Chalcogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/312)
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Publication number: 20130184315Abstract: 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: ApplicationFiled: July 18, 2011Publication date: July 18, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbHInventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
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Publication number: 20130184222Abstract: 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: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20130178633Abstract: 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: ApplicationFiled: December 22, 2010Publication date: July 11, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Pascale Mauvais, Jean-Michel Linget, Sandrine Rethore, Patrice Lucien Maurice Collette, Isabelle Marie Joëlle Martine Collette
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Publication number: 20130172564Abstract: 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: ApplicationFiled: December 22, 2010Publication date: July 4, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Jean-Michel Rethore, Patrice Lucien Maurice Collette, Isabelle Marie Joëlle Collette
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Publication number: 20130150368Abstract: 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: ApplicationFiled: April 22, 2011Publication date: June 13, 2013Applicant: 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
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Publication number: 20130143932Abstract: 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: ApplicationFiled: January 28, 2013Publication date: June 6, 2013Applicant: FERMENTA BIOTECH (UK) LIMITEDInventor: FERMENTA BIOTECH (UK) LIMITED
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Publication number: 20130131056Abstract: 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: ApplicationFiled: January 15, 2013Publication date: May 23, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130131036Abstract: 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: ApplicationFiled: October 23, 2012Publication date: May 23, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130090347Abstract: 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: ApplicationFiled: September 27, 2012Publication date: April 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130082233Abstract: 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: ApplicationFiled: September 29, 2011Publication date: April 4, 2013Applicant: International Business Machines CorporationInventors: Ali Afzali-Ardakani, Hongsik Park, George Stojan Tulevski
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Publication number: 20130085272Abstract: 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: ApplicationFiled: June 1, 2011Publication date: April 4, 2013Applicant: INSTYTUT CHEMII BIOORGANICZNEJ POLSKIEJ AKADEMII NAUKInventor: Marcin Krzysztof Chmielewski
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Patent number: 8389551Abstract: 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: GrantFiled: February 16, 2010Date of Patent: March 5, 2013Assignee: Fermenta Biotech (UK) LimitedInventors: Anupama Datla, Pramod Abaji Walavalker, Ashok Konda, Sreenath Babunath Trivikram
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Patent number: 8383827Abstract: 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: GrantFiled: May 14, 2010Date of Patent: February 26, 2013Assignee: Novartis AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Publication number: 20130035354Abstract: 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: ApplicationFiled: September 14, 2012Publication date: February 7, 2013Applicant: NOVARTIS AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Publication number: 20130018054Abstract: 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: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
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Publication number: 20130012530Abstract: 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: ApplicationFiled: July 6, 2012Publication date: January 10, 2013Applicant: H. Lundbeck A/SInventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
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Publication number: 20120329786Abstract: 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: ApplicationFiled: August 31, 2012Publication date: December 27, 2012Applicant: 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
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Patent number: 8338612Abstract: 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: GrantFiled: July 29, 2008Date of Patent: December 25, 2012Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Shigeo Murai, Hiroshi Yoshizawa, Takeshi Ohshima, Katsuyoshi Murakami, Takayoshi Ando, Tadashi Nakamura, Norio Adachi, Akihiko Isogai
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Patent number: 8334402Abstract: 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: GrantFiled: October 6, 2010Date of Patent: December 18, 2012Inventor: Thomas Daly
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Publication number: 20120316171Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.Type: ApplicationFiled: November 4, 2010Publication date: December 13, 2012Inventor: Tamas Oravecz
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Patent number: 8318781Abstract: 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: GrantFiled: April 25, 2008Date of Patent: November 27, 2012Assignees: Japan Science and Technology Agency, Kyoto University, Nagoya City UniversityInventors: Gozoh Tsujimoto, Akira Hirasawa, Naoki Miyata, Takayoshi Suzuki, Yoshiyuki Takahara, Masaji Ishiguro, Mie Hata
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Publication number: 20120283101Abstract: 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: ApplicationFiled: September 17, 2010Publication date: November 8, 2012Inventors: Mathilde Clement, Thierry Desnos, Laurent Nussaume
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Patent number: 8288421Abstract: 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: GrantFiled: September 5, 2005Date of Patent: October 16, 2012Assignee: Basilea Pharmaceutica AGInventors: Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Goutam Saha, Godhuli Nandi
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Publication number: 20120259123Abstract: 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: ApplicationFiled: December 24, 2010Publication date: October 11, 2012Applicant: UBE INDUSTRIES, LTD.Inventors: Ryo Iwamura, Masayuki Tanaka, Tetsushi Katsube, Nobuhiko Shibakawa, Manabu Shigetomi, Eiji Okanari, Tomoko Kanda, Yasunori Tokunaga, Hiroshi Fujiwara
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Publication number: 20120225847Abstract: 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, ankylType: ApplicationFiled: June 24, 2009Publication date: September 6, 2012Inventors: Mette Knak Christensen, Fredrik Bjorkling
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Publication number: 20120220635Abstract: 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: ApplicationFiled: February 27, 2012Publication date: August 30, 2012Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
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Publication number: 20120202849Abstract: 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: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Inventor: Anil Pareek
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Publication number: 20120196838Abstract: 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: ApplicationFiled: January 25, 2012Publication date: August 2, 2012Applicant: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
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Publication number: 20120197023Abstract: 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: ApplicationFiled: April 11, 2012Publication date: August 2, 2012Applicant: Makhteshim Chemical Works Ltd.Inventors: Shlomi Cohen, Sharona Zamir
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Publication number: 20120184747Abstract: 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: ApplicationFiled: September 10, 2010Publication date: July 19, 2012Applicant: UBE INDUSTRIES, LTD.Inventors: Ryo Iwamura, Yoko Murakami, Masahiko Hagihara, Eiji Okanari
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Patent number: 8211913Abstract: Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof used in the form of pharmaceutical compositions.Type: GrantFiled: February 17, 2009Date of Patent: July 3, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
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Patent number: 8198457Abstract: 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: GrantFiled: May 20, 2011Date of Patent: June 12, 2012Assignee: 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
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Publication number: 20120094964Abstract: 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: ApplicationFiled: May 6, 2010Publication date: April 19, 2012Inventors: Tadashi Inoue, Masashi Ohmi, Kiyoshi Kawamura, Kazuo Ando, Yuji Shishido
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Publication number: 20120088746Abstract: 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: ApplicationFiled: May 10, 2007Publication date: April 12, 2012Applicants: 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
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Publication number: 20120088803Abstract: 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: ApplicationFiled: June 4, 2010Publication date: April 12, 2012Applicant: Ishihara Sangyo Kaisha, LtdInventors: Yoshikazu Kurata, Hiroyuki Hayashi
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Publication number: 20120028985Abstract: 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: ApplicationFiled: November 6, 2009Publication date: February 2, 2012Applicant: 4SC AGInventors: Manfred Gröppel, Johann Leban
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Publication number: 20120022258Abstract: 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: ApplicationFiled: July 15, 2011Publication date: January 26, 2012Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
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Publication number: 20120022116Abstract: 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: ApplicationFiled: July 13, 2011Publication date: January 26, 2012Inventors: Huayun Deng, Ye Fang, Mingqian He, Haibei Hu, Weijun Niu, Haiyan Sun
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Publication number: 20120022070Abstract: 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: ApplicationFiled: October 6, 2009Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventors: Jaeki Min, Pahk Thepchatri, Yuhong Du, Dennis C. Liotta, Haian Fu
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Publication number: 20120015967Abstract: 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: ApplicationFiled: August 21, 2008Publication date: January 19, 2012Applicant: PROTEOLOGICS, LTD.Inventors: Philippe Nakache, Nurit Livnah
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Publication number: 20120004244Abstract: 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: ApplicationFiled: March 12, 2010Publication date: January 5, 2012Applicant: BIOLIPOX ABInventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics
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Publication number: 20110288296Abstract: 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, orType: ApplicationFiled: February 11, 2010Publication date: November 24, 2011Inventors: Paul Knochel, Marc Mosrin
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Publication number: 20110269774Abstract: 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: ApplicationFiled: April 29, 2011Publication date: November 3, 2011Inventors: Jerry ADAMS, Thomas Faitg, Neil Johnson, Jiri Kasparec, Hong Lin, Mark Mellinger, Xin Peng, Ren Xie
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Publication number: 20110269760Abstract: 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: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: Cytopia Research Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
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Publication number: 20110251393Abstract: 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: ApplicationFiled: October 20, 2009Publication date: October 13, 2011Applicant: KYOTO UNIVERSITYInventors: Takumi Furuta, Takeo Kawabata
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Patent number: 8034951Abstract: 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: GrantFiled: March 31, 2010Date of Patent: October 11, 2011Inventor: Thomas Daly
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Publication number: 20110245375Abstract: 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: ApplicationFiled: November 18, 2009Publication date: October 6, 2011Applicant: BASF SEInventors: Peter Nesvadba, Lucienne Bugnon Folger, Ralf Knischka
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Publication number: 20110218208Abstract: 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: ApplicationFiled: June 23, 2009Publication date: September 8, 2011Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Publication number: 20110212945Abstract: 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: ApplicationFiled: August 8, 2008Publication date: September 1, 2011Applicant: 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
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Publication number: 20110201609Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.Type: ApplicationFiled: June 30, 2009Publication date: August 18, 2011Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South FloridaInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida