N-c(=x)-n, N-c(=n)n, N-n, Nitrogen Directly Bonded To Oxygen By Nonionic Bonding Or Cyano Containing Patents (Class 514/482)
  • Patent number: 9486538
    Abstract: The present invention is related to uses of a composition comprising a pharmaceutically active component and a compound according to formula (I), wherein R1 and R2 are each and independently selected from the group comprising alkyl; n is any integer between 1 and 4; R3 is an acyl selected from the group comprising lysyl, ornithyl, 2,4-diaminobutyryl, histidyl and an acyl moiety according to formula (II), wherein m is any integer from 1 to 3 and Y? is a pharmaceutically acceptable anion.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: November 8, 2016
    Assignee: SILENCE THERAPEUTICS GMBH
    Inventors: Oliver Keil, Jörg Kaufmann, Ansgar Santel
  • Patent number: 9371276
    Abstract: The invention relates to the compounds and compositions of Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprises a salt of metformin and the methods for treating or preventing metabolic syndrome, prediabetes and diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes mellitus, obesity, lipid disorders, hypertriglyceridemia, hyperglycemia, hyperinsulinemia and insulin resistance.
    Type: Grant
    Filed: November 11, 2015
    Date of Patent: June 21, 2016
    Inventor: Mohan Murali Alapati
  • Publication number: 20150133509
    Abstract: The present invention provides a tree trunk injection agent whereby pathogenic fungi and/or pests in trees can be effectively controlled merely by a short-time application in a low chemical dose, and a method for controlling tree diseases using the tree trunk injection agent. According to one embodiment of the present invention, the tree trunk injection agent is obtained by adding, to an aqueous solution of an insecticidal component such as acetamiprid, a hardly soluble fungicidal component such as thiophanate-methyl so as to suspend the hardly soluble fungicidal component, wherein a particle size based on 50% volume of the fungicidal component is 4 ?m or less, or adding thereto at least one fungicidal component selected from a group consisting of triflumizole and metconazole.
    Type: Application
    Filed: April 30, 2013
    Publication date: May 14, 2015
    Applicant: NIPPON SODA CO., LTD.
    Inventors: Takahiro Maekawa, Yasuhiro Omori
  • Publication number: 20150099636
    Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 9, 2015
    Inventors: Robert Eugene HORMANN, Bing Li
  • Patent number: 8962672
    Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, AND G have the meanings given in the disclosure, and (b) the active compounds (1) to (29) listed in the disclosure.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: February 24, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Patent number: 8858991
    Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: October 14, 2014
    Assignee: Pathologica LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 8765811
    Abstract: Provided herein are tri-salt compounds comprising a compound having two acidic functional groups and one basic functional groups (e.g., aspartate or glutamate), metformin, and polyunsaturated fatty acids, such as eicosapentaenoate or docosahexaenoate. The salts can be used in the treatment of diabetes, diabetes with concomitant dyslipidemia (e.g., high triglycerides) and diabetes exacerbated cardiovascular complications, such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke. The compounds of this invention are also useful in treating obesity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 1, 2014
    Assignee: Thetis Pharmaceuticals LLC
    Inventors: Banavara L. Mylari, Frank C. Sciavolino
  • Patent number: 8728442
    Abstract: The present invention relates to novel compounds and compositions and the use of them for the control of fungal and bacterial pathogens, insect pests, acari, nematodes and other invertebrate pests including, but not limited to post-harvest and soil diseases, building mold remediation, and seed and grain sanitation.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: May 20, 2014
    Assignee: Bayer CropScience LP
    Inventors: Jorge I. Jimenez, Jonathan S. Margolis, John Kenneth Baird, Sarah F. Lego
  • Patent number: 8637058
    Abstract: Composition for controlling phytopathogens comprising compound of the formula: wherein: R1 represents H, or a CO—R? acyl group; R2, the same or different when n is equal to 2, is a halogen, optionally selected from fluorine, chlorine, bromine or iodine; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C1-C9 thioalkyl group; a C1-C9 halothioalkyl group; a C3-C9 cycloalkyl group; a C2-C10 carboalkoxyl group; a cyano group; a hydroxyl group; R? represents a hydrogen; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C2-C10 carboalkoxyl group; a phenyl group; n is a number ranging from 0 to 2; X represents an oxygen atom, a nitrogen or sulfur atom in combination with a fungicide; method for controlling phytopathogens with compound of formula (1) with or without another fungicide.
    Type: Grant
    Filed: November 18, 2002
    Date of Patent: January 28, 2014
    Assignee: Isagro S.p.A.
    Inventors: Lucio Filippini, Marilena Gusmeroli, Alexia Elmini, Carlo Garavaglia, Luigi Mirenna
  • Publication number: 20140018419
    Abstract: Provided herein are tri-salt compounds comprising a compound having two acidic functional groups and one basic functional groups (e.g., aspartate or glutamate), metformin, and polyunsaturated fatty acids, such as eicosapentaenoate or docosahexaenoate. The salts can be used in the treatment of diabetes, diabetes with concomitant dyslipidemia (e.g., high triglycerides) and diabetes exacerbated cardiovascular complications, such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke. The compounds of this invention are also useful in treating obesity.
    Type: Application
    Filed: March 15, 2013
    Publication date: January 16, 2014
    Applicant: Thetis Pharmaceuticals LLC
    Inventors: Banavara L. MYLARI, Frank C. SCIAVOLINO
  • Publication number: 20130338165
    Abstract: Methods of treating Parkinson's Disease comprising administering compounds that up-regulate cystine-glutamate exchange (system Xc?) and/or increase glutathione levels in the brain cells. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.
    Type: Application
    Filed: June 17, 2013
    Publication date: December 19, 2013
    Inventors: David A. Baker, Daniel G. Lawton, Chad Beyer, Michael Neary
  • Patent number: 8609720
    Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: December 17, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
  • Patent number: 8597876
    Abstract: Disclosed is a method of treating human immunodeficiency virus (HIV) infection in an antiretroviral treatment-experienced mammal, which involves administering to the mammal an effective amount of a compound of the formula: or a pharmaceutically acceptable salt, a prodrug, or an ester thereof, or a pharmaceutically acceptable composition of the compound, the salt, the prodrug, or the ester thereof, wherein A, X, Q, W, m, and R2-R6 are as defined herein.
    Type: Grant
    Filed: October 11, 2007
    Date of Patent: December 3, 2013
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Board of Trustees of the University of Illinois
    Inventors: John W. Erickson, Sergei V. Gulnik, Hiroaki Mitsuya, Arun K. Ghosh
  • Publication number: 20130190278
    Abstract: The present invention relates to the use of the compounds of formula (I) and their pharmaceutically acceptable salts for the treatment or the prevention of ocular inflammatory diseases, in particular for the treatment and/or prevention of uveitis, severe conjunctivitis, dry eye syndrome or diabetic retinopathy.
    Type: Application
    Filed: July 8, 2011
    Publication date: July 25, 2013
    Applicant: Laboratoires Fournier SA
    Inventors: Jocelyne Annat, Hélène-Céline Huguet, Olivier Lacombe, Luc Lebreton
  • Publication number: 20130090379
    Abstract: A method of providing a patient with controlled release of tapentadol using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing tapentadol is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of tapentadol from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
    Type: Application
    Filed: October 14, 2010
    Publication date: April 11, 2013
    Applicant: SIGNATURE THERAPEUTICS, INC.
    Inventors: Thomas E. Jenkins, Julie D. Seroogy, Jonathan W. Wray
  • Patent number: 8410168
    Abstract: Compounds that cause reversible night blindness may be used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods and compositions using such compounds and their derivatives to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions. Such compounds and their derivatives may be used as single agent therapy or in combination with other agents or therapies.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: April 2, 2013
    Assignee: Acucela, Inc.
    Inventors: Kenneth Widder, Jay Lichter, Nathan L. Mata
  • Publication number: 20120178666
    Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 12, 2012
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Robert G. Tyson, Bernard T. Golding, Rhys Whomsley
  • Publication number: 20120178805
    Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.
    Type: Application
    Filed: March 13, 2012
    Publication date: July 12, 2012
    Inventor: Yousef Al-Abed
  • Publication number: 20120065152
    Abstract: Prodrugs of guanfacine, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for improving the pharmacokinetics of guanfacine or minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration are provided herein.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 15, 2012
    Applicant: SHIRE LLC
    Inventors: Rhys Whomsley, Bernard T. Golding, Robert G. Tyson
  • Publication number: 20120014884
    Abstract: The present invention discloses novel uses of specific menthol-derivative compounds of Formula 1, and compositions thereof, for methods of providing oral and systemic health care benefits, and methods of up-regulating or down-regulating periodontal disease metabolites: Formula 1 wherein, X is an oxygen atom or an NH radical; and R is an unsubstituted or substituted aryl or aliphatic radical. In some embodiments, the oral and systemic health care benefits include biofilm anti-attachment, anti-inflammation, anti-oxidant, anti-bone loss, and anti-microbial benefits. In some embodiments, the periodontal disease metabolites correspond to healthy and/or diseased oral status and allow differential diagnosis of oral health.
    Type: Application
    Filed: April 1, 2009
    Publication date: January 19, 2012
    Applicant: Colgate-Palmolive Company
    Inventors: Harsh M. Trivedi, Tao Xu, Davide Miksa, Cortney Worrell, Chanda Macias, Ying Yang, Yanan Hu
  • Publication number: 20110305632
    Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).
    Type: Application
    Filed: December 11, 2009
    Publication date: December 15, 2011
    Applicant: THE UNIVERSITY OF MELBOURNE
    Inventors: Paul Stephen Donnelly, Brett Michael Paterson
  • Publication number: 20110218102
    Abstract: A water-dispersible particle is provided that includes organic origin potash in an amount ranging from 5% to 99.9% by weight of the total dry weight of the particle. A binder component is present in an amount from 1% to 95% by weight. The organic origin potash and the binder component on that contact with water causes particle dispersion into more than 100 pieces. A process for making a water-dispersible particle includes mechanical aggregation of the potash into a pellet. A binder component is present in the particle in an amount ranging from 1% to 95% by weight. The potash and the binder component are present in a form such that contact with water causes particle dispersion into more than 100 pieces. The pellet is then dried and ready to be applied.
    Type: Application
    Filed: September 7, 2010
    Publication date: September 8, 2011
    Applicant: The Andersons, Inc.
    Inventors: Charles W. Anderson, Timothy D. Birthisel
  • Publication number: 20110104057
    Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.
    Type: Application
    Filed: May 13, 2009
    Publication date: May 5, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Ludger Dinkelborg, Keith Graham, Mathias Berndt, Norman Koglin, Heribert Schmitt-Willich, Matthias Friebe, Lutz Lehmann
  • Publication number: 20110039705
    Abstract: A method of producing a granular agrochemical composition having excellent handling properties, wherein a powdered agrochemical wettable composition or powdered agrochemical water-soluble composition is converted in form to a granular agrochemical composition, without altering the formulation thereof. The method of producing a granular agrochemical composition includes: treating a powdered agrochemical wettable composition or powdered agrochemical water-soluble composition by (1) a step of adding water, kneading, extruding and drying, (2) a step of adding water, granulating by stirring and drying, (3) a step of adding water, kneading and spray-drying, (4) a step of adding water and performing fluidized bed granulation, or (5) a step of pressure molding the powdered agrochemical wettable composition or powdered agrochemical water-soluble composition; followed by (a) a step of performing microgranulation by grinding, and if necessary, (b) a step of performing grain size regulation by sieving.
    Type: Application
    Filed: April 23, 2009
    Publication date: February 17, 2011
    Inventors: Yoshihisa Endo, Satoru Yamamura
  • Publication number: 20100249165
    Abstract: This invention relates to compounds useful as PDZ domain modulators, in particular the PDZ domain of PICK1. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions.
    Type: Application
    Filed: June 3, 2008
    Publication date: September 30, 2010
    Applicants: University of Copenhagen, NeuroSearch A/S
    Inventors: Ulrik Gether, Kenneth Madsen, Thor Seneca Thorsen, Dan Peters, Tino Dyhring, Lars Christian Rønn
  • Publication number: 20100035930
    Abstract: The invention relates to compounds of the formula I as defined herein, which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. The compounds of the formula I are suitable for manufacturing medicaments for the prophylaxis, secondary prevention and therapy of one or more disorders which are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: June 8, 2009
    Publication date: February 11, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Christopher KALLUS, Mark BROENSTRUP, Werngard CZECHTIZKY, Andreas EVERS, Markus FOLLMANN, Nis HALLAND, Herman SCHREUDER
  • Publication number: 20090318481
    Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.
    Type: Application
    Filed: August 28, 2009
    Publication date: December 24, 2009
    Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
  • Patent number: 7566738
    Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions of 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, methods of using prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: July 28, 2009
    Assignee: XenoPort, Inc.
    Inventor: Mark A. Gallop
  • Publication number: 20080287535
    Abstract: Pesticidal compounds having the structural formula wherein: R2 is C1-C6 branched or straight chain alkyl; C1-C4 branched or straight-chain haloalkyl; or C3-C6 cycloalkyl; m is 0, 1, or 2; X is selected from the group consisting of: C1-C6 branched or straight-chain alkoxy; halogen; C1-C6 branched or straight-chain alkyl; or C1-C6 branched or straight-chain alkylthio; n is 0 or 1; A is 0; CH2; or NR?, wherein R? is (C1-C6 alkyl)carbonyl; Y is phenyl; benzyl; thiazolyl; thienyl; pyridyl; or tetrahydrofuranyl, the aromatic ring of each substituent being optionally substituted with one or more of halogen, C1-C6 branched or straight-chain alkyl, or C1-C6 branched or straight-chain haloalkyl; use of the compounds as pesticides and pesticidal compositions comprising the compounds.
    Type: Application
    Filed: February 20, 2008
    Publication date: November 20, 2008
    Inventors: Mark A. Dekeyser, Paul T. McDonald
  • Publication number: 20080139505
    Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.
    Type: Application
    Filed: November 15, 2005
    Publication date: June 12, 2008
    Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
  • Patent number: 7192965
    Abstract: Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1–C6alkylene bridge; A4 is a C1–C6alkylene bridge; D is CH or N; W is, for example, O, NR7 or S; T is, for example, a bond, O, NH or NR7; Q is O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, CN, nitro, C1–C6alkyl, C1–C6haloalkyl, C1–C6alkylcarbonyl or C2–C6alkenyl; R4 is, for example, H, halogen, CN, nitro or C1–C6alkyl; R5 and R6 are, for example, H, CN, OH, C1–C6alkyl, C3–C8cycloalkyl, C3–C8cycloalkyl-C1–C6alkyl, C1–C6haloalkyl, C1–C6alkoxy or C1–C6haloalkoxy; R7 is H, C1–C6alkyl, C1–C6alkoxyalkyl or C1–C6alkylcarbonyl; k, when D is nitrogen, is 1, 2 or 3; or, when D is CH, is 1, 2, 3 or 4; and m is 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds and
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: March 20, 2007
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Werner Zambach, Peter Renold, Arthur Steiger, Stephan Trah, Roger Graham Hall
  • Patent number: 7135498
    Abstract: There is provided a method of promoting neurogenesis by administering a therapeutic amount of a nitric oxide donor compound to a patient in need of neurogenesis promotion. Also provided is a compound for providing neurogenesis having an effective amount of a nitric oxide donor sufficient to promote neurogenesis. A nitric oxide compound for promoting neurogenesis is also provided. Further, a method of augmenting the production of brain cells and facilitating cellular structural and receptor changes by administering an effective amount of a nitric oxide donor compound to a site in need of augmentation is provided. There is provided method of increasing both neurological and cognitive function by administering an effective amount of a nitric oxide donor compound to a patient.
    Type: Grant
    Filed: June 14, 2000
    Date of Patent: November 14, 2006
    Assignee: Henry Ford Health System
    Inventors: Michael Chopp, Rui Lan Zhang
  • Patent number: 7030157
    Abstract: The present invention relates to pharmaceutical compositions, kits and methods comprising combinations of (?)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or nontoxic pharmacologically acceptable acid addition salts thereof and estrogens. The present invention also relates to pharmaceutical compositions, kits and methods comprising combinations of (?)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or nontoxic pharmacologically acceptable acid addition salts thereof, estrogens and progestins.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: April 18, 2006
    Assignee: Pfizer Inc.
    Inventors: HuaZhu Ke, David D. Thompson
  • Patent number: 6982263
    Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: January 3, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Eugene R. Hickey, Younes Bekkali, Usha R. Patel, Denice Mary Spero, David S. Thomson, Erick Richard Roush Young
  • Patent number: 6906051
    Abstract: The present invention relates to a class of compounds represented by the Formula I: or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?V?3 and/or the ?V?5 integrin.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: June 14, 2005
    Assignee: Pharmacia Corporation
    Inventors: Peter Ruminiski, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Thomas Rogers, Jennifer VanCamp, Chester Yuan
  • Patent number: 6849626
    Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: February 1, 2005
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
  • Patent number: 6825224
    Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds and compositions of this invention.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: November 30, 2004
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Dean P. Stamos, Randy S. Bethiel
  • Patent number: 6777440
    Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1, R2 and B1 are as defined herein.
    Type: Grant
    Filed: December 6, 2002
    Date of Patent: August 17, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Jacques Banville, Roger Remillard, Serge Plamondon
  • Publication number: 20040116445
    Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.
    Type: Application
    Filed: November 18, 2003
    Publication date: June 17, 2004
    Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Matthew S. Miller, Rabindranath Tripathy, Jeffry L. Vaught
  • Publication number: 20040077690
    Abstract: Novel quaternary amidino-containing compounds of the general formulae (I), (II), (III), (IV), (V) and (VI): including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and the compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.
    Type: Application
    Filed: October 16, 2003
    Publication date: April 22, 2004
    Inventors: Bing-Yan Zhu, Wenrong Huang, Penglie Zhang, Zhaozhong Jon Jia, Liang Bao, Yanhong Wu, Robert M. Scarborough
  • Patent number: 6720327
    Abstract: The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or the &agr;v&bgr;5 integrin.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: April 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: Peter Ruminski, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Thomas Rogers, Jennifer VanCamp, Chester Yuan
  • Patent number: 6693202
    Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: February 17, 2004
    Assignee: Theravance, Inc.
    Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
  • Patent number: 6686391
    Abstract: Methods for the treatment of cancers or viral infections in mammals are disclosed that include administration of an N-chlorophenylcarbamate, or an N-chlorophenylthiocarbamate, or a salt thereof. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: February 3, 2004
    Assignee: University of Arizona Foundation
    Inventor: James Berger Camden
  • Patent number: 6683215
    Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: January 27, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
  • Publication number: 20030181442
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: November 27, 2001
    Publication date: September 25, 2003
    Applicant: BAYER CORPORATION
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
  • Patent number: 6613942
    Abstract: Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.
    Type: Grant
    Filed: December 23, 1998
    Date of Patent: September 2, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Anthony Ling, Vlad Gregor, Javier Gonzalez, Yufeng Hong, Dan Kiel, Atsuo Kuki, Shenghua Shi, Lars Naerum, Peter Madsen, Christian Sams, Jesper Lau, Michael Bruno Plewe, Jun Feng, Min Teng, Michael David Johnson, Kimberly Ann Teston, Ulla Grove Sidelmann, Lotte Bjerre Knudsen
  • Patent number: 6593362
    Abstract: This invention relates to pharmaceutical compositions and methods of using non-peptidic cyclophilin-binding compounds in medical conditions involving breakdown of mitochondrial energy metabolism induced by calcium overload, in treating alopecia and promoting hair growth, in treating infections with filarial and helmintic parasites, and in treating and preventing infections with the human immunodeficiency virus.
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: July 15, 2003
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Joseph P. Steiner, Gregory S. Hamilton
  • Publication number: 20030109526
    Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Application
    Filed: December 2, 2002
    Publication date: June 12, 2003
    Inventors: David Lauffer, Michael Mullican
  • Publication number: 20030078297
    Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.
    Type: Application
    Filed: July 15, 2002
    Publication date: April 24, 2003
    Inventors: L. David Waterbury, Allan L. Wilcox, John M. Carney, Farah Mavandadi, Albert Danielzadeh
  • Patent number: 6538029
    Abstract: A method of treating renal cell carcinoma in a mammal with that disease comprising administering to the mammal a physiologically effective amount of an inhibitor of PDE10.
    Type: Grant
    Filed: May 29, 2002
    Date of Patent: March 25, 2003
    Assignee: Cell Pathways
    Inventors: W. Joseph Thompson, John R. Fetter, Robert E. Bellet, Han Li