Benzene Ring Bonded Directly At The 2- Position Of The Diazole Ring Patents (Class 548/310.7)
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Publication number: 20100252817Abstract: 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: ApplicationFiled: January 25, 2007Publication date: October 7, 2010Inventors: Kong-Kyeom Kim, Hye-Young Jang, Jae-Chol Lee, Jae-Soon Bae, Dong-Seob Jeong, Tae-Yoon Park
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Publication number: 20100240580Abstract: 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: ApplicationFiled: February 18, 2010Publication date: September 23, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Marc Dietrich VOSS, Hans MATTER, Andreas HERLING, Christophe Philippo, Claudie NAMANE, Juan-Antonio SANCHEZ-ARIAS
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Publication number: 20100239496Abstract: 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: ApplicationFiled: March 23, 2010Publication date: September 23, 2010Applicant: 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
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Patent number: 7781596Abstract: 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: GrantFiled: October 28, 1999Date of Patent: August 24, 2010Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Michael Kock, Thomas Höger
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Patent number: 7777051Abstract: 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: GrantFiled: May 12, 2004Date of Patent: August 17, 2010Assignee: Icagen, Inc.Inventors: Xiaodong Wang, Alan Bradley Fulp
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Publication number: 20100193773Abstract: 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: ApplicationFiled: April 7, 2010Publication date: August 5, 2010Applicant: Idemitsu Kosan Co., Ltd,Inventors: Hiroshi Yamamoto, Masahide Matsuura, Mineyuki Kubota, Masahiro Kawamura
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Publication number: 20100190826Abstract: 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: ApplicationFiled: July 23, 2008Publication date: July 29, 2010Inventors: Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano, Akio Kamikawa, Kentaro Enjo, Takashi Furutani
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Publication number: 20100187505Abstract: 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: ApplicationFiled: April 29, 2008Publication date: July 29, 2010Inventors: Philipp Stoessel, Arne Buesing, Holger Heil
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Publication number: 20100179147Abstract: 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: ApplicationFiled: December 10, 2009Publication date: July 15, 2010Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo
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Publication number: 20100120802Abstract: 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: ApplicationFiled: January 15, 2010Publication date: May 13, 2010Inventors: Francesco MAKOVEC, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpiliq, Simona Zanzola, Lucio Claudio Rovati
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Patent number: 7709518Abstract: 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: GrantFiled: September 21, 2005Date of Patent: May 4, 2010Assignee: 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
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Patent number: 7687639Abstract: 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: GrantFiled: June 30, 2006Date of Patent: March 30, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Michael K. Ameriks, Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher
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Publication number: 20100071769Abstract: 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: ApplicationFiled: December 6, 2007Publication date: March 25, 2010Inventors: Jae-Soon Bae, Dong-Hoon Lee, Dae-Woong Lee, Sung-Ku Hong, Hyun Nam, Chang-Hwan Kim
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Publication number: 20100063122Abstract: 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: ApplicationFiled: November 15, 2007Publication date: March 11, 2010Inventors: Anders Klarskov Peterson, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
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Publication number: 20100039027Abstract: 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: ApplicationFiled: February 19, 2008Publication date: February 18, 2010Applicant: IDEMITSU KOSAN CO., LTDInventors: Yoriyuki Takashima, Masakazu Funahashi, Takashi Arakane, Yumiko Mizuki, Hiroshi Yamamoto, Chishio Hosokawa, Kiyoshi Ikeda
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Publication number: 20100016372Abstract: 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: ApplicationFiled: January 28, 2008Publication date: January 21, 2010Applicant: Merck Patent GmbHInventors: Lars Thore Burgdorf, Bertram Cezanne, Markus Klein, Rolf Gericke, Christos Tsaklakidis, Werner Mederski, Norbert Beier
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Patent number: 7595406Abstract: 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: GrantFiled: July 30, 2007Date of Patent: September 29, 2009Assignee: Abbott Laboratories Inc.Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong, Vincent L. Giranda, Viraj B. Gandhi
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Publication number: 20090239915Abstract: 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: ApplicationFiled: March 27, 2009Publication date: September 24, 2009Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Hartmut STROBEL, David William WILL, Paulus WOHLFART
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Publication number: 20090197889Abstract: 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: ApplicationFiled: January 30, 2009Publication date: August 6, 2009Applicant: SPELMAN COLLEGEInventor: Leyte L. Winfield
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Publication number: 20090174312Abstract: The present invention provides a novel tetraphenylnaphthalene derivative, and an organic light emitting device using the same.Type: ApplicationFiled: March 9, 2007Publication date: July 9, 2009Inventors: Yeon-Hwan Kim, Dong-Hoon Lee, Hye-Young Jang, Sung-Kil Hong, Sung-Jin Yeo, Kong-Kyeom Kim, Dong-Seob Jeong
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Publication number: 20090170921Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R1-R7 are as disclosed in the specification.Type: ApplicationFiled: January 13, 2005Publication date: July 2, 2009Inventors: Marc Gerspacher, Sven Weiler
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Publication number: 20090149649Abstract: 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: ApplicationFiled: April 30, 2008Publication date: June 11, 2009Inventors: 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
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Patent number: 7479502Abstract: 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: GrantFiled: December 3, 2003Date of Patent: January 20, 2009Assignee: Pharmacyclics, Inc.Inventors: Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, Steven M. Torkelson, Kieron E. Wesson, Wendy B. Young
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Patent number: 7462724Abstract: 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: GrantFiled: November 15, 2006Date of Patent: December 9, 2008Assignee: Abbott LaboratoriesInventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong, Vincent L. Giranda, Viraj B. Gandhi
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Publication number: 20080284322Abstract: 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: ApplicationFiled: July 7, 2006Publication date: November 20, 2008Applicant: Idemitsu Kosan Co., Ltd.Inventors: Chishio Hosokawa, Hiroshi Yamamoto, Takashi Arakane
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Publication number: 20080275250Abstract: 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: ApplicationFiled: June 2, 2005Publication date: November 6, 2008Applicant: PHARMACYCLICS, INC.Inventors: Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader, Kieron Wesson
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Publication number: 20080247992Abstract: Disclosed are compounds, compositions and methods for treating Flaviviridae family virus infections.Type: ApplicationFiled: October 24, 2007Publication date: October 9, 2008Inventors: Christopher D. Roberts, Dong-Fang Shi, Ronald C. Griffith
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Patent number: 7414138Abstract: 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: GrantFiled: April 8, 2003Date of Patent: August 19, 2008Assignee: DSM IP Assets B.V.Inventor: Ulrich Huber
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Publication number: 20080100207Abstract: 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: ApplicationFiled: July 18, 2007Publication date: May 1, 2008Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son
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Publication number: 20080079356Abstract: 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: ApplicationFiled: July 18, 2007Publication date: April 3, 2008Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son, Byoung-Ki Choi, O-Hyun Kwon, Myeong-Suk Kim
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Patent number: 7345075Abstract: 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: GrantFiled: December 16, 2005Date of Patent: March 18, 2008Assignee: Schering AktiengesellschaftInventors: Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning
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Patent number: 7304085Abstract: Disclosed are compounds, compositions and methods for treating Flaviviridae family virus infections.Type: GrantFiled: June 4, 2004Date of Patent: December 4, 2007Assignee: Genelabs Technologies, Inc.Inventors: Christopher D. Roberts, Dong-Fang Shi, Ronald C. Griffith
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Patent number: 7273939Abstract: 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: GrantFiled: December 15, 2005Date of Patent: September 25, 2007Assignee: E. I. du Pont de Nemours and CompanyInventors: Mark A. Guidry, Steven W. Shuey, William J. Delaney
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Patent number: 7271261Abstract: 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: GrantFiled: October 18, 2002Date of Patent: September 18, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher, Liming Huang, Alice Lee, Kelly J. McClure
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Patent number: 7244847Abstract: 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: GrantFiled: February 6, 2002Date of Patent: July 17, 2007Assignee: Isis Pharmaceuticals, Inc.Inventors: Eric E. Swayze, Yun He, Punit P. Seth, Elizabeth Anne Jefferson
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Patent number: 7179832Abstract: Novel compounds having hydroxybenzoimidazole carboxylic amide are useful for inhibiting glycogen synthase kinase 3?(GSK-3?).Type: GrantFiled: January 20, 2004Date of Patent: February 20, 2007Assignees: 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
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Patent number: 7132440Abstract: 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: GrantFiled: April 16, 2004Date of Patent: November 7, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Michael K. Ameriks, Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher
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Patent number: 6919366Abstract: 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: GrantFiled: October 16, 2001Date of Patent: July 19, 2005Assignee: Avanir PharmaceuticalsInventors: Jagadish C. Sircar, Mark L. Richards, Michael G. Campbell, Michael W. Major
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Patent number: 6888005Abstract: 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: GrantFiled: September 16, 2003Date of Patent: May 3, 2005Assignee: Bayer AktiengesellschaftInventors: Günter Rauchschwalbe, Herbert Emde, Wolfram Kissener, Klaus-Christian Paetz
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Patent number: 6878469Abstract: 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: GrantFiled: January 16, 2003Date of Patent: April 12, 2005Assignee: 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
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Patent number: 6855714Abstract: 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: GrantFiled: July 5, 2002Date of Patent: February 15, 2005Assignee: Schering AktiengesellschaftInventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Herbert Schneider, Bernd Elger
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Publication number: 20040214857Abstract: 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: ApplicationFiled: April 16, 2004Publication date: October 28, 2004Inventors: Michael K. Ameriks, Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher
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Publication number: 20040102458Abstract: 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: ApplicationFiled: May 1, 2003Publication date: May 27, 2004Inventors: Gabriela Chiosis, Neal Rosen
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Publication number: 20040059126Abstract: 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: ApplicationFiled: September 16, 2003Publication date: March 25, 2004Inventors: Gunter Rauchschwalbe, Herbert Emde, Wolfram Kissener
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Publication number: 20040059125Abstract: 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: ApplicationFiled: September 16, 2003Publication date: March 25, 2004Inventors: Gunter Rauchschwalbe, Herbert Emde, Wolfram Kibener, Klaus-Christian Paetz
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Patent number: 6696437Abstract: 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: GrantFiled: March 25, 2002Date of Patent: February 24, 2004Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Uta Holzenkamp, Sabine Schult, Reinhold Mueller
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Patent number: 6660742Abstract: 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: GrantFiled: September 19, 2001Date of Patent: December 9, 2003Assignee: Taiho Pharmaceutical Co. Ltd.Inventor: Moses Lee
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Publication number: 20030216583Abstract: 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: ApplicationFiled: June 12, 2003Publication date: November 20, 2003Inventors: Wen-Chung Shieh, Steven Dell
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Patent number: 6649642Abstract: 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: GrantFiled: October 23, 2002Date of Patent: November 18, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Eugene Richard Hickey, Weimin Liu, David S. Thomson
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Publication number: 20030191160Abstract: 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: ApplicationFiled: April 9, 2002Publication date: October 9, 2003Inventors: Christopher J. Michejda, Marshall Morningstar, Thomas Roth