Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/326.5)
  • Patent number: 10710966
    Abstract: The present disclosure relates to: a) solid state forms of hydrobromide salts of Compound 1; b) pharmaceutical compositions comprising one or more solid state forms of hydrobromide salts of Compound 1, and, optionally, a pharmaceutically acceptable carrier; c) methods of treating tumors or cancers by administering one or more solid state forms of hydrobromide salts of Compound 1 to a subject in need thereof; and d) methods for the preparation of solid state forms of Compound 1.
    Type: Grant
    Filed: March 13, 2020
    Date of Patent: July 14, 2020
    Assignee: Pfizer Inc.
    Inventors: Elaine Greer, Stephen Anderson, Mark Maloney, Shu Yu, Ekaterina Albert, Emily Rigsbee
  • Patent number: 10590087
    Abstract: The present disclosure relates to: a) solid state forms of hydrobromide salts of Compound 1; b) pharmaceutical compositions comprising one or more solid state forms of hydrobromide salts of Compound 1, and, optionally, a pharmaceutically acceptable carrier; c) methods of treating tumors or cancers by administering one or more solid state forms of hydrobromide salts of Compound 1 to a subject in need thereof; and d) methods for the preparation of solid state forms of Compound 1.
    Type: Grant
    Filed: August 9, 2019
    Date of Patent: March 17, 2020
    Assignee: Pfizer Inc.
    Inventors: Elaine Greer, Stephen Anderson, Mark Maloney, Shu Yu, Ekaterina Albert, Emily Rigsbee
  • Patent number: 8980932
    Abstract: The present invention concerns novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety and their use in therapy of hypoxic conditions, in particular cancer treatment, especially chemotherapy and radiotherapy. The compounds of the invention have an increased specificity for the carbonic anhydrase IX enzyme compared to the art. The present invention relates to novel nitroimidazole derivates represented by formula (1).
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: March 17, 2015
    Assignees: Stichting Maastricht Radiation Oncology “Maastro-Clinic”, Université Montpellier 2 Sciences et Techniques
    Inventors: Philippe Lambin, Jean-Yves Winum, Claudiu Supuran
  • Patent number: 8921406
    Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.
    Type: Grant
    Filed: August 21, 2006
    Date of Patent: December 30, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Alfred Hahn
  • Publication number: 20140329871
    Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.
    Type: Application
    Filed: December 2, 2012
    Publication date: November 6, 2014
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 8835480
    Abstract: The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: September 16, 2014
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Nicholas G. Nickols
  • Patent number: 8815910
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Patent number: 8815923
    Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: August 26, 2014
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
  • Publication number: 20140194473
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 10, 2013
    Publication date: July 10, 2014
    Applicant: E I Du Pont De Nemours And Company
    Inventor: THOMAS FRANCIS PAHUTSKI, JR.
  • Patent number: 8716471
    Abstract: The present invention provides a process for the preparation of a tetrazine derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein R1 represents a hydrogen atom, a straight or branched C1-C6 alkyl group, C2-C6 alkenyl group or C2-C6 alkynyl group, which C1-C6 alkyl group, C2-C6 alkenyl group and C2-C6 alkynyl group is unsubstituted or substituted with 1, 2 or 3 substituents selected from halogen atoms, straight or branched C1-C4 alkoxy groups, C1-C4 alkylthio groups, C1-C4 alkylsulphinyl groups, C1-C4 alkylsulphonyl groups and phenyl groups, which phenyl groups are unsubstituted or substituted with one or more substituents selected from C1-C4 alkyl groups, C1-C4 alkoxy groups and nitro groups; or R1 represents a C3-C8 cycloalkyl group; and R2 represents a group of formula —(C?O)NR3R4, wherein R3 and R4 are independently selected from hydrogen atoms, C1-C4 alkyl groups, C2-C4 alkenyl groups and C3-C8 cycloalkyl groups, which process comprises: i) providing a compound N of formula (III
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: May 6, 2014
    Assignee: Reliance Life Sciences Pvt. Ltd.
    Inventors: Gupte Rajan, Chaturvedi Rohit, Baviskar Pravin
  • Publication number: 20130331413
    Abstract: Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Erik DE LEEUW, Alexander D. MACKERELL, JR.
  • Publication number: 20130274305
    Abstract: The present invention concerns novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety and their use in therapy of hypoxic conditions, in particular cancer treatment, especially chemotherapy and radiotherapy. The compounds of the invention have an increased specificity for the carbonic anhydrase IX enzyme compared to the art. The present invention relates to novel nitroimidazole derivates represented by formula (1).
    Type: Application
    Filed: December 21, 2011
    Publication date: October 17, 2013
    Applicants: STICHTING MAASTRICHT RADIATION ONCOLOGY "MAASTRO-CLINIC", CNRS CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Philippe Lambin, Jean-Yves Winum, Claudiu Supuran
  • Patent number: 8492387
    Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: July 23, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
  • Patent number: 8476455
    Abstract: The invention relates to the compounds of formula (I): in which R1, R2, R3, R4, Q and Z are as defined in the specification. The invention also relates to the pharmaceutical compositions containing these compounds.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: July 2, 2013
    Assignee: Laboratoire Theramex
    Inventors: Jean Lafay, Benoit Rondot, Paule Bonnet, Thierry Clerc, Jacqueline Shields, Igor Duc, Eric Duranti, Francois Puccio, Christian Blot, Philippe Maillos
  • Patent number: 8436027
    Abstract: This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. This invention also refers to a pharmaceutical composition comprising at least one of the azole compounds represented by the general formula VIII, to the use of such compositions and to methods of treatment or inhibition of tuberculosis and leishmaniasis.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: May 7, 2013
    Assignee: Fundacão Oswaldo Cruz—FIOCRUZ
    Inventors: Nubia Boechat, Marilia dos Santos Costa, Maria Cristina da Silva Lourenço, Ivan Neves, Jr., Marcelo da Silva Genestra, Vitor Francisco Ferreira
  • Patent number: 8426454
    Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: April 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
  • Patent number: 8420684
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(he
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: April 16, 2013
    Assignee: Probiodrug AG
    Inventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
  • Patent number: 8399501
    Abstract: The invention provides a micronized 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid having improved stability. The invention also provides pharmaceutical compositions comprising the stable micronized compound, processes for preparing the stable micronized compound, and methods of using the stable micronized compound to treat diseases such as hypertension.
    Type: Grant
    Filed: March 3, 2011
    Date of Patent: March 19, 2013
    Assignee: Theravance, Inc.
    Inventor: Paul R. Fatheree
  • Patent number: 8399463
    Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: March 19, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 8357710
    Abstract: There is provided a compound of formula I, wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: January 22, 2013
    Assignee: Vicore Pharma AB
    Inventors: Mathias Alterman, Anders Hallberg, Murugaiah Andappan Murugaiah Subbaiah
  • Publication number: 20120309673
    Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
    Type: Application
    Filed: December 10, 2010
    Publication date: December 6, 2012
    Applicant: Medivir UK Ltd
    Inventors: Susana Ayesa, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jönsson, Pia Kahnberg, Björn Klasson, Peter Lind, Stina Lundgren, Lourdes Odén, Kevin Parkes, Daniel Wiktelius
  • Publication number: 20120295910
    Abstract: The present invention relates to new sulfonamide derivatives of formula (I), wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: August 1, 2012
    Publication date: November 22, 2012
    Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
  • Patent number: 8273899
    Abstract: A method for producing N-(2-amino-1,2-dicyanovinyl)imidates represented by the following formula (1-III) under low temperature conditions within a short period of time in high yield is provided. In addition, a method for producing N-(2-amino-1,2-dicyanovinyl)formamidine represented by the following formula (2-II) which is suitably applicable to a cyclization reaction for producing AICN, AICA or the like and which enhances yield of the cyclization reaction is provided. In addition, a method for producing aminoimidazole derivatives represented by the following formula (3-V) in high yield by using diaminomaleonitrile as a starting material is provided.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: September 25, 2012
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Mitsuru Takase, Fuminori Komatsu
  • Patent number: 8258294
    Abstract: A process for the preparation of compounds of formula IA, where R?CH3 (i.e. temozolomide): comprising diazotizing a compound of the formula IIA: where in R is as defined above in the presence of at least one metal halide, an acid and a source of nitrous acid, followed by conversion of acidic solution containing temozolomide. The conversion can be carried out by a liquid-liquid extraction technique in a water immiscible solvent. The temozolomide may be further purified in an acetone-water mixture.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: September 4, 2012
    Assignee: CIPLA Limited
    Inventors: Srinivas Laxminarayan Pathi, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
  • Patent number: 8252831
    Abstract: The present invention provides compounds of the formula below or pharmaceutical salts thereof, wherein R1, R2 and R3 are as described herein; methods of treating osteoarthritis using the compounds; and a process for preparing the compounds.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: August 28, 2012
    Assignee: Eli Lilly and Company
    Inventors: Steven Lee Kuklish, Matthew Allen Schiffler, Jeremy Schulenburg York
  • Patent number: 8232392
    Abstract: Described is a new process for producing temozolomide, comprising the reaction between 5-aminoimidazole-4-carboxamide and N-succinimidyl-N?-methyl carbamate and the subsequent reaction of the thus obtained carbamoyl 5-aminoimidazole-4-carboxamide with sodium nitrite. Temozolomide is then purified by chromatography on adsorbent polymeric resin and subsequent crystallization from water and acetone.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: July 31, 2012
    Assignee: Chemi S.p.A.
    Inventors: Stefano Turchetta, Lorenzo De Ferra, Maurizio Zenoni, Mauro Anibaldi
  • Patent number: 8232428
    Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: July 31, 2012
    Assignee: PolyMedix,Inc.
    Inventors: Shaker Mousa, Dahui Liu
  • Publication number: 20120130083
    Abstract: A method for producing N-(2-amino-1,2-dicyanovinyl)imidates represented by the following formula (1-III) under low temperature conditions within a short period of time in high yield is provided. In addition, a method for producing N-(2-amino-1,2-dicyanovinyl)formamidine represented by the following formula (2-II) which is suitably applicable to a cyclization reaction for producing AlCN, AlCA or the like and which enhances yield of the cyclization reaction is provided. In addition, a method for producing aminoimidazole derivatives represented by the following formula (3-V) in high yield by using diaminomaleonitrile as a starting material is provided.
    Type: Application
    Filed: January 31, 2012
    Publication date: May 24, 2012
    Applicant: NIPPON SODA CO., LTD.
    Inventors: Mitsuru TAKASE, Fuminori KOMATSU
  • Patent number: 8168802
    Abstract: Methods and intermediates useful for making compounds of the formula: and the preparation of compounds of Formula I, preferably including the formation of intermediate compounds of the formula:
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: May 1, 2012
    Assignee: 3M Innovative Properties Company
    Inventors: David S. Hays, Sonja S. Mackey, William H. Moser, Doris D. Stoermer, Matthew R. Radmer, Shri Niwas
  • Patent number: 8163790
    Abstract: Cocrystals of metronidazole are described herein. Such cocrystals are a cocrystal of metronidazole with gentisic acid and a cocrystal of metronidazole with gallic acid. Cocrystals of imipramine hydrochloride are also described. Such cocrystals are a cocrystal of imipramine hydrochloride with (+)-camphoric acid, a cocrystal of imipramine hydrochloride with fumaric acid, and a cocrystal of imipramine hydrochloride with 1-hydroxy-2-naphthoic acid.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: April 24, 2012
    Assignee: New Form Pharmaceuticals, Inc.
    Inventor: Scott Lawrence Childs
  • Publication number: 20120095047
    Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.
    Type: Application
    Filed: December 22, 2011
    Publication date: April 19, 2012
    Applicant: UNIVERSITY OF CONNECTICUT
    Inventors: Alexandros Makriyannis, Rajesh Thotapally, Venkata Kiran Rao Vemuri, Teresa Olszewska
  • Patent number: 8133911
    Abstract: The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: March 13, 2012
    Assignee: Dompe S.p.A
    Inventors: Alessio Moriconi, Andrea Aramini
  • Publication number: 20120004230
    Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.
    Type: Application
    Filed: September 19, 2011
    Publication date: January 5, 2012
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 8053435
    Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: November 8, 2011
    Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.
    Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
  • Publication number: 20110269803
    Abstract: This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII.
    Type: Application
    Filed: December 29, 2010
    Publication date: November 3, 2011
    Applicant: Fundacao Oswaldo Cruz - FIOCRUZ
    Inventors: Nubia Boechat, Marilia dos Santos Costa, Maria Cristina da Silva Lourenco, Ivan Neves, JR., Marcelo da Silva Genestra, Vitor Francisco Ferreira
  • Publication number: 20110269965
    Abstract: Methods and intermediates useful for making compounds of the formula: and the preparation of compounds of Formula I, preferably including the formation of intermediate compounds of the formula:
    Type: Application
    Filed: March 31, 2006
    Publication date: November 3, 2011
    Applicant: Coley Pharmaceutical Group, Inc.
    Inventors: David S. Hays, Sonja S. Mackey, William H. Moser, Doris D. Stoermer, Matthew R. Radmer, Shri Niwas
  • Publication number: 20110263553
    Abstract: Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.
    Type: Application
    Filed: February 26, 2009
    Publication date: October 27, 2011
    Inventors: Christopher Macnevin, Donald G. Stein, Dennis C. Liotta, Iqbal Sayeed, David B. Guthrie, Mark A. Lockwood, Michael G. Natchus
  • Patent number: 7951958
    Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: May 31, 2011
    Assignee: Pfizer Inc.
    Inventors: Michael A. Brodney, Karen J. Coffman
  • Publication number: 20110118199
    Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.
    Type: Application
    Filed: January 11, 2007
    Publication date: May 19, 2011
    Inventor: Matthias Dormeyer
  • Patent number: 7943625
    Abstract: The present invention relates to a compound according to Formula (I) wherein R1 is selected from C1-C6 alkyl, and said C1-C6 alkyl is substituted with C1-C6 alkoxy; and at least one of said C1-C6 alkyl or said C1-C6 alkoxy is branched; or a pharmaceutically acceptable salt thereof, solvate or solvate of a salt thereof, as well as, to compositions containing at least one compound according to Formula (I) and methods of treating at least one disease or condition therewith.
    Type: Grant
    Filed: June 1, 2007
    Date of Patent: May 17, 2011
    Assignee: AstraZeneca AB
    Inventor: Anna-Karin Tidén
  • Publication number: 20110034483
    Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: February 18, 2009
    Publication date: February 10, 2011
    Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
  • Patent number: 7871960
    Abstract: The present invention relates to 1-(imidazolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and their agriculturally acceptable salts, wherein A is a radical of the formula A1 or A2. The invention relates also to agricultural compositions and to seed comprising at least one compound I and/or a salt thereof, as well as a method of combating animal pests, a method for protecting crops from attack or infestation by animal pests and a method for protecting non-living materials from attack or infestation by animal pests, a method for the protection of seeds from animal pests and of the seedlings' roots and shoots from animal pests by applying a pesticidally effective amount of at least one 1-(imidazolin-2-yl)amino-1,2-diphenylethane compound I and/or a salt thereof.
    Type: Grant
    Filed: May 18, 2006
    Date of Patent: January 18, 2011
    Assignee: BASF SE
    Inventors: Markus Kordes, Norbert Götz, Michael Rack, Christopher Koradin, Livio Tedeschi, Deborah L. Culbertson
  • Publication number: 20100292274
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: May 11, 2010
    Publication date: November 18, 2010
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 7816389
    Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.
    Type: Grant
    Filed: January 11, 2007
    Date of Patent: October 19, 2010
    Assignee: Nabriva Therapeutics Forschungs GmbH
    Inventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
  • Publication number: 20100249132
    Abstract: Compounds of the formula (I), in which R1, D, E, L, Q, X and q have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.
    Type: Application
    Filed: September 9, 2008
    Publication date: September 30, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Melanie Schultz, Kai Schiemann, Gerard Botton, Andree Blaukat, Ingo Kober
  • Patent number: 7795447
    Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: September 14, 2010
    Assignee: Pfizer Inc
    Inventors: Michael A. Brodney, Karen J. Coffman
  • Patent number: 7767704
    Abstract: The invention relates to the substituted imidazoles of formula (I) and to methods for producing the same, to their use in the treatment and/or prophylaxis of diseases and to their use for producing drugs for use in the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, especially against cytomegaloviruses.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: August 3, 2010
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Holger Zimmermann, David Brueckner, Dirk Heimbach, Martin Hendrix, Kerstin Henninger, Guy Hewlett, Ulrich Rosentreter, Joerg Keldenich, Dieter Lang, Martin Radtke
  • Publication number: 20100184737
    Abstract: The present invention relates to compounds of Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of Formula I.
    Type: Application
    Filed: March 12, 2010
    Publication date: July 22, 2010
    Applicant: Pfizer Inc
    Inventors: Michael A. Brodney, Karen J. Coffman, Edward F. Kleinman, Brian T. O'Neill, Yuhpyng L. Chen
  • Publication number: 20100168107
    Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.
    Type: Application
    Filed: March 12, 2010
    Publication date: July 1, 2010
    Applicant: Pfizer Inc
    Inventors: Michael A. Brodney, Karen J. Coffman