Aralkyl Bonded Directly To Urea Nitrogen Patents (Class 564/56)
  • Publication number: 20150099883
    Abstract: The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: in the formula, Cy represents an unsubstituted or X-substituted phenyl group or the like, X represents a halogen atom or the like, R1 represents an ethyl group or the like, R2 represents a hydrogen atom or the like, R3 and R4 represents a methyl group or the like, X1 represents a methylthio group or the like, m1 represents an integer of 1 to 4, X2 represents a methyl group or the like, m2 is an integer of 0 to 3.
    Type: Application
    Filed: April 8, 2013
    Publication date: April 9, 2015
    Inventors: Hironori Furukawa, Daisuke Hanai, Tetsuo Tamai, Jun Kanazawa, Katsunori Tanaka, Asaho Nagagata
  • Publication number: 20140303384
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical compositions containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: October 5, 2012
    Publication date: October 9, 2014
    Inventors: Brian A. Duclos, Richard Andrew Ewin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Derek James Sheehan, Susan Mary Kult Sheehan, Donald James Skalitzky, Rajendran Vairagoundar
  • Publication number: 20140221657
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: PRISM BioLab Corporation
    Inventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
  • Publication number: 20140147403
    Abstract: Compounds of the formula (I) 5 or salts thereof, wherein R1 represents alkyl, aryl, alkyl-aryl or aryl-alkyl, compositions containing same, and their use in counteracting human axillary malodour.
    Type: Application
    Filed: October 28, 2011
    Publication date: May 29, 2014
    Applicant: GIVAUDAN, S.A.
    Inventors: Andreas Natsch, Thierry Granier
  • Patent number: 8642576
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 8642657
    Abstract: 4-(methylsulfonylamino)phenyl analogues as potent vanilloid receptor antagonists and pharmaceutical compositions comprising the same. The compounds are useful as analgesics to prevent, alleviate or treat pain diseases or inflammatory disease including pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease and urgent urinary incontinence.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: February 4, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Jee Woo Lee, Young Ho Kim, Hee Kim, Hyun Kyung Choi, Hee Jin Ha
  • Publication number: 20130345255
    Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, prodrugs, or combinations thereof, wherein X1, L, Rx, Ry, Rz, R1, R2, A, m, n, p, q, and r are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: June 20, 2013
    Publication date: December 26, 2013
    Inventors: Arthur Gomtsyan, Jerome Daanen, Michael E. Kort, Philip R. Kym, Eric A. Voight, Kevin R. Woller
  • Publication number: 20130184279
    Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130065963
    Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Application
    Filed: July 17, 2012
    Publication date: March 14, 2013
    Applicant: Georgetown University
    Inventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
  • Publication number: 20130053392
    Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.
    Type: Application
    Filed: February 14, 2011
    Publication date: February 28, 2013
    Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
  • Publication number: 20130023463
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Application
    Filed: April 19, 2012
    Publication date: January 24, 2013
    Applicant: ABBOTT LABORATORIES
    Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
  • Publication number: 20120322877
    Abstract: The invention provides for novel (bis)urea and (bis)thiourea compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer.
    Type: Application
    Filed: August 18, 2010
    Publication date: December 20, 2012
    Inventors: Robert A. Casero, Patrick M. Woster
  • Publication number: 20120322761
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 20, 2012
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 8329745
    Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: December 11, 2012
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
  • Publication number: 20120088837
    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: Application
    Filed: December 8, 2011
    Publication date: April 12, 2012
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 8143364
    Abstract: Process for preparing a composition by reacting a polyisocyanate, a monoalkoxy polyoxyalkylene monoamine and water. The composition and its use in making cellular products are claimed as well.
    Type: Grant
    Filed: February 12, 2007
    Date of Patent: March 27, 2012
    Assignee: Huntsman International LLC
    Inventors: Gerhard Jozef Bleys, Hans Godelieve Guido Verbeke
  • Publication number: 20120061325
    Abstract: Novel compounds useful as chelators, intermediates for their production and methods for removing trivalent and tetravalent metal ions from solution are presented.
    Type: Application
    Filed: October 21, 2011
    Publication date: March 15, 2012
    Inventors: Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Robert Joseph Kuhn, Surendra Dawadi
  • Publication number: 20120053342
    Abstract: The present invention provides methods of forming carbamates, ureas, and isocyanates. In certain embodiments these methods include the step of reacting an amine with an ester-substituted diaryl carbonate to form an activated carbamate which can be further derivatized to form non-activated carbamate or a urea. The urea or carbamate can be subjected to a pyrolysis reaction to form isocyanate.
    Type: Application
    Filed: November 4, 2011
    Publication date: March 1, 2012
    Applicant: SABIC INNOVATIVE PLASTICS IP B.V.
    Inventors: Hatem Abdallah Belfadhel, Hans-Peter Brack, Ricardo Godoy-Lopez, Dennis James Patrick Maria Willemse
  • Patent number: 8013015
    Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: September 6, 2011
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
  • Publication number: 20110178316
    Abstract: Fullerene compounds represented by the formulae Cm[C(R)CON3]n, Cm[C(R)NCO]n, Cm[C(R)NHCORd]n, and Cm[C(R)NH2]n, wherein Cm represents a fullerene moiety having m carbon atoms, m represents an even integer from about 60 to about 200, n represents an integer of about 1 or more, R represents an electron-withdrawing group, and Rd represents an alkoxy or alkylamino group. In addition, processes for preparing these fullerene compounds involving reacting an acyl azide with a fullerene in the presence of a base.
    Type: Application
    Filed: July 28, 2009
    Publication date: July 21, 2011
    Applicant: Luna Innovations Incorporated
    Inventor: Jing Zhang
  • Patent number: 7981923
    Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: July 19, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 7964642
    Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.
    Type: Grant
    Filed: June 16, 2005
    Date of Patent: June 21, 2011
    Assignee: Pharmeste S.R.L.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti
  • Patent number: 7960584
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: June 14, 2011
    Assignee: Amorepacific Corporation
    Inventors: Young-Ger Suh, Hee-Doo Kim, Hyeung-Geun Park, Uh Taek Oh, Yong-Sil Lee, Seol Rin Park, Chong Hyon Ryu, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-II Kim, Joon Ho Bae
  • Publication number: 20110098322
    Abstract: The present invention provides compounds that can inhibit the activity of soluble epoxide hydrolases. In particular, the present invention provides compounds of Formula I.
    Type: Application
    Filed: August 5, 2008
    Publication date: April 28, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: James R. Sanborn, Bruce D. Hammock, Sung Hee Hwang, Paul D. Jones, Christophe Morisseau
  • Publication number: 20110098504
    Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Application
    Filed: October 25, 2010
    Publication date: April 28, 2011
    Applicant: Georgetown University
    Inventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
  • Publication number: 20110021633
    Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
    Type: Application
    Filed: July 23, 2010
    Publication date: January 27, 2011
    Inventor: IBERT CLIFTON WELLS
  • Patent number: 7763657
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.
    Type: Grant
    Filed: March 15, 2006
    Date of Patent: July 27, 2010
    Assignee: Amorepacific Corporation
    Inventors: Hee-Doo Kim, Young-Ger Suh, Hyeung-Geun Park, Uh Taek Oh, Seol Rin Park, Joo Hyun Kim, Mi Jung Jang, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-Il Kim, Byoung Young Woo
  • Patent number: 7750049
    Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: July 6, 2010
    Assignee: Pharmeste S.R.L.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Francesca Fruttarolo, Maria Giovanna Pavani, Marcello Trevisani
  • Publication number: 20100160682
    Abstract: Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 Ru(Z)2(L)??j1; Ru(E)(E?)(L)(D)??j2; wherein m, n, Ar, Y, R1 E, E?, D, Z and L are as defined herein.
    Type: Application
    Filed: December 14, 2009
    Publication date: June 24, 2010
    Inventors: Kieran Durkin, Lawrence Emerson Fisher, Arthur Meili, Michaelangelo Scalone, Xianqing Shi, Justin Vitale
  • Publication number: 20100105740
    Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-car-boxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl.
    Type: Application
    Filed: December 6, 2007
    Publication date: April 29, 2010
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Francesca Fruttarolo, Maria Giovanna Pavani, Marcello Trevisani
  • Publication number: 20100068553
    Abstract: The invention relates to a novel ultra-thin hydrophobic and oleophobic layer, formed by self-assembly on a solid substrate surface, of compounds of the general formula A-B in which A represents a group of the formula in which Z represents C or N+, X represents C—H or C-L, L being an electron-attracting group selected from F, Cl, Br, I, CF3, NO2 and N(CH3)3+, Y represents H or CH3, or Y forms a 5- or 6-atom heterocycle with X, T represents NH, CO, CONH or NH2+U?, U? being a soluble anion such as e.g. F?, Cl?, Br?, I, OH?, NO3?, HSO4?, SO42?, CO32?, HCO3? or SCN?, and B represents a C1-C20 linear aliphatic alkyl group partially or completely substituted with F, and a method of preparing this layer and its use as an epilame.
    Type: Application
    Filed: November 29, 2007
    Publication date: March 18, 2010
    Applicant: ROLEX S.A.
    Inventors: Samuele Tosatti, Stefan Zurcher
  • Patent number: 7671052
    Abstract: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.
    Type: Grant
    Filed: October 3, 2005
    Date of Patent: March 2, 2010
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Karin Worm, Q. Jean Zhou
  • Publication number: 20100048711
    Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans,trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
    Type: Application
    Filed: October 16, 2009
    Publication date: February 25, 2010
    Inventor: Ibert Clifton Wells
  • Patent number: 7655695
    Abstract: Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: February 2, 2010
    Assignee: The Regents of The University of California
    Inventors: Trevor C. McMorris, Michael J. Kelner
  • Patent number: 7579378
    Abstract: The invention relates to sulfonamido derivatives of formula (I) wherein R1-R7 are as defined in the description. Compounds (I) antagonize the vanilloid receptor and can be used for the preparation of medicaments for the treatment of inflammatory states.
    Type: Grant
    Filed: October 18, 2005
    Date of Patent: August 25, 2009
    Assignee: Pharmeste S.R.L.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti
  • Publication number: 20090163543
    Abstract: One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Application
    Filed: December 19, 2008
    Publication date: June 25, 2009
    Applicant: Georgetown University
    Inventors: Alan P. Kozikowski, Bin Chen
  • Patent number: 7544716
    Abstract: This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.
    Type: Grant
    Filed: November 28, 2003
    Date of Patent: June 9, 2009
    Assignee: Xention Limited
    Inventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
  • Patent number: 7531577
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.
    Type: Grant
    Filed: June 20, 2007
    Date of Patent: May 12, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 7531576
    Abstract: Biphenyl derivatives represented by the following formula (1): wherein R1 represents a C5-7 alkyl group, R2 represents a substituted or unsubstituted aromatic hydrocarbon, or cycloalkyl group, R3 represents a tetrazolyl group, —NHCOCF3, —NHSO2CF3 or —SO2NHCONHR4 in which R4 represents a substituted or unsubstituted aromatic hydrocarbon group, and Z represents a single bond, a C1-4 alkylene group or —SO2NH—, and salts thereof; and ACAT inhibitors and medicines containing them as active ingredients. The compounds according to the present invention possess excellent ACAT inhibitory activities, and are useful as preventives and/or therapeutics for diseases cased by the enhancement of ACAT activity, for example, hypercholesterolemia, atherosclerosis and the like.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: May 12, 2009
    Assignee: Pola Chemical Industries, Inc.
    Inventors: Takayuki Namiki, Kenichi Kishii, Masaki Mitani, Masashi Tamai, Naoki Hiyama, Makoto Kimura, Satoshi Ichinomiya
  • Publication number: 20090105258
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.
    Type: Application
    Filed: March 15, 2006
    Publication date: April 23, 2009
    Applicant: AMOREPACIFIC CORPORATION
    Inventors: Hee-Doo Kim, Young-Ger Suh, Hyeung-Geun Park, Uh Taek Oh, Seol Rin Park, Joo Hyun Kim, Mi Jung Jang, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-II Kim, Byoung Young Woo
  • Patent number: 7482487
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: January 27, 2009
    Assignee: Pfizer Inc
    Inventors: Alan Daniel Brown, Justin Stephen Bryans, Paul Alan Glossop, Charlotte Alice Louise Lane, Simmon John Mantell
  • Publication number: 20080234383
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receotor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.
    Type: Application
    Filed: March 17, 2006
    Publication date: September 25, 2008
    Inventors: Young-Ger Suh, Hee-Doo Kim, Hyeung-Geun Park, Uh Taek Oh, Yong-Sil Lee, Seol Rin Park, Chong Hyon Ryu, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-II Kim, Joon Ho Bae
  • Patent number: 7351738
    Abstract: The invention provides compounds of formula I: useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
    Type: Grant
    Filed: November 26, 2003
    Date of Patent: April 1, 2008
    Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
    Inventors: Shon R. Pulley, John A. Tucker
  • Patent number: 7326746
    Abstract: Electron donor compounds, suitable for use as adhesives or as components in adhesives, contain a carbon to carbon double bond attached to an aromatic ring and conjugated with the unsaturation in the aromatic ring.
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: February 5, 2008
    Inventors: Osama M. Musa, Donald E. Herr, Nikola A. Nikolic
  • Patent number: 6908957
    Abstract: Electron donor compounds, suitable for use as adhesives or as components in adhesives, contain a carbon to carbon double bond attached to an aromatic ring and conjugated with the unsaturation in the aromatic ring.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: June 21, 2005
    Assignee: National Starch and Chemical Investment Holding Corporation
    Inventors: Osama M. Musa, Donald E. Herr, Nikola A. Nikolic
  • Patent number: 6900213
    Abstract: The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.
    Type: Grant
    Filed: July 21, 2003
    Date of Patent: May 31, 2005
    Assignee: Pharmacopeia Drug Discovery, Inc.
    Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
  • Patent number: 6872851
    Abstract: The invention concerns compounds of formula (I): R—A—R? wherein: A is as defined in the description; R represent, a group (V), wherein R?a and R?a are as defined in the description, or R forms with A a cyclic structure as defined in the description; R? represents a (CH2)t—R2 group wherein q, t, and R2 are as defined in the description. The invention is useful for preparing medicines.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: March 29, 2005
    Assignee: Les Laboratories Servier
    Inventors: Daniel Lesieur, Frédérique Klupsch, Gérald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6841701
    Abstract: The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for treating cardiovascular diseases and thrombotic events.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: January 11, 2005
    Assignee: Curacyte AG
    Inventors: Jörg Stürzebecher, Torsten Steinmetzer, Sebastian Künzel, Andrea Schweinitz
  • Patent number: 6777561
    Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
    Type: Grant
    Filed: June 1, 2000
    Date of Patent: August 17, 2004
    Assignee: AstraZeneca Canada Inc.
    Inventors: Daniel Delorme, Vlad Gregor, Edward Roberts, Eric Sun
  • Patent number: 6730784
    Abstract: Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S— or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: May 4, 2004
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara