Plural 1,3-diazine Rings Patents (Class 544/296)
  • Patent number: 10703692
    Abstract: A reconfigurable polar molecule includes a symmetric nonpolar molecule portion having an elongated shape defined by a longitudinal axis and lateral axis, the longitudinal axis being longer than the lateral axis; a positive ionically charged group at a first end and a negative ionically charged group at a second end of the longitudinal axis, the positive and negative ionically charged groups forming a permanent dipole; a first bridging group and a second bridging group on opposing ends of the lateral axis, the first and second bridging groups being linear nonpolar groups; and a first support portion bonded to the first bridging group, and a second support portion bonded to the second bridging group, the first bridging group and the second bridging group being nonpolar and having structures that enable free rotation of the symmetric nonpolar molecule portion through the first bridging group and the second bridging group.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: July 7, 2020
    Assignee: RAYTHEON COMPANY
    Inventors: Michael Pitman, Teresa J. Clement, Glafkos K. Stratis, Alphonso A. Samuel, Alex Dely, Wayne L. Sunne
  • Patent number: 9982210
    Abstract: The present invention relates to a lubricating composition containing (a) an oil of lubricating viscosity; and (b) a compound selected from the group consisting of: (i) an ester-containing heterocycle; (ii) an amide-containing heterocycle; and (iii) a pyrimidine, wherein the ester-containing heterocycle and the amide-containing heterocycle have a hydrocarbyl group containing 6 to 40 carbon atoms. The invention further provides for a method of supplying an internal combustion engine with the lubricating composition.
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: May 29, 2018
    Assignee: The Lubrizol Corporation
    Inventors: Patrick E. Mosier, Jason R. Brown, Matthew D. Gieselman, Calvin W. Schroeck, Seth L. Crawley, William R. S. Barton, William C. Ward, Jr.
  • Patent number: 9868705
    Abstract: The present disclosure provides tetra-substituted cyclobutane inhibitors of Androgen Receptor Action, and methods of using such inhibitors, for the treatment of hormone-refractory cancers.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: January 16, 2018
    Assignees: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS, DUKE UNIVERSITY
    Inventors: John Katzenellenbogen, Donald McDonnell, John D. Norris, Alexander Parent, Julie Pollock, Jillian Gunther, Kathryn E. Carlson, Teresa Martin
  • Patent number: 9783505
    Abstract: Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: October 10, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Patrick Papa, Brian Edwin Cathers, Andrew Antony Calabrese, Brandon Wade Whitefield, Brydon Bennett, Daniel Cashion, Deborah Mortensen, Dehua Huang, Eduardo Torres, Jason Parnes, John Sapienza, Joshua Hansen, Katerina Leftheris, Matthew Correa, Maria Mercedes Delgado, Raj K. Raheja, Sogole Bahmanyar, Sayee Hegde, Stephen Norris, Veronique Plantevin-Krenitsky
  • Patent number: 9745283
    Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: August 29, 2017
    Assignee: IGNYTA, INC.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Patent number: 9505980
    Abstract: A subject is to provide a polymerizable liquid crystal composition from which an optically anisotropic substance having twist alignment that is excellent in chemical strength (chemical resistance) and has only a small amount of alignment defects can be obtained. A solution is a polymerizable liquid crystal composition containing an optically active compound having a binaphthol moiety, an achiral polymerizable liquid crystal compound and a photopolymerization initiator having oxime ester.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: November 29, 2016
    Assignees: JNC CORPORATION, JNC PETROCHEMICAL CORPORATION
    Inventors: Yoshiharu Hirai, Nagahisa Miyagawa, Daisuke Ootsuki
  • Patent number: 9419227
    Abstract: An OLED (organic light emitting diode) comprises a series of spirally configured cis-stilbene/fluorene hybrid materials. The spirally configured cis-stilbene/fluorene hybrid materials are spirally-configured cis-stilbene/fluorene derivatives having the functions to block holes and constructed by at least one cis-Stilbene based component and at least one fluorene based component.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: August 16, 2016
    Assignee: NICHEM FINE TECHNOLOGY CO., LTD.
    Inventors: Chien-Tien Chen, Jwo-Huei Jou
  • Patent number: 9266862
    Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.
    Type: Grant
    Filed: May 1, 2014
    Date of Patent: February 23, 2016
    Assignee: Genentech, Inc.
    Inventors: Anthony Estrada, Alan G. Olivero, Snahel Patel, Michael Siu
  • Patent number: 9209413
    Abstract: The present invention provides a series of spirally configured cis-stilbene/fluorene hybrid materials, which are spirally-configured cis-stilbene/fluorene derivatives having glass transition temperatures ranged from 110° C. to 135° C., decomposition temperatures ranged from 380° C. to 425° C., reversible electron transport property, and balanced charges motilities. In addition, a variety of experimental data have proved that this spirally configured cis-stilbene/fluorene hybrid materials can indeed be used as a hole-blocking type electron-transporter and/or a host material for phosphorescent OLEDs.
    Type: Grant
    Filed: December 27, 2014
    Date of Patent: December 8, 2015
    Assignee: NICHEM FINE TECHNOLOGY CO. LTD.
    Inventors: Chien-Tien Chen, Jwo-Huei Jou
  • Patent number: 9089500
    Abstract: The present invention relates to a cosmetic process for treating keratin materials, which can give them, especially in a long-lasting and reversible manner, interesting cosmetic properties; this process comprising the application to said materials: in a first stage, of a cosmetic composition comprising at least one graftable species, comprising at least one unit of formula (Ia): and in a second stage, of a cosmetic composition comprising at least one cosmetic active agent bearing at least one unit of formula (Ia): The invention also relates to a kit comprising said compositions.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: July 28, 2015
    Assignee: L'OREAL
    Inventors: Anne-Claude Dublanchet, Christian Blaise
  • Patent number: 9066518
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: June 30, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Bretschneider, Martin Füβlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Publication number: 20150148358
    Abstract: The present invention provides compounds of the Formula below: where R is H or —CH3; methods of treating patients for hypertriglyceridemia and cardiovascular disease including dyslipidemia and atherosclerosis, and processes for preparing the compounds.
    Type: Application
    Filed: November 19, 2014
    Publication date: May 28, 2015
    Applicant: Eli Lilly and Company
    Inventors: Manisha NAIK, Nicholas Paul CAMP
  • Patent number: 9040538
    Abstract: The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: May 26, 2015
    Assignee: Universite Laval
    Inventors: Giorgio Attardo, Sasmita Tripathy, Martin Gagnon
  • Publication number: 20150141434
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R1, R4, X, G, n, p, W1, W2, W3, W4, and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.
    Type: Application
    Filed: September 5, 2014
    Publication date: May 21, 2015
    Inventor: Jae Hyun Park
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Publication number: 20150131302
    Abstract: A novel organic compound is provided. Alternatively, an organic compound that can be used as an electron-transport material of a light-emitting element is provided. An organic compound in which heteroaromatic groups each including two pyridine rings are bonded to the 2- and 8-positions of dibenzofuran is provided. The organic compound is an organic compound that can be used as an electron-transport material of a light-emitting element.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Hideko Inoue, Yui Yamada, Tsunenori Suzuki, Satoshi Seo
  • Patent number: 9029531
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: May 12, 2015
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
  • Patent number: 9029538
    Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.
    Type: Grant
    Filed: May 13, 2014
    Date of Patent: May 12, 2015
    Assignee: Ignyta, Inc.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Publication number: 20150126504
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • Patent number: 9018224
    Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
  • Publication number: 20150111871
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 23, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Publication number: 20150111735
    Abstract: A pesticidal composition comprises a pyridine triazole compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, Z, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse
  • 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: 9012461
    Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Cancer Therapeutics CRC Pty Ltd
    Inventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
  • Publication number: 20150105401
    Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.
    Type: Application
    Filed: October 7, 2014
    Publication date: April 16, 2015
    Applicant: The University of Rochester
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin J. Loweth, Torsten Wiemann
  • Patent number: 9006228
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: June 11, 2012
    Date of Patent: April 14, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
  • Patent number: 9006232
    Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: April 14, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
  • Publication number: 20150099756
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Yun JIN, Zehong WAN, Qing ZHANG
  • Patent number: 9000003
    Abstract: The present invention is anti-folate antimalarials with dual-binding modes of the general formula (I) [refer to structure in the abstract] wherein R1 and R2 which may be the same or different are independently selected from methyl or ethyl or alkylphenyl, R3 is independently hydrogen, halide, lower alkyl substituted with ester, carboxylic, amide, and ether. Linker is X(CH2)nY wherein X and Y which may be the same or different are independently selected from oxygen, carbon, nitrogen, substituted phenyl where n is an integer from 1 to 2-6, or pharmaceutically acceptable salts therefore. The anti-folate antimalarials with dual-binding modes act as novel inhibitors with good inhibition constants against wild-type, double (C59R+SIOSN), triple (N51+C59R+SIOSN, C59R+S 1 OSN+I164L), and quadruple (N51+C59R+S108N+I164L) mutant enzymes. The compounds are also effective against wild type (Tm4/S.2) and mutants (K1CB1, W2, Cs1-2 and V1/S) malaria parasites.
    Type: Grant
    Filed: February 9, 2012
    Date of Patent: April 7, 2015
    Assignee: National Science and Technology Development Agency
    Inventors: Bongkoch Tarnchompoo, Penchit Chitnumsub, Sumalee Kamchonwongpaisan, Philip James Shaw, Roonglawan Rattanajak, Sinothai Poen, Tosapol Anukunwithaya, Chayaphat Wongsombat, Yongyuth Yuthavong
  • Publication number: 20150094298
    Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 2, 2015
    Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Yonghong Song, Qing Xu, Wolin Huang, Chandrasekar Venkataramani, Jack W. Rose, Anjali Pandey
  • Patent number: 8993754
    Abstract: Provided is an iridium complex having a substructure represented by the following formula (1), which is a luminescent element material capable of luminescence with high brightness/high efficiency and excellent in durability and can be used in a luminescent element, etc.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: March 31, 2015
    Assignee: National Institute of Advanced Industrial Science and Technology
    Inventor: Hideo Konno
  • Publication number: 20150087651
    Abstract: The present invention relates to novel compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the integers are as defined in the description. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 26, 2015
    Inventors: Jean-Francois Bonfanti, Philippe Muller, Frederic Marc Maurice Doubler, Jerome Michel Claude Fortin, Nacer Lounis
  • Publication number: 20150087665
    Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Application
    Filed: September 20, 2013
    Publication date: March 26, 2015
    Inventor: Hubert Maehr
  • Publication number: 20150087043
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 11, 2014
    Publication date: March 26, 2015
    Applicants: Coferon, Inc, Cornell University
    Inventors: Lee Daniel Arnold, Maneesh Pingle, Douglas S. Werner
  • Publication number: 20150084016
    Abstract: An organic electroluminescent element including a luminescent compound represented by the following formula (in which R1 to R14 each independently represent a hydrogen atom, a deuterium atom, an alkyl group, an aryl group, a heteroaryl group, a fluorine atom, a cyano group, an amino group, an alkoxy group, an aryloxy group, a thio group, or a silyl group, and 8 to 13 groups out of R1 to R14 each represent a hydrogen atom or a deuterium atom.) in a light emitting layer has high durability and excellent chromaticity.
    Type: Application
    Filed: October 5, 2012
    Publication date: March 26, 2015
    Applicant: UDC IRELAND LIMITED
    Inventors: Toru Watanabe, Yuki Hirai, Tianhua Ouyang, Koji Takaku, Wataru Sotoyama, Tetsu Kitamura, Yasunori Yonekuta
  • Publication number: 20150080568
    Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
    Type: Application
    Filed: July 28, 2014
    Publication date: March 19, 2015
    Inventors: Weirong Chen, Benjamin Lane, Hairuo Peng
  • Publication number: 20150080368
    Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Applicant: VERASTEM, INC.
    Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
  • Patent number: 8975402
    Abstract: The present invention relates to a new HPLC method for the analysis of the drug substance bosentan and related substances and to the use of said substances as reference standards and markers.
    Type: Grant
    Filed: November 2, 2009
    Date of Patent: March 10, 2015
    Assignee: Generics [UK] Limited
    Inventors: Erra Koteswara Satya Vijaya Kumar, Avinash Prabhakar Nikam
  • Publication number: 20150065505
    Abstract: The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: March 29, 2013
    Publication date: March 5, 2015
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
  • Publication number: 20150065523
    Abstract: The present invention provides compounds of formula (I) including stereoisomers or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein X is NH, or O; Q is 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; A is phenyl or a 5-6 heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; B may assume different meanings from A and is phenyl or a 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; and processes for their preparation, pharmaceutical compositions containing them and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.
    Type: Application
    Filed: March 18, 2013
    Publication date: March 5, 2015
    Inventors: Luigi Piero Stasi, Lucio Claudio Rovati
  • Publication number: 20150065532
    Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
  • Patent number: 8962622
    Abstract: Compounds of formula I modulate jnk and cdk: or a pharmaceutically acceptable salt thereof, where R, R1, R2, R3, and m are defined herein.
    Type: Grant
    Filed: September 7, 2007
    Date of Patent: February 24, 2015
    Assignee: Roche Palo Alto LLC
    Inventors: David Michael Goldstein, Levi Gong, Christophe Michoud, Wylie Solang Palmer, Achyutharao Sidduri
  • Patent number: 8962158
    Abstract: Provided is an organic electroluminescent device (organic EL device), which has improved luminous efficiency, has sufficient driving stability, and has a simple construction. The organic EL device of the present invention is an organic electroluminescent device, including a light-emitting layer and a hole-transporting layer between an anode and a cathode laminated on a substrate, in which the light-emitting layer contains a phosphorescent light-emitting dopant and an indolocarbazole compound that serves as a host material, or alternatively, the hole-transporting layer contains an indolocarbazole compound. The indolocarbazole compound is represented by the following formula (1). In the formula: A1's each represent an aromatic hydrocarbon group or an aromatic heterocyclic group, provided that at least one of A1's has a fused ring structure; and R1's each represent a hydrogen atom, an alkyl group, an alkoxy group, or an acyl group.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: February 24, 2015
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Masaki Komori, Takahiro Kai, Toshihiro Yamamoto
  • Publication number: 20150051238
    Abstract: Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 19, 2015
    Applicant: GENENTECH, INC.
    Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Bryan K. Chan, Mark Chambers, Huifen Chen, Anthony Estrada, Zachary Kevin Sweeney
  • Publication number: 20150051395
    Abstract: Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent ?4 integrin-inhibitory action.
    Type: Application
    Filed: April 24, 2013
    Publication date: February 19, 2015
    Applicant: AJINOMOTO CO., LTD.
    Inventors: Hirokazu Ueno, Takashi Yamamoto, Ryuta Takashita, Ryohei Yokoyama, Toshihiko Sugiura, Shunsuke Kageyama, Ayatoshi Ando, Hiroyuki Eda, Agung Eviryanti, Tomoko Miyazawa, Aya Kirihara, Itsuya Tanabe, Tarou Nakamura, Misato Noguchi, Manami Shuto, Masayuki Sugiki, Mizuki Dohi
  • Patent number: 8957068
    Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: February 17, 2015
    Assignee: Novartis AG
    Inventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
  • Publication number: 20150045378
    Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Application
    Filed: February 12, 2013
    Publication date: February 12, 2015
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
  • Publication number: 20150038460
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: October 16, 2014
    Publication date: February 5, 2015
    Applicant: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
  • Publication number: 20150038481
    Abstract: Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described.
    Type: Application
    Filed: May 21, 2013
    Publication date: February 5, 2015
    Inventors: Xiaodong Wang, Weihe Zhang, Dmitri Kireev, Dehui Zhang, Andrew Mclver