Ring Oxygen Bonded Directly To Ring Carbon Which Is A Member Of Two Cyclos In The Tetracyclo Ring System Patents (Class 549/279)
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Patent number: 9150535Abstract: The present invention is directed to a method for producing artemisinin having the formula from dihydroartemisinic acid in a continuous flow reactor using singlet oxygen as well as to the continuous flow reactor for producing artemisinin.Type: GrantFiled: August 29, 2012Date of Patent: October 6, 2015Assignee: MAX-PLANCK-GESELLSCHAFT ZUR FĂ–RDERUNG DER WISSENSCHAFTEN E.V.Inventors: Peter H. Seeberger, Daniel Kopetzki, Francois Levesque
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Patent number: 8952003Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 22, 2010Date of Patent: February 10, 2015Assignee: Kyowa Hakko Kirin Co., LtdInventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
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Publication number: 20150038728Abstract: The present invention relates to arylated camphenes, processes for their preparation and uses thereof for the manufacture of medicaments for the treatment of diseases, disorders or conditions associated with, or benefiting from stimulation of CB2 receptors.Type: ApplicationFiled: March 31, 2014Publication date: February 5, 2015Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Raphael MECHOULAM, Lital MAGID, Esther SHOHAMI, Itai BAB
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Patent number: 8829205Abstract: The present invention relates to a method for preparing coumestrol, comprising a step in which beans are germinated and a step in which the beans are fermented, and to coumestrol prepared by the method.Type: GrantFiled: January 31, 2011Date of Patent: September 9, 2014Assignee: Amorepacific CorporationInventors: Hee Young Jeon, Dae Bang Seo, Si Young Cho, Sang Jun Lee
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Publication number: 20140135507Abstract: The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material.Type: ApplicationFiled: May 10, 2012Publication date: May 15, 2014Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Silas Cook, Chun-Yin Zhu
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Patent number: 8686028Abstract: The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substitutedType: GrantFiled: May 14, 2009Date of Patent: April 1, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Atul Goel, Amit Kumar, Sumit Chaurasia, Divya Singh, Abnish Kumar Gautam, Rashmi Pandey, Ritu Trivedi, Man Mohan Singh, Naibedya Chattopadhyay, Lakshmi Manickavasagam, Girish Kumar Jain, Anil Kumar Dwivedi
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Patent number: 8420834Abstract: Disclosed is a process for manufacturing crude Artemisinin comprising the extraction of Artemisia annua from plant material with carbon dioxide or water in a critical physical state such that after extraction, the solvent evaporates completely from the resulting extract.Type: GrantFiled: September 25, 2008Date of Patent: April 16, 2013Assignee: Lachifarma S.r.l. Laboratorio Chimico Farmaceutico SalentinoInventors: Felicia Cisale, Azzurra Villanova, Luciano Villanova
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Publication number: 20130066048Abstract: Described herein is an enriched substance containing a ground edible material comprising one or more concentrated bioactive natural products from plant juice, as well as methods of producing such enriched substances and methods of using such solids to provide beneficial effects to humans or other animals. Enriched foods comprising the enriched substance(s) are also provided. Also provided are non-sorbed natural products such as sugars, fats oils, and carotenoids found in the non-sorbed plant liquor fraction of plant juice.Type: ApplicationFiled: March 14, 2011Publication date: March 14, 2013Applicant: Rutgers, The State University of New JerseyInventors: Ilya Raskin, Diana Roopchand, Slavko Komarnytsky
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Publication number: 20120289714Abstract: The present invention relates to a method for preparing coumestrol, comprising a step in which beans are germinated and a step in which the beans are fermented, and to coumestrol prepared by the method.Type: ApplicationFiled: January 31, 2011Publication date: November 15, 2012Inventors: Hee Young Jeon, Dae Bang Seo, Si Young Cho, Sang Jun Lee
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Publication number: 20120245366Abstract: The present invention relates to arylated camphenes, processes for their preparation and uses thereof for the manufacture of medicaments for the treatment of diseases, disorders or conditions associated with, or benefiting from stimulation of CB2 receptors.Type: ApplicationFiled: November 18, 2010Publication date: September 27, 2012Inventors: Raphael Mechoulam, Lital Magid, Esther Shohami, Itai Bab
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Publication number: 20120172348Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 22, 2010Publication date: July 5, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
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Publication number: 20120161063Abstract: Various uses of monochlorotrifluoropropenes, in combination with one or more other components, including other fluoroalkenes, hydrocarbons; hydrofluorocarbons (HFCs), ethers, alcohols, aldehydes, ketones, methyl formate, formic acid, water, trans-1,2-dichloroethylene, carbon dioxide and combinations of any two or more of these, in a variety of applications, including as blowing agents, are disclosed.Type: ApplicationFiled: September 8, 2010Publication date: June 28, 2012Applicant: HONEYWELL INTERNATIONAL INC.Inventor: Rajiv R. Singh
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Publication number: 20120015922Abstract: Artesunate is a derivative of artemisinin isolated from a Chinese herb Artemisia annua L. It is used clinically for the treatment of malaria. We investigated potential anti-inflammatory actions of artemisinin derivatives. artemisinin derivatives significantly inhibited OVA-induced signs, symptoms and parameter of airway disorders Taken together, our results clearly demonstrate anti-inflammatory effects of artemisinin derivatives. Artemisinin derivatives can be used to complement or to replace oral steroids during asthma exacerbation treatment. Further artemisinin derivatives can be used as an anti-inflammatory agent for controlling airway disorders.Type: ApplicationFiled: March 24, 2010Publication date: January 19, 2012Applicant: NATIONAL UNIVERSITY OF SINGAPOREInventor: Wai Shiu Fred Wong
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Publication number: 20120003273Abstract: The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substitutedType: ApplicationFiled: May 14, 2009Publication date: January 5, 2012Inventors: Atul Goel, Amit Kumar, Sumit Chaurasia, Divya Singh, Abnish Kumar Gautam, Rashmi Pandey, Ritu Trivedi, Man Mohan Singh, Naibedya Chattopadhyay, Lakshmi Manickavasagam, Girish Kumar Jain, Anil Kumar Dwivedi
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Publication number: 20100331553Abstract: Disclosed is a process for manufacturing crude Artemisinin comprising the extraction of Artemisia annua from plant material with carbon dioxide or water in a critical physical state such that after extraction, the solvent evaporates completely from the resulting extract.Type: ApplicationFiled: September 25, 2008Publication date: December 30, 2010Applicant: Lachifarma S.R.L.-Laboratorio Chimico FarmaceuticoInventors: Luigi Villanova, Felicia Cisale, Azzurra Villanova, Luciano Villanova
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Patent number: 7795299Abstract: Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmaceutical formulations thereof.Type: GrantFiled: January 16, 2009Date of Patent: September 14, 2010Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Xihong Wang, Kenneth F. Bastow, Tian-Shung Wu
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Patent number: 7727545Abstract: A polymeric material having improved gas permeability comprises units of fluorinated dioxole. The polymeric material may further comprise units of a hydrophobic monomer, a hydrophilic monomer, or combinations thereof. Such a polymeric material is desirably used to produce medical devices, such as ophthalmic devices that provide increased comfort to a user.Type: GrantFiled: February 22, 2006Date of Patent: June 1, 2010Assignee: Bausch & Lomb IncorporatedInventors: Joseph C. Salamone, Derek A. Schorzman
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Publication number: 20100093651Abstract: This disclosure provides improved derivatives of artemisinin; pharamaceutical compositions containing these compounds; methods for preparing these compounds and compositions; methods of using these compounds and compositions for preventing, controlling or treating infectious diseases including but not limited to parasitic infectious diseases such as T. gondii infection, trypanosome parasite infection, plasmodia parasite infection, and cryptosporidium parasite infection; methods for preventing, controlling or treating toxoplasma infection; and methods for treating psychiatric disorders associated with toxoplasma infection including but not limited to schizophrenia using the disclosed compounds and compositions alone or in combination with one or more antipsychotic drugs.Type: ApplicationFiled: October 19, 2007Publication date: April 15, 2010Inventors: Lorraine V. Brando, Gary H. Posner, John G. D'Angelo, Robert H. Yolken, Christopher P. Hencken, Lauren Woodard
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Publication number: 20100069474Abstract: The present invention is directed to novel coumarin derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channelsType: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Inventors: Nareshkumar F. Jain, Zhihua Sui
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Publication number: 20100061948Abstract: The present invention relates to a skin-whitening composition comprising artemisinine. Artemsinine according to the present invention suppresses melanin synthesis and tyrosinase activity to inhibit pigmentation, and has excellent whitening effect and safety without side effects, thereby being used for improving melasma or freckles, and whitening skin.Type: ApplicationFiled: January 9, 2008Publication date: March 11, 2010Inventors: Deok Hoon Park, Jong Sung Lee, Kwang Sun Jung, Eunsun Jung, Saebom Kim
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Patent number: 7495026Abstract: Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmeutical formulations thereof.Type: GrantFiled: March 9, 2005Date of Patent: February 24, 2009Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Xihong Wang, Kenneth F. Bastow, Tian-Shung Wu
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Patent number: 7208518Abstract: The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers thereof, to the pharmaceutically acceptable salts and solvates thereof, to the processes and reactive intermediates for their preparation and to their use in the prophylaxis and treatment of asthma and other inflammatory diseases and/or conditions in humans.Type: GrantFiled: January 23, 2006Date of Patent: April 24, 2007Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.Inventors: Mladen Mercep, Milan Mesic, Boska Hrvacic, Ivaylo Jivkov Elenkov, Ivica Malnar, Stribor Markovic, Lidija Simicic, Andreja Cempuh Klonkay, Anita Filipovic
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Patent number: 6503941Abstract: The present invention relates to a skin cosmetic product containing 3,9-diferulylcoumestrol, especially to a skin cosmetic product containing a compound in which ferulylic acid is bonded to a coumestrol. The skin cosmetic product has several excellent effects for improving cosmetic disorders, such as anti-aging effect, whitening effect and hair-seeding effect.Type: GrantFiled: February 22, 2002Date of Patent: January 7, 2003Assignee: Hanbul Cosmetics Co., Ltd.Inventors: Hyeong-Bae Pyo, Chung-Woo Lee, Sung-Min Park, Young-Ho Cho, Jeong-Jae Lee, Jin-Hwa Kim
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Patent number: 5985913Abstract: The present invention provides a compound in substantially pure form having the structure: ##STR1## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 may independently be hydrogen, halogen, nitro, CF.sub.3, hydroxy, C.sub.1-5 alkyl, aryl or OR.sub.9, wherein R.sub.9 is C.sub.1-5 alkyl, wherein R.sub.10 is COC.sub.1-5 alkyl; or wherein any two consecutive R groups may be members of a C.sub.5 -C.sub.6 membered ring, and wherein the intracyclic-dashed line represents a covalent bond which may be present or absent, with the proviso that when R.sub.10 is present, the exocyclic-covalent bond is absent, and when R.sub.10 is absent, the exocyclic-covalent bond is present, and with the proviso that when R.sub.10 is absent, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen and when R.sub.10 is absent, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen when either R.sub.1, R.sub.2, R.sub.3, or R.sub.Type: GrantFiled: April 29, 1998Date of Patent: November 16, 1999Assignee: OSI Pharmaceuticals, Inc.Inventors: Jonathan Gareth Williams, David R. Houck, David Edward Smith, Daniel Lee Rathbone, David Charles Billington, Bernard T. Golding, Eric W. Collington, John Kitchin, Nicholas Rich
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Patent number: 5216175Abstract: Polyoxoheterocyclic tetracycles related to the Chinese antimalarial natural product qinghaosu (artemisinin) are disclosed. These materials have a ##STR1## core structure with an oxygen (carbonyl or alkyl ether) at position 12 and in some cases one or two alkyl or aralkyl substituents at position 11. These materials have antimalarial properties.Type: GrantFiled: March 23, 1990Date of Patent: June 1, 1993Assignee: SRI InternationalInventors: Mitchell A. Avery, Wesley K. M. Chong, James E. Bupp
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Patent number: 5019590Abstract: A process for synthesizing oxygen-containing polyoxatetracycle compounds and in particular analogs of the antimalarial agent known as qinghaosu or artemisinin is disclosed. The process employs as a reactant an olefinically unsaturated bicyclic bridging ketone having nonenolizable bridgehead moieties for both of its alpha positions. This ketone is converted to a vinylsilane that is subjected to ozonolytic cleavage of its olefinic bond to yield a member of a family of unique carboxyl/carbonyl-substituted vinylsilanes which may in turn optionally be subjected to a wide range of reactions prior to a final ozonolysis/acidification step which closes the oxygen-containing ring structure. The various intermediates are claimed as aspects of this invention as are novel tetracycles and their use as antimalarials.Type: GrantFiled: September 27, 1989Date of Patent: May 28, 1991Assignee: SRI InternationalInventors: Mitchell A. Avery, Wesley K. M. Chong
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Patent number: 4997848Abstract: Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl of hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group] have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.Type: GrantFiled: October 21, 1988Date of Patent: March 5, 1991Assignee: Sankyo Company, LimitedInventors: Masaaki Kurabayashi, Hiroshi Kogen, Hiroshi Kadokawa, Hideshi Kurihara, Kazuo Hasegawa, Masao Kuroda
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Patent number: 4992561Abstract: This invention relates to a novel process for producing artemisinin from emisinic acid. The artemisinic acid is reduced to dihydroartemisinic acid by reduction of the exocyclic methylene group. The dihydroartemisinic acid is then oxidized in two successive steps to form artemisinin.Type: GrantFiled: May 11, 1990Date of Patent: February 12, 1991Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Ronald J. Roth, Nancy A. Roth
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Patent number: 4963683Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring matrial. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.Type: GrantFiled: February 15, 1989Date of Patent: October 16, 1990Assignee: SRI InternationalInventors: Mitchell A. Avery, Clive Jennings-White