The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System (e.g., Benzofuranyl-benzimidazole, Etc.) Patents (Class 548/305.1)
-
Publication number: 20130090342Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.Type: ApplicationFiled: June 16, 2011Publication date: April 11, 2013Applicant: NOVARTIS AGInventors: Frederic Berst, Pascal Furet, Andreas Marzinzik
-
Publication number: 20130085150Abstract: Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: September 24, 2012Publication date: April 4, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Oswy Z. Pereira, John Maxwell, Youssef L. Bennani, Sanjoy Kumar Das, Laval Chan Chun Kong, Jagadeeswar T. Reddy, Simon Giroux, Kevin M. Cottrell, Mark A. Morris
-
Publication number: 20130075705Abstract: A carbazole compound which can be used for a transport layer or as a host material or a light-emitting material of a light-emitting element is provided. Specifically, a carbazole compound which makes it possible to obtain a light-emitting element having good characteristics when used in a light-emitting element emitting blue phosphorescence is provided. In the carbazole compound, the 9-position of one carbazole, the 9-position of the other carbazole, and the 1-position of a benzimidazole skeleton are bonded to the 1-position, the 3-position, and the 5-position of benzene.Type: ApplicationFiled: September 12, 2012Publication date: March 28, 2013Applicant: Semiconductor Energy Laboratory Co., Ltd.Inventors: Takako TAKASU, Nobuharu OHSAWA
-
Publication number: 20130065896Abstract: Provided is a novel compound which shows an antagonistic effect against T-type calcium channels, and is useful as a pharmaceutical product. A compound represented by general formula (I), and a pharmaceutical agent containing the same, are disclosed: wherein n represents the number of nitrogen atoms contained in the 6-membered fused aromatic ring, and is 0, 1 or 2; p represents the number of nitrogen atoms contained in the 6-membered aromatic ring, and is 0 or 1; X represents an oxygen atom, —SO2— or —N(R9)—; and R1 to R5 each represents a hydrogen atom or other substituents.Type: ApplicationFiled: May 24, 2011Publication date: March 14, 2013Applicant: TOA Eiyo Ltd.Inventors: Hidekazu Masaki, Hiroshi Takasugi, Tomoyuki Nagayama, Ryutaro Shimono, Yujiro Uchino, Koichi Takayanagi
-
Patent number: 8394803Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: GrantFiled: November 6, 2006Date of Patent: March 12, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, David Deininger, Joseph Drumm, Anne-Laure Grillot, Arnaud LeTiran, Yusheng Liao, Emanuele Perola, Steven Ronkin, Dean Stamos, Tiansheng Wang
-
Publication number: 20130053403Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: ApplicationFiled: April 25, 2011Publication date: February 28, 2013Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
-
Publication number: 20130048975Abstract: The present invention relates to a material for an organic electroluminescent device, including a phenanthrocarbazole-based compound having a specific structure, and an organic electroluminescent device including the same. More specifically, the phenanthrocarbazole-based compound is applied as a material for a phosphorescent and fluorescent organic electroluminescent device, thereby providing an organic light emitting device with improved light emitting efficiency, luminance, thermal stability, driving voltage, lifetime and the like.Type: ApplicationFiled: May 6, 2011Publication date: February 28, 2013Applicant: Doosan CorporationInventors: Jin-Seok Hong, Eun Jung Lee, Shin Han Kim, Kyoung-Soo Kim
-
Patent number: 8383662Abstract: Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds.Type: GrantFiled: October 1, 2010Date of Patent: February 26, 2013Assignees: National Chiao Tung University, National Taiwan UniversityInventors: Chung-Ming Sun, Min-Liang Kuo, Yufeng Jane Tseng
-
Patent number: 8383830Abstract: Cyanine compounds having the general formula I for staining biological samples, wherein R1, R2, X, Y, A1 and A2 are as defined in the specification. These kinds of compounds may show good light illumination stability, have a maximum absorption peak around 640 nm that may not change as a function of ambient temperature, have rapidly increased fluorescence intensity upon binding to nucleic acids to form compound/nucleic acid complexes, and have a light spectrum in the near-infrared region, thereby effectively reducing interference from background fluorescence and increasing the accuracy of the detection when used as a staining agent for nucleic acids in a flow cytometer. The compounds provided can be used as a staining agent for erythroblasts in the blood.Type: GrantFiled: October 28, 2009Date of Patent: February 26, 2013Assignee: Shenzhen Mindray Bio-Medical Electronics Co., LtdInventors: Jianhui Shao, Bing Xu
-
Publication number: 20130045935Abstract: This invention relates to bis-flavonoid compounds of formula Flavonoid-Linker-Y-Linker-Flavonoid, their synthesis and use for inhibiting multidrug resistance in chemotherapy and protozoan infection.Type: ApplicationFiled: May 3, 2011Publication date: February 21, 2013Inventors: Tak-Hang Chan, Larry Ming-Cheung Chow, Kin-Fai Chan, Iris Lai King Wong
-
Publication number: 20130041005Abstract: The present invention relates to a compound of general formula (I), and to a pharmaceutical composition comprising a compound of general formula (I) or esters or salts thereof, in association with at least one pharmaceutically acceptable vehicle; and to the use thereof for inhibiting the Neuropilin pathways in the treatment of cancer and of angiogenic diseases.Type: ApplicationFiled: October 19, 2012Publication date: February 14, 2013Applicant: TRAGEX PHARMAInventor: TRAGEX PHARMA
-
Publication number: 20130032787Abstract: A heterocyclic compound represented by Formula 1 or Formula 2 below, and an organic light-emitting device including the heterocyclic compound. The organic light-emitting device may include an organic layer containing the heterocyclic compound, and thus may have a low driving voltage, a high-emission efficiency, and long lifespan characteristics. wherein R1 to R12, Ar1, Ar2, A, B, a, and b are defined as in the specification.Type: ApplicationFiled: November 25, 2011Publication date: February 7, 2013Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jin-O Lim, Sang-Hyun Han, Se-Jin Cho, Jong-Hyuk Lee
-
Publication number: 20130035337Abstract: The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound having the general formula (I): wherein R1 represents a C1-C6 alkyl group, a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; R2 represents a C1-C6 alkyl group; R3 represents a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; Q represents a group represented by the formula ?CH— or a nitrogen atom; and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, and the like, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: March 13, 2012Publication date: February 7, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kousei Shimada, Yoshiyuki Onishi, Makoto Mori, Eri Tokumaru
-
Publication number: 20130023525Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: ApplicationFiled: April 24, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
-
Publication number: 20130018039Abstract: Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.Type: ApplicationFiled: March 31, 2011Publication date: January 17, 2013Inventors: Vera Q. Bodmer, Linda N. Casillas, Michael P. DeMartino, Philip A. Harris, Bryan W. King, Ami Lakdawala Shah, Lara Kathryn Leister, Joshi M. Ramanjulu, Joseph J. Romano, Gren Z. Wang, Matthew A. Wilson, David Duff Wisnoski
-
Patent number: 8354542Abstract: Objects of the present invention are to provide the following: a novel heterocyclic compound which can be used as a material in which a light-emitting substance of a light-emitting layer in a light-emitting element is dispersed; a novel heterocyclic compound having a high electron-transport property; a light-emitting element having high current efficiency; and a light-emitting device, an electronic device and a lighting device each having reduced power consumption. Provided are a heterocyclic compound represented by General Formula (G1-1) or (G1-2) below, and a light-emitting element, a light-emitting device, an electronic device and a lighting device each including the heterocyclic compound. Such use of the heterocyclic compound represented by General Formula (G1-1) or (G1-2) makes it possible to provide a light-emitting element having high current efficiency, and a light-emitting device, an electronic device and a lighting device each having reduced power consumption.Type: GrantFiled: December 20, 2010Date of Patent: January 15, 2013Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Yuko Kawata, Hiroshi Kadoma, Harue Osaka, Nobuharu Ohsawa, Satoshi Seo
-
Publication number: 20130001537Abstract: The present invention provides a novel organic compound that is chemically stable and can be used as a host material for phosphorescence emission. The present invention provides a benzimidazolyl carbazole compound shown by Formula [1] described in the description.Type: ApplicationFiled: March 14, 2011Publication date: January 3, 2013Inventors: Hajime Muta, Takeshi Sekiguchi, Ryuji Ishii, Koichi Suzuki
-
Patent number: 8329705Abstract: The present invention relates to substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: December 11, 2012Assignee: ArQule, Inc.Inventor: Neil Westlund
-
Publication number: 20120309736Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: February 21, 2011Publication date: December 6, 2012Inventors: Jinlong Jiang, Andrew J. Kassick, Ahmet Kekec, Iyassu K. Sebhat
-
Publication number: 20120306727Abstract: Provided are a fused polycyclic compound suitable for use mainly as a component for a blue-light-emitting device, and an organic light-emitting device using the compound. The fused polycyclic compound is represented by the general formulae (1), (2), (8) and (9).Type: ApplicationFiled: May 1, 2012Publication date: December 6, 2012Applicant: CANON KABUSHIKI KAISHAInventors: Hiroki Ohrui, Hironobu Iwawaki, Kei Tagami, Masanori Muratsubaki, Ryuji Ishii
-
Publication number: 20120302748Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: February 28, 2012Publication date: November 29, 2012Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
-
Patent number: 8309721Abstract: The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R?1; R is selected from the group comprising Formula (A?), (B), (C), (D), or (E), with R1 and/or R?1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.Type: GrantFiled: September 14, 2010Date of Patent: November 13, 2012Assignee: SanofiInventors: Jean-Marie Ruxer, Victor Certal, Marcel Alasia, Luc Bertin, Herve Minoux, Patrick Mailliet, Frank Halley, Maria Mendez-Perez
-
Publication number: 20120277229Abstract: In one aspect, the invention relates to substituted 3-(1H-benzo[d]imidazol-2-yl)-1H-indazole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the PDK1 kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the PDK1 kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 31, 2012Publication date: November 1, 2012Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
-
Publication number: 20120270859Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 14, 2012Publication date: October 25, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias TREU, Ulrich GUERTLER, Thomas KARNER, Oliver KRAEMER, Jens Juergen QUANT, Stephan Karl ZAHN
-
Patent number: 8293923Abstract: The present invention relates to modulators of IRAK kinases of formula (I) and provides compositions comprising such modulators, as well as methods therewith for treating IRAK-mediated or IRAK-associated conditions or diseases.Type: GrantFiled: September 7, 2007Date of Patent: October 23, 2012Assignee: Biogen Idec MA Inc.Inventors: Kevin Guckian, Charles Jewell, Patrick Conlon, Edward Yin Shiang Lin, Timothy Chan
-
Publication number: 20120264711Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: June 7, 2012Publication date: October 18, 2012Applicant: GILEAD SCIENCES, INC.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Michael Graupe, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard L. Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
-
Patent number: 8288425Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.Type: GrantFiled: January 4, 2005Date of Patent: October 16, 2012Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael L. Edwards, Paul J. Cox, Shelley Amendola, Stephanie D. Deprets, Timothy A. Gillespy, Christopher D. Edlin, Andrew D. Morley, Charles J. Gardner, Brian Pedgrift, Herve Bouchard, Didier Babin, Laurence Gauzy, Alain Le-Brun, Tahir N. Majid, John C. Reader, Lloyd J. Payne, Nawaz M. Khan, Michael Cherry
-
Publication number: 20120251491Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 12, 2010Publication date: October 4, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
-
Publication number: 20120252770Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: March 23, 2012Publication date: October 4, 2012Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
-
Patent number: 8273269Abstract: A composition, for producing dispersions, thermoplastic masses and/or color filters, comprising (a) a colorant of formula (1) wherein 20-100 mol % R1 are Br and 80-100 mol % R3 are H, especially of formula (Ib) and/or (Ic); (b) from 0 to 150% by weight, based on (a), of C. I. Pigment Red 144, 188, 190, 224, 242 or 2,4,6-trimethylphenylperylene diimide; (c) from 3 to 25% by weight, based on (a), of a di- or tri-azacyclopentylmethyl-substituted colorant (formulae given); (d) from 0 to 10% by weight, preferably from 0.01 to 8% by weight, based on the sum of (a) and (b), of an additionally sulfonated colorant of the same kernels as in (c); and (e) from 0 to 30% by weight, preferably from 3 to 25% by weight, especially from 5 to 20% by weight, based on (a), of a diketopyrrolopyrrole colorant substituted by at least one chain containing a plurality of nitrogen atoms (cf. formula (V)).Type: GrantFiled: May 5, 2009Date of Patent: September 25, 2012Assignee: BASF SEInventors: Roman Lenz, Gerardus De Keyzer, Mathias Duggeli, Patrick Christopher Holzhuter
-
Publication number: 20120211736Abstract: A compound for an organic photoelectric device, the compound being represented by the following Chemical Formula (“CF”) 1:Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicant: CHEIL INDUSTRIES, INC.Inventors: Hyung-Sun KIM, Eun-Sun YU, Soo-Hyun MIN, Ho-Jae LEE, Eui-Su KANG, Mi-Young CHAE, Young-Hoon KIM, Ja-Hyun KIM
-
Publication number: 20120208811Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: ApplicationFiled: August 5, 2010Publication date: August 16, 2012Applicants: F. HOFFMANN-LA ROCHE AG, CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
-
Publication number: 20120208827Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.Type: ApplicationFiled: October 27, 2010Publication date: August 16, 2012Inventors: Steven Dock, Jason Hallman, Christopher Laudeman, Ronggang Liu, Aaron Miller, Michael Lee Moore, David Musso, Cynthia Parrish
-
Publication number: 20120202856Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: ApplicationFiled: February 2, 2012Publication date: August 9, 2012Inventors: Mark R. PLAYER, Raul CALVO, Jinsheng CHEN, Carl ILLIG, Sanath MEEGALLA, Daniel PARKS, William PARSONS
-
Publication number: 20120202997Abstract: The present invention relates to compounds of the formula (1) and formula (2) which are suitable for use in electronic devices, in particular organic electroluminescent devices.Type: ApplicationFiled: September 9, 2010Publication date: August 9, 2012Applicant: Merck Patent GmbHInventors: Amir Hossain Parham, Christof Pflumm
-
Publication number: 20120190639Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: July 26, 2012Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
-
Publication number: 20120184533Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.Type: ApplicationFiled: July 2, 2010Publication date: July 19, 2012Applicant: ANGION BIOMEDICA CORP.Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
-
Publication number: 20120184556Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.Type: ApplicationFiled: July 23, 2010Publication date: July 19, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
-
Patent number: 8217044Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.Type: GrantFiled: March 28, 2011Date of Patent: July 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jing Zhang, Zhuming Zhang
-
Publication number: 20120172351Abstract: A compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof have a GPR40 receptor activation action and is useful as an insulin secretagogue or a prophylactic or therapeutic drug for diabetes and the like.Type: ApplicationFiled: June 8, 2010Publication date: July 5, 2012Inventors: Nobuyuki Negoro, Yoshito Terao, Satoshi Mikami, Tomoya Yukawa
-
Publication number: 20120149676Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
-
Publication number: 20120142921Abstract: The invention relates to substituted hydrazide compounds as shown by general formula I, including geometrical isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and use of the same, wherein the substitutents Ar and R have the same meanings as given in the Description. The invention further relates to the use of compounds of general formula I in the preparation of medicament for the treatment and/or prevention of cancer and other proliferative diseases.Type: ApplicationFiled: August 9, 2010Publication date: June 7, 2012Applicant: SHENYANG J & HEALTH PHARMACEUTICAL CO., LTD.Inventor: Xiulan Shi
-
Publication number: 20120133274Abstract: An object is to provide a novel carbazole compound that can be used for a transport layer, a host material, or a light-emitting material in a light-emitting element. A carbazole compound where nitrogen of a carbazole group, the carbazole skeleton of which whose 3-position is bonded to the 4-position of a dibenzofuran skeleton or a dibenzothiophene skeleton, is bonded to a benzimidazole skeleton through a phenylene group, is provided. The carbazole compound has a high carrier-transport property, and can be suitably used for a material for a light-emitting element or for an organic semiconductor material.Type: ApplicationFiled: November 28, 2011Publication date: May 31, 2012Inventors: Sachiko Kawakami, Nobuharu Ohsawa
-
Publication number: 20120122810Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
-
Publication number: 20120122892Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: ApplicationFiled: January 25, 2012Publication date: May 17, 2012Applicant: AstraZeneca ABInventors: Michelle Lamb, Tao Wang, Dingwei Yu, Peter Mohr, Bin Wang
-
Patent number: 8178687Abstract: Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R?1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1, 2 and m=0, 1; R1 and/or R?1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products beingType: GrantFiled: December 16, 2010Date of Patent: May 15, 2012Assignee: Sanofi-AventisInventors: Marcel Alasia, Hervé Minoux, Jean-Marie Ruxer
-
Publication number: 20120115856Abstract: A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. wherein, R1 represents (1) a C3-6 alkyl group, (2) a C1-6 alkyl group substituted with one or more substituent group(s) selected from those consisting a halogen atom, etc., (3) a C3-10 non-aromatic cyclic hydrocarbon group or a 5- to 6-membered non-aromatic heterocyclic group which respectively is optionally substituted with one or more substituent group(s) selected from those consisting an oxo group, etc., (4) an aromatic cyclic hydrocarbon group substituted with one or more substituent selected from the group consisting halogen atom and C1-4 alkoxy group; X represents NH, O, or S; Y represents CH or N; Z represents N or a C—R2; R2 represents (1) hydrogen atom, (2) a C1-6 alkyl group, a C2-6 alkenyl group or a C2-6 alkynyl group that respectively is optionally substituted with one or more substituent group(s) selected from among those consisting (a) a halogen atom, etc.Type: ApplicationFiled: May 28, 2010Publication date: May 10, 2012Inventors: Junichi Ishikawa, Koichi Saito, Norihisa Ohe, Kentaro Kobayashi
-
Publication number: 20120115820Abstract: The present invention relates to a use of a compound having an acid pump antagonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for prevention or treatment of diseases in which abnormal gastrointestinal motility is involved. In addition, the present invention relates to the method of prevention or treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agent. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound having an acid pump antagonistic activity or a pharmaceutically acceptable salt thereof for the prevention or treatment of said diseases.Type: ApplicationFiled: July 9, 2010Publication date: May 10, 2012Inventors: Nobuyuki Takahashi, Shinichi Koizumi
-
Publication number: 20120097929Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein R1 to R12 are defined as in the specification.Type: ApplicationFiled: August 16, 2011Publication date: April 26, 2012Applicant: Samsung Mobile Display CO., LTD.Inventors: Young-Kook Kim, Seok-Hwan Hwang, Yoon-Hyun Kwak, Sun-Young Lee, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee
-
Patent number: 8153682Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: July 18, 2008Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman