Chalcogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/312)
  • Publication number: 20130184315
    Abstract: Compounds of formula (I) and formula (II) 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: Application
    Filed: July 18, 2011
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • Publication number: 20130184222
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 18, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
  • Publication number: 20130178633
    Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.
    Type: Application
    Filed: December 22, 2010
    Publication date: July 11, 2013
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Cédric Poinsard, Pascale Mauvais, Jean-Michel Linget, Sandrine Rethore, Patrice Lucien Maurice Collette, Isabelle Marie Joëlle Martine Collette
  • Publication number: 20130172564
    Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.
    Type: Application
    Filed: December 22, 2010
    Publication date: July 4, 2013
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Cédric Poinsard, Jean-Michel Rethore, Patrice Lucien Maurice Collette, Isabelle Marie Joëlle Collette
  • Publication number: 20130150368
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R2, R4, R5, R6, R7, R8, R9, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 22, 2011
    Publication date: June 13, 2013
    Applicant: CYTOKINETICS, INC.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R. Muci, Xiangping Qian, Antonio Romero, Jeffrey Warrington, Zhe Yang
  • Publication number: 20130143932
    Abstract: The present invention discloses optically pure (R) and (S) Phenyramidol enantiomers and their pharmaceutically acceptable salts, a process for synthesizing such enantiomers by means of a styrene oxide based synthesis, and also a clinical evaluation of (R) and (S) enantiomers of Phenyramidol, their salts and compositions thereof for enhanced/newer therapeutic benefits.
    Type: Application
    Filed: January 28, 2013
    Publication date: June 6, 2013
    Applicant: FERMENTA BIOTECH (UK) LIMITED
    Inventor: FERMENTA BIOTECH (UK) LIMITED
  • Publication number: 20130131056
    Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 23, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130131036
    Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Application
    Filed: October 23, 2012
    Publication date: May 23, 2013
    Applicant: AbbVie Inc.
    Inventor: AbbVie Inc.
  • Publication number: 20130090347
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, W, Y, R, R1, R2, R3 and R3? are as described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: September 27, 2012
    Publication date: April 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130082233
    Abstract: A method of forming a structure having selectively placed carbon nanotubes, a method of making charged carbon nanotubes, a bi-functional precursor, and a structure having a high density carbon nanotube layer with minimal bundling. Carbon nanotubes are selectively placed on a substrate having two regions. The first region has an isoelectric point exceeding the second region's isoelectric point. The substrate is immersed in a solution of a bi-functional precursor having anchoring and charged ends. The anchoring end bonds to the first region to form a self-assembled monolayer having a charged end. The substrate with charged monolayer is immersed in a solution of carbon nanotubes having an opposite charge to form a carbon nanotube layer on the self-assembled monolayer. The charged carbon nanotubes are made by functionalization or coating with an ionic surfactant.
    Type: Application
    Filed: September 29, 2011
    Publication date: April 4, 2013
    Applicant: International Business Machines Corporation
    Inventors: Ali Afzali-Ardakani, Hongsik Park, George Stojan Tulevski
  • Publication number: 20130085272
    Abstract: A procedure for using thermolabile groups to protect a hydroxyl function, above all in nucleosides, nucleotides, oligomers, nucleic acids during the reactions of organic synthesis. Various new compounds that can be used to implement the procedure. The way of using thermolabile groups to protect hydroxyl functions consists in a primary, secondary and tertiary hydroxyl group converting into a groups during the reaction between a compound and a compound whose hydroxyl group is to be blocked. The blocking reaction is carried out by means of widely known methods appropriate for that purpose in the presence of a chemically basic catalyst. The obtained product has its hydroxyl group blocked. Then the compound with the group blocked can be used for the purposes of various chemical processes. After their completion, the hydroxyl group is unblocked by dissolving it in a solvent at a temperature of 50-95° C.
    Type: Application
    Filed: June 1, 2011
    Publication date: April 4, 2013
    Applicant: INSTYTUT CHEMII BIOORGANICZNEJ POLSKIEJ AKADEMII NAUK
    Inventor: Marcin Krzysztof Chmielewski
  • Patent number: 8389551
    Abstract: The present invention discloses optically pure (R) and (S) Phenyramidol enantiomers and their pharmaceutically acceptable salts, a process for synthesizing such enantiomers by means of a styrene oxide based synthesis, and also a clinical evaluation of (R) and (S) enantiomers of Phenyramidol, their salts and compositions thereof for enhanced/newer therapeutic benefits.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: March 5, 2013
    Assignee: Fermenta Biotech (UK) Limited
    Inventors: Anupama Datla, Pramod Abaji Walavalker, Ashok Konda, Sreenath Babunath Trivikram
  • Patent number: 8383827
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: February 26, 2013
    Assignee: Novartis AG
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • Publication number: 20130035354
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: September 14, 2012
    Publication date: February 7, 2013
    Applicant: NOVARTIS AG
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • Publication number: 20130018054
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: NOVARTIS AG
    Inventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
  • Publication number: 20130012530
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20120329786
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.
    Type: Application
    Filed: August 31, 2012
    Publication date: December 27, 2012
    Applicant: Myrexis, Inc.
    Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup
  • Patent number: 8338612
    Abstract: Because fluazinam is excellent as an active ingredient of pesticides and highly useful, it is desired to produce it efficiently in a proper form with simple operations at low cost in an environmentally friendly manner. The desired product is obtained in good yields with simple operations by using industrially advantageous reaction systems by a process comprising (1) a step of reacting ACTF and DCDNBTF in the presence of an alkali component, a solvent selected from the group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water to substantially dissolve the alkali component, (2) a step of neutralizing or acidifying the reaction mixture with an acid and (3) a step of removing the solvent by distillation from the mixture containing fluazinam as the reaction product and the reaction solvent to precipitate crystals the product.
    Type: Grant
    Filed: July 29, 2008
    Date of Patent: December 25, 2012
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Shigeo Murai, Hiroshi Yoshizawa, Takeshi Ohshima, Katsuyoshi Murakami, Takayoshi Ando, Tadashi Nakamura, Norio Adachi, Akihiko Isogai
  • Patent number: 8334402
    Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: December 18, 2012
    Inventor: Thomas Daly
  • Publication number: 20120316171
    Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.
    Type: Application
    Filed: November 4, 2010
    Publication date: December 13, 2012
    Inventor: Tamas Oravecz
  • Patent number: 8318781
    Abstract: Disclosed is a novel aralkyl carboxylic acid compound which has an agonistic activity on GPR-120 and/or GPR-40, particularly GPR-120, and is therefore useful as an appetite regulator, an anti-obesity agent, a therapeutic agent for diabetes, a pancreatic beta differentiating cell growth enhancer, a therapeutic agent for metabolic syndrome, a therapeutic agent for a gastrointestinal disease, a therapeutic agent for a neuropathy, a therapeutic agent for a mental disorder, a therapeutic agent for a pulmonary disease, a therapeutic agent for a pituitary hormone secretion disorder or a lipid flavoring/seasoning agent. The aralkyl carboxylic acid compound is represented by the general formula (I).
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: November 27, 2012
    Assignees: Japan Science and Technology Agency, Kyoto University, Nagoya City University
    Inventors: Gozoh Tsujimoto, Akira Hirasawa, Naoki Miyata, Takayoshi Suzuki, Yoshiyuki Takahara, Masaji Ishiguro, Mie Hata
  • Publication number: 20120283101
    Abstract: The present invention pertains to plant additives containing a molecule selected in a family of compounds, wherein said molecule can modulate some molecular markers and physiological modifications observed in cases of phosphate deficiency. The family of compounds comprises the molecule MC2 of formula (I) as well as analogues thereof.
    Type: Application
    Filed: September 17, 2010
    Publication date: November 8, 2012
    Inventors: Mathilde Clement, Thierry Desnos, Laurent Nussaume
  • Patent number: 8288421
    Abstract: The invention relates to novel substituted 3-phenylamino-5-(3-aminophenyl)pyridines and corresponding pyrazines of formula (I), wherein A is CH or N, R1 represents C(?O)R9, S(?O)2R10, P(?O)(OR11)2, optionally substituted phenyl or optionally substituted heteroaryl, and the other substituents have the meaning described in the specification, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune diseases, and a method for the treatment of such a diseases.
    Type: Grant
    Filed: September 5, 2005
    Date of Patent: October 16, 2012
    Assignee: Basilea Pharmaceutica AG
    Inventors: Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Goutam Saha, Godhuli Nandi
  • Publication number: 20120259123
    Abstract: The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, a medical composition containing the same, and a medical composition for the treatment or prophylaxis of respiratory diseases or glaucoma.
    Type: Application
    Filed: December 24, 2010
    Publication date: October 11, 2012
    Applicant: UBE INDUSTRIES, LTD.
    Inventors: Ryo Iwamura, Masayuki Tanaka, Tetsushi Katsube, Nobuhiko Shibakawa, Manabu Shigetomi, Eiji Okanari, Tomoko Kanda, Yasunori Tokunaga, Hiroshi Fujiwara
  • Publication number: 20120225847
    Abstract: The present application discloses novel squaric acid derivatives of the formula A: from —C(?O)—, —S(?O)2—, —C(?S)— and —P(?O)(R5)—; B: -, —O—, —NR6— and —C(?O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankyl
    Type: Application
    Filed: June 24, 2009
    Publication date: September 6, 2012
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Publication number: 20120220635
    Abstract: The present invention relates to aromatic compounds of the formula (I) and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
    Type: Application
    Filed: February 27, 2012
    Publication date: August 30, 2012
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
  • Publication number: 20120202849
    Abstract: Disclosed herein is a novel synergistic pharmaceutical composition comprising hydroxychloroquine with insulin sensitizing agents and lipid lowering agents such as statins along with pharmaceutical excipients/carriers useful in treating Non-Alcoholic Fatty Liver Disease.
    Type: Application
    Filed: October 12, 2010
    Publication date: August 9, 2012
    Inventor: Anil Pareek
  • Publication number: 20120196838
    Abstract: The invention relates to certain compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders and immune disorders.
    Type: Application
    Filed: January 25, 2012
    Publication date: August 2, 2012
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
  • Publication number: 20120197023
    Abstract: The present invention relates to an improved process for the synthesis and purification of 3-chloro-N-(3-chloro-5-tri-fluoromethyl-2-pyridyl)-?,?,?-trifluoro-2,6-di-nitro-p-toluidine (fluazinam) and other pyridinamines, which implements methyl isobutyl ketone (MIBK) as the reaction solvent. The process of the invention overcomes the drawbacks of prior art methods, by reducing the side reactions such as hydrolysis, eliminating the need for difficult and labor-intensive purification methods, and providing pure products in higher yields. The present invention relates to novel crystalline polymorphic forms fluazinam, and to mixtures of the polymorphs. The present invention also provides methods for preparing the novel polymorphs, as well as pharmaceutical compositions comprising same, and methods of using the polymorphs as pesticidal agents for combating noxious living organisms on agricultural and horticultural crops.
    Type: Application
    Filed: April 11, 2012
    Publication date: August 2, 2012
    Applicant: Makhteshim Chemical Works Ltd.
    Inventors: Shlomi Cohen, Sharona Zamir
  • Publication number: 20120184747
    Abstract: This is to provide a novel aniline compound represented by the following formula (I) having an excellent broncho dilatory action based on potent EP2 agonistic action. A compound represented by the formula (I): or a salt thereof.
    Type: Application
    Filed: September 10, 2010
    Publication date: July 19, 2012
    Applicant: UBE INDUSTRIES, LTD.
    Inventors: Ryo Iwamura, Yoko Murakami, Masahiko Hagihara, Eiji Okanari
  • Patent number: 8211913
    Abstract: Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: July 3, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
  • Patent number: 8198457
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: June 12, 2012
    Assignee: Merck Serono S.A.
    Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
  • Publication number: 20120094964
    Abstract: The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.
    Type: Application
    Filed: May 6, 2010
    Publication date: April 19, 2012
    Inventors: Tadashi Inoue, Masashi Ohmi, Kiyoshi Kawamura, Kazuo Ando, Yuji Shishido
  • Publication number: 20120088746
    Abstract: Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Application
    Filed: May 10, 2007
    Publication date: April 12, 2012
    Applicants: PFIZER INC., RENOVIS, INC.
    Inventors: Yuji Shishido, Kazunari Nakao, Satoshi Nagayama, Hirotaka Tanaka, Matthew Alexander James Duncton, Matthew Cox, John Kincaid, Kiran Sahasrabudhe, Maria de Los Angeles Estiarte-Martinez
  • Publication number: 20120088803
    Abstract: Provided is a novel control agent for soft rot and a novel control method for the same. The control agent for soft rot of a plant contains 3-chloro-N-(3-chloro-5-trifluoromethyl-2-pyridyl)-alpha,alpha,alpha-trifluoro-2,6-dinitro-p-toluidine as an active ingredient, which is applied to plant cultivation soil.
    Type: Application
    Filed: June 4, 2010
    Publication date: April 12, 2012
    Applicant: Ishihara Sangyo Kaisha, Ltd
    Inventors: Yoshikazu Kurata, Hiroyuki Hayashi
  • Publication number: 20120028985
    Abstract: The present invention relates to the treatment and prevention of immunological and inflammatory disorders with a compound of formula (I) in combination with methotrexate,
    Type: Application
    Filed: November 6, 2009
    Publication date: February 2, 2012
    Applicant: 4SC AG
    Inventors: Manfred Gröppel, Johann Leban
  • Publication number: 20120022258
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: July 15, 2011
    Publication date: January 26, 2012
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • Publication number: 20120022116
    Abstract: Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject.
    Type: Application
    Filed: July 13, 2011
    Publication date: January 26, 2012
    Inventors: Huayun Deng, Ye Fang, Mingqian He, Haibei Hu, Weijun Niu, Haiyan Sun
  • Publication number: 20120022070
    Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.
    Type: Application
    Filed: October 6, 2009
    Publication date: January 26, 2012
    Applicant: EMORY UNIVERSITY
    Inventors: Jaeki Min, Pahk Thepchatri, Yuhong Du, Dennis C. Liotta, Haian Fu
  • Publication number: 20120015967
    Abstract: Pyridine and pyrimidine derivatives inhibit ubiquitination of human polypeptides, particularly of POSH and POSH-associated proteins such as HERPUD1, and can be used as medicaments for treatment of viral infections caused by virus such as HIV and for treatment of neurological disorders or diseases.
    Type: Application
    Filed: August 21, 2008
    Publication date: January 19, 2012
    Applicant: PROTEOLOGICS, LTD.
    Inventors: Philippe Nakache, Nurit Livnah
  • Publication number: 20120004244
    Abstract: There is provided compounds of formula I, wherein E1, E2a, E2b, E2c, E4, D1, D2, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
    Type: Application
    Filed: March 12, 2010
    Publication date: January 5, 2012
    Applicant: BIOLIPOX AB
    Inventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics
  • Publication number: 20110288296
    Abstract: The application relates to a reagent of the general formula R1R2N—ZnY LiY??(I) wherein R1, R2 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 is other than H; Y is selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; Halon, wherein n=3 or 4 and Hal is selected from Cl, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RXCO2; an alcoholate of the general formula ORX; a thiolate of the general formula SRX; RXP(O)O2; or SCORX; or SCSRX; OnSRx; wherein n=2 or 3; or NOn, wherein n=2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or
    Type: Application
    Filed: February 11, 2010
    Publication date: November 24, 2011
    Inventors: Paul Knochel, Marc Mosrin
  • Publication number: 20110269774
    Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.
    Type: Application
    Filed: April 29, 2011
    Publication date: November 3, 2011
    Inventors: Jerry ADAMS, Thomas Faitg, Neil Johnson, Jiri Kasparec, Hong Lin, Mark Mellinger, Xin Peng, Ren Xie
  • Publication number: 20110269760
    Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
    Type: Application
    Filed: July 14, 2011
    Publication date: November 3, 2011
    Applicant: Cytopia Research Pty Ltd
    Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
  • Publication number: 20110251393
    Abstract: The invention provides a helicene derivative, axially chiral amino acid, amine or amino alcohol derivative, and azaperylene, such as compounds represented by Formulae (I), (I?), (II), (II?), and (III): and a method for producing the same.
    Type: Application
    Filed: October 20, 2009
    Publication date: October 13, 2011
    Applicant: KYOTO UNIVERSITY
    Inventors: Takumi Furuta, Takeo Kawabata
  • Patent number: 8034951
    Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: October 11, 2011
    Inventor: Thomas Daly
  • Publication number: 20110245375
    Abstract: The present invention relates to curable compositions comprising a thermolatent amidine base and an organic material which is polymerisable or crosslinkable with a basic or nucleophilic catalyst. In particular, the invention relates to curable coating compositions, especially powder coating compositions, and curable adhesive compositions, as well as to the use a thermo-latent amidine base as a curing catalyst for thermally induced base- catalyzed polymerisation or crosslinking reactions.
    Type: Application
    Filed: November 18, 2009
    Publication date: October 6, 2011
    Applicant: BASF SE
    Inventors: Peter Nesvadba, Lucienne Bugnon Folger, Ralf Knischka
  • Publication number: 20110218208
    Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.
    Type: Application
    Filed: June 23, 2009
    Publication date: September 8, 2011
    Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
  • Publication number: 20110212945
    Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
    Type: Application
    Filed: August 8, 2008
    Publication date: September 1, 2011
    Applicant: ALMIRALL, S.A.
    Inventors: Julio Cesar Castro Palomino Laria, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
  • Publication number: 20110201609
    Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.
    Type: Application
    Filed: June 30, 2009
    Publication date: August 18, 2011
    Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida