Sulfoxy Patents (Class 562/429)
  • Publication number: 20150105581
    Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Inventors: Yasumichi FUKUDA, Yoshikazu ASAHINA, Masanori TAKADOI, Masanori YAMAMOTO
  • Patent number: 8871971
    Abstract: The invention provides compositions comprising sulindac, R-epimer sulindac, S-epimer sulindac, derivatives, metabolites, and structural analogs thereof which protect normal cells against damage caused by solar rays, oxidative damage, environmental factors, diseases and organisms.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: October 28, 2014
    Assignee: CHS Pharma, Inc.
    Inventors: Herbert Weissbach, Nathan Brot
  • Publication number: 20140187786
    Abstract: Compounds that are 1,3,4-trisubstituted benzenes which modulate (e.g., inhibit) the activity of ?-secretase. The compounds are expected to reduce the level of A?42 in patients and be useful in the treatment of diseases (e.g., Alzheimer's disease) characterized by elevated levels of A?42 and/or the formation of A? plaques.
    Type: Application
    Filed: July 18, 2013
    Publication date: July 3, 2014
    Applicant: EnVivo Pharmaceuticals, Inc.
    Inventors: Gideon Shapiro, Richard Chesworth
  • Publication number: 20140058125
    Abstract: There is provided novel fluoro-substituted compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
    Type: Application
    Filed: April 3, 2012
    Publication date: February 27, 2014
    Applicant: SYDDANSK UNIVERSITET
    Inventors: Trond Ulven, Elisabeth Christiansen
  • Patent number: 8487128
    Abstract: The invention provides compositions comprising sulindac, R-epimer sulindac, S-epimer sulindac, derivatives, metabolites, and structural analogs thereof which protect normal cells against damage caused by solar rays, oxidative damage, environmental factors, diseases and organisms.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: July 16, 2013
    Assignee: CHS Pharma, Inc.
    Inventors: Herbert Weissbach, Nathan Brot
  • Patent number: 8415394
    Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: April 9, 2013
    Assignee: Astrazeneca AB
    Inventors: Timothy Jon Luker, Rukhsana Tanseem Mohammed, Mark Dickinson, Stephen Thom
  • Publication number: 20130066093
    Abstract: The present invention relates to metal (II) coordination polymers and synthesizing method therefore, and particularly relates to metal (II) coordination polymers, in which divalent metal ions are Mg, Ca, Sr, Mn, or Zn and organic ligands are 4,4?-sulfonyldibenzoic acids (H2SBA), and synthesizing method therefore.
    Type: Application
    Filed: November 16, 2011
    Publication date: March 14, 2013
    Applicant: CHUNG YUAN CHRISTIAN UNIVERSITY
    Inventors: Chia-Her LIN, Chun-Ting YEH
  • Publication number: 20130053364
    Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: April 23, 2012
    Publication date: February 28, 2013
    Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
  • Publication number: 20130018202
    Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.
    Type: Application
    Filed: January 11, 2012
    Publication date: January 17, 2013
    Applicant: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
  • Patent number: 8349897
    Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: January 8, 2013
    Assignee: Astrazeneca AB
    Inventors: Timothy Jon Luker, Rukhsana Tanseem Mohammed, Mark Dickinson, Stephen Thom
  • Patent number: 8247602
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: August 21, 2012
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda
  • Publication number: 20120204763
    Abstract: An object of the present invention is to provide a recording material that is excellent in color-developing properties and background and image stabilities, and a compound used therein. The present invention relates to a compound represented by the formula (I) [wherein R11 to R14 each independently represent a halogen atom or the like; n, p, q, and r each independently represent 0 or any integer of 1 to 4; m represents 0 or any integer of 1 to 2; a represents any integer of 1 to 10; R2 represents a hydrogen atom or the like; R3 represents an OR51 group or the like; and R41 and R42 each independently represent a hydrogen atom or the like], a composition containing the compound, a method for producing the compound, a recording material containing at least one compound represented by the formula (I), and a recording sheet having the recording material.
    Type: Application
    Filed: September 28, 2010
    Publication date: August 16, 2012
    Inventors: Toshio Aihara, Hiroshi Sakai, Shuntaro Kinoshita, Satoshi Kodama, Tadahiro Kondo, Kazumi Jyujyo
  • Publication number: 20120178732
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 6, 2011
    Publication date: July 12, 2012
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Publication number: 20120178814
    Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 21, 2011
    Publication date: July 12, 2012
    Inventors: Timothy Jon Luker, Rukhsana Tanseem Mohammed, Mark Dickinson, Stephen Thom
  • Patent number: 8193121
    Abstract: 2-(3-Alkylthiobenzoyl)cyclohexanediones of the formula (I) are described as herbicides. In this formula (I), X, Y, R1 to R8 represent radicals such as hydrogen, organic radicals such as alkyl and alkoxy.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: June 5, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Andreas Almsick, Jan Dittgen, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Stefan Lehr, Dieter Feucht
  • Patent number: 8163727
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: April 24, 2012
    Assignee: AstraZeneca AB
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Publication number: 20120021904
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Application
    Filed: July 20, 2011
    Publication date: January 26, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Hartmut AHRENS, Dieter FEUCHT, Elmar GATZWEILER, Isolde HAUSER-HAHN, Christopher Hugh ROSINGER
  • Publication number: 20120021903
    Abstract: A description is given of 4-(4-haloalkyl-3-thiobenzoyl)pyrazoles of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl.
    Type: Application
    Filed: July 20, 2011
    Publication date: January 26, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: HARTMUT AHRENS, ELMAR GATZWEILER, ISOLDE HÄEUSER-HAHN, CHRISTOPHER HUGH ROSINGER
  • Patent number: 8093386
    Abstract: There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: January 10, 2012
    Assignee: Bracco Imaging S.p.A
    Inventors: Armando Rossello, Elisabetta Orlandini, Aldo Balsamo, Laura Panelli, Elisa Nuti
  • Patent number: 8093253
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.
    Type: Grant
    Filed: February 23, 2009
    Date of Patent: January 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Romyr Dominique, Robert Alan Goodnow, Jr., Agnieszka Kowalczyk, Jianping Lou, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Patent number: 8071807
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: December 6, 2011
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns
  • Publication number: 20110288066
    Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
    Type: Application
    Filed: February 9, 2010
    Publication date: November 24, 2011
    Applicant: MERCK SERONO S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Christophe Cleva, Adeline Pretre
  • Publication number: 20110281898
    Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: July 26, 2011
    Publication date: November 17, 2011
    Inventors: Roger Victor Bonnert, Anil Patel, Stephen Thom
  • Publication number: 20110282070
    Abstract: A benzoylpyrazole compound represented by the formula (I) or its salt: wherein R1 is alkyl or cycloalkyl, R2 is a hydrogen atom or alkyl, R3 is alkyl; cycloalkyl; haloalkyl; alkoxyalkyl; alkoxycarbonylalkyl; alkenyl; or arylalkyl which may be substituted by R8, R4 is alkyl; haloalkyl; alkoxy; halogen; nitro; cyano; alkylthio; alkylsulfinyl; or alkylsulfonyl, R5 is a hydrogen atom; alkyl; alkenyl; alkynyl; halogen; cyano; cyanoalkyl; cyanoalkeny; haloalkyl; alkoxyalkyl; haloalkoxyalkyl; amino(thiocarbonyl)alkyl which may be substituted by at least one substituent selected from alkyl, cyano, is cyanoalkyl, (alkylthio)carbonylalkyl, alkyl(thiocarbonyl)alkyl, —C(O)OR7 and —C(O)SR7; thiocyanatoalkyl; alkoxy; alkenyloxy; alkynyloxy; haloalkoxy; alkoxyalkoxy; haloalkoxyalkoxy; alkoxyhaloalkoxy; haloalkoxyhaloalkoxy; alkoxyalkoxyalkyl; alkylthio; alkoxyalkylthio; haloalkoxyalkylthio; alkoxyhaloalkylthio; haloalkoxyhaloalkylthio; alkylthioalkylthio; haloalkylthioalkylthio; alkylthiohaloalkylthio; haloalkylthiohalo
    Type: Application
    Filed: July 21, 2011
    Publication date: November 17, 2011
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Hiroshi SHIMOHARADA, Masamitsu Tsukamoto, Masahiko Ikeguchi, Hiroshi Kikugawa, Makiko Sano, Yoshinori Kitahara, Hidemasa Kominami, Tatsuya Okita
  • Patent number: 8022248
    Abstract: The invention relates to substituted acids of formula (I), where T, W, X, Y, Z, R1 and R2 as defined in the claims, as useful pharmaceutical compounds for treating asthma and rhinitis, pharmaceutical compositions containing them, and a processes for their preparation.
    Type: Grant
    Filed: July 6, 2005
    Date of Patent: September 20, 2011
    Assignee: AstraZeneca AB
    Inventors: Roger Victor Bonnert, Stephen Thom, Anil Patel, Timothy Jon Luker
  • Patent number: 8008350
    Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Grant
    Filed: October 5, 2006
    Date of Patent: August 30, 2011
    Assignee: AstraZeneca AB
    Inventors: Timothy Jon Luker, Rukhsana Tasneem Mohammed, Mark Dickinson, Stephen Thom
  • Publication number: 20110190227
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists Of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: July 2, 2009
    Publication date: August 4, 2011
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns, Jeffrey Roger Roppe
  • Publication number: 20110160211
    Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).
    Type: Application
    Filed: April 27, 2009
    Publication date: June 30, 2011
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
  • Publication number: 20110118354
    Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula, (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein T, W, X, Y, Z, R1, R2, R4 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula, (I) are disclosed.
    Type: Application
    Filed: July 14, 2009
    Publication date: May 19, 2011
    Inventors: Percy H. Carter, Gregory D. Brown, George V. De Lucca, Douglas G. Batt, Rui-Qin Liu, Feng Qiu
  • Publication number: 20110105781
    Abstract: This invention relates to processes for preparing long-chain fatty acids of Formula I: and salts thereof, as well as intermediates for the processes, wherein L1 and L2 are described herein.
    Type: Application
    Filed: August 30, 2010
    Publication date: May 5, 2011
    Applicant: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH
    Inventors: Abdul H. Fauq, Albert O. Edwards
  • Publication number: 20110053779
    Abstract: 2-(3-Alkylthiobenzoyl)cyclohexanediones of the formula (I) are described as herbicides. In this formula (I), X, Y, R1 to R8 represent radicals such as hydrogen, organic radicals such as alkyl and alkoxy.
    Type: Application
    Filed: July 27, 2010
    Publication date: March 3, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Hartmut AHRENS, Andreas VAN ALMSICK, Jan DITTGEN, Christopher Hugh ROSINGER, Isolde HÄEUSER-HAHN, Stefan LEHR, Dieter FEUCHT
  • Publication number: 20110053974
    Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.
    Type: Application
    Filed: September 29, 2010
    Publication date: March 3, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
  • Publication number: 20110040105
    Abstract: Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.
    Type: Application
    Filed: April 15, 2009
    Publication date: February 17, 2011
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Christian H. Huber, Young Mi Khulman, Sagun K. Tandel, Stephen R. Johannsen, Tingmin Wang, Paul Angell
  • Publication number: 20110040091
    Abstract: The present invention relates to a process for the preparation of (R)-2-phenyl propionic acid derivatives of the formula wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen, or of a salt thereof.
    Type: Application
    Filed: July 26, 2010
    Publication date: February 17, 2011
    Inventors: Stephan Bachmann, Alec Fettes, Michelangelo Scalone
  • Patent number: 7879907
    Abstract: Novel 3-phenylpropanoic acid compounds have the general formula (I) below: and are formulated into pharmaceutical compositions for administration in human or veterinary medicine (in dermatology, and also in the field of cardiovascular diseases, immune diseases and/or lipid metabolism-related diseases), or, alternatively, into cosmetic compositions.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: February 1, 2011
    Assignee: Galderma Research & Development
    Inventors: Jean-Guy Boiteau, Laurence Clary, Jean-Claude Pascal, Veronique Parnet
  • Patent number: 7863482
    Abstract: A method for reducing the cyanide levels in a mesotrione sample, said method comprising: (i) taking an aqueous solution of the mesotrione sample in an aqueous solvent, (ii) adjusting the pH of said aqueous solution to a value of 9.5 or higher, and (iii) crystallising the mesotrione out of solution is disclosed.
    Type: Grant
    Filed: March 3, 2005
    Date of Patent: January 4, 2011
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Alan Henry Benke, Julie Marie Wichert
  • Publication number: 20100240678
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.
    Type: Application
    Filed: March 10, 2010
    Publication date: September 23, 2010
    Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Patent number: 7737135
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: June 15, 2010
    Assignee: AstraZeneca AB
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Publication number: 20100125058
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein W, X, Y, and R1-R7 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Application
    Filed: November 9, 2009
    Publication date: May 20, 2010
    Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Eric Mertz, Sung-Sau So, Hong Ying Yun, Zhenshan Zhang
  • Publication number: 20100120727
    Abstract: In one aspect, the present invention provides a composition of a covalent conjugate of an eflornithine analog with an anti-inflammatory drug. In another aspect, the present invention provides a composition of an eflornithine prodrug. In another aspect, the present invention provides a composition of an eflornithine or its derivatives aspirin salt. In another aspect, the present invention provides methods for treating or preventing cancer using the conjugates or salts of eflornithine analogs or eflornithine prodrugs.
    Type: Application
    Filed: November 12, 2009
    Publication date: May 13, 2010
    Applicant: Kyphia Pharmaceuticals, Inc.
    Inventor: Feng Xu
  • Patent number: 7687541
    Abstract: The invention encompasses the novel compounds of Formula (I) and Formula (II), which are prodrugs that convert in vivo to diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. These prodrugs are far more soluble in aqueous media than the active agents into which they convert, in vivo. As such compounds of Formula (I) and (II) are advantageous for, among other things intravenous administration. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula (I) and Formula (II).
    Type: Grant
    Filed: October 18, 2004
    Date of Patent: March 30, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Jeannie M. Arruda, Benito Munoz, Brian A. Stearns
  • Publication number: 20100076034
    Abstract: The present invention relates to (R,S) 2-aryl-2-fluoropropanoic acids, their single enantiomers (R) and (S), their derivatives amides and acylsulfonamides and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the treatment of damages caused by ischemia and reperfusion.
    Type: Application
    Filed: December 18, 2007
    Publication date: March 25, 2010
    Applicant: DOMPE PHA.R.MA S.P.A.
    Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta
  • Patent number: 7662993
    Abstract: The present invention is directed to labeled compounds of the formulae wherein Q is selected from the group consisting of —S(?O)—, and —S(?O)2—, Z is selected from the group consisting of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure wherein R1, R2, R3, R4 and R5 are each independently selected from the group consisting of hydrogen, a C1-C4 lower alkyl, a halogen, and an amino group selected from the group consisting of NH2, NHR and NRR? where R and R? are each independently selected from the group consisting of a C1-C4 lower alkyl, an aryl, and an alkoxy group, and X is selected from the group consisting of hydrogen, a C1-C4 lower alkyl group, and a fully-deuterated C1-C4 lower alkyl group.
    Type: Grant
    Filed: November 2, 2006
    Date of Patent: February 16, 2010
    Assignee: Los Alamos National Security, LLC
    Inventors: Marc A. Alvarez, Rodolfo A. Martinez, Clifford J. Unkefer
  • Publication number: 20090227603
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.
    Type: Application
    Filed: February 23, 2009
    Publication date: September 10, 2009
    Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Jianping Lou, Qi Qiao, Achyutharao Siddurl, Jefferson Wright Tilley
  • Publication number: 20090192163
    Abstract: The invention relates to substituted phenylacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: October 5, 2006
    Publication date: July 30, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Timothy Jon Luker, Rukhsana Tanseem Mohammed, Stephen Thom, Anil Patel
  • Publication number: 20090124828
    Abstract: ?,?-Unsaturated sulfides, sulfones, sulfoxides and sulfonamides according to Formula I: wherein Ar1, Ar2, X, n, * and R are as defined herein, are prepared by dehydration of ?-hydroxy sulfides, sulfones, sulfoxides or sulfonamides.
    Type: Application
    Filed: February 24, 2006
    Publication date: May 14, 2009
    Applicants: TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION, ONCONOVA THERAPEUTICS INC.
    Inventors: M.V. Ramana Reddy, E. Premkumer Reddy, Stanley C. Bell
  • Publication number: 20090036535
    Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: October 5, 2006
    Publication date: February 5, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Timothy Jon Luker, Rukhsana Tanseem Mohammed, Mark Dickinson, Stephen Thom
  • Patent number: 7482484
    Abstract: Disclosed are Compounds of formula I And methods of use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: January 27, 2009
    Assignee: Merck Patent GmbH
    Inventors: Nathalie Adje, Michel Brunet, Didier Roche, Jean-Jacques Zeiller, Stéphane Yvon, Valérie Guyard-Dangremont, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
  • Patent number: 7468360
    Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.
    Type: Grant
    Filed: August 8, 2007
    Date of Patent: December 23, 2008
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7453010
    Abstract: The invention relates to compounds of general formula (I): where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4)alkylphenyl group, said phenyl optionally being substituted; R3 represents an —X—R4 group—in which X represents a bond, an oxygen atom or a —CH2— group and R4 represents H or a —CR5R6—COOR7 group, where R5, R6 and R7 independently represent H or a (C1-C4)alkyl group—a phenyl group optionally substituted or fused with a dioxolane group, a —CO—NR8R9 group—where R8 represents H, a (C1-C4)alkyl group or a (C1-C4)alkyl(C1-C4)alkoxy group and R9 represents a (C1-C4)alkyl(C1-C4)alkoxy group, a —(CH2)n-A group, where n is equal to 0, 1, 2, 3 or 4 and where A represents an indolyl group, a fluorenyl group or a phenyl group which is substituted, an optiona
    Type: Grant
    Filed: May 26, 2003
    Date of Patent: November 18, 2008
    Assignee: Sanofi Aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier