Hydroxy, Bonded Directly To Carbon, Or Ether In A Substituent E (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/223)
  • Patent number: 10286504
    Abstract: Disclosed is a method to make N-acetyl-p-aminophenol. The method includes steps for converting biomass-derived p-hydroxybenzoates to p-hydroxybenzamide, then to p-aminophenol; and then N-acetylating the p-aminophenol.
    Type: Grant
    Filed: March 7, 2018
    Date of Patent: May 14, 2019
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: John Ralph, Steven Karlen, Justin Mobley
  • 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
  • Publication number: 20150045396
    Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like
    Type: Application
    Filed: March 18, 2013
    Publication date: February 12, 2015
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Akihiko Takeuchi, Hiroyuki Tsuchiya
  • Publication number: 20140228443
    Abstract: Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Feng Hong, Ryo Kubota, Jennifer Gage
  • Publication number: 20140094426
    Abstract: Amphiphilic prodrugs of general formula A-X are disclosed, wherein A is a biologically active agent or may be metabolized to a biologically active agent; and X is R, or up to three R moieties attached to a linker, Y1, Y2 or Y3. Self-assembly of the amphiphilic prodrugs into reverse lyotropic phases, particularly hexagonal, cubic and sponge, is disclosed.
    Type: Application
    Filed: November 8, 2013
    Publication date: April 3, 2014
    Inventors: Calum John Drummond, Sharon Marie Sagnella, Minoo Jalili Moghaddam, Xiaojuan Gong
  • Patent number: 8685453
    Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.
    Type: Grant
    Filed: March 20, 2013
    Date of Patent: April 1, 2014
    Assignee: Wellesley Pharmaceuticals, LLC
    Inventor: David A. Dill
  • Patent number: 8673982
    Abstract: This invention relates to certain ceramide-analogues of FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol; fingolimod). In particular, the present invention relates to pharmaceutical compositions comprising these compounds, as well as processes for their preparation and their use in the treatment of autoimmune conditions, such as multiple sclerosis.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: March 18, 2014
    Assignee: Novartis AG
    Inventors: Volker Brinkmann, Guido Jordine, Markus Zollinger, Claudia Sayer
  • Patent number: 8664441
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: March 4, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Publication number: 20130216620
    Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.
    Type: Application
    Filed: March 20, 2013
    Publication date: August 22, 2013
    Applicant: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: Wellesley Pharmaceuticals, LLC
  • Patent number: 8501994
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: August 6, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Publication number: 20130101684
    Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.
    Type: Application
    Filed: April 15, 2011
    Publication date: April 25, 2013
    Applicant: Chromocell Corporation
    Inventors: Jane V. Leland, Louise Slade, David Hayashi, William P. Jones, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Jessica Langer, Kambiz Shekdar
  • Publication number: 20130079416
    Abstract: The present invention relates to a composition comprising phenacetin, in particular a Phenacetinum 4CH homeopathic medicament for use in the treatment of cancer.
    Type: Application
    Filed: April 7, 2011
    Publication date: March 28, 2013
    Applicant: BOIRON
    Inventors: Christophe Schneider, Caroline Laheurte, Laurent Martiny
  • Patent number: 8404891
    Abstract: The present invention concerns a liquid formulation that is stable to oxidation and that is based on paracetamol in an aqueous solvent obtainable by the following steps: (i) dissolving in a reaction vessel paracetamol in an aqueous solvent having a temperature between 65° C. and 95° C., and having pH between 5.0 and 6.0; (ii) cooling the solution so formed to a temperature equal to or above 35° C. and below 40° C. under an atmosphere of nitrogen; (iii) adding cysteine hydrochloride and sodium hydroxide simultaneously to the solution without stirring; (iv) closing the reaction vessel, and stirring the solution of step iii) in a nitrogen atmosphere. It further relates to a method for preparing the formulation.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: March 26, 2013
    Assignee: Neogen N.V.
    Inventor: Khaled Al Dandachi Atassi
  • Patent number: 8178121
    Abstract: The present invention refers to ready-to-use highly stable paracetamol injectable solutions, prepared by mixing paracetamol, water, propylene glycol, and a citrate buffer. (pH 4.5 to 6.5), and by heating said solution under preset conditions. The resulting solution may be stored for an extended period of time within a wide range of temperatures, with no paracetamol precipitation and/or its chemical modification.
    Type: Grant
    Filed: October 15, 2002
    Date of Patent: May 15, 2012
    Assignees: Baxter International Inc., Baxter Healthcare S.A.
    Inventor: Tho Nguyen-Xuan
  • Publication number: 20120065423
    Abstract: The present invention relates to continuous processes for the preparation of primary and secondary N-acetylated aromatic amines of formula I or O-acetylated product of o-hydroxy benzoic acid of Formula II using acetic acid as an acetylating agent. wherein R1 has a definition of hydrogen atom, C1-C4 alkyl group or C1-C4 alkoxy group.
    Type: Application
    Filed: July 29, 2011
    Publication date: March 15, 2012
    Applicant: GRANULES INDIA LIMITED
    Inventors: Bhaskar Arumugam Krishna, Hasnat Abul, Pamidipati Sirisha
  • Publication number: 20110306672
    Abstract: This invention relates to certain ceramide-analogues of FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol; fingolimod). In particular, the present invention relates to pharmaceutical compositions comprising these compounds, as well as processes for their preparation and their use in the treatment of autoimmune conditions, such as multiple sclerosis.
    Type: Application
    Filed: February 23, 2010
    Publication date: December 15, 2011
    Applicant: NOVARTIS AG
    Inventors: Volker Brinkmann, Guido Jordine, Markus Zollinger, Claudia Sayer
  • Publication number: 20110229565
    Abstract: This invention discloses drug-delivery compositions, methods of making prodrugs, and methods of drug delivery using a self-assembled gelator. The backbone of the gelator can contain a drug or prodrug, such as acetaminophen or salicin. Additional drugs or agents can be encapsulated in the gelator. Enzymatic or hydrolytic cleavage can be used to release the drugs.
    Type: Application
    Filed: September 17, 2009
    Publication date: September 22, 2011
    Inventors: Jeffrey M. Karp, Praveen Kumar Vemula, George John, Greg Cruikshank
  • Publication number: 20110212173
    Abstract: There is described a pharmaceutical composition for controlled release of an active compound wherein the active compound is selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof for the treatment or alleviation of depression. More particularly, there is described an abuse resistant pharmaceutical composition for the treatment of inter alia, depression and controlled release pharmaceutical compositions of related thereto.
    Type: Application
    Filed: June 17, 2009
    Publication date: September 1, 2011
    Applicant: e-Therapeutics Ple
    Inventors: Malcolm Philip Young, Olusola Clement Idowu, Philip McKeown
  • Publication number: 20110209227
    Abstract: This invention pertains to chemometric methods for the analysis of chemical, biochemical, and biological data, for example, spectral data, for example, nuclear magnetic resonance (NMR) spectra, and their applications, including, e.g., classification, diagnosis, prognosis, etc., especially in the context of bone disorders, e.g., conditions associated with low bone mineral density, e.g., osteoporosis.
    Type: Application
    Filed: February 4, 2011
    Publication date: August 25, 2011
    Inventors: Jeremy Kirk Nicholson, Elaine Holmes, John Christopher Lindon, Joanne Tracey Brindle, David John Grainger
  • Publication number: 20110159050
    Abstract: Disclosed is a process for modifying the morphology and/or polymorphism of an organic substance, which process comprises treating the solid substance, or a solution or dispersion thereof, with one or more amphiphilic proteins.
    Type: Application
    Filed: June 23, 2009
    Publication date: June 30, 2011
    Applicant: BASF SE
    Inventors: Andreas Hafner, Andreas Buthe, Paul Adriaan Van Der Schaaf, Franz Kaufmann, Gordon Bradley
  • Publication number: 20110098359
    Abstract: A new use for paracetamol in a method of treating glaucoma, which method comprises administering to a patient in need of such treatment 500 mg to 1000 mg of paracetamol in oral format 4 to 6 hourly. An ophthalmic solution is also provided containing between 0.1 to 5% of paracetamol which is administered as one to two drops in each eye 4 to 6 hourly. The ophthalmic solution further includes one or more of the following excipients: hydroxypropylmethylcellulose, benzalconium chloride, polyacrylic acid such as Teargel®.
    Type: Application
    Filed: July 30, 2008
    Publication date: April 28, 2011
    Applicant: Stellenbosch University
    Inventor: David Meyer
  • Publication number: 20110071142
    Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.
    Type: Application
    Filed: March 19, 2010
    Publication date: March 24, 2011
    Applicant: BETH ISRAEL DEACONESS MEDICAL CENTER
    Inventors: Peter Oettgen, Alan C. Rigby, Towia Libermann
  • Patent number: 7906556
    Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
    Type: Grant
    Filed: October 12, 2006
    Date of Patent: March 15, 2011
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: R. Jeffrey Neitz, Eric Tisdale, Barbara Jagodzinska, Anh Truong, Jay Tung
  • Patent number: 7772434
    Abstract: The invention provides a novel ?2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel ?2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with ?2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: August 10, 2010
    Assignee: Theravance, Inc.
    Inventors: Ioanna Stergiades, Edward Yost, Cristin Hubbard, Weijiang Zhang
  • Publication number: 20100152272
    Abstract: Compounds selected from: where DRUG-OH, DRUG-COOH and DRUG-NH2 are biologically active compounds; each X is independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone moiety), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO—, where y is 2-4 or 6-24 and —(CH2CH2O)zCH2COO—, where z is 2-24; each Y is independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester moiety), —COCH2CH2CH2CH2CH2O— (caprolactone ester moiety), —CO(CH2)mO—, where m is 2-4 or 6-24 and —COCH2O(CH2CH2O)n— where n is between 2-24; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; and p is 1-6. Multi-functional compounds and drug dimers, oligomers and polymers are also disclosed.
    Type: Application
    Filed: February 17, 2010
    Publication date: June 17, 2010
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20100068553
    Abstract: The invention relates to a novel ultra-thin hydrophobic and oleophobic layer, formed by self-assembly on a solid substrate surface, of compounds of the general formula A-B in which A represents a group of the formula in which Z represents C or N+, X represents C—H or C-L, L being an electron-attracting group selected from F, Cl, Br, I, CF3, NO2 and N(CH3)3+, Y represents H or CH3, or Y forms a 5- or 6-atom heterocycle with X, T represents NH, CO, CONH or NH2+U?, U? being a soluble anion such as e.g. F?, Cl?, Br?, I, OH?, NO3?, HSO4?, SO42?, CO32?, HCO3? or SCN?, and B represents a C1-C20 linear aliphatic alkyl group partially or completely substituted with F, and a method of preparing this layer and its use as an epilame.
    Type: Application
    Filed: November 29, 2007
    Publication date: March 18, 2010
    Applicant: ROLEX S.A.
    Inventors: Samuele Tosatti, Stefan Zurcher
  • Publication number: 20100041906
    Abstract: The present invention concerns a method for the controlled precipitation of organic compounds giving crystals with a very small average size and a very narrow size distribution.
    Type: Application
    Filed: January 26, 2007
    Publication date: February 18, 2010
    Inventors: Huibert Albertus Van Boxtel, Servatius Hubertus Johannes Wilhelmus Leenen, Matheus Lambertus Spapens
  • Publication number: 20100041905
    Abstract: The present invention relates to a novel process for the preparation of compounds of formula (V) wherein X, Q, R1, R1a and R2 are as defined in the specification, the compounds being useful in the preparation of therapeutic agents.
    Type: Application
    Filed: July 17, 2007
    Publication date: February 18, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Debra Ainge, Philip Cornwall, Duncan Michael Gill, Luis Manuel Vaz
  • Patent number: 7601869
    Abstract: The present invention relates to a method for the preparation of Florfenicol from Fluoroamine compound, namely (1R,2S)-1-[4-(methylsulfonyl)phenyl]-2-amino-3-fluoro-1-propanol (II), by reaction with dihaloacetic acid ester in an organic solvent in presence of an inorganic base.
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: October 13, 2009
    Assignee: Aurobindo Pharma Ltd.
    Inventors: Mallikarjuna Reddy Karuru, Arun Kumar Gupta, Sivakumaran Meenakshisunderam
  • Patent number: 7557247
    Abstract: The invention provides a novel ?2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel ?2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with ?2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.
    Type: Grant
    Filed: May 26, 2004
    Date of Patent: July 7, 2009
    Assignee: Theravance, Inc.
    Inventors: Ioanna Stergiades, Edward Yost
  • Publication number: 20090060922
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 5, 2009
    Applicant: Sepracor Inc.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Patent number: 7268252
    Abstract: Disclosed herein are novel binaphthol derivatives and methods for the optical resolution of amino acids or amino alcohols and for the optical transformation of D, L-forms of amino acids using the same.
    Type: Grant
    Filed: January 30, 2006
    Date of Patent: September 11, 2007
    Assignee: Green of Life Co., Ltd.
    Inventors: Kwan Mook Kim, Won Woo Nam, Hyun Jung Park, Jik Chin
  • Patent number: 7173152
    Abstract: The present invention provides a method for the reductive acetamidation of an aryl nitro compound by reacting a substituted acid with an aryl nitro compound and adding a catalytic amount of a base with the substituted acid and the aryl nitro compound to form an acetamidation aryl nitro compound. The acetamidation aryl nitro compound is then purified.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: February 6, 2007
    Assignee: The Texas A&M University System
    Inventors: Apurba Bhattacharya, Victor Suarez
  • Patent number: 7169748
    Abstract: Novel compounds having the structure (I) where R=methyl, ethyl or propyl, R1=methyl or H, R2=methyl, ethyl or propyl, R3=methyl or H, R4=methyl or ethyl, R5?H or methyl, and where R3 and R5 are not both H, excluding N-ethyl-2-methyl-N-(3-methylphenyl) propanamide, can have desirable odour properties, typically of a tropical fruit, cassis character and find use in perfumes and perfumed products
    Type: Grant
    Filed: June 10, 2002
    Date of Patent: January 30, 2007
    Assignee: Quest International Services B.V.
    Inventors: Karl Andrew Dean Swift, Kim Joyce Yarwood
  • Patent number: 6992218
    Abstract: A method for obtaining aqueous formulations with easily oxidizable active principles, notably phenols, stable over a prolonged period, comprising subjecting them to extreme deoxygenation by bubbling with an inert gas and/or placing wider vaccum, protecting them against possible resorption of oxygen by keeping them under an inert gas atmosphere, by filling, under inert gas, into bottles previously cleared of air by insufflation with inert gas, then subjecting them, while stoppering, to low pressure as obtained in the bottle, of 65,000 Pa maximum, to obtain aqueous solutions having a residual oxygen concentration in the solution below 2 ppm, and preferably of the order of 1 ppm and even 0.5 ppm useful as injectable preparations having an oxygen concentration in the solution below 2 ppm.
    Type: Grant
    Filed: June 6, 2001
    Date of Patent: January 31, 2006
    Assignee: Pharmatop SCR
    Inventors: Francois Dietlin, Daniele Fredj
  • Patent number: 6969775
    Abstract: A process of producing organic compounds, such as acetaminophen, nitroalcohols and indoles, employs a catalyst system of an oxyethylene ether and a metal containing inorganic or organic reagent. The oxyethylene ether at least partially complexes the metal of the inorganic or organic reagent. As such, the reactions may be conducted neat. The processes are environmentally friendly and operationally simple.
    Type: Grant
    Filed: September 19, 2003
    Date of Patent: November 29, 2005
    Assignee: The Texas A&M University System
    Inventors: Apurba Bhattacharya, Gaurang L. Parmar, Vikram C. Purohit, Nitin C. Patel
  • Patent number: 6964963
    Abstract: The present invention describes a process for preparing 4-amino-1-naphthol ethers which is characterized in that naphthol ethers are first prepared from 1-naphthols, the former are then converted to the corresponding 4-acetamino-1-naphthol ethers and then the acyl group is cleaved off, and further describes 4-acetamino-1-naphthol ethers obtained thereby.
    Type: Grant
    Filed: August 27, 2002
    Date of Patent: November 15, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Komoschinski, Herbert Diehl
  • Patent number: 6888015
    Abstract: A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16. (in the formula, X is an aliphatic alkyl group, desirably is an aliphatic alkyl group having 7 to 15 carbon atoms).
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: May 3, 2005
    Assignee: Japan Science and Technology Agency
    Inventors: Shu Kobayashi, Kentaro Hanada
  • Patent number: 6706765
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: February 6, 2003
    Date of Patent: March 16, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
  • Patent number: 6657083
    Abstract: Disclosed is a 2-amino-5-acylamino-4-substituted-phenol compound having the structural formula I: wherein Y is a substituent group, and R′ is a ballast group. Also disclosed is a simplified method for preparing a photographic coupler using this compound.
    Type: Grant
    Filed: December 3, 2001
    Date of Patent: December 2, 2003
    Assignee: Eastman Kodak Company
    Inventor: Chang-Kyu Kim
  • Patent number: 6613943
    Abstract: Disclosed is a 4-acylamino-2-hydroxy-5-substituted-acylanilide compound having the structural formula I: wherein R is hydrogen or an alkyl group, Y is a group linked to the rest of the compound by a —O—, —S—, or —N— atom; and R′ is a substituent group. Also disclosed is a method of using the compound in making a cyan dye-forming photographic coupler.
    Type: Grant
    Filed: December 3, 2001
    Date of Patent: September 2, 2003
    Assignee: Eastman Kodak Company
    Inventor: Chang-Kyu Kim
  • Publication number: 20030113802
    Abstract: The present invention relates to systems and methods for generating polymorphs of compounds. In particular, the present invention provides high throughput systems and methods for generating and identifying new crystalline polymorphs that find use as improved drugs, pigments, explosives, nonlinear optical crystals, solid-state reactive compounds, and other polymorphic materials.
    Type: Application
    Filed: October 11, 2002
    Publication date: June 19, 2003
    Applicant: The Regents of the University of Michigan
    Inventors: Adam J. Matzger, Meidong Lang, Kibum Kim
  • Patent number: 6576793
    Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: June 10, 2003
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, John H. Griffin, Seok-Ki Choi
  • Patent number: 6518310
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: February 11, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
  • Patent number: 6372800
    Abstract: A benzene compound of the formula wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient.
    Type: Grant
    Filed: October 19, 2000
    Date of Patent: April 16, 2002
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Tetsuro Fujita, Kunitomo Adachi, Toshiyuki Kohara, Masatoshi Kiuchi, Kenji Chiba, Koji Teshima, Tadashi Mishina
  • Publication number: 20010011146
    Abstract: The present invention relates to a compound having the formula: 1
    Type: Application
    Filed: April 23, 1998
    Publication date: August 2, 2001
    Inventors: TONG H. JOH, SUNGHEE CHO, CHUNG K. CHU, JINFA DU
  • Patent number: 6255496
    Abstract: Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: July 3, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jacques Banville, Yonghua Gai, Graham Johnson, Fred Christopher Zusi, James R. Burke
  • Patent number: 6242646
    Abstract: The present invention relates to a process for preparing 2,4-dichloro-5-hydroxyacetanilide by reacting 3-hydroxyacetanilide with sulfuryl chloride in the presence of from 3 to 30 parts by weight of an aliphatic carboxylic acid having from 1 to 6 carbon atoms per part by weight of 3-hydroxyacetanilide with vigorous mixing at from 20 to 100° , removing gaseous components from the reaction mixture, setting a ratio of from 1.0 to 6 parts by weight of aliphatic carboxylic acid per part by weight of 3-hydroxyacetanilide employed and removing 2,4-dichloro-5-hydroxyacetanilide as a solid.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: June 5, 2001
    Assignee: Clariant GmbH
    Inventors: Frank Sistig, Hans-Jürgen Leitung, Stefan Krause
  • Patent number: 6242609
    Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: June 5, 2001
    Assignee: Konica Corporation
    Inventor: Fumio Ishii
  • Patent number: 6187819
    Abstract: A composition for the upregulation of expression of cell antigens, without inducing shedding, which comprises a protein kinase C activator is provided by this invention. Further provided by this invention is a method of detecting and treating tumor cells comprising contacting tumor cells with an effective amount of a protein kinase C activator for the upregulation of expression of antigens of tumor cells, without inducing antigen shedding, and detecting the presence of said antigen or then further contacting said tumor cells with an effective amount of an antibody directed to said antigen.
    Type: Grant
    Filed: June 10, 1996
    Date of Patent: February 13, 2001
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Paul B. Fisher, Jorge A. Leon