Two Benzene Rings Bonded Directly To The Same Nitrogen Patents (Class 514/658)
  • Patent number: 9265742
    Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: February 23, 2016
    Assignee: Infirst Healthcare Limited
    Inventors: Robin M. Bannister, John Brew
  • Publication number: 20150011628
    Abstract: The invention relates to substituted diphenylamine compounds using as antitumor agents. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) showed potent antitumor activity, especially to cure or alleviate the cancer causing by cancer cells of human tissue or organ. The preferred cancers are: colon cancer, liver cancer, lymph cancer, lung cancer, esophageal cancer, breast cancer, central nervous system cancer, melanoma, ovarian cancer, cervical cancer, renal cancer, leukemia, prostatic cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, nasopharynx cancer or stomach cancer.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 8, 2015
    Inventors: Changling Liu, Baoshan Chai, Huichao Li, Aiying Guan
  • Patent number: 8911769
    Abstract: The invention relates to pharmaceutical compositions suitable for oral administration in the form of edible films comprising diclofenac.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: December 16, 2014
    Assignee: Novartis AG
    Inventors: Gavin Murray Spencer, Alexander Mark Schobel, Greg Slominski, Stephan Meyer, Isabelle Rault
  • Publication number: 20140303226
    Abstract: The present disclosure relates to methods and compositions for modulating the activity of KCNQ channels as a means for reducing the effects of aberrant KCNQ channel function associated with epilepsy, deafness and arrhythmias including but not limited to, Long-QT syndrome (“LQTS”), and atrial fibrillation. The present disclosure also relates to the discovery of certain regions of KCNQ channels that interact with various channel stimulating molecules such as, ATP, and PIP2, as well as KCNQ channel domains that effect voltage dependant channel activation. The disclosure is also directed to the use of small molecules to modulate KCNQ channel activity in a cell. Moreover, the present disclosure relates to the therapeutic effects of treating a subject with modulators of KCNQ channel activity.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 9, 2014
    Applicants: WASHINGTON UNIVERSITY, Curators of the University of Missouri, The Research Foundation for The State University of New York
    Inventors: Jianmin Cui, Ira S. Cohen, Xiaoqin Zou
  • Publication number: 20140296242
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of the invention. In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of the invention. Pharmaceutical compositions of some embodiments of the present invention comprise a compound of the invention.
    Type: Application
    Filed: April 27, 2012
    Publication date: October 2, 2014
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: J. Chistopher States, Ben Frazier Taylor, John O. Trent
  • Patent number: 8697680
    Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.
    Type: Grant
    Filed: September 6, 2009
    Date of Patent: April 15, 2014
    Assignee: Ramot At Tel Aviv University Ltd.
    Inventors: Roni Scherzer, Ehud Gazit, Daniel Segal
  • Publication number: 20140079741
    Abstract: Treatment of a fungal biofilm on implants is via a combination of drugs and/or via the implant pre-treatment with one drug or via the combination of drugs.
    Type: Application
    Filed: March 19, 2012
    Publication date: March 20, 2014
    Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN KU LEUVEN RESEARCH & DEVELOPMENT
    Inventors: Anna Bink, Bruno Cammue, Johan Martens, Bram Neirinck, Karin Thevissen, Jozef Vleugels
  • Publication number: 20130289076
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 31, 2013
    Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal
  • Publication number: 20130243698
    Abstract: The present invention provides a variety of radicals, which are useful as polarizing compounds. Exemplary radicals are represented by compounds of Structural Formulae (I), (II), (III) and (IV) as described herein.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 19, 2013
    Applicant: Massachusetts Institute of Technology
    Inventors: Timothy Manning Swager, Robert Guy Griffin, Olesya Haze, Bjorn Corzilius, Albert A. Smith
  • Patent number: 8415393
    Abstract: The present invention provides methods for the design and identification of novel antimicrobial compounds, and provides antimicrobial compounds identified using these methods. These antimicrobial compounds inhibit the binding of a prokaryotic single-stranded DNA binding protein to a polypeptide that binds to the prokaryotic single-stranded DNA binding protein. In some examples, the prokaryotic single-stranded DNA binding protein is prokaryotic Exonuclease I. In one embodiment, the antimicrobial compound has the structure wherein Y is selected from the group consisting of CH2, O, and NH, R1 is selected from the group consisting of H, F, Cl, Br, and I, R2 is selected from the group consisting of H and CF3, R3 is selected from the group consisting of H and CO2H, R4 is selected from the group consisting of H and OH, and R5 is selected from the group consisting of H, alkoxy, and NO2.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: April 9, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: James L. Keck, Douglas A. Bernstein
  • Publication number: 20130071353
    Abstract: Inhibitors of retroviral propagation, methods of treatment and prevention of retroviral infections using the inhibitors, and pharmaceutical compositions including the inhibitors, are disclosed.
    Type: Application
    Filed: March 14, 2011
    Publication date: March 21, 2013
    Applicant: TRANA DISCOVERY, INC
    Inventors: Richard H. Guenther, Jerzy R. Szewczyk
  • Publication number: 20120309844
    Abstract: Substituted diphenylamine compounds of general formula I are provided, in which each substituted group is defined as in the description. The compounds of general formula I have broad-spectrum fungicidal activity in the field of agriculture. Furthermore, the preparation methods of the above compounds are simple.
    Type: Application
    Filed: March 21, 2011
    Publication date: December 6, 2012
    Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATION
    Inventors: Changling Liu, Huichao Li, Zhinian Li, Guang Huang, Hong Zhang
  • Patent number: 8309602
    Abstract: The present invention relates to multi-substituted m-diarylanilines or pharmaceutically acceptable salts thereof, wherein X, R1-R7 are as defined in the claims, their preparation process, pharmaceutical compositions comprising them and their use for the manufacture of a medicament for anti-HIV.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: November 13, 2012
    Assignees: Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Bingjie Qin, Kuo-Hsiung Lee, Shibo Jiang, Hong Lu
  • Publication number: 20120003316
    Abstract: This invention relates to a multi-configured, transmucosal pharmaceutical dosage form and, more particularly, to a pharmaceutical dosage form which has a single monolithic/heterogeneous layer or a plurality of such layers. The dosage form is suitable for the delivery of one or more pharmaceutical compositions via the buccal, sublingual, rectal, vaginal or transmucosal delivery route in a human or animal body. It provides for selected delivery profiles resulting from, but not limited to, a porosity-enabled composite matrix of one or more layers/components of the pharmaceutical composition/s. The invention also provides for a method of manufacturing said transmucosal pharmaceutical dosage form in a plurality of configurations.
    Type: Application
    Filed: June 3, 2009
    Publication date: January 5, 2012
    Inventors: Deshika Reddy, Oluwatoyin Ayotomilola Adeleke, Viness Pillay, Yahya Choonara
  • Publication number: 20110224184
    Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.
    Type: Application
    Filed: September 6, 2009
    Publication date: September 15, 2011
    Applicant: RAMOT AT TEL AVIV UNIVERSITY LTD.
    Inventors: Roni Scherzer, Ehud Gazit, Daniel Segal
  • Patent number: 7977387
    Abstract: The invention provides novel compounds according to formula I relates to compounds with the general formula I said compounds being useful, e.g. in the treatment of inflammatory, ophthalmic diseases or cancer.
    Type: Grant
    Filed: July 9, 2004
    Date of Patent: July 12, 2011
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang, Søren Christian Schou, Sophie Elisabeth Havez, Thomas Peter Sabroe
  • Patent number: 7947743
    Abstract: The present invention relates to the use of agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, on its own or in association, in obtaining medicaments intended for the treatment of bipolar disorders, especially bipolar disorders of types I and II, and more especially bipolar disorders of type I.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: May 24, 2011
    Assignee: Les Laboratories Servier
    Inventors: Christian De Bodinat, Elisabeth Mocaer
  • Publication number: 20110039819
    Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: April 9, 2009
    Publication date: February 17, 2011
    Inventors: Marion Hitchcock, Ingo Hartung
  • Publication number: 20100292324
    Abstract: The present invention relates to multi-substituted m-diarylanilines or pharmaceutically acceptable salts thereof, wherein X, R1-R7 are as defined in the claims, their preparation process, pharmaceutical compositions comprising them and their use for the manufacture of a medicament for anti-HIV.
    Type: Application
    Filed: October 7, 2008
    Publication date: November 18, 2010
    Inventors: Lan Xie, Bingjie Qin, Kou-Hsiung Lee, Shibo Jiang, Hong Lu
  • Patent number: 7829597
    Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: September 29, 2004
    Date of Patent: November 9, 2010
    Assignee: Merck, Sharp & Dohme, Inc.
    Inventors: Philippe G. Nantermet, Hemaka Anthony Rajapakse, Harold G. Selnick
  • Publication number: 20100267773
    Abstract: The present invention relates to methods of treating androgen deprivation therapy (ADT) induced hot flashes and severe hot flashes in a subject.
    Type: Application
    Filed: February 23, 2010
    Publication date: October 21, 2010
    Inventors: James T. DALTON, Mitchell S. Steiner, Jeetendra Eswaraka
  • Patent number: 7799338
    Abstract: Plaster for topical use having an analgesic activity and at the same time being able to re-absorb haematomas, comprising: a substrate layer; an adhesive layer in the form of a hydrogel matrix containing a pharmaceutically acceptable diclofenac salt, heparin or a heparinoid; a protective film which can be removed at the moment of use.
    Type: Grant
    Filed: October 4, 2004
    Date of Patent: September 21, 2010
    Assignee: Altergon SpA
    Inventors: Elisabetta Donati, Irina Rapaport
  • Publication number: 20100203134
    Abstract: The invention relates to a directly-compressible gastro-resistant spheroid. The spheroid comprises: (i) a core containing one or more active substances; (ii) a flexible, deformable film which directly coats the aforementioned core and which comprises an enteric polymer and a mixture of saturated and/or unsaturated polyglycosylated glycerides, the fatty acids of which include at least 8 carbon atoms; and (iii) an outer water-dispersible layer containing at least one disintegrating agent. The invention further relates to multiparticular tablets comprising said spheroids.
    Type: Application
    Filed: April 23, 2010
    Publication date: August 12, 2010
    Applicant: Ethypharm
    Inventors: Philippe Chenevier, Dominique Marechal
  • Patent number: 7772258
    Abstract: An agent for the treatment of allergic eye disease containing a 3-anilino-2-cycloalkenone derivative having the formula (I): wherein R1 is an unsubstituted or substituted C1 to C8 alkyl group provided that an unsubstituted methyl group is excluded, a C3 to C7 cycloalkyl group, a C6 to C10 bicycloalkyl group or an indanyl group, etc., R2 is a C1 to C4 alkyl group, R3 is a hydrogen atom, a C1 to C5 alkyl group, a C3 to C7 cycloalkyl group, etc., R4 is a hydrogen atom, an unsubstituted or substituted C1 to C5 alkyl group, a halogen atom, etc., R5, R6, R7 and R8 are independently a hydrogen atom, a C1 to C5 alkyl group, etc., X is —(CR11R12)n— or NR13—, wherein n is 0 to 2, R11, R12 and R13 are independently a hydrogen atom, a C1 to C5 alkyl group, etc.
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: August 10, 2010
    Assignee: Nikken Chemicals Co., Ltd.
    Inventors: Shinji Ina, Akane Takahama
  • Patent number: 7754772
    Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.
    Type: Grant
    Filed: May 23, 2005
    Date of Patent: July 13, 2010
    Assignee: NicOx, S.A.
    Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
  • Publication number: 20100113608
    Abstract: Disclosed herein are novel compounds and pharmaceutical compositions comprising these compounds. In some embodiments, the compounds are inhibitors of the tryptase enzyme and are useful for treating allergic rhinitis, asthma, vascular injury (e.g., restenosis and atherosclerosis), inflammatory bowel disease, arthritis, psoriasis, anaphylaxis, wounds, infections, and other allergy and inflammatory related diseases.
    Type: Application
    Filed: November 3, 2009
    Publication date: May 6, 2010
    Inventors: Randall S. Alberte, William P. Roschek, JR.
  • Patent number: 7696251
    Abstract: A neuronal cell death induced by an oxidative glutamate toxicity is substantially inhibited by administrating to an mammal an effective amount of a phenylenediamine derivative compound of formula (I), wherein R is phenyl or butyl.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: April 13, 2010
    Assignee: Incorporated National University Iwate University
    Inventor: Takumi Satoh
  • Publication number: 20100086495
    Abstract: The present invention provides transmucosal pharmaceutical or nutraceutical compositions and methods for enhancing transmucosal delivery of pharmaceutical and nutraceutical ingredients through use of methylsulfonylmethane (MSM) as a transmucosal delivery enhancer. In particular, the invention provides transmucosal compositions comprising an active agent selected from a non-steroid anti-inflammatory drug (NSAID); an analgesic; a migraine medication; a menopause medication; a sleep disorder medication; an erectile dysfunction medication, an appetite suppressant, a vitamin, a food supplement and a macromolecule. In certain particular exemplary formulations the appetite suppressant is DL-phenylalanine, and the vitamin is B12.
    Type: Application
    Filed: February 14, 2008
    Publication date: April 8, 2010
    Applicant: DERMA-YOUNG LTD.
    Inventor: Yosef Rubinstein
  • Publication number: 20100034894
    Abstract: A method of making a granulation comprising the steps of (a) combining sucralose, a polar solvent, a wettable material and an active agent, thereby forming a mixture; and (b) drying the mixture, thereby forming the granulation.
    Type: Application
    Filed: August 7, 2009
    Publication date: February 11, 2010
    Inventors: Christopher E. Szymczak, Ryan Snyder, Kristin Costello
  • Publication number: 20100029624
    Abstract: A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.
    Type: Application
    Filed: July 16, 2009
    Publication date: February 4, 2010
    Applicant: King's College London
    Inventors: Nnaemeka Ikechukwu AMOBI, Ian Christopher SMITH
  • Publication number: 20090074887
    Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 19, 2009
    Applicant: Bayer CropScience AG
    Inventors: Wilhelm Brandes, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Kruger
  • Publication number: 20080269105
    Abstract: Formulations of drugs and crystalline side chain polymers to provide controlled and/or sustained release drug formulations.
    Type: Application
    Filed: December 4, 2007
    Publication date: October 30, 2008
    Inventors: David Taft, Steven Bitler, Qiang Zheng, Adam Bell, Stelios Tzannis
  • Publication number: 20080187581
    Abstract: A solid pharmaceutical dosage form comprises a substrate containing an active agent and a solid composition deposited onto areas of a surface of the substrate and containing an active agent.
    Type: Application
    Filed: March 16, 2006
    Publication date: August 7, 2008
    Inventors: Subhash Pandurang Gore, Verma Sanjay, Vijay Dinanath Nasare, Indu Bhushan, Venkata Nookaraju Sreedharala, Harshal Prabhakar Bhagwatwar, Mailatur Sivaraman Mohan
  • Publication number: 20080103212
    Abstract: Techniques for melting and forming aerosols from solid diphenylamine are disclosed. Solid diphenylamine in block, flake or powder form is convenient to ship and to handle. Solid diphenylamine is melted by controlled techniques to form a substantially pure liquid stream of diphenylamine. The molten or liquid stream of diphenylamine is converted to an aerosol of diphenylamine either by a pressurized, hot air stream or by a combustion gas stream.
    Type: Application
    Filed: October 27, 2006
    Publication date: May 1, 2008
    Inventor: Sukas Wartanessian
  • Patent number: 7226949
    Abstract: The present invention provides pharmaceutical preparations and the uses thereof for preventing and/or treating seizures and other electroconvulsive disorders by administering a pharmaceutically effective amount of a therapeutic compound having the following formula (I): Embodiments include administering an effective amount of 4,4?-thiodianiline, 4,4?-diaminobenzophenone, 4,4?-methylenedianiline, 4,4?-diaminodiphenyl ether, or (3-aminophenyl)-(4-aminophenyl) amine, an analog, or a pharmaceutically accepted salt or complex thereof to a mammal in need of treatment or prevention of epilepsy, seizure, or other electroconvulsive disorder.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: June 5, 2007
    Assignee: University of Kentucky
    Inventors: Peter A. Crooks, Aimee Karis Bence, David Robert Worthern
  • Patent number: 6972287
    Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: December 6, 2005
    Assignee: Pfizer Inc.
    Inventors: Corinne Elizabeth Augelli-Szafran, Mark Robert Barvian, Christopher Franklin Bigge, Shelly Ann Glase, Shunichiro Hachiya, John Steven Kiely, Takenori Kimura, Yingjie Lai, Annette Theresa Sakkab, Mark James Suto, Larry Craswell Walker, Tomoyuki Yasunaga, Nian Zhuang
  • Patent number: 6924313
    Abstract: The invention relates to substituted tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid trans: protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: August 2, 2005
    Assignee: Pfizer Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Melvin L. Rueppel, Deborah A. Mischke, Barry L. Parnas
  • Patent number: 6835719
    Abstract: An environmentally safe pesticidal liquid suspension composition including a mixture of sulfur combined with pyrethrins and/or pyrethroids is provided. The pesticidal composition is effective to control plant diseases, as well as insect and mite pests. The composition can be prepared as concentrated or ready-to-use formulations. Formulations can be applied to plants, both indoors and outdoors, to control plant disease and insect and mite pests and reduce plant damage from such pests. The formulations can be applied to plants with minimal phytotoxicity (plant damage) and do not leave unacceptable levels of visible sulfur residue.
    Type: Grant
    Filed: December 18, 2002
    Date of Patent: December 28, 2004
    Assignee: W. Neudorff GmbH KG
    Inventors: Diana L. Parker, George S. Puritch, David S. Almond, Frederick S. Sedun, Cameron D. Wilson
  • Patent number: 6803388
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N,N-bis-phenyl aminoalcohols. A preferred specific (R)-Chiral N,N-bis phenyl aminoclcohol is the compound.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: October 12, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6765023
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: July 20, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6683099
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted cycloalkyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 27, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6677380
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted mercapto amines.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6677382
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-bis-phenyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6608109
    Abstract: A composition for stimulating muscle growth, comprising an effective amount of L-arginine or a salt thereof, a pH control agent for controlling the pH at less than 7 and a pharmaceutically acceptable carrier. A method of using the composition to achieve muscle growth or an immune response is also described.
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: August 19, 2003
    Inventor: Ann de Wees Allen
  • Patent number: 6593347
    Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
    Type: Grant
    Filed: August 27, 2001
    Date of Patent: July 15, 2003
    Assignee: NitroMed, Inc.
    Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang
  • Patent number: 6592891
    Abstract: Plaster for topical use having an analgesic activity and at the same time being able to re-absorb haematomas, comprising: a substrate layer; an adhesive layer in the form of a hydrogel matrix containing a pharmaceutically acceptable diclofenac salt, heparin or a heparinoid; a protective film which can be removed at the moment of use.
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: July 15, 2003
    Assignee: Altergon S.A.
    Inventors: Elisabetta Donati, Irina Rapaport
  • Patent number: 6495567
    Abstract: A method and product for treating and preventing diarrhea and scours is provided. The method involves treating a subject who has diarrhea, or scours, or is at risk of getting diarrhea or scours with an aromatic compound of the invention. The products of the invention are a veterinary preparation of the aromatic compound of the invention and an anti-scours agent, and a pharmaceutical preparation of the aromatic compound of the invention and an anti-diarrheal agent.
    Type: Grant
    Filed: September 23, 1998
    Date of Patent: December 17, 2002
    Assignees: Beth Israel Deaconess Medical Center, Children's Medical Center Corporation
    Inventors: Wayne I. Lencer, Carlo Brugnara, Seth Alper
  • Publication number: 20020177626
    Abstract: The present invention provides a new composition for treating pain-associated sleep disturbances, especially shortened sleep duration, comprising ibuprofen and diphenhydramine. The composition is further prepared as a bilayer tablet or caplet, or alternatively as a soft gelatin capsule composition, to prevent interaction between the active ingredients.
    Type: Application
    Filed: January 17, 2002
    Publication date: November 28, 2002
    Inventors: Graham D. Cook, Todd S. Koch, David H. Giamalva, Justin Bianco, James J. Fort, Geraldine Doyle, Steven Cooper
  • Patent number: 6476057
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted cycloalkyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: November 5, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6462092
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: October 8, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel