Plural Hetero Atoms In The Hetero Ring Patents (Class 514/439)
  • Patent number: 9044439
    Abstract: Compositions containing low doses of lipoic acid-based active agents and methods for using the same are provided. In particular, compositions containing low dose lipoic acid, lipoic acid derivatives, and lipoic acid seleno-derivatives and are provided to prevent and/or treat ocular diseases.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: June 2, 2015
    Assignee: Encore Health, LLC
    Inventors: William Garner, Margaret Garner
  • Patent number: 8916183
    Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
  • Patent number: 8901176
    Abstract: New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinson's Disease are described. More specifically, the invention relates to methods for treating Parkinson's Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinson's Disease agents or treatments, such as levodopa/PDI or dopamine agonists.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: December 2, 2014
    Assignee: Newron Pharmaceuticals, S.P.A.
    Inventors: Ruggero Fariello, Carlo Cattaneo, Patricia Salvati, Luca Benatti
  • Patent number: 8883180
    Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8859612
    Abstract: The invention relates to the use of the compound hesperidin or of one of its derivatives for the manufacture of a composition designed to stimulate bone formation and/or inhibit bone resorption in man or animals.
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: October 14, 2014
    Assignee: Institut National de la Recherche Agronomique (INRA)
    Inventors: Marie-Noëlle Horcajada, Véronique Coxam, Christine Morand, Marie-Jeanne Davicco
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Publication number: 20140100242
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Application
    Filed: September 17, 2013
    Publication date: April 10, 2014
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 8673963
    Abstract: The present invention is directed to provide an efficient production method which is capable of not only obtaining a cyclic sulfonic acid ester (sultone) at low cost and in high yield, but also the sulfonic acid ester (sultone) stably even in a commercial scale. The present invention relates to a method for producing hydroxysultone comprising a first step where a diol having a specified structure and a thionyl halide are reacted to obtain a cyclic sulfite having a specified structure, and a second step where the cyclic sulfite is reacted with water or/and alcohol; a method for producing an unsaturated sultone having a specified structure comprising a third step where a hydroxylsultone having a specified structure is reacted with an acid halide or an acid anhydride to obtain an intermediate, subsequently the intermediate is treated with a base; as well as a cyclic sulfite having a specified structure.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: March 18, 2014
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Ayako Kuramoto, Kuniaki Okamoto, Tsutomu Watahiki, Motoshige Sumino
  • Patent number: 8592466
    Abstract: Treatment of humans suffering from conditions caused by higher-than-normal dopaminergic activity in basal ganglia includes administering the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: November 26, 2013
    Assignee: Neuropill, Inc.
    Inventor: Ahmed Elkashef
  • Patent number: 8568756
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: October 29, 2013
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 8541466
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: September 24, 2013
    Assignee: Duke University
    Inventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
  • Patent number: 8450336
    Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias. wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: May 28, 2013
    Assignee: NPS Pharmaceuticals, Inc
    Inventors: Guy Higgins, Abdelmalik Slassi, Methvin Isaac
  • Patent number: 8410162
    Abstract: Compounds, formulations, and methods are provided containing the choline ester of a reducing agent, especially lipoic acid or derivatives thereof. The compounds may be administered via a topical ocular route to treat or prevent oxidative damage.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: April 2, 2013
    Assignee: Encore Health LLC
    Inventors: William Garner, Margaret Garner, George Minno, David Gooden
  • Publication number: 20130078233
    Abstract: Compounds having one or more phenol moieties, derivatives thereof, compositions containing same and uses thereof for the treatment of amyloid-associated diseases are provided.
    Type: Application
    Filed: November 27, 2012
    Publication date: March 28, 2013
    Applicant: Tel Aviv University Future Technology Development L.P.
    Inventor: Tel Aviv University Future Technology Development
  • Patent number: 8372880
    Abstract: Compounds having one or more phenol moieties, derivatives thereof, compositions containing same and uses thereof for the treatment of amyloid-associated diseases are provided.
    Type: Grant
    Filed: March 23, 2006
    Date of Patent: February 12, 2013
    Assignee: Tel Aviv University Future Technology Development L.P.
    Inventors: Ehud Gazit, Yair Porat
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Patent number: 8318785
    Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.
    Type: Grant
    Filed: July 17, 2006
    Date of Patent: November 27, 2012
    Assignee: Orion Corporation
    Inventors: Marko Ahlmark, Reijo Bäckström, Anne Luiro, Jarmo Pystynen, Eija Tiainen
  • Patent number: 8282952
    Abstract: The invention relates to insect attractants containing compounds with pentagonal heterocyclic structures that are effective in attracting fruitflies.
    Type: Grant
    Filed: March 11, 2008
    Date of Patent: October 9, 2012
    Assignee: Activetrad (Proprietary) Limited
    Inventor: Christoffel J. Smit
  • Patent number: 8268862
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: September 18, 2012
    Assignee: Sirtris Pharmaceuticals, Inc.
    Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Patent number: 8263640
    Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: September 11, 2012
    Assignee: NUtech Ventures
    Inventors: Concetta Dirusso, Paul Black
  • Patent number: 8247438
    Abstract: Treatment of schizophrenia or humans suffering from conditions associated with high dopamine levels in ventral striatum or caudate nucleus administers the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.
    Type: Grant
    Filed: June 10, 2008
    Date of Patent: August 21, 2012
    Assignee: Neuropill, Inc.
    Inventor: Ahmed Elkashef
  • Patent number: 8183281
    Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: May 22, 2012
    Assignee: Novartis AG
    Inventors: Neil John Press, Simon James Watson
  • Patent number: 8168212
    Abstract: Cosmetic compositions comprising non-natural, non-proteogenic amino acids and methods of using such compositions to impart antiaging benefits to the skin are disclosed. The non-natural, non-proteogenic amino acids are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging, and in particular, are enhancers of LOXL-1.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: May 1, 2012
    Assignee: Avon Products, Inc
    Inventors: Dmitri S. Ptchelintsev, Laurence Dryer, Xiaochun Luo
  • Patent number: 8143215
    Abstract: Compositions for enhancing satiety and weight loss in an individual, assays for assessing a tastant for enhancing satiety and weight loss, and methods of using the composition to suppress appetite and enhance weight loss are provided.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: March 27, 2012
    Inventor: Alan R. Hirsch
  • Patent number: 8119686
    Abstract: A novel spiroquinone derivative having a high ABCA1 stabilization effect and being useful for prophylactic and/or therapeutic agents for various diseases developing hypo-high density lipoproteinemia is obtained. The novel spiroquinone derivative is a compound represented by the following formula: wherein R1a, R1b, R1c and R1d each represents a hydrogen atom, a halogen atom, an alkyl group which may have a substituent, or an alkoxy group which may have a substituent, and R2a and R2b each represents a hydrogen atom, or an alkyl group which may have a substituent (e.g.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: February 21, 2012
    Assignee: Hykes Laboratories LLC
    Inventors: Shinji Yokoyama, Hashime Kanazawa, Tomoji Aotsuka
  • Patent number: 8030346
    Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: April 29, 2008
    Date of Patent: October 4, 2011
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Roland Burli, Michael J. Frohn, Randall W. Hungate, Susana C. Neira, Anthony B. Reed
  • Patent number: 7973037
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: July 5, 2011
    Assignees: Axys Pharmaceuticals, Inc., Merck Canada Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
  • Patent number: 7968572
    Abstract: It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.
    Type: Grant
    Filed: October 2, 2006
    Date of Patent: June 28, 2011
    Assignee: Ono Pharmaceuticals Co., Ltd.
    Inventors: Hisao Nakai, Shingo Yamamoto, Shingo Nakatani, Tomomi Hirosaki
  • Publication number: 20110123586
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Application
    Filed: June 2, 2009
    Publication date: May 26, 2011
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 7928137
    Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.
    Type: Grant
    Filed: March 2, 2007
    Date of Patent: April 19, 2011
    Assignee: Tularik Limited
    Inventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan
  • Publication number: 20110071125
    Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 24, 2011
    Inventors: Joachim Rudolph, Jaques Dumas, Li Yingfu, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther, Benjamin Bader
  • Patent number: 7893086
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: February 22, 2011
    Assignee: Sirtris Pharmaceuticals, Inc.
    Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • 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: 20100317725
    Abstract: Compounds, formulations, and methods are provided containing the choline ester of a reducing agent, especially lipoic acid or derivatives thereof. The compounds may be administered via a topical ocular route to treat or prevent oxidative damage.
    Type: Application
    Filed: June 15, 2010
    Publication date: December 16, 2010
    Applicant: Encore Health LLC
    Inventors: William Garner, Margaret Garner, George Minno, Gooden David
  • Patent number: 7803796
    Abstract: Provided is a homopiperazine compound for inhibiting ribosomal frameshifting by binding to an RNA pseudoknot structure of SARS coronavirus. Particularly, the present invention provides a pharmaceutical composition for inhibiting synthesis of protein induced by ?1 frameshifting by binding to an RNA pseudoknot structure specifically existing in SARS coronavirus. The composition includes a therapeutically effective amount of homopiperazine compound of following chemical formula 1 or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted carrier or excipient.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: September 28, 2010
    Assignee: Sungkyunkwan University Foundation For Corporate Collaboration
    Inventors: Hyun-Ju Park, So-Jung Park, Yang-Gyun Kim
  • Publication number: 20100210683
    Abstract: There is provided a compound having an excellent controlling effect on arthropod pests represented by the formula (I-1): wherein Z represents an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; G represents a -A1-R1 group, etc.; X0 represents a -A2-R4 group, etc.; X represents a -A2-R4 group, etc.; X0 represents a -A3-R6 group, etc.; or X and X0 are optionally taken together to form a -A2-T0-A3- group; M1 represents a —R8 group, etc.; A1, A2 and A3 independently represent an oxygen atom, etc.; R1 and R8 independently represents an optionally substituted C1-C20 chain hydrocarbon group, etc.; R4 and R6 independently represent an optionally substituted C1-C6 chain hydrocarbon group, etc.; and T0 represents an optionally substituted C2-C6 alkanediyl group.
    Type: Application
    Filed: July 25, 2008
    Publication date: August 19, 2010
    Applicant: SUMITOMO CHEMICAL COMPANY LIMITED
    Inventors: Hideo Kamiyama, Shigeyuki Itoh
  • Publication number: 20100160411
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R1, R2, R3, R4, y, n, m, p, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
    Type: Application
    Filed: October 24, 2007
    Publication date: June 24, 2010
    Applicant: Wyeth
    Inventors: Gary Paul Stack, Ivana Bianchi, Stefania Vallese, Giovanna Luoni
  • Publication number: 20100029745
    Abstract: The present invention relates to compounds derived from substituted 3-phenyl-1-(thien-2-yl)propan-1-ones, pharmaceutical compositions comprising them as well as their therapeutic applications, notably in the field of human and animal health.
    Type: Application
    Filed: December 28, 2007
    Publication date: February 4, 2010
    Inventor: Jean-Francois Delhomel
  • Publication number: 20090291102
    Abstract: There are provided various compounds and compositions comprising polyunsaturated fatty acid monoglycerides and derivatives thereof. These compounds and compositions can be useful as cancer chemopreventive agents. They can also be useful for enhancing solubility of various active agents and enhancing their bioavailability.
    Type: Application
    Filed: August 5, 2009
    Publication date: November 26, 2009
    Inventor: Samuel FORTIN
  • Publication number: 20090192212
    Abstract: Dithiol compounds and derivatives thereof are disclosed. The agents are useful for treating ocular disease, especially presbyopia and cataract.
    Type: Application
    Filed: February 23, 2009
    Publication date: July 30, 2009
    Applicant: Encore Health, LLC
    Inventors: William Garner, Margaret Garner, Ronald D. Blum
  • Publication number: 20090176805
    Abstract: The present application discloses derivatives of ethylene methanedisulfonate as cancer chemotherapeutic agents and methods of synthesizing such derivatives. The derivatives include modifications of ethylene methanedisulfonate by replacing one or both of the chemically most reactive hydrogens of the cyclic sulfonate ester structure. The derivatives of ethylene methanedisulfonate are more active than the parent ester (i.e., ethylene methanedisulfonate) as anticancer agents against a variety of cancers.
    Type: Application
    Filed: November 26, 2008
    Publication date: July 9, 2009
    Inventors: Marshall W. Cronyn, Gail Marie Cronyn, Lori Ruth Cronyn
  • Publication number: 20090048315
    Abstract: A composition having sustained pain-relieving properties such that the composition may be administered to a subject to alleviate chronic pain. The composition includes an effective amount of at least one glutaminase inhibitor. A method for alleviating chronic pain in a subject for an extended period of time is also disclosed, in which the compound is administered to a subject suffering from chronic pain at a site of inflammation such that the administration of the compound results in a reduction in at least one of thermal and mechanical pain responses at the site of inflammation for a period of at least two days without any resulting acute pain behavior. The composition may further include an effective amount of at least one compound having analgesic effects such that the composition also alleviates acute pain.
    Type: Application
    Filed: May 9, 2006
    Publication date: February 19, 2009
    Inventor: Kenneth E. Miller
  • Patent number: 7435834
    Abstract: The present invention relates to compounds of 2-thia-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-?(TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.
    Type: Grant
    Filed: April 9, 2003
    Date of Patent: October 14, 2008
    Assignee: GlaxoSmithKline Istrazivacki Center Zagreb D.O.O.
    Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic, Ivana Ozimec
  • Patent number: 7417156
    Abstract: In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (I), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities.
    Type: Grant
    Filed: September 26, 2003
    Date of Patent: August 26, 2008
    Assignee: Johns Hopkins University
    Inventors: Gary H. Posner, Theresa A. Shapiro, Surojit Sur, Tanzina Labonte, Kristina Borstnik, Ik-Hyeon Paik, Andrew J. McRiner
  • Patent number: 7407987
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: November 30, 2006
    Date of Patent: August 5, 2008
    Assignee: Duke University
    Inventors: Mitchell Anthony deLong, John McMillan McIver, Robert Scott Youngquist
  • Patent number: 7388029
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: May 26, 2005
    Date of Patent: June 17, 2008
    Assignee: Duke University
    Inventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
  • Patent number: 7335673
    Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: February 26, 2008
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Yoichiro Hoshina, Satoru Ikegami, Akihiko Okuyama, Tatsuhiro Harada, Atsushi Matsuo
  • Patent number: 7288246
    Abstract: A composition having sustained pain-relieving properties such that the composition may be administered to a subject to alleviate chronic pain. The composition includes an effective amount of at least one glutaminase inhibitor. A method for alleviating chronic pain in a subject for an extended period of time is also disclosed, in which the compound is administered to a subject suffering from chronic pain at a site of inflammation such that the administration of the compound results in a reduction in at least one of thermal and mechanical pain responses at the site of inflammation for a period of at least two days without any resulting acute pain behavior. The composition may further include an effective amount of at least one compound having analgesic effects such that the composition also alleviates acute pain.
    Type: Grant
    Filed: September 13, 2002
    Date of Patent: October 30, 2007
    Assignee: The Board of Regents of the University of Oklahoma
    Inventor: Kenneth E. Miller
  • Patent number: 7262309
    Abstract: The present invention relates to benzonaphthoazulene derivatives of tiophene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumor necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: August 28, 2007
    Assignee: GlaxoSmith Kline Istrazivocki Centar Zagreb, D.O.O.
    Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic, Ivana Ozimec, Rudolf Trojko
  • Patent number: RE40558
    Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: October 28, 2008
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko