Ring Oxygen Bonded Directly To Ring Carbon Which Is A Member Of Two Cyclos In The Tetracyclo Ring System Patents (Class 549/279)
  • Patent number: 9150535
    Abstract: 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: Grant
    Filed: August 29, 2012
    Date of Patent: October 6, 2015
    Assignee: MAX-PLANCK-GESELLSCHAFT ZUR FĂ–RDERUNG DER WISSENSCHAFTEN E.V.
    Inventors: Peter H. Seeberger, Daniel Kopetzki, Francois Levesque
  • Patent number: 8952003
    Abstract: 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: Grant
    Filed: July 22, 2010
    Date of Patent: February 10, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Publication number: 20150038728
    Abstract: 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: Application
    Filed: March 31, 2014
    Publication date: February 5, 2015
    Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Raphael MECHOULAM, Lital MAGID, Esther SHOHAMI, Itai BAB
  • Patent number: 8829205
    Abstract: 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: Grant
    Filed: January 31, 2011
    Date of Patent: September 9, 2014
    Assignee: Amorepacific Corporation
    Inventors: Hee Young Jeon, Dae Bang Seo, Si Young Cho, Sang Jun Lee
  • Publication number: 20140135507
    Abstract: The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material.
    Type: Application
    Filed: May 10, 2012
    Publication date: May 15, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Silas Cook, Chun-Yin Zhu
  • Patent number: 8686028
    Abstract: 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 substituted
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: April 1, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: 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
  • Patent number: 8420834
    Abstract: 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: Grant
    Filed: September 25, 2008
    Date of Patent: April 16, 2013
    Assignee: Lachifarma S.r.l. Laboratorio Chimico Farmaceutico Salentino
    Inventors: Felicia Cisale, Azzurra Villanova, Luciano Villanova
  • Publication number: 20130066048
    Abstract: 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: Application
    Filed: March 14, 2011
    Publication date: March 14, 2013
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Ilya Raskin, Diana Roopchand, Slavko Komarnytsky
  • Publication number: 20120289714
    Abstract: 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: Application
    Filed: January 31, 2011
    Publication date: November 15, 2012
    Inventors: Hee Young Jeon, Dae Bang Seo, Si Young Cho, Sang Jun Lee
  • Publication number: 20120245366
    Abstract: 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: Application
    Filed: November 18, 2010
    Publication date: September 27, 2012
    Inventors: Raphael Mechoulam, Lital Magid, Esther Shohami, Itai Bab
  • Publication number: 20120172348
    Abstract: 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: Application
    Filed: July 22, 2010
    Publication date: July 5, 2012
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Publication number: 20120161063
    Abstract: 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: Application
    Filed: September 8, 2010
    Publication date: June 28, 2012
    Applicant: HONEYWELL INTERNATIONAL INC.
    Inventor: Rajiv R. Singh
  • Publication number: 20120015922
    Abstract: 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: Application
    Filed: March 24, 2010
    Publication date: January 19, 2012
    Applicant: NATIONAL UNIVERSITY OF SINGAPORE
    Inventor: Wai Shiu Fred Wong
  • Publication number: 20120003273
    Abstract: 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 substituted
    Type: Application
    Filed: May 14, 2009
    Publication date: January 5, 2012
    Inventors: 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
  • Publication number: 20100331553
    Abstract: 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: Application
    Filed: September 25, 2008
    Publication date: December 30, 2010
    Applicant: Lachifarma S.R.L.-Laboratorio Chimico Farmaceutico
    Inventors: Luigi Villanova, Felicia Cisale, Azzurra Villanova, Luciano Villanova
  • 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: 7727545
    Abstract: 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: Grant
    Filed: February 22, 2006
    Date of Patent: June 1, 2010
    Assignee: Bausch & Lomb Incorporated
    Inventors: Joseph C. Salamone, Derek A. Schorzman
  • Publication number: 20100093651
    Abstract: 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: Application
    Filed: October 19, 2007
    Publication date: April 15, 2010
    Inventors: Lorraine V. Brando, Gary H. Posner, John G. D'Angelo, Robert H. Yolken, Christopher P. Hencken, Lauren Woodard
  • Publication number: 20100069474
    Abstract: 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 channels
    Type: Application
    Filed: November 24, 2009
    Publication date: March 18, 2010
    Inventors: Nareshkumar F. Jain, Zhihua Sui
  • Publication number: 20100061948
    Abstract: 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: Application
    Filed: January 9, 2008
    Publication date: March 11, 2010
    Inventors: Deok Hoon Park, Jong Sung Lee, Kwang Sun Jung, Eunsun Jung, Saebom Kim
  • Patent number: 7495026
    Abstract: Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmeutical formulations thereof.
    Type: Grant
    Filed: March 9, 2005
    Date of Patent: February 24, 2009
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Xihong Wang, Kenneth F. Bastow, Tian-Shung Wu
  • Patent number: 7208518
    Abstract: 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: Grant
    Filed: January 23, 2006
    Date of Patent: April 24, 2007
    Assignee: 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
  • Patent number: 6503941
    Abstract: 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: Grant
    Filed: February 22, 2002
    Date of Patent: January 7, 2003
    Assignee: Hanbul Cosmetics Co., Ltd.
    Inventors: Hyeong-Bae Pyo, Chung-Woo Lee, Sung-Min Park, Young-Ho Cho, Jeong-Jae Lee, Jin-Hwa Kim
  • Patent number: 5985913
    Abstract: 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: Grant
    Filed: April 29, 1998
    Date of Patent: November 16, 1999
    Assignee: 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
  • Patent number: 5216175
    Abstract: 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: Grant
    Filed: March 23, 1990
    Date of Patent: June 1, 1993
    Assignee: SRI International
    Inventors: Mitchell A. Avery, Wesley K. M. Chong, James E. Bupp
  • Patent number: 5019590
    Abstract: 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: Grant
    Filed: September 27, 1989
    Date of Patent: May 28, 1991
    Assignee: SRI International
    Inventors: Mitchell A. Avery, Wesley K. M. Chong
  • Patent number: 4997848
    Abstract: 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: Grant
    Filed: October 21, 1988
    Date of Patent: March 5, 1991
    Assignee: Sankyo Company, Limited
    Inventors: Masaaki Kurabayashi, Hiroshi Kogen, Hiroshi Kadokawa, Hideshi Kurihara, Kazuo Hasegawa, Masao Kuroda
  • Patent number: 4992561
    Abstract: 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: Grant
    Filed: May 11, 1990
    Date of Patent: February 12, 1991
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Ronald J. Roth, Nancy A. Roth
  • Patent number: 4963683
    Abstract: 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: Grant
    Filed: February 15, 1989
    Date of Patent: October 16, 1990
    Assignee: SRI International
    Inventors: Mitchell A. Avery, Clive Jennings-White