Polycyclo Ring System Patents (Class 562/427)
  • Patent number: 9127103
    Abstract: The present invention relates to a polymerizable liquid crystal compound, a liquid crystal composition including the same, and an optically anisotropic body. The polymerizable liquid crystal compound according to the present invention has not only large solubility in various solvents but also high birefringence and excellent coating orientation, and thus it can provide an optically anisotropic body which is thin but superior in optical properties.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: September 8, 2015
    Assignee: LG CHEM, LTD.
    Inventors: Kyung Chang Seo, Sung-Ho Chun, Dai Seung Choi, Mi-Ra Hong, Hyeong Bin Jang
  • Publication number: 20150112035
    Abstract: The present invention relates to a polymerizable liquid crystal compound, a liquid crystal composition including the same, and an optically anisotropic body. The polymerizable liquid crystal compound according to the present invention has not only large solubility in various solvents but also high birefringence and excellent coating orientation, and thus it can provide an optically anisotropic body which is thin but superior in optical properties.
    Type: Application
    Filed: June 11, 2013
    Publication date: April 23, 2015
    Inventors: Kyung Chang Seo, Sung-Ho Chun, Dai Seung Choi, Mi-Ra Hong, Hyeong Bin Jang
  • Patent number: 9000044
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X 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: Grant
    Filed: February 14, 2013
    Date of Patent: April 7, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Tai-An Lin, Eric Mertz, Sung-Sau So, Achyutharao Sidduri, Jefferson Wright Tilley
  • 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: 20140296270
    Abstract: Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.
    Type: Application
    Filed: April 15, 2014
    Publication date: October 2, 2014
    Applicant: Baylor College of Medicine
    Inventors: David J. Tweardy, Xuejun Xu, Moses M. Kasembeli
  • Publication number: 20140235702
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Application
    Filed: October 8, 2012
    Publication date: August 21, 2014
    Inventors: Zaneta Nikolovska-Coleska, Hollis D. Showalter, Chenzhong Liao, Ramzi Mohammad, Fardokht Abulwerdi
  • Publication number: 20140206741
    Abstract: The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.
    Type: Application
    Filed: April 12, 2012
    Publication date: July 24, 2014
    Applicant: Sichuan Guokang Pharmaceutical Co., Ltd
    Inventors: Luyun Zhang, Fang Yang, Wanqi Shi, Ping Zhang, Ying Li, Shufan Yin
  • Publication number: 20140080222
    Abstract: The present invention relates to a new type of fluorescent with the following formula (I), its preparation process, and also an optical pH sensor which comprises this fluorescent dye immobilized on an analyte-permeable carrier.
    Type: Application
    Filed: March 28, 2012
    Publication date: March 20, 2014
    Applicant: SARTORIUS STEDIM BIOTECH GMBH
    Inventors: Daniel Riechers, Eberhard Wuenn
  • Publication number: 20140011129
    Abstract: A polymerizable monomer is provided which is represented by the following formula (1): wherein R1 represents a hydrogen atom or an alkyl group; A represents —CO— or —SO2—; and the moiety represented by the formula (1) is, at the part shown by an asterisk *, linked to a moiety represented by the following formula (2), at any position of a, b, c or d thereof; wherein the sites among a, b, c and d at which the moiety represented by the formula (2) is not linked to the moiety represented by the formula (1) each has a hydrogen atom or a substituent selected from the group consisting of an alkyl group, an alkoxy group and a sulfonic acid group, or any of which may connect at mutually adjoining positions to form a ring.
    Type: Application
    Filed: March 27, 2012
    Publication date: January 9, 2014
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Yasuaki Murai, Kei Inoue, Ryuji Murayama, Kazuyuki Sato, Masashi Hirose
  • Publication number: 20130324514
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Application
    Filed: May 22, 2013
    Publication date: December 5, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter HAMPRECHT, Sara FRATTINI, Iain LINGARD, Stefan PETERS
  • Publication number: 20130252890
    Abstract: The invention relates to selective oestrogen receptor modulators (SERM) and methods of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception.
    Type: Application
    Filed: June 21, 2011
    Publication date: September 26, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Tim Wintermantel, Carsten Möller, Ulrich Bothe, Reinhard Nubbemeyer, Ludwig Zorn, Dirk Kosemund, Antonius Ter Laak, Rolf Bohlmann, Lars Wortmann, Donald Bierer
  • Patent number: 8524194
    Abstract: The invention is directed to radiolabelled MMP selective compounds, a processes for the preparation thereof, and uses thereof. The derivatives of the invention have formula (I) wherein Y represents O, CH2, (CH2)2, S, NH, or C(?O)NH; X represents 1-5 substituents, wherein said substituents can be the same or different and wherein at least one of said substituents comprises a radioisotope suitable for PET and/or SPECT and/or a ?-emitter; Z is S; Q is chosen from the group consisting of 3-pyridyl and carboxyl; and R is chosen from the group consisting of C(?O)—NH—OH, (II), (III, (IV). The MMP selective compounds of the invention are selective for MMPs and can be used for the identification and treatment of unstable atherosclerotic plaques.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: September 3, 2013
    Assignee: Academisch Medisch Centrum Bij de Universiteit van Amsterdam
    Inventors: Bertha Louise Frederike Van Eck-Smit, Victorine Augustine Pinas, Albert Dirk Windhorst
  • Publication number: 20130225588
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X 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: February 14, 2013
    Publication date: August 29, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130225621
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 2, 2011
    Publication date: August 29, 2013
    Applicants: University of Toronto Mississauga, University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Patrick Gunning
  • 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: 8470884
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 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: Grant
    Filed: October 23, 2012
    Date of Patent: June 25, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Tai-An Lin, Sung-Sau So, Achyutharao Sidduri
  • Publication number: 20130116322
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 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: October 23, 2012
    Publication date: May 9, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20120309796
    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 inflammatory diseases and disorders such as, for example, asthma and COPD.
    Type: Application
    Filed: May 11, 2012
    Publication date: December 6, 2012
    Inventors: Fariborz Firooznia, Paul Gillespie, Tai-An Lin, Sung-Sau So
  • Patent number: 8318760
    Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John E. Stelmach, Keith G. Rosauer, Emma R. Parmee, James R. Tata
  • Publication number: 20120232104
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
  • Patent number: 8263656
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R4 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 at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: September 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Paul Gillespie, Robert Alan Goodnow, Jr., Tai-An Lin, Achyutharao Sidduri, Sung-Sau So, Jenny Tan
  • Publication number: 20120129902
    Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Application
    Filed: November 15, 2011
    Publication date: May 24, 2012
    Applicant: ELI LILLY AND COMPANY
    Inventors: Stephon Cornell SMITH, Renhua LI, Charles Howard MITCH, Tatiana Natali VETMAN
  • Patent number: 8163781
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R5, A, B, Q, W, and X 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 at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: April 24, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jean-Baptiste Blanc, Li Chen, Fariborz Firooznia, Paul Gillespie, Robert Alan Goodnow, Jr., Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
  • Publication number: 20120095048
    Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.
    Type: Application
    Filed: February 19, 2010
    Publication date: April 19, 2012
    Applicants: REGION MIDT JYLLAND, AARHUS UNIVERSITET
    Inventors: Henrik Amtoft Neubauer, Ove Kjaer Wiborg, Henrik Helligsø Jensen
  • Publication number: 20120015960
    Abstract: Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy.
    Type: Application
    Filed: November 23, 2009
    Publication date: January 19, 2012
    Applicants: The Industry & Academic Cooperation in Chungnam National University, Pusan National University Industry-University Cooperation Foundation
    Inventors: Bum Joon Park, Nam Chul Ha, Sun Hye Lee, Gyu Yong Song, Jee Hyun Lee
  • Publication number: 20110301200
    Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta (TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.
    Type: Application
    Filed: October 22, 2009
    Publication date: December 8, 2011
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Saurin Raval, Preeti Raval
  • Patent number: 8053598
    Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.
    Type: Grant
    Filed: May 3, 2005
    Date of Patent: November 8, 2011
    Assignee: High Point Pharmaceuticals, LLC
    Inventor: Zdenék Polivka
  • Patent number: 8008297
    Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: August 30, 2011
    Assignee: Ambrilia Biopharma Inc.
    Inventors: Brent Richard Stranix, Valerie Perron
  • Publication number: 20110201609
    Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.
    Type: Application
    Filed: June 30, 2009
    Publication date: August 18, 2011
    Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
  • Publication number: 20110184147
    Abstract: The present invention provides a substrate of TGase represented by (fluorescent group)-(linker)-(a portion containing a Gln residue capable of recognition by transglutaminase (TGase))-R, wherein the fluorescent group is fluorescein isothiocyanate (FITC), Texas Red (TE) or dansyl (Dns) or a group derived therefrom; the linker is a group represented by —NH—(CH2)n—CO— (n is an integer of 1 to 6); the portion containing a Gln residue capable of recognition by TGase is a group derived from a peptide selected from among QG and the like; and R is a hydroxyl group, or biotin, nucleic acid, azide, alkyne, maleimide or cyclopentadiene, or a group derived therefrom.
    Type: Application
    Filed: July 3, 2009
    Publication date: July 28, 2011
    Applicant: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION
    Inventors: Noriho Kamiya, Masahiro Goto, Hiroki Abe
  • Publication number: 20110124856
    Abstract: An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.
    Type: Application
    Filed: July 31, 2009
    Publication date: May 26, 2011
    Applicant: NIPPON ZOKI PHARMACEUTICAL CO., LTD.
    Inventors: Kunihiko Higashiura, Takashi Ogino, Taizo Ito, Koji Kunimasu, Kazuhito Furukawa
  • Publication number: 20100298347
    Abstract: Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.
    Type: Application
    Filed: December 1, 2008
    Publication date: November 25, 2010
    Applicant: MERCK FROSST CANADA LTD
    Inventors: Michel Belley, Denis Deschenes, Rejean Fortin, Jean-Francois Fournier, Sebastien Gagne, Yves Gareau, Jacques Yves Gauthier, Lianhai Li, Joel Robichaud, Michel Therien, Geoffrey K. Tranmer, Zhaoyin Wang
  • 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: 20100041714
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R5, A, B, Q, W, and X 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 at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Application
    Filed: August 13, 2009
    Publication date: February 18, 2010
    Inventors: Jean-Baptiste Blanc, Li Chen, Fariborz Firooznia, Paul Gillespie, Robert Alan Goodnow, JR., Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
  • Publication number: 20100041713
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R4 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 at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Application
    Filed: August 13, 2009
    Publication date: February 18, 2010
    Inventors: Fariborz Firooznia, Paul Gillespie, Robert Alan Goodnow, JR., Tai-An Lin, Achyutharao Sidduri, Sung-Sau So, Jenny Tan
  • 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
  • Patent number: 7645779
    Abstract: Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.
    Type: Grant
    Filed: August 20, 2004
    Date of Patent: January 12, 2010
    Assignees: Amgen Inc., Japan Tobacco, Inc.
    Inventors: Hiroyuki Abe, Jonathan Houze, Hisashi Kawasaki, Frank Kayser, Rajiv Sharma, Samuel Sperry
  • Publication number: 20090318703
    Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.
    Type: Application
    Filed: October 27, 2008
    Publication date: December 24, 2009
    Applicant: ONO PHARMACEUTICAL CO., LTD
    Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
  • Patent number: 7576238
    Abstract: The present invention relates to novel processes for the preparation of substituted tetralin and substituted indane derivatives. The present invention is further directed to novel processes for the preparation of intermediates in the preparation of the substituted tetralin and substituted indane derivatives.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: August 18, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Fan Zhang-Plasket, Hua Zhong, Frank Villani
  • Patent number: 7547716
    Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a physiologically acceptable salt thereof: wherein R represents an aryl-substituted alkyl group, an heteroaryl-substituted alkyl group, a cycloalkyl-substituted alkyl group, or a cyclic hydrocarbon group wherein said cyclic hydrocarbon group may be saturated, partly saturated, or aromatic; or Z may bind to R to form a cyclic structure, Z represents a hydrogen atom or a C1 to C6 alkyl group. The medicament enhanced the effect of the cancer therapy and decreases a dose of an anticancer agent and/or radiation, and therefore, can reduce side effects resulting from the cancer therapy.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: June 16, 2009
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventors: Susumu Muto, Masayuki Komukai, Akiko Itai
  • 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: 7476754
    Abstract: The present invention relates to compounds derived from biphenyl with activity as calpain inhibitors. One compound of the present invention is a 2,2?-disubstituted biphenyl, where the substituents in the 2 and 2? positions of the biphenyl skeleton are chains containing structures related to amino acids, including fragments of aminocarbonylic compounds where at least one of the substituents in said 2- or 2?-positions is bonded to the biphenyl skeleton via a thiocarbonyl group, forming compounds with thioamide functionality. The present invention also encompasses any of the conformational isomers (atropisomers) of said compound of formula I. The compounds of formula I have application in the preventive or therapeutic treatment of a degenerative disease.
    Type: Grant
    Filed: May 6, 2005
    Date of Patent: January 13, 2009
    Assignee: Consejo Superior de Investigaciones Cientificas
    Inventors: Bernardo Herradon Garcia, Mercedes Alonso Giner, Esperanza Benito Cano, Antonio Chana Lopez, Ana Montero Aguado
  • Publication number: 20090012171
    Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.
    Type: Application
    Filed: May 3, 2005
    Publication date: January 8, 2009
    Applicant: NOVO NORDISK A/S
    Inventor: Zdenek Polivka
  • Patent number: 7446222
    Abstract: Compounds of formula (I) or derivatives thereof: wherein A, B, Z, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: November 4, 2008
    Assignee: Glaxo Group Limited
    Inventors: Rino Antonio Bit, Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Neil Derek Miller, Tiziana Scoccitti
  • Patent number: 7423176
    Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: September 9, 2008
    Assignees: Cephalon, Inc., Cephalon France
    Inventors: Edward R. Bacon, Sankar Chatterjee, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet
  • Patent number: 7388008
    Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.
    Type: Grant
    Filed: August 2, 2004
    Date of Patent: June 17, 2008
    Assignee: Ambrilia Biopharma Inc.
    Inventors: Brent Richard Stranix, Valérie Perron
  • Publication number: 20080119513
    Abstract: It is considered that MMP-13 inhibitors contribute to the treatment or prevention against the diseases caused by or related to activity of MMP-13, especially osteoarthritis (OA). Therefore, the development of MMP-13 inhibitors has been desired. A compound represented by the general formula (I): wherein Z is 1,4-phenylene and the like; R1 is hydroxy and the like; R2 is hydrogen atom, optionally substituted lower alkyl, and the like; R12 is hydrogen atom; or R2 and R12 taken together with the adjacent carbon atom may form a ring; R3 is hydrogen atom, optionally substituted lower alkyl, and the like; R4 is halogen, lower alkyl, and the like; m is 0, 1, or 2; X is a bond, —C?C—, and the like; Y is optionally substituted phenyl, optionally substituted naphthyl, and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: September 6, 2004
    Publication date: May 22, 2008
    Inventors: Fumihiko Watanabe, Yoshinori Tamura, Naoki Yoshikawa
  • Patent number: 7371895
    Abstract: Organic amine salts of compounds of the formula: and their pharmaceutically acceptable salts, and uses in medical therapy are provided.
    Type: Grant
    Filed: November 1, 2005
    Date of Patent: May 13, 2008
    Assignee: AtheroGenics, Inc.
    Inventor: Charles Q. Meng
  • Patent number: 7365223
    Abstract: The invention provides novel methods for selective targeting of chemical compounds to cells undergoing a death process, in particular apoptosis, and to platelets undergoing activation during blood coagulation. The invention further provides compounds to be used in said methods for medical practice, for diagnostic and therapeutic purposes.
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: April 29, 2008
    Assignee: NST NeuroSurvival Technologies Ltd
    Inventors: Ilan Ziv, Anat Shirvan
  • Patent number: 7351825
    Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: April 1, 2008
    Assignee: Japan Tobacco Inc.
    Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro