Polyguanidines Patents (Class 564/236)
  • Patent number: 8969622
    Abstract: In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to compounds comprising the structure: and at least one guanidinium residue, wherein m is zero or a positive integer. Also disclosed are methods of preparing the disclosed compounds. Also disclosed are methods of intracellular delivery comprising administering the disclosed compounds and compositions to a subject. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of one or more compounds or compositions of the invention and a pharmaceutically acceptable carrier. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: August 23, 2007
    Date of Patent: March 3, 2015
    Assignee: Vanderbilt University
    Inventors: Eva M. Harth, James E. Crowe, Jr., Kui Huang, Sharon K. Hamilton, Heidi E. Hamm, Bryan Voss
  • Patent number: 8946299
    Abstract: A product comprising a calixarene for its use in the treatment of pathologies involving at least one bacterial strain having a resistance to at least one defined antibiotic, on patients undergoing simultaneous or sequential treatment with a given antibiotic to which said bacterial strain optionally has a resistance.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: February 3, 2015
    Assignee: Universite de Lorraine
    Inventors: Marion Grare, Raphaël Emmanuel Duval
  • Publication number: 20150031738
    Abstract: The present invention provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 10, 2012
    Publication date: January 29, 2015
    Applicant: University of Massachusetts
    Inventors: Yan Li, Hitest Thaker, Gregory N. Tew, Dahui Liu, Wenxi Pan
  • Patent number: 8889163
    Abstract: Facially amphiphilic polyphenylene and heteroarylene polymers and articles made therform having biocidal surfaces are disclosed. The polymers can inhibit the growth of microorganisms in contact with the surface or in areas adjacent to said biocidal surface. There is also disclosed a methods to attach facially amphiphilic polmers to a solid support. Utility as a contact disinfectant is disclosed.
    Type: Grant
    Filed: March 7, 2002
    Date of Patent: November 18, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Gregory N. Tew, Michael L. Klein
  • Patent number: 8877872
    Abstract: The present technology provides an carbon fiber reinforced plastic having an organoamine coated carbon fiber and a carbonyl functionalized matrix polymer. Also described is a method for recycling the carbon fiber reinforced plastic using an acidic gas.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: November 4, 2014
    Assignee: Empire Technology Development LLC
    Inventors: Kraig Anderson, Angele Sjong
  • Publication number: 20140308317
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 9, 2013
    Publication date: October 16, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventors: Xiaodong Fan, Yongjiang Xu, Dahui Liu, Michael J. Costanzo
  • Patent number: 8785679
    Abstract: Hydrophilic, biocidal coating compositions and methods to make and use the compositions are disclosed. The coatings include compounds with quaternary amine polyethylene glycol groups and polyaminoalkyl biguanide groups as substituents. The compounds when incorporated in paints provide hydrophilic, self-cleaning and biocidal property to the coating.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: July 22, 2014
    Assignee: Empire Technology Development LLC
    Inventors: Glen Leon Brizius, Phillip Kent Montgomery
  • Patent number: 8716530
    Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: May 6, 2014
    Assignee: The Trustess of the University of Pennsylvania
    Inventors: William F. DeGrado, Dahui Liu, Gregory N. Tew, Michael L. Klein
  • Patent number: 8703825
    Abstract: Novel compounds of the following formula (I): in which: n represents an integer from 1 to 12, in particular from 1 to 8, m and m? represent, independently of one another, integers from 0 to 8, q and q? represent, independently of one another, integers from 0 to 2, p and p? represent, independently of one another, integers from 0 to 4, A and A? represent, independently of one another, a CH2 group, (particular case of amidines) an NH group or an NR? group, in which R? is a linear or branched alkyl group with 1 to 3 carbon atoms, B and B? represent, independently of one another, an oxygen atom or a CH2 group, R and R? are, independently of one another, a halogen, such as chlorine, bromine, iodine or fluorine atoms, or a linear or branched alkyl group with 1 to 3 carbon atoms, use thereof as medicaments and the method of preparation thereof.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: April 22, 2014
    Assignee: Universite de Lorraine
    Inventors: Raphaël Emmanuel Duval, Marion Grare, Maxime Mourer, Jean-Bernard Regnouf-De-Vains
  • Publication number: 20140066517
    Abstract: A product comprising a calixarene for its use in the treatment of pathologies involving at least one bacterial strain having a resistance to at least one defined antibiotic, on patients undergoing simultaneous or sequential treatment with a given antibiotic to which said bacterial strain optionally has a resistance.
    Type: Application
    Filed: April 11, 2012
    Publication date: March 6, 2014
    Inventors: Marion Grare, Raphaël Emmanuel Duval
  • Publication number: 20140066576
    Abstract: The present technology provides an carbon fiber reinforced plastic having an organoamine coated carbon fiber and a carbonyl functionalized matrix polymer. Also described is a method for recycling the carbon fiber reinforced plastic using an acidic gas.
    Type: Application
    Filed: August 30, 2012
    Publication date: March 6, 2014
    Inventors: Kraig K. Anderson, Angele Sjong
  • Publication number: 20130252964
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.
    Type: Application
    Filed: January 18, 2013
    Publication date: September 26, 2013
    Applicant: PolyMedix, Inc.
    Inventors: Richard W. Scott, Katie Freeman, Haizhong Tang, Gill Diamond
  • Patent number: 8389768
    Abstract: Provided herein are novel cationic lipids, compositions comprising the cationic lipids, and methods of using the cationic lipids. In some claims, the cationic lipids have cytotoxic activity and can be used alone or in combination with a cytotoxic bioactive compound to kill a cell. In some of these claims, the cationic lipid enhances the cytotoxic activity of the cytotoxic bioactive compound. Methods for treating a subject afflicted with a disease or unwanted condition are provided, wherein the method comprises administering a delivery system comprising a novel cationic lipid to the subject. The invention further provides methods for making delivery systems comprising the novel cationic lipids of the invention.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: March 5, 2013
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Leaf Huang, Yunching Chen, Joyeeta Sen, Surendar Reddy Bathula, Sumio Chono, Shyh-Dar Li, Michael Hackett
  • Publication number: 20130040388
    Abstract: A drug composition containing as a drug substance a polymeric guanidine derivative based on a diamine containing oxyalkylene chains between two amino groups, with the guanidine derivative representing a product of polycondensation between a guanidine acid addition salt and a diamine containing polyalkylene chains between two amino groups, as well as the pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: June 12, 2012
    Publication date: February 14, 2013
    Inventor: Oskar Schmidt
  • Publication number: 20120309801
    Abstract: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.
    Type: Application
    Filed: April 24, 2012
    Publication date: December 6, 2012
    Applicant: Regents of the University of Minnesota
    Inventors: Kevin H. Mayo, Thomas R. Hoye, Xuemei Chen
  • Patent number: 8247500
    Abstract: A polymeric resin comprising guanidine groups having at least one C4-C22 tertiary alkyl substituent.
    Type: Grant
    Filed: February 3, 2009
    Date of Patent: August 21, 2012
    Assignee: Rohm and Haas Company
    Inventors: Rajiv Manohar Banavali, Alfred Karl Schultz
  • Patent number: 8222456
    Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: July 17, 2012
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Dahui Liu, Gregory N. Tew, Michael L. Klein
  • Publication number: 20120157474
    Abstract: The present invention is based on the discovery of a cell-based system to identify novel modulators of splicing or splicing dependent processes. The cell-based system of the present invention utilizes a fast and highly sensitive reporter, that responds to defects in the splicing machinery itself and is sensitive to changes in the signals that regulate splicing dependent processes such as those that modulate the EJC, splicing-dependent export, localization or translation efficiency. The present invention further uses the cell-based screen to identify several small molecules that modulate both constitutive and alternative splicing. Accordingly, the present invention includes general or alternative splicing inhibitors identified using the assay described herein. The present invention also provides methods of treating a subject having a condition associated with aberrant target RNA expression.
    Type: Application
    Filed: May 21, 2010
    Publication date: June 21, 2012
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Gideon Dreyfuss, Ihab Younis, Lili Wan
  • Patent number: 8158827
    Abstract: Disclosed are cationic lipid compounds and compositions of lipid aggregates for delivery of macromolecules and other compounds into cells. The compounds can be used alone or in combination with other compounds to prepare liposomes and other lipid aggregates suitable for transfection or delivery of compounds to target cells, either in vitro or in vivo. The compounds are preferably polycationic and preferably form highly stable complexes with various anionic macromolecules, particularly polyanions such as nucleic acids. These compounds have the property, when dispersed in water, of forming lipid aggregates which associate strongly, via their cationic portion, with polyanions. Also disclosed are intermediates for preparing the compound and compositions of the invention and methods of using the compounds to introduce other compounds into cells.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: April 17, 2012
    Assignee: Life Technologies Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Patent number: 8148577
    Abstract: Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: April 3, 2012
    Assignees: The Johns Hopkins University, Wayne State University
    Inventors: Patrick M. Woster, Tracey Boncher, Robert A. Casero
  • Publication number: 20120077863
    Abstract: A compound of formula I, or a pharmaceutically acceptable salt thereof, wherein —X1, X2 and X3 are each independently where Y is an alkylene, alkenylene or alkynylene group, each of which may be optionally substituted with one or more substituents selected from alkyl, halo, CF3, OH, alkoxy, NH2, CN, NO2 and COOH; W is absent or is O, S or NH; R1, R2, R3 and R4 are each independently selected from H, alkyl, aryl and a protecting group Pi; R7, R8 and R9 are each independently selected from H, alkyl, halo, CF3, OH, alkoxy, CN, NO2 and COOH; —q is 1, 2, 3 or 4; q? is 0, 1, 2 or 3, where q+q? equals 4; p and r are each independently 1, 2, 3, 4 or 5; p? and r? are each independently 0, 1, 2, 3 or 4, where p+p? and r+r? each equal 5; and —n is 0, 1, 2, 3, 4, 5 or 6.
    Type: Application
    Filed: March 1, 2010
    Publication date: March 29, 2012
    Applicant: UCL Business PLC
    Inventors: David Selwood, Roberta Worthington, Anne-Sophie Rebstock, Michela Simone, Matt Gooding, Henry Dube, Kai Stoeber, Slavica Tudzarova, Christoffer Boshoff, Gareth Williams, Sarah Kingsbury, Dimitrios Lagos, Juan Manuel Funes Quesada
  • Publication number: 20110318280
    Abstract: Polymeric anti-microbial agents produced by substituting the nitrogen atoms in the backbone of ethylenimine polymers, for example, substitution with aralkyl groups, are provided. The agents are believed to have low human toxicity while being effective against a variety of pathogens and are useful in applications involving human contact, such as cosmetics, hair care products and textiles, as well as in applications with much less human contact, such as coatings.
    Type: Application
    Filed: September 7, 2011
    Publication date: December 29, 2011
    Inventors: Xinyu Huang, Ted Deisenroth, Andrea Preuss, Sophie Marquais-Bienewald, Carmen Hendricks-Guy, John Jennings
  • Publication number: 20110257199
    Abstract: Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.
    Type: Application
    Filed: June 17, 2011
    Publication date: October 20, 2011
    Inventors: Richard R. Tidwell, David W. Boykin, W. David Wilson, Reto Brun, Karl Werbovetz, Mohamed A. Ismail, Reem K. Arafa, Laixing Hu
  • Patent number: 8012985
    Abstract: The invention relates to compounds having an anti-parasitic, in particular antimalarial activity, characterized in that they correspond to general formula (I) Applications in particular as compounds with anti-parasitic activity.
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: September 6, 2011
    Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Henri Vial, Michele Calas, Roger Escale, Valerie Vidal, Francoise Bressolle, Marie-Laure Ancelin
  • Publication number: 20110184070
    Abstract: Novel compounds of the following formula (I): in which: n represents an integer from 1 to 12, in particular from 1 to 8, m and m? represent, independently of one another, integers from 0 to 8, q and q? represent, independently of one another, integers from 0 to 2, p and p? represent, independently of one another, integers from 0 to 4, A and A? represent, independently of one another, a CH2 group, (particular case of amidines) an NH group or an NR? group, in which R? is a linear or branched alkyl group with 1 to 3 carbon atoms, B and B? represent, independently of one another, an oxygen atom or a CH2 group, R and R? are, independently of one another, a halogen, such as chlorine, bromine, iodine or fluorine atoms, or a linear or branched alkyl group with 1 to 3 carbon atoms, use thereof as medicaments and the method of preparation thereof.
    Type: Application
    Filed: July 10, 2009
    Publication date: July 28, 2011
    Applicant: UNIVERSITE HENRI POINCARE NANCY 1
    Inventors: Raphael Emmanuel Duval, Marion Grare, Maxime Mourer, Jean-Bernard Regnouf-De-Vains
  • Publication number: 20110092601
    Abstract: Polyamine, polyamine/guanidino, and polyamine/biguanide compounds bearing allene, propargyl, cyclopropyl, and other reactive moieties are disclosed. The compounds are useful as irreversible inhibitors of the enzyme lysine-specific demethylase-1 and for the treatment of cancer.
    Type: Application
    Filed: April 14, 2008
    Publication date: April 21, 2011
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Patrick M. Woster, Robert A. Casero
  • Publication number: 20110076766
    Abstract: A drug composition containing as a drug substance a polymeric guanidine derivative based on a diamine containing oxyalkylene chains between two amino groups, with the guanidine derivative representing a product of polycondensation between a guanidine acid addition salt and a diamine containing polyalkylene chains between two amino groups, as well as the pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: September 27, 2010
    Publication date: March 31, 2011
    Inventor: Oskar Schmidt
  • Publication number: 20100331384
    Abstract: The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into ? and ? subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel guanidine and 2-aminoimidazoline compounds which are ligands of the alpha2-adrenoceptor (?2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of ?2-ARs associated disorders, such as depression, schizophrenia, glaucoma and analgesia.
    Type: Application
    Filed: December 22, 2008
    Publication date: December 30, 2010
    Applicants: UNIVERSIDAD DEL PAIS VASCO/EUSKAL HERRIKO UNIBERTSITATEA, UNIDIVIDED TRINITY OF QUEEN ELIZABETH
    Inventors: Maria Isabel Rozas Hernando, Fernando Rodriguez Royo, Javier Meana, Luis Callado
  • Patent number: 7847124
    Abstract: Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: December 7, 2010
    Assignee: Green Formula Co., Ltd.
    Inventors: Kwan Mook Kim, Lijun Tang
  • Patent number: 7745392
    Abstract: Disclosed herein are guanidinium containing compounds consisting of a core moiety with a plurality of side chains containing guanidinium groups. Such compounds have enhanced translocation across cellular membranes and epithelial tissues. The compounds may also have a therapeutic or other biologically active moiety attached so that these moieties may be effectively transported into a cell by the guanidinium containing compound.
    Type: Grant
    Filed: September 21, 2006
    Date of Patent: June 29, 2010
    Assignee: Nitto Denko Corporation
    Inventors: Zheng Hou, Jian Liu, Lei Yu
  • Patent number: 7601872
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and w
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: October 13, 2009
    Assignee: Life Technologies Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Publication number: 20090169608
    Abstract: Topical composition for use especially as a skin lightener, characterized in that it contains an effective amount of at least one compound of general formula (I) or a mixture of such compounds and/or an acid addition salt thereof: in which X is NH or a direct bond and n is 2, 3 or 4, preferably 2 or 3, and its use for lightening skin colour, for depigmenting liver spots and for evening out non-uniformities in skin colouration. The invention further relates to dermatologically effective compositions containing at least one disulfide of general formula (I) and at least one additional skin care ingredient.
    Type: Application
    Filed: October 9, 2006
    Publication date: July 2, 2009
    Applicant: DSM IP ASSETS B.V.
    Inventors: Hugo Ziegler, Peter Wikstroem, Martin Stockli
  • Publication number: 20090023931
    Abstract: Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided.
    Type: Application
    Filed: February 8, 2008
    Publication date: January 22, 2009
    Applicant: Ewha University - Industry Collaboration Foundation
    Inventors: Kim Kwan Mook, Tang Lijun
  • Patent number: 7470817
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)I, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and w
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: December 30, 2008
    Assignee: Invitrogen Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Patent number: 7442682
    Abstract: Compositions and methods are disclosed for the treatment of diabetes and related diseases using peptides with incretin hormone activity. Preferably, the peptide with incretin hormone activity is GLP-1, exendin or an analog of GLP-1 or exendin. The peptides with incretin hormone activity are administered transepithelially using a transepithelial carrier peptide. The transepithelial peptide contains sufficient amino, guanidine or amidino groups to stimulate transepithelial delivery. In some embodiments, the transepithelial carrier and the peptide with incretin hormone activity are embedded in a pressure sensitive adhesive layer of a plaster or patch.
    Type: Grant
    Filed: September 2, 2005
    Date of Patent: October 28, 2008
    Assignee: Nitto Denko Corporation
    Inventors: Chieko Kitaura, Kenjiro Minomi, Katsuyuki Okubo, Keisaku Okada, Natsuko Kagehisa, Masashi Kamiyama, Zheng Hou, Jian Liu, Yucheng Song, Lei Yu
  • Publication number: 20080234384
    Abstract: This invention is directed to compounds of formula (I): wherein m, n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.
    Type: Application
    Filed: March 19, 2008
    Publication date: September 25, 2008
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Mikhail Chafeev, Nagasree Chakka, Jean-Jacques Cadieux, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Jonathan Langille, Shifeng Liu, Jianyu Sun, Serguei Sviridov, Zaihui Zhang
  • Publication number: 20080221043
    Abstract: In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to compounds comprising the structure: and at least one guanidinium residue, wherein m is zero or a positive integer. Also disclosed are methods of preparing the disclosed compounds. Also disclosed are methods of intracellular delivery comprising administering the disclosed compounds and compositions to a subject. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of one or more compounds or compositions of the invention and a pharmaceutically acceptable carrier. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 23, 2007
    Publication date: September 11, 2008
    Inventors: Eva M. Harth, James E. Crowe, Kui Huang, Sharon K. Hamilton, Heidi E. Hamm, Bryan Voss
  • Patent number: 7323594
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by -X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: January 29, 2008
    Assignee: Invitrogen Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Patent number: 7166745
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)1, or {(CH2)i—Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1—L?—X2—Z or —Z; R1–R6, independently of one another, are selected from the group consisting of H, —CH2)p—D—Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: January 23, 2007
    Assignee: Invitrogen Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Patent number: 7067698
    Abstract: Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ?-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.
    Type: Grant
    Filed: August 2, 2002
    Date of Patent: June 27, 2006
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Paul A. Wender, Christopher L. VanDeusen, Kanaka Pattabiraman, Erin T. Pelkey, Theodore C. Jessop
  • Patent number: 6669951
    Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: December 30, 2003
    Assignee: CellGate, Inc.
    Inventors: Jonathan B. Rothbard, Paul A. Wender, P. Leo McGrane, Lalitha V. S. Sista, Thorsten A. Kirschberg
  • Patent number: 6423748
    Abstract: Amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of amido polybiguanides is also disclosed. The amido polybiguanides are useful in the preservation of pharmaceutical compositions, particulary opthalmic and otic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting contact lenses.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: July 23, 2002
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Joonsup Park, Nathaniel D. McQueen
  • Patent number: 6316669
    Abstract: Bis-amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of bis-amido polybiguanides is also disclosed. The bis-amido polybiguanides are useful in the preservation of pharmaceutical compositions, particularly ophthalmic and otic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting/cleaning contact lenses.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: November 13, 2001
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Joonsup Park, Nathaniel D. McQueen
  • Patent number: 6114392
    Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.
    Type: Grant
    Filed: April 16, 1996
    Date of Patent: September 5, 2000
    Inventors: Gad M. Gilad, Varda H. Gilad
  • Patent number: 5910549
    Abstract: An improved process for free radical polymerization is produced making it possible to control the growth steps of a polymerization to produce homopolymers and copolymers, including block and graft copolymers. The process uses a long half-life radical initiators and compounds which have the structure of formula I ##STR1## wherein X is a group having at least one carbon atom and is such that the free radical X is capable of polymerizing the unsaturated monomer by free radical polymerization, and the radical functionality resides on the or one of the carbon atoms, R.sup.1, R.sup.2, R.sup.5 and R.sup.6 represent the same or different straight chain or branched substituted or unsubstituted alkyl groups of a chain length sufficient to provide steric hindrance and weakening of the O--X bond, and R.sup.3 and R.sup.4 represent the same or different, straight chain or branched, substituted alkyl groups or R.sup.3 CNCR.sup.
    Type: Grant
    Filed: August 22, 1996
    Date of Patent: June 8, 1999
    Assignee: Carnegie-Mellon University
    Inventors: Krzysztof Matyjaszewski, Dorota Greszta
  • Patent number: 5830917
    Abstract: There is disclosed a novel amino alcohol amine derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: September 11, 1995
    Date of Patent: November 3, 1998
    Assignee: G. D. Searle & Co.
    Inventors: William M. Moore, E. Ann Hallinan
  • Patent number: 5646188
    Abstract: A compound of general formula I ##STR1## wherein n is 1 or 2; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy or halogeno;R.sub.5 is hydrogen, substituted or unsubstituted C.sub.1-4 alkyl, amino or NR.sub.6 R.sub.7 ;R.sub.3, R.sub.4, R.sub.6 and R.sub.7 are each independently hydrogen or (CH.sub.2).sub.m --[NH(CH.sub.2).sub.x ].sub.y --NHR.sub.11 wherein m is from 0-5, y is from 0-5 and each x is independently from 1-5 and R.sub.11 is hydrogen or C(NH)NH.sub.2 ;provided that when R.sub.3 and R.sub.4 are both hydrogen, R.sub.5 is amino or NR.sub.6 R.sub.7 ; pharmaceutically acceptable salts and optically active isomers thereof.
    Type: Grant
    Filed: July 5, 1995
    Date of Patent: July 8, 1997
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Gad Gilad, Varda Gilad, Jeffrey Sterling, Yaacov Herzig, David Lerner, Alex Veinberg, Isaac Milman, Nina Finkelstein
  • Patent number: 5637621
    Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: June 10, 1997
    Assignee: NZYM, Inc.
    Inventors: Joel Bolonick, Terrance J. Leighton, Ida K. Yu
  • Patent number: 5629348
    Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: May 13, 1997
    Assignee: NZYM, Inc.
    Inventors: Joel Bolonick, Terrance J. Leighton, Ida K. Yu
  • Patent number: 5627194
    Abstract: Novel guanidino-substituted compounds are described having the following general formula (I): ##STR1## in which X may be carbon, oxygen, nitrogen or sulfur; R.sub.1 may be H, OH, linear or branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine, lower alkyl-thio, hydroxy substituted lower alkoxy, lower alkoxy-alkoxy substituted lower alkoxy, hydroxy substituted lower alkyl-amine, alkoxy substituted lower alkyl-amine and terminally guanidino-substituted linear of branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine or lower alkyl-thio; and R.sub.2 and R.sub.3 are independently one of linear or branched lower alkyl, alkoxy, alkyl-substituted alkoxy and alkylamine.These compounds have been found to inhibit effectively herpesvirus replication. Particularly preferred compounds in accordance with formula (I) for this purpose are guanidino-substituted sugar derivatives.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: May 6, 1997
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Sumanas Rakhit, Abdelmalik Slassi