Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/174)
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Publication number: 20130184464Abstract: Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. In Formula 2, X represents F, Cl, Br or I.Type: ApplicationFiled: December 28, 2012Publication date: July 18, 2013Applicant: Dong Kook Pharm. Co., Ltd.Inventor: Dong Kook Pharm. Co., Ltd.
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Publication number: 20130178499Abstract: The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: October 7, 2011Publication date: July 11, 2013Applicant: N30 PHARMACEUTICALS, INC.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Patent number: 8481534Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: June 25, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20130157998Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.Type: ApplicationFiled: November 19, 2012Publication date: June 20, 2013Applicant: CALITHERA BIOSCIENCES INC.Inventor: Calithera Biosciences Inc.
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Publication number: 20130131096Abstract: The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R1 represents a hydrogen atom, lower alkyl group, lower alkenyl group, lower cycloalkyl group, aryl group, aralkyl group or heterocyclic group, wherein, the above groups are optionally substituted in ortho, meta and/or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R2 represents a hydrogen atom, lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted with one or more halogen atoms; R3 represents a lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted in ortho, meta or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R4 represents a hydrogen atom, lower alkyl group or any acidic functional group; n is 1 or 2).Type: ApplicationFiled: May 6, 2011Publication date: May 23, 2013Inventors: Laszlo Puskas, Csaba Szabo, Ivan Kanizsai, Mario Gyuris, Ramona Madacsi, Bela Ozsvari, Liliana Feher, Gabor Tamas
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Publication number: 20130123344Abstract: Disclosed are compounds and pharmaceutical compositions containing compounds that inhibit JMJD2 proteins, including those of the formula (I): wherein R1, R2, R3, R4, and R5 are as defined herein or pharmaceutically acceptable salts thereof. Also disclosed is a method of preventing or treating a viral infection of a host, comprising administering to the host an effective amount of an inhibitor of the JMJD2 family of histone demethylases, for example, a compound of the formula (I). The viral infection may be a primary infection, reactivation of a virus after latency in a host, or may be in a mammal that has undergone, is undergoing, or will undergo immunosuppressive therapy.Type: ApplicationFiled: January 22, 2013Publication date: May 16, 2013Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventor: The United States of America, as Represented by the Secretary, Department of Health and Human Services
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Patent number: 8426600Abstract: Disclosed is a method for preparing a montelukast sodium salt of Formula 1. The method includes coupling a methanesulfonyl compound of Formula 2 below with a compound of Formula 3 below in the presence of a bistrimethylsilylamide alkali metal salt, further adding an alkali metal base thereto and hydrolyzing the mixture by heating to prepare a compound of Formula 4 below, reacting the compound of Formula 4 with 4-tert-butylcyclohexylamine, followed by purification, to prepare an amine salt of Formula 5, and converting the amine salt of Formula 5 into a sodium salt.Type: GrantFiled: September 25, 2009Date of Patent: April 23, 2013Assignee: LG Life Sciences, Ltd.Inventors: In Sang Lee, Seok Ju Lee, Jae Eun Kang
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Patent number: 8426599Abstract: The present invention relates to a method for preparing Montelukast acid or its sodium salt by reacting a thiol compound with a Montelukast intermediate in the presence of a base in a medium comprising an ionic liquid compound. In accordance with the inventive method, highly pure Montelukast acid or its sodium salt, which is advantageously used as a raw material in the preparation of Montelukast, a leukotriene antagonist, can be easily prepared in a high yield.Type: GrantFiled: October 1, 2008Date of Patent: April 23, 2013Assignee: Hanmi Science Co., LtdInventors: Chul-Hyun Park, Eun-Ju Park, Choong-Hahn Kim, Suk Man Jang, Eun Jung Lim, Young Kil Chang, Gwan Sun Lee, Jaeheon Lee
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Publication number: 20130045935Abstract: This invention relates to bis-flavonoid compounds of formula Flavonoid-Linker-Y-Linker-Flavonoid, their synthesis and use for inhibiting multidrug resistance in chemotherapy and protozoan infection.Type: ApplicationFiled: May 3, 2011Publication date: February 21, 2013Inventors: Tak-Hang Chan, Larry Ming-Cheung Chow, Kin-Fai Chan, Iris Lai King Wong
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Publication number: 20130005963Abstract: An organic photoelectric conversion material for use in an organic thin-film photoelectric conversion device, containing a compound represented by formula 1; and an organic thin-film photoelectric conversion device having a photoelectric conversion layer which containing the organic photoelectric conversion material: wherein D represents an electron-donating aromatic substituent whose bonding site atom is a sp2 carbon atom; and a plurality of D may be the same or different from each other.Type: ApplicationFiled: September 7, 2012Publication date: January 3, 2013Applicant: FUJIFILM CORPORATIONInventor: Tetsu KITAMURA
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Patent number: 8343970Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: GrantFiled: March 10, 2011Date of Patent: January 1, 2013Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Publication number: 20120282223Abstract: The invention relates to a stable amorphous form of (5-Fluoro-2-methyl-3-quinolin-2-ylmethyl-indol-1-yl)-acetic acid and its use in the treatment of conditions mediated by the action of PGD2 at the CRTH2 receptor.Type: ApplicationFiled: March 7, 2012Publication date: November 8, 2012Inventors: Aimesther BETANCOURT, Marc LEMIEUX, Roch THIBERT
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Patent number: 8299250Abstract: The invention relates to a compound of the formula (I) or the formula (II) in which: W is an oxygen atom or a radical of the formula NH; X is hydrogen or an alkaline cation or a C1-C8 alkyl or a —(CH2)n3—C(R4)(R5)(R6) radical; X and R on the one hand and X and R1 on the other hand may independently form an optionally substituted cycle with 5, 6 or 7 links. The invention also relates to complexes of said compounds with at least one metal selected from the group comprising copper, palladium, ruthenium, iridium and rhodium, and to a method for the synthesis of these compounds. These compounds and complexes can be used in various asymmetrical catalysis methods.Type: GrantFiled: October 17, 2008Date of Patent: October 30, 2012Assignees: Ecole Nationale Supérieure de Chimie de Rennes, CNRS (Centre National de la Recherche Scientifique)Inventors: Marc Mauduit, Diane Rix, Christophe Crevisy, Joanna Wencel
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Publication number: 20120264730Abstract: The present invention relates to novel substituted bicyclic methyl azetidine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: ApplicationFiled: April 9, 2012Publication date: October 18, 2012Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
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Publication number: 20120259121Abstract: The present invention relates to an improved process for the preparation of Montelukast and pharmaceutical acceptable salts or derivatives thereof, in particular to a process for large scale production of Montelukast and salts thereof in high yield and high purity and pharmaceutical preparations containing said compounds.Type: ApplicationFiled: December 23, 2009Publication date: October 11, 2012Applicant: PHARMATHEN S.A.Inventors: Theoharis V. Koftis, Ravikant R. Soni
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Publication number: 20120253040Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.Type: ApplicationFiled: December 14, 2010Publication date: October 4, 2012Applicant: Shionogi & Co., Ltd.Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
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Publication number: 20120252836Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Phillippe Meyer, Peteris Alberts, Mainkar Prathama
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Patent number: 8268803Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: December 17, 2007Date of Patent: September 18, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
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Publication number: 20120177749Abstract: A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.Type: ApplicationFiled: November 30, 2011Publication date: July 12, 2012Applicants: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC., ADVANCED CANCER THERAPEUTICS, LLCInventors: Gilles Tapolsky, Pooran Chand, John O. Trent, Sucheta Telang, Brian F. Clem, Jason A. Chesney
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Publication number: 20120178717Abstract: The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases.Type: ApplicationFiled: November 18, 2011Publication date: July 12, 2012Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Patent number: 8217029Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: GrantFiled: April 11, 2008Date of Patent: July 10, 2012Assignee: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8217174Abstract: The present invention relates to a method for preparing montelukast, an inhibitor against leukotrienes, and an intermediate used therein. According to the inventive method, high-purity montelukast or its sodium salt can be prepared in a high yield.Type: GrantFiled: December 11, 2007Date of Patent: July 10, 2012Assignee: Hanmi Holdings Co., Ltd.Inventors: Gwan Sun Lee, Young-Kil Chang, Jaeheon Lee, Chul Hyun Park, Eun-Ju Park, Jaeho Yoo
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Publication number: 20120165535Abstract: A synthesis method for preparing Montelukast sodium intermediate 2-(2-(3-(2-(7-chloro-2-quinolyl)vinyl)phenyl-3-oxopropyl)phenyl) propanol is provided. In this method, the target compound is prepared by condensing the starting materials 7-chloroquinaldine and 3-cyanobenzaldehyde, and then reacting the resultant product with 2-(2-ortho-(2-haloethyl)-phenylpropyl)tetrahydropyrane ether. The present invention can easily obtain start materials and is applicable for mass production.Type: ApplicationFiled: August 24, 2010Publication date: June 28, 2012Applicant: SHANDONG NEW TIME PHARMACEUTICAL CO. LTD.Inventors: Zhiquan Zhao, Haixin Wang, Zengxue Wang
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Patent number: 8207194Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is benzene or an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: GrantFiled: March 10, 2009Date of Patent: June 26, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
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Publication number: 20120142931Abstract: This invention concerns generally with a process for purifying crude pharmaceutical compositions, wherein the crude pharmaceutical composition comprises a sodium salt of Montelukast and more particularly relates to a process for the production of pharmaceutically pure preparations of Montelukast sodium using simulated moving bed technology, without requiring an intermediate acid formation step to separate isomers and to remove impurities.Type: ApplicationFiled: December 6, 2010Publication date: June 7, 2012Applicant: Arch Pharmalabs LimitedInventors: Arun Kanti Mandal, Kamlesh Jayantilal Ranbhan, Ganesh Gurpur Pai, Abhilesh Agarwal, Rakesh Vikraman Nair Rema, Asha Oroskar
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Patent number: 8188285Abstract: It comprises a process for the purification of Montelukast, or its salts or its solvates, including any stereoisomer or mixture thereof, which comprises converting Montelukast acid or a solvate thereof, including any stereoisomer or mixtures thereof, into an amine salt selected from the group consisting of tris-(hydroxymethyl)aminomethane, L-(+)-treo-2-amino-1-phenyl-1,3-propanediol, and L-(+)-?-phenylglycinol salt, in the presence of an appropriate solvent. It also comprises novel salts of Montelukast, in particular, tris-(hydroxymethyl)aminomethane, L-(+)-treo-2-amino-1-phenyl-1,3-propanediol, and L-(+)-?-phenylglycinol salts.Type: GrantFiled: August 7, 2007Date of Patent: May 29, 2012Assignee: Esteve Quimica, S.A.Inventors: Yolanda Gasanz Guillén, Pedro Talavera Escasany, Montserrat Monsalvatje Llagostera
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Patent number: 8178680Abstract: An improved process for the preparation of Montelukast and its pharmaceutically acceptable salts comprises of reacting (S) Benzenepropanol ?-[3-[2-(7-chloro2-quinolinyl)ethenyl]phenyl]-2-(1-hydroxy-1-methyl ethyl)-?-methane sulfonate compound of formula (II) with 1-(mercapto methyl)cyclo propane acetic acid or its ester or nitrile in presence of alkali or alkaline carbonates and/or alkali or alkaline earth metal alkoxide in a suitable polar aprotic solvent with or without combination of C1-C4 alcoholic solvents and then treating with organic amine in a suitable ester and/or acetone and/or aliphatic or aromatic hydrocarbon solvents, and converting the corresponding amine salt compound of montelukast into its sodium salt compound of formula (I) using sodium ion source in methanol, without converting into montelukast free acid.Type: GrantFiled: March 10, 2006Date of Patent: May 15, 2012Assignee: MSN Laboratories LimitedInventors: Manne Satyanarayana Reddy, Muppa Kishore Kumar, Srinivasan Thirumalai Rajan, Karamala Ramasubba Reddy
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Patent number: 8163924Abstract: Dicyclohexylamine salt of formula (IIa) or a pharmaceutically acceptable solvate thereof, including a hydrate, and its process for preparation are provided. The invention also relates to processes for the preparation of montelukast of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, including a hydrate, based on the conversion of a salt of formula (IIa) into its form of free acid, followed by reaction with a compound of formula (III) CH3MgX, wherein X is halogen, in a suitable solvent, optionally in the presence of a Lewis acid.Type: GrantFiled: July 30, 2008Date of Patent: April 24, 2012Assignee: Moehs Ibérica, S.L.Inventors: Carles Sánchez Casals, Helena Camps Ramírez De Cartagena
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Publication number: 20120071502Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).Type: ApplicationFiled: September 13, 2011Publication date: March 22, 2012Applicant: CELL VIABLE CORPORATIONInventors: Iraj Lalezari, Jill Fabricant
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Publication number: 20120065188Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.Type: ApplicationFiled: November 22, 2011Publication date: March 15, 2012Inventors: Steven Joseph Brickner, Jinshan Michael Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang, Shaughnessy Robinson
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Publication number: 20120046307Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.Type: ApplicationFiled: October 16, 2009Publication date: February 23, 2012Applicant: UNIVERSITAET DES SAARLANDESInventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
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Patent number: 8115004Abstract: The present invention provides an improved process for the preparation of highly pure montelukast sodium through highly pure diol intermediate compound of formula (2) and (1)-(mercapto methyl)cyclopropane acetic acid methyl ester compound of formula (4) or mercaptomethyl cyclopropane acetic acid compound of formula (7). The present invention also provides novel organic amine salts of montelukast.Type: GrantFiled: November 19, 2007Date of Patent: February 14, 2012Assignee: MSN Laboratories LimitedInventors: Manne Satyanarayana Reddy, Muppa Kishore Kumar, Karamala Rama Subba Reddy, Durgadas Shyla Prasad
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Publication number: 20120029016Abstract: There is provided compounds of formula I, wherein ring R1a to R1c, R2a to R2e, and X 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: December 30, 2009Publication date: February 2, 2012Applicant: BIOLIPOX ABInventor: Peter Nilsson
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Patent number: 8076324Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: December 3, 2009Date of Patent: December 13, 2011Assignee: Sanofi-AventisInventors: Thomas Bohme, Uwe Gerlach, Dirk Gretzke, Heinz-Werner Kleemann, Stefania Pfeiffer-Marek, Henning Vollert, Jean-Michel Altenburger, Sergio Mallart
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Publication number: 20110301150Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.Type: ApplicationFiled: February 25, 2010Publication date: December 8, 2011Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
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Publication number: 20110281811Abstract: The invention relates to the use of at least one leukotriene inhibitor for preparing a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants. The invention further relates to a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants, the pharmaceutical composition comprising at least one leukotriene inhibitor. The invention additionally relates to a method for the treatment and/or prophylaxis of a lung disease, more particularly of a bronchopulmonary dysplasia, in a prematurely born infant, where the prematurely born infant is administered a pharmacologically active amount of at least one leukotriene inhibitor.Type: ApplicationFiled: November 12, 2009Publication date: November 17, 2011Inventor: Sabine Rupprecht
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Publication number: 20110275792Abstract: A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.Type: ApplicationFiled: July 15, 2011Publication date: November 10, 2011Inventor: Thomas Piccariello
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Publication number: 20110275627Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salt thereof, wherein X1 to X4, R1 to R4, A, B, D and m are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: August 25, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Todd Bosanac, Stephane De Lombaert, Ho Yin Lo, Peter Allen Nemoto, Alan Olague
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Publication number: 20110265878Abstract: The present invention relates to a dye comprising a chromophore to which an acyloin group as anchoring group is attached, to a method of synthesis of such dye, to an electronic device comprising such dye and to the use of such dye.Type: ApplicationFiled: September 23, 2009Publication date: November 3, 2011Applicant: Sony CorporationInventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Markus Obermaier
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Publication number: 20110237798Abstract: A method is provided for the preparation of an aromatic carboxylic acid aryl ester or an N-aryl aromatic carboxamide. The method comprises contacting an O,O-diaryl thiocarbonate or an O-aryl-N-aryl thiocarbamate with a reactant that regioselectively reacts with sulfur, which contact causes an O-neophyl rearrangement, thereby forming either the aromatic carboxylic acid aryl ester or the N-aryl aromatic carboxamide, respectively.Type: ApplicationFiled: March 22, 2011Publication date: September 29, 2011Applicant: The Florida State University Research Foundation, Inc.Inventors: Igor Alabugin, Abdulkader Baroudi
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Publication number: 20110230488Abstract: The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.Type: ApplicationFiled: November 25, 2009Publication date: September 22, 2011Applicant: TRT PHARMA INC.Inventors: Jian Hui Wu, Gerald Batist, Jinming Zhou, Guoyan Geng, Rongtuan Lin
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Publication number: 20110224202Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Applicant: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Publication number: 20110224207Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.Type: ApplicationFiled: September 23, 2009Publication date: September 15, 2011Applicant: GEORGETOWN UNIVERSITYInventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
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Publication number: 20110189127Abstract: The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: June 10, 2009Publication date: August 4, 2011Inventors: Srikanth Venkatraman, Anilkumar Gopinadhan Nair, Kevin X. Chen, Francisco Valazquez, Qingbei Zeng, Duan Liu, Yueheng Jiang, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Stephen J. Gavalas, Patrick A. Pinto, Oleg B. Selyutin, Bancha Vibulbhan
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Patent number: 7989472Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: March 19, 2007Date of Patent: August 2, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Ashley Rouse Lins, Jiang Chang, Cangming Yang
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Publication number: 20110183976Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 25, 2009Publication date: July 28, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110166356Abstract: Disclosed is a method for preparing a montelukast sodium salt of Formula 1. The method includes coupling a methanesulfonyl compound of Formula 2 below with a compound of Formula 3 below in the presence of a bistrimethylsilylamide alkali metal salt, further adding an alkali metal base thereto and hydrolyzing the mixture by heating to prepare a compound of Formula 4 below, reacting the compound of Formula 4 with 4-tert-butylcyclohexylamine, followed by purification, to prepare an amine salt of Formula 5, and converting the amine salt of Formula 5 into a sodium salt.Type: ApplicationFiled: September 25, 2009Publication date: July 7, 2011Applicant: LG Life Sciences, LtdInventors: In Sang Lee, Seok Ju Lee, Jae Eun Kang
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Publication number: 20110152315Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type I1 diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.Type: ApplicationFiled: July 23, 2009Publication date: June 23, 2011Inventors: Trond Ulven, Elisabeth Christiansen
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Patent number: 7964729Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: August 28, 2006Date of Patent: June 21, 2011Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
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Publication number: 20110137039Abstract: The present invention relates to an improved process for the preparation of 1-[[[(IR)-I-[3[(IE)-2-(7chloro-2-quino-linyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid and its salts using Methyl 2-[(3S)-[3-[(2E)-(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoate.Type: ApplicationFiled: November 24, 2010Publication date: June 9, 2011Inventors: CHAVA SATYANARAYANA, GORANTLA SEETA RAMANJANEYULU, INDUKURI VENKATA SUNIL KUMAR, SIMHADRI SRINIVAS, JAMMULA VEERA VENKATA KRISHNA KISHORE