At Least Three Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 548/151)
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Patent number: 9243000Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: April 22, 2010Date of Patent: January 26, 2016Assignee: Boehringer Ingelheim International GmbHInventors: Lars Van Der Veen, Darryl McConnell, Siegfried Schneider, Matthias Grauert, Andreas Schoop, Tobias Wunberg
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Patent number: 9024037Abstract: Diphenylamine-benzobisthiazole-diphenylamine monomers having two-photon absorption cross-sections and high solubility in organic solvents are provided. Also provided are the corresponding organo-soluble, wholly conjugated and two-photon absorbing benzobisthiazole-triarylamine polymers.Type: GrantFiled: May 18, 2012Date of Patent: May 5, 2015Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Loon-Seng Tan, Ramamurthi Kannan, Matthew Dalton
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Publication number: 20150011528Abstract: Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.Type: ApplicationFiled: September 21, 2012Publication date: January 8, 2015Applicant: YUHAN CORPORATIONInventors: Youn Hur, Dong-Hyun Kim, Eun-Kyung Kim, Jin-Hwi Park, Jae-Eun Joo, Ho-Woong Kang, Se-Woong Oh, Dong-Kyun Kim, Kyoung-Kyu Ahn
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Patent number: 8921369Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: GrantFiled: December 2, 2009Date of Patent: December 30, 2014Assignee: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
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Patent number: 8901157Abstract: The present invention discloses compositions and a method of improving the pharmacokinetics of pharmaceutical agents (or pharmaceutically acceptable salts, esters, and prodrugs thereof) which are metabolized by cytochrome P450 monoxygenase comprising coadministering ritonavir or a pharmaceutically acceptable salt, ester, and prodrug thereof.Type: GrantFiled: December 2, 2010Date of Patent: December 2, 2014Assignee: AbbVie Inc.Inventors: Dale J. Kempf, Kennan C. Marsh
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Patent number: 8895751Abstract: A process comprising the step of synthesizing 2,6-dibromo-4,8-dihexylbenzo[1,2-d:4,5-d?]bis(thiazole) from 2,5-dihyxylbenzene-1,4-diamine.Type: GrantFiled: July 30, 2013Date of Patent: November 25, 2014Assignee: Phillips 66 CompanyInventor: Hui Huang
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Patent number: 8865713Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: September 3, 2013Date of Patent: October 21, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Publication number: 20140288302Abstract: A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R1R2)—C(?O)—NR3R4 and a group represented by formula: —R5, a broken line represents presence or absence of a bond, Z is —NR6—, ?N—, —O—, or —S—, R6 is halogen or substituted or unsubstituted alkyl, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen or substituted or unsubstituted alkyl, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: Shionogi & Co., Ltd.Inventors: Koji MASUDA, Shiro KIDA, Kyohei HAYASHI, Manabu KATOU, Naoki YOSHIKAWA, Akira KUGIMIYA, Mado NAKAJIMA, Nobuyuki TANAKA
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Patent number: 8822698Abstract: Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.Type: GrantFiled: November 28, 2012Date of Patent: September 2, 2014Assignees: Universite d'Aix-Marseille, Universite de Lorraine, Oreste Piccolo Studio di Consulenza Scientifica, Universitat de Barcelona, Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Flavio Maina, Rosanna Dono, Oreste Piccolo, Daniele Passarella, Francesco Colombo, Joan Bosch, Bernard Maigret, Vincent Leroux
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Publication number: 20140227320Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: ApplicationFiled: September 27, 2012Publication date: August 14, 2014Inventors: Shawn P. Iadonato, Kristin Bedard, Myra Wang Imanaka, Kerry W. Fowler
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Publication number: 20140221664Abstract: The inventions disclosed and described herein relate to new and efficient generic methods for making a wide variety of compounds having HAr—Z-Har tricyclic cores, wherein HAr is an optionally substituted five or six membered heteroaryl ring, and Hal is a halogen, and Z is a bridging radical, such as S, Sc, NR5, C(O), C(O)C(O), Si(R5)2, SO, SO2, PR5, BR5, C(R5)2 or P(O)R5 and both HAr are covalently bound to one another. The synthetic methods employ a “Base-Catalyzed Halogen Dance” reaction to prepare a metallated compound comprising a five or six membered heteroaryl ring comprising a halogen atom, and then oxidatively coupling the reactive intermediate compound. The compounds of Formula (II) and/or oligomer or polymers comprising repeat units having Formula (II) can be useful for making semi-conducting materials, and/or electronic devices comprising those materials. Acyl compounds can be prepared. Heteroarylene substituents can be used. The core tricyclic core can be coupled to itself.Type: ApplicationFiled: August 9, 2012Publication date: August 7, 2014Applicant: GEORGIA TECH RESEARCH CORPORATIONInventors: Yulia A. Getmanenko, Seth Marder, Do Kyung Hwang, Bernard Kippelen
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Publication number: 20140199348Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: ApplicationFiled: February 12, 2013Publication date: July 17, 2014Applicant: KINETA, INC.Inventors: Shawn P. Iadonato, Kristin M. Bedard, Ernesto J. Muñoz, Myra W. Imanaka, Kerry W. Fowler
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Patent number: 8779154Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 25, 2007Date of Patent: July 15, 2014Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
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Publication number: 20140193340Abstract: This disclosure relates to luciferin amides of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to detect fatty acid amide hydrolase activities in vitro, in live cells, or in vivo.Type: ApplicationFiled: March 15, 2013Publication date: July 10, 2014Applicant: University of MassachusettsInventor: Stephen C. Miller
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Patent number: 8759345Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: April 28, 2009Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Patent number: 8735434Abstract: The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 15, 2008Date of Patent: May 27, 2014Assignee: AbbVie Inc.Inventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Jennifer M. Frost, Sridhar Peddi
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Patent number: 8703960Abstract: A composition having the structure comprising: wherein Z is a halogen; wherein X is selected from the group consisting of N, O, P, S, and Se; wherein Y is selected from the group consisting of N, O, P, S and Se; and wherein R is an n-alkane chain.Type: GrantFiled: July 25, 2013Date of Patent: April 22, 2014Assignee: Phillips 66 CompanyInventor: Hui Huang
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Publication number: 20140066629Abstract: Aromatic azole compounds such as 2-(4-aminophenyl)-5-amino-benzimidazole are prepared in an organic sulfonic acid solvent instead of polyphosphoric acid. This allows recovery and recycle of the solvent and avoids the handling and environmental concerns resulting from the use of polyphosphoric acid. The resulting compounds find use in the pharmaceutical industry, as anticorrosion agents, and as precursors for high-performance fibers having high strength, stiffness, and flame resistance.Type: ApplicationFiled: August 29, 2012Publication date: March 6, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: MARC B. GOLDFINGER, TIMOTHY PELLENBARG
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Publication number: 20140058111Abstract: A process comprising the step of synthesizing 2,6-dibromo-4,8-dihexylbenzo[1, 2-d:4,5-d?]bis(thiazole) from 2,5-dihyxylbenzene-1,4-diamine.Type: ApplicationFiled: July 30, 2013Publication date: February 27, 2014Applicant: PHILLIPS 66 COMPANYInventor: Hui Huang
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Publication number: 20140058110Abstract: A composition having the structure comprising: wherein Z is a halogen; wherein X is selected from the group consisting of N, O, P, S, and Se; wherein Y is selected from the group consisting of N, O, P, S and Se; and wherein R is an n-alkane chain.Type: ApplicationFiled: July 25, 2013Publication date: February 27, 2014Applicant: PHILLIPS 66 COMPANYInventor: Hui Huang
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Publication number: 20140005193Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Frances Meredith Hocutt, BARRY EASTMAN LEONARD, JR., HILLARY M. PELTIER, VICTOR K. PHUONG, MICHAEL H. RABINOWITZ, MARK D. ROSEN, KYLE T. TARANTINO, HARIHARAN VENKATESAN, LUCY XIUMIN ZHAO
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Publication number: 20130296315Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.Type: ApplicationFiled: March 11, 2013Publication date: November 7, 2013Inventor: Bayer CropScience AG
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Patent number: 8557810Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: January 24, 2012Date of Patent: October 15, 2013Assignee: Ambit Biosciences CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Patent number: 8552215Abstract: Disclosed is a method for producing an optically active 2-hydroxy ester, comprising selectively esterifying one enantiomer of a racemic 2-hydroxy ester in a solvent containing a catalyst such as tetramisole or benzotetramisole, and a carboxylic acid anhydride, or a carboxylic acid anhydride and a carboxylic acid. In particular, in the case where the solvent contains a carboxylic acid anhydride, but does not contain a carboxylic acid, as the carboxylic acid anhydride, a carboxylic acid anhydride containing a tertiary or quaternary carbon atom in the a-position is used. On the other hand, in the case where the solvent contains a carboxylic acid anhydride and a carboxylic acid, as the carboxylic acid, a carboxylic acid containing a tertiary or quaternary carbon atom in the a-position is used.Type: GrantFiled: March 8, 2010Date of Patent: October 8, 2013Assignee: Tokyo University of Science Educational Foundation Administrative OrganizationInventors: Isamu Shiina, Kenya Nakata
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Patent number: 8551963Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: November 5, 2009Date of Patent: October 8, 2013Assignee: Ambit Biosciences CorporationInventors: Julius L. Apuy, Darren E. Insko, Joyce J. James
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Publication number: 20130214208Abstract: The invention relates to novel polymers containing repeating units based on benzo[1,2-d;4,3-d?]bisthiazole, monomers and methods for their preparation, their use as semiconductors in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices, and to OE and OPV devices comprising these polymers.Type: ApplicationFiled: September 21, 2011Publication date: August 22, 2013Applicant: MERCK PATENT GMBHInventors: William Mitchell, Mansoor D'Lavari, Steven Tierney, Nicolas Blouin, Thorsten Schwalm
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Publication number: 20130178505Abstract: Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.Type: ApplicationFiled: June 28, 2011Publication date: July 11, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Michael Chorev, Bertal Huseyin Aktas, Jose A. Halperin, Gerhard Wagner
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Publication number: 20130167930Abstract: The invention relates to compounds of general formula IIIa and their use in optoelectronic components.Type: ApplicationFiled: December 29, 2011Publication date: July 4, 2013Applicant: Heliatek GmbhInventors: Dirk Hildebrandt, Gunter Mattersteig, Olga Gerdes, Serge Vetter, Andre Weiss
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Patent number: 8471035Abstract: Two-photon absorbing arylamine-endcapped and dialkylfluorene-bridged benzobisthiazole-based compounds are provided. These two-photon absorbing benzobisthiazole-based compounds show high solubility in nonpolar hydrocarbon solvents (oleophilicity) and high two-photon properties, especially in the nanosecond domain of pulse-laser excitation.Type: GrantFiled: May 18, 2012Date of Patent: June 25, 2013Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Loon-Seng Tan, Ramamurthi Kannan, Matthew Dalton
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Publication number: 20130144065Abstract: The present invention provides semiconducting compounds, oligomers and polymers of formula wherein A1 and A2 can be the same or different and are S or Se, E is selected from the group consisting of The compounds, oligomers and polymers of formula of formula (1) are suitable for use in electronic devices such as organic field effect transistors.Type: ApplicationFiled: July 29, 2011Publication date: June 6, 2013Applicants: Polyera Corporation, BASF SEInventors: Ashok Kumar Mishra, Subramanian Vaidyanathan, Hiroyoshi Noguchi, Florian Doetz, Bo Zhu, Johan Sebastian Basuki
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Publication number: 20130085143Abstract: Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.Type: ApplicationFiled: November 28, 2012Publication date: April 4, 2013Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE LORRAINE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S), UNIVERSITAT DE BARCELONA, ORESTE PICCOLO STUDIO DI CONSULENZA SCIENTIFICAInventors: Universite D'aix-Marseille, Universite De Lorraine, Oreste Piccolo Studio Di Consulenza Scientifica, Universitat De Barcelona, Centre National De La Recherche Scientifique (C.
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Patent number: 8389736Abstract: The invention provides compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The compositions pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The compositions and pharmaceutical preparations of the invention may comprise one or more bithiazole-containing compounds of the invention, or an analog or derivative thereof.Type: GrantFiled: September 5, 2008Date of Patent: March 5, 2013Assignee: The Regents of the University of CaliforniaInventors: Mark J. Kurth, Alan S. Verkman
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Patent number: 8357707Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.Type: GrantFiled: July 2, 2010Date of Patent: January 22, 2013Assignee: Novartis AGInventors: Robin Alec Fairhurst, Marc Gerspacher, Robert Mah
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Publication number: 20130012488Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 7, 2012Publication date: January 10, 2013Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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Publication number: 20130005966Abstract: Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-fe][1,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert-Butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-&][1,3]benzo-thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers.Type: ApplicationFiled: November 4, 2010Publication date: January 3, 2013Applicant: Ambit Biosciences Corp.Inventors: Timothy David Gross, Rathan Prasad Achampeta, Janakiram Citineni
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Patent number: 8344018Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: GrantFiled: July 14, 2009Date of Patent: January 1, 2013Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Chandrasekar Venkataramani
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Patent number: 8304556Abstract: 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 characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: January 11, 2012Date of Patent: November 6, 2012Assignee: 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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Publication number: 20120276047Abstract: The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 23, 2010Publication date: November 1, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge
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Patent number: 8288379Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: April 20, 2010Date of Patent: October 16, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Lars Van Der Veen, Maria Impagnatiello, Darryl McConnell, Siegfried Schneider, Tobias Wunberg
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Patent number: 8262949Abstract: The instant invention relates to novel benzotriazole UV-absorbers having a long wavelength shifted absorption spectrum with significant absorbance up to 410-420 nm. Further aspects of the invention are a process for their preparation, a UV stabilized composition containing the new UV-absorbers and the use of the new compounds as UV-light stabilizers for organic materials.Type: GrantFiled: June 18, 2007Date of Patent: September 11, 2012Assignee: BASF SEInventors: Katharina Fritzsche, Markus Grob, Adalbert Braig, Ilona Marion Kienzle, Gérard Daniel Georges Vilain
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Publication number: 20120196852Abstract: The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds.Type: ApplicationFiled: August 5, 2010Publication date: August 2, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Jun O. Liu, Omonike Arike Olaleye, Shridhar Bhat
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Patent number: 8203001Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: June 13, 2007Date of Patent: June 19, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20120129811Abstract: This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Aihua WANG, Yan Zhang, Kristi Anne Leonard, Michael Hawkins, Brett Andrew Tounge, Umar S.M. Maharoof, Joseph Kent Barbay
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Publication number: 20120108618Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X 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: April 22, 2010Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars Van Der Veen, Darryl Mcconnell, Siegfried Schneider, Matthias Grauert, Andreas Schoop, Tobias Wunberg
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Patent number: 8143291Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: GrantFiled: January 3, 2011Date of Patent: March 27, 2012Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Patent number: 8143414Abstract: This disclosure concerns novel compounds of Formula (I) or Formula (II) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: GrantFiled: April 7, 2010Date of Patent: March 27, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Rico Lavoie, John A. Bender, Carol Bachand, Edward H. Ruediger, John F. Kadow
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Publication number: 20120070410Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: ApplicationFiled: November 5, 2009Publication date: March 22, 2012Inventors: Julius L. Apuy, Darren E. Insko, Joyce J. James
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Publication number: 20120070374Abstract: The invention relates to the provision of compounds, methods for producing them, and their use for imaging and quantification of aggregates of ?-amyloid peptides in vivo. In a preferred aspect of the invention, a tracer is administered to humans and displays enrichment in body parts that are containing aggregates of amyloid peptides. Tracers of the invention can be used for non-invasive depiction and quantification of aggregates of ?-amyloid peptides in humans affected with diseases that are characterized in the generation of such aggregates.Type: ApplicationFiled: February 11, 2010Publication date: March 22, 2012Inventors: Henriksen Gjermund, Behrooz Hooshyar Yousefi, Hans-Juergen Wester
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Patent number: 8115008Abstract: Disclosed is a method for producing an optically active ester by highly selectively esterifying one enantiomer of a racemic carboxylic acid, while producing an optically active carboxylic acid which is the other enantiomer. An optically active ester is produced while producing an optically active carboxylic acid at the same time by reacting a racemic carboxylic acid with a specific alcohol or phenol derivative in the presence of benzoic anhydride or a derivative thereof and a catalyst such as tetramisole or benzotetramisole, thereby selectively esterifying one enantiomer of the racemic carboxylic acid.Type: GrantFiled: March 4, 2009Date of Patent: February 14, 2012Assignee: Tokyo University of Science Education Foundation Administrative OrganizationInventors: Isamu Shiina, Kenya Nakata
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Publication number: 20120009519Abstract: The present invention provides a compound represented by the formula (I): wherein R1 represents a hydrogen atom, a halogen atom or a C1-C6 alkyl group which may have one or more halogen atoms, A1 represents a divalent connecting group, X1 represents a C2-C36 heterocyclic group and one or more —CH2— in the C2-C36 heterocyclic group can be replaced by —CO— or —O—, R2 is independently in each occurrence a halogen atom, a hydroxyl group, a C1-C24 hydrocarbon group, a C1-C12 alkoxy group, a C2-C4 acyl group or a C2-C4 acyloxy group, and m represents an integer of 0 to 10.Type: ApplicationFiled: July 1, 2011Publication date: January 12, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hyungjoo KIM, Akira KAMABUCHI, Yuichi MUKAI