Hydroxy, Bonded Directly To Carbon, Or Ether Containing (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/158)
-
Patent number: 8143446Abstract: A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].Type: GrantFiled: May 11, 2006Date of Patent: March 27, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Kazumasa Aoki, Koji Suda, Toshio Kaneko, Tomio Kimura
-
Publication number: 20120059188Abstract: The present invention relates to halogenated compounds of formula (I) with the substituents as described within the specification. The compounds may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation.Type: ApplicationFiled: December 19, 2008Publication date: March 8, 2012Applicants: The University of Melbourne, Fibrotech Therapeutics Pty LtdInventors: Darren James Kelly, Spencer John Williams, Steven Zammit
-
HYDROPHOBIC MONOMERS, HYDROPHOBICALLY-DERIVATIZED SUPPORTS, AND METHODS OF MAKING AND USING THE SAME
Publication number: 20120039920Abstract: A composition is disclosed comprising a hydrophobic monomer having the structure: CH2?CR4C(O)NHC(R1R1)(C(R1R1))nC(O)XR3 wherein n is an integer of 0 or 1; R1 is independently selected from at least one of: a hydrogen atom, alkyls aryls, and alkylaryls, wherein the alkyls, aryls, and alkylaryls have a total of 10 carbon atoms or less; R3 is a hydrophobic group selected from at least one of: alkyls, aryls, alkylaryls and ethers, wherein the alkyls, aryls, alkylaryls and ethers have a total number of carbon atoms ranging from 4 to 30; R4 H or CH3; X is O or NH. In some embodiments the hydrophobic monomer is derived from an amine or an alcohol (HXR3) that has a hydrophilicity index of 25 or less. A polymerizable composition comprising the hydrophobic monomer is disclosed, which optionally may comprise a cross-linking monomer and/or a non-cross-linking monomer.Type: ApplicationFiled: March 19, 2010Publication date: February 16, 2012Inventors: Jerald K. Rasmussen, Cary A. Kipke, James I. Hembre, Peter D. Wickert -
Publication number: 20120027844Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.Type: ApplicationFiled: February 9, 2010Publication date: February 2, 2012Applicants: XAVIER UNIVERSITY OF LOUISIANA, TULANE UNIVERSITYInventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
-
Publication number: 20120029067Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Applicants: UNIVERSITY OF SOUTH FLORIDA, THE HONG KONG POLYTECHNIC UNIVERSITY, MCGILL UNIVERSITYInventors: Q. Ping DOU, Tak-Hang CHAN, David M. SMITH
-
Patent number: 8097758Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.Type: GrantFiled: March 9, 2009Date of Patent: January 17, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Markus Follmann, Jochen Goerlitzer, Herman Schreuder
-
Publication number: 20120004243Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: April 5, 2011Publication date: January 5, 2012Applicant: AstraZeneca ABInventors: Dearg Sutherland Brown, John Graham Cumming, Ian Alun Nash
-
Patent number: 8088763Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.Type: GrantFiled: November 9, 2006Date of Patent: January 3, 2012Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann
-
Publication number: 20110313057Abstract: The present invention relates to compounds of formula I, which are difunctionalized aromatic compounds, and polymers formed from the same. [R?—(X)a—OC(O)]p—Ar—[NR?—(Y)b—R?]q??I Polymers formed from the difunctionalized aromatics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.Type: ApplicationFiled: August 13, 2011Publication date: December 22, 2011Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
-
Publication number: 20110312092Abstract: Disclosed is a benzamide derivative represented by formula (1). In the formula, k1 represents an integer from 0-4, m1 represents an integer from 1-100, and n1 represents an integer from 1-6. In addition, R1 represents a hydrocarbon group with 8-22 carbon atoms bonded via an oxygen atom; R2 represents H or a hydrocarbon group with 1-22 carbon atoms bonded via an oxygen atom; R3 represents H or a hydrocarbon group with 1-22 carbon atoms bonded via an oxygen atom; and R2 and R3 are not H at the same time.Type: ApplicationFiled: February 23, 2010Publication date: December 22, 2011Inventors: Hitoshi Tamiaki, Keishiro Ogawa, Kazunori Toma
-
Publication number: 20110306668Abstract: A process for synthesizing and screening solution phase derived libraries of fenbufen and ethacrynic acid is provided in the present invention. Compounds in the present invention having cytotoxicities are useful for a variety of therapeutic applications.Type: ApplicationFiled: June 9, 2010Publication date: December 15, 2011Applicant: NATIONAL TSING HUA UNIVERSITYInventors: Chung-Shan Yu, Yuan-Hsiao Su, Li-Wu Chiang, Chia-Rong Chen, Shao-Wei Chen, Chia-Wen Huang, Ho-Lien Huang, Yin-Cheng Huang
-
Patent number: 8071575Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.Type: GrantFiled: February 22, 2008Date of Patent: December 6, 2011Assignee: University of Louisville Research FoundationInventors: William M. Pierce, Jr., K. Grant Taylor, Leonard C. Waite
-
Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
-
Publication number: 20110294892Abstract: The use of substances capable of inhibiting one or more enzymes of the histone deacetylase family (histone deacetylase inhibitors) for the therapeutic treatment of Philadelphia-negative myeloproliferative syndromes (polycythemia vera, essential thrombocythemia or idiopathic myelofibrosis) is described. The dosage of the above-mentioned substances is significantly lower than that normally used for the care of other tumor syndromes and may be from 10 to 150 mg/day/patient.Type: ApplicationFiled: March 25, 2011Publication date: December 1, 2011Inventors: Tiziano Oldoni, Paolo Mascagni, Alessandro Rambaldi, Tiziano Barbui
-
Publication number: 20110288076Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicant: EXELIXIS, INC.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
-
Publication number: 20110263626Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: August 28, 2008Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
-
Publication number: 20110263899Abstract: The present patent application relates to an alternative process for the preparation of amino derivatives. In particular, the present application relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide, which is useful as an anticonvulsive drug. In a particular aspect, the present invention relates to a process of manufacture of optically enriched (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (I) comprising resolution of 2-acetamido-N-benzyl-3-methoxypropion-amide (II).Type: ApplicationFiled: November 6, 2009Publication date: October 27, 2011Applicant: UCB PHARMA GMBHInventors: Didier Bouvy, Alain Merschaert, Véronique Pinilla, Joerg Hamann, Ralf Kanzler, Antoine Thomas
-
Publication number: 20110257374Abstract: Described herein are methods, compositions and articles of manufacture involving neutral conjugated polymers including methods for synthesis of neutral conjugated water-soluble polymers with linkers along the polymer main chain structure and terminal end capping units. Such polymers may serve in the fabrication of novel optoelectronic devices and in the development of highly efficient biosensors. The invention further relates to the application of these polymers in assay methods.Type: ApplicationFiled: January 19, 2011Publication date: October 20, 2011Applicant: Sirigen, Inc.Inventors: Brent S. Gaylord, Jean M. Wheeler, Glenn P. Bartholomew, Yongchao Liang, Janice W. Hong, William H. Huisman, Frank Peter Uckert, Lan T. Tran, Adrian Charles Vernon Palmer, Trung Nguyen, Russell A. Baldocchi
-
Publication number: 20110251131Abstract: This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NMDA glycine-site antagonist.Type: ApplicationFiled: September 15, 2009Publication date: October 13, 2011Applicant: CONCERT PHARMACEUTICALS INC.Inventor: Craig E. Masse
-
Publication number: 20110251248Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: December 9, 2009Publication date: October 13, 2011Inventors: Songnian Lin, Xibin Liao, Roman Kats-Kagan, John E. Stelmach, Emma R. Parmee
-
Patent number: 8013015Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: GrantFiled: October 1, 2009Date of Patent: September 6, 2011Assignee: Board of Regents, The University of Texas SystemInventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
-
Publication number: 20110178092Abstract: Described are novel protease inhibitors and methods for using said protease inhibitors in the treatment of human immunodeficiency virus (HIV) infection.Type: ApplicationFiled: December 19, 2007Publication date: July 21, 2011Inventors: Akbar Ali, Michael D. Altman, Saima G. Anjum, Hong Cao, Sripriya Chellappan, Miguel X. Fernandes, Michael K. Gilson, Visvaldas Kairys, Nancy King, Ellen Nalivaika, Moses Prabu, Tariq M. Rana, Kiran Kumar Sai, Celia A. Schiffer, Bruce Tidor
-
Publication number: 20110172303Abstract: The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.Type: ApplicationFiled: July 22, 2009Publication date: July 14, 2011Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: Weiping Tang, James Elliot Bradner, Stuart L. Schreiber
-
Publication number: 20110172239Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: ApplicationFiled: July 16, 2010Publication date: July 14, 2011Inventors: Alan D. SNOW, Beth NGUYEN, Gerardo CASTILLO, Virginia SANDERS, Thomas LAKE, Lesley LARSEN, Rex T. WEAVERS, Stephen LORIMER, David LARSEN, David L. COFFEN, Charlotte COFFEN
-
Publication number: 20110137047Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of enantiomerically pure 8-aryloctanoic acids of general formula I from readily available key intermediate, chiral cis-diacid of formula II, aziridine of formula XI and a monocyclic compound of formula III.Type: ApplicationFiled: October 15, 2010Publication date: June 9, 2011Applicant: CarboDesign LLCInventor: Milan Soukup
-
Publication number: 20110136878Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.Type: ApplicationFiled: June 29, 2009Publication date: June 9, 2011Applicant: Mitsui Chemicals Agro., Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
-
Publication number: 20110131029Abstract: Provided are the expression method of influenza virus polymerase PAc-PB1N complex, the co-crystallization method of the complex and the three-dimendional structure of the crystal of PAc-PB1N complex. Also provided are the compounds binding to the influenza virus polymerase PAc and the expression method of influenza virus polymerase PAN. The three-dimensional structure of the crystal of PAc-PB1N complex can be used for screening and designing the drug for the treatment of influenza.Type: ApplicationFiled: February 22, 2009Publication date: June 2, 2011Inventors: Yingfang Liu, Xiaojing He, Zonghao Zeng, Jie Zhou
-
Publication number: 20110130350Abstract: The present invention is concerned with an improved method of producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide) comprising the 0-methylation of a compound of formula (I) to produce a compound of formula (II) in a single step reaction.Type: ApplicationFiled: December 7, 2010Publication date: June 2, 2011Applicant: UCB PHARMA GMBHInventors: Jens Riedner, Gavin Dunne
-
Publication number: 20110117055Abstract: Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.Type: ApplicationFiled: November 18, 2010Publication date: May 19, 2011Inventors: James E. MacDonald, McKelvy F. Jeffrey, Flossie Wong-Staal
-
Patent number: 7919530Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as Parkinson's disease, and the manufacture of medicaments for such treatment.Type: GrantFiled: July 10, 2009Date of Patent: April 5, 2011Assignee: Proteotech, Inc.Inventors: Luke A. Esposito, Joel Cummings, F. Michael Hudson, Alan D. Snow
-
Publication number: 20110039851Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: ApplicationFiled: October 14, 2008Publication date: February 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
-
Publication number: 20110034731Abstract: The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: Medichem, S.A.Inventors: Ernesto Durán López, Monica Benito Velez, Jordi Bosch i Lladó
-
Patent number: 7884134Abstract: The present invention is concerned with an improved method of producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide) comprising the O-methylation of a compound of formula I to produce a compound of formula II in a single step reaction.Type: GrantFiled: September 30, 2005Date of Patent: February 8, 2011Assignee: UCB Pharma GmbHInventors: Jens Riedner, Gavin Dunne
-
Publication number: 20110021482Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.Type: ApplicationFiled: September 17, 2010Publication date: January 27, 2011Inventors: Harold L. Kohn, Christophe Salomé, Elise Salomé-Grosjean
-
Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
-
Publication number: 20110021815Abstract: The present invention relates to halogenated compounds of formula (I) with the substituents as described within the specification. The compounds may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation.Type: ApplicationFiled: December 19, 2008Publication date: January 27, 2011Applicants: Fibrotech Therapeutics Pty Ltd, The University of MelbourneInventors: Darren James Kelly, Spencer John Williams, Steven Zammit
-
Publication number: 20100331410Abstract: A compound of formula: for treating ocular hypertension.Type: ApplicationFiled: February 5, 2009Publication date: December 30, 2010Applicant: Asterand UK LimitedInventors: Robert Coleman, David Middlemiss
-
Publication number: 20100298308Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: ApplicationFiled: November 14, 2006Publication date: November 25, 2010Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
-
Patent number: 7838706Abstract: The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4?-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3?-position of their B aryl ring. Similarly, 3?-amino combretastatin is 4?-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.Type: GrantFiled: May 16, 2007Date of Patent: November 23, 2010Assignee: Zhejiang Dade Pharmaceutical Group Co. LtdInventors: Weiping Shen, Jianping Wang, Jianguo Wang
-
Publication number: 20100280108Abstract: A compound of general formula (I) wherein, R11, R12, R13, R14, R15, W, Y, R1, R2, R3, R4, R5, and R6 take various meanings for use in the treatment of cancer.Type: ApplicationFiled: December 19, 2008Publication date: November 4, 2010Applicant: Pharma Mar, S.A.Inventors: Alberto Rodriguez Vicente, Maria Garranzo García-Ibarrola, Carmen Murcia Pérez, Francisco Sánchez Sancho, Maria del Carmen Cuevas Marchante, Cristina Mateo Urbano, Isabel Digón Juárez
-
Publication number: 20100249123Abstract: The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.Type: ApplicationFiled: March 19, 2008Publication date: September 30, 2010Applicant: ADDEX PHARMA SAInventors: Beatrice Bonnet, Brice Campo, Luca Raveglia, Mauro Riccaboni
-
Patent number: 7803970Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: June 7, 2004Date of Patent: September 28, 2010Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka, Dong Jin Hwang, Jiyun Chen
-
Publication number: 20100240712Abstract: Novel aromatic compounds of formula (I): wherein A1, A2, A3, A4, R1, R2, R5, G1, G2, Q1, Q2, Y1, Y2, Y3 and Y4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.Type: ApplicationFiled: October 13, 2008Publication date: September 23, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andre Denis Stoller, Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, William Lutz, Peter Maienfisch, Werner Zambach
-
Patent number: 7790926Abstract: Alpha, omega-difunctional aldaramides, in particular diaminoaldaramides, dihydroxyaldaramides, bis(alkoxycarbonylalkyl)aldaramides, and bis(carboxyalkyl)aldaramides, and processes for preparing the aldaramides are provided.Type: GrantFiled: January 31, 2008Date of Patent: September 7, 2010Assignee: E. I. du Pont de Nemours and CompanyInventors: Mark Allen Andrews, Henry Keith Chenault, Garret D. Figuly
-
Patent number: 7776922Abstract: The invention relates to substituted [(phenylethanoyl)amino]benzamides and methods for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of inflammatory disorders such as, for example, cutaneous, respiratory tract and cardiovascular disorders such as, for example, arteriosclerosis and coronary heart disease.Type: GrantFiled: November 17, 2005Date of Patent: August 17, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulf Brüggemeier, Petros Gatsios, Mark Meininghaus, Leila Telan, Elisabeth Woltering, Martina Wuttke, Hartmut Beck, Nils Griebenow, Frank Süβmeier, Niels Svenstrup, Axel Kretschmer, Marcus Bauser, Johannes Köbberling, Wahed Moradi, Siegfried Zaiss, Claudia Hirth-Dietrich, Barbara Albrecht
-
Publication number: 20100203650Abstract: The invention provides biomolecule binding ligands, collections of biomolecule binding ligands, and their use in the purification of biological mixtures and in the identification of ligands having an affinity for a substance.Type: ApplicationFiled: June 27, 2008Publication date: August 12, 2010Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventors: Christopher Robin Lowe, Abid Hussain, Michael Luis Mimmack, Jonathan Michael Haigh
-
Patent number: 7772432Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno-(1-6C)alkyl, hydroxyl-(1-6C)alkyl, di-[(1-6C)akly]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6C)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytType: GrantFiled: September 23, 2004Date of Patent: August 10, 2010Assignee: AstraZeneca ABInventors: Dearg Sutherland Brown, George Robert Brown
-
Patent number: 7767853Abstract: The present invention is directed to a compound represented by Structural Formula I: wherein the variables are described herein. Also included are methods of making the compounds of Structural Formula (I) and methods of using the compounds as antioxidants.Type: GrantFiled: October 17, 2007Date of Patent: August 3, 2010Assignee: Polnox CorporationInventors: Ashok L. Cholli, Rajesh Kumar, Taizoon Canteenwala, Vijayendra Kumar
-
Patent number: 7759520Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: February 23, 2005Date of Patent: July 20, 2010Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
-
Publication number: 20100173985Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.Type: ApplicationFiled: February 25, 2010Publication date: July 8, 2010Applicants: University of South Florida, McGill University, The Hong Kong Polytechnic UniversityInventors: Q. Ping Dou, Tak-Hang Chan, David M. Smith