Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 514/313)
  • SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
    Publication number: 20110172236
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: September 21, 2009
    Publication date: July 14, 2011
    Inventors: Prasun K. Chakravarty, Joseph L. Duffy, Pengcheng Patric Shao
  • UREA COMPOUND OR SALT THEREOF
    Publication number: 20110172230
    Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.
    Type: Application
    Filed: August 22, 2007
    Publication date: July 14, 2011
    Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
  • METHOD FOR TREATMENT OF BONE DISEASES AND FRACTURES
    Publication number: 20110166180
    Abstract: Described herein are compounds, compositions, and methods useful for treating bone diseases or defects. Also described herein are compounds, compositions and methods for treating bone diseases or defects by inhibiting phosphatase complexes.
    Type: Application
    Filed: July 24, 2009
    Publication date: July 7, 2011
    Inventors: Hiroki Yokota, Ping Zhang
  • COATED DRUG SPHEROIDS AND USES THEREOF FOR ELIMINATING OR REDUCING CONDITIONS SUCH AS EMESIS AND DIARRHEA
    Publication number: 20110165257
    Abstract: The present invention provides an oral pharmaceutical formulation comprising coated spheroids of a kinase inhibitor such as neratinib, which formulation is designed to reduce or eliminate side effects associated with existing oral formulations of kinase inhibitors.
    Type: Application
    Filed: November 5, 2010
    Publication date: July 7, 2011
    Applicant: Wyeth LLC
    Inventors: Sripriya Venkata Ramana Rao, Syed Muzafar Shah, Christopher Richard Diorio, Maja Vencl-Joncic, Eugene Murphy
  • Compound with antimalarial activity and antimalarial drug containing the same as active ingredient
    Patent number: 7973027
    Abstract: Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R1 is H, Cl or OCH3; R2 is H or CH3; R3 is CH, CH2, C(CH3), CH(CH3) or C(CH3)2; Ar is imidazole, triazole, pyridine, benzene, pyrrole, furan, thiophene or derivatives thereof; n is 1 to 5; and m is 1 to 5). Further, there are provided antimalarial drugs containing these compounds with antimalarial activity or pharmacologically acceptable salts thereof as active ingredients.
    Type: Grant
    Filed: February 26, 2007
    Date of Patent: July 5, 2011
    Assignee: Nagoya City University
    Inventors: Tsunehiko Higuchi, Hirohisa Omiya, Naoki Umezawa, Hye-Sook Kim, Yusuke Wataya
  • Compounds that Inhibit HIV Particle Formation
    Publication number: 20110152301
    Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 23, 2011
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: David Rekosh, Marie-Louise Hammarskjöld
  • PREVENNTING THE OCCURRENCE OF OBESITY
    Publication number: 20110152317
    Abstract: Administration of autophagy inhibitor (e.g. 400 mg chloroquine daily) prevents occurrence of obesity and insulin resistance in human subject on prolonged high-fat diet.
    Type: Application
    Filed: July 9, 2009
    Publication date: June 23, 2011
    Applicant: DUKE UNIVERSITY
    Inventor: Zhen Yan
  • Compounds 679
    Patent number: 7964616
    Abstract: The invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, wherein R1, R2, R3 and n are as defined in the specification
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: June 21, 2011
    Assignee: AstraZeneca AB
    Inventors: Mark Ebden, Simon David Guile
  • Alkyl sulfoxide quinolines as NK-3 receptor ligands
    Patent number: 7964733
    Abstract: Compounds of Formula I wherein R1, A, R2, R3, R4, R5, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
    Type: Grant
    Filed: September 19, 2006
    Date of Patent: June 21, 2011
    Assignee: AstraZeneca AB
    Inventors: Jeffrey S. Albert, Gerard M. Koether, Cristobal Alhambra, James Kang, Thomas R. Simpson, James Woods, Yan Li
  • Stat modulators
    Publication number: 20110144043
    Abstract: The present invention is directed to methods, kits and compositions for modulating the activity of Stat molecules (e.g., Stat1, Stat3 and Stat5). The compounds of the invention are useful for treating and/or preventing disorders characterized by Stat dysregulation, such as hyperproliferative disorders. Further, the compounds of the present invention are also useful in culturing stem cells and treating ischemic disorders.
    Type: Application
    Filed: December 11, 2009
    Publication date: June 16, 2011
    Applicant: Dana-Farber Cancer Institute
    Inventor: David A. Frank
  • A3 ADENOSINE RECEPTOR ALLOSTERIC MODULATORS
    Publication number: 20110144156
    Abstract: Provided are 2,4-disubstituted quinoline derivatives that are A3 adenosine receptor modulators (A3RM), for use in the treatment of a condition which is treatable by adenosine, an A3 adenosine receptor (A3AR) agonist, or an A3 adenosine receptor antagonist. The 2,4-disubstituted quinoline derivatives can be used in the treatment of a condition treatable by an adenosine or an A3AR agonist, by enhancing activity of a protein (by binding of said 2,4-disubstituted quinoline derivative to the A3AR). Some conditions treatable by the 2,4-disubstituted quinoline derivative when used for enhancing activity include, malignancy, an immuno-compromised affliction, high intraocular pressure, or a condition associated with high intraocular pressure.
    Type: Application
    Filed: August 12, 2009
    Publication date: June 16, 2011
    Applicants: UNIVERSITEIT LEIDEN, CAN-FITE BIOPHARMA LTD.
    Inventors: Adriaan P. Ijzerman, Aniko Goblyos, Johannes Brussee
  • SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME
    Publication number: 20110144066
    Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
    Type: Application
    Filed: April 14, 2009
    Publication date: June 16, 2011
    Applicants: The Board of Regents of the University of Texas System, Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Vijay Gokhale, Garth Powis, Shuxing Zhang
  • TETRAHYDROQUINOLINE INDOLE DERIVATIVES AND USES THEREOF
    Publication number: 20110136864
    Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Application
    Filed: December 1, 2010
    Publication date: June 9, 2011
    Inventor: Ryan Craig Schoenfeld
  • COMPOSITIONS AND METHODS FOR PROTECTING SENSORY HAIR CELLS
    Publication number: 20110135756
    Abstract: The invention provides compounds, compositions and methods that can be used for the attenuation of damage to sensory hair cells and symptoms thereof. More particularly, the invention identifies drugs that can be used to protect sensory hair cells from ototoxic medications, noise-induced damage and age-related loss.
    Type: Application
    Filed: December 8, 2010
    Publication date: June 9, 2011
    Applicants: University of Washington, Fred Hutchinson Cancer Research Center
    Inventors: Kelly N. Owens, Anna L. Corke, Henry C. Ou, Edwin W. Rubel, David W. Raible, Julian A. Simon
  • Fluorinated Heteroaryls
    Publication number: 20110130365
    Abstract: The present invention provides Formula (1A) XN O R 3 HN R 5 O R 4 R 2 R 1 (1A) 5 compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the glucokinase enzyme, where X, R 1, R 2, R 3, R 4, and R 5 are as described herein.
    Type: Application
    Filed: July 15, 2009
    Publication date: June 2, 2011
    Inventors: John W. Benbow, Jihong Lou, Jeffrey A. Pferfferkorn, Meihua M. Tu
  • NOVEL ANTHRANILAMIDE PYRIDINUREAS AS VASCULAR ENDOTHELIAL GROWTH FACTOR (VEGF) RECEPTOR KINASE INHIBITORS
    Publication number: 20110124680
    Abstract: The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis.
    Type: Application
    Filed: February 2, 2011
    Publication date: May 26, 2011
    Inventors: Rolf BOHLMANN, Martin Haberey, Andreas Huth, Stuart James Ince, Martin Krueger, Karl-Heinz Thierauch, Holger Hess-Stumpp, Andreas Reichel
  • Bicyclic-substituted amines as histamine-3 receptor ligands
    Patent number: 7947711
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: May 24, 2011
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Yu-ming Pu, Yi-Yin Ku
  • Carboxamide compound and use of the same
    Patent number: 7943638
    Abstract: A carboxamide compound represented by the formula (1): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, one of ring constitutional atoms of the heterocyclic group is a nitrogen atom and the heterocyclic group may be substituted with a group selected from the group consisting of a C1-C3 alkyl and the like, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom or the like] and a plant disease controlling agent comprising this as an active ingredient.
    Type: Grant
    Filed: July 12, 2006
    Date of Patent: May 17, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shin-ichiro Souma, Yoshiharu Kinoshita
  • Compositions and methods for inhibiting TGF-?
    Patent number: 7943640
    Abstract: The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R8, Pg, and n are those defined herein. The present invention also provides pharmaceutical compositions comprising the same and methods for using the same. In particular, compounds of Formula I are useful in modulating TGF-? activity.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: May 17, 2011
    Assignee: Millenium Pharmaceuticals, Inc.
    Inventors: Anjali Pandey, Robert M. Scarborough, Meenakshi S. Venkatraman
  • AMINOQUINOLINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS
    Publication number: 20110112092
    Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (I).
    Type: Application
    Filed: January 18, 2011
    Publication date: May 12, 2011
    Applicant: sanofi-aventis
    Inventors: Peter ARANYI, Sandor BATORI, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin URBAN-SZABO, Katalin GERBER, Judit VARGANE SZEREDI, Michel FINET
  • Quinoline derivatives for modulating DNA methylation
    Patent number: 7939546
    Abstract: Quinoline derivatives, particularly 4-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine-2-carboxylic acid; 3-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine; N-(4-(piperidin-4-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide; and N-(4-(piperidin-3-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide, or a physiologically acceptable salt thereof, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: May 10, 2011
    Assignee: SuperGen, Inc.
    Inventors: Pasit Phiasivongsa, Sanjeev G. Redkar, Swarna Gamage, Darby Brooke, William Denny, David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Krzysztof Swierczek
  • Pyridine, quinoline and pyrimidine derivatives
    Patent number: 7939661
    Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Grant
    Filed: August 30, 2007
    Date of Patent: May 10, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andreas D. Christ, Rainer E. Martin, Peter Mohr
  • TETRAHYDROQUINOLINE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS
    Publication number: 20110104315
    Abstract: The invention provides for compounds of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.
    Type: Application
    Filed: January 5, 2011
    Publication date: May 5, 2011
    Inventors: Chongqing Sun, Doree Sitkoff, William R. Ewing, Yanting Huang, Bruce A. Ellsworth, Richard B. Sulsky, Annapurna Pendri, Samuel Gerritz, Natesan Murugesan, Zhengxiang Gu
  • AMINO-QUINOXALINE AND AMINO-QUINOLINE COMPOUNDS FOR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS
    Publication number: 20110105513
    Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof. Care adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
    Type: Application
    Filed: March 3, 2009
    Publication date: May 5, 2011
    Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
  • ORGANIC COMPOUNDS
    Publication number: 20110105530
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: June 25, 2009
    Publication date: May 5, 2011
    Inventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
  • SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20110104110
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: August 27, 2008
    Publication date: May 5, 2011
    Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • GENETIC ALTERATION ASSOCIATED WITH PRE-MALIGNANT CANCER
    Publication number: 20110104065
    Abstract: Described herein are progenitor cancer cells and cell lines isolated from human breast ductal carcinoma in situ (DCIS) lesions and the uses of these cells or cell lines in drug design, drug screening, and monitoring in vivo therapy. The DCIS malignant precursor cells or cell lines are epithelial in origin, are positive for markers of autophagy, show at least one genetic difference from normal cells of said fragment, form 3-D tube-like structures or ball aggregates, or are inhibited in formation of 3-D structures and migration by treatment with chloroquine. In one embodiment, there is a loss of heterozygosity (LOH) that is narrowly confined to a region of chromosome 6p (6p21.1-6p12.3) that contains the SUPT3H gene.
    Type: Application
    Filed: October 28, 2010
    Publication date: May 5, 2011
    Inventors: Virginia Espina, Lance Liotta
  • COMPOUNDS WITH ANTI-CANCER ACTIVITY
    Publication number: 20110092514
    Abstract: Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.
    Type: Application
    Filed: November 19, 2010
    Publication date: April 21, 2011
    Applicant: CanBas Co., Ltd.
    Inventors: TAKUMI KAWABE, Machiyo Ishigaki, Takuji Sato, Sayaka Yamamoto, Yoko Hasegawa
  • Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
    Patent number: 7928239
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions in such therapy.
    Type: Grant
    Filed: February 7, 2001
    Date of Patent: April 19, 2011
    Assignee: Bayer Healthcare LLC
    Inventors: Jacques Dumas, Bernd Riedl, Uday Khire, Jill E. Wood, Robert N. Sibley, Mary-Katherine Monahan, Joel Renick, David E. Gunn, Timothy B. Lowinger, William J. Scott, Roger A. Smith
  • Compounds and compositions as hedgehog signaling pathway modulators
    Patent number: 7928133
    Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.
    Type: Grant
    Filed: July 24, 2007
    Date of Patent: April 19, 2011
    Assignee: IRM LLC
    Inventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
  • Compounds which modulate the CB2 receptor
    Patent number: 7928123
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: April 19, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Pier Francesco Cirillo, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Chowdhury, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
  • Small Molecule Inhibitors of Botulinum Neurotoxins
    Publication number: 20110086877
    Abstract: Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 14, 2011
    Inventors: SINA BAVARI, RICK GUSSIO, JAMES C. BURNETT
  • Treatments for Neuropathy
    Publication number: 20110086878
    Abstract: Small fiber neuropathy is treated or prevented by topically administering to a subject in need thereof topically active quinoline compounds or pharmaceutically acceptable salts thereof under conditions effective to treat or prevent neuropathy in the subject. Glial cell-derived neurotrophic factor (GDNF) receptors are modulated with the subject active quinoline compounds, which may be formulated in topical lotions.
    Type: Application
    Filed: December 16, 2010
    Publication date: April 14, 2011
    Inventors: Gabriel Corfas, Joshua C. Murtie
  • Method for treating chronic pain
    Patent number: 7923458
    Abstract: A method for the treatment of chronic pain in a mammal is provided. The method comprises administering to a mammal (e.g., a human) suffering from chronic pain a pain relieving amount of a diarylureido-dihalokynurenate compound. Preferred diarylureido-dihalokynurenate compounds are esters (e.g., ethyl esters). Particularly preferred are diphenylureido-dichlorokynurenate compounds.
    Type: Grant
    Filed: October 6, 2006
    Date of Patent: April 12, 2011
    Assignee: Lohocla Research Corporation
    Inventor: Boris Tabakoff
  • Biaryl sulfonamides and methods for using same
    Patent number: 7923446
    Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: April 12, 2011
    Assignee: Wyeth LLC
    Inventors: Jason Shaoyun Xiang, Steve Yikkai Tam, Yonghan Hu, Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini, Thomas Saltmarsh Rush, III, Elisabeth Ann Morris, Katy Evangelia Georgiadis
  • 4-anilino-3-quinolinecarbonitriles for the treatment of chronic myelogenous leukemia (CML)
    Patent number: 7919625
    Abstract: Compounds of the formula: wherein: n is an integer from 1-3; X is N, CH, provided that when X is N, n is 2 or 3; R is alkyl of 1 to 3 carbon atoms; R1 is 2,4-diCl, 5-OMe; 2,4-diCl; 3,4,5-tri-OMe; 2-Cl, 5-OMe; 2-Me, 5-OMe; 2,4-di-Me; 2,4-diMe-5-OMe, 2,4-diCl, 5-OEt; R2 is alkyl of 1 to 2 carbon atoms, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: April 5, 2011
    Assignee: Wyeth LLC
    Inventors: Frank Boschelli, Jennifer M. Golas, Kim T. Arndt
  • Compositions and Methods for Treating Ocular Inflammation with Lower Risk of Increased Intraocular Pressure
    Publication number: 20110077270
    Abstract: A composition for treating or controlling an ocular disease or condition comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), which disease or condition has an etiology, or results, in inflammation. The composition can optionally include an anti-inflammatory agent, an anti-infective agent, or both. The composition can be formulated for topical application, injection, or implantation in an affected eye to treat or control the ocular inflammatory disease or condition.
    Type: Application
    Filed: March 26, 2010
    Publication date: March 31, 2011
    Inventors: Bruce A. Pfeffer, Mercedes Salvador-Silva, Charu A. DeWitt, Keith W. Ward, Francisco J. Lopez
  • TREATMENT OF MALARIA
    Publication number: 20110077258
    Abstract: The invention contemplates compositions for the treatment of malaria comprising an anti-malaria drug and an adjuvant which promotes vasodilation and methods of using same.
    Type: Application
    Filed: September 13, 2010
    Publication date: March 31, 2011
    Inventors: Leonardo Jose de Moura Carvalho, Pedro Cabrales
  • Hepatitis C virus inhibitors
    Patent number: 7915291
    Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: September 2, 2008
    Date of Patent: March 29, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
  • BICYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS
    Publication number: 20110059965
    Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:
    Type: Application
    Filed: July 6, 2010
    Publication date: March 10, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Aarti Sameer Kawatkar, Tara Whitney, Timothy D. Neubert, Nicole Hilgraf, Andreas P. Termin, Esther Martinborough
  • PYRAZOLE DERIVATIVES AND USE THEREOF AS OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20110059964
    Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.
    Type: Application
    Filed: February 3, 2010
    Publication date: March 10, 2011
    Applicant: sanofi-aventis
    Inventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
  • ACRIDINE ANALOGS IN THE TREATMENT OF GLIOMAS
    Publication number: 20110060000
    Abstract: Disclosed are methods and compositions for treating gliomas that involve quinacrine and other acridine analogs. 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: September 10, 2010
    Publication date: March 10, 2011
    Inventors: Maurizio Grimaldi, Subramaniam Ananthan
  • Phenyl derivatives as factor XA inhibitors
    Patent number: 7902223
    Abstract: Novel compounds of the formula (I), in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: March 8, 2011
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Bertram Cezanne, Christos Tsaklakidis, Werner Mederski, Johannes Gleitz, Christopher Barnes
  • Inhibitors of the Interaction Between MDM2 and P53
    Publication number: 20110053937
    Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.
    Type: Application
    Filed: November 3, 2010
    Publication date: March 3, 2011
    Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Yannick Aimé Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
  • METHOD TO PROGNOSE RESPONSE TO ANTI-EGFR THERAPEUTICS
    Publication number: 20110052570
    Abstract: The present invention provides methods to determine the likelihood of effectiveness of an EGFR targeting treatment in a subject affected with a tumor based on the expression of EGFR of endothelial cells associated with the tumor. The present invention also provides methods of treating a subject affected with, or at risk for developing cancer with an EGFR targeting treatment and methods to screen for an EGFR targeting treatment.
    Type: Application
    Filed: October 24, 2006
    Publication date: March 3, 2011
    Applicant: CHILDREN'S MEDICAL CENTER CORPORATION
    Inventors: Michael Klagsbrun, Dhara N. Amin, Kyoko Hida
  • COMPOUNDS AND METHODS OF TREATMENT
    Publication number: 20110053934
    Abstract: A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity.
    Type: Application
    Filed: January 21, 2010
    Publication date: March 3, 2011
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: RICHARD MARTYN ANGELL, IAN ROBERT BALDWIN, GEORGE STUART COCKERILL, STEPHEN SEAN FLACK, KAREN ELIZABETH LACKEY, PHILIP ALAN SKONE, KATHRYN JANE SMITH
  • QUINOLINE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS
    Publication number: 20110053976
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salts thereof. A pharmaceutical composition having a therapeutically effective amount of the compound. The compound is useful for the treatment of cancer, diabetic retinopathy, age-related macular degeneration, inflammation, stroke, ischemic myocardium, atherosclerosis, macular edema or psoriasis.
    Type: Application
    Filed: November 14, 2008
    Publication date: March 3, 2011
    Applicant: CLANOTECH AB
    Inventors: Jacob Westman, Natalia Nekhotiaeva, Johan Wannberg, Ulrika Backman, Johan Malm
  • Antimalarial Quinolines and Methods of Use Thereof
    Publication number: 20110045100
    Abstract: One aspect of the invention relates to substitute quinolines with antimalarial activity, and compositions and kits comprising at least one of them. Another aspect of the invention relates to methods for the treatment or prevention or both of malaria comprising administering to a subject a therapeutically effective amount of such a compound. Importantly, a number of the compounds show excellent potency against both chloroquine-sensitive and chloroquine-resistant strains.
    Type: Application
    Filed: March 5, 2009
    Publication date: February 24, 2011
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Christian Wolf, Paul D. Roepe, Angel C. De Dios
  • ANTIBIOTIC COMPOUNDS
    Publication number: 20110046142
    Abstract: Methods for identifying prodrug antibiotic compounds and direct inhibitory antibiotic compounds utilizing various screens are provided. Also provided are methods for treating infections using these compounds.
    Type: Application
    Filed: June 11, 2008
    Publication date: February 24, 2011
    Applicant: Northeastern University
    Inventors: Kim Lewis, Gabriele Casadei
  • Substituted 3-cyanoquinolines
    Patent number: RE42376
    Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: May 17, 2011
    Assignee: Wyeth Holdings Corporation
    Inventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Philip Frost