Nitrogen Or Sulfur In Phenolic Moiety Patents (Class 560/142)
  • Patent number: 11213496
    Abstract: The disclosure provides a method for systemic delivery of a therapeutically effective amount of epinephrine to a subject comprising orally administering dipivefrin or a dipivefrin salt to the subject. The disclosure also includes a method of treatment of a disease amenable to treatment by in vivo delivery of systemic epinephrine comprising administering dipivefrin or a dipivefrin salt to a subject in need of in vivo delivery of systemic epinephrine. The disease can be a respiratory disorder, anaphylaxis, cancer, or a microbial infection. The disclosure also includes dipivefrin or dipivefrin HCl orally dissolving tablets.
    Type: Grant
    Filed: September 10, 2018
    Date of Patent: January 4, 2022
    Assignee: INSIGNIS THERAPEUTICS, INC.
    Inventor: Mingbao Zhang
  • Patent number: 9650332
    Abstract: Provided is a compound of formula (II) as a prodrug of probucol, and a method for preparing the same, as well as a method for preventing or treating dyslipidemia with an effective amount of a compound of formula (II) to a subject in need thereof,
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: May 16, 2017
    Inventor: Yong Xu
  • Patent number: 8987262
    Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: March 24, 2015
    Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de Bordeaux
    Inventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
  • Patent number: 8946456
    Abstract: The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: February 3, 2015
    Assignee: Chemi S.p.A.
    Inventors: Umberto Ciambecchini, Stefano Turchetta, Lorenzo De Ferra, Maurizio Zenoni
  • Publication number: 20140357678
    Abstract: A pharmaceutically acceptable salt, prodrug or derivative compound of the formula I, wherein R1 is selected from H, a (C1-C5) alkyl group and a COR4 group; R2 is selected from H, a (C1-C5) alkyl group and a COR5 group; R3 is selected from H, a (C1-C5) alkyl group, a (C1-C5)-O-alkyl group, a cycloalkyl of (C5-C6) carbon atoms, an aryl group, and an aryl (C1-C5) alkyl group wherein the aryl group can be an unsubstituted aryl or substituted with one or more R6 groups and an NHCOR5 group, or the R2 and R3 groups together with N may form a piperidine, morpholine or piperazine group; R4 is selected from H and a (C1-C5)alkyl group; R5 is selected from an aryl group unsubstituted or substituted with one or more R6, linear or branched(C1-C5) alkyl or pyridyne groups and a pyridine group; R6 is selected from (C1-C5)alkyl groups, halogen and nitro.
    Type: Application
    Filed: January 10, 2013
    Publication date: December 4, 2014
    Inventors: Gerardo Burton, Javier Duran, David Martinez, Elvira Zini, Veronica Mora Munoz, Lucila Bertoncello
  • Patent number: 8816001
    Abstract: This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2?-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a Methanococcus jannaschii (Mj) tyrosyl-tRNA synthetase/tRNACUA pair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1).
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: August 26, 2014
    Assignee: Franklin and Marshall College
    Inventors: Ryan A. Mehl, Krzysztof Matyjaszewski, Saadyah Averick
  • Patent number: 8722937
    Abstract: The present invention provides N-alkylthio ?-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and method of their use as anti-bacterial agents.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: May 13, 2014
    Assignee: University of South Florida
    Inventors: Edward Turos, Kevin D. Revell
  • Patent number: 8618323
    Abstract: A composition comprising a polymer backbone and at least one side group, wherein the side group comprises a benzene ring-based chromophore comprising a ketone at the 1-position, a substituted or unsubstituted amino group at the 2-position, and an oxygen atom at the 3-position of the benzene ring. The chromophore is a kynurenine-based compound. Methods of making and using the composition are also provided. The composition can be used in an ophthalmic lens or device for protecting the retina by blocking UV rays and filtering violet rays.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: December 31, 2013
    Assignee: Benz Research and Development Corporation
    Inventors: Patrick H. Benz, Jose A. Ors
  • Publication number: 20130261259
    Abstract: This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2?-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a Methanococcus jannaschii (Mj) tyrosyl-tRNA synthetase/tRNACUA pair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1).
    Type: Application
    Filed: March 7, 2013
    Publication date: October 3, 2013
    Applicant: FRANKLIN AND MARSHALL COLLEGE
    Inventors: Ryan A. Mehl, Krzysztof Matyjaszewski, Saadyah Averick
  • Publication number: 20130079399
    Abstract: The present invention refers to the compounds corresponding to the following general formula (I): wherein: R?C4-C8 alkanoyl; and X?NH—R1 where R1?H, or an amine protecting group; and/or the pharmaceutically acceptable salts thereof. Preferred compounds according to the present invention are represented by the following formula (Ia): wherein: R?C4-C8 alkanoyl; and/or the pharmaceutically acceptable salts thereof. In a preferred embodiment, an object of the present invention is to provide 5-amino-2-(butyryloxy)benzoic acid and/or the pharmaceutically acceptable salts thereof, preferably hydrochloride salt. A further object of the present invention is represented by the use of the compounds of formula (Ia), in particular 5-amino-2-(butyryloxy)benzoic acid and/or pharmaceutically acceptable salts thereof, as a medicament and by the use thereof for the treatment of intestinal inflammatory diseases.
    Type: Application
    Filed: November 21, 2012
    Publication date: March 28, 2013
    Applicant: SOFAR SPA
    Inventor: Carla LABRUZZO
  • Publication number: 20130079532
    Abstract: The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B.
    Type: Application
    Filed: April 29, 2011
    Publication date: March 28, 2013
    Applicant: CHEMI S.P.A.
    Inventors: Umberto Ciambecchini, Stefano Turchetta, Lorenzo De Ferra, Maurizio Zenoni
  • Patent number: 8389671
    Abstract: The present invention can provide a composition for optical members, which contains (a) a compound having one or more of any group selected from the group consisting of an acryloyl group, a methacryloyl group, an allyl group and a vinyl group and one or more ?-epithiopropyl groups in a molecule. In a preferable embodiment of the present invention, the composition for optical members further contains at least one compound selected from (b) a compound having one or more ?-epithiopropyl groups in a molecule while having no polymerizable unsaturated bond group, (c) an inorganic compound having a sulfur atom and/or a selenium atom, (d) a compound having one or more thiol groups in a molecule, (e) a compound having one or more amino groups in a molecule while having no heterocyclic ring, and (f) a compound having one or more of at least one group selected from the group consisting of a vinyl group, an acryloyl group, a methacryloyl group and an allyl group in a molecule.
    Type: Grant
    Filed: March 11, 2008
    Date of Patent: March 5, 2013
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Motoharu Takeuchi, Hiroshi Horikoshi, Hiroaki Tanaka, Hirohito Ishizuka
  • Publication number: 20120322715
    Abstract: The storage stability of a serine hydrolase acting on ester bonds in a formulation without a protease can be improved by incorporating a serine protease inhibitor.
    Type: Application
    Filed: January 4, 2011
    Publication date: December 20, 2012
    Applicant: NOVOZYMES A/S
    Inventors: Lise Munch Mikkelsen, Tomas Tage Hansen, Esben Peter Friis
  • Patent number: 8222296
    Abstract: Conjugates of a gamma-aminobutyric acid (GABA) compound or a glycine compound and an analgesic drug are disclosed. Further disclosed are pharmaceutical compositions containing these conjugates and uses thereof in the treatment of CNS-associated diseases or disorders, optionally in combination with a psychotropic drug.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: July 17, 2012
    Assignees: Ramot at Tel-Aviv University Ltd., Bar-Ilan University, BioLineRX Ltd.
    Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman, Ran Lifshitz, Ilan Winkler
  • Publication number: 20120108549
    Abstract: Apocynin derivative compounds, active pharmaceutical ingredients, dosage forms, and methods of use thereof as neuroprotectants in the brain of mammals.
    Type: Application
    Filed: April 15, 2010
    Publication date: May 3, 2012
    Inventors: Balaraman Kalyanaraman, Joy Joseph, Anumantha Kanthasamy
  • Patent number: 8168734
    Abstract: The invention relates to compounds represented by Formula (1): wherein Ra is independently halogen, cyano, —CF3, —CF2H, —CFH2, —OCF3, —OCF2H, —N?C?O, —N?C?S or alkyl having a carbon number of approximately 1 to approximately 20; in the alkyl, optional —CH2— may be substituted with —O—, —S—, —SO2—, —CO—, —COO—, —OCO—, —CH?CH—, —CF?CF— or —C?C—, and optional hydrogen may be substituted with halogen; Rb is fluorine or —CF3; A is independently 1,4-cyclohexylene, 1,4-cyclohexenylene, 1,4-phenylene, naphthalene-2,6-diyl, tetrahydronaphthalene-2,6-diyl, fluorene-2,7-diyl or bicyclo[2.2.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: May 1, 2012
    Assignees: JNC Corporation, Chisso Petrochemical Corporation
    Inventor: Takashi Kato
  • Patent number: 8143325
    Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the diamines and diisocyanates thereof, wherein each X represents a member independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO— where y is one of the numbers 2, 3, 4 or 6-24 inclusive, and —(CH2CH2O)z?CH2COO— where z? is an integer between 2 and 24, inclusive; each Y represents a member independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester), —COCH2CH2CH2CH2CH2O— (caprolactone ester), —CO(CH2)mO— where m is an integer between 2, 3, 4 or 6-24 inclusive, —COCH2O(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; p is an integer between 1 and 4, inclusive; and Rn represents one or more
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: March 27, 2012
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20110312890
    Abstract: This invention relates to pharmaceutical compounds and nutritional supplements that are acetylated derivatives of naturally occurring amino acids and acetylated derivatives of peptides derived from naturally occurring amino acids containing hydroxyl groups. They are as useful as anti-platelet drugs, and as nutritional supplements.
    Type: Application
    Filed: August 1, 2011
    Publication date: December 22, 2011
    Applicant: SIGNATURE R&D HOLDINGS, LLC
    Inventor: V. Ravi Chandran
  • Publication number: 20110263545
    Abstract: The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.
    Type: Application
    Filed: May 20, 2009
    Publication date: October 27, 2011
    Inventors: Naweed Muhammad, Keith R. Bley, Jeffrey Tobias
  • Patent number: 8044235
    Abstract: A monomer is provided which is excellent in reactivity, can give high heat resistance and high refractive index, and has two or more polymerizable functional groups with different polymerization properties and an aromatic ring in the molecule. An industrial advantageous process for producing the monomer is also provided. The monomer is an aromatic isocyanate compound containing a (meth)acryloyl group, and is represented by Formula (I): wherein R1 is a single bond or a linear or branched alkylene group of 1 to 5 carbon atoms, R2 is a hydrogen atom or a methyl group, R3 is a single bond or a linear or branched alkylene group of 1 to 3 carbon atoms, X is independently a halogen atom or an electron-withdrawing group, m is an integer ranging from 0 to 4, n is an integer ranging from 1 to 3, and 1?m+n?5.
    Type: Grant
    Filed: March 15, 2006
    Date of Patent: October 25, 2011
    Assignee: Showa Denko K.K.
    Inventors: Kaneo Nozawa, Katsutoshi Ohno, Yotaro Hattori
  • Patent number: 7919648
    Abstract: The invention relates to compounds represented by Formula (1): wherein Ra is alkyl or the like; Rb is fluorine or —CF3; A is 1,4-cyclohexylene, 1,4-phenylene or the like; Z is a single bond, alkylene or the like; Y is a single bond, alkylene or the like; and m and n are an integer of approximately 0 to approximately 5.
    Type: Grant
    Filed: December 7, 2006
    Date of Patent: April 5, 2011
    Assignees: Chisso Corporation, Chisso Petrochemical Corporation
    Inventor: Takashi Kato
  • Publication number: 20100273725
    Abstract: The present invention relates to photosensitizer compounds for use in cosmetic and therapeutic applications of photodynamic therapy. The compounds of the present invention are designed for topical application and are characterized by a low permeability to the stratum corneum (the outer skin layer of an individual) and/or a low allergenic potential. Surprisingly, such compounds have beneficial properties in the treatment of certain diseases and lack the undesired damages to healthy skin entailed by prior art compounds. ALA (5-aminolevulinic acid)-esters of body-owned, natural compound such as aminoacids, steroids, carbohydrades, alcohols are preferred, examples of photosensitizers of the present invention. The compounds of the present invention are used in the treatment of skin diseases such as psoriasis, sebaceous glands related conditions including acne, seborrhoic dermatitis, rosacea, skin cancer and precancer, as well as in cosmetic hair removal.
    Type: Application
    Filed: December 12, 2008
    Publication date: October 28, 2010
    Inventors: Thomas Glanzmann, Jérôme Barge, Georges Wagnieres
  • Publication number: 20100256231
    Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.
    Type: Application
    Filed: June 14, 2010
    Publication date: October 7, 2010
    Applicant: UCB Pharma GmbH
    Inventors: Claus MEESE, Bengt SPARF
  • Patent number: 7772352
    Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the diamines and diisocyanates thereof, wherein each X represents a member independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO— where y is one of the numbers 2, 3, 4 or 6-24 inclusive, and —(CH2CH2O)z?CH2COO— where z? is an integer between 2 and 24, inclusive; each Y represents a member independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester), —COCH2CH2CH2CH2CH2O— (caprolactone ester), —CO(CH2)mO— where m is an integer between 2, 3, 4 or 6-24 inclusive, —COCH2O(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; p is an integer between 1 and 4, inclusive; and Rn represents one or more
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: August 10, 2010
    Assignee: Bezwada Biomedical LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20100120912
    Abstract: Provided are nutraceutical or dietary supplemental compositions comprising esterified capsaicinoids. The esterified capsaicinoids may converted to the active parent capsaicinoid compound following enzymatic or chemical hydrolysis. In various embodiments, these esterified capsaicinoids have a higher lipophilicity, lipid solubility and result in less irritation to the stomach than the parent capsaicinoid, and hence may be included in certain dietary supplement formulations, including capsules, pills and tablets dietary supplement formulations. The dietary supplement compositions may be used for pain management in mammals in vivo and/or in the treatment of various pathological conditions in humans.
    Type: Application
    Filed: October 30, 2009
    Publication date: May 13, 2010
    Applicant: Trinity Laboratories Inc.
    Inventors: Chandra Ulagaraj Singh, Rao Nulu Jagaveerabhadra
  • Patent number: 7649114
    Abstract: The invention concerns a method for the isolation of a stereoisomer from a mixture comprising the two stereoisomers of the general formulae (I-A) and (I-A?) and/or the two stereoisomers of the general formulae (I-B) and (I-B?) in which R1, R2 and R3, identical or different, are selected from the group consisting of —H, —F, —Cl, —C1-C6-alkyl, —S—C1-C6-alkyl, —OH, —O—C1-C6-alkyl, —O—C1-C6-alkylenephenyl, —OCO—C1-C6-alkyl, —OCON(C1-C6-alkyl)2 and —O—SiR8R9R10 (in which R8, R9 and R10, identical or different, are —C1-C6-alkyl or -phenyl); R4 is —H or —C1-C6-alkyl; R5 is —C1-C6-alkyl; and R6 and R7, identical or different, are —H or —C1-C6-alkyl; or their salts with organic or inorganic acids; comprising the step (a) manipulating the mixture ratio of the stereoisomers in the mixture so that at least one of the stereoisomers is present in an enantiomeric excess.
    Type: Grant
    Filed: May 29, 2006
    Date of Patent: January 19, 2010
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Heinrich Buschmann, Wolfgang Hell
  • Patent number: 7622604
    Abstract: A probucol or a probucol derivative can be efficiently converted to a monoester or monoether of probucol by reacting the free hydroxyl-containing probucol or a derivative thereof (by which is meant a probucol compound with at least one substituent that is different from that on the parent probucol molecule but which maintains the two free hydroxyl groups) with a Grignard reagent or a lithium reagent that produces a magnesium bromide or lithium salt of probucol or the probucol derivative. The probucol compound anion is then reacted with an ester or ether forming compound.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: November 24, 2009
    Assignee: Salutria Pharmaceuticals LLC
    Inventor: M. David Weingarten
  • Patent number: 7598419
    Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.
    Type: Grant
    Filed: March 22, 2005
    Date of Patent: October 6, 2009
    Assignee: HSC Research and Development Limited Partnership
    Inventors: Chaim M. Roifman, Peter Demin, Andrew Freywald, Thomas Grunberger, Olga Rounova, Nigel Sharfe
  • Publication number: 20090082590
    Abstract: The present invention provides a 4-mercaptophenyl ester of acetic acid, which is useful as a raw material for synthesizing a developer, etc., and a process for producing the same. The present invention provides a 4-mercaptophenyl ester of acetic acid represented by Formula (1); wherein Ac is an acetyl group, and R is a C1-4 alkyl group, and a process for producing the 4-mercaptophenyl ester of acetic acid having a step of reducing a 4-halosulfonylphenyl ester of acetic acid represented by Formula (2); wherein Ac is an acetyl group, R is a C1-4 alkyl group, and X is a halogen atom.
    Type: Application
    Filed: April 26, 2006
    Publication date: March 26, 2009
    Applicant: SUMITOMO SEIKA CHEMICALS CO., LTD.
    Inventors: Koji Fujita, Sachio Iida, Mikio Yamamoto, Kohei Washizaki
  • Patent number: 7345191
    Abstract: A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R5, R6, Z and Z? are defined herein.
    Type: Grant
    Filed: February 26, 2005
    Date of Patent: March 18, 2008
    Assignee: Cambrex Charles City, Inc.
    Inventors: Paul Alan Jass, Jason Scott Douglas
  • Patent number: 7294737
    Abstract: Provided are methods for manufacturing compounds of Formula I wherein all substituents are described herein.
    Type: Grant
    Filed: April 20, 2005
    Date of Patent: November 13, 2007
    Assignee: AtheroGenics, Inc.
    Inventor: M. David Weingarten
  • Patent number: 7294736
    Abstract: A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R5, R6, Z and Z? are defined herein.
    Type: Grant
    Filed: April 9, 2004
    Date of Patent: November 13, 2007
    Assignee: Cambrex Charles City, Inc.
    Inventors: Paul Alan Jass, Jason Scott Douglas
  • Patent number: 7189870
    Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
    Type: Grant
    Filed: August 25, 2003
    Date of Patent: March 13, 2007
    Assignee: AtheroGenic, Inc.
    Inventor: Patricia K. Somers
  • Patent number: 6864381
    Abstract: A process for preparing acyloxybenzenesulfonates by reacting a carboxylic acid derivative with a salt of a phenolsulfonic acid in the presence of an antioxidant, preferably 2,6-di-tert-butyl-4-methylphenol. The addition of such antioxidants gives a product having a high color quality.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: March 8, 2005
    Assignee: Clariant GmbH
    Inventors: Alexander Lerch, Michael Seebach, Wolf-Dieter Mueller
  • Patent number: 6858650
    Abstract: The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(?)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.
    Type: Grant
    Filed: November 15, 2000
    Date of Patent: February 22, 2005
    Assignee: Schwarz Pharma AG
    Inventor: Claus Meese
  • Patent number: 6822113
    Abstract: A process for preparing acyloxybenzenesulfonates by reacting anhydrous phenolsulfonates with carboxylic acid derivatives comprises conducting the reaction with a salt of a phenolsulfonic acid which has a water content of less than 0.5% by weight and has been contacted with a substance having basic properties.
    Type: Grant
    Filed: May 8, 2003
    Date of Patent: November 23, 2004
    Assignee: Clariant GmbH
    Inventors: Gerd Reinhardt, Peter Naumann, Alexander Lerch, Wolf-Dieter Mueller, Narayan D. Sadanani
  • Patent number: 6790981
    Abstract: The invention relates to a process for the preparation of acyloxybenzenesulfonates starting from carbonyl halides and salts of phenolsulfonic acid which have a low water content. Surprisingly, it was discovered that acyloxybenzenesulfonates can be prepared in high yields and good grades, irrespective of the grade or reactivity of the phenolsulfonic acid derivative, if the reaction of the phenolsulfonic acid with an alkanecarboxylic acid derivative is carried out in an aliphatic or aromatic solvent in the presence of 0.5 to 25% by weight of a polyglycol ether.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: September 14, 2004
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Wolf-Dieter Mueller, Peter Naumann
  • Patent number: 6639096
    Abstract: Process for the preparation of acyloxybenzenesulfonates by reaction of phenolsulfonate with a water content of less than 0.5% by weight and alkanecarbonyl halide in a hydrocarbon as solvent and in the presence of a catalyst in the form of a basic nitrogen-containing compound.
    Type: Grant
    Filed: August 1, 2002
    Date of Patent: October 28, 2003
    Assignee: Clariant GmbH
    Inventors: Gerd Reinhardt, Peter Naumann, Miriam Ladwig, Ina Golla, Torsten Pilz, Reto Wieduwilt, Henri Jourdan
  • Patent number: 6624193
    Abstract: The present invention provides a prophylactic and therapeutic medicament for ophthalmic diseases, especially ophthalmic inflammatory diseases and corneal ulcer, comprising as an active ingredient a compound represented by the formula (I): or a pharmacologically acceptable salt or hydrate thereof.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: September 23, 2003
    Assignees: Ono Pharmaceutical Co., Ltd., Senju Pharmaceutical Co., Ltd.
    Inventors: Hiroaki Naka, Kazuhito Kawabata, Hideki Tokushige
  • Publication number: 20030125577
    Abstract: A compound of the formula (I) 1
    Type: Application
    Filed: November 4, 2002
    Publication date: July 3, 2003
    Inventors: Paul F. Corey, Steven W. Felman, Gary E. Rehm, Michael J. Pugia
  • Publication number: 20030105148
    Abstract: The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.
    Type: Application
    Filed: August 9, 2002
    Publication date: June 5, 2003
    Inventors: Robert F. Kaltenbach, Simon P. Robinson, George L. Trainor
  • Patent number: 6573297
    Abstract: A (2-substituted oxyphenyl)alkanamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C3-30 expressed by R1 and the other is —(CH2)n-NR2R3; Z is —CO— or —CONR6—; R2 and R3 individually represent H, lower alkyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members; wherein —CONR5—(CH2)n-NR2R3 or —CONR6—(CH2)n-NR2R3 may be the following Group (II): wherein ring Y is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, lower alkyl, lower acyl and etc; R5 and R6 are individually H, lower alkyl, lower acyl or lower alkylcarbamoyl, or may form a part of said Group(II); 1 is 0 or 1; m is 1 or 2; and n is an integer of 0-5.
    Type: Grant
    Filed: October 29, 2001
    Date of Patent: June 3, 2003
    Assignee: Shiseido Co., Ltd.
    Inventors: Koji Kobayashi, Hirotada Fukunishi, Tokuro Iwabuchi
  • Publication number: 20030100698
    Abstract: Materials for dielectrics and/or buffer layers in microelectronics utilize polymers can be based on bis-o-nitrophenols. The bis-o-nitrophenols carry a tert-butoxycarbonyl group on at least one of the hydroxyl groups. The polybenzoxazoles prepared from these compounds have a lower dielectric constant than corresponding polymers which are prepared from bis-o-nitrophenols that do not have a tert-butoxycarbonyl group.
    Type: Application
    Filed: September 16, 2002
    Publication date: May 29, 2003
    Inventor: Recai Sezi
  • Publication number: 20030096992
    Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.
    Type: Application
    Filed: September 20, 2002
    Publication date: May 22, 2003
    Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
  • Patent number: 6566394
    Abstract: Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-&kgr;B with little side effects.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: May 20, 2003
    Assignees: Mercian Corporation, Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Tomio Takeuchi, Kazuo Umezawa, Sakino To-E, Naoki Matsumoto, Tsutomu Sawa, Takeo Yoshioka, Naoki Agata, Shin-ichi Hirano, Kunio Isshiki
  • Patent number: 6527690
    Abstract: The invention relates to a process for purifying and decolorizing a phenyl ester salt. The process combines a phenyl ester salt with a solvent to form a mixture and then stirs the mixture to form a slurry. The phenyl ester salt is substantially insoluble in this solvent. The process then collects the phenyl ester salt from the slurry. The collected phenyl ester salt may then be optionally dried or recrystallized. The collected phenyl ester salt is dissolved in a solvent to form a solution. The solution is decolorized and then spray dried to form a powder of the phenyl ester salt. As a result of the process the phenyl ester salt powder has a higher purity and an improved color as compared to the starting phenyl ester salt.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: March 4, 2003
    Inventors: Bhaskar Krishna Arumugam, Michael Eugene Burns, Dimmick Lee Bymaster, Jeffrey Scott DuPont, Robert Richard Dykstra, Robert Lee Eagan, Eddie Joseph Eckart, Jarvey Eugene Felty, Jr., Kevin John Fontenot, Jeffrey William Green, Shane Kipley Kirk, Gary Paul Lutz, Tony Lee Sander, Thomas Hugh Williams, George Chester Zima
  • Patent number: 6476076
    Abstract: The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: November 5, 2002
    Assignees: Pacific Corporation, Digital Biotech Co., Ltd.
    Inventors: Jeewoo Lee, Uhtaek Oh, Young-Ho Park, Young-Ger Suh, Hyeung-Geun Park, Hee-Doo Kim
  • Patent number: 6448442
    Abstract: The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents of formula I wherein n is 0 or 1, and where n is 1 each C6R5 moiety may be the same or different; X denotes a bond or a group providing a 1 to 7 atom chain linking two C6R5 moieties or, where n is 0, X denotes a group R; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M1, two or three non-adjacent R groups in each C6R5 moiety being iodine and at least one R group in each C6R5 moiety being an M or M1 moiety; each M which may be the same or different, is a non-ionic hydrophilic moiety; and each M1 independently represents a —CHOHCON(R1)2 group wherein each R1, which may be the same or different, is a hydrogen atom, an OH group or a C1-6 alkoxy or optionally hydroxylated C1-5 alkyl group; at least one R group in the molecule being an M1 moiety; and isomers thereof.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: September 10, 2002
    Assignee: Amersham Health AS
    Inventors: Torsten Almen, Fredrik Ek
  • Publication number: 20020099096
    Abstract: This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.
    Type: Application
    Filed: August 23, 2001
    Publication date: July 25, 2002
    Inventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
  • Patent number: 6410775
    Abstract: aPL analogs that (a) bind specifically to B cells to which an aPL epitope binds and are disclosed. Optimized analogs lack T cell epitope(s) are useful as conjugates for treating aPL antibody-mediated diseases. Conjugates comprising aPL analogs and nonimmunogenic valency platform molecules are provides as are novel nonimmunogenic valency platform molecules and linkers. Methods of preparing and identifying said analogs, methods of treatment using said analogs, methods and compositions for preparing conjugates of said analogs and diagnostic immunoassays for aPL antibodies are disclosed.
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: June 25, 2002
    Assignee: La Jolla Pharmaceutical Company
    Inventors: Edward Jess Victoria, David Matthew Marquis, David S. Jones, Lin Yu