Plural Ring Hetero Atoms In The Tetracyclo Ring System (e.g., Acronycines, Etc.) Patents (Class 546/62)
  • Patent number: 10249824
    Abstract: Embodiments of the present invention are directed to a condensed-cyclic compound represented by Formula 1, and to an organic light-emitting diode including the same.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: April 2, 2019
    Assignee: Samsung Display Co., Ltd.
    Inventors: Bum-Woo Park, Yoon-Hyun Kwak, Sun-Young Lee, Se-Jin Cho
  • Patent number: 10214536
    Abstract: Provided herein are amlexanox analogs and methods for the treatment and/or prevention of diabetes, impaired insulin signaling, obesity, or other related diseases and conditions therewith.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: February 26, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Hollis D. Showalter, Alan R. Saltiel, John J. Tesmer, Xinmin Gan
  • Patent number: 9812645
    Abstract: The present invention relates to new semiconductor materials prepared from perylene-based compounds. Such compounds can exhibit high carrier mobility and/or good current modulation characteristics. In addition, the compounds of the present teachings can possess certain processing advantages such as solution-processability and/or good stability at ambient conditions.
    Type: Grant
    Filed: February 15, 2016
    Date of Patent: November 7, 2017
    Assignee: Flexterra, Inc.
    Inventors: Antonio Facchetti, Mitchell Denti
  • Patent number: 9499853
    Abstract: The present disclosure relates to biosensing systems and biosensing elements having increased storage capability and increased functional lifetimes through using compositions and methods for recycling cofactors.
    Type: Grant
    Filed: August 2, 2012
    Date of Patent: November 22, 2016
    Assignee: COLORADO STATE UNIVERSITY RESEARCH FOUNDATION
    Inventor: Kenneth F. Reardon
  • Patent number: 9085574
    Abstract: A synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds wherein said procedures provides an increment in the compounds biological activity. The compounds are further used for intra cellular binding, cytotoxicity on malignant cells through apoptosis activation mediated by mitochondrial damage, cellular organelles binding and damage, DNA fragmentation, marker of bacterial growth, antibacterial activity, cell cycle disruption, and a marker due to the auto-fluorescent properties.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: July 21, 2015
    Inventors: Beatriz Zayas, Osvaldo Cox
  • Publication number: 20150141419
    Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
  • Publication number: 20150086491
    Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.
    Type: Application
    Filed: November 5, 2014
    Publication date: March 26, 2015
    Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
  • Patent number: 8969373
    Abstract: A compound of general formula (I); A is O, S, CH, NH or NR?, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1? is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
    Type: Grant
    Filed: July 23, 2012
    Date of Patent: March 3, 2015
    Assignee: Shanghai Tangrun Pharmaceuticals Co., Ltd.
    Inventor: Suoming Zhang
  • Patent number: 8962620
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: February 24, 2015
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Patent number: 8927717
    Abstract: The invention provides a series of novel thiochromeno[2,3-c]quinolin-12-one derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with treating effective amount are prepared into pharmaceutical compositions for inhibition of topoisomerase type I and II, inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: January 6, 2015
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Dah-Shyong Yu, Tsung-Chih Chen
  • Publication number: 20140374733
    Abstract: An object of the present invention is to provide a photoelectric conversion element having a photoelectric conversion film which exhibits heat resistance, a high photoelectric conversion efficiency, a low level of dark currents, rapid response, and sensitivity characteristics to red and can be produced by a vapor deposition processing that is continuously performed under a high-temperature condition. The photoelectric conversion element of the present invention is a photoelectric conversion element in which a conductive film, a photoelectric conversion film containing a photoelectric conversion material, and a transparent conductive film are laminated on one another in this order, wherein the photoelectric conversion material includes a compound represented by Formula (1).
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Yuki HIRAI, Yosuke YAMAMOTO, Tomoaki YOSHIOKA, Eiji FUKUZAKI, Katsuyuki YOFU, Masaaki TSUKASE, Mitsumasa HAMANO, Takahiko ICHIKI
  • Publication number: 20140371459
    Abstract: Provided is a method for producing a compound represented by formula (7) or a salt thereof: the method comprising the steps of: removing a R1 group and a R2 group from a compound represented by formula (5) or a salt thereof: and reacting the compound (in which R1 and R2 in formula (5) are hydrogen atoms) obtained in the removing step or a salt thereof with a compound represented by formula (d): or a salt thereof in the presence of a base. The method is a method for producing a 1,2-dihydroquinoline derivative having glucocorticoid receptor binding activity or a salt thereof. This method does not require a purification step by column chromatography and is suitable for industrial production.
    Type: Application
    Filed: January 21, 2013
    Publication date: December 18, 2014
    Applicants: SANTEN PHARMACEUTICAL CO., LTD., KYOWA HAKKO BIO CO., LTD.
    Inventors: Noriyoshi Yamamoto, Atsushi Ohno, Kazuhiro Kudou, Masakazu Ban, Takashi Mimura, Takashi Ohtani
  • Publication number: 20140356873
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Zhenjun DIWU, Jixiang LIU, Kyle GEE
  • Publication number: 20140302987
    Abstract: Use of substituted isoquinolinones, isoquinolinediones, isoquinolinetriones and dihydroisoquinolinones of the general formula (I) or their respective salts where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.
    Type: Application
    Filed: July 2, 2012
    Publication date: October 9, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiss, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döering, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills
  • Publication number: 20140163012
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
  • Patent number: 8629158
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 14, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden, Emily Elizabeth Freeman
  • Patent number: 8592424
    Abstract: A method of treating a disease state or condition in humans via topical brainstem afferent stimulation therapy via the administration of a drug to the back of the neck of a human patient at the hairline in close proximity to and under or on the area of skin above the brain stem to provide regional neuro-affective therapy is disclosed.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: November 26, 2013
    Assignee: Afgin Pharma LLC
    Inventor: Ronald Aung-Din
  • Publication number: 20130196362
    Abstract: Provided herein are improved fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening peroxynitrite. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. Also provided herein are fluorogenic compounds for selectively staining peroxynitrite in the mitochondria of living cells. Provided also herein are methods that can be used to measure, directly or indirectly, the presence and/or amount of peroxynitrite in chemical samples and biological samples such as cells and tissues in living organisms. Also provided are high-throughput screening methods for detecting or screening peroxynitrite or compounds that can increase or decrease the level of peroxynitrite in chemical and biological samples.
    Type: Application
    Filed: January 30, 2013
    Publication date: August 1, 2013
    Applicant: THE UNIVERSITY OF HONG KONG
    Inventor: THE UNIVERSITY OF HONG KONG
  • Publication number: 20130131091
    Abstract: The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. wherein Het represents pyridyl; X represents an oxygen atom; R1, R2, R3, R7, R10a, R10b, R11, and R12 represent a hydrogen atom; R4, R5, and R6 represent a hydrogen atom, hydroxyl, optionally substituted C1-18 alkylcarbonyloxy, optionally substituted C1-18 alkylsulfonyloxy, optionally substituted arylcarbonyloxy, C1-6 alkyloxy-C1-6 alkyloxy, C1-6 alkyloxy-C1-6 alkyloxy-C1-6 alkyloxy; R8 represents a hydrogen atom; and R13a, R13b, and R13c represent methyl.
    Type: Application
    Filed: May 23, 2011
    Publication date: May 23, 2013
    Inventors: Kimihiko Goto, Ryo Horikoshi, Kazuhiko Oyama, Yoshimasa Fukuda, Nozomu Nakanishi, Masato Tani, Nobuto Minowa, Masaaki Mitomi, Satoshi Omura, Toshiaki Sunazuka, Hiroshi Tomoda
  • Publication number: 20120315661
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Application
    Filed: May 14, 2012
    Publication date: December 13, 2012
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Zhenjun DIWU, Jixiang LIU, Kyle GEE
  • Patent number: 8318938
    Abstract: Optionally substituted chromenoisoquinolines and analogs and derivatives thereof are described herein. In addition, syntheses of these compounds are described herein. In addition, uses of these compounds as dopamine receptor binding compounds are described herein.
    Type: Grant
    Filed: August 20, 2008
    Date of Patent: November 27, 2012
    Assignee: Purdue Research Foundation
    Inventors: David Nichols, Val J. Watts
  • Publication number: 20120263659
    Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 18, 2012
    Applicants: BASF SE, SYMRISE AG
    Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
  • Publication number: 20120083488
    Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).
    Type: Application
    Filed: June 9, 2010
    Publication date: April 5, 2012
    Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
  • Patent number: 8134146
    Abstract: The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof to organic semiconductive materials and to electronic and optoelectronic components.
    Type: Grant
    Filed: March 20, 2007
    Date of Patent: March 13, 2012
    Assignee: Novaled AG
    Inventors: Michael Limmert, Olaf Zeika, Martin Ammann, Horst Hartmann, Ansgar Werner
  • Patent number: 8124770
    Abstract: A synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of amino-substituent and nitro-substituent resulting in four compounds such as NBQ-38 (7-Ethyl-3-nitrobenzimidazolo[3,2-a]quinolinium Chloride), NBQ-95(2-Chloro-10-methyl-3-nitrobenzothiazolo[3,2-a]quinolinium chloride), ABQ-38(3-amino-7-ethylbenzimidazo [3,2-a]quinolinium chloride), and ABQ-95 (3-amino-2-chloro-10-methylbenzothiazolo[3,2-a]quinolinium chloride) wherein said procedures provides an increment in the compounds biological activity. The compounds are further used for intra cellular binding, cytotoxicity on malignant cells through apoptosis activation mediated by mitochondrial damage and caspases 3 and 7 activation, cellular organelles binding and damage, and a marker due to the auto-fluorescent properties.
    Type: Grant
    Filed: April 1, 2009
    Date of Patent: February 28, 2012
    Inventors: Beatriz Zayas, Osvaldo Cox
  • Publication number: 20110269790
    Abstract: The present invention provides compounds and pharmaceutically acceptable salts thereof methods for synthesizing thienopyridines and methods for inhibiting TNF-? activity for the treatment of cancer, asthma, arthritis, diabetes and inflammation. Provided are compounds of formula (I).
    Type: Application
    Filed: January 5, 2010
    Publication date: November 3, 2011
    Inventors: Shireesha Boyapati, Akkinepally Raghuram Rao, Banda Narsaiah, Prakash V. Diwan, Sistla Ramakrishna, Madhusudhana, Tallapally Yakaiah
  • Publication number: 20110245353
    Abstract: The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.
    Type: Application
    Filed: March 31, 2011
    Publication date: October 6, 2011
    Applicant: SENOMYS, INC.
    Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy DAVIS, Vincent DARMOHUSODO, Melissa WONG, Victor SELCHAU
  • Patent number: 8022102
    Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substitutents are defined as in Claim 1.
    Type: Grant
    Filed: June 21, 2005
    Date of Patent: September 20, 2011
    Assignee: Janssen Pharmaceutica, NV
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Patent number: 7960548
    Abstract: Compounds and methods for treating, inhibiting, or delaying the onset of cancer in a subject by administering a therapeutically effective amount of a keratinocyte growth factor receptor tyrosine kinase (KGFR TK) inhibitor to the subject in need of such treatment. Also provided are compounds and methods for the treating, inhibiting, or delaying the onset of metastasis in a subject with cancer by administering a therapeutically effective amount of a KGFR TK inhibitor to the subject in need of such treatment.
    Type: Grant
    Filed: May 1, 2006
    Date of Patent: June 14, 2011
    Assignees: The Ohio State University Research Foundation, The Board of Regents of the University of Oklahoma
    Inventors: J. Thomas Pento, Pui-Kai Li, Robert W. Brueggemeier, John C. Hackett
  • Publication number: 20110110948
    Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.
    Type: Application
    Filed: July 15, 2008
    Publication date: May 12, 2011
    Applicant: SCHERING CORPORATION
    Inventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien
  • Patent number: 7834180
    Abstract: Compounds having formula 1: are produced by contacting a compound having formula (6A) with a compound having formula (7), or tautomers thereof, in the presence of a non-nucleophilic base, wherein V, A, Z, L, L1, W, X, B?, R and n are as defined herein.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: November 16, 2010
    Assignee: Cylene Pharmaceuticals, Inc.
    Inventors: Peter C. Chua, Johnny Y. Nagasawa, Michael Schwaebe, Fabrice Pierre
  • Patent number: 7829576
    Abstract: This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: November 9, 2010
    Assignee: Adolor Corporation
    Inventors: Bertrand Le Bourdonnec, Roland E. Dolle
  • Patent number: 7816519
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: October 19, 2010
    Assignee: Life Technologies Corporation
    Inventors: Zhenjun Diwu, Jixiang Liu, Kyle Gee
  • Publication number: 20100261706
    Abstract: Provided herein are tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analogs and derivatives, compositions comprising an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog and/or derivative and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, a reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, an ocular or opthalmologic disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, contrast induced nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog or derivative.
    Type: Application
    Filed: December 8, 2009
    Publication date: October 14, 2010
    Applicant: INOTEK PHARMACEUTICALS CORPORATION
    Inventors: Prakash JAGTAP, Duy-Phong Pham-Huu, Frederick COHEN, Huiyong HU, Xiaojing WANG
  • Publication number: 20100256378
    Abstract: A synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of amino-substituent and nitro-substituent resulting in four compounds such as NBQ-38(7-Ethyl-3-nitrobenzimidazolo[3,2-a]quinolinium Chloride), NBQ-95(2-Chloro-10-methyl-3-nitrobenzothiazolo[3,2-a]quinolinium chloride), ABQ-38(3-amino-7-ethylbenzimidazo[3,2-a]quinolinium chloride), and ABQ-95(3-amino-2-chloro-10-methylbenzothiazolo[3,2-a]quinolinium chloride) wherein said procedures provides an increment in the compounds biological activity. The compounds are further used for intra cellular binding, cytotoxicity on malignant cells through apoptosis activation mediated by mitochondrial damage and caspases 3 and 7 activation, cellular organelles binding and damage, and a marker due to the auto-fluorescent properties.
    Type: Application
    Filed: April 1, 2009
    Publication date: October 7, 2010
    Inventors: Beatriz Zayas, Osvaldo Cox
  • Patent number: 7795299
    Abstract: Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmaceutical formulations thereof.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: September 14, 2010
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Xihong Wang, Kenneth F. Bastow, Tian-Shung Wu
  • Patent number: 7763633
    Abstract: Indolo[3,2-c]quinoline compounds of formula (I) shown below. Each variable in this formula is defined herein. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: July 27, 2010
    Assignee: Kaohsiung Medical University
    Inventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Jing-Jer Lin, Chih-Ming Lu
  • Patent number: 7728000
    Abstract: Compounds of formula G1-L-G2, where -G1 is a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from (CH2)rNR??(CH2)s and —(CH2)rNR??(CH2)sNR??(CH2)t—, —R?? and —R?? are radicals, same or different, selected from the group consisting of H and (C1-C3)-alkyl; r, s and t are an integer from 1 to 3 and, -G2 is H or a radical structurally close to -G1, are intercalators. They are compounds which intercalate between DNA base pairs, and are useful as therapeutic agents against cancer, as assess by an in vitro test of cytotoxicity with human leukemia cells Jurkat E6-1 and human carcinoma cells GLC-4. Preferred compounds are those where -G1 is bonded to -L- through a carbonyl amino and -L- is —(CH2)3NCH3(CH2)3 or —(CH2)2NCH3(CH2)sNCH3(CH2)2— where s =2 or 3.
    Type: Grant
    Filed: November 18, 2004
    Date of Patent: June 1, 2010
    Assignees: Crystax Pharmaceuticals, Universitat Politecnica de Catalunya, Consejo Superior de Investigactiones Cientificas
    Inventors: Juan Aymami Bofarull, Miquel Coll Capella, Amadeo Llebaria Soldevila, Isabel Navarro Muñoz
  • Publication number: 20100069380
    Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.
    Type: Application
    Filed: September 21, 2007
    Publication date: March 18, 2010
    Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
  • Publication number: 20100048604
    Abstract: The present invention relates to compounds useful for detecting the activity of human aldoketoreductase 1Cs, compounds useful for competitively inhibiting human aldoketoreductase 1Cs and compounds useful for treating human aldoketoreductase 1C-related cancers, as well as pharmaceutical compositions and methods of manufacture thereof.
    Type: Application
    Filed: August 19, 2005
    Publication date: February 25, 2010
    Inventors: Dominic J. Yee, Vojtech Balsanek, Dalibor Sames
  • Patent number: 7605263
    Abstract: Naphthalene-1,4,5,8-tetracarboxylic bisimides of the general formula I where the variables are defined as follows: R1 and R2 independently of one another are hydrogen, substituted or unsubstituted alkyl or substituted or unsubstituted aryl; X and Y independently of one another are halogen, amino or a radical with the formula —NHR3, —OR3, where R3 has the formula —CH2R4, —CHR4R5, or —CR4R5R6, where R4, R5, and R6 independently of one another are hydrogen, substituted or unsubstituted alkyl, aryl, alkoxy, alkylthio, aryloxy or arylthio, and at least one of the two substituents X and Y is other than halogen, their preparation and use as fluorescent dyes, for coloring high molecular mass organic materials and inorganic materials, as laser dyes, and also for fluorescence marking and as fluorescent labels for biomolecules.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: October 20, 2009
    Assignee: Infineon Technologies AG
    Inventors: Gunter Schmid, Christoph Thalacker, Frank Wurthner
  • Patent number: 7592350
    Abstract: A compound of formula I, wherein X, Z, R1 to R10, R15, R16, m, n, r and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2 antagonist. The compounds of formula I can be used for the treatment of diseases or conditions where antagonists of alpha-2 adrenoceptors are indicated to be effective.
    Type: Grant
    Filed: April 3, 2003
    Date of Patent: September 22, 2009
    Assignee: Orion Corporation
    Inventors: David Din Belle, Reija Jokela, Arto Tolvanen, Antti Haapalinna, Arto Karjalainen, Jukka Sallinen, Jari Ratilainen
  • Publication number: 20090203725
    Abstract: Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors and/or modulate the amount of androgen receptors; and to methods for making and using such compounds. Also provided are compositions containing such compounds and methods for making and using such compositions.
    Type: Application
    Filed: December 21, 2006
    Publication date: August 13, 2009
    Inventors: Cornelis Arjan Van Oeveren, Yixing Shen, Shuo Zhao, Lin Zhi
  • Patent number: 7511064
    Abstract: The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament and for the manufacture of a medicament for treatment of a disease state which can be alleviated by treatment with a 5-HT2B antagonist.
    Type: Grant
    Filed: April 19, 2006
    Date of Patent: March 31, 2009
    Assignee: Biofrontera Bioscience GmbH
    Inventors: Hermann Lubbert, Christoph Ullmer, Emile Bellott, Mark Froimowitz, Douglas Gordon
  • Publication number: 20090030025
    Abstract: Optionally substituted chromenoisoquinolines and analogs and derivatives thereof are described herein. In addition, syntheses of these compounds are described herein. In addition, uses of these compounds as dopamine receptor binding compounds are described herein.
    Type: Application
    Filed: August 20, 2008
    Publication date: January 29, 2009
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: David Nichols, Val J. Watts
  • Patent number: 7465742
    Abstract: This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and to the use of such compositions to treat Hepatitis B and other diseases.
    Type: Grant
    Filed: February 3, 2006
    Date of Patent: December 16, 2008
    Inventors: Huanming Chen, Robert Tam, Anneke K. Raney
  • Publication number: 20080293757
    Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 6, 2008
    Publication date: November 27, 2008
    Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki, Dmitry Koltun
  • Publication number: 20080262016
    Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.
    Type: Application
    Filed: June 16, 2008
    Publication date: October 23, 2008
    Applicant: Inotek Pharmaceuticals Corporation
    Inventors: Prakash Jagtap, Erkan Baloglu, John H. van Duzer, Csaba Szabo, Andrew L. Salzman, Aloka Roy, William Williams, Alexander Nivorozhkin
  • Patent number: 7432276
    Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 27, 2006
    Date of Patent: October 7, 2008
    Assignee: CV Therapeutics, Inc.
    Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki, Dmitry Koltun, Melanie Boze
  • Publication number: 20080221118
    Abstract: Compounds of the formula I, in which s, k, I, W, R1, R2, R3, and U have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: May 31, 2006
    Publication date: September 11, 2008
    Inventors: Wolfgang Staehle, David Bruge, Kai Schiemann, Dirk Finsinger, Hans-Peter Buchstaller, Frank Zenke, Christiane Amendt