Quinoxalines (including Hydrogenated) Patents (Class 544/353)
  • Publication number: 20110198574
    Abstract: The present invention provides a novel organic compound having excellent heat resistance. By using the novel organic compound, a light-emitting device and an electronic device having excellent heat resistance can be provided. A quinoxaline derivative represented by the general formula (1) is provided. Since the quinoxaline derivative represented by the general formula (1) has excellent heat resistance, when it is used for a light-emitting element, a light-emitting device using the light-emitting element also have excellent heat resistance. Further, electronic devices having excellent heat resistance can be provided.
    Type: Application
    Filed: April 25, 2011
    Publication date: August 18, 2011
    Inventors: Masakazu Egawa, Nobuharu Ohsawa
  • Publication number: 20110201607
    Abstract: The present invention is directed to fused heterocyclic compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: October 13, 2009
    Publication date: August 18, 2011
    Inventors: Scott D. Kuduk, Christina Ng Di Marco
  • Publication number: 20110195963
    Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.
    Type: Application
    Filed: April 30, 2008
    Publication date: August 11, 2011
    Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
  • Patent number: 7994170
    Abstract: The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.
    Type: Grant
    Filed: October 12, 2009
    Date of Patent: August 9, 2011
    Assignee: Novartis AG
    Inventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
  • Patent number: 7993761
    Abstract: The present invention provides a quinoxaline derivative represented by a general formula (G1). In the formula, ?1 and ?2 each independently represent an arylene group which has 13 or less carbon atoms forming a ring; Ar represents an aryl group which has 13 or less carbon atoms forming a ring; R1 and R6 each independently represent any of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an aryl group which has 13 or less carbon atoms forming a ring; and R2 to R5 and R7 to R10 each independently represent any of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, or a substituted or unsubstituted biphenyl group.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: August 9, 2011
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Harue Osaka, Nobuharu Ohsawa, Sachiko Kawakami
  • Patent number: 7994169
    Abstract: The present invention relates to 3,4-diaminopyridine derivatives of formula (I) wherein R1 and R2 are, independently of each other, electron donors, wherein R2 is optionally H; and R3, R4, R5, and R6 are, independently of each other, H, optionally substituted straight-chain or branched alkyl, alkenyl, alkynyl, alkoxyl, or aryl, wherein R3 and/or R4 together with R5 and/or R6, optionally define a ring; processes for their preparation, and their use as catalysts.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: August 9, 2011
    Assignee: Bayer MaterialScience AG
    Inventors: Hendrik Zipse, Ingmar Held
  • Publication number: 20110183988
    Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line.
    Type: Application
    Filed: December 21, 2010
    Publication date: July 28, 2011
    Inventors: Prabha N. Ibrahim, Guoxian Wu, Jack Lin, Wayne Spevak, Hanna Cho, Todd Ewing, Chao Zhang
  • Publication number: 20110183976
    Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.
    Type: Application
    Filed: June 25, 2009
    Publication date: July 28, 2011
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Publication number: 20110178089
    Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: January 13, 2011
    Publication date: July 21, 2011
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ulmer
  • Publication number: 20110178091
    Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.
    Type: Application
    Filed: September 23, 2009
    Publication date: July 21, 2011
    Applicant: GREEN CROSS CORPORATION
    Inventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
  • Patent number: 7981925
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: July 19, 2011
    Assignee: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20110160210
    Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.
    Type: Application
    Filed: March 8, 2011
    Publication date: June 30, 2011
    Applicant: ALCON, INC.
    Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shapard, Mark R. Hellberg, Abbot F. Clark, Peter G. Klimko
  • Publication number: 20110147720
    Abstract: The present invention relates to novel quinoxaline derivatives and their use in an organic light-emitting diode device. The quinoxaline derivative is of luminescence and rigidity, can increase glass transition temperature (Tg) and has better thermal stability, and thus can be used as a hole transporting layer, a host or guest of an emitting layer or an electron transporting layer of an organic light-emitting diode device.
    Type: Application
    Filed: June 8, 2010
    Publication date: June 23, 2011
    Inventors: Min Sheng Chen, Yue Lin Du, Hsiao Chan Liu
  • Publication number: 20110152271
    Abstract: The invention provides compositions and methods for treating nasal congestion through ophthalmic delivery. The provided compositions and methods utilize low concentrations of selective ?-2 adrenergic receptor agonists. The compositions preferably include brimonidine.
    Type: Application
    Filed: December 17, 2010
    Publication date: June 23, 2011
    Inventor: Gerald Horn
  • Patent number: 7960384
    Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound of the formula: wherein the substituents are as defined herein.
    Type: Grant
    Filed: March 27, 2007
    Date of Patent: June 14, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun Feng, Stephen L. Gwaltney, Michael B. Wallace, Zhiyuan Zhang
  • Publication number: 20110127513
    Abstract: The present invention provides a novel nitrogen-containing heterocyclic derivative and an organic electronic device using the same. The organic electronic device according to the present invention has excellent properties in terms of efficiency, driving voltage, and a life span.
    Type: Application
    Filed: November 3, 2009
    Publication date: June 2, 2011
    Applicant: LG CHEM, LTD.
    Inventors: Dong-Hoon Lee, Tae-Yoon Park, Jae-Soon Bae, Hyun Nam, Jun-Gi Jang, Sung-Kil Hong
  • Publication number: 20110121721
    Abstract: The present invention provides light-emitting element having long lifetime, and light-emitting devices and electronic devices having long lifetime. A light-emitting element comprises a first layer and a second layer including a light-emitting substance between a first electrode and a second electrode. The first layer includes a first organic compound and a second organic compound, the first layer is formed between the second layer and the second electrode, the first layer includes the first organic compound more than the second organic compound, the first organic compound is an organic compound having an electron-transporting property, the second organic compound is an organic compound having an electron-trapping property, an energy gap of the second organic compound is larger than that of the light-emitting substance; and a voltage is applied such that a potential of the first electrode is higher than that of the second electrode, so that the light-emitting layer emits light.
    Type: Application
    Filed: January 21, 2011
    Publication date: May 26, 2011
    Inventors: Tsunenori Suzuki, Satoshi Seo, Sachiko Kawakami
  • Patent number: 7947833
    Abstract: Certain methods that are useful in the preparation of amidophenyl-sulfonylamino-quinoxaline compounds are disclosed. The compounds are of the class of quinoxaline sulfonamides and constitute CCK2 receptor modulators, useful in the treatment of gastrointestinal diseases.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: May 24, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Xiaohu Deng, Jimmy T. Liang, Neelakandha Mani, Chennagiri R. Pandit
  • Publication number: 20110118270
    Abstract: The present invention relates to compounds of Formula (I) below, to their pharmaceutically acceptable salts and to their isomers or mixtures of isomers: HetAr—X—CHR1R2 (I) in which: -HetAr represents a group chosen from: —X represents a linear, saturated or unsaturated, hydrocarbon-based chain comprising from 8 to 22 carbon atoms, optionally interrupted by an —NH— or —NH—CO— group, —R1 represents a hydrogen atom or an —OH, —O(C1-C6)alkyl, —OCO((C1-C6)alkyl), —OSO2((C1-C6)alkyl) or —OSO3H group, and —R2 represents a hydrogen atom or a (C2-C6)alkynyl, (C2-C6)alkenyl or (C3-C6)cycloalkyl group. The present invention also relates to a process for preparing the compounds of Formula (I), and also to the use thereof, especially in the treatment of neurodegenerative diseases.
    Type: Application
    Filed: July 20, 2009
    Publication date: May 19, 2011
    Inventor: Fanny Schmidt
  • Publication number: 20110112077
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: January 15, 2009
    Publication date: May 12, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. KUDUK, Ronald K, CHANG
  • Publication number: 20110112100
    Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HCV replication.
    Type: Application
    Filed: August 25, 2010
    Publication date: May 12, 2011
    Inventors: Jared Bruce John Milbank, David Cameron Pryde, Thien Duc Tran
  • Publication number: 20110112058
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Application
    Filed: October 6, 2010
    Publication date: May 12, 2011
    Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: MEYYAPPAN MUTHUPPALANIAPPAN, Srikant Viswanadha, Kanthikiran V. Varanasi, Gayatri S. Merikapudi, Swaroop Kumar V.S. Vakkalanka
  • Publication number: 20110105329
    Abstract: Substituted quinolinones of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one compound of the formula I to act on plants, their seed and/or their habitat.
    Type: Application
    Filed: October 29, 2010
    Publication date: May 5, 2011
    Applicant: BASF SE
    Inventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree van der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska, Anja Simon, Richard Roger Evans
  • Publication number: 20110092504
    Abstract: The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein Q, X1, X2, R1 and Z are as defined herein.
    Type: Application
    Filed: May 29, 2009
    Publication date: April 21, 2011
    Inventors: Yunxin Y. Bo, Shon Booker, Marian Bryan, Holly L. Deak, Longbin Liu, Kristin Andrews, Nobuko Nishimura, Mark H. Norman, Kathleen Panter, Laurie Schenkel, Aaron C. Siegmund, Nuria A. Tamayo, Kevin Yang
  • Patent number: 7927720
    Abstract: An object is to provide a novel quinoxaline derivative. Another object is to provide a light-emitting element with low driving voltage. Another object is to provide a light-emitting element with low power consumption. Another object is to provide a light-emitting device and an electronic device with low power consumption by using such a light-emitting element. A quinoxaline derivative which has a structure in which at least one of carbon at a 2-position and carbon at a 3-position of quinoxaline, and carbon of 1,3,4-oxadiazole ring are bound via an arylene group is provided.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: April 19, 2011
    Assignee: Semiconductor Energy laboratory Co., Ltd.
    Inventors: Hiroko Nomura, Hiroshi Kadoma, Sachiko Kawakami, Satoko Shitagaki, Satoshi Seo
  • Publication number: 20110081316
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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 1, 2010
    Publication date: April 7, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: David Messersmith, Alex Aronov, David J. Lauffer, Anne-Laure Grillot, Robert J. Davies
  • Patent number: 7914706
    Abstract: The present invention relates to charge transport compositions. The invention further relates to electronic devices in which there is at least one active layer comprising such charge transport compositions.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: March 29, 2011
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Daniel David LeCloux, Mark A. Guidry, Norman Herron, Nora Sabina Radu, Eric Maurice Smith, Ying Wang
  • Publication number: 20110071149
    Abstract: The present invention relates to methods of modulating (for example, inhibiting) activity of JAK3, comprising contacting the JAK3 with a compound of Formula I: or pharmaceutically acceptable salt thereof, wherein constituent members are provided hereinwith. The present invention further provides novel compounds and compositions as well as their methods of preparation and use of the same as JAK3 inhibitors in the treatment of JAK3-associated diseases including, for example, inflammatory and autoimmune disorders.
    Type: Application
    Filed: February 11, 2010
    Publication date: March 24, 2011
    Applicants: REACTION BIOLOGY CORP., SYNERGA LIMITED
    Inventors: Haiching MA, Sorin Vasile FILIP
  • Publication number: 20110059964
    Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.
    Type: Application
    Filed: February 3, 2010
    Publication date: March 10, 2011
    Applicant: sanofi-aventis
    Inventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
  • Patent number: 7901792
    Abstract: A quinoxaline derivative expressed by the general formula (1) is provided. (Each of R1 to R12 represents one of a hydrogen atom, a halogen atom, an alkyl group, an alkoxyl group, an acyl group, a dialkyl amino group, a diarylamino group, a substituted or unsubstituted vinyl group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocycle group. Ar1 represents one of a substituted or unsubstituted biphenyl group and a substituted or unsubstituted terphenyl group, and Ar2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, a substituted or unsubstituted terphenyl group, and a substituted or unsubstituted monocyclic heterocycle group.
    Type: Grant
    Filed: September 8, 2006
    Date of Patent: March 8, 2011
    Assignee: Semiconductor Energy laboratory Co., Ltd.
    Inventors: Masakazu Egawa, Sachiko Kawakami, Nobuharu Ohsawa, Hideko Inoue, Satoshi Seo, Ryoji Nomura
  • Publication number: 20110049495
    Abstract: A quinoxaline derivative represented by Formula (I) or (II) is provided. In Formula (I) or (II), R1 and R2 are, independently, hydrogen, halogen, methyl, ethyl, propyl, butyl, aryl or heteroaryl, for example phenyl, furyl, thienyl, pyridyl, pyrimidyl, benzothiazolyl or benzoimidazolyl. The invention also provides an organic light-emitting diode including the quinoxaline derivative.
    Type: Application
    Filed: August 27, 2010
    Publication date: March 3, 2011
    Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE
    Inventors: Heh-Lung Huang, Teng-Chih Chao, Hao-Chun Lee
  • Publication number: 20110046113
    Abstract: It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1): In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(?O) or NR11; and D is a group represented by the following general formula (4) or (6). In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). —(CR18R19)m3— Or —(CR20R21)m4-z-(CR22R23)m5??(7) z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26.
    Type: Application
    Filed: October 12, 2010
    Publication date: February 24, 2011
    Applicant: KUREHA CORPORATION
    Inventors: Toru YAMAZAKI, Shigeyuki KIKUMOTO, Masahiro ONO, Atsushi SAITOU, Haruka TAKAHASHI, Sei KUMAKURA, Kunitaka HIROSE, Mikiro YANAKA, Yoshiyuki TAKEMURA, Shigeru SUZUKI, Ryo MATSUI
  • Publication number: 20110046133
    Abstract: The present invention provides compounds of the following structure; A-L1-B-C-D that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: October 17, 2007
    Publication date: February 24, 2011
    Inventors: Moo Je Sung, Gary Mark Coppola, Taeyoung Yoon, Thomas A. Gilmore
  • Publication number: 20110039864
    Abstract: Disclosed herein is an alpha-adrenergic compound having a structure. Therapeutic methods, compositions, and medicaments for treating pain are also disclosed herein.
    Type: Application
    Filed: August 14, 2008
    Publication date: February 17, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
  • Patent number: 7888359
    Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: February 15, 2011
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Christian Hubschwerlen, Rueedi Georg, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 7888358
    Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: February 15, 2011
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Birgitte L. Eriksen, Elsebet Østergaard Nielsen, Jørgen Scheel-Krüger, Gunnar M. Olsen
  • Publication number: 20110028482
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Application
    Filed: May 18, 2010
    Publication date: February 3, 2011
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Patent number: 7875879
    Abstract: A substrate including a semiconductor layer, where characteristics of an element can be evaluated with high reliability, and an evaluating method thereof are provided. A substrate including a semiconductor layer of the invention has a closed-loop circuit in which an antenna coil and a semiconductor element are connected in series, and a surface of an area over which the circuit is formed is covered with an insulating film. By using such a circuit, a contactless inspection can be carried out. Further, a ring oscillator can be substituted for the closed-loop circuit.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: January 25, 2011
    Assignee: Semiconductor Energy laboratory Co., Ltd.
    Inventors: Tsunenori Suzuki, Satoshi Seo, Sachiko Kawakami
  • Patent number: 7875618
    Abstract: The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: January 25, 2011
    Assignees: Wyeth, elbion GmbH
    Inventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Norbert Höfgen, Hans Stange, Rudolf Schindler, Ute Egerland, Barbara Langen
  • Publication number: 20110006295
    Abstract: A compound of the formula R1(CR3?CR4)nAr(CR4?CR3)nR2 wherein: n is 0 or 1; Ar represents aryl or heteroaryl having 1-5 aromatic rings which may be chain or fused or a combination of chain and fused, which may be substituted with alkoxy, fluoro, fluoroalkyl or cyano and which in the case of a 5-membered ring nitrogen heteroatom may be N-substituted with aryl or substituted aryl optionally further substituted with alkoxy, fluoro, fluoroalkyl or cyano; R1 and R2 independently represent aryl or nitrogen, oxygen or sulphur-containing heteroaryl having two to four fused aromatic rings one of which may be 5-membered and optionally substituted by aryl or heteroaryl having 1-5 chain or fused aromatic rings which may be further substituted with alkoxy, fluoro, fluoroalkyl or cyano; and R3 and R4 independently represent hydrogen, methyl, ethyl or benzyl.
    Type: Application
    Filed: February 24, 2009
    Publication date: January 13, 2011
    Inventors: Poopathy Kathirgamanathan, Sivagnanasundram Surendrakumar
  • Publication number: 20110009391
    Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.
    Type: Application
    Filed: July 26, 2010
    Publication date: January 13, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Alain Jean BRAUN, Olivier CRESPIN, Claudie NAMANE, Eric NICOLAI, Francois PACQUET, Cecile PASCAL, Christophe PHILIPPO, Olivier VENIER
  • Publication number: 20110003823
    Abstract: The invention provides compositions and methods for treating diseases and conditions, including systemic diseases and conditions, through an intravenous administration of a selective ?-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for ?-2 over ?-1 adrenergic receptors. The amounts of the selective ?-2 adrenergic receptor agonists are substantially lower than the amounts normally used to cause sedation. The compositions preferably include dexmedetomidine.
    Type: Application
    Filed: May 26, 2010
    Publication date: January 6, 2011
    Inventor: Gerald Horn
  • Publication number: 20100331326
    Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.
    Type: Application
    Filed: June 28, 2010
    Publication date: December 30, 2010
    Inventors: Mark G. BOCK, Christoph GAUL, Venkateshwar Rao GUMMADI, Saumitra SENGUPTA
  • Publication number: 20100331335
    Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 30, 2010
    Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
  • Patent number: 7858799
    Abstract: An ionic organic compound having a repeating unit of formula (I) can be synthesized easily from a readily available organic compound through a small number of reaction steps, can be produced without any purification technique such as chromatography, and can be used in a quite small amount for gelation of water or an ionic liquid without any other auxiliary solvent: [-(A-B-C)n-]•m(X)??(I) wherein A represents a group having a quaternary ammonium cation which is formed from a heterocyclic compound having at least one nitrogen atom; B represents a functional group, which may have a substituent, selected from amide, urea, urethane and peptide groups; C represents a divalent hydrocarbon group, which may have a substituent, capable of linking between A and B; X represents an anion; n represents the number of repeating units; m represents the total number of anions; and n and m are the same integer.
    Type: Grant
    Filed: January 30, 2006
    Date of Patent: December 28, 2010
    Assignee: National Institute of Advanced Industrial Science and Technology
    Inventors: Masaru Yoshida, Nagatoshi Koumura, Nobuyuki Tamaoki, Hajime Kawanami, Hajime Matsumoto, Said Kazaoui, Nobutsugu Minami
  • Publication number: 20100324030
    Abstract: The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.
    Type: Application
    Filed: April 11, 2008
    Publication date: December 23, 2010
    Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische Chemie
    Inventors: Glenn Dale, Sabine Pierau, Michael W. Cappi, Christopher Gray, Christian Hubschwerlen, Jean P. Surivet, Cornelia Zumbrunn
  • Patent number: 7855292
    Abstract: Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.
    Type: Grant
    Filed: November 20, 2007
    Date of Patent: December 21, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Brett Allison, Victor K. Phuong, Marna C. W. Pippel, Michael H. Rabinowitz, Hariharan Venkatesan
  • Publication number: 20100316605
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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: June 9, 2010
    Publication date: December 16, 2010
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Kevin Michael Cottrell, Alex Aronov, Robert J. Davies, Jon H. Come, David Messersmith
  • Publication number: 20100317646
    Abstract: A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; —O—C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C4-7-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-h
    Type: Application
    Filed: March 19, 2010
    Publication date: December 16, 2010
    Applicant: Medical Research Council Technology
    Inventors: Edward Giles Mciver, Ela Smiljanic, Denise Jamilla Harding, Joanne Hough
  • Publication number: 20100317667
    Abstract: Provided herein are 1-aryl or 1-heteroarylsubstituted phenanthrene diketo acid compounds. These compounds comprise a ?-carboline ring structure substituted at C1 with an aryl or heteroaryl moiety and individually substituted at C3-C8 and N9 with a C1-C4 alkyl, a C1-C4 alkoxy, a C1-C4 alkoxyphenyl, halogen, thiol, alkylthiol, sulfonyl, sulfomainde, amide, substituted amide, ester, nitrile, OH, amino, substituted amine, haloalkyl, haloalkoxy, acyl, or a hydrogen. Also provided are methods for inhibiting proliferation of a cancer cell or for treating a cell proliferative disease by contacting the cancer cell or tumor comprising the same with the compounds provided herein or by administering the compounds to a subject with a cell proliferative disease.
    Type: Application
    Filed: April 26, 2010
    Publication date: December 16, 2010
    Inventors: John K. Buolamwini, Shivaputra Patil, James K. Addo, D. Parker Suttle, Ruiwen Zhang, Zhengxiang Zhu, Sharma Horrick