1,3-diazines Patents (Class 544/242)
  • Patent number: 8389734
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: October 10, 2008
    Date of Patent: March 5, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Weichuan Caroline Chen, Paul Krenitsky, Andreas Termin, Dean Wilson
  • Publication number: 20130048964
    Abstract: A light-emitting element includes an EL layer between a pair of electrodes. The EL layer contains a first compound and a second compound. The first compound is a phosphorescent iridium metal complex having a LUMO level of greater than or equal to ?3.5 eV and less than or equal to ?2.5 eV, and the second compound is an organic compound having a pyrimidine skeleton. The light-emitting element includes an EL layer between a pair of electrodes. The EL layer contains a first compound and a second compound. The first compound is a phosphorescent iridium metal complex having a diazine skeleton, and the second compound is an organic compound having a pyrimidine skeleton.
    Type: Application
    Filed: August 21, 2012
    Publication date: February 28, 2013
    Inventors: Kyoko Takeda, Harue Osaka, Satoko Shitagaki, Nobuharu Ohsawa, Satoshi Seo, Hiromi Seo
  • Patent number: 8377935
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: February 19, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Patrick René Angibaud, Laurence Françoise Bernadette Marconnet-Decrane, Sven Franciscus Anna Van Brandt, Isabelle Noëlle Constance Pilatte
  • Patent number: 8367680
    Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.
    Type: Grant
    Filed: March 27, 2009
    Date of Patent: February 5, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Helen E. Blackwell, Matthew D. Bowman, Joseph R. Stringer
  • Publication number: 20130029988
    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: January 20, 2011
    Publication date: January 31, 2013
    Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Dirk Winkler, Frederick Brookfield, Paula C. De Aguiar Pena
  • Patent number: 8362002
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: January 29, 2013
    Assignee: Exelixis, Inc.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 8354408
    Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: January 15, 2013
    Assignee: YM Biosciences Australia Pty Ltd
    Inventors: David Gerard Bourke, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Marcel Robert Kling, Tracy Leah Nero
  • Patent number: 8349833
    Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: January 8, 2013
    Assignee: Cerenis Therapeutics Holding SA
    Inventors: Daniela Carmen Oniciu, Jean-Louis Henri Dasseux, Ronald Barbaras, Valery Kochubey, Dmitry Kovalsky, Oleg Gennadievich Rodin, Otto Geoffroy, Anna Rzepiela
  • Patent number: 8343640
    Abstract: A material for an organic photoelectric device includes a compound represented by the following Formula 1:
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: January 1, 2013
    Assignee: Cheil Industries, Inc.
    Inventors: Nam-Soo Kim, Eun-Sun Yu, Young-Hoon Kim, Mi-Young Chae
  • Publication number: 20120319044
    Abstract: Ionic mesogenic compounds of formula (I) can be used to form liquid crystal displays, such as ferroelectric liquid crystal displays, having enhanced anti-image sticking properties. The mesogenic compounds may contain a cationic group such as an ammonium or phosphonium group bonded to an alkyl chain that is terminally bonded to a para-substituted pyrimidyl benzene moiety. The counterion can be an organic or inorganic anion. The compounds can be used either as dopants in art ferroelectric liquid crystal compositions to reduce image sticking, or can be used as the primary or predominant component of a liquid crystal display system. Additional compounds, devices, and methods are disclosed.
    Type: Application
    Filed: June 14, 2011
    Publication date: December 20, 2012
    Inventors: Yongqiang Zhang, Su Yang
  • Publication number: 20120319099
    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 electro-luminescence device emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.
    Type: Application
    Filed: August 31, 2012
    Publication date: December 20, 2012
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro IWAKUMA, Hiroshi Yamamoto, Yoshio Hironaka, Hidetsugu Ikeda, Chishio Hosokawa, Seiji Tomita, Takashi Arakane
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Patent number: 8334292
    Abstract: Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: December 18, 2012
    Assignee: Cystic Fibrosis Foundation Therapeutics, Inc.
    Inventor: Phoebe Chiang
  • Patent number: 8329691
    Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
    Type: Grant
    Filed: October 14, 2008
    Date of Patent: December 11, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Tawada
  • Patent number: 8329902
    Abstract: The present invention relates to an optically pure compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, a process for preparing the optically pure compound of formula (I), and use of the optically pure compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof as a medicament, in particular as a medicament for the treatment and prevention of type B hepatitis.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: December 11, 2012
    Assignee: Beijing Molecule Science And Technology Co., Ltd.
    Inventors: Song Li, Guangqiang Xia, Guoming Zhao, Lili Wang, Zhibing Zheng, Yunde Xie, Wu Zhong, Junhai Xiao, Xingzhou Li, Hao Cui
  • Patent number: 8324403
    Abstract: There are provided an organic having both excellent hole transporting property and satisfactory electron transporting and showing excellent durability against electric oxidation/reduction and a high triplet excitation level, and a charge transporting material and an organic electroluminescent device each using the organic compound.
    Type: Grant
    Filed: December 9, 2005
    Date of Patent: December 4, 2012
    Assignees: Pioneer Corporation, Mitsubishi Chemical Corporation
    Inventors: Masayoshi Yabe, Hideki Sato
  • Publication number: 20120298975
    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: Application
    Filed: May 31, 2012
    Publication date: November 29, 2012
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro IWAKUMA, Hiroshi Yamamoto, Yoshio Hironaka, Hidetsugu Ikeda, Chishio Hosokawa, Seiji Tomita, Takashi Arakane
  • Patent number: 8318759
    Abstract: The present invention relates to a compounds of formula I wherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: November 27, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
  • Patent number: 8318749
    Abstract: The present invention relates to a compounds of formula I wherein R1, R2, R3, R4, R5, and n are as defined herein and to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: November 27, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Publication number: 20120295923
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: January 19, 2011
    Publication date: November 22, 2012
    Inventors: Christopher William Am Ende, Benjamin Adam Fish, Douglas Scott Johnson, Ricardo Lira, Christopher John O'Donnell, Martin Youngjin Pettersson, Corey Michael Stiff
  • Publication number: 20120287354
    Abstract: The present invention relates to an electro-optical light modulation element and to electro-optical displays and display systems, such as television screens and computer monitors, containing elements of this type. The light modulation elements according to the invention contain a mesogenic modulation medium which is in the isotropic phase during operation of the light modulation elements and are particularly distinguished by very short response times in addition to good contrast and low viewing-angle dependence. The mesogenic modulation media used in the electro-optical light modulation elements are likewise a subject-matter of the present invention.
    Type: Application
    Filed: June 7, 2012
    Publication date: November 15, 2012
    Applicant: MERCK Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Michael HECKMEIER, Achim Götz
  • Patent number: 8309726
    Abstract: The present invention provides novel anthranilic acid derivative useful as potential anticancer agent. More particularly, the present invention relates novel anthranilic acid derivative of general formula (8), R?=alkyl-2-methoxyphenyl piperazine or benzyl; R=2-methoxyphenyl, piperazine, 2-pyridyl piperazine-1-yl, 2-pyrimidyl piperazine-1-yl, 4-quinazolinyl piperazine-1-yl, 9H-9-fluorenylamine, 4-{(2{amino-5-(methoxy)-4-[(phenylmethyl)oxy]phenyl}carbonyl)-hexahydro-1-pyrazinyl], and [(4[2-amino-4-(benzyloxy)-5-methoxybenzoyl]aminophenyl)-sulfonyl]-4-benzamine; X?H or pyrazine-2-carbonyl. The present invention also provides a process for the preparation of novel anthranilic acid derivative of general formula (8), which is useful as potential anticancer agent.
    Type: Grant
    Filed: March 13, 2008
    Date of Patent: November 13, 2012
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Bandari Rajendra Prasad
  • Publication number: 20120277325
    Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers that when m is 0, n is 1; when m is 1, n is 0 or 1; or when m is 2, n is 0; wherein (CH)m and (CH)n are each independently optionally substituted with a substituent selected from the group consisting of methyl and ethyl; wherein X is selected from the group consisting of N, O, and S; and wherein R1 and R2 each independently represent H or a hydrocarbon group, or R1 and R2 together represent a fused ring or a ring system, with the proviso that when R1 is H, R2 is not H.
    Type: Application
    Filed: July 3, 2012
    Publication date: November 1, 2012
    Inventors: Robert P. Belko, Paul D. Jones, Anthony T. Levorse, JR., Michael G. Monteleone, Anubhav P.S. Narula, Franc T. Schiet
  • Patent number: 8299065
    Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic ra
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: October 30, 2012
    Assignee: Biota Europe Ltd.
    Inventors: David John Haydon, Lloyd George Czaplewski
  • Publication number: 20120267620
    Abstract: A compound for an organic photoelectric device, an organic photoelectric device including the same, and a display device including the organic photoelectric device, the compound being represented by the following Chemical Formula 1:
    Type: Application
    Filed: June 27, 2012
    Publication date: October 25, 2012
    Inventors: Soo-Hyun MIN, Eun-Sun YU, Ho-Jae LEE, Hyung-Sun KIM, Young-Hoon KIM, Eui-Su KANG, Nam-Heon LEE, Young-Sung PARK, Mi-Young CHAE
  • Patent number: 8293756
    Abstract: A pharmaceutical composition, especially capsules, comprising granules containing nilotinib or a salt thereof with at least one pharmaceutically acceptable excipient. The granules may be produced by a wet granulation process.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: October 23, 2012
    Assignee: Novartis AG
    Inventor: Nathalie Bruneau
  • Patent number: 8283383
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: October 9, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Patent number: 8268809
    Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.
    Type: Grant
    Filed: September 5, 2007
    Date of Patent: September 18, 2012
    Assignees: Emory University, M.D. Anderson Cancer Center
    Inventors: Daniel Kalman, William Bornmann
  • Patent number: 8269001
    Abstract: A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis.
    Type: Grant
    Filed: October 4, 2006
    Date of Patent: September 18, 2012
    Assignee: Lek Pharmaceuticals d.d.
    Inventor: Zdenko Casar
  • Publication number: 20120225895
    Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.
    Type: Application
    Filed: November 9, 2010
    Publication date: September 6, 2012
    Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
  • Patent number: 8252925
    Abstract: The present invention relates to a process for preparing 3-phenyl(thio)uracils and -dithiouracils of the formula I where the variables are each as defined in the description, and also intermediates for their preparation.
    Type: Grant
    Filed: July 13, 2005
    Date of Patent: August 28, 2012
    Assignee: BASF Aktiengesellschaft
    Inventors: Sandra Löhr, Joachim Gebhardt, Guido Mayer, Michael Keil, Thomas Schmidt, Bernd Wolf
  • Patent number: 8247422
    Abstract: The invention relates to the use of a compound of the formula (I), or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for use in modulating an immune or inflammatory response: wherein: Z=O or S; n=1-3; R3=—CO2R8, —C(O)SR8, —C(O)NHR8, —C(S)OR8, —C(S)SR8, —C(S)NHR8, —C(NH)SR8 or —C(NH)NHR8, wherein R8 is —H or alkyl; R4=—H, —CH2R5 or —CH2CH2R5, wherein R5 independently has one of the meanings of R3; B=—NR2—, —CH2NR2—, —CH2CH2NR2—, —CH2CHR7— or —CH2O—, wherein R2 is H or a C1-3 alkyl, alkenyl or alkynyl group, and R7 is H or a C1-3 alkyl or alkoxy group; A=wherein R1=—NH2 or —OH, C and D are each, independently, a 5- or 6-membered, substituted or unsubstituted, aromatic or non-aromatic ring which may also contain one or more heteroatoms, and C is connected to group B in any available position.
    Type: Grant
    Filed: February 13, 2008
    Date of Patent: August 21, 2012
    Inventor: Dan Stoicescu
  • Publication number: 20120208820
    Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
    Type: Application
    Filed: January 31, 2012
    Publication date: August 16, 2012
    Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
  • Publication number: 20120207698
    Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions.
    Type: Application
    Filed: March 27, 2012
    Publication date: August 16, 2012
    Inventors: Robert P. Belko, Anthony T. Levorse, JR., Anubhav P.S. Narula, Michael G. Monteleone
  • Patent number: 8242260
    Abstract: The present invention provides compounds of Formula I or II: wherein R1, R1b, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds of Formula (I) or (II) and pharmaceutical compositions thereof are useful for the treatment of B-Raf-associated diseases.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: August 14, 2012
    Assignee: Novartis AG
    Inventors: Abran Q. Costales, Shenlin Huang, Jeff Xianming Jin, Zuosheng Liu, Sabina Pecchi, Daniel Poon, John Tellew, Qiong Zhang
  • Patent number: 8236950
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: August 7, 2012
    Assignee: Abbott Laboratories
    Inventors: David A. Betebenner, Clarence J. Maring, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
  • Patent number: 8211929
    Abstract: The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O—R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: July 3, 2012
    Assignee: Exelixis, Inc.
    Inventors: Jeff Chen, Lisa Esther Dalrymple Meyr, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Mohamed Abdulkader Ibrahim, James W. Leahy, Gary Lee Lewis, Grace Mann, Larry W. Mann, Robin Tammie Noguchi, Brian Hugh Ridgway, Joan Cruz Sangalang, Kevin Luke Schnepp, Xian Shi, Craig Stacy Takeuchi, Matthew Alan Williams, John Nuss, Atwood K. Cheung
  • Patent number: 8212048
    Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: July 3, 2012
    Assignees: Sumitomo Chemical Company, Limited, Osaka University
    Inventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
  • Patent number: 8207172
    Abstract: The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: June 26, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Chengzhi Zhang, Jacques Dumas, Qingming Zhu, Roger Smith, Qingjie Liu, Sharad Verma, Jason Duquette, Qian Zhao, Dongping Fan, Georgiy Bondar, Philip Coish
  • Patent number: 8207333
    Abstract: A new process for preparing pure amorphous rosuvastatin calcium, substantially free of impurities, is disclosed. A process comprising hydrolysing a C1 to C5 alkyl ester of rosuvastatin, preferably methyl rosuvastatin or tert-butyl rosuvastatin, with a base, e.g. sodium hydroxide, in the presence of an aprotic solvent, preferably tetrahydrofuran and N,N-dimethyl acetamide, or in the presence of a mixture of an aprotic solvent and water, to obtain a solution of rosuvastatin salt, which may be converted to another rosuvastatin salt using another cation, e.g. with calcium cation to obtain rosuvastatin calcium. Rosuvastatin amine salts may be obtained as well. In another preferred aspect of the invention rosuvastatin free acid may be converted to various rosuvastatin salts, e.g. to rosuvastatin calcium, rosuvastatin sodium or various rosuvastatin amine salts, including rosuvastatin solvates, e.g. rosuvastatin calcium hydrate.
    Type: Grant
    Filed: June 22, 2006
    Date of Patent: June 26, 2012
    Assignee: Lek Pharmaceuticals d. d.
    Inventors: Zdenko Casar, Marko Zlicar
  • Publication number: 20120142915
    Abstract: This disclosure concerns a protected cyclopropylboronic acid comprising a substituted cyclopropyl group and a boronic ester group having a protecting group. The protecting group is an N-methyliminodiacetic acid (MIDA) group or MIDA-based group.
    Type: Application
    Filed: December 1, 2011
    Publication date: June 7, 2012
    Inventors: Matthew Duncton, Rajinder Singh
  • Patent number: 8193197
    Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: June 5, 2012
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Ankush Argade, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Kin Tso, Somasekhar Bhamidipati
  • Patent number: 8193207
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: June 5, 2012
    Assignee: Incyte Corporation
    Inventors: Jincong Zhuo, Ding-Quan Qian, Wenqing Yao
  • Patent number: 8188095
    Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: May 29, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
  • Publication number: 20120126221
    Abstract: A charge-transporting material contains a compound represented by the following formula (1) in an organic layer, in which the contents of specific halogen-containing compounds are 0.1% or less to the compound represented by formula (1). In formula (1), each of A1 and A2 independently represents N, —CH or —CR; R represents a substituent; L represents a single bond, an arylene group, a cycloalkylene group or an aromatic heterocyclic group; each of R1 to R5 independently represents a substituent; each of n1, n2 and n3 independently represents an integer of 0 to 4; each of n4 and n5 independently represents an integer of 0 to 5; and each of p and q independently represents an integer of 1 to 4.
    Type: Application
    Filed: July 27, 2010
    Publication date: May 24, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Tetsu Kitamura, Toru Watanabe, Toshihiro Ise, Hiroo Takizawa
  • Patent number: 8178540
    Abstract: The present invention relates to novel pyrimidylmethyl-sulfonamide compounds and to their N-oxides, their agriculturally acceptable salts and their veterinarily acceptable salts and also to agricultural compositions comprising at least one such compound as active component, and also to their use for controlling harmful fungi. The present invention also relates to a method for controlling arthropod pests.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: May 15, 2012
    Assignee: BASF SE
    Inventors: Jan Klaas Lohmann, Wassilios Grammenos, Michael Puhl, Jochen Dietz, Bernd Müller, Joachim Rheinheimer, Jens Renner, Marianna Vrettou, Sarah Ulmschneider, Thomas Grote
  • Patent number: 8180572
    Abstract: The present invention relates to methods and systems for the analysis of the dissociation behavior of nucleic acids and the identification of nucleic acids. In one aspect, methods and systems are disclosed for resolving a denaturation curve of a sample containing a first and second nucleic acid into a resolved denaturation curve for the first nucleic acid and a resolved denuration curve for the second nucleic acid.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: May 15, 2012
    Assignee: Canon U.S. Life Sciences, Inc.
    Inventor: Weidong Cao
  • Patent number: 8158607
    Abstract: The disclosure herein relates to a new Lamivudine polymorphic form, methods of making the same, and pharmaceutical formulations thereof. A (?) cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one in the form of monoclinic crystals has characteristic powder X-ray diffractogram, as disclosed herein, is disclosed along with a process for preparation of the same. A pharmaceutical composition in solid dosage unit form comprising a therapeutically effective amount of a new Lamivudine polymorphic form in combination with a pharmaceutically acceptable carrier is also disclosed along with a pharmaceutical composition useful for treating HIV infections in humans.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: April 17, 2012
    Assignee: Lupin Limited
    Inventors: Girij Pal Singh, Dhananjai Srivastava, Manmeet Brijkishore Saini, Pritesh Rameshbhai Upadhyay
  • Patent number: 8158631
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: April 17, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Ryan Craig Schoenfeld, Francisco Xavier Talamas
  • Patent number: 8153652
    Abstract: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.
    Type: Grant
    Filed: April 12, 2010
    Date of Patent: April 10, 2012
    Assignee: Affinium Pharmaceuticals, Inc.
    Inventors: Walter J. Burgess, Dalia R. Jakas, William F. Huffman, William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas