separation and identification of a novel type of piperidine flavan alkaloids from an African herbal tea, the leaves of Combretum micranthum commonly known as kinkeliba, and the procedures for preparing the total piperidine flavan alkaloids (TPFA). In particular, this invention relates to the use of the plant extract that may contain TPFA as anti-diabetic agents in treatment of metabolic disorders and other applications related to this new chemical structure and derivatives thereof.
    Type: Application
    Filed: May 3, 2011
    Publication date: June 6, 2013
    Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: James E. Simon, Qingli Wu, Cara Welch
  • Patent number: 8455521
    Abstract: Diaminoalkanes of below Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity: They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: June 4, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Patent number: 8440832
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: July 14, 2008
    Date of Patent: May 14, 2013
    Assignee: Board of Regents, The University of Texas System
    Inventors: Mohamed Naguib Attala, Philippe Diaz
  • Patent number: 8440691
    Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: May 14, 2013
    Assignee: AbbVie Inc.
    Inventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
  • Publication number: 20130116247
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: April 5, 2011
    Publication date: May 9, 2013
    Applicant: MANNKIND CORPORATION
    Inventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
  • Publication number: 20130116232
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: June 8, 2011
    Publication date: May 9, 2013
    Applicant: ARAGON PHARMACEUTICALS, INC.
    Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
  • Patent number: 8435978
    Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: May 7, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
  • Patent number: 8436021
    Abstract: This invention relates to the use of a ligand of the 5-HT4 receptor or of a pharmaceutically acceptable salt of this ligand and to a nucleic acid coding for a 5-HT4 receptor or of a functionally equivalent receptor for a drug for treating and/or preventing a pathology associated with an obsessional behavior such as anorexia, bulimia and the addiction to drugs of abuse or obesity. The invention also relates to a method for identifying a compound that is biologically active in the treatment and/or the prevention of a pathology associated with an obsessional conduct or obesity including: a) placing the 5-HT4 receptor or a functionally equivalent receptor in contact with this biologically active compound, and b) the determination of whether this biologically active compound is capable of modulating the basal activity of the 5-HT4 receptor or of a functionally equivalent receptor.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: May 7, 2013
    Assignee: Centre National de la Recherche Scientifique-CNRS
    Inventor: Valerie Compan
  • Patent number: 8410271
    Abstract: This invention relates to chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: April 2, 2013
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
  • Publication number: 20130065859
    Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 12, 2011
    Publication date: March 14, 2013
    Applicant: SANOFI
    Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary MCCORT
  • Patent number: 8394794
    Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: March 12, 2013
    Assignee: Regents of The University of Minnesota
    Inventors: Chengguo Xing, Jignesh Doshi
  • Patent number: 8389548
    Abstract: Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3?,17?-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
    Type: Grant
    Filed: February 18, 2005
    Date of Patent: March 5, 2013
    Assignee: Endorecherche, Inc.
    Inventor: Fernand Labrie
  • Patent number: 8389546
    Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
    Type: Grant
    Filed: July 1, 2011
    Date of Patent: March 5, 2013
    Assignee: Hydra Biosciences, Inc.
    Inventors: Magdalene M. Moran, Jayhong A. Chong, Christopher Fanger, Amy Ripka, Glenn R. Larsen, Xiaoguang Zhen, Dennis John Underwood, Manfred Weigele
  • Publication number: 20130053415
    Abstract: In some aspects, the invention provides compositions and methods of use for treating a variety of diseases. In some aspect, the compositions and methods involve combined modulation of transcriptional modulators.
    Type: Application
    Filed: February 4, 2011
    Publication date: February 28, 2013
    Inventors: Peter B. Rahl, Richard A. Young
  • Publication number: 20130045988
    Abstract: Described herein is a combination comprising at least one 5-HT4 receptor agonist and at least one phosphodiesterase 4 (PDE4) inhibitor, and methods and uses thereof in the prevention and/or treatment of one or more disorders in which an increased acetylcholine release is desired; for example in the prevention and/or treatment of gastrointestinal disorders, urinary disorders, and/or respiratory disorders.
    Type: Application
    Filed: August 17, 2012
    Publication date: February 21, 2013
    Inventors: Romain Adelin Lefebvre, Joris Herman De Maeyer
  • Publication number: 20130035323
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: August 3, 2012
    Publication date: February 7, 2013
    Applicant: Abbott GmbH & Co. KG
    Inventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
  • Publication number: 20130018030
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: January 20, 2012
    Publication date: January 17, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Bernd NOSSE
  • Publication number: 20120328661
    Abstract: The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: October 20, 2010
    Publication date: December 27, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Todd M. Heidelbaugh, John R. Cappiello, Phong X. Nguyen, Dario G. Gomez
  • Publication number: 20120329832
    Abstract: This invention relates to novel coumarin derivative, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
  • Patent number: 8338416
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: December 25, 2012
    Assignee: Pharmacylics, Inc.
    Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
  • Publication number: 20120322784
    Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: December 16, 2011
    Publication date: December 20, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
  • Patent number: 8334304
    Abstract: The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine of said compounds.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: December 18, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Paul Rene Marie Andre Bosmans, Henricus Jacobus Maria Gijsen, Laurence Anne Mevellec
  • Publication number: 20120302539
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 29, 2012
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
  • Patent number: 8318742
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: November 27, 2012
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef DeCleyn, Michel Surkyn
  • Publication number: 20120283254
    Abstract: The present invention is concerned with novel selective dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein R1, R2, R3, n, and Y are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Application
    Filed: April 27, 2012
    Publication date: November 8, 2012
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Publication number: 20120270736
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Application
    Filed: June 30, 2011
    Publication date: October 25, 2012
    Applicant: Lixte Biotechnology, Inc.
    Inventors: John S. Kovach, Francis Johnson
  • Publication number: 20120269901
    Abstract: The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.
    Type: Application
    Filed: December 19, 2011
    Publication date: October 25, 2012
    Applicant: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
    Inventors: John C. Reed, Maurizio Pellecchia
  • Patent number: 8293765
    Abstract: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: October 23, 2012
    Assignee: Novartis AG
    Inventors: Dierk Wieckhusen, Alexandra Glausch, Markus Ahlheim
  • Publication number: 20120263790
    Abstract: Disclosed is a method of treating small intestinal bacterial overgrowth (SIBO) or a SIBO-caused condition in a human subject. SIBO-caused conditions include irritable bowel syndrome, fibromyalgia, chronic pelvic pain syndrome, chronic fatigue syndrome, depression, impaired mentation, impaired memory, halitosis, tinnitus, sugar craving, autism, attention deficit/hyperactivity disorder, drug sensitivity, an autoimmune disease, and Crohn's disease. Also disclosed are a method of screening for the abnormally likely presence of SIBO in a human subject and a method of detecting SIBO in a human subject. A method of determining the relative severity of SIBO or a SIBO-caused condition in a human subject, in whom small intestinal bacterial overgrowth (SIBO) has been detected, is also disclosed.
    Type: Application
    Filed: December 9, 2011
    Publication date: October 18, 2012
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Henry C. Lin, Mark Pimentel
  • Publication number: 20120252745
    Abstract: The disclosure provides novobiocin analogues with noviose replacements which are useful as Hsp90 inhibitors in the treatment of cancer.
    Type: Application
    Filed: February 19, 2010
    Publication date: October 4, 2012
    Inventors: Brian S. J. Blagg, Huiping Zhao, Alison Catherine Donnelly
  • Publication number: 20120245165
    Abstract: The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder.
    Type: Application
    Filed: June 5, 2012
    Publication date: September 27, 2012
    Applicants: DAEWOONG PHARMACEUTICAL CO., LTD, MEDIFRON DBT CO., LTD.
    Inventors: Dong Wook KANG, Jee Woo LEE, Young Ho KIM, Hee KIM, Hee Jin HA, Eun Joo NAM, Chan Mi JOUNG
  • Publication number: 20120237591
    Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.
    Type: Application
    Filed: May 8, 2012
    Publication date: September 20, 2012
    Applicant: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20120220630
    Abstract: The present invention is concerned with an oral aqueous solution comprising prucalopride or pharmaceutically acceptable acid addition salts thereof having good organoleptic properties.
    Type: Application
    Filed: February 28, 2012
    Publication date: August 30, 2012
    Inventor: Roger Carolus Augusta Embrechts
  • Patent number: 8247562
    Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by histone deacetylase.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: August 21, 2012
    Assignee: Astrazeneca AB
    Inventors: Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
  • Patent number: 8242138
    Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: August 14, 2012
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu
  • Patent number: 8242115
    Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: August 14, 2012
    Assignee: Luitpold Pharmaceuticals, Inc.
    Inventors: James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G. Schiro, Hongmei Huang, Michael Evans, Yongxin Han
  • Publication number: 20120201749
    Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C?O or —C?O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR2, OR1, CN or CO2R; Z1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.
    Type: Application
    Filed: August 25, 2010
    Publication date: August 9, 2012
    Inventors: Melanie Jayne Crawshaw, Philip Spencer Fallon, Ashley Nicholas Jarvis, Jonathan Raymond Powell, Natalie Louise Winfield, David Selwood, Ian Charles Zachary, Haiyan Jia
  • Publication number: 20120202738
    Abstract: There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhoea, chronic idiopathic nausea, IBD-associated constipation and diarrhoea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the composition comprising: (i) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (ii) at least one anti-clostridial agent selected from the above combined with an opioid blocking agent.
    Type: Application
    Filed: October 22, 2010
    Publication date: August 9, 2012
    Inventor: Thomas Julius Borody
  • Patent number: 8236820
    Abstract: Compounds of the general formula are disclosed with activity towards treating diseases related to inflammation, such as cancer, neurodegenerative and cardiovascular diseases. Pharmaceutical compositions and methods of use are also described.
    Type: Grant
    Filed: August 11, 2008
    Date of Patent: August 7, 2012
    Inventor: Basil Rigas
  • Patent number: 8232405
    Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.
    Type: Grant
    Filed: January 20, 2011
    Date of Patent: July 31, 2012
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Tomohiro Toyoda, Hidefumi Yoshinaga
  • Patent number: 8232295
    Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: July 31, 2012
    Assignee: Heartdrug Research, L.L.C.
    Inventor: Victor L. Serebruany
  • Patent number: 8227488
    Abstract: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: July 24, 2012
    Assignee: Novartis AG
    Inventors: Dierk Wieckhusen, Alexandra Glausch, Markus Ahlheim
  • Patent number: 8222255
    Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: July 17, 2012
    Assignees: Merck Sharp & Dohme Corp., Scynexis, Inc.
    Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, legal representative, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
  • Publication number: 20120178735
    Abstract: Provided is a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action. The 2H-chromene compound or derivative is particularly useful for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.
    Type: Application
    Filed: February 15, 2012
    Publication date: July 12, 2012
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Sunao Imada, Tatsuaki Morokata