Substituent Q Contains Benzene Ring Patents (Class 564/84)
  • Patent number: 9681647
    Abstract: Provided are compositions and methods that involve cancer cells which are modified so that they can form orthotopic tumors in a non-human mammal, and wherein metastasis of the tumor can be controlled. The cancer cells, which may be human cancer cells, are modified so that expression of a human chemokine receptor can be modulated. Modulating expression of the human chemokine receptor allows selective initiation of metastasis. Kits which contain the modified cancer cells are provided. A method for identifying agents which can inhibit metastasis using non-human mammals having orthotopic tumors formed using the modified cancer cells is also included.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: June 20, 2017
    Assignee: Cornell University
    Inventors: Huanhuan Chen, Steven M. Lipkin, Xiling Shen
  • Patent number: 9085659
    Abstract: The invention provides a water-soluble polymer comprising (i) an imide group comprising a linking nitrogen atom, a first carbonyl group covalently attached to the linking nitrogen atom, and a second carbonyl group covalently attached to the linking nitrogen atom; (ii) a first water-soluble polymer segment covalently attached, either directly or through one or more atoms, to the first carbonyl group of the imide group and (iii) a second water-soluble polymer segment covalently attached, either directly or through one or more atoms, to the second carbonyl group of the imide group. The invention also provides, among other things, methods for preparing polymers, conjugates, pharmaceutical compositions and the like.
    Type: Grant
    Filed: May 3, 2005
    Date of Patent: July 21, 2015
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski
  • Patent number: 9040587
    Abstract: Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. This disclosure deals with the use of halo active aromatic sulfonamide organic compounds as odor control and/or biocidal agents in a cleaning solution for use with bovines and other dairy animals.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: May 26, 2015
    Inventors: David J. Schneider, Charles A. Schneider
  • Patent number: 9035096
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 19, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Patent number: 9000045
    Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity. the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 7, 2015
    Assignee: Japan Tobacco Inc.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • Patent number: 8889906
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: November 18, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Publication number: 20140315947
    Abstract: The present invention relates to a pharmaceutical composition for inhibiting angiogenesis and a novel sulfonyl amide derivative compound which can be useful for the prevention or treatment of angiogenesis-related diseases or disorders. Since the compound used as an active ingredient in the pharmaceutical composition of the invention is specifically bound to UQCRB and inhibits biological functions thereof, apoptosis is not induced and angiogenic responses are inhibited. Therefore, the compound used as an active ingredient in the pharmaceutical composition of the invention can be useful as an effective and safe angiogenesis inhibitory agent.
    Type: Application
    Filed: May 23, 2011
    Publication date: October 23, 2014
    Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
    Inventors: Ho Jeong Kwon, Gyoon Hee Han, Hye Jin Jung, Jeong Jea Seo
  • Publication number: 20140315954
    Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Inventors: Geoffrey C. WINTERS, Alexander L. Mandel, BRADLEY J. HEDBERG
  • Patent number: 8829052
    Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: September 9, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Patent number: 8822507
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: September 2, 2014
    Assignee: PIMCO 2664 Limited
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Patent number: 8809584
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: August 19, 2014
    Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Patent number: 8808742
    Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: August 19, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Colin Edward Rowlings
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Patent number: 8759399
    Abstract: Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. This disclosure deals with the use of halo active aromatic sulfonamide organic compounds as odor control and/or biocidal agents in a cleaning solution for use with bovines and other dairy animals.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: June 24, 2014
    Inventors: David J. Schneider, Charles A. Schneider
  • Patent number: 8754237
    Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: June 17, 2014
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: James Elliot Bradner, Ralph Mazitschek, Weiping Tang, Stuart L. Schreiber
  • Patent number: 8741960
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: June 3, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Yu Xie
  • Publication number: 20140123342
    Abstract: The role of extracellular nucleotides and apyrase enzymes in the guard cells that border stomata in regulating stomatal aperture and the plant's resistance to drought and pathogens is disclosed herein. Expression of apyrases APY1 and APY2, in guard cell protoplasts is strongly correlated with cell growth, cell secretory activity and with conditions that favor stomatal opening. Both short-term inhibition of ectoapyrase activity and long-term suppression of APY1 and APY2 transcript levels significantly disrupt normal stomatal behavior in light. Furthermore, two punnoceptor inhibitors in mammals, pyridoxalphosphate-6-azo-phenyl-2?,4?-disulphonic acid (PPADS) and Reactive Blue 2, block ATPS- and ADP?S-induced opening and closing, and also partially block the ability of abscisic acid (ABA) to induce stomatal closure, and light-induced stomatal opening.
    Type: Application
    Filed: June 1, 2012
    Publication date: May 1, 2014
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Stanley J. Roux, Iris Steinebrunner, Gregory B. Clark
  • Patent number: 8648116
    Abstract: This invention concerns N-(2-arylamino) aryl sulfonamide compounds which are inhibitors of MEK including crystalline polymorphic forms which exhibit a specific powder x-ray diffraction profile and/or a specific differential scanning calorimetry profile. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer, hyperproliferative diseases and inflammatory conditions. The invention also concerns methods of making the compounds and compositions described herein.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: February 11, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Michel Vernier, Colin Edward Rowlings, Jean-Luc Girardet, Stuart Dimock, Barry Quart, Jeffrey N. Miner
  • Publication number: 20140038822
    Abstract: Use of substituted spirocyclic sulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof for enhancement of stress tolerance in plants. The invention relates to the use of spirocyclic sulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof of the formula (I) in which the respective substituents have the meanings given in the description, for increasing stress tolerance in plants with respect to abiotic stress, and also for increasing plant growth and/or for increasing plant yield.
    Type: Application
    Filed: December 27, 2011
    Publication date: February 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jens Frackenpohl, Lothar Willms, Thomas Müller, Stefan Lehr, Pascal Von Koskull-Döring, Ines Heinemann, Christopher Hugh Rosinger, Isolde Häuser-hahn, Martin Jeffrey Hills
  • Patent number: 8642808
    Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: February 4, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
  • Patent number: 8642761
    Abstract: The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 4, 2014
    Assignee: Wilex AG
    Inventors: Hugo Ziegler, Peter Wikstroem
  • Patent number: 8623859
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: January 7, 2014
    Assignee: Evotec AG
    Inventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xiaolu Wang
  • Patent number: 8569543
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: October 29, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20130245018
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).
    Type: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Applicant: PIMCO 2664 LIMITED
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Publication number: 20130236969
    Abstract: Use of a compound of Formula 1 for inducing differentiation of mesenchymal stem cells to chondrocytes, and a pharmaceutical composition for treating a cartilage disease, which includes chondrocytes in which differentiation from mesenchymal stem cells is induced by the compound of Formula 1, are provided. Differentiation of the mesenchymal stem cells treated with the compound of Formula 1 to chondrocytes is specifically induced, and thus the compound can be used to effectively treat a cartilage disease such as arthritis, cartilage damage, and a cartilage defect.
    Type: Application
    Filed: September 16, 2011
    Publication date: September 12, 2013
    Applicant: Industry-Academic Cooperation Foundation, Yonsei University
    Inventors: Ki Chul Hwang, Yang Soo Jang, Gyoon Hee Han
  • Patent number: 8524778
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as ‘BPSAAA compounds’), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: September 3, 2013
    Assignee: PIMCO 2664 Limited
    Inventors: Iain Robert Greig, Robert Jurgen Van't Hof, Stuart Hamilton Ralston
  • Patent number: 8461209
    Abstract: The invention provides a sulfonyl malonamide derivative, or a pharmacologically acceptable salt thereof or a solvate thereof, that has therapeutic and/or preventive effects(s) on various diseases due to its agonist action at AT2 receptor, and is useful as a pharmaceutical agent for the treatment and/or prevention of diseases involving the renin-angiotensin-aldosterone system (RAAS).
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: June 11, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Tomohiro Yoshida, Hiroshi Sakashita, Atsushi Numata, Saori Tahara, Hisashi Kawasumi
  • Patent number: 8450367
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Grant
    Filed: December 9, 2011
    Date of Patent: May 28, 2013
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8425890
    Abstract: An odor-controlling bodily fluid absorbent member comprises (a) an absorbent material or substrate; and (b) a halo active aromatic sulfonamide compound of Formula (I): wherein R1, R2, R3, R4, R5, X, M, and n are as described herein; and wherein at least one of R1, R2, R3, R4, and R5 is not hydrogen. The absorbent member effectively controls odor arising from various body fluids.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: April 23, 2013
    Inventors: David J. Schneider, Charles A. Schneider
  • Publication number: 20130040975
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Applicant: NEUROCRINE BIOSCIENCES, INC.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
  • Patent number: 8314148
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: November 20, 2012
    Assignee: Novartis AG
    Inventors: Thomas Leutert, Jonathan E. Grob, Ruben Alberto Tommasi, Erin Keaney, Ayako Honda
  • Publication number: 20120245348
    Abstract: Disclosed herein are phosphine compounds represented by the general formula (4): and corresponding phosphonium salts represented by the general formula (4a): Also disclosed are processes for the preparation of these phosphines and phosphonium salts as well as their use as ligands in catalytic reactions.
    Type: Application
    Filed: April 2, 2012
    Publication date: September 27, 2012
    Inventors: Herbert PLENIO, Christoph FLECKENSTEIN, Renat KADYROV, Juan ALMENA, Axel MONSEES, Thomas RIERMEIER
  • Patent number: 8257611
    Abstract: A compound of formula (1): wherein A1 and A2 are —O—, —NR—, —S—, or —CO—, in which R is a hydrogen atom or substituent; Z is one or two atoms selected from a carbon atom or a non-metal atom of Group 14, 15 or 16 in the Periodic Table, and forms a five- or six-membered ring with the C—C?C—C or C?C—C?C; R1, R2, and R3 each are a substituent; m is an integer of 0 to 4; L1 and L2 are a single bond or divalent linking group; X is a non-metal atom of Group 14, 15 or 16 in the Periodic Table, and may have a hydrogen atom or R4; and at least one of R, R1, R2, R3, and R4 is substituted with a polymerizable group; a liquid crystal composition, an optical film, a retardation sheet, a polarizing plate, and a liquid crystal display.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: September 4, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Shigeki Uehira, Michitaka Matsuumi, Shinichi Morishima, Mitsuyoshi Ichihashi, Kotaro Yasuda, Hiroshi Takeuchi
  • Patent number: 8236987
    Abstract: The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs are disclosed, including pharmaceutical formulations of the disclosed novel compounds in useful compositions.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: August 7, 2012
    Assignees: The Regents of the University of California, Oregon Health & Science University
    Inventors: Thomas S. Scanlan, Toru Iijima
  • Publication number: 20120196884
    Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).
    Type: Application
    Filed: June 14, 2010
    Publication date: August 2, 2012
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
  • Patent number: 8232427
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Grant
    Filed: March 27, 2007
    Date of Patent: July 31, 2012
    Assignee: Novartis AG
    Inventors: Thomas Leutert, Jonathan E Grob, Ruben Alberto Tommasi, Erin E. Pusateri, Ayako Honda
  • Patent number: 8222423
    Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
    Type: Grant
    Filed: February 14, 2007
    Date of Patent: July 17, 2012
    Assignees: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard College, Howard Hughes Medical Institute
    Inventors: James Elliot Bradner, Ralph Mazitschek, Tang Weiping, Stuart S. Schreiber
  • Publication number: 20120149909
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Application
    Filed: December 21, 2011
    Publication date: June 14, 2012
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Publication number: 20120142917
    Abstract: Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl4. The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.
    Type: Application
    Filed: September 6, 2011
    Publication date: June 7, 2012
    Applicants: H. Lee Moffitt Cancer Center and Research Institute, Inc., UNIVERSITY OF SOUTH FLORIDA
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
  • Patent number: 8138218
    Abstract: A family of peptides and peptidomimetic compounds useful as GHS analogs according to either formula (I) or (II) as depicted below: or a pharmaceutically acceptable salts thereof, wherein the variables are as defined in the specification.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: March 20, 2012
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Zheng Xin Dong, John S. Eynon, Yeelana Shen
  • Patent number: 8128958
    Abstract: The present invention provides a sustained-release pharmaceutical composition, characterized in that, there are contained tamsulosin or a pharmaceutically acceptable salt thereof and a carrier for a sustained-release pharmaceutical composition and the ratio (Cmin/Cmax ratio) of the plasma tamsulosin concentration at 24 hours after the administration of the preparation per os (Cmin) to the maximum plasma tamsulosin concentration after the administration (Cmax) is about 0.4 or more.
    Type: Grant
    Filed: May 10, 2004
    Date of Patent: March 6, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Kazuhiro Sako, Toyohiro Sawada, Hiromu Kondo, Keiichi Yoshihara, Hiroyuki Kojima
  • Patent number: 8101799
    Abstract: This invention concerns N—(2-arylamino) aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: January 24, 2012
    Assignee: Ardea Biosciences
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoui, Zhi Hong
  • Patent number: 8030517
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: October 4, 2011
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20110223177
    Abstract: Inhibitors of myosin activity are used to treat or prevent a fibrotic disorder of the eye, for example posterior capsule opacification (PCO).
    Type: Application
    Filed: September 9, 2009
    Publication date: September 15, 2011
    Applicant: UNIVERSITY OF EAST ANGLIA
    Inventors: Ian Michael Wormstone, Lucy Dawes, Julie Ann Eldred, Lixin Wang
  • Patent number: 8008283
    Abstract: The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and/or inhibiting the activity of a Na+—K+-2Cl? (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl? co-transporter is NKCC1.
    Type: Grant
    Filed: October 17, 2005
    Date of Patent: August 30, 2011
    Assignee: Neurotherapeutics Pharma, Inc.
    Inventors: Daryl W. Hochman, John J. Partridge
  • Patent number: 8003823
    Abstract: Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. The most widely used halogen sulfonamide organic compound for these applications is Chloramine-T. This invention deals with the new use of discovered compositions of matter, halo active aromatic sulfonamide organic compounds and use of solutions of these compounds as, odor control agents. The odor control solutions may be buffered to a predetermined pH. The odor control compositions may further incorporate small percentages of low molecular weight alcohols and wetting agents.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: August 23, 2011
    Inventors: David J. Schneider, Charles A. Schneider
  • Publication number: 20110174179
    Abstract: There is provided a lithographic printing plate precursor that enables image recording using a laser and that provides an excellent scumming resistance and an excellent developability while maintaining a satisfactory printing durability. Also provided are a platemaking method, and a novel polymerizable monomer. A lithographic printing plate precursor has a support, and an image recording layer disposed thereon and containing a radical polymerization initiator and a polymerizable monomer that has a sulfonamide group and at least two ethylenically unsaturated groups; a lithographic printing plate platemaking method uses this lithographic printing plate precursor; and a polymerizable monomer has a sulfonamide group and at least two ethylenically unsaturated groups.
    Type: Application
    Filed: September 30, 2009
    Publication date: July 21, 2011
    Inventors: Katsuhiro Shimono, Norio Aoshima, Junji Kawaguchui
  • Patent number: RE43327
    Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: April 24, 2012
    Assignee: Aminex Therapeutics, Inc.
    Inventors: Mark R. Burns, Gerard F. Graminski, Nand Baindur