1,3-diazines Patents (Class 544/242)
  • Patent number: 8884008
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: November 11, 2014
    Assignee: OliPass Corporation
    Inventors: Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
  • Publication number: 20140329816
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Application
    Filed: July 26, 2012
    Publication date: November 6, 2014
    Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson
  • Patent number: 8859766
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: October 14, 2014
    Assignee: OliPass Corporation
    Inventors: Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8859566
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: October 14, 2014
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Patent number: 8859591
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: October 14, 2014
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Publication number: 20140239273
    Abstract: An anthracene derivative is represented by a formula (1) below, in which at least one of Ar1, Ar2, Ar3, L1, L2 and L3 is a group derived from a skeleton represented by a formula (10) below,
    Type: Application
    Filed: December 18, 2013
    Publication date: August 28, 2014
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Sayaka MIZUTANI, Takayasu Sado
  • Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • Patent number: 8791299
    Abstract: 3D protein modeling and virtual screening of commercially-available compounds were performed to identify new inhibitors of the herpesvirus DNA polymerase, a key enzyme in the viral replication cycle. Two compounds (Nos 2 and 9) were particularly active against HSV-1 and HSV-2 strains and one compound (No 3) inhibited specifically cytomegalovirus (CMV) strains (overall hit rate of 25%). Some of the tested compounds inhibited wild-type viruses and strains resistant to current antiviral agents. New chemical entity derivatives of compound 2 with binding potential to the DNA polymerase retained an excellent activity against HSV-1, HSV-2 and VZV like the parental compound, as well against strains resistant to current antiviral agents. These non-nucleosidic herpesvirus DNA polymerase inhibitors with in vitro activity against drug-resistant clinical isolates warrant further pre-clinical studies.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: July 29, 2014
    Assignee: Universite Laval
    Inventors: Guy Boivin, Sheng-Xiang Lin, Melanie Martin, Arezki Azzi
  • Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8772291
    Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: July 8, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
  • Publication number: 20140166988
    Abstract: The present invention discloses a novel organic compound is represented by the following formula(I), the organic EL device employing the organic compound as host material or dopant material of emitting layer and/or as electron transporting material can lower driving voltage, prolong half-lifetime and increase the efficiency. wherein m represent an integer of 0 to 10, n represent an integer of 0 to 2. X is a divalent bridge selected from the atom or group consisting from O, S, C(R5)2, N(R5), Si(R5)2. Ar, R1 to R4 are substituents and the same definition as described in the present invention.
    Type: Application
    Filed: December 17, 2012
    Publication date: June 19, 2014
    Applicant: LUMINESCENCE TECHNOLOGY CORPORATION
    Inventors: Feng-Wen Yen, Chen-Hao Chang
  • Publication number: 20140160384
    Abstract: The present invention relates to a smectic A phase liquid crystal material, which contains at least one heterocyclic compound. The smectic A phase liquid crystal material of the present invention may further contain at least one ester compound and an ionic compound. By using the smectic A phase liquid crystal material in a display device, a displayed image can be completely erased without any residual images after a long-term placement or a long-term drive, the contrast is generally higher than 10, and the drive voltage is generally 20 to 50 V.
    Type: Application
    Filed: September 27, 2012
    Publication date: June 12, 2014
    Inventors: Wenlei Li, Gang Sun, Huan Yin, Zhixian Tan, Huaibin Zhai
  • Patent number: 8748434
    Abstract: This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: June 10, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Henrietta Dehmlow, Shawn David Erickson, Patrizio Mattei, Hans Richter
  • Patent number: 8741450
    Abstract: A material for organic electroluminescence devices comprising a compound in which a heterocyclic group having nitrogen is bonded to an arylcarbazolyl group or a carbazolylalkylene group and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer comprising at least one layer and disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the material for organic electroluminescence devices described above. The material can provide an organic electroluminescence device emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: June 3, 2014
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Hiroshi Yamamoto, Yoshio Hironaka, Hidetsugu Ikeda, Chishio Hosokawa, Seiji Tomita, Takashi Arakane
  • Patent number: 8735417
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: May 27, 2014
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michael D. Altman, Kenneth L. Arrington, Jason Burch, Bernard Cote, Jean-Francois Fournier, Jacques Yves Gauthier, Solomon Kattar, Sandra Lee Knowles, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Michael H. Reutershan, Joel S. Robichaud, Adam J. Schell, Kerrie B. Spencer
  • Patent number: 8728567
    Abstract: The present invention pertains to the double complex salts in optoelectronic components, like organic diodes, organic transistors or organic lasers, in particular an organic solar cell (OSC, OPP) and in particular from oligomers built from charged metal complexes.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: May 20, 2014
    Assignee: Cynora GmbH
    Inventors: Hartmut Yersin, Tobias Fischer, Uwe Monkowius
  • Patent number: 8716472
    Abstract: A tri-podal compound according to formula (I) wherein, each Z is the same and is a substituted or unsubstituted N-heteroaromatic single-, multiple-, or fused-ring; and each A is the same, and can represent a direct bond between the cyclohexane ring and Z, or a carboxamide group (—C(O)—N(H)—). Use of the compounds in combinatorial libraries, methods of making the tripodal compounds, sensor devices for detecting carbohydrate targets, and methods of using the tripodal compounds to detect carbohydrate targets in a sample are also disclosed.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: May 6, 2014
    Assignee: University of Rochester
    Inventors: Benjamin L. Miller, Prakash B. Palde, Peter C. Gareiss
  • Patent number: 8716289
    Abstract: Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or o
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: May 6, 2014
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Mourad Saady, Julien Vache, Corinne Veronique, Philippe Yaiche
  • Patent number: 8703721
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: April 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8703771
    Abstract: The invention provides a new kind of dihydroindene amide compounds of general formula I or their pharmaceutically acceptable salts or prodrug thereof which can be used as protein kinase inhibitor. The invention provides a preparation method of the kind of compounds, the pharmaceutical compositions containing the compounds, the method for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR, using them as protein kinase inhibitor, and their preparation use of drug used for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR.
    Type: Grant
    Filed: December 24, 2009
    Date of Patent: April 22, 2014
    Assignee: Harbin Gloria Pharmaceuticals Co., Ltd.
    Inventors: Xuqing Yang, Long Xue, Juan Luo
  • Patent number: 8697256
    Abstract: A composition comprising a phosphorescent compound, and a compound having a structure containing three or more repeating units having a dipole moment dimension of 1.0 Debye or more connected in series, wherein, based on the total number of dimer structures composed of any two repeating units connected in series contained in the above-described structure, the proportion of the number of dimer structures in which the dimension D2 of the dipole moment of the dimer structure, the dimension D1a of the dipole moment of the first repeating unit constituting the dimer structure and the dimension D1b of the dipole moment of the second repeating unit constituting the dimer structure satisfy a relation represented by the following formula (A): D1a<D2 and D1b<D2??(A) is 50% or more.
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: April 15, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Nobuhiko Akino, Kenta Tanaka, Hideyuki Higashimura
  • Patent number: 8691998
    Abstract: Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: April 8, 2014
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Adam S. Veige, Mathew S. Jeletic, Roxy J. Lowry, Khalil A. Abboud
  • Patent number: 8680271
    Abstract: A process for the preparation of the compound of Formula (I) is described.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: March 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Melodie D. Christensen, Jungchul Kim
  • Patent number: 8680159
    Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
  • Publication number: 20140077130
    Abstract: The instant invention relates to mesogenic media exhibiting a blue phase, comprising one, two or more compounds of formula I-A wherein the parameters are as specified in the text, preferably stabilised by a polymer, and their use in electro-optical light modulation elements and their respective use in displays, as well as to such displays.
    Type: Application
    Filed: September 18, 2013
    Publication date: March 20, 2014
    Applicant: MERCK PATENT GmbH
    Inventors: Michael WITTEK, Norihiko TANAKA, Mila FISCHER, Matthias BREMER, Erdal DURMAZ, Malgorzata RILLICH
  • Patent number: 8674093
    Abstract: The present invention is directed to processes for preparing a pyridyl piperidine compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: March 18, 2014
    Assignees: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Louis-Charles Campeau, John Y. Chung, Danny Gauvreau, Melina Girardin-Rondeau, Gregory Hughes, Kevin M. Maloney, Christophe Mellon, Jeffrey C. Moore, Paul O'Shea, Stephane Ouellet
  • Publication number: 20140070146
    Abstract: The present application relates to a compound of a formula (I), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compound of the formula (I) and to a formulation comprising one or more compounds of the formula (I).
    Type: Application
    Filed: April 12, 2012
    Publication date: March 13, 2014
    Applicant: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Arne Buesing, Christof Pflumm, Teresa Mujica-Fernaud, Philipp Stoessel, Thomas Eberle
  • Publication number: 20140066460
    Abstract: The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
    Type: Application
    Filed: November 7, 2013
    Publication date: March 6, 2014
    Applicant: Targacept, Inc.
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Timothy J. Cuthbertson, Gary Maurice Dull, Craig Harrison Miller, Joseph Pike Mitchener, Julio A. Munoz, Pieter Albert Otten
  • Patent number: 8664230
    Abstract: The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3? OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: March 4, 2014
    Assignee: The Asan Foundation
    Inventors: Gilnam Lee, Chul Soo Lim, Han Won Cho, Jeongbeob Seo, Albert Charles Gyorkos, Suk Young Cho, Eun Kyung Choi, Choung Soo Kim, Jung Jin Hwang
  • Patent number: 8664386
    Abstract: Methods for isolating 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: March 4, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Denise A. Colby, Andrew Anthony Martins, Benjamin James Roberts, Robert William Scott, Nicole S. White
  • Publication number: 20140051611
    Abstract: A crosslinking composition for hydrocarbon gels containing phosphate ester gelling agents comprising a modified imidazoline or pyrimidine including an alkyl group (or unsaturated carbon chain) or of 10 to 22 carbon atoms, a polyamine, and ferric sulfate. The method of making the crosslinking agent features adding the polyamine after reaction of the other ingredients; unique gels formed with the crosslinking agent are particularly effective for LNG at very cold temperatures.
    Type: Application
    Filed: August 14, 2012
    Publication date: February 20, 2014
    Inventors: Larry W. Gatlin, Glen E. Walden, Emest McMillan
  • Patent number: 8653263
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: February 18, 2014
    Assignee: Janssen Pharmaceutica
    Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
  • Patent number: 8653266
    Abstract: A novel process for the preparation of Etravirine comprises the condensing of ethyl cyanoacetate with N-cyanophenylguanidine to obtain an —OH compound of formula (II), which is further converted to a leaving group of formula (III). The compound of formula (III) is optionally protected and brominated to yield compound of formula (IV). The condensation of formula (IV) with 3,5-dimethyl-4-hydroxybenzonitrile yields a compound of formula (VI), and an optional deprotection of the compound of formula (VI) results in Etravirine.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: February 18, 2014
    Assignee: Mylan Laboratories Limited
    Inventors: Vinayak Gore, Choudhari Bharati, Mahesh Hublikar, Prakash Bansode, Sandip Sinore
  • Patent number: 8653097
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k 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: Grant
    Filed: October 15, 2009
    Date of Patent: February 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Lars Van Der Veen, Darryl McConnell, Tobias Wunberg
  • Publication number: 20140034938
    Abstract: The invention provides an organic compound incorporating a specific structure into a pyridine skeleton or a 1,3,5-triazine skeleton and adapting the molecular weight to a specific range, a composition comprising the organic compound and a solvent, organic electroluminescent element comprising a layer that is formed by using the composition, and the uses thereof.
    Type: Application
    Filed: October 7, 2013
    Publication date: February 6, 2014
    Applicant: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Koichi ISHIBASHI, Hideki Gorohmaru, Wataru Shimizu, Tomomi Okamoto
  • Patent number: 8642585
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
  • Publication number: 20140021406
    Abstract: A liquid crystal compound having a high stability to heat, light and so forth, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectric anisotropy, a suitable elastic constant and an excellent solubility in other liquid crystal compounds, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition. The compound is represented by formula (1): wherein, for example, R1 is fluorine or alkyl having 1 to 10 carbons; ring A1 and ring A2 are 1,4-phenylene, or 1,4-phenylene in which at least one of hydrogen is replaced by fluorine; Z1, Z2 and Z3 are a single bond; L1 and L2 are hydrogen or fluorine; X1 is fluorine or —CF3; and m is 1, and n is 0.
    Type: Application
    Filed: July 10, 2013
    Publication date: January 23, 2014
    Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATION
    Inventors: Yasuyuki GOTOH, Keiji KIMURA
  • Publication number: 20140018536
    Abstract: An aromatic amine derivative represented by the following formula (1), wherein at least one of Ar1 to Ar3 is represented by the following formula (2), wherein X1 to X3 are independently a nitrogen atom or CR2, provided that two of X1 to X3 are a nitrogen atom and X1 and X3 are not simultaneously a nitrogen atom
    Type: Application
    Filed: July 15, 2013
    Publication date: January 16, 2014
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventor: Tomoki KATO
  • Patent number: 8628863
    Abstract: Provided is an organic light-emitting device having an optical output with high luminance and high color purity with extremely high efficiency. The organic light-emitting device includes an organic layer between the anode and the cathode, in which one of the anode and the cathode is a transparent electrode or a semi-transparent electrode and at least one layer of the organic layer contains at least one kind of indenopyrene compound having a specific structure.
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: January 14, 2014
    Assignee: Canon Kabushiki Kaisha
    Inventors: Takeshi Sekiguchi, Hiroshi Tanabe, Hiroki Ohrui, Masanori Seki
  • Patent number: 8618288
    Abstract: Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: December 31, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Curt A. Dvorak, Dale A. Rudolph, Brock T. Shireman
  • Patent number: 8614201
    Abstract: Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: December 24, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Didier Jean-Calude Berthelot, Henricus Jacobus Maria Gijsen, Mirko Zaja, Jason Rech, Alec Lebsack, Bryan Branstetter, Wei Xiao, J. Guy Breitenbucher
  • Patent number: 8614221
    Abstract: The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: December 24, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Weiming Fan, Thomas F. N. Haxell, Matthew G. Jenks, Nobuhiko Kawanishi, Shuliang Lee, Hao Liu, Michael J. Malaska, Joseph A. Moore, III, Yoshio Ogino, Yu Onozaki, Bharathi Pandi, Michael R. Peel, Toshihiro Sakamoto, Tony Siu
  • Patent number: 8609839
    Abstract: Camphor-derived compounds are disclosed, which are represented as the following formula (I): wherein R1, R2, R3, and R4 each are defined as described in the specification. In addition, a method for manufacturing the camphor-derived compounds and application thereof are disclosed.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: December 17, 2013
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Bo-Yao Yang
  • Patent number: 8609842
    Abstract: In the present invention, a synthesis method of Imatinib is disclosed, which comprises the following steps: the Imatinib, namely 4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-[4-(3-pyridinyl)-pyrimidin-2-ylamino]-benzami de shown in formula (III), is formed by reacting 4-methyl-N-3-(4-pyridin-3-yl-pyrimidin-2-yl)-1,3-benzenediamine shown in formula (I) with 4-(4-methyl-piperazin-1-methyl)-benzoic ester shown in formula (II), under the action of a base and in a non-protonic organic solvent, in the above generic chemical structural formula, R represents aliphatic alkyl having 1-10 carbon, phenyl, substituted phenyl, benzyl or substituted benzyl. The present invention provides a new synthesis method of Imatinib, which is formed under mild reaction conditions, and is environmentally friendly with a high-yield.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: December 17, 2013
    Assignees: Fujian South Pharmaceutical Co., Ltd., Shanghai Parling Pharmatech Co., Ltd.
    Inventors: Xin Shen, Xiao He, Jidong Yang, Shaohong Wu, Huaxing Zhan
  • Patent number: 8606529
    Abstract: The application relates to methods and systems for analysis of dissociation behavior of nucleic acids and identification of nucleic acids. In one aspect, methods and systems are disclosed for identifying a nucleic acid in a sample including an unknown nucleic acid and for detecting a single nucleotide polymorphism in a nucleic acid in a sample. Methods and systems are also disclosed for identification of a nucleic acid in a biological sample including at least one unknown nucleic acid by fitting denaturation data including measurements of a quantifiable physical change of the sample at a plurality of independent sample property points to a function to determine an intrinsic physical value and to obtain an estimated physical change function, and identifying the nucleic acid in the biological sample by comparing the intrinsic physical value for at least one unknown nucleic acid to an intrinsic physical value for a known nucleic acid.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: December 10, 2013
    Assignee: Canon U.S. Life Sciences, Inc.
    Inventors: Deborah Boles, Kenton C. Hasson, Sami Kanderian
  • Patent number: 8604191
    Abstract: The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-yl)pyrimidine, novel salt forms, and novel polymorphic forms of these salts.
    Type: Grant
    Filed: November 30, 2009
    Date of Patent: December 10, 2013
    Assignee: Targacept, Inc.
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Timothy J. Cuthbertson, Gary Maurice Dull, Craig Harrison Miller, Joseph Pike Mitchener, Jr., Julio A. Munoz, Pieter Albert Otten
  • Patent number: 8598202
    Abstract: Certain aryl-hydroxyethylamino-pyrimidine and triazine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: December 3, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Richard Apodaca, J. Guy Breitenbucher, Alison L. Chambers, Xiaohu Deng, Natalie A. Hawryluk, John M. Keith, Neelakandha S. Mani, Jeffrey E. Merit, Joan M. Pierce, Mark Seierstad, Wei Xiao
  • Patent number: 8598341
    Abstract: 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile is a key intermediate for the preparation of etravirine. The present invention provides a process for preparation of 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile. The present invention also provides a novel process for the preparation of etravirine crystalline form I. The present invention further provides novel crystalline forms of etravirine, processes for their preparation and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: December 3, 2013
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Bandi Vamsi Krishna, Adulla Venkat Narsimha Reddy