Ring Oxygen In The Tricyclo Ring System Patents (Class 546/89)
  • Patent number: 10308665
    Abstract: The present invention relates to a method for the production of a rapamycin derivative of formula (I), the method comprising the preparation of a 2-(tri-substituted silyl)oxyethyl triflate by reacting ethylene oxide and a tri-substituted silyl triflate, reaction of the resulting 2-(tri-substituted silyl)oxyethyl triflate with rapamycin in the presence of a molar excess of organic base, and deprotection to obtain the rapamycin derivative of compound (I).
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: June 4, 2019
    Assignee: Synbias Pharma AG
    Inventors: Oleksandr Zabudkin, Christian Schickaneder, Iaroslav Matviienko, Volodymyr Sypchenko
  • Patent number: 9957277
    Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X, Y, R1, R2, R3a, R3b, R4a, R4b and R5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: May 1, 2018
    Assignee: eFFECTOR Therapeutics, Inc.
    Inventors: Justin T. Ernst, Siegfried H. Reich, Paul A. Sprengeler, Chinh Viet Tran, Garrick Kenneth Packard, Alan X. Xiang, Christian Nilewski, Theo Michels
  • Patent number: 9944652
    Abstract: Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: April 17, 2018
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Alan R. Saltiel, Hollis D. Showalter, Scott Larsen
  • Patent number: 9738654
    Abstract: The problem of the present invention is to provide a production method for safely synthesizing a nitrogen-containing heterocyclic N-oxide compound in high yield. Another problem of the present invention is to provide a novel N-oxide compound. There is provided a method for producing a nitrogen-containing heterocyclic N-oxide compound of Formula (2), such as 2,2,7,9-tetramethyl-2H-pyrano[2,3-g]quinoline N-oxide, by oxidizing a nitrogen-containing heterocyclic compound of Formula (1), such as 2,2,7,9-tetramethyl-2H-pyrano[2,3-g]quinoline with a persulfate.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: August 22, 2017
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Hironobu Yoshino, Kenichi Seki, Hirohide Kitsuyama, Ikumasa Hidaka
  • Patent number: 9708337
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: July 18, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Carolyn Diane Dzierba, Joanne J. Bronson, John E. Macor, Susheel Jethanand Nara, Ramkumar Rajamani, Maheswaran Sivasamban Karatholuvhu
  • Patent number: 9464095
    Abstract: A method for producing a high-purity nitrogen-containing heterocyclic compound includes: a process (a) and a process (b): (a) a process of mixing a mixture containing a compound and as an impurity compound with a solvent and a metal salt, and (b) a process of obtaining a mixture in a solution state in which the content of the compound has decreased compared to that in the mixture in the process (a) by filtering a mixed solution obtained in the process (a), or a process of obtaining a mixture in which the content of the compound has decreased compared to that in the mixture in the process (a) by further evaporating the solvent or crystallizing following the filtering; (where R1 and R2 are each independently a hydrogen atom, a C1-6 alkyl group, etc., R3 is a hydrogen atom, a C1-6 alkyl group, etc., X is a hydrogen atom, etc.).
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: October 11, 2016
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Hirohide Kitsuyama, Akihiro Nagaya, Hironobu Yoshino, Ikumasa Hidaka
  • Patent number: 9365581
    Abstract: Provided herein is technology relating to deuterated amiexanox and particularly, but not exclusively, to compositions comprising deuterated amiexanox, methods of producing deuterated amiexanox, and uses of deuterated amiexanox. Provided herein are deuteratecl amiexanox compounds for the treatment of obesity, insulin resistance, diabetes, and steatosis. In addition, the deuterated compounds are anti-inflammatory antiallergic immunomodulators. e.g., for the treatment of diseases associated with inflammation. The deuterium kinetic isotope effect associated with placing deuterium at the site of metabolic derivatization slows metabolic derivatization and thus increases the lifetime of the active drug in vivo.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: June 14, 2016
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Alan R. Saltiel, Hollis D. Showalter, Scott Larsen
  • Patent number: 9193738
    Abstract: The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: November 24, 2015
    Assignee: LABORATORIOS DEL DR. ESTEVE S.A.
    Inventors: José-Luis Diaz-Fernández, Ute Christmann
  • Patent number: 9150583
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this protein.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: October 6, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thomas Trieselmann, Dieter Hamprecht, Holger Wagner
  • Patent number: 9035042
    Abstract: The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: May 19, 2015
    Assignee: ATTO-TEC GmbH
    Inventors: Alexander Zilles, Jutta Arden-Jacob, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Monika Hamers-Schneider
  • Patent number: 9029544
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: May 12, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Daniela Berta, Klaus Fuchs, Riccardo Giovannini, Dieter Wolfgang Hamprecht, Ingo Konetzki, Ruediger Streicher, Thomas Trieselmann
  • Publication number: 20150111891
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: April 23, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
  • Patent number: 9006229
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: April 14, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael L. Mitchell, Paul A. Roethle, Lianhong Xu, Hong Yang, Ryan McFadden, Kerim Babaoglu
  • Publication number: 20150072975
    Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Berangere Gaucher, JR., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin XU
  • Patent number: 8969373
    Abstract: A compound of general formula (I); A is O, S, CH, NH or NR?, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1? is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
    Type: Grant
    Filed: July 23, 2012
    Date of Patent: March 3, 2015
    Assignee: Shanghai Tangrun Pharmaceuticals Co., Ltd.
    Inventor: Suoming Zhang
  • Patent number: 8969564
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: March 3, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, John E. Macor, Joanne J. Bronson, Carolyn Diane Dzierba, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu
  • Publication number: 20150045374
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: February 12, 2015
    Inventors: Kerim Babaoglu, Kyla L. Bjornson, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu
  • Patent number: 8952363
    Abstract: A new class of compounds containing aza-dibenzothiophene or aza-dibenzofuran are provided. The compounds may be used in organic light emitting devices giving improved stability, improved efficiency, long lifetime and low operational voltage. In particular, the compounds may be used as the host material of an emissive layer having a host and an emissive dopant, or as a material in an enhancement layer.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: February 10, 2015
    Assignee: Universal Display Corporation
    Inventors: Chun Lin, Alexey Borisovich Dyatkin, Zeinab M. Elshenawy
  • Patent number: 8952033
    Abstract: Disclosed herein are novel 4-anilinofuro[2,3-b]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives and their uses in the manufacture of pharmaceutical compositions and in the treatment of cancers.
    Type: Grant
    Filed: December 30, 2011
    Date of Patent: February 10, 2015
    Assignee: Kaohsiung Medical University
    Inventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Yu-Wen Chen, Pei-Jung Lu
  • Publication number: 20150038438
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 5, 2015
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
  • Patent number: 8946424
    Abstract: Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: February 3, 2015
    Assignee: The Regents of the University of Michigan
    Inventors: Alan R. Saltiel, Hollis D. Showalter, Scott Larsen
  • Publication number: 20150031692
    Abstract: The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: January 24, 2013
    Publication date: January 29, 2015
    Inventors: José-Luis Diaz-Fernández, Ute Christmann
  • Publication number: 20150025067
    Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.
    Type: Application
    Filed: February 13, 2013
    Publication date: January 22, 2015
    Applicant: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventors: Yi Zheng, Prakash Jagtap, Emily E. Bosco, Jaroslaw Meller, Marie-Dominique Filippi
  • Publication number: 20150010921
    Abstract: The present invention relates to a method for detecting cell death using a luminescent compound; to the luminescent compounds for particular uses; to a kit comprising compounds and to a protein. The method is applicable for detecting cell death, essentially regardless of the mechanism through which cell death occurred or is occurring and is therefore not limited e.g. to detecting cell death resulting from only one mechanism selected from apoptosis and necrosis.
    Type: Application
    Filed: February 6, 2013
    Publication date: January 8, 2015
    Applicants: HQ Medical Netherlands B.V., Publiekrechtelijk rechtspersoon Academisch Ziekenhuis Leiden h.o.d.n. LUMC
    Inventors: Markwin Hendrik Maring, Clemens Waltherus Gerardus Löwik, Ermond Reijer Van Beek
  • Publication number: 20140371207
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: December 13, 2013
    Publication date: December 18, 2014
    Applicants: Kyowa Hakko Kirin Co., Ltd., Millennium Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C.B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Publication number: 20140367667
    Abstract: A compound represented by the following formula (1):
    Type: Application
    Filed: December 28, 2012
    Publication date: December 18, 2014
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Kazuki Nishimura
  • Publication number: 20140356873
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Zhenjun DIWU, Jixiang LIU, Kyle GEE
  • Patent number: 8889704
    Abstract: Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: November 18, 2014
    Assignee: Array BioPharma Inc.
    Inventors: James F. Blake, Robert Kirk Delisle, Lisa A. De Meese, James M. Graham, Yvan Le Huerou, Michael Lyon, John E. Robinson, Eli M. Wallace, Bin Wang, Rui Xu
  • Publication number: 20140329848
    Abstract: Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox.
    Type: Application
    Filed: May 2, 2014
    Publication date: November 6, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Alan R. Saltiel, Hollis D. Showalter, Scott Larsen
  • Publication number: 20140315927
    Abstract: The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: Andrew Simon Bell, lain Brian GARDNER, Karl Richard GIBSON, David Cameron PRYDE, Florian Michel WAKENHUT
  • Patent number: 8859529
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Publication number: 20140296272
    Abstract: The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Dorothée Bardiot, Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
  • Patent number: 8846925
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Grant
    Filed: May 14, 2012
    Date of Patent: September 30, 2014
    Assignee: Life Technologies Corporation
    Inventors: Zhenjun Diwu, Jixiang Liu, Kyle Gee
  • Publication number: 20140249306
    Abstract: The present invention provides a novel compound having an antiviral action, in particular, an HIV replication inhibiting action, as well as a pharmaceutical composition, in particular, an anti-HIV agent. wherein, a broken line means the presence or absence of a bond; R1 is substituted or unsubstituted alkyl etc., R2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R3 is a substituted or unsubstituted aromatic carbocyclic group; R4 is a hydrogen atom etc.; R5 is a substituted or unsubstituted aromatic carbocyclic group etc.; Y is a single bond etc.; R6 is substituted or unsubstituted alkyl; R7 is —Z—R71 etc.; Z is —NR72—CO— etc.; R71 is substituted or unsubstituted alkyl etc.; R72 is a hydrogen atom etc.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 4, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Tsutomu Iwaki, Kenji Tomita
  • Publication number: 20140231794
    Abstract: A compound represented by the following formula (1): wherein in the formula (1), Ar1 and Ar2 are independently a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or a substituted or unsubstituted alkyl group; X1 to X4 and X13 to X16 are independently CR1, CH or N; one of X5 to X8 is a carbon atom bonding to one of X9 to X12, and at least one of X5 to X8 that is adjacent to the carbon atom bonding to one of X9 to X12 is CR2; one of X9 to X12 is a carbon atom bonding to one of X5 to X8, and X9 to X12 that is adjacent to the carbon atom bonding to one of X5 to X8 is CH or N; and the remaining X5 to X8 and the remaining X9 to X12 are CR1, CH or N.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 21, 2014
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Kei Yoshida
  • Patent number: 8809533
    Abstract: The instant invention pertains to novel bi- or tricyclic sterically hindered alkoxyamines, their precursors, a process for their preparation and their use as light stabilizers for polymers or coatings, as flame retardants, as peroxide substitutes (rheology modifiers) or carbon radical scavengers.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: August 19, 2014
    Assignee: BASF SE
    Inventors: Stefan Hauck, Walter Fischer, Kai-Uwe Schoening
  • Publication number: 20140220588
    Abstract: The invention relates to novel fluorescent dyes with phosphorylated hydroxymethyl groups, a method for preparing the same as well as to their use in imaging techniques. The fluorescent dyes are coumarin, rhodamine or BODIPY dyes having of one of the following general formulae I-III: wherein W=OP(O) Y1Y2 or P(O) Y1Y2, where Y1 and Y2 independently denote any of the following residues: OH, O(?), ORa and ORb, NHRa and NHRb, NRaRb and NRcRd, ORa and NHRb, ORa and NRbRc, NHRa and NRbRc; and any salt thereof.
    Type: Application
    Filed: October 18, 2011
    Publication date: August 7, 2014
    Applicant: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.
    Inventors: Stefan W. Hell, Shamil Nizamov, Gerald Donnert, Kirill Kolmakov, Heiko Schill, Lars Kastrup, Christian A. Wurm, Vladimir N. Belov, Johanna Bueckers, Katrin Willig
  • Publication number: 20140183486
    Abstract: A specific material for organic electroluminescence device having m-phenylene skeleton in its molecule realizes a highly heat-resistant and long lifetime organic electroluminescence device capable of driving at low voltage with high efficiency.
    Type: Application
    Filed: May 9, 2012
    Publication date: July 3, 2014
    Applicant: Idemitsu Kosan Co., Ltd
    Inventors: Yuki Nakano, Masaki Numata, Hideaki Nagashima
  • Patent number: 8765779
    Abstract: This application relates to tricyclic compounds of Formula I: including all stereoisomers, mixtures of stereoisomers, and salts thereof. This application also relates to compositions comprising compounds of Formula I and uses therefore.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: July 1, 2014
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Derek D. Dunn, Greg A. Hostetler, Robert J. McHugh, George C. Morton, Gerard C. Rosse, Joseph M. Salvino, Babu G. Sundar, Rabindranath Tripathy
  • Publication number: 20140175419
    Abstract: A compound represented by the following formula (1). In the formula, A1 is O, S, Si(Ar1)(Ar2), P(?O)(Ar3)(Ar4), a substituted or unsubstituted arylene group including 6 to 30 ring carbon atoms, or a substituted or unsubstituted heteroarylene group including 5 to 30 ring atoms.
    Type: Application
    Filed: September 11, 2012
    Publication date: June 26, 2014
    Inventors: Yuki Nakano, Kei Yoshida, Hideaki Nagashima, Ryohei Hashimoto
  • Publication number: 20140163012
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
  • Patent number: 8716307
    Abstract: The present invention is directed to methods of using a sirolimus drug and chloroquine or a quinoline derivative in combination. Methods of use are also described.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: May 6, 2014
    Assignee: The Trustees Of The University of Pennsylvania
    Inventors: Ravi Kumar Amaravadi, Craig B. Thompson
  • Publication number: 20140121231
    Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof wherein X, M, Y, R1 and R2 are as defined herein. The compounds have activity as anticancer agents.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 1, 2014
    Inventors: David Robert Bolin, Javier de Vicente Fidalgo, Johannes Hermann, Parcharee Tivitmahaisoon, Lin Yi, Mark Zak
  • Patent number: 8703953
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: April 22, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, John E. Macor, Joanne J. Bronson, Carolyn Diane Dzierba, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu
  • Patent number: 8703793
    Abstract: Compounds of formula (I) wherein the groups R1 to R8 have the meanings indicated in the description, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof have valuable pharmacological properties, which make them useful for the treatment of cardiovascular and related disorders.
    Type: Grant
    Filed: March 2, 2009
    Date of Patent: April 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Daniela Berta, Riccardo Giovannini, Alessandro Mazzacani, Ruediger Streicher, Klaus Fuchs
  • Publication number: 20140094609
    Abstract: The present invention is directed to an improved process for the preparation of Compounds of Formula (I), which are useful in the treatment of HIV infection. In particular, the present invention is directed to an improved process for the preparation of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, which is useful in the treatment of HIV infection.
    Type: Application
    Filed: October 2, 2013
    Publication date: April 3, 2014
    Inventors: Brandon H. Brown, Xiang Wang, Keith R. Fandrick, Joe Ju Gao, Nizar Haddad, Serge R. Landry, Wenjie Li, Zhi-Hui Lu, Bo Qu, Diana C. Reeves, Carl Thibeault, Yongda Zhang
  • Publication number: 20140094486
    Abstract: The invention relates to novel crystalline forms of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, the hydrochloride salt thereof, novel crystalline forms of the hydrochloride salt, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection.
    Type: Application
    Filed: October 3, 2013
    Publication date: April 3, 2014
    Inventors: Zheng Jane LI, Zhibin LI, Laibin LUO, Thomas OFFERDAHL, Soojin KIM, Bing-Shiou YANG
  • Publication number: 20140094485
    Abstract: The invention relates to a novel hemi-succinate salt form of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid and a novel crystalline form thereof, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection.
    Type: Application
    Filed: October 2, 2013
    Publication date: April 3, 2014
    Inventors: Brandon H. Brown, Ernest Anthony Carra, Xiang Wang
  • Publication number: 20140094610
    Abstract: The present invention is directed to an improved process for the preparation of Compounds of Formula (I) or salts thereof which are useful in the treatment of HIV infection. In particular, the present invention is directed to an improved process for the preparation of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid or salt thereof which is useful in the treatment of HIV infection.
    Type: Application
    Filed: October 3, 2013
    Publication date: April 3, 2014
    Inventors: Wenjie LI, Philomen DECROOS, Keith R. FANDRICK, Joe Ju GAO, Nizar HADDAD, Zhi-Hui LU, Bo QU, Sonia RODRIGUEZ, Chris H. SENANAYAKE, Yongda ZHANG, Wenjun TANG
  • Publication number: 20140088078
    Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 27, 2014
    Applicant: ZAFGEN, Inc.
    Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler