Unsaturated Hetero Ring Attached Directly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/167)
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Patent number: 8377962Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: GrantFiled: April 7, 2010Date of Patent: February 19, 2013Assignee: Idenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Michel Derock, Frederic Leroy, Jean-Christophe Meillon, Thierry Convard, Dominique Surleraux
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Publication number: 20130040907Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 4, 2012Publication date: February 14, 2013Applicant: Ardea Biosciences Inc.Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
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Publication number: 20130029845Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: July 30, 2012Publication date: January 31, 2013Applicant: E.I. du Pont de Nemours and CompanyInventors: George Philip LAHM, Wesley Lawrence SHOOP, Ming XU
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Publication number: 20130023635Abstract: A catalyst system useful for polymerizing olefins is disclosed. The catalyst system comprises an activator and a Group 4 metal complex. The complex incorporates a dianionic, tridentate heterocyclic-8-anilinoquinoline ligand. In one aspect, a supported catalyst system is prepared by first combining a boron compound having Lewis acidity with excess alumoxane to produce an activator mixture, followed by combining the activator mixture with a support and the dianionic, tridentate Group 4 metal complex. The Group 4 metal complexes are easy to synthesize, support, and activate, and they enable facile production of high-molecular-weight polyolefins.Type: ApplicationFiled: July 18, 2011Publication date: January 24, 2013Inventors: Ilya E. NIFANT'EV, Sander Nagy, Vladimir V. Bagrov, Pavel V. Ivchenko, Shahram Mihan
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Publication number: 20130018052Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.Type: ApplicationFiled: July 13, 2012Publication date: January 17, 2013Applicant: SK CHEMICALS CO., LTD.Inventors: Ju Young LEE, Keun-Ho RYU, Jae-Sun KIM, Yong-Hyuk KIM, Dong Chul SHIN, Bong-yong LEE, Sang-hwan KANG, Hyun-Jung LEE, Hoechul JUNG, Young Ah SHIN, Euisun PARK, Jaeseung AHN
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Patent number: 8354429Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.Type: GrantFiled: September 11, 2008Date of Patent: January 15, 2013Assignee: Gilead Sciences, Inc.Inventors: Youla S. Tsantrizos, Murray D. Bailey, Francois Bilodeau, Rebekah J. Carson, Rene Coulombe, Lee Fader, Teddy Halmos, Stephen Kawai, Serge Landry, Steven LaPlante, Sebastien Morin, Mathieu Parisien, Marc-Andre Poupart, Bruno Simoneau
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Publication number: 20130012521Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: Gilead Sciences, Inc.Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
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Publication number: 20130005976Abstract: A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R,2S)-(?)-ephedrine, thus preparing the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of (V), and (b) precipitating selectively the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of (1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of [(1S,2S)-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution; (c) liberating the acid II by removal of brucine or (1R,2S)-(?)-ephedrine from the precipitated salt obtained in step (b).Type: ApplicationFiled: March 16, 2011Publication date: January 3, 2013Applicant: JANSSEN PHARMACEUTICALS, INC.Inventors: Dominic John Ormerod, Dominique Paul Michel Depre, Andras Horvath
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Publication number: 20130005721Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.Type: ApplicationFiled: September 23, 2010Publication date: January 3, 2013Applicant: PANMIRA PHARMACEUTICALS, LLCInventors: Brian Andrew Stearns, Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
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Publication number: 20120316200Abstract: The present invention is directed to novel phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be useful in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases.Type: ApplicationFiled: April 7, 2011Publication date: December 13, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Linus S. Lin, Richard Soll, Jingchao Dong, Hao Wu, Takao Suzuki, Bin Hu, Dejun Liu, Jinglai Hao, Ming Xu
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Patent number: 8329899Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: February 14, 2011Date of Patent: December 11, 2012Assignee: Synta Pharmaceuticals, Corp.Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
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Patent number: 8329723Abstract: Provided herein are 1-aryl or 1-heteroaryl pyrido[b]indoles compounds with the structure These compounds comprise a ?-carboline ring structure substituted at C1 with an aryl or heteroaryl moiety and individually substituted at C3-C8 and N9 with a C1-C4 alkyl, a C1-C4 alkoxy, a C1-C4 alkoxyphenyl, or a hydrogen. Also provided are methods for inhibiting proliferation of cancer cells or for treating a cell proliferative disease by contacting the cancer cell or tumor comprising the same with the compounds provided herein or by administering the compounds to a subject with a cell proliferative disease.Type: GrantFiled: April 26, 2010Date of Patent: December 11, 2012Inventors: John K Buolamwini, Shrivaputra Patil, Sharma Horrick, James K Addo
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Patent number: 8329705Abstract: The present invention relates to substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: December 11, 2012Assignee: ArQule, Inc.Inventor: Neil Westlund
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Publication number: 20120287524Abstract: Disclosed are a novel compound, a pigment dispersion composition including the same, a photosensitive resin composition including the same, and a color filter using the same.Type: ApplicationFiled: June 22, 2010Publication date: November 15, 2012Applicant: CHEIL INDUSTRIES INC.Inventors: Seong-Yong Uhm, Seong-Ryong Nam, Taek-Jin Baek, Tae-Gyu Chun, Kyung-Hee Hyung
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Publication number: 20120289483Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.Type: ApplicationFiled: July 26, 2012Publication date: November 15, 2012Applicant: SYNTA PHARMACEUTICALS CORPORATIONInventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
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Patent number: 8308996Abstract: A photochromic chromene compound which develops a color of a neutral tint, has high color optical density, a high fading speed and high durability, and has an indeno(2,1-f)naphtho(1,2-b)pyran structure represented by the following formula as the basic skeleton, wherein a sulfur-containing substituent selected from thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group and heteroarylthio group is bonded to the 6-position and/or 7-position carbon atom(s).Type: GrantFiled: August 4, 2010Date of Patent: November 13, 2012Assignee: Tokuyama CorporationInventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi
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Patent number: 8308995Abstract: A chromene compound represented by the following formula (1): wherein R1, R2, R3, R4, R5, R6, m, and n are defined in the specification. The chromene compound is rarely deteriorated by exposure.Type: GrantFiled: February 9, 2012Date of Patent: November 13, 2012Assignee: Tokuyama CorporationInventors: Soko Kasai, Shinobu Izumi
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Patent number: 8309734Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: October 19, 2009Date of Patent: November 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Henrietta Dehmlow, Rainer E. Martin, Ulrike Obst Sander, Hans Richter, Christoph Ullmer
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Publication number: 20120283259Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: July 12, 2012Publication date: November 8, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20120258948Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of formula I, wherein the variables G, T, D, L, R1, R2, R3 are as described herein, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections in a patient in need thereof.Type: ApplicationFiled: December 6, 2010Publication date: October 11, 2012Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20120247561Abstract: Disclosed is a 4,4?-dicarboxy-2,2?-bipyridine derived tridentate ligand represented by formula (I): wherein definitions of Y1, Y2, and R are the same as those defined in the specification. Also disclosed are a metal complex containing the aforesaid tridentate ligand and a dye-sensitized solar cell containing the metal complex.Type: ApplicationFiled: November 29, 2011Publication date: October 4, 2012Inventors: Yun CHI, Cheng-Xuan Li, Shen-Han Yang, Hsin-Pei Wu, Kuan-Lin Wu, Chien-Wei Hsu, Shih-Han Chang
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Publication number: 20120238517Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: December 1, 2010Publication date: September 20, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
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Patent number: 8269019Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: GrantFiled: March 10, 2011Date of Patent: September 18, 2012Assignee: Probiodrug AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20120232265Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described 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. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: November 7, 2011Publication date: September 13, 2012Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Patent number: 8263775Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.Type: GrantFiled: November 18, 2008Date of Patent: September 11, 2012Assignees: Howard Florey Institute, St. Vincent's Institute of Medical ResearchInventors: Siew Yeen Chai, Michael William Parker, Anthony Lloyd Albiston, Frederick A. O. Mendelsohn, Keith Geoffrey Watson
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Patent number: 8263774Abstract: A quinoline-oxazoline compound having the formula: where one of X1 and X2 is N and the other is C and one of R1, R2 and R3 is Z wherein Z is an oxazoline radical having the formula such that when X1 is N R2 is Z and R1 is absent, and when X2 is N either R1 or R3 is Z and R2 is absent. R1 and R3 through R12 are independently H or a pendant moiety which does not interfere with coordination of either N in the quinoline compound with a coordination center. These compounds can be complexed with a suitable coordination center such as catalytically active palladium and can be highly useful in catalytically oxidizing alkenes with high regioselectivity.Type: GrantFiled: September 3, 2009Date of Patent: September 11, 2012Assignee: University of Utah Research FoundationInventors: Matthew Scott Sigman, Brian William Michel
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Publication number: 20120220587Abstract: Compounds of the formula (I), in which X1, X2, L, Y, R2, R3, R4, R5, R6, R7, R8, R9, R10 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 6, 2010Publication date: August 30, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Ulrich Emde, Hans Peter Buchstaller, Markus Klein, Christina Esdar, Joerg Bomke
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Patent number: 8247432Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs).Type: GrantFiled: May 19, 2011Date of Patent: August 21, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Patent number: 8247437Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: June 8, 2011Date of Patent: August 21, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20120205636Abstract: A compound for an organic photoelectric device an organic photoelectric device, and a display device, the compound being represented by the following Chemical Formula 1:Type: ApplicationFiled: April 20, 2012Publication date: August 16, 2012Inventors: Young-Hoon Kim, Ja-Hyun Kim, Eun-Sun Yu, Ho-Jae Lee, Young-Sung Park, Mi-Young Chae, Hyung-Sun Kim, Soo-Hyun Min, Eui-Su Kang, Sung-Hyun Jung
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Publication number: 20120199818Abstract: It is an object of the present invention to provide a novel triazole derivative. Further, it is another object of the present invention to provide a light-emitting element having high luminous efficiency with the use of the novel triazole derivative. Moreover, it is still another object of the present invention to provide a light-emitting device and electronic devices which have low power consumption. A light-emitting element having high luminous efficiency can be manufactured with the use of a triazole derivative which is a 1,2,4-triazole derivative, in which an aryl group or a heteroaryl group is bonded to each of 3-position, 4-position, and 5-position, and in which any one of the aryl group or heteroaryl group has a 9H-carbazol-9-yl group.Type: ApplicationFiled: April 19, 2012Publication date: August 9, 2012Applicant: SEMICONDUCTOR ENERGY LABORATORY CO., LTD.Inventors: Hiroko NOMURA, Sachiko KAWAKAMI, Nobuharu OHSAWA, Satoshi SEO
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Patent number: 8231888Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: June 9, 2011Date of Patent: July 31, 2012Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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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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Publication number: 20120165534Abstract: Disclosed are methods for the preparation of bromo-substituted quinolines of the formula (I) where R is aryl, heteroaryl, alkyl, alkenyl or alkynyl, which are useful as intermediates in the preparation of agents for the treatment of hepatitis C viral (HCV) infections: Formula (I).Type: ApplicationFiled: May 3, 2010Publication date: June 28, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Nitinchandra D. Patel, Chris H. Senanayake, Wenjun Tang, Xudong Wei, Nathan K. Yee
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Publication number: 20120165321Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: March 5, 2012Publication date: June 28, 2012Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerrard Darcy, Carla A. Donatelli, Steven David Knight, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Stanley J. Schmidt
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Publication number: 20120149729Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: December 13, 2011Publication date: June 14, 2012Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
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Publication number: 20120142727Abstract: [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided. [Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.Type: ApplicationFiled: August 5, 2010Publication date: June 7, 2012Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Takuya Washio, Wataru Hamaguchi
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Publication number: 20120139410Abstract: An organic electroluminescence device includes: a cathode; an anode; and a single-layered or multilayered organic thin-film layer provided between the cathode and the anode. In the organic electroluminescence device, the organic thin-film layer includes at least one emitting layer, and the at least one emitting layer contains: at least one phosphorescent material; and a host material represented by the following formula (1).Type: ApplicationFiled: December 7, 2011Publication date: June 7, 2012Applicant: Idemitsu Kosan Co., Ltd.Inventors: Kazuki NISHIMURA, Toshihiro IWAKUMA, Kenichi FUKUOKA, Chishio HOSOKAWA, Masahiro KAWAMURA, Mitsunori ITO, Yoriyuki TAKASHIMA, Toshinari OGIWARA
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Patent number: 8193199Abstract: Substituted bicyclic heteroaryls having the structures: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid LeukemiType: GrantFiled: March 24, 2008Date of Patent: June 5, 2012Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20120129886Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: November 10, 2011Publication date: May 24, 2012Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
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Patent number: 8178687Abstract: Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R?1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1, 2 and m=0, 1; R1 and/or R?1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products beingType: GrantFiled: December 16, 2010Date of Patent: May 15, 2012Assignee: Sanofi-AventisInventors: Marcel Alasia, Hervé Minoux, Jean-Marie Ruxer
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Publication number: 20120115855Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 2, 2009Publication date: May 10, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20120104941Abstract: A compound for an organic photoelectric device, an organic photoelectric device, and a display device, the compound being represented by the following Chemical Formula 3a, 3b, or 3c:Type: ApplicationFiled: January 9, 2012Publication date: May 3, 2012Inventors: Sung-Hyun JUNG, Myeong-Soon KANG, Ho-Kuk JUNG, Nam-Soo KIM, Dong-Min KANG, Nam-Heon LEE, Mi-Young CHAE
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Publication number: 20120108567Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darryl McCONNELL, Maria IMPAGNATIELLO, Dirk KESSLER, Oliver KRAEMER, Siegfried SCHNEIDER, Lars VAN DER VEEN, Ulrike WEYER-CZERNILOFSKY, Tobias WUNBERG
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Patent number: 8163901Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: GrantFiled: January 9, 2009Date of Patent: April 24, 2012Assignee: Evotec AGInventors: Matthew Duncton, Donogh John Roger O'Mahony, Matthew Cox, Maria De Los Angeles Estiarte-Martinez
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Publication number: 20120094958Abstract: The invention relates to a compound of formula (I) wherein the substituents are as described in the specification, which are useful as farnesyl pyrophosphate synthase modulators, e.g. in the treatment of proliferative diseases, to methods of manufacturing such compounds and to intermediates thereof.Type: ApplicationFiled: February 26, 2009Publication date: April 19, 2012Applicant: NOVARTIS AGInventors: Rene Amstutz, Guido Bold, Simona Cotesta, Wolfgang Jahnke, Andreas Marzinzik, Juliane Constanze Desiree Hartwieg, Silvio Ofner, Frédérik Stauffer, Johann Zimmermann
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Publication number: 20120094832Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: August 6, 2008Publication date: April 19, 2012Applicant: SYNGENTA LIMITEDInventors: Melloney Tyte, Christopher John Mathews, Gavin John Hall, William Guy Whittingham, Jeffrey Steven Wailes, James Nicholas Scutt, Stephane André Marie Jeanmart, Russell Viner
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Patent number: 8158037Abstract: The present invention provides ophthalmic devices comprising at least one photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic materials. Other non-limiting embodiments relate to methods of making the ophthalmic devices comprising photochromic materials.Type: GrantFiled: September 1, 2010Date of Patent: April 17, 2012Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, Jr., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Patent number: 8147726Abstract: A chromene compound represented by the following formula (1): wherein R1, R2, R3, R4, R5, R6, m, and n are defined in the specification. The chromene compound is rarely deteriorated by exposure.Type: GrantFiled: May 8, 2009Date of Patent: April 3, 2012Assignee: Tokuyama CorporationInventors: Soko Kasai, Shinobu Izumi
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Patent number: 8147725Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.Type: GrantFiled: September 1, 2010Date of Patent: April 3, 2012Assignee: Transitions Optical, IncInventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank Molock, Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu