Plural Ring Oxygens In The Tricyclo Ring System Patents (Class 549/387)
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Patent number: 10787428Abstract: The present invention provides an ?,?-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I): [wherein, “A” represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO2—, —NRX1— (wherein, RX1 represents hydrogen atom or lower alkyl), —CHRX2— (wherein, RX2 represents hydrogen atom or hydroxy), —CH?CH—, —CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].Type: GrantFiled: December 22, 2016Date of Patent: September 29, 2020Assignee: KYOWA KIRIN CO., LTD.Inventors: Tomohiro Danjo, Katsuaki Fujiwara, Tomoyuki Nishikawa, Takahiro Nakajima, Nobumasa Otsubo, Toshihiro Seike
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Patent number: 9822125Abstract: Provided are benzopyran compounds of formula I, for example, pomiferin-3?,4?-dimethyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.Type: GrantFiled: August 12, 2014Date of Patent: November 21, 2017Assignee: NEW YORK UNIVERSITYInventor: Seth J. Orlow
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Patent number: 9783551Abstract: Provided are a pyranochromenyl phenol derivative, a pharmaceutically acceptable salt thereof, or a solvate thereof. Also provided is a pharmaceutical composition for preventing or treating metabolic syndrome or inflammatory disease comprising same. The present invention is efficacious in preventing or treating metabolic syndrome or inflammatory disease and is chemically stable.Type: GrantFiled: December 23, 2014Date of Patent: October 10, 2017Assignee: Glaceum Inc.Inventors: Sang Ku Yoo, Jin Wook Chung, In Geun Jo, Jeong Ho Im, Ku Suk Kang, Jin Young Kim
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Patent number: 9303038Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of epilepsy and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of convulsions, Lennox-Gastaut syndrome, migraine, bipolar disorder, post traumatic stress disorder.Type: GrantFiled: August 16, 2013Date of Patent: April 5, 2016Assignee: CELLIX BIO PRIVATE LIMITEDInventor: Mahesh Kandula
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Patent number: 9290472Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: GrantFiled: May 7, 2012Date of Patent: March 22, 2016Assignee: Zafgen, Inc.Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
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Publication number: 20150148409Abstract: Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.Type: ApplicationFiled: January 15, 2015Publication date: May 28, 2015Inventors: Guangdi WANG, Matthew E. BUROW, Stephen M. BOUE, Thomas E. WIESE, Quan JIANG
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Publication number: 20150119406Abstract: Tricyclic pyrone compounds having high oral bioavailability, excellent blood-brain barrier permeability, and low toxicity are presented. Administration of the compounds to Alzheimer's Disease transgenic models resulted in substantially reduced soluble and insoluble A? species in the brain without affecting general behavior and motor coordination. Furthermore, in addition to blocking the toxicity and formation of both intraneuronal and extracellular A? aggregates, the compounds also increase cellular cholesterol efflux, restore axonal trafficking, and enhance hippocampal synaptic plasticity.Type: ApplicationFiled: September 30, 2014Publication date: April 30, 2015Inventors: Duy H. Hua, Lee-way Jin, Izumi Maezawa, Xinmin Xie
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Publication number: 20150119424Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of epilepsy and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of convulsions, Lennox-Gastaut syndrome, migraine, bipolar disorder, post traumatic stress disorder.Type: ApplicationFiled: August 16, 2013Publication date: April 30, 2015Inventor: Mahesh KANDULA
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Topiramate Sustained-Release Pharmaceutical Composition, Method for Preparing Same, and Uses Thereof
Publication number: 20150099003Abstract: A sustained-release pharmaceutical composition of topiramate, which is free of binding agent. The sustained-release pharmaceutical composition of topiramate is a sustained-release pellet, comprising a blank pellet core, a drug layer, and a sustained-release coating layer.Type: ApplicationFiled: March 7, 2013Publication date: April 9, 2015Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Song Li, Chunsheng Gao, Wu Zhong, Yuli Wang, Meiyan Yang, Li Shan, Xinbo Zhou, Zhibing Zheng, Xiaokui Wang -
Publication number: 20150056166Abstract: The present invention relates to flavone derivatives and to compositions containing one or more of these flavone derivatives. The present invention further relates to flavone derivatives or compositions for use in the treatment and/or prevention of a viral infection, and to a method of preventing or treating these infections.Type: ApplicationFiled: March 22, 2013Publication date: February 26, 2015Inventors: Thomas Pietschmann, Sibylle Haid, Juliane Gentzsch, Christina Grethe, Elisabeth Davioud-Charvet, Don Antoine Lanfranchi, Mourad Elhabiri, Xavier Benlloch-Martin
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Patent number: 8933116Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.Type: GrantFiled: April 4, 2012Date of Patent: January 13, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
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Publication number: 20150005514Abstract: Disclosed herein is single step process for the synthesis of 4-aryl substituted chromanes of compound of formula 2 comprising subjecting 3-aryloxy-1-phenylpropan-1-ol of formula 1 to gold(III) chloride-catalyzed intramolecular Friedel-Crafts reaction to obtain 4-aryl substituted chromanes. The invention further discloses novel 4-substituted Chromane compounds.Type: ApplicationFiled: December 17, 2012Publication date: January 1, 2015Inventors: Vilasrao Chouthaiwale Pandurang, Ambadas Devalankar Dattatray, Arumugam Sudalai
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Patent number: 8889190Abstract: An extended-release topiramate capsule that includes a capsule shell containing a single population of coated particles; wherein each coated particle includes a core and a coating thereon; wherein each particle core includes a homogeneous mixture comprising topiramate throughout its core; and wherein the coating includes one or more release controlling agent(s).Type: GrantFiled: January 17, 2014Date of Patent: November 18, 2014Assignee: Upsher-Smith Laboratories, Inc.Inventors: Sarah Michelle Betterman, Jaidev Srinivas Tantry, Laura Marie Patrick
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Patent number: 8877949Abstract: Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as uses thereof as estrogen receptor modulators.Type: GrantFiled: April 13, 2011Date of Patent: November 4, 2014Assignee: Shenyang Pharmaceutical UniversityInventors: Chun Hu, Shihui Wang, Yan Wang, Erfang Huang, Xiaoping Liu, Dawei Li
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Publication number: 20140221468Abstract: Store operated calcium channel modulating compounds, and methods for using the same, are provided. These compounds and methods find use in a variety of applications in which modulation of store operated calcium channels is desired.Type: ApplicationFiled: December 9, 2011Publication date: August 7, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Chan Young Park, Amir M. Sadaghiani, Ricardo Ei Dolmetsch
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Publication number: 20140179754Abstract: Tricylic ether carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are describes. Methods of using the disclosed compounds for treating patients infected with HIV are also described.Type: ApplicationFiled: October 8, 2013Publication date: June 26, 2014Applicants: NATIONAL UNIVERSITY CORPORATION KUMAMOTO UNIVERSITY, PURDUE RESEARCH FOUNDATIONInventors: Arun K. GHOSH, Chun-Xiao Xu, Hiroaki Mitsuya, Garth Parham
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Publication number: 20140161731Abstract: Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.Type: ApplicationFiled: February 14, 2014Publication date: June 12, 2014Applicant: WisTa Laboratories Ltd.Inventors: Scott Clunas, John Mervyn David Storey, Janet Elizabeth Rickard, David Horsley, Charles Robert Harrington, Claude Michel Wischik
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Publication number: 20140088078Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: May 7, 2012Publication date: March 27, 2014Applicant: ZAFGEN, Inc.Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
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Patent number: 8664411Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.Type: GrantFiled: July 1, 2008Date of Patent: March 4, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Wen-Lian Wu, Thomas A. Bara, Duane A. Burnett, John W. Clader, Martin S. Domalski, Yan Jin, Hubert B. Josien, Hongmei Li, Xian Liang, Dmitri A. Pissarnitski, Thavalakulamgara K. Sasikumar, Jesse K. Wong, Ruo Xu, Zhiqiang Zhao, Paul McNamara
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Patent number: 8652527Abstract: An extended-release topiramate capsule that includes a capsule shell containing a single population of coated particles; wherein each coated particle includes a core and a coating thereon; wherein each particle core includes a homogeneous mixture comprising topiramate throughout its core; and wherein the coating includes one or more release controlling agent(s).Type: GrantFiled: March 19, 2013Date of Patent: February 18, 2014Assignee: Upsher-Smith Laboratories, IncInventors: Sarah Michelle Betterman, Jaidev Srinvas Tantry, Laura Marie Patrick
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Publication number: 20140018552Abstract: The present invention provides an AGE inhibitor and a health functional food for inhibiting an occurrence of diabetic complications. Particularly, the present invention comprises a compound selected from the group consisting of mulberrofuran G, mulberrofuran K, kuwanon G, kuwanon Z, oxyresveratrol, 2?,4?,5,7-tetrahydroxyflavanone, morusignin L and dihydromorin isolated from Morus Bark as an active ingredient. The compounds disclosed above inhibit the production of AGE which is a causative substance of diabetic complications. Thus, the compounds could be used as an AGE inhibitor and a health functional food for inhibiting diabetic nephropathy, diabetic retinopathy and diabetic neuropathy.Type: ApplicationFiled: March 26, 2012Publication date: January 16, 2014Applicant: Dong Wha Pharm. Co., Ltd.Inventors: Hwan Bong Chang, Joobyoung Yoon, Hyun Yong Lee, Hyun Sik Choi, Hyung Bok Lee
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Publication number: 20140018342Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.Type: ApplicationFiled: April 4, 2012Publication date: January 16, 2014Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
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Publication number: 20130296344Abstract: Compounds according to the general formula (I) wherein X1, X2, X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different, and wherein up to 3 of the group X1, X2, X3 and X4 may be N; A is a 5- or 6-membered aromatic or heteroaromtic cycle containing 1 to 3 heteroatoms selected from the group consisting of N, O and S wherein A may be substituted by 1 to 5 substituents R which may be same or different; their solvates, hydrates, and pharmaceutically acceptable salts for the treatment of a disorder or disease associated with an aberrant activation of Wnt signalling in a mammal selected from a cell proliferative disorder, rheumatoid arthritis, increased bone density, aging or age-related disorders and/or diseases or Dupuytren disease (superficial fibromatosis).Type: ApplicationFiled: November 11, 2011Publication date: November 7, 2013Applicants: Ruprecht-Karls-Universitat Heidelberg, Deutsches KrebsforschungszentrumInventors: Michael Boutros, Rajendra-Prasad Maskey, Corinna Koch, Florian Fuchs, Sandra Steinbrink, Daniel Gilbert
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Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Patent number: 8569521Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: GrantFiled: October 6, 2011Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Anne Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Patent number: 8563754Abstract: A method for preventing hyperpigmented skin, undesired pigmentation disorder of skin, or undesired darkening of skin using coumarin compounds, the use of such compounds, and compositions and formulations thereof are disclosed. In a particular embodiment, the coumarin compounds are selected from robustic acid methyl ether, scandenin, and coumophos. The compounds may be prepared as additives to pharmaceutical and cosmetic compositions, and in personal care products such as antiperspirants. In a particular embodiment extends to an antiperspirant product containing a skin darkening inhibitory amount of a compound of the invention. Also, the present skin darkening compounds may be prepared in combination with each other.Type: GrantFiled: January 28, 2011Date of Patent: October 22, 2013Assignee: New York UniversityInventors: Seth J. Orlow, Li Ni Komatsu
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Patent number: 8558016Abstract: A novel substance exhibiting physiologically active effects is produced from a tea leaf. A novel polyphenol derivative is produced, for example, by subjecting a microbially fermented tea leaf obtained by culturing Aspergillus sp. (PK-1) with a tea leaf, to an extraction treatment.Type: GrantFiled: September 17, 2010Date of Patent: October 15, 2013Assignees: Kabaushiki Kaisha Riverson, Saga UniversityInventors: Teruyoshi Yanagita, Kanji Ishimaru, Takashi Tanaka, Kazunori Koba, Hitoshi Miyazaki, Naohito Aoki, Denbei Kawamura
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Patent number: 8546376Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: GrantFiled: September 17, 2010Date of Patent: October 1, 2013Assignee: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Publication number: 20130184475Abstract: Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.Type: ApplicationFiled: July 8, 2011Publication date: July 18, 2013Applicants: THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND, XAVIER UNIVERSITY OF LOUISIANNA, UNITED STATES DEPARTMENT OF AGRICULTUREInventors: Guangdi Wang, Matthew E. Burow, Stephen M. Boue, Thomas E. Wiese, Quan Jiang
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Publication number: 20130158094Abstract: Tricylic ether carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are describes. Methods of using the disclosed compounds for treating patients infected with HIV are also described.Type: ApplicationFiled: September 2, 2011Publication date: June 20, 2013Applicant: PURDUE RESEARCH FOUNDATIONInventors: Arun K. Ghosh, Chun-Xiao Xu, Hiroaki Mitsuya, Garth Parham
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Publication number: 20130123235Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: July 21, 2011Publication date: May 16, 2013Inventors: David Clark, Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
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Publication number: 20130096112Abstract: Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as uses thereof as estrogen receptor modulators.Type: ApplicationFiled: April 13, 2011Publication date: April 18, 2013Applicant: SHENYANG PHARMACEUTICAL UNIVERSITYInventors: Chun Hu, Shihui Wang, Yan Wang, Erfang Huang, Xiaoping Liu, Dawei Li
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Patent number: 8394974Abstract: [PROBLEMS] To provide an efficient process for producing an optically active chromene oxide compound which is an important intermediate for a benzopyran compound effective in the treatment of arrhythmia. [MEANS FOR SOLVING PROBLEMS] The process for producing an optically active chromene oxide compound comprises using an optically active titanium complex represented by, e.g., the formula (1) or (2) as a catalyst to asymmetrically oxidize an optically active chromene compound with high enantioselectivity in high chemical yield.Type: GrantFiled: March 9, 2007Date of Patent: March 12, 2013Assignee: Nissan Chemical Industries, Ltd.Inventors: Shoichi Kondo, Kowichiro Saruhashi, Hisayuki Watanabe, Tsutomu Katsuki
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Publication number: 20130012576Abstract: The present invention discloses a composition for lowering blood lipid and elevating high-density lipoprotein and a method for manufacturing the same; the composition comprises monascin or ankaflavin, or a combination thereof; the manufacturing method comprises the steps of: treating a Monascus fermented product with acetone for three times; elevating the concentration of the Monascus fermented product by a process of decompress concentration; and extracting the monascin and the ankaflavin from the Monascus fermented product with a silica gel column chromatography, a Sephadex LH-20 column chromatography, the silica gel column chromatography, and a preparative high performance liquid chromatography sequentially.Type: ApplicationFiled: August 23, 2011Publication date: January 10, 2013Applicant: SUNWAY BIOTECH CO., LTD.Inventors: Tzu-Ming PAN, Chun-Lin LEE, Chen-Lun WU
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Patent number: 8303844Abstract: The present invention relates to benzo[f]chromene and pyrano[3,2-f]-chromene derivatives of the formula I in which L1, L2, R1, R2, A1, A2, Z1, Z2, m and n are as defined in claim 1, to the preparation thereof, to the use thereof as components in liquid-crystalline media, and to electro-optical display elements which contain the liquid-crystalline media according to the invention.Type: GrantFiled: November 3, 2008Date of Patent: November 6, 2012Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Axel Jansen, Melanie Klasen-Memmer
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20120264736Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: ApplicationFiled: October 6, 2011Publication date: October 18, 2012Applicant: Schering CorporationInventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Patent number: 8283478Abstract: The present invention is directed to novel process for the preparation of sulfonylimine and sulfamide derivatives.Type: GrantFiled: April 19, 2006Date of Patent: October 9, 2012Assignee: Janssen Pharmaceutica NVInventors: Ahmed F. Abdel-Magid, Steven J. Mehrman
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Publication number: 20120220789Abstract: A novel substance exhibiting physiologically active effects is produced from a tea leaf. A novel polyphenol derivative is produced, for example, by subjecting a microbially fermented tea leaf obtained by culturing Aspergillus sp. (PK-1) with a tea leaf, to an extraction treatment.Type: ApplicationFiled: September 17, 2010Publication date: August 30, 2012Applicants: SAGA UNIVERSITY, KABUSHIKI KAISHA RIVERSONInventors: Teruyoshi Yanagita, Kanji Ishimaru, Takashi Tanaka, Kazunori Koba, Hitoshi Miyazaki, Naohito Aoki, Denbei Kawamura
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Patent number: 8252923Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: GrantFiled: September 8, 2008Date of Patent: August 28, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
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Patent number: 8217189Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: GrantFiled: October 4, 2007Date of Patent: July 10, 2012Assignee: Bionomics LimitedInventors: Bernard Luke Flynn, Jonathan B. Baell, Andrew J. Harvey, Jason Hugh Chaplin, Dharam Paul, Jorgen Alvar Mould
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Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Patent number: 8067621Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: GrantFiled: January 18, 2007Date of Patent: November 29, 2011Assignee: Schering CorporationInventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Patent number: 8058427Abstract: Coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a method for treating cancer with coumarin compounds.Type: GrantFiled: June 10, 2009Date of Patent: November 15, 2011Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Jang-Yang Chang, Ching-Chuan Kuo, Yu-Sheng Chao
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Publication number: 20110236400Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.Type: ApplicationFiled: July 1, 2008Publication date: September 29, 2011Inventors: Wen-Lian Wu, Thomas A. Bara, Duane A. Burnett, John W. Clader, Martin S. Domalski, Yan Jin, Hubert B. Josien, Hongmei Li, Xian Liang, Dmitri A. Pissarnitski, Thavalakulamgara K. Sasikumar, Jesse K. Wong, Ruo Xu, Zhiqiang Zhao, Paul E. McNamara
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Publication number: 20110144194Abstract: Compounds of general formula (I) and (II) in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 and R15 have the meanings given in the specification, are useful in the treatment of neurodegenerative disease.Type: ApplicationFiled: April 22, 2009Publication date: June 16, 2011Inventors: Djalil Coowar, Emmanuel Couche, Eric Koncina
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Publication number: 20110144193Abstract: The present invention relates to the effects of the epimeric mixture of cinchonains Ia and Ib on pathologies that involve alterations in the cardiovascular system, essentially in combating, preventing and reverting ventricular fibrillation in human beings and animals, especially for combating spontaneous or electric-stimulus-induced ventricular fibrillation, to revert spontaneous or electric-stimulus-induced ventricular fibrillations, for preventing ventricular fibrillation, for the treatment of ventricular fibrillation of any etiology or for the treatment of post-fibrillation to maintain normal cardiac rhythm. The present invention further relates to methods for the synthesis of an epimeric mixture of the chemical substances cinchonain Ia and Ib. The present invention also relates to the use of these chemical substances in reverting/combating ventricular fibrillation and/or in protecting against ventricular fibrillation.Type: ApplicationFiled: November 16, 2010Publication date: June 16, 2011Inventors: Ney Osvaldo Silva Filho, Irineu Tadeu Velasco, Augusto Scalabrini Neto, Luiz Pianowski
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Publication number: 20110112182Abstract: A method of synthesizing rottlerin analogs is described. The synthesis methods described are the first known method of synthesizing rottlerin analogs from commercially-available materials to produce cost effective analogs. Rottlerin analog structures made by the synthesis methods and methods of use for treating a neurological or inflammatory response mediated by protein kinase C (PKC) are further described.Type: ApplicationFiled: November 12, 2010Publication date: May 12, 2011Applicant: IOWA STATE UNIVERSITY RESEARCH FOUNDATION, INC.Inventors: ANUMANTHA G. KANTHASAMY, GEORGE A. KRAUS, VELLAREDDY ANANTHARAM
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Publication number: 20110054013Abstract: Disclosed are novel gamma secretase inhibitors of the formula: wherein at least one (e.g., 1-4, 1-3, 1-2, 2 or 1) H is replaced by deuterium. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease.Type: ApplicationFiled: August 26, 2010Publication date: March 3, 2011Inventor: John W. Clader
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Publication number: 20110043746Abstract: The present invention relates to benzo[f]chromene and pyrano[3,2-f]-chromene derivatives of the formula I in which L1, L2, R1, R2, A1, A2, Z1, Z2, m and n are as defined in claim 1, to the preparation thereof, to the use thereof as components in liquid-crystalline media, and to electro-optical display elements which contain the liquid-crystalline media according to the invention.Type: ApplicationFiled: November 3, 2008Publication date: February 24, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Axel Jansen, Melanie Klasen-Memmer
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Publication number: 20110015158Abstract: The presently disclosed subject matter is described to metalloenzyme inhibitors having metal binding moieties linked to a targeting moiety through a linking group or a direct bond, method of screening for metalloenzyme inhibitors, and methods for treating a metalloenzyme related disorder by administering a metalloenzyme inhibitor to a subject in need of treatment thereof.Type: ApplicationFiled: December 3, 2008Publication date: January 20, 2011Applicant: Viamet Pharmaceuticals, Inc.Inventors: Robert J. Schotzinger, William J. Hoekstra
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Publication number: 20100168160Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.Type: ApplicationFiled: November 19, 2009Publication date: July 1, 2010Applicant: Beth Israel Deaconess Medical Center , Inc. And Trustees of Boston UniversityInventors: Chen-Yu Zhang, Bradford B. Lowell, John A. Porco, JR., Ruichao Shen, Cheng T. Lin, Stefan Krauss