Tricyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/280)
  • Patent number: 11731951
    Abstract: A novel abyssomicin analogue compound and method of synthesizing the novel abyssomicin analogue compound are provided. The synthesis method includes the novel abyssomicin analogue compound being simply produced from a mixture of water and a co-solvent with linear precursors. The water molecules in the synthesis method can have dual roles, which are cyclisation followed by hydration via a unique mechanism. Abyssomicins are a family of spirotetronate natural products exhibiting promising bioactivities.
    Type: Grant
    Filed: March 6, 2023
    Date of Patent: August 22, 2023
    Assignee: KING FAISAL UNIVERSITY
    Inventor: Jawaher Alnawah
  • Patent number: 9381187
    Abstract: Methods and compositions for reducing radiation damage in a subject with analog or derivative of benzo[c]chromen-6-one.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: July 5, 2016
    Assignee: PALOMA PHARMACEUTICALS, INC.
    Inventor: David I. Sherris
  • Patent number: 9029572
    Abstract: A method of manufacturing a compound or a salt thereof expressed with a formula (III) below, characterized by causing a compound or a salt thereof expressed with a formula (I) below and a compound or a salt thereof expressed with a formula (II) below to react in the presence of carbonate and copper salt or in the presence of hydroxide salt, carbonate, and copper salt.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: May 12, 2015
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Kazuhiro Kudou, Noriyoshi Yamamoto, Masakazu Ban, Atsushi Ohno
  • Publication number: 20140296540
    Abstract: A method of manufacturing a compound or a salt thereof expressed with a formula (III) below, characterized by causing a compound or a salt thereof expressed with a formula (I) below and a compound or a salt thereof expressed with a formula (II) below to react in the presence of carbonate and copper salt or in the presence of hydroxide salt, carbonate, and copper salt.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Kazuhiro KUDOU, Noriyoshi Yamamoto, Masakazu Ban, Atsushi Ohno
  • Patent number: 8802869
    Abstract: A method of manufacturing a compound or a salt thereof expressed with a formula (III) below, characterized by causing a compound or a salt thereof expressed with a formula (I) below and a compound or a salt thereof expressed with a formula (II) below to react in the presence of carbonate and copper salt or in the presence of hydroxide salt, carbonate, and copper salt.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: August 12, 2014
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Kazuhiro Kudou, Noriyoshi Yamamoto, Masakazu Ban, Atsushi Ohno
  • Patent number: 8716496
    Abstract: Substituted sulfonated coumarins are expressed in the general formula (I), where: R1 is H, OH, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, R2 is H or a halogen, in particular fluorine, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, R1 and R2 being capable of together forming a ring, such as a substituted or unsubstituted aryl or furane, R3 is H or a halogen, in particular fluorine, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, where R4 is H, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or a substituted or unsubstituted aryl, and M is Na or K.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 6, 2014
    Assignees: Universite de Strasbourg
    Inventors: Antoine Drevelle, Sylvain Ladame, Majdi Najah, Estelle Mayot
  • Publication number: 20140105920
    Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 17, 2014
    Inventor: David Sherris
  • Publication number: 20140018415
    Abstract: Disclosed are methods, compounds, and compositions useful for increasing autophagy and promoting longevity. The methods, compounds, and compositions relate to urolithins and urolithin precursors and use thereof. Certain urolithins are represented by Formula I, while certain urolithin precursors are represented by Formula IV. The urolithin may be urolithin A, urolithin B, urolithin C, or urolithin D. The urolithin precursor may be ellagic acid or an ellagitannin. The methods include in vivo, ex vivo, and in vitro uses of the compounds and compositions.
    Type: Application
    Filed: June 27, 2013
    Publication date: January 16, 2014
    Inventors: Christopher Lawrence Rinsch, William Blanco-Bose, Bernard Schneider, Laurent Mouchiroud, Dongryeol Ryu, Penelope Andreux, Johan Auwerx
  • Publication number: 20130310576
    Abstract: A method of manufacturing a compound or a salt thereof expressed with a formula (III) below, characterized by causing a compound or a salt thereof expressed with a formula (I) below and a compound or a salt thereof expressed with a formula (II) below to react in the presence of carbonate and copper salt or in the presence of hydroxide salt, carbonate, and copper salt.
    Type: Application
    Filed: February 8, 2012
    Publication date: November 21, 2013
    Applicant: Santen Pharmaceutical Co., Ltd.
    Inventors: Kazuhiro Kudou, Noriyoshi Yamamoto, Masakazu Ban, Atsushi Ohno
  • Patent number: 8492564
    Abstract: The invention features salvinorin compositions that are selective for kappa opioid receptors; methods of treating mania by using a selective kappa receptor agonist; and methods of treating mood disorders, such as depressive disorders and manic disorders, using salvinorin compositions.
    Type: Grant
    Filed: December 14, 2009
    Date of Patent: July 23, 2013
    Assignees: The McLean Hospital Corporation, Temple University School of Medicine
    Inventors: Cecile Beguin, Justin Stephen Potuzak, Thomas Anthony Munro, Katharine K. Duncan, William A. Carlezon, Bruce M. Cohen, Lee-yuan Liu-Chen
  • Publication number: 20130183700
    Abstract: Substituted sulfonated coumarins are expressed in the general formula (I), where: R1 is H, OH, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, R2 is H or a halogen, in particular fluorine, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, R1 and R2 being capable of together forming a ring, such as a substituted or unsubstituted aryl or furane, R3 is H or a halogen, in particular fluorine, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, where R4 is H, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or a substituted or unsubstituted aryl, and M is Na or K.
    Type: Application
    Filed: September 16, 2011
    Publication date: July 18, 2013
    Applicants: UNIVERSITE DE STRASBOURG, ETS J. SOUFFLET
    Inventors: Antoine Drevelle, Sylvain Ladame, Majdi Najah, Estelle Mayot
  • Publication number: 20130116247
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: April 5, 2011
    Publication date: May 9, 2013
    Applicant: MANNKIND CORPORATION
    Inventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
  • Publication number: 20130102659
    Abstract: The invention relates to salvinorin compositions and uses thereof. Specifically, the invention relates to administering a salvinorin compound to produce vasodilatory effect and organ protective effect from hypoxia/ischemia and reperfusion. The invention further relates to treating various diseases or disorders.
    Type: Application
    Filed: June 29, 2011
    Publication date: April 25, 2013
    Inventor: Renyu Liu
  • Patent number: 8378125
    Abstract: This invention relates to substance FKI-3864 represented by the following formula [I] having an inhibitory activity on the synthesis of triacylglycerols and a method for preparing the same. The substance FKI-3864 can be prepared by a method comprising culturing a microorganism which belongs to the genus Penicillium and is capable of producing the substance FKI-3864, and particularly Penicillium pinophilum FKI-3864 (FERM BP-11093) so as to accumulate the substance FKI-3864 in the culture and collecting the substance FKI-3864 from the culture. The substance has an inhibitory activity on the synthesis of intracellular triacylglycerols and is useful for prevention or treatment of obesity.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: February 19, 2013
    Assignee: School Juridical Person Kitasato Institute
    Inventors: Hiroshi Tomoda, Ryuji Uchida, Rokuro Masuma, Satoshi Omura
  • Publication number: 20120245113
    Abstract: The use or methods of use of extracts comprising one or more special clerodane compounds against inflammatory (including allergic) diseases or conditions, as well as novel compounds of this type, said clerodane derivatives for use against inflammatory (including allergic) diseases or conditions, pharmaceutical formulations comprising them especially for use against inflammatory disease or conditions, and related embodiments; said extract and/or compound(s) for use in the treatment or in the preparation of a medicament (including a nutraceutical) for the prophylactic and/or therapeutic treatment of said disease or condition, as well as their preparation; pharmaceutical or nutraceutical formulations comprising said extract and/or natural compound(s) which are useful in said prophylactic and/or therapeutic treatment, and related embodiments.
    Type: Application
    Filed: February 22, 2012
    Publication date: September 27, 2012
    Applicant: BIOTROPICS MALAYSIA BHD
    Inventors: Matthias GEHLING, Torsten GROTHE, Ernst ROEMER, Peter REINEMER, Kathrin REINHARDT, Annie GEORGE, Nur Hanisah MOHTAR, Noorsyarida Mohd Sapiai
  • Publication number: 20120164243
    Abstract: Provided are compositions comprising compounds or precursors to compounds which may be used for a variety of therapeutic applications including, for example, treating and/or preventing a disease or disorder related to reduced or inadequate mitochondrial activity, including aging or stress, diabetes, obesity, and neurodegenerative diseases. The compounds relate generally to urolithins and precursors thereof, including but not limited to ellagitannins and urolithin A. In certain embodiments the compositions are presented in or as food products or nutritional supplements. These same compounds and compositions can also be used advantageously in generally healthy individuals to increase or maintain metabolic rate, decrease percent body fat, increase or maintain muscle mass, manage body weight, improve or maintain mental performance (including memory), improve or maintain muscle performance, improve or maintain mood, and manage stress.
    Type: Application
    Filed: December 23, 2011
    Publication date: June 28, 2012
    Applicant: Amazentis SA
    Inventors: Christopher L. Rinsch, William Blanco-Bose, Bernard Schneider, Charles Thomas, Carmen Sandi, Johan Auwerx, Penelope Andreux, Richardus Houtkooper, Eija Pirinen, Laurent Mouchiroud, David Genoux
  • Publication number: 20120122917
    Abstract: This invention discloses cannabinoid derivatives and pharmaceutical uses thereof.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Inventor: Craig Rick Travis
  • Patent number: 8168796
    Abstract: There are provided novel fluorescent agents, such as pyrazoline compounds represented by formula (I): (wherein R1, R2 and R3 are as defined in the specification), having an ethynyl group in the molecule, which have high absorptivity in the ultraviolet-visible short wavelength range (for example, 350 nm-420 nm).
    Type: Grant
    Filed: January 19, 2009
    Date of Patent: May 1, 2012
    Assignee: Nippon Chemical Works Co., Ltd.
    Inventors: Kazuhiko Mizuno, Hideyuki Takagaki, Hirokazu Iwahashi, Kaname Inoue
  • Patent number: 8148551
    Abstract: The invention relates to tricyclic aromatics of the general formula I in which A1, A2, A3, A4, Q1-Q2, R1, R2, X1, X2, X3, Z1, Z2, Z3, Z4, q, r, s, t and u have the meaning indicated, and to the use thereof as components of liquid-crystalline media and to an electro-optical display element containing same.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: April 3, 2012
    Assignee: Merck Patent Gesellschaft MIT Beschraenkter Haftung
    Inventors: Rudolf Eidenschink, Holger Kretzschmann
  • Publication number: 20120010219
    Abstract: The invention features salvinorin compositions that are selective for kappa opioid receptors; methods of treating mania by using a selective kappa receptor agonist; and methods of treating mood disorders, such as depressive disorders and manic disorders, using salvinorin compositions.
    Type: Application
    Filed: December 14, 2009
    Publication date: January 12, 2012
    Applicant: The McLean Hospital Corporation
    Inventors: Cecile Beguin, Justin Stephen Potuzak, Thomas Anthony Munro, Katherine K. Duncan, William A. Carlezon, Bruce M. Cohen, Lee-yuan Liu Chen
  • Publication number: 20110105769
    Abstract: This invention relates to substance FKI-3864 represented by the following formula [I] having an inhibitory activity on the synthesis of triacylglycerols and a method for preparing the same. The substance FKI-3864 can be prepared by a method comprising culturing a microorganism which belongs to the genus Penicillium and is capable of producing the substance FKI-3864, and particularly Penicillium pinophilum FKI-3864 (FERM BP-11093) so as to accumulate the substance FKI-3864 in the culture and collecting the substance FKI-3864 from the culture. The substance has an inhibitory activity on the synthesis of intracellular triacylglycerols and is useful for prevention or treatment of obesity.
    Type: Application
    Filed: February 12, 2009
    Publication date: May 5, 2011
    Applicant: SCHOOL JURIDICAL PERSON KITASATO INSTITUTE
    Inventors: Hiroshi Tomoda, Ryuji Uchida, Rokuro Masuma, Satoshi Omura
  • Publication number: 20100317045
    Abstract: Compounds used as dyes comperable to Alexa Fluor 350 dyes. The inventive compounds have high fluorescence quantum yield and high photostability. The dyes facilitate analysis of biological structures with enhanced sensitivity and selectivity.
    Type: Application
    Filed: June 16, 2009
    Publication date: December 16, 2010
    Applicant: PIERCE BIOTECHNOLOGY, INC.
    Inventors: Surbhi Desai, Boguslawa Dworecki, Matthias S. Wenzel, Peter T. Czerney, Frank G. Lehmann, Bernd G. Schweder, Wilhelm G. Frank
  • Patent number: 7846965
    Abstract: A compound is described. In particular, a non-steroidal sulphamate compound is described. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound is of general Formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein X is any one of S, NH, a substituted N, CH2, or a substituted C.
    Type: Grant
    Filed: February 26, 2007
    Date of Patent: December 7, 2010
    Assignee: Sterix Limited
    Inventors: Michael John Reed, Barry Victor Lloyd Potter
  • Publication number: 20100210678
    Abstract: Provided are non-steroidal tricyclic compounds that are modulators of androgen receptors and methods for making and using such compounds.
    Type: Application
    Filed: March 19, 2010
    Publication date: August 19, 2010
    Inventors: Lin Zhi, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Robert I. Higuchi
  • Publication number: 20100179217
    Abstract: The invention provides novel compounds of formula I: that are opioid receptor ligands. The invention also provides pharmaceutical compositions comprising such compounds as well as methods for treating diseases associated with opioid receptor function by administering such compounds to a mammal in need of treatment. Compounds of the invention are useful to modulate (e.g. agonize or antagonize) opioid receptor function.
    Type: Application
    Filed: November 2, 2007
    Publication date: July 15, 2010
    Applicant: University of Iowa Research Foundation
    Inventor: Thomas Prisinzano
  • Patent number: 7741365
    Abstract: Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites.
    Type: Grant
    Filed: December 29, 2005
    Date of Patent: June 22, 2010
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Atmaram Khanolkar
  • Patent number: 7728001
    Abstract: The invention provides novel compounds of formula I: that are opioid receptor ligands. The invention also provides pharmaceutical compositions comprising such compounds as well as methods for treating diseases associated with opioid receptor function by administering such compounds to a mammal in need of treatment. The invention also provides an improved method for isolating intermediate materials useful for obtaining compounds of formula I.
    Type: Grant
    Filed: September 12, 2005
    Date of Patent: June 1, 2010
    Assignee: University of Iowa Research Foundation
    Inventors: Thomas Prisinzano, Richard Brian Rothman
  • Patent number: 7687538
    Abstract: Compounds and compositions that are salvinorin A and salvinorin B derivatives that demonstrate selectivity and/or potency for the k-opioid receptor (KOR), allowing for their use as medicines, as well as chemical probes (both radiolabeled and cold) for fields utilizing the techniques of radiolabeled binding assays.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: March 30, 2010
    Assignees: University of Mississippi, Case Western Reserve University
    Inventors: Jordan Zjawiony, Hesham Fahmy, David Jeremy Stewart, Bryan Roth
  • Patent number: 7629475
    Abstract: The invention features salvinorin compositions that are selective for kappa opioid receptors; methods of treating mania by using a selective kappa receptor agonist; and methods of treating mood disorders, such as depressive disorders and manic disorders, using salvinorin compositions.
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: December 8, 2009
    Assignee: The McLean Hospital Corporation
    Inventors: Cécile Béquin, William A. Carlezon, Bruce M. Cohen, Minsheng He, David Yue-Wei Lee, Michele R. Richards, Lee-Yuan Liu-Chen
  • Publication number: 20090247620
    Abstract: The present invention relates to benzochromene derivatives of the formula I where the various parameters have the meaning indicated in the text, and to liquid-crystal media which comprise these compounds, and to the use of the media in electro-optical displays, in particular in TN, OCB, LCOS and/or IPS-LCDs, and to the use of the compounds and physiologically acceptable derivatives thereof as therapeutic active ingredients.
    Type: Application
    Filed: December 5, 2006
    Publication date: October 1, 2009
    Inventors: Andreas Taugerbeck, Elvira Montenegro, Atsutaka Manabe, Herbert Plach
  • 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
  • Publication number: 20090088466
    Abstract: The invention provides novel compounds of formula (I), (II), (III), and (IV). The invention also provides pharmaceutical compositions comprising such compounds as well as methods for treating diseases associated with opioid receptor function by administering such compounds to an animal in need of treatment. The invention also provides therapeutic methods for the use of compounds of formula (V), as well as methods for treating diseases by administering such compounds.
    Type: Application
    Filed: June 16, 2006
    Publication date: April 2, 2009
    Applicant: UNIVERSITY OF IOWA RESEARCH FOUNDATION
    Inventors: Laura M. Bohn, Thomas E. Prisinzano
  • Patent number: 7507395
    Abstract: Systems, including compositions and methods, for measuring pH, particularly in cells, organelles, and other samples. The compositions include pH-sensitive fluorescent and fluorogenic 2?,7?-dialkylfluorescein derivatives and associated nonfluorescent precursor compounds. The compositions may permit ratiometric measurement in the excitation spectrum and the emission spectrum. The methods include adding a precursor compound to a sample cell, incubating the sample cell to release the free indicator, illuminating the sample cell, and detecting the fluorescence response of the free indicator.
    Type: Grant
    Filed: October 4, 2004
    Date of Patent: March 24, 2009
    Assignee: MDS Analytical Technologies (US) Inc.
    Inventors: Zhenjun Diwu, Jesse J. Twu, Guoliang Yi, Luke D. Lavis, Yen-Wen Chen, Kelly J. Cassutt
  • Patent number: 7446229
    Abstract: Bicyclic-cannabinoids and methods of preparation and use are presented. These compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.
    Type: Grant
    Filed: December 12, 2006
    Date of Patent: November 4, 2008
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Atmaram D. Khanolkar, Ganeshsingh A. Thakur, Dai Lu
  • Publication number: 20080138651
    Abstract: High-molecular compounds comprising repeating units represented by the general formula (1) or (2) and having number-average molecular weights of 103 to 108 in terms of polystyrene: (1) [wherein Ar1 and Ar2 are each independently a trivalent aromatic hydrocarbon group or a trivalent heterocyclic group; and X1 and X2 are each independently O, S, C(?O), S(?O), SO2, C(R1)(R2), Si(R3)(R4), N(R5), B(R6), P(R7), or P(?O)(R8), with the provisos that X1 and X2 must not be the same and that X1 and Ar2 are bonded respectively to the adjacent carbon atoms constituting the aromatic ring of Ar1, and X2 and Ar1 are bonded respectively to the adjacent carbon atoms constituting the aromatic ring of Ar2] (2) [wherein Ar3 and Ar4 are each independently a trivalent aromatic hydrocarbon group or a trivalent heterocyclic group; and X3 and X4 are each independently N, B, P, C(R9), or Si(R10), with the provisos that X3 and X4 must not be the same and that X3 and Ar4 are bonded respectively to the adjacent carbon atoms constituting t
    Type: Application
    Filed: October 3, 2003
    Publication date: June 12, 2008
    Inventors: Shuji Doi, Satoshi Kobayashi, Takanobu Noguchi
  • Patent number: 7341715
    Abstract: The preparation for permanently deforming hair has a pH of 6.5 to 9.5 and contains, as keratin-reducing agent, a 2-mercaptopropion-amide of the formula (I): in which R1 and R2, independently of one another, represent H, a linear or branched alkylaminoalkyl group with 2 to 8 carbon atoms, or a morpholinoalkyl group with 2 to 3 carbon atoms in the alkyl portion of the morpholinoalkyl group, with the proviso that R1 and R2 are not simultaneously H, or that R1 and R2, together with the nitrogen atom, form a five-or six-membered heterocyclic ring, which optionally contain an additional N or O and are optionally substituted with one or two OH and/or methyl groups.
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: March 11, 2008
    Assignee: Wella AG
    Inventors: Beate Dannecker, Ursus Schweizer, Guenther Lang, Regina Ortmann, Wolfgang Hanefeld
  • Patent number: 7326447
    Abstract: The present invention relates to benzochromene derivatives of the formula I in which the various parameters are as defined in the text, and to liquid-crystal media which comprise these compounds, and to the use of the media in electro-optical displays, in particular in VAN LCDs.
    Type: Grant
    Filed: January 28, 2004
    Date of Patent: February 5, 2008
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Andreas Taugerbeck, Melanie Klasen-Memmer
  • Patent number: 7285683
    Abstract: Novel bicyclic-cannabinoids and hexahydrocannabinol analogs are presented. These compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response useful to treat a number of physiological conditions.
    Type: Grant
    Filed: January 31, 2006
    Date of Patent: October 23, 2007
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Spyridon P Nikas, Atmaram D Khanolkar
  • Patent number: 7183313
    Abstract: Novel tricyclic cannabinoid compounds are presented. Some of these compounds exhibit fluorescence properties. The fluorescent cannabinoid compounds are typically endogenously fluorescent. Some of these compounds, when administered in a therapeutically effective amount to an individual or animal, result in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response useful to treat a number of physiological conditions.
    Type: Grant
    Filed: August 25, 2003
    Date of Patent: February 27, 2007
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Dai Lu, Xin-Zhong Lai
  • Patent number: 7057076
    Abstract: Novel bicyclic-cannabinoids and hexahydrocannabinol analogs are presented. These compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response useful to treat a number of physiological conditions.
    Type: Grant
    Filed: July 11, 2002
    Date of Patent: June 6, 2006
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Spyridon P Nikas, Atmaram D Khanolkar
  • Patent number: 6995187
    Abstract: Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.
    Type: Grant
    Filed: October 18, 2000
    Date of Patent: February 7, 2006
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Atmaram Khanolkar
  • Patent number: 6939977
    Abstract: Disclosed are novel compounds represented by the following structural formula: R-X-Y; and physiologically acceptable salts thereof. R is a tricyclic core of a cannabinoid or substituted cannabinoid. X is a covalent bond, —CH2— or —CHR1—, wherein R1 a C1 to C3 substituted or unsubstituted alkyl group. Y is a heterocyclic ring, a substituted heterocyclic ring, a carbocyclic ring, a substituted carbocyclic ring, a fused bicyclic ring system, a substituted fused bicyclic ring system, a bridged bicyclic ring system, a substituted bridged bicyclic ring system, a bridged tricyclic ring system or a substituted bridged tricyclic ring system. Also disclosed is a method of stimulating a CB1 and/or CB2 receptor in a subject. The method comprises administering to the subject a therapeutically effective amount of R-X-Y.
    Type: Grant
    Filed: December 4, 2002
    Date of Patent: September 6, 2005
    Assignee: The University of Connecticut
    Inventors: Alexandros Makriyannis, Dai Lu, Atmaram Khanolkar
  • Patent number: 6936719
    Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: August 30, 2005
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
  • Patent number: 6800765
    Abstract: Systems, including compositions and methods, for measuring pH, particularly in cells, organelles, and other samples. The compositions include pH-sensitive fluorescent and fluorogenic 2′,7′-dialkylfluorescein derivatives and associated nonfluorescent precursor compounds. The compositions may permit ratiometric measurement in the excitation spectrum and the emission spectrum. The methods include adding a precursor compound to a sample cell, incubating the sample cell to release the free indicator, illuminating the sample cell, and detecting the fluorescence response of the free indicator.
    Type: Grant
    Filed: March 27, 2002
    Date of Patent: October 5, 2004
    Assignee: Molecular Devices Corporation
    Inventors: Zhenjun Diwu, Jesse J. Twu, Guoliang Yi, Luke D. Lavis, Yen-Wen Chen, Kelly J. Cassutt
  • Patent number: 6784204
    Abstract: This disclosure describes new antibiotic Cytosporacin having the structure: The invention relates to a new antibiotic designated Cytosporacin, to its production by fermentation, to methods for its recovery and concentration from the crude solutions, and to process for its purification. The invention includes within its scope the agent in dilute form, as a crude concentrate, and in pure form. The invention also relates to the use of the compound according to the invention in antimicrobial compositions and as antiseptics or disinfectants.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: August 31, 2004
    Assignee: Wyeth Holdings Corporation, Five Giralda Farms
    Inventors: Haiyin He, Jeffrey Edwin Janso
  • Publication number: 20030207344
    Abstract: Ethers and esters of cyanohydrins that contain optically detectable moieties are highly effective for detecting, monitoring, and measuring the activity of enzymes that cause the cleavage of certain types of substrates. The cyanohydrins function as proaldehydes and proketones, spontaneously converting to aldehydes and ketones, respectively, which provide a large increase in optical detectability relative to both the starting esters and ethers and the cyanohydrins.
    Type: Application
    Filed: January 7, 2003
    Publication date: November 6, 2003
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Bruce D. Hammock, Guomin Shan, Rong Zhang
  • Patent number: 6632835
    Abstract: Molecules demonstrating anti-proliferative effects against epithelial cancer cell lines and endothelial cells and methods of synthesis are disclosed. The molecules are intended for use in therapeutic preparations for the treatment of cancer through either anti-angiogenesis or other anti-cancer mechanisms. The compounds specified are 6H-dibenzo[b,d]pyran-6-one derivatives and have been shown to be antiproliferative against human endothelial cells.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: October 14, 2003
    Assignee: Nanodesign Inc.
    Inventors: Jonathan Martin Schmidt, Peter Redden, Julie Mercure, Shuguang Zhu, John Whelan, Natalie Lazarowych
  • Patent number: 6613797
    Abstract: Therapeutic compounds and compositions for the treatment of infectious diseases are disclosed. The compounds are xanthones and xanthone derivatives, such as 3,5-bis-&egr;-(N,N-diethylamino)amyloxyxanthone. The described compositions include such compounds and a pharmaceutical carrier. These compositions also can include additional materials conventionally used to form therapeutic compositions. 3,5-bis-&egr;-(N,N-diethylamino)amyloxyxanthone has an IC50 for Plasmodium falciparum of about 0.15 &mgr;M, and an IC50 for Leishmania mexicana of <<0.5 &mgr;M. These compositions are additionally useful for forming soluble complexes with heme and porphyrins.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: September 2, 2003
    Assignee: Interlab, Inc.
    Inventors: Rolf W. Winter, Michael K. Riscoe, David J. Hinrichs
  • Publication number: 20030031736
    Abstract: A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.
    Type: Application
    Filed: July 11, 2002
    Publication date: February 13, 2003
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Dirk Lichtblau, Nina Berova, John Berger, Koji Nakanishi
  • Publication number: 20020115711
    Abstract: Molecules demonstrating anti-proliferative effects against epithelial cancer cell lines and endothelial cells and methods of synthesis are disclosed. The molecules are intended for use in therapeutic preparations for the treatment of cancer through either anti-angiogenesis or other anti-cancer mechanisms. The compounds specified are 6H-dibenzo[b,d]pyran-6-one derivatives and have been shown to be antiproliferative against human endothelial cells.
    Type: Application
    Filed: August 21, 2001
    Publication date: August 22, 2002
    Inventors: Johnathan Martin Schmidt, Peter Redden, Julie Mercure, Shuguang Zhu, John Whelan, Natalie Lazarowych