One Of The Cyclos Is Five-membered Patents (Class 546/84)
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Publication number: 20140004111Abstract: The present invention relates to polycyclic antiviral compounds, and salts thereof, methods for their preparation and compositions containing them, and the use of the compounds and composition in the treatment of viral infections.Type: ApplicationFiled: August 30, 2013Publication date: January 2, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Jeffrey Peter Mitchell, Alistair George Draffan, Vanessa Anne Sanford, Silas Bond, Chin Yu Lim, Anne Mayes
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Patent number: 8609423Abstract: The present invention provides methods and compositions for labeling, separating and analyzing proteins, particularly a specific protein of interest within a cell lysate or in a mixture of proteins. The proteins are labeled with an amine reactive or thiol reactive fluorescent dye, or an amine reactive fluorogenic reagent that becomes fluorescent upon reacting to amine groups located on the protein. Following the labeling step, the proteins within the mixture can be separated and analyzed. In a further embodiment, a tag binding fluorogenic reagent that can bind to a tag on a tagged protein is added to specifically label the protein of interest.Type: GrantFiled: May 16, 2008Date of Patent: December 17, 2013Assignee: Life Technologies CorporationInventors: Thomas Diller, George Hanson, Bethany Sutton, Timothy Updyke
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Patent number: 8598193Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B—C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.Type: GrantFiled: December 24, 2004Date of Patent: December 3, 2013Assignee: Biota Scientific Management Pty Ltd.Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Jeffrey Peter Mitchell, Alistair George Draffan, Roland Henry Nearn
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Publication number: 20130310366Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 12, 2013Publication date: November 21, 2013Applicant: Albany Molecular Research, Inc.Inventors: David D. MANNING, Christopher L. CIOFFI
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Publication number: 20130303375Abstract: The present invention relates to novel strigolactam derivatives of formula (I) to processes and intermediates for pre-paring them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: ApplicationFiled: December 9, 2011Publication date: November 14, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Mathilde Denise Lachia, Alain De Mesmaeker, Hanno Christian Wolf, Pierre Joseph Marcel Jung
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Publication number: 20130253001Abstract: An object of the present invention is to provide a salt of pyrroloquinoline quinone having a high solubility in water and in an organic solvent and a method for producing the same. According to the present invention, there are provided an ammonium salt of pyrroloquinoline quinone having a high solubility in water and in an organic solvent, consisting of a pyrroloquinoline quinone ion and an ammonium salt having a hydroxyl group.Type: ApplicationFiled: November 25, 2011Publication date: September 26, 2013Applicant: MITSUBISHI GAS CHEMICAL COMPANY INC.Inventor: Kazuto Ikemoto
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Publication number: 20130225632Abstract: An object of the present invention is to provide an industrially useful method for producing a calcium salt of pyrroloquinoline quinone, without using large amounts of organic solvents, and highly pure crystals produced thereby. According to the present invention, a highly pure calcium salt of pyrroloquinoline quinone can be produced by reacting an alkali metal salt of pyrroloquinoline quinone with a source of calcium ions.Type: ApplicationFiled: September 22, 2011Publication date: August 29, 2013Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.Inventors: Kazuto Ikemoto, Masahiko Nakano
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Publication number: 20130203869Abstract: An object of the present invention is to provide a gel containing pyrroloquinoline quinone that is capable of easily forming a gel near room temperature and is useful even in the food sector, and a method for producing the gel. According to the present invention, there is provided a gel containing pyrroloquinoline quinone that uses pyrroloquinoline quinone itself as a gelling agent and a method for producing the gel by adding a salt of pyrroloquinoline quinone to water and subsequently adjusting the temperature or the pH to reduce solubility.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.Inventors: Tsuyoshi Mikekado, Kazuto Ikemoto, Hajime Shimizu
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Patent number: 8501729Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: GrantFiled: February 14, 2012Date of Patent: August 6, 2013Assignee: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Patent number: 8481561Abstract: The present invention relates to novel GABAA/BzR ligands of the general formulas (I), (II) and (III) wherein R1 is selected from the group consisting of hydrogen, halogen, haloalkyl having 1-2 carbon atoms, alkoxy having 1 to 3 carbon atoms in the alkyl chain, alkyl having 1 to 3 carbon atoms, and nitro, and R2 is selected from the group consisting of hydrogen, halogen and alkyl having 1 to 2 carbon atoms, as well as the use of these compounds for treating anxiolytic, anticonvulsant, sedative-hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals including pharmaceutical compositions comprising the same.Type: GrantFiled: April 2, 2009Date of Patent: July 9, 2013Assignee: Innovationspatent Sverige ABInventors: Mogens Peter Cherly Nielsen, Tommy Liljefors, Jakob Alexander Nilsson, Olov A Sterner
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Patent number: 8461175Abstract: The invention relates to a compound of formula (I), where: R1 is a phenyl group optionally substituted by one or more halogen atoms; R2 is: a hydrogen atom or a halogen atom or a cyano group; a —C(?O)Y group where Y is a hydrogen atom, or a —NH2 or —OR3 group; a —C(?S)NH2 group; a —C(?NH)NH—OH group; a —CH2OH or —CH2F group; a —CH?N—OH group; a —CH?CH2 or —C?C—R3 group; a H or H R1 group being a hydrogen or (C1-C4)alkyl group; R3 is a hydrogen atom or (C1-C4)alkyl group; and R4 is a —NH2, (C1-C4)alkyl, (C1-C4)fluoroalkyl or (C3-C7)cycloalkyl group.Type: GrantFiled: April 22, 2010Date of Patent: June 11, 2013Assignee: Sanofi-AventisInventors: Georges Delettre, Stéphanie Deprets, Frank Halley, Laurent Schio, Fabienne Thompson
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Publication number: 20130123215Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: November 9, 2012Publication date: May 16, 2013Applicant: ALLERGAN, INC.Inventor: Allergan, Inc.
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Publication number: 20130109686Abstract: The present invention is directed to isoindolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: June 27, 2011Publication date: May 2, 2013Inventors: Douglas C. Beshore, Scott D. Kuduk, Youheng Shu, Zhi-Qiang Yang
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Publication number: 20130071927Abstract: The present invention provides a cell passaging medium comprising at least one agent capable of detaching from a surface a cell that is culture in vitro on said surface, and a water-soluble polymer capable of protecting the detached cell. The present invention also provides a cell culturing medium comprising one or more cell culture protectants capable of protecting cells in culture. The present invention further relates to the use of said media in methods for culturing cells in vitro or for deriving monolayer cell cultures of mammalian stem cells.Type: ApplicationFiled: May 5, 2011Publication date: March 21, 2013Applicant: Sydney IVF LimitedInventors: David Lu, Uli Schmidt, Cara Bradley, Sandra Lubitz, Tomas Stojanov
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Patent number: 8399449Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: GrantFiled: February 25, 2009Date of Patent: March 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
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Publication number: 20130059879Abstract: Small molecule inhibitors of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) having the following formula: Formula (1) are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting PFK.FB3 enzymatic activity, methods of inhibiting glycolytic flux, and methods of treating tumors by administering an effective amount of a Formula I compound.Type: ApplicationFiled: February 22, 2011Publication date: March 7, 2013Applicants: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC., ADVANCED CANCER THERAPEUTICS, LLCInventors: Pooran Chand, Jason A. Chesney, Brian F. Clem, Gilles H. Tapolsky, Sucheta Telang, John O. Trent
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Publication number: 20120323009Abstract: An object of the present invention is to provide a method for conveniently producing reduced pyrroloquinoline quinone from oxidized pyrroloquinoline quinone without needing expensive equipment, and a method for stabilizing reduced pyrroloquinoline quinone. According to the present invention, high-quality reduced pyrroloquinoline quinone can be obtained conveniently and efficiently in a manner suitable for industrial-scale production by mixing pyrroloquinoline quinone and ascorbic acid in a solvent.Type: ApplicationFiled: February 16, 2011Publication date: December 20, 2012Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.Inventors: Kazuto Ikemoto, Masahiko Nakano, Junichi Edahiro
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Publication number: 20120301427Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HW).Type: ApplicationFiled: January 25, 2012Publication date: November 29, 2012Inventors: Gary BRIDGER, Al KALLER, Curtis HARWIG, Renato SKERLJ, David BOGUCKI, Trevor R. WILSON, Jason CRAWFORD, Ernest J. MCEACHERN, Bem ATSMA, Siqiao NAN, Yuanxi ZHOU, Dominique SCHOLS, Christopher D. SMITH, Maria R. DI FLURI
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Patent number: 8299090Abstract: The present invention relates to substituted thiazolyl- and oxazoyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.Type: GrantFiled: June 18, 2009Date of Patent: October 30, 2012Inventors: Roberto Pellicciari, Flavio Moroni, Adam Matthew Gilbert
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Patent number: 8293732Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.Type: GrantFiled: December 4, 2007Date of Patent: October 23, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Ismet Dorange, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
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Publication number: 20120251491Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 12, 2010Publication date: October 4, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
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Publication number: 20120231995Abstract: There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.Type: ApplicationFiled: May 17, 2012Publication date: September 13, 2012Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Petra Helga Beck, Marc Barry Brown, David Edward Clark, Anthony Coates, Hazel Joan Dyke, Yanmin Hu, Derek John Londesbrough, Keith Mills, Thomas David Pallin, Gary Patrick Reid, Gerlinda Stoddart
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Publication number: 20120225873Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: April 13, 2012Publication date: September 6, 2012Applicant: Myrexis, Inc.Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
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Publication number: 20120226045Abstract: An object of the present invention is to provide a method for conveniently producing pyrroloquinoline quinone in the free form without any organic solvent or ion-exchange resin and highly-pure crystals thereof. According to the present invention, there is provided a production method of pyrroloquinoline quinone in the free form and highly-pure crystals thereof, wherein the production method comprises preparing a solution having a pH of 1.5 or less by dissolving an alkali metal salt of pyrroloquinoline quinone to obtain a precipitate.Type: ApplicationFiled: November 5, 2010Publication date: September 6, 2012Applicant: MITSUBISHI GAS CHEMICAL COMPANY INC.Inventors: Kazuto Ikemoto, Junichi Edahiro
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Publication number: 20120219641Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: February 14, 2012Publication date: August 30, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20120220621Abstract: The invention relates to a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [?]D=?38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a base or an acid addition salt, in particular a pharmaceutically acceptable acid. The compound is a selective Aurora A and B kinase inhibitor and can be used as an anticancer drug.Type: ApplicationFiled: May 17, 2010Publication date: August 30, 2012Applicant: SANOFIInventors: Jean-Christophe Carry, Michel Cheve, Francois Clerc, Cecile Combeau, Sylvie Gontier, Alain Krick, Sylvette Lachaud, Laurent Schio
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Publication number: 20120172598Abstract: The present invention provides compounds having superior TAFIa inhibitory activity.Type: ApplicationFiled: September 17, 2010Publication date: July 5, 2012Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Hideaki Amada, Daisuke Matsuda, Ayako Bohno
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Patent number: 8207180Abstract: The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.Type: GrantFiled: November 23, 2007Date of Patent: June 26, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Francesco Casuscelli, Barbara Forte, Maria Menichincheri, Alessandra Scolaro, Gabriella Traquandi, Paola Vianello
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Publication number: 20120149688Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 10, 2011Publication date: June 14, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
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Patent number: 8198290Abstract: The present invention provides for compounds of Formula I and II: wherein y, X, Y, Z, R1, and R2 have any of the values defined there for in the specification. The compounds of formula I are useful as reagents in the isolation and the assay of PQQ dependent enzymes. Also provided are compositions comprising compounds of Formula I and II.Type: GrantFiled: December 23, 2009Date of Patent: June 12, 2012Assignee: Berry and Associates, Inc.Inventor: John C. Hodges
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Patent number: 8193357Abstract: Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors, and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: GrantFiled: June 12, 2006Date of Patent: June 5, 2012Assignee: Ligand Pharmaceuticals IncorporatedInventors: Bijan Pedram, Cornelis Arjan Van Oeveren, Lin Zhi, Shuo Zhao, Yixing Shen
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Publication number: 20120129884Abstract: The present invention concerns the synthesis of new analogs of angelicins, pyrrolo [3,2-h]quinoline, for the treatment of pathologies having hyperproliferative character included those having neoplastic nature. The treatment is based on the combined action of pyrrolo [3,2-h]quinolines and UV-A light, through a clinical approach defined as PUVA (psoralen-UVA light). The most important feature of these compounds is that they exert their remarkable photoxicity without any DNA damage, which is the main origin of the side effects of the PUVA therapy.Type: ApplicationFiled: July 28, 2010Publication date: May 24, 2012Applicant: UNIVERSITA DEGLI STUDI DI PADOVAInventors: Francesco Dall'Acqua, Girolamo Cirrincione, Paolo Barraja, Alessia Vador
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Publication number: 20120116087Abstract: A crystal of pyrroloquinoline quinone disodium salt having peaks at 2? of 9.1°, 10.3°, 13.8°, 17.7°, 18.3°, 24.0°, 27.4°, 31.2° and 39.5° (±0.2° for each) in powder X-ray diffractometry using Cu K? radiation, or a crystal of pyrroloquinoline quinone trisodium salt having peaks at 2? of 6.6°, 11.4°, 13.0°, 22.6°, 26.9°, 27.9°, 37.0°, 38.9° and 43.4° (±0.2° for each) in powder X-ray diffractometry using Cu K? radiation.Type: ApplicationFiled: June 9, 2010Publication date: May 10, 2012Applicant: Mitsubishi Gas Chemical Company, Inc.Inventors: Junichi Edahiro, Hitoshi Sakamoto, Kazuto Ikemoto, Hajime Shimizu, Tatsuya Hasegawa, Masahiko Nakano
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Publication number: 20120108581Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.Type: ApplicationFiled: March 25, 2010Publication date: May 3, 2012Applicant: Kowa Company, LtdInventors: Masanori Ashikawa, Toshiharu Morimoto, Hajime Yamada, Shunji Takemura, Tatsuaki Nishiyama, Takeshi Doi, Hiroyuki Ishiwata
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Patent number: 8168308Abstract: The present invention is to provide an organic compound having excellent characteristics as a material for an organic EL device having a high efficiency and a high durability, and to provide an organic EL device having a high efficiency and a high durability by using the compound.Type: GrantFiled: August 16, 2007Date of Patent: May 1, 2012Assignee: Hodogaya Chemical Co., Ltd.Inventors: Norimasa Yokoyama, Shuichi Hayashi, Shigeru Kusano
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Patent number: 8163752Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: June 3, 2008Date of Patent: April 24, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Ian Bell, Craig A. Stump
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Patent number: 8163768Abstract: This invention relates to compounds of formula (I) to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.Type: GrantFiled: January 15, 2008Date of Patent: April 24, 2012Assignee: Aventis Pharma S.A..Inventors: Jacques Mauger, Anil Nair, Nina Ma, Kirsten Bjergarde, Bruno Filoche-Romme, Odile Angouillant-Boniface, Serge Mignani, Jean-Christophe Carry, Francois Clerc, Herve Minoux, Laurent Schio, Cecile Combeau
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Patent number: 8138333Abstract: The present invention relates to novel compounds of formula (I): wherein R1, R2, R3, R4, and R5 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: GrantFiled: March 13, 2008Date of Patent: March 20, 2012Assignee: Proximagen LimitedInventors: Johan Angbrant, Peter Brandt, Rune Ringom, Bengt Lindqvist
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Patent number: 8133902Abstract: A compound having the general the general structure I is provided: (Formula I), wherein Z is a substituent selected from a group consisting of S and O; X is a substituent selected from a group consisting of Cl, Br, I, OH and NH2; each of R1 and R2 is a substituent independently selected from a group consisting of H, a linear, cyclic or branched, substituted or unsubstituted C1-C6 alkyl, a substituted or unsubstituted aryl, and a substituted or unsubstituted heteroaryl; and each of Y and Y1 is a substituent independently selected from a group consisting of H and C(O)—C6H4—Br.Type: GrantFiled: June 27, 2008Date of Patent: March 13, 2012Assignee: The Regents of the University of CaliforniaInventors: William Fenical, Paul Jensen, John MacMillan, Chambers C. Hughes, James J. LaClair
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Patent number: 8124600Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: GrantFiled: May 28, 2009Date of Patent: February 28, 2012Assignee: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20120022056Abstract: Compounds of formula (I) wherein R1, R2, X, A, Y, B, Z1, Q, p, r and s are defined in the specification for treating inter alia psychotic disorders, depressive disorders, anxiety disorders and sexual dysfunctions.Type: ApplicationFiled: August 29, 2005Publication date: January 26, 2012Inventors: Jonathan Bentley, Markus Bergauer, Babara Bertani, Matteo Biagetti, Manuela Borriello, Steven Mark Bromidge, Massimo Gianotti, Enrica Granci, Colin Philip Leslie, Alessandra Pasquarello, Valeria Zucchelli
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Publication number: 20110313164Abstract: Lithium derivatives of pyrroloquinoline quinone and preparation method thereof are disclosed. In said method, lithium derivatives of pyrroloquinoline quinone are obtained by an acid-base neutralization reaction in a basic solvent with pyrroloquinoline quinine (PQQ) as a starting material. Lithium ion is brought in the molecular structure of pyrroloquinoline quinone to form said lithium derivatives of pyrroloquinoline quinone. The reaction condition of said method is mild, the product is easy to be purified, the preparation procedure is simple, and the yield is more than 80%. Said lithium derivatives of pyrroloquinoline quinone possess GSK-3 inhibiting activity and possess the functions such as reducing the formation of age pigment in the brain of a transgenic mouse and reducing the phosphorylation of tau proteins. Said lithium derivatives of pyrroloquinoline quinone may be used in the manufacture of medicaments for preventing and treating senile dementia, senility or Parkinson's disease.Type: ApplicationFiled: March 29, 2010Publication date: December 22, 2011Inventors: Chun-Jiu Zhong, Qing Yang
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Publication number: 20110312957Abstract: The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV.Type: ApplicationFiled: September 15, 2009Publication date: December 22, 2011Applicant: CSIRInventors: Moira Leanne Bode, Amanda Louise Rousseau, David Gravestock, Simon Sana Moleele, Christiaan Wynand Van Der Westhuyzen
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Patent number: 8048895Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: GrantFiled: April 18, 2008Date of Patent: November 1, 2011Assignee: Research Triangle InstituteInventors: Frank Ivy Carroll, Hernan A. Navarro, James B. Thomas, Tingwei Cai
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Publication number: 20110263494Abstract: Disclosed are compounds of Formula (I) wherein: one of A and D is —N— and the other of A and D is —C—; or enantiomers, diastereomers, or pharmaceutically-acceptable salts thereof. Also disclosed are methods of using such compounds to modulate the function of glucocorticoid receptor activity and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: October 30, 2008Publication date: October 27, 2011Inventors: T.G. Murali Dhar, Hai-Yun Xiao
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Publication number: 20110245503Abstract: Described herein is a new asymmetric synthesis of imines to obtain ?-carboline derivatives useful as key intermediate compounds for the synthesis of phosphodiesterase inhibitors using a new process with palladium or ruthenium hydride and/or nickel boride to reduce chiral intermediates. The use of chloroformate chiral auxiliaries is further described for the reduction and asymmetric hydrogenation of imines to obtain ?-carboline derivatives and intermediate compounds used in the preparation thereof.Type: ApplicationFiled: November 27, 2009Publication date: October 6, 2011Applicant: UNIVERSIDAD DE TALCAInventors: Leonardo Santos, Marlene Espinoza Moraga, Nagula Shankarajah
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Publication number: 20110224334Abstract: A near-infrared-ray absorbing material which contains a cyanine compound represented by general formula (I), shows a narrow peak of light absorption in the range of wavelengths of 800-1,000 nm, and has excellent light resistance. In formula (I), R1 to R4, Y1, and Y2 each represents a hydrogen atom, a group of formula (II) or (II?), etc., and Anq? represents a q-valent anion, provided that at least R1 is a group of formula (II) or (II') or Anq? is an ion of formula (III); R11 to R13 each represents a hydrogen atom, hydroxy, etc.; and Z1 and Z2 each represents a C1-10 alkyl, etc. In formula (II?), the bond between G? and T? is a double bond or a conjugated double bond; G? represents a carbon atom; T? represents a carbon atom or a nitrogen atom; the ring including G? and T? represents a 6-membered ring, etc.; w? is 0-4; and R01? represents a hydrogen atom, hydroxy, etc. In formula (III), R5 and R6 each represents a C1-8 haloalkyl.Type: ApplicationFiled: November 18, 2009Publication date: September 15, 2011Applicant: ADEKA CORPORATIONInventors: Yosuke Maeda, Ryoya Otsuki, Koichi Shigeno
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Patent number: 8013159Abstract: The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.Type: GrantFiled: May 15, 2006Date of Patent: September 6, 2011Assignee: Merck Canada Inc.Inventors: Michel Belley, Jason Burch, John Colucci, Julie Farand, Mario Girard, Yongxin Han
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Publication number: 20110213143Abstract: Provided are compounds having superior TAFIa inhibitory activity.Type: ApplicationFiled: October 28, 2009Publication date: September 1, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Hideaki Amada, Daisuke Matsuda, Masahiro Bohno, Shiuji Saito, Ayako Bohno
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Patent number: 8003661Abstract: The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: March 25, 2008Date of Patent: August 23, 2011Assignee: Merck Canada Inc.Inventors: Jason Burch, Julie Farand, Yongxin Han, Claudio Sturino