The Six-membered Hetero Ring Shares Ring Members With The Five-membered Cyclo Only (e.g., Pyrido-indoles, Etc.) Patents (Class 546/85)
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Patent number: 8476294Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.Type: GrantFiled: June 2, 2010Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Pascal Furet, Frank Stephan Kalthoff, Robert Mah, Christian Ragot, Frédéric Stauffer
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Patent number: 8471008Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.Type: GrantFiled: November 25, 2011Date of Patent: June 25, 2013Assignee: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
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Publication number: 20130137705Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: September 23, 2010Publication date: May 30, 2013Inventor: Sarvajit Chakravarty
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Publication number: 20130131077Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical-compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: December 21, 2012Publication date: May 23, 2013Applicant: Medivation Technologies, Inc.Inventor: Medivation Technologies, Inc.
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Publication number: 20130131099Abstract: Nitrated and non-nitrated compounds capable of protecting brain tissue from injury and useful as therapeutic agents to treat neurodegenerative diseases and conditions are disclosed. Methods of using the compounds in therapeutic treatments, and methods of preparing the compounds, also are disclosed.Type: ApplicationFiled: May 4, 2011Publication date: May 23, 2013Inventors: Gregory R.J. Thatcher, Zhihui Qin, Jia Luo
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Publication number: 20130131070Abstract: Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure: where X is NH, N—C1-C4 alkyl, S, or O; R1 is 1-naphthyl or 1-dihydroacenaphthenyl, each optionally substituted with a halogen; and R2, R3, R4, R5, R6, and R7 are independently H H, OH, halogen, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl with the proviso that X is NH, R1 is 1-naphthyl or 1-naphthyl substituted with a halogen and one of R5, R6, or R7 is C1-C4 alkoxy, then R2, R3, R4, R5, R6, and R7 are independently H, OH, halogen, CN, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl such that at least two of R2, R3, R4, R5, R6, and R7 are other than H. Also provided are methods for inhibiting proliferation of cells associated with a cell proliferative disease by contacting the cell with the compounds provided herein.Type: ApplicationFiled: October 30, 2012Publication date: May 23, 2013Inventor: John K. Buolamwini
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Publication number: 20130123277Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in the variety of therapeutic application, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or neuronal disorder.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: Medivation Technologies, Inc.Inventor: Medivation Technologies, Inc.
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Publication number: 20130116219Abstract: The invention provides compositions comprising carboline compounds for treating infections such as viral conjunctivitis. The invention also provides methods for treating of other infections, including ocular infections.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: ALCON RESEARCH, LTD.Inventor: ALCON RESEARCH, LTD.
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Publication number: 20130109713Abstract: The invention provides a compound of formula I:or a salt thereof, wherein R3-R8 and X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.Type: ApplicationFiled: June 24, 2011Publication date: May 2, 2013Inventors: Edmond J. Lavoie, Ajit Parhi, Daniel S. Pilch
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Publication number: 20130099207Abstract: The present invention provides a bipolar compound represented by formula (I) and the derivatives thereof as a host material having excellent bipolar transporting properties for organic light-emitting diodes (OLEDs). The present invention also relates to a device including at least a layer of the bipolar compound and/or the derivatives thereof as a host material and a method of making the same.Type: ApplicationFiled: April 19, 2012Publication date: April 25, 2013Applicant: NANO AND ADVANCED MATERIALS INSTITUTE LIMITEDInventors: Chun Sing LEE, Xiao Hong ZHANG, Shuit Tong LEE, Caijun ZHENG, Man Keung FUNG
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Publication number: 20130079352Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: November 16, 2012Publication date: March 28, 2013Applicant: Medivation Technologies, Inc.Inventor: Medivation Technologies, Inc.
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Publication number: 20130046097Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.Type: ApplicationFiled: August 23, 2012Publication date: February 21, 2013Inventors: John Charles TOMESCH, Peng LI, Wei YAO, Qiang ZHANG, James David Beard, Andrew S. Thompson, Hua Cheng
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Patent number: 8367691Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: June 4, 2010Date of Patent: February 5, 2013Assignee: Vertex Pharmaceutical IncorporatedInventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
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Patent number: 8367694Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.Type: GrantFiled: July 21, 2009Date of Patent: February 5, 2013Assignee: PTC Therapeutics, Inc.Inventors: Young-Choon Moon, Liangxian Cao, Nadarajan Tamilarasu, Hongyan Qi, Soongyu Choi, William Joseph Lennox, Donald Thomas Corson, Seongwoo Hwang
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Publication number: 20130028958Abstract: The present invention is directed at ?-carbolines, preferred 9-alkyl-?-carbolines (9-alkyl-?-BC), their manufacture as well as their use in prophylaxis and treatment of hearing damages, tinnitus, acute acoustic trauma, vertigo and vestibular disorder as well as pharmaceutical compositions containing theses ?-carbolines.Type: ApplicationFiled: December 28, 2010Publication date: January 31, 2013Inventor: Hans Rommelspacher
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Patent number: 8357803Abstract: The present invention relates to the process of preparation of 2,3,4,9-tetrahydro-1/?/-?-carbolin-3-carboxylic acid esters substituted in position 1 of the general formula (I). in the preferred diastereoisomeric form through a single step starting from tryptophan in racemic form and/or its enantiomers and from 3,4-(methylenedioxy)benzaldehyde.Type: GrantFiled: February 20, 2009Date of Patent: January 22, 2013Assignee: Endura S.p.A.Inventors: Valerio Borzatta, Dina Scarpi, Antonio Guarna, Ernesto G. Occhiato
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Patent number: 8338448Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof. These compounds, and pharmaceutical composition comprising such compounds are useful treating or preventing HIV infections, and in treating proliferative disorders such as inhibiting the metastasis of various cancers.Type: GrantFiled: March 30, 2009Date of Patent: December 25, 2012Assignee: Altiris Therapeutics, Inc.Inventors: Michael P. Clark, Florence F. Wagner, Brandon C. Doroh, Tricia L. Johnson, Yesim Altas Tahirovic, Lawrence Wilson, John M. Wiseman, Jason W. Skudlarek, Mark A. Lockwood, Michael G. Natchus
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Patent number: 8338408Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: October 27, 2008Date of Patent: December 25, 2012Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew A. Protter, Rajendra P. Jain, Sundeep Dugar, Sarvajit Chakravarty, Sergey O. Bachurin, Anatoly K. Ustinov, Bogdan K. Beznosko, Nadezhda Sergeevna Beznosko, legal representative, Elena F. Shevtsova, Vladimir V. Grigoriev
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Patent number: 8338447Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds of formula (I) are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: March 24, 2009Date of Patent: December 25, 2012Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra P. Jain, Sundeep Dugar
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Patent number: 8334299Abstract: The embodiments relate to derivatives of 9-alkyl-?-carboline, their production and pharmaceutical compositions containing these 9-alkyl-?-carboline derivatives. Further, the use of 9-alkyl-?-carboline derivatives and pharmaceutical compositions for the treatment and prevention of movement disorders, neurodegenerative diseases, Alzheimer's disease and Parkinson's disease is described. Additionally, these effects can be utilized for the cultivation of cells such as dopaminergic cells or stem cells which shall be engrafted for the treatment of Parkinson's disease.Type: GrantFiled: February 26, 2008Date of Patent: December 18, 2012Assignee: Ellneuroxx, Ltd.Inventor: Hans Rommelspacher
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Publication number: 20120309781Abstract: Certain 2-halophenyl, 2,4-dihalophenyl (e.g. 2,4-dichlorophenyl), 3,4-dichlorophenyl (e.g. 3,4-dichlorophenyl), 2,6-dichlorophenyl (2,6-dichlorophenyl) and 2,5-diakoxyphenyl (e.g. 2,5-dimethoxyphenyl) derivatives of tetrahydro-?-carbolines are provided, along with their pharmaceutically acceptable salts; prodrugs and solvates, and compositions containing the compounds. The compounds are useful for the prevention and treatment of cancer, and other indications where PDE5 inhibitors have shown benefits including erectile dysfunction, pulmonary hypertension, enhancing cognitive function, cystic fibrosis, or enhancing the activity of conventional chemotherapeutic drugs. Methods for fabricating the compounds are also provided.Type: ApplicationFiled: November 19, 2010Publication date: December 6, 2012Applicant: Southern Research InstituteInventors: Gary A. Piazza, Ashraf H. Abadi
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Publication number: 20120302755Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.Type: ApplicationFiled: May 22, 2012Publication date: November 29, 2012Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Anna Katrin Szardenings, Hartmuth C. Kolb, Joseph C. Walsh, Gang Chen, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Changhui Liu, Anjana Sinha, Eric Wang, Chul Yu, Wei Zhang, Kai Chen, Vani P. Mocharla, Peter J.H. Scott
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Publication number: 20120298969Abstract: The invention relates to a compound having a pyridoindole ring structure having a substituted pyridyl group of formula (1); and to an organic electroluminescent device comprising a pair of electrodes and at least one organic layer interposed between the electrodes, wherein at least one of the organic layer(s) contains the compound: wherein Ar represents a substituted or unsubstituted aromatic hydrocarbon group, a substituted or unsubstituted aromatic heterocyclic group, or a substituted or unsubstituted condensed polycyclic aromatic group; R1 to R10 may be the same or different from one another and each independently represents a hydrogen atom, a fluorine atom, a cyano group, an alkyl group, or a substituted or unsubstituted aromatic hydrocarbon group; Z represents a 6-membered aromatic heterocyclic ring containing one nitrogen atom; and m and n each independently represents an integer of 1 to 3, provided that n is 1 when m is 2 or 3.Type: ApplicationFiled: March 14, 2012Publication date: November 29, 2012Applicant: Hodogaya Chemical Co., Ltd.Inventors: Norimasa YOKOYAMA, Shuichi Hayashi, Shigeru Kusano
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Patent number: 8309722Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.Type: GrantFiled: March 12, 2008Date of Patent: November 13, 2012Assignee: Intra-Cellular Therapies, Inc.Inventors: John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng
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Patent number: 8309730Abstract: Disclosed are compounds of Formula (I) wherein: one of A and D is —N— and the other of A and D is —C—; or enantiomers, diastereomers, or pharmaceutically-acceptable salts thereof. Also disclosed are methods of using such compounds to modulate the function of glucocorticoid receptor activity and pharmaceutical compositions comprising such compounds.Type: GrantFiled: October 30, 2008Date of Patent: November 13, 2012Assignee: Bristol-Myers Squibb CompanyInventors: T. G. Murali Dhar, Hai-Yun Xiao
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Patent number: 8288376Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: GrantFiled: January 24, 2012Date of Patent: October 16, 2012Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
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Patent number: 8268854Abstract: Provided are compounds having the general structure according to Formula (I): Further provided are pharmaceutical compositions comprising these compounds. The invention still further provides methods of treating alcoholism, methods of reducing alcohol intake, methods of treating anhedonia, and methods of treating anxiety using theses compounds or the compositions containing them.Type: GrantFiled: May 22, 2009Date of Patent: September 18, 2012Assignee: The UWM Research Foundation, Inc.Inventors: James M. Cook, Michael L. Van Linn, Wenyuan Yin
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Publication number: 20120228598Abstract: The present invention relates to a compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2); and an organic electroluminescent device having a pair of electrodes and at least one organic layer interposed therebetween, in which the compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2), is used as a constituent material of the aforementioned at least one organic layer.Type: ApplicationFiled: November 10, 2010Publication date: September 13, 2012Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Norimasa Yokoyama, Shuichi Hayashi, Kouki Kase, Hiroshi Ohkuma, Eiji Takahashi, Daizou Kanda
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Publication number: 20120202763Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.Type: ApplicationFiled: May 27, 2010Publication date: August 9, 2012Applicant: PTC THERAPEUTICS, INCInventors: Neil Almstead, Tamil Arasu, Soongyu Choi, Liangxian Cao, Jeffrey Allen Campbelll, Donald Corson, Thomas W. Davis, Jason D. Graci, Zhengxian Gu, Peter Seong Woo Hwang, William Lennox, Harry H. Miao, Langdon Miller, Young-Choon Moon, Hongyan Qi, Christopher Trotta, Marla L. Weetall
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Publication number: 20120172377Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: April 29, 2010Publication date: July 5, 2012Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Patent number: 8207187Abstract: There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.Type: GrantFiled: November 8, 2006Date of Patent: June 26, 2012Assignee: Helperby Therapeutics LimitedInventors: Petra Helga Beck, Marc Barry Brown, David Edward Clark, Anthony Coates, Hazel Joan Dyke, Yanmin Hu, Derek John Londesbrough, Keith Mills, Thomas David Pallin, Gary Patrick Reid, Gerlinda Stoddart
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Patent number: 8202881Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: GrantFiled: September 2, 2010Date of Patent: June 19, 2012Assignee: Bristol-Meyers Squibb CompanyInventors: Ashok V. Purandare, James W. Grebinski, Amy Hart, Jennifer Inghrim, Gretchen Schroeder, Honghe Wan
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Publication number: 20120136154Abstract: Provided herein are improved processes for the synthesis of substituted tetrahydro beta-carboline derivatives. In particular, provided herein are improved processes useful for the preparation of (S)-4-chlorophenyl 6-chloro-1-(4-methoxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate.Type: ApplicationFiled: May 27, 2010Publication date: May 31, 2012Inventors: Peter Seongwoo Hwang, Young-Choon Moon, Arasu Tamil, Hongyan Qi, Neil Almstead
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Publication number: 20120136008Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: April 29, 2010Publication date: May 31, 2012Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Publication number: 20120126220Abstract: There is provided an organic compound having excellent characteristics, including excellent electron-injecting/transporting performance, hole blocking ability, and high stability in the thin-film state, for use as material of an organic electroluminescent device having high efficiency and high durability. There is also provided a high-efficient and high-durable organic electroluminescent device using the compound. The compound is represented by general formula (1) having a substituted anthracene ring structure and a pyridoindole ring structure. The organic electroluminescent device includes a pair of electrodes, and one or more organic layers sandwiched between the pair of electrodes, and the compound is used as a constituent material of at least one organic layer.Type: ApplicationFiled: July 28, 2010Publication date: May 24, 2012Applicant: Hodogaya Chemical Co., Ltd.Inventors: Norimasa Yokoyama, Shuichi Hayashi, Naoki Kabasawa, Daizou Kanda, Shigeru Kusano
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Publication number: 20120123124Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I, having (6R,12aR)-configuration, used for treatment of erectile dysfunction. Starting from racemic or L-tryptophan the invention describes preparation of an enantiomerically pure intermediate of formula II which is a known precursor in the synthesis of Tadalafil (formula I).Type: ApplicationFiled: April 22, 2011Publication date: May 17, 2012Applicant: Drug Process Licensing Associates, LLCInventor: Milan Soukup
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Publication number: 20120101121Abstract: Compositions based on hydrogenated pyrido[4,3-b]indoles (variants) of formula (1) or formula (2): are provided, as are methods and kits using those compositions for the treatment of anxiety or mood disorders characterized by stresses, anxiety, neuroses, obsessive fears and their consequences.Type: ApplicationFiled: June 27, 2008Publication date: April 26, 2012Inventors: Sergey Olegovich BACHURIN, Taisiya Leonovna GARIBOVA, Tatiana Alexandrovna VORONINA, Vladimir Viktorovich CRIGORIEV
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Patent number: 8143248Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: GrantFiled: August 1, 2008Date of Patent: March 27, 2012Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
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Publication number: 20120032121Abstract: A metallic composite in which a conjugated compound having a molecular weight of 200 or more is adsorbed to a metallic nanostructure having an aspect ratio of 1.5 or more, for example, a metallic composite in which a compound having a group represented by the formula (I) or a repeating unit represented by the formula (II) or both of them is adsorbed to a metallic nanostructure having an aspect ratio of 1.5 or more, is useful for electronic devices such as a light-emitting device, a solar cell and an organic transistor.Type: ApplicationFiled: April 6, 2010Publication date: February 9, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hideyuki Higashimura, Takayuki Iijima, Masahiro Fujioka, Kenta Tanaka
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Publication number: 20120022096Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: July 7, 2011Publication date: January 26, 2012Applicant: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Publication number: 20120015911Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: September 20, 2011Publication date: January 19, 2012Applicant: Bellus Health Inc.Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Patent number: 8084937Abstract: The present invention provides a novel binaphthyl compound and an organic light emitting element having a good light emitting efficiency and a high durability at a low driving voltage.Type: GrantFiled: October 2, 2008Date of Patent: December 27, 2011Assignee: Canon Kabushiki KaishaInventors: Tetsuya Kosuge, Jun Kamatani, Shigemoto Abe, Ryota Ooishi, Kengo Kishino
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Patent number: 8080658Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex contains a compound represented by formula 1: wherein R1 to R10 are each independently hydrogen atom, halogen atom, alkyl group having 1 to 40 carbon atoms, cycloalkyl group having 3 to 15 carbon atoms, heterocyclic group having 3 to 20 carbon atoms which is optionally substituted, alkoxy group having 1 to 40 carbon atoms, non-condensed aryl group having 6 to 40 carbon atoms, condensed aryl group having 10 to 18 carbon atoms, aryloxy group having 6 to 20 carbon atoms, aralkyl group having 7 to 20 carbon atoms, arylamino group having 6 to 40 carbon atoms, alkylamino group having 1 to 40 carbon atoms, aralkylamino group having 7 to 60 carbon atoms, arylcarbonyl group having 7 to 40 carbon atoms, alkyl halide group having 1 to 40 carbon atoms, or cyano group, R8 and R9 being optionally bonded to each other to form a ring structure and each of R1 to R10 being optionallyType: GrantFiled: July 10, 2007Date of Patent: December 20, 2011Assignee: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
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Patent number: 8071587Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: May 25, 2010Date of Patent: December 6, 2011Assignee: N. V. OrganonInventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
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Publication number: 20110281862Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, to their pharmaceutical compositions and use thereof for the treatment of cancer expressing oncogenic ALK protein, particularly anaplastic large cell lymphoma (ALCL), diffuse large B cell lymphoma (DLBCL), inflammatory myofibroblastic tumours (IMT) and non-small cell lung cancer (NSCLC).Type: ApplicationFiled: August 27, 2009Publication date: November 17, 2011Applicants: Universita' Degli Studi di Milano - Bicocca, Universite' Claude Bernard de Lyon 1, Universite' de GeneveInventors: Carlo Gambacorti Passerini, Luca Mologni, Leonardo Scapozza, Shaheen Ahmed, Peter G. Goekjian, David Gueyrard, Florence Popowycz, Benoit Joseph, Cedric Schneider, Pierre Garcia
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Publication number: 20110282063Abstract: The present invention provides a novel diazafluorene compound for manufacturing a 4,5-diazafluorene derivative. The diazafluorene compound is represented by the general formula (1): wherein R1 and R2 each represent a hydrogen atom, a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aryl group, and may be the same or different from each other; and X1 and X2 each represent a halogen atom, and may be the same or different from each other.Type: ApplicationFiled: July 21, 2011Publication date: November 17, 2011Applicant: CANON KABUSHIKI KAISHAInventors: Hiroki Ohrui, Akihiro Senoo, Tetsuya Kosuge
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Patent number: 8013160Abstract: A fluorene-based derivative having a specific structure and an organic electroluminescence device in which an organic thin film layer comprising a single layer or plural layers including at least a light emitting layer is sandwiched between a cathode and an anode, wherein at least one layer of the organic thin film layers described above comprises the above fluorene-based derivative having a specific structure in the form of a single component or a mixed component. The organic electroluminescence device has a high luminous efficiency, and the fluorene-based derivative materializes the same.Type: GrantFiled: July 19, 2010Date of Patent: September 6, 2011Assignee: Idemitsu Kosan Co., Ltd.Inventors: Mitsunori Ito, Hiroshi Yamamoto, Satoshi Hachiya, Hisayuki Kawamura
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Publication number: 20110201615Abstract: Beta-carboline derivatives of structural formula (I) are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.Type: ApplicationFiled: October 19, 2009Publication date: August 18, 2011Inventors: Liangqin Guo, Jian Liu, Ravi P. Nargund, Alexander Pasternak, Lihu Yang, Zhixiong Ye
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Publication number: 20110175079Abstract: The present invention provides an organic compound having excellent properties, which is excellent in electron-injection/transport performance, has hole-blocking ability and is high stability in a thin-film state, as a material for an organic electroluminescence device having a high efficiency and a high durability, and provides is an organic electroluminescence device having a high efficiency and a high durability using the compound. The present invention relates to a compound having a substituted anthracene ring structure and a pyridoindole ring structure represented by general formula (1); and an organic electroluminescence device having a pair of electrodes and at least one organic layer interposed between the electrodes in which the at least one organic layer contains the compound.Type: ApplicationFiled: September 18, 2009Publication date: July 21, 2011Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Norimasa Yokoyama, Shuichi Hayashi, Sawa Izumi, Naoaki Kabasawa, Shigeru Kusano
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Publication number: 20110178068Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.Type: ApplicationFiled: December 23, 2010Publication date: July 21, 2011Applicant: Alkermes, Inc.Inventors: Orn Almarsson, Laura Cook Blumberg, Julius F. Remenar