Benzene Ring Bonded Directly At The 2- Position Of The Diazole Ring Patents (Class 548/310.7)
  • Publication number: 20100252817
    Abstract: The present invention provides a novel anthracene derivative, a method for preparing the same, and an organic electronic device using the same. The anthracene derivative according to the invention can function alone as a light emitting host, in particular, as a blue host in an organic electronic device. Further, the anthracene derivative according to the invention can also function as a hole injecting or hole transporting material, an electron injecting or electron transporting material, or a light emitting material in an organic electronic device including a light emitting device. Therefore, the organic electronic device according to the present invention shows excellent characteristics in efficiency, drive voltage and stability.
    Type: Application
    Filed: January 25, 2007
    Publication date: October 7, 2010
    Inventors: Kong-Kyeom Kim, Hye-Young Jang, Jae-Chol Lee, Jae-Soon Bae, Dong-Seob Jeong, Tae-Yoon Park
  • Publication number: 20100240580
    Abstract: The invention relates to azoloarine derivatives of formula I wherein R, A, B, D, Y, X, M and W are as defined herein, and their physiologically tolerated salts.
    Type: Application
    Filed: February 18, 2010
    Publication date: September 23, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard ZOLLER, Marc Dietrich VOSS, Hans MATTER, Andreas HERLING, Christophe Philippo, Claudie NAMANE, Juan-Antonio SANCHEZ-ARIAS
  • Publication number: 20100239496
    Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.
    Type: Application
    Filed: March 23, 2010
    Publication date: September 23, 2010
    Applicant: Siemens Medical Solutions USA, Inc.
    Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharia, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
  • Patent number: 7781596
    Abstract: The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the production of said compounds and to their use.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: August 24, 2010
    Assignee: Abbott Laboratories
    Inventors: Wilfried Lubisch, Michael Kock, Thomas Höger
  • Patent number: 7777051
    Abstract: The present invention provides a genus of asymmetric benzimidazole compounds, methods and pharmaceut1cal compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.
    Type: Grant
    Filed: May 12, 2004
    Date of Patent: August 17, 2010
    Assignee: Icagen, Inc.
    Inventors: Xiaodong Wang, Alan Bradley Fulp
  • Publication number: 20100193773
    Abstract: A novel derivative of heterocyclic compound having nitrogen atom with a structure made by bonding special groups to benzimidazole, a material for an organic electroluminescence (EL) device comprising the derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising at least one organic compound layer containing a light emitting layer sandwiched between a pair of electrodes, wherein the device contains the derivative of heterocyclic compound having nitrogen atom. An organic EL device achieving elevation of luminance and of efficiency in light emission even under low driving voltage is obtainable by an employment of the derivative of heterocyclic compound having nitrogen atom for at least one layer composing organic compound layers of the EL device.
    Type: Application
    Filed: April 7, 2010
    Publication date: August 5, 2010
    Applicant: Idemitsu Kosan Co., Ltd,
    Inventors: Hiroshi Yamamoto, Masahide Matsuura, Mineyuki Kubota, Masahiro Kawamura
  • Publication number: 20100190826
    Abstract: Provided is a novel and excellent method for treating and/or preventing benign prostatic hyperplasia, prostate cancer, and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an indole or benzimidazole derivative, where a nitrogen atom of the indole ring or benzimidazole ring is substituted with a phenyl group substituted with COOH, has a potent selective inhibitory activity against 17?HSD type 5 and may become an agent for treating and/or an agent for preventing a disease associated with 17?HSD type 5, such as benign prostatic hyperplasia, prostate cancer and the like, without accompanying adverse effects due to a decrease in testosterone; and the present invention has thus been completed.
    Type: Application
    Filed: July 23, 2008
    Publication date: July 29, 2010
    Inventors: Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano, Akio Kamikawa, Kentaro Enjo, Takashi Furutani
  • Publication number: 20100187505
    Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.
    Type: Application
    Filed: April 29, 2008
    Publication date: July 29, 2010
    Inventors: Philipp Stoessel, Arne Buesing, Holger Heil
  • Publication number: 20100179147
    Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.
    Type: Application
    Filed: December 10, 2009
    Publication date: July 15, 2010
    Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo
  • Publication number: 20100120802
    Abstract: Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
    Type: Application
    Filed: January 15, 2010
    Publication date: May 13, 2010
    Inventors: Francesco MAKOVEC, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpiliq, Simona Zanzola, Lucio Claudio Rovati
  • Patent number: 7709518
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Grant
    Filed: September 21, 2005
    Date of Patent: May 4, 2010
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Jun Jiang, Hao Li, David James, Dinesh Chimmanamada, Christopher Borella, Lijun Sun, Yu Xie, Mats Holmqvist, Jerome Mahiou, Zhi Qiang Xia
  • Patent number: 7687639
    Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: March 30, 2010
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael K. Ameriks, Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher
  • Publication number: 20100071769
    Abstract: Disclosed is a novel fluorene derivative and an organic electronic device using the same. The organic electronic device has excellent efficiency, driving voltage, and a lifespan.
    Type: Application
    Filed: December 6, 2007
    Publication date: March 25, 2010
    Inventors: Jae-Soon Bae, Dong-Hoon Lee, Dae-Woong Lee, Sung-Ku Hong, Hyun Nam, Chang-Hwan Kim
  • Publication number: 20100063122
    Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
    Type: Application
    Filed: November 15, 2007
    Publication date: March 11, 2010
    Inventors: Anders Klarskov Peterson, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
  • Publication number: 20100039027
    Abstract: An organic electroluminescent device including, a cathode, an anode, and at least an emitting layer and an electron transporting layer between the cathode and the anode, the emitting layer including a host compound and a fluoranthene compound, the electron transporting layer including a compound represented by (A)u-(B)v wherein A is a group containing an aromatic hydrocarbon group having 3 or more carbon rings, B is a heterocyclic group which may be substituted, and u and v are each an integer of 1 to 6.
    Type: Application
    Filed: February 19, 2008
    Publication date: February 18, 2010
    Applicant: IDEMITSU KOSAN CO., LTD
    Inventors: Yoriyuki Takashima, Masakazu Funahashi, Takashi Arakane, Yumiko Mizuki, Hiroshi Yamamoto, Chishio Hosokawa, Kiyoshi Ikeda
  • Publication number: 20100016372
    Abstract: Novel compounds of the formula I (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R, Q, W, X and Z have the meanings indicated in Patent Claim 1, are suitable as antidiabetics.
    Type: Application
    Filed: January 28, 2008
    Publication date: January 21, 2010
    Applicant: Merck Patent GmbH
    Inventors: Lars Thore Burgdorf, Bertram Cezanne, Markus Klein, Rolf Gericke, Christos Tsaklakidis, Werner Mederski, Norbert Beier
  • Patent number: 7595406
    Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: September 29, 2009
    Assignee: Abbott Laboratories Inc.
    Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong, Vincent L. Giranda, Viraj B. Gandhi
  • Publication number: 20090239915
    Abstract: The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, in which X, R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.
    Type: Application
    Filed: March 27, 2009
    Publication date: September 24, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard ZOLLER, Hartmut STROBEL, David William WILL, Paulus WOHLFART
  • Publication number: 20090197889
    Abstract: This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated.
    Type: Application
    Filed: January 30, 2009
    Publication date: August 6, 2009
    Applicant: SPELMAN COLLEGE
    Inventor: Leyte L. Winfield
  • Publication number: 20090174312
    Abstract: The present invention provides a novel tetraphenylnaphthalene derivative, and an organic light emitting device using the same.
    Type: Application
    Filed: March 9, 2007
    Publication date: July 9, 2009
    Inventors: Yeon-Hwan Kim, Dong-Hoon Lee, Hye-Young Jang, Sung-Kil Hong, Sung-Jin Yeo, Kong-Kyeom Kim, Dong-Seob Jeong
  • Publication number: 20090170921
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R1-R7 are as disclosed in the specification.
    Type: Application
    Filed: January 13, 2005
    Publication date: July 2, 2009
    Inventors: Marc Gerspacher, Sven Weiler
  • Publication number: 20090149649
    Abstract: The present invention provides an aromatic heterocyclic compound represented by Formula 1 below, an organic light-emitting diode including an organic layer comprising the aromatic heterocyclic compound, and a method of manufacturing the organic light-emitting diode: wherein A, Ar1, Ar2, n, m, and k are as described in the detailed description of the present invention.
    Type: Application
    Filed: April 30, 2008
    Publication date: June 11, 2009
    Inventors: Dong-woo Shin, Myeong-suk Kim, Tae-woo Lee, Yu-jin Kim, Eun-sil Han, Woon-jung Paek, Yu-ri Choi, Byoung-ki Choi, Tae-yong Noh, O-hyun Kwon, Haa-jin Yang, Young-mok Son
  • Patent number: 7479502
    Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
    Type: Grant
    Filed: December 3, 2003
    Date of Patent: January 20, 2009
    Assignee: Pharmacyclics, Inc.
    Inventors: Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, Steven M. Torkelson, Kieron E. Wesson, Wendy B. Young
  • Patent number: 7462724
    Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).
    Type: Grant
    Filed: November 15, 2006
    Date of Patent: December 9, 2008
    Assignee: Abbott Laboratories
    Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong, Vincent L. Giranda, Viraj B. Gandhi
  • Publication number: 20080284322
    Abstract: A novel nitrogen-containing heterocyclic compound having a specific structure and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer which comprises a single layer or a plurality of layers comprising at least a light emitting layer and is disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the above nitrogen-containing heterocyclic derivative singly or as a component of a mixture. The organic electroluminescence device exhibits a great luminance of emitted light and a great efficiency of light emission even under application of a low voltage.
    Type: Application
    Filed: July 7, 2006
    Publication date: November 20, 2008
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Chishio Hosokawa, Hiroshi Yamamoto, Takashi Arakane
  • Publication number: 20080275250
    Abstract: The present invention relates to novel inhibitors or Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
    Type: Application
    Filed: June 2, 2005
    Publication date: November 6, 2008
    Applicant: PHARMACYCLICS, INC.
    Inventors: Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader, Kieron Wesson
  • Publication number: 20080247992
    Abstract: Disclosed are compounds, compositions and methods for treating Flaviviridae family virus infections.
    Type: Application
    Filed: October 24, 2007
    Publication date: October 9, 2008
    Inventors: Christopher D. Roberts, Dong-Fang Shi, Ronald C. Griffith
  • Patent number: 7414138
    Abstract: The present invention relates to 1,3-benzoxazole or benzodiazole UV-A sunscreens and to compositions, in particular topical compositions, containing the above UV-A sunscreens.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: August 19, 2008
    Assignee: DSM IP Assets B.V.
    Inventor: Ulrich Huber
  • Publication number: 20080100207
    Abstract: Provided are a cyclopentaphenanthrene-based compound and an organoelectroluminescent device employing the same. The cyclopentaphenanthrene-based compound is easy to prepare and excellent in solubility, color purity, color stability, and thermal stability. The cyclopentaphenanthrene-based compound is useful as a material for forming an organic layer, in particular, an emitting layer, in an organoelectroluminescent device, and as an organic dye or an electronic material such as a nonlinear optical material.
    Type: Application
    Filed: July 18, 2007
    Publication date: May 1, 2008
    Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son
  • Publication number: 20080079356
    Abstract: A cyclopentaphenanthrene-based compound is easy to prepare and excellent in solubility, color purity, and color stability. The cyclopentaphenanthrene-based compound is useful as a material for forming an organic layer, in particular, an emitting layer, in an organoelectroluminescent device, and as an organic dye or an electronic material such as a nonlinear optical material.
    Type: Application
    Filed: July 18, 2007
    Publication date: April 3, 2008
    Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son, Byoung-Ki Choi, O-Hyun Kwon, Myeong-Suk Kim
  • Patent number: 7345075
    Abstract: Benzimidazoles of general formula I and the use of benzimidazole derivatives for the production of pharmaceutical agents for treatment and prophylaxis of diseases that are associated with a microglia activation are described.
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: March 18, 2008
    Assignee: Schering Aktiengesellschaft
    Inventors: Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning
  • Patent number: 7304085
    Abstract: Disclosed are compounds, compositions and methods for treating Flaviviridae family virus infections.
    Type: Grant
    Filed: June 4, 2004
    Date of Patent: December 4, 2007
    Assignee: Genelabs Technologies, Inc.
    Inventors: Christopher D. Roberts, Dong-Fang Shi, Ronald C. Griffith
  • Patent number: 7273939
    Abstract: Provided are methods for preparing a compound of Formula I: where the method comprises the steps of: contacting a compound of Formula II: with 1,3,5-benzene-tricarbonyl chloride in the presence of a polar aprotic solvent to form an amide adduct; and subsequently condensing the amide with a proximate anilino group present in the adduct in the presence of a condensing agent to form a compound of Formula I wherein R1, R2, Ar, m, p, and t are as defined in the specification.
    Type: Grant
    Filed: December 15, 2005
    Date of Patent: September 25, 2007
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Mark A. Guidry, Steven W. Shuey, William J. Delaney
  • Patent number: 7271261
    Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
    Type: Grant
    Filed: October 18, 2002
    Date of Patent: September 18, 2007
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher, Liming Huang, Alice Lee, Kelly J. McClure
  • Patent number: 7244847
    Abstract: The present invention is directed to novel benzimidazoles according to representative structures I and II, and their derivatives that possess antibacterial activity. This invention is also directed to compositions including the benzimidazole derivatives, and methods for using the same.
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: July 17, 2007
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Eric E. Swayze, Yun He, Punit P. Seth, Elizabeth Anne Jefferson
  • Patent number: 7179832
    Abstract: Novel compounds having hydroxybenzoimidazole carboxylic amide are useful for inhibiting glycogen synthase kinase 3?(GSK-3?).
    Type: Grant
    Filed: January 20, 2004
    Date of Patent: February 20, 2007
    Assignees: Crystalgenomics, Inc., Yuyu Inc.
    Inventors: Joong Myung Cho, Seonggu Ro, Tae Gyu Lee, Kyung Joo Lee, Dongkyu Shin, Young-Lan Hyun, Seung Chul Lee, Jin Hwan Kim, Young Ho Jeon
  • Patent number: 7132440
    Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
    Type: Grant
    Filed: April 16, 2004
    Date of Patent: November 7, 2006
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Michael K. Ameriks, Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher
  • Patent number: 6919366
    Abstract: This invention relates to a family of benzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy, asthma, or any diseases where IgE is pathogenic.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: July 19, 2005
    Assignee: Avanir Pharmaceuticals
    Inventors: Jagadish C. Sircar, Mark L. Richards, Michael G. Campbell, Michael W. Major
  • Patent number: 6888005
    Abstract: A process for the preparation of 2-phenylbenzimidazole-5-sulphonic acid, characterized in that 3,4-diaminobenzenesulphonic acid is reacted at a pH between 4 and 7 in aqueous solution with 0.9 to 1.5 mol of benzaldehyde per mole of 3,4-diaminobenzenesulphonic acid and with 1.0 to 3.0 mol of SO2 per mole of 3,4-diaminobenzenesulphonic acid, or an agent which comprises 1.0 to 3.0 mol of SO2 per mole of 3.4-diaminobenzenesulphonic acid, is described.
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: May 3, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Günter Rauchschwalbe, Herbert Emde, Wolfram Kissener, Klaus-Christian Paetz
  • Patent number: 6878469
    Abstract: Novel materials for electron injection/transportation and emitting layers can greatly improve the stability of an organic electroluminescent display. Electroluminescent displays incorporating these materials produce blue light at low voltage levels. These novel organic materials include compounds in which 1 to 2 imidazole functional groups are introduced in the 2 or 2,6-site of 9,10 substituted anthracene. An organic electroluminescent display with an organic compound layer of these materials has high efficiency, thermal stability, operationally stability and maintains driving voltage before and after operation.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: April 12, 2005
    Assignee: LG Chem, Ltd.
    Inventors: Seok-Hee Yoon, Jae-Soon Bae, Youn-Gu Lee, Sung-Gap Im, Jae-Chol Lee, Ji-Eun Kim, Kong-Kyeom Kim, Se-Hwan Son, Young-Kyu Han
  • Patent number: 6855714
    Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: February 15, 2005
    Assignee: Schering Aktiengesellschaft
    Inventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Herbert Schneider, Bernd Elger
  • Publication number: 20040214857
    Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
    Type: Application
    Filed: April 16, 2004
    Publication date: October 28, 2004
    Inventors: Michael K. Ameriks, Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher
  • Publication number: 20040102458
    Abstract: Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with an affinity which is greater than ADP and different from the ansamycin antibiotics for at least one species of the HSP90 family. Moreover, these small molecules can be designed to be soluble in aqueous media, thus providing a further advantage over the use of ansamycin antibiotics. Pharmaceutical compositions can be formulated containing a pharmaceutically acceptable carrier and a molecule that includes a binding moiety which binds to the N-terminal pocket of at least one member of the HSP90 family of proteins. Such binding moieties were found to have antiproliferative activity against tumor cells which are dependent on proteins requiring chaperones of the HSP90 family for their function.
    Type: Application
    Filed: May 1, 2003
    Publication date: May 27, 2004
    Inventors: Gabriela Chiosis, Neal Rosen
  • Publication number: 20040059126
    Abstract: Described herein is a process for the preparation of 3,4-diaminobenzenesulphonic acid, characterized in that 1,2-diaminobenzene is reacted with anhydrous sulphuric acid which optionally comprises SO3 in up to stoichiometric amount, at a temperature in the range from 100 to 160° C. with stirring for a reaction time of from 1 to 20 hours; water or ice is added to the reaction mixture, optionally with cooling, up to a sulphuric acid concentration in the range from 30 to 75% by weight, based on the total mixture; the 3,4-diaminobenzenesulphonic acid precipitated out of the reaction mixture is filtered off, optionally washed with dilute sulphuric acid and worked up.
    Type: Application
    Filed: September 16, 2003
    Publication date: March 25, 2004
    Inventors: Gunter Rauchschwalbe, Herbert Emde, Wolfram Kissener
  • Publication number: 20040059125
    Abstract: A process for the preparation of 2-phenylbenzimidazole-5-sulphonic acid, characterized in that 3,4-diaminobenzenesulphonic acid is reacted at a pH between 4 and 7 in aqueous solution with 0.9 to 1.5 mol of benzaldehyde per mole of 3,4-diaminobenzenesulphonic acid and with 1.0 to 3.0 mol of SO2 per mole of 3,4-diaminobenzenesulphonic acid, or an agent which comprises 1.0 to 3.0 mol of SO2 per mole of 3.4-diaminobenzenesulphonic acid, is described.
    Type: Application
    Filed: September 16, 2003
    Publication date: March 25, 2004
    Inventors: Gunter Rauchschwalbe, Herbert Emde, Wolfram Kibener, Klaus-Christian Paetz
  • Patent number: 6696437
    Abstract: The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: February 24, 2004
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Uta Holzenkamp, Sabine Schult, Reinhold Mueller
  • Patent number: 6660742
    Abstract: The present invention relates to novel achiral seco-analogues of DNA minor groove and sequence-selective alkylating agents (+)-CC1065 and the duocarmycins, depicted as general class I, II, III, IV and V: wherein X is a good leaving group, such as a chloride, a bromide, an iodide, a mesylate, a tosylate, an acetate, a quaternary ammonium moiety, a mercaptan, an alkylsulfoxyl, or an alkylsulfonyl group, preferably either a chloride, a bromide, or an iodide group. R1 is a suitable minor groove binding agent to enhance the interactions of the achiral seco-cyclopropaneindole (Cl) or an achiral seco-duocarmycin with specific sequences of DNA.
    Type: Grant
    Filed: September 19, 2001
    Date of Patent: December 9, 2003
    Assignee: Taiho Pharmaceutical Co. Ltd.
    Inventor: Moses Lee
  • Publication number: 20030216583
    Abstract: An accelerated process for preparing an O-methyl phenol comprising reacting a phenol with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to another aspect, the invention provides an accelerated process for preparing an N-methyl heteroaromatic compound comprising reacting an NH-containing heteroaromatic compound with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to an additional aspect, the invention provides an accelerated process for preparing a methylated aminophenol comprising reacting an aminophenol having at least one N—H with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine.
    Type: Application
    Filed: June 12, 2003
    Publication date: November 20, 2003
    Inventors: Wen-Chung Shieh, Steven Dell
  • Patent number: 6649642
    Abstract: Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: November 18, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Eugene Richard Hickey, Weimin Liu, David S. Thomson
  • Publication number: 20030191160
    Abstract: The present invention provides compositions and methods for the treatment of HIV infection. In particular, the present invention provides non-nucleoside inhibitors of reverse transcriptase (RT), as well as methods to treat HIV infection using these non-nucleoside inhibitors of RT. In preferred embodiments, the present invention provides a novel class of substituted benzimidazoles, effective in the inhibition of human immunodeficiency virus (HIV) RT.
    Type: Application
    Filed: April 9, 2002
    Publication date: October 9, 2003
    Inventors: Christopher J. Michejda, Marshall Morningstar, Thomas Roth