Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
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Publication number: 20120041009Abstract: A pyrimidine compound represented by below formula (I) has excellent control activity against pests and is useful as an active ingredient of a pest controlling agent.Type: ApplicationFiled: March 11, 2010Publication date: February 16, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Hajime Mizuno
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Publication number: 20120040950Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: December 21, 2010Publication date: February 16, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, JR., Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Suganthini S. Nanthakumar, Jingrong Cao, Upul Keerthi Bandarage, Anne-Laure Grillot
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Patent number: 8114994Abstract: Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.Type: GrantFiled: February 10, 2009Date of Patent: February 14, 2012Assignee: Emory UniversityInventors: Dennis C. Liotta, Shuli Mao, Michael Hager, Raymond F Schinazi
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Publication number: 20120035181Abstract: A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.Type: ApplicationFiled: April 26, 2010Publication date: February 9, 2012Applicant: NIPPON SUISAN KAISHA, LTD.Inventors: Fumi Kawano, Noritaka Hirazawa
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Publication number: 20120035196Abstract: [Problem] The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes. [Means for Solution] The present inventors have extensively studied a compound having a GPR40 agonistic activity, and as a result, they have found that the compound (I) of the present invention or a pharmaceutically acceptable salt thereof, in which a carboxylic acid is bonded to a bicyclic or tricyclic moiety through methylene, and further, a benzene ring substituted with a monocyclic 6-membered aromatic ring is bonded to a bicyclic or tricyclic moiety through —O-methylene or —NH-methylene, has an excellent GPR40 agonistic activity. They have also found that the compound has an excellent insulin secretion promoting action and strongly inhibits increase in the blood glucose after glucose loading, thereby completing the present invention.Type: ApplicationFiled: April 21, 2010Publication date: February 9, 2012Inventors: Kenji Negoro, Kei Ohnuki, Yasuhiro Yonetoku, Kazuyuki Kuramoto, Yasuharu Urano, Hideyuki Watanabe
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Publication number: 20120035157Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AstraZeneca ABInventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
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Publication number: 20120035171Abstract: The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: April 15, 2010Publication date: February 9, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gordon Saxty, Valerio Berdini, Eddy Jean Edgard Freyne, Alexandra Papanikos, Pascal Benderitter, Werner Constant Johan Embrechts, Berthold Wroblowski, Rhalid Akkari
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Publication number: 20120034216Abstract: The present invention relates to spiroketal compounds that are useful in methods of treating or preventing protozoal infections, parasitic infections, bacterial infections, cell proliferative disorders and anti inflammatory disorders. The spiroketal compounds are also useful as immunosuppressive agents, and also in methods of controlling pests.Type: ApplicationFiled: August 11, 2011Publication date: February 9, 2012Applicant: ECOBIOTICS LTDInventors: Paul Warren Reddell, Victoria Anne Gordon
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Publication number: 20120028997Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.Type: ApplicationFiled: December 16, 2010Publication date: February 2, 2012Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara Miskowski, Janet L. Ralbovsky, Mark Schulz
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Publication number: 20120029000Abstract: The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).Type: ApplicationFiled: March 25, 2010Publication date: February 2, 2012Applicant: MAPI PHARMA LIMITEDInventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
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Publication number: 20120027857Abstract: This invention relates to sustained release pharmaceutical compositions comprising O-desmethyl-venlafaxine, in particular to sustained pharmaceutical compositions comprising O-desmethyl-venlafaxine orotate and/or O-desmethyl-venlafaxine glucuronate.Type: ApplicationFiled: November 26, 2009Publication date: February 2, 2012Applicant: LEK PHARMACEUTICALS D.D.Inventors: Zrinka Abramovic, Zdenka Jerala-Strukelj, Igor Legen, Uros Klancar
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Patent number: 8106064Abstract: The invention is related to pyrimidine-2,4-dione HIV reverse transcriptase inhibitors of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: July 24, 2007Date of Patent: January 31, 2012Assignee: Korea Research Institute of Chemical TechnologyInventors: Hongyan Guo, Choung U. Kim, Thorsten A. Kirschberg, Ill Young Lee, Michael L. Mitchell, Jong Chan Son, Lianhong Xu
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Publication number: 20120021036Abstract: The invention provides nanostructures or products of manufacture for use as ex vivo or in vivo composition (e.g., a drug, or a therapeutic, diagnostic or imaging reagent) delivery vehicles. In one aspect, the invention provides nanoparticles comprising several compartments which in unison function as a composite nanostructure. In one embodiment, the nanoparticles of the invention comprise a combination of polymer core/lipid bilayer interface which incorporate covalently attached lipid-vascular targeting ligands. These composite nanoparticles can deliver highly effective and selective payloads for diagnostic, prophylactic or therapeutic applications.Type: ApplicationFiled: January 14, 2010Publication date: January 26, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Bharat Majeti, Eric Murphy, Wolfgang Wrasidlo, David Cheresh
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Publication number: 20120022074Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: ApplicationFiled: October 4, 2011Publication date: January 26, 2012Inventors: Dominik FEUERBACH, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
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Publication number: 20120020915Abstract: Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.Type: ApplicationFiled: January 13, 2011Publication date: January 26, 2012Applicants: QUEENS UNIVERSITY AT KINGSTON, THE SIR MORTIMER B. DAVIS JEWISH GENERAL HOSPITAL, OSTA BIOTECHNOLOGIES, INC.Inventors: Ajay Gupta, Hyman M. Schipper, Moulay Alaoui-Jamali, Walter A. Szarek, Kanji Nakatsu, Jason Z. Vlahakis
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Publication number: 20120022087Abstract: The invention relates to amorphous ambrisentan, preferably together with a surface stabiliser in the form of a stable intermediate. The invention further relates to methods of producing stable amorphous ambrisentan and pharmaceutical formulations containing stable amorphous ambrisentan.Type: ApplicationFiled: August 7, 2009Publication date: January 26, 2012Applicant: Ratiopharm GmbHInventors: Kathrin Rimkus, Frank Muskulus, Sandra Brueck, Jana Paetz
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Publication number: 20120022089Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.Type: ApplicationFiled: September 22, 2011Publication date: January 26, 2012Applicant: ABBOTT LABORATORIESInventors: Jöerg Rosenberg, Ulrich Reinhold, Bernd Liepold, Gunther Berndl, Jörg Breitenbach, Laman L. Alani, Soumojeet Ghosh
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Publication number: 20120020877Abstract: An intrauterine device and more specifically an intracervical device (ICD) for the local release of drugs in the loco-regional treatment of tumours of the uterine cervix comprises an elongated stem (2) to be positioned in the cervical canal (15), this stem consisting of an inner hollow core (3) and a coating (4) containing a gradual-release drug, the stem being attached to: a first element (5) for blocking the stem (2) inside the uterine cavity (12), and located at the cranial or upper end; a second blocking element (7, 71) positioned inside the vagina (11), against the ectocervix (16), located at the caudal or lower end of the stem (2).Type: ApplicationFiled: January 29, 2009Publication date: January 26, 2012Applicant: Fondazione IRCSSInventor: Francesco Raspagliesi
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Publication number: 20120022088Abstract: New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I wherein R is a lower alkyl group, which is methyl or ethyl R1 and R2 is sodium carboxylate-methyl ester, having synergistic cytotoxic effect combined with 5-fluorouracil.Type: ApplicationFiled: March 11, 2010Publication date: January 26, 2012Applicant: JSC GRINDEKSInventors: Gunars Duburs, Egils Bisenieks, Irina Sestakova, Ivars Kalvinsh, Brigita Vigante, Janis Uldrikis, Ilona Domraceva, Elina Jascenko, Janis Poikans, Imanta Bruvere, Ilmars Stonans
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Publication number: 20120022065Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: September 30, 2011Publication date: January 26, 2012Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Patent number: 8101615Abstract: The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: February 15, 2005Date of Patent: January 24, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Barbara Albrecht, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Patent number: 8101625Abstract: A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1 and R2 are defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.Type: GrantFiled: October 23, 2006Date of Patent: January 24, 2012Assignee: Exelixis, Inc.Inventors: Kenneth D. Rice, Neel Kumar Anand, Arlyn Arcalas, Charles M. Blazey, Joerg Bussenius, Wai Ki Vicky Chan, Hongwang Du, Sergey Epshteyn, Mohamed Abdulkader Ibrahim, Patrick Kearney, Abigail R. Kennedy, Moon Hwan Kim, Jean-Claire Limun Manalo, Csaba J. Peto, Tsze H. Tsang, Amy Lew Tsuhako, Peiwen Zhou, Elena S. Koltun
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Patent number: 8101626Abstract: The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.Type: GrantFiled: April 1, 2010Date of Patent: January 24, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Zhi-Liang Chu, James N. Leonard, Juerg Lehmann, Robert M. Jones
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Publication number: 20120014917Abstract: The invention relates to methods of treating patients infected with human immunodeficiency virus (HIV) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Applicants: University of Minnesota, INTERMUNE, INC.Inventors: Karl Kossen, Timothy Schacker, Ashley T. Haase
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Publication number: 20120015966Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Inventors: Jack Lin, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
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Publication number: 20120016467Abstract: Disclosed is a sustained release system that includes a polymer and a prodrug having a solubility less than about 1 mg/ml dispersed in the polymer. Advantageously, the polymer is permeable to the prodrug and may be non-release rate limiting with respect to the rate of release of the prodrug from the polymer. This permits improved drug delivery within a body in the vicinity of a surgery via sustained release rate kinetics over a prolonged period of time, while not requiring complicated manufacturing processes.Type: ApplicationFiled: July 19, 2011Publication date: January 19, 2012Applicant: pSivida Inc.Inventors: Jianbing Chen, Paul Ashton, Thomas J. Smith
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Publication number: 20120014913Abstract: This disclosure is directed to: (a) processes for preparing a compound and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compound and salts; (c) pharmaceutical compositions comprising the compound or salts; and (d) methods of use of such compositions.Type: ApplicationFiled: July 15, 2011Publication date: January 19, 2012Applicant: ABBOTT LABORATORIESInventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
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Publication number: 20120009240Abstract: The present disclosure relates to self-supporting films for delivery of a therapeutic agent containing at least one hydrophobic polymer and at least one therapeutic agent. Methods of forming the multilayer films are also disclosed.Type: ApplicationFiled: June 30, 2011Publication date: January 12, 2012Inventors: Joshua Stopek, Daniel Broom, Amin Elachchabi, Garrett Ebersole
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Publication number: 20120010165Abstract: To provide a radiation therapy potentiator, which, when employed in combination with cancer radiation therapy, can reduce radiation dose and can mitigate adverse effects. The invention provides a radiation therapy potentiator containing, as an effective ingredient, a uracil derivative represented by formula (1) (wherein R1 represents a halogen atom or a cyano group; and R2 represents a 4- to 8-membered heterocyclic group having 1 to 3 nitrogen atoms and optionally having as a substituent a lower alkyl group, an imino group, a hydroxyl group, a hydroxymethyl group, a methanesulfonyloxy group, or an amino group; an amidinothio group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group; a guanidino group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group or a cyano group; a lower alkylamidino group; or a 1-pyrrolidinylmethyl group) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 12, 2012Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventor: Masakazu FUKUSHIMA
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Publication number: 20120010161Abstract: The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.Type: ApplicationFiled: January 25, 2010Publication date: January 12, 2012Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE CLAUDE BERNARD LYON IInventor: Joelle Paris
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Publication number: 20120009243Abstract: The present invention provides liposomes that are useful for delivery of bioactive agents such as therapeutics. Among others, the liposomes of the invention are capable of delivering their payload at sites of increased secretory phospholipase A2 (sPLA2) activity, because phospholipase A2 (PLA2) will hydrolyse lipids of the liposome. Thus, the liposomes of the invention may e.g. be used in relation to cancer therapy. Another aspect of the invention is a liposomal formulation comprising the liposome of the invention. Still another aspect is a method of producing a liposomal formulation of the invention.Type: ApplicationFiled: May 25, 2009Publication date: January 12, 2012Applicant: LIPLASOME PHARMA APSInventors: Anders Falk Vikbjerg, Sune Allan Petersen, Fredrik Melander, Jonas Rosager Henriksen, Kent Jørgensen
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Publication number: 20120010192Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 30, 2011Publication date: January 12, 2012Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Publication number: 20120010227Abstract: The invention relates to a pharmaceutical composition with a content in active ingredient that can be an antimycotic, so that the composition is suitable for the treatment of onychomycoses, in particular severe onychomycoses. The inventive formulation is an ointment-like thermogel at body temperature and an inviscid thermogel at lower temperatures and facilitates the permeation of sufficient active ingredient quantities through human fingernails and toenails, in order to also treat severe onychomycoses.Type: ApplicationFiled: July 29, 2010Publication date: January 12, 2012Applicant: Technische Universitat BraunschweigInventors: Lusiana, Christel Müller-Goymann
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Patent number: 8093245Abstract: 4-Amino-1H-pyrimidin-2-one-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of various diseases and disorders are disclosed.Type: GrantFiled: December 12, 2007Date of Patent: January 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Alexander Heim-Riether, Theodore C. Jessop, James E. Tarver, Jerry A. Taylor
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Patent number: 8093246Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.Type: GrantFiled: December 12, 2007Date of Patent: January 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Theodore C. Jessop, Philip E. Keyes, Min Shen, James E. Tarver, Jerry A. Taylor, Xiaolian Xu
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Publication number: 20120003321Abstract: The present invention relates to crosslinked dextran magnetic composite microparticles and a preparation process and a using method thereof. The composite microparticles comprise magnetic nanoparticles and dextran with crosslinked structure, wherein the magnetic nanoparticles are dispersed in the dextran with crosslinked structure. The process for preparing the composite microparticles comprises: preparing a dextran solution; synthesizing dextran magnetic composite microparticles; and synthesizing the crosslinked dextran magnetic composite microparticles. The using method of composite microparticles comprises: preparing crosslinked dextran magnetic composite microparticles loaded with anti-cancer drug; and adding a sustained-releasing solution thereto.Type: ApplicationFiled: December 29, 2008Publication date: January 5, 2012Applicant: XI'AN GOLDMAG NANOBIOTECH CO. LTD.Inventors: Mingli Peng, Yanhong Liu, Yali Cui, Chao Chen, Ke Li
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Publication number: 20120004252Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: ApplicationFiled: December 16, 2010Publication date: January 5, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Kai Gerlach, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Marco Santagostino, Stefan Scheuerer, Christofer Tautermann, Thomas Trieselmann
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Patent number: 8088783Abstract: Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(pyrimidinylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provided for use as inhibitors of with MEK kinase.Type: GrantFiled: April 7, 2011Date of Patent: January 3, 2012Inventors: Qing Dong, Stephen W. Kaldor
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Publication number: 20110319439Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.Type: ApplicationFiled: March 9, 2010Publication date: December 29, 2011Inventor: Saleem Ahmad
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Publication number: 20110319354Abstract: The invention relates to combination anticancer therapy with certain Akt inhibitor and other anticancer agents such as anticancer antimetabolites, anticancer antibiotics, plant-derived anticancer agents, anticancer platinum-coordinated complex compounds, anticancer camptothecin derivatives and anticancer tyrosine kinase inhibitors.Type: ApplicationFiled: February 23, 2010Publication date: December 29, 2011Inventors: Mark E. Layton, Hiroshi Hirai, Hidehito Kotani
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Publication number: 20110319418Abstract: Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, L2, and Q are defined herein.Type: ApplicationFiled: June 27, 2011Publication date: December 29, 2011Inventors: Christopher M. Flores, Paul R. Wade
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Publication number: 20110319438Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: September 7, 2011Publication date: December 29, 2011Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
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Publication number: 20110319437Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: August 31, 2011Publication date: December 29, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Shigeyuki ITOH, Atsushi IWATA
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Publication number: 20110319400Abstract: Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.Type: ApplicationFiled: June 27, 2011Publication date: December 29, 2011Inventors: Christopher M. Flores, Paul R. Wade
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Publication number: 20110319333Abstract: The present application relates to methods of treating HIV-associated nephropathy (HIVAN) and/or focal segmental glomerulosclerosis (FSGS) using endothelin-1 (ET-1) antagonists. The application further relates to a composition for the treatment of HIVAN and/or FSGS. A kit for detecting the presence of ET-1 or ET-1-associated biomarker in a biological sample is also disclosed.Type: ApplicationFiled: June 16, 2011Publication date: December 29, 2011Applicant: MOREHOUSE SCHOOL OF MEDICINEInventors: Gale W. NEWMAN, Barbara A. JACOB-MUNGIN, Chamberlain OBIALO
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Patent number: 8084605Abstract: Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula: wherein the Compound I is present in one or more polymorphic forms. Also provided are novel methods for the preparation of the polymorphs of Compound I, and kits and articles of manufacture of the compositions, and methods of using the compositions to treat various diseases.Type: GrantFiled: November 29, 2007Date of Patent: December 27, 2011Inventors: Ron C. Kelly, Lien H. Koztecki
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Patent number: 8084458Abstract: Methods are described for the synthesis of Locked Nucleic Acid (LNA) derivatives using certain nitrogen-containing nucleophiles.Type: GrantFiled: August 3, 2009Date of Patent: December 27, 2011Assignee: Santaris Pharma A/SInventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Publication number: 20110312974Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Nicholas Simone Stock, Yen Pham Truong, Jeffrey Roger Roppe, Deborah Volkots, Jill Melissa Scott, Timothy Andrew Parr, Bowei Wang, Thomas Jon Seiders, Ryan Clark, Heather Renee Coate
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Publication number: 20110312983Abstract: The present application describes deuterium-enriched alogliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: December 9, 2010Publication date: December 22, 2011Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Publication number: 20110311648Abstract: Compositions and methods for the treatment of malignancy and chronic viral infection are disclosed.Type: ApplicationFiled: July 20, 2011Publication date: December 22, 2011Inventors: George C. Prendergast, Alexander J. Muller, James B. DuHadaway, William Malachowski