Tricyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/280)
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Patent number: 11731951Abstract: 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: GrantFiled: March 6, 2023Date of Patent: August 22, 2023Assignee: KING FAISAL UNIVERSITYInventor: Jawaher Alnawah
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Patent number: 9381187Abstract: Methods and compositions for reducing radiation damage in a subject with analog or derivative of benzo[c]chromen-6-one.Type: GrantFiled: February 16, 2012Date of Patent: July 5, 2016Assignee: PALOMA PHARMACEUTICALS, INC.Inventor: David I. Sherris
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Patent number: 9029572Abstract: 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: GrantFiled: June 13, 2014Date of Patent: May 12, 2015Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuhiro Kudou, Noriyoshi Yamamoto, Masakazu Ban, Atsushi Ohno
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Publication number: 20140296540Abstract: 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: ApplicationFiled: June 13, 2014Publication date: October 2, 2014Inventors: Kazuhiro KUDOU, Noriyoshi Yamamoto, Masakazu Ban, Atsushi Ohno
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Patent number: 8802869Abstract: 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: GrantFiled: February 8, 2012Date of Patent: August 12, 2014Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuhiro Kudou, Noriyoshi Yamamoto, Masakazu Ban, Atsushi Ohno
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Patent number: 8716496Abstract: 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: GrantFiled: September 16, 2011Date of Patent: May 6, 2014Assignees: Universite de StrasbourgInventors: Antoine Drevelle, Sylvain Ladame, Majdi Najah, Estelle Mayot
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Publication number: 20140105920Abstract: 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: ApplicationFiled: May 23, 2013Publication date: April 17, 2014Inventor: David Sherris
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Publication number: 20140018415Abstract: 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: ApplicationFiled: June 27, 2013Publication date: January 16, 2014Inventors: Christopher Lawrence Rinsch, William Blanco-Bose, Bernard Schneider, Laurent Mouchiroud, Dongryeol Ryu, Penelope Andreux, Johan Auwerx
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Publication number: 20130310576Abstract: 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: ApplicationFiled: February 8, 2012Publication date: November 21, 2013Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Kazuhiro Kudou, Noriyoshi Yamamoto, Masakazu Ban, Atsushi Ohno
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Patent number: 8492564Abstract: 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: GrantFiled: December 14, 2009Date of Patent: July 23, 2013Assignees: The McLean Hospital Corporation, Temple University School of MedicineInventors: Cecile Beguin, Justin Stephen Potuzak, Thomas Anthony Munro, Katharine K. Duncan, William A. Carlezon, Bruce M. Cohen, Lee-yuan Liu-Chen
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Publication number: 20130183700Abstract: 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: ApplicationFiled: September 16, 2011Publication date: July 18, 2013Applicants: UNIVERSITE DE STRASBOURG, ETS J. SOUFFLETInventors: Antoine Drevelle, Sylvain Ladame, Majdi Najah, Estelle Mayot
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Publication number: 20130116247Abstract: 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: ApplicationFiled: April 5, 2011Publication date: May 9, 2013Applicant: MANNKIND CORPORATIONInventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
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Publication number: 20130102659Abstract: 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: ApplicationFiled: June 29, 2011Publication date: April 25, 2013Inventor: Renyu Liu
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Patent number: 8378125Abstract: 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: GrantFiled: February 12, 2009Date of Patent: February 19, 2013Assignee: School Juridical Person Kitasato InstituteInventors: Hiroshi Tomoda, Ryuji Uchida, Rokuro Masuma, Satoshi Omura
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Publication number: 20120245113Abstract: 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: ApplicationFiled: February 22, 2012Publication date: September 27, 2012Applicant: BIOTROPICS MALAYSIA BHDInventors: Matthias GEHLING, Torsten GROTHE, Ernst ROEMER, Peter REINEMER, Kathrin REINHARDT, Annie GEORGE, Nur Hanisah MOHTAR, Noorsyarida Mohd Sapiai
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Publication number: 20120164243Abstract: 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: ApplicationFiled: December 23, 2011Publication date: June 28, 2012Applicant: Amazentis SAInventors: Christopher L. Rinsch, William Blanco-Bose, Bernard Schneider, Charles Thomas, Carmen Sandi, Johan Auwerx, Penelope Andreux, Richardus Houtkooper, Eija Pirinen, Laurent Mouchiroud, David Genoux
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Publication number: 20120122917Abstract: This invention discloses cannabinoid derivatives and pharmaceutical uses thereof.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Inventor: Craig Rick Travis
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Patent number: 8168796Abstract: 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: GrantFiled: January 19, 2009Date of Patent: May 1, 2012Assignee: Nippon Chemical Works Co., Ltd.Inventors: Kazuhiko Mizuno, Hideyuki Takagaki, Hirokazu Iwahashi, Kaname Inoue
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Patent number: 8148551Abstract: 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: GrantFiled: December 29, 2006Date of Patent: April 3, 2012Assignee: Merck Patent Gesellschaft MIT Beschraenkter HaftungInventors: Rudolf Eidenschink, Holger Kretzschmann
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Publication number: 20120010219Abstract: 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: ApplicationFiled: December 14, 2009Publication date: January 12, 2012Applicant: The McLean Hospital CorporationInventors: Cecile Beguin, Justin Stephen Potuzak, Thomas Anthony Munro, Katherine K. Duncan, William A. Carlezon, Bruce M. Cohen, Lee-yuan Liu Chen
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Publication number: 20110105769Abstract: 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: ApplicationFiled: February 12, 2009Publication date: May 5, 2011Applicant: SCHOOL JURIDICAL PERSON KITASATO INSTITUTEInventors: Hiroshi Tomoda, Ryuji Uchida, Rokuro Masuma, Satoshi Omura
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Publication number: 20100317045Abstract: 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: ApplicationFiled: June 16, 2009Publication date: December 16, 2010Applicant: PIERCE BIOTECHNOLOGY, INC.Inventors: Surbhi Desai, Boguslawa Dworecki, Matthias S. Wenzel, Peter T. Czerney, Frank G. Lehmann, Bernd G. Schweder, Wilhelm G. Frank
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Patent number: 7846965Abstract: 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: GrantFiled: February 26, 2007Date of Patent: December 7, 2010Assignee: Sterix LimitedInventors: Michael John Reed, Barry Victor Lloyd Potter
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Publication number: 20100210678Abstract: Provided are non-steroidal tricyclic compounds that are modulators of androgen receptors and methods for making and using such compounds.Type: ApplicationFiled: March 19, 2010Publication date: August 19, 2010Inventors: Lin Zhi, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Robert I. Higuchi
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Publication number: 20100179217Abstract: 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: ApplicationFiled: November 2, 2007Publication date: July 15, 2010Applicant: University of Iowa Research FoundationInventor: Thomas Prisinzano
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Patent number: 7741365Abstract: Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites.Type: GrantFiled: December 29, 2005Date of Patent: June 22, 2010Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Atmaram Khanolkar
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Patent number: 7728001Abstract: 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: GrantFiled: September 12, 2005Date of Patent: June 1, 2010Assignee: University of Iowa Research FoundationInventors: Thomas Prisinzano, Richard Brian Rothman
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Patent number: 7687538Abstract: 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: GrantFiled: July 29, 2005Date of Patent: March 30, 2010Assignees: University of Mississippi, Case Western Reserve UniversityInventors: Jordan Zjawiony, Hesham Fahmy, David Jeremy Stewart, Bryan Roth
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Patent number: 7629475Abstract: 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: GrantFiled: March 14, 2005Date of Patent: December 8, 2009Assignee: The McLean Hospital CorporationInventors: Cécile Béquin, William A. Carlezon, Bruce M. Cohen, Minsheng He, David Yue-Wei Lee, Michele R. Richards, Lee-Yuan Liu-Chen
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Publication number: 20090247620Abstract: 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: ApplicationFiled: December 5, 2006Publication date: October 1, 2009Inventors: Andreas Taugerbeck, Elvira Montenegro, Atsutaka Manabe, Herbert Plach
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Publication number: 20090203725Abstract: 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: ApplicationFiled: December 21, 2006Publication date: August 13, 2009Inventors: Cornelis Arjan Van Oeveren, Yixing Shen, Shuo Zhao, Lin Zhi
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Publication number: 20090088466Abstract: 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: ApplicationFiled: June 16, 2006Publication date: April 2, 2009Applicant: UNIVERSITY OF IOWA RESEARCH FOUNDATIONInventors: Laura M. Bohn, Thomas E. Prisinzano
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Patent number: 7507395Abstract: 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: GrantFiled: October 4, 2004Date of Patent: March 24, 2009Assignee: MDS Analytical Technologies (US) Inc.Inventors: Zhenjun Diwu, Jesse J. Twu, Guoliang Yi, Luke D. Lavis, Yen-Wen Chen, Kelly J. Cassutt
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Patent number: 7446229Abstract: 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: GrantFiled: December 12, 2006Date of Patent: November 4, 2008Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Spyridon P. Nikas, Atmaram D. Khanolkar, Ganeshsingh A. Thakur, Dai Lu
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Publication number: 20080138651Abstract: 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 tType: ApplicationFiled: October 3, 2003Publication date: June 12, 2008Inventors: Shuji Doi, Satoshi Kobayashi, Takanobu Noguchi
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Patent number: 7341715Abstract: 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: GrantFiled: May 21, 2001Date of Patent: March 11, 2008Assignee: Wella AGInventors: Beate Dannecker, Ursus Schweizer, Guenther Lang, Regina Ortmann, Wolfgang Hanefeld
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Patent number: 7326447Abstract: 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: GrantFiled: January 28, 2004Date of Patent: February 5, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Andreas Taugerbeck, Melanie Klasen-Memmer
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Patent number: 7285683Abstract: 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: GrantFiled: January 31, 2006Date of Patent: October 23, 2007Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Spyridon P Nikas, Atmaram D Khanolkar
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Patent number: 7183313Abstract: 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: GrantFiled: August 25, 2003Date of Patent: February 27, 2007Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Dai Lu, Xin-Zhong Lai
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Patent number: 7057076Abstract: 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: GrantFiled: July 11, 2002Date of Patent: June 6, 2006Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Spyridon P Nikas, Atmaram D Khanolkar
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Patent number: 6995187Abstract: 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: GrantFiled: October 18, 2000Date of Patent: February 7, 2006Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Atmaram Khanolkar
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Patent number: 6939977Abstract: 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: GrantFiled: December 4, 2002Date of Patent: September 6, 2005Assignee: The University of ConnecticutInventors: Alexandros Makriyannis, Dai Lu, Atmaram Khanolkar
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Patent number: 6936719Abstract: 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: GrantFiled: December 18, 2003Date of Patent: August 30, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
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Patent number: 6800765Abstract: 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: GrantFiled: March 27, 2002Date of Patent: October 5, 2004Assignee: Molecular Devices CorporationInventors: Zhenjun Diwu, Jesse J. Twu, Guoliang Yi, Luke D. Lavis, Yen-Wen Chen, Kelly J. Cassutt
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Patent number: 6784204Abstract: 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: GrantFiled: October 14, 2003Date of Patent: August 31, 2004Assignee: Wyeth Holdings Corporation, Five Giralda FarmsInventors: Haiyin He, Jeffrey Edwin Janso
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Publication number: 20030207344Abstract: 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: ApplicationFiled: January 7, 2003Publication date: November 6, 2003Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Bruce D. Hammock, Guomin Shan, Rong Zhang
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Patent number: 6632835Abstract: 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: GrantFiled: August 21, 2001Date of Patent: October 14, 2003Assignee: Nanodesign Inc.Inventors: Jonathan Martin Schmidt, Peter Redden, Julie Mercure, Shuguang Zhu, John Whelan, Natalie Lazarowych
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Patent number: 6613797Abstract: 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: GrantFiled: December 1, 2000Date of Patent: September 2, 2003Assignee: Interlab, Inc.Inventors: Rolf W. Winter, Michael K. Riscoe, David J. Hinrichs
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Publication number: 20030031736Abstract: 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: ApplicationFiled: July 11, 2002Publication date: February 13, 2003Applicant: The Trustees of Columbia University in the City of New YorkInventors: Dirk Lichtblau, Nina Berova, John Berger, Koji Nakanishi
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Publication number: 20020115711Abstract: 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: ApplicationFiled: August 21, 2001Publication date: August 22, 2002Inventors: Johnathan Martin Schmidt, Peter Redden, Julie Mercure, Shuguang Zhu, John Whelan, Natalie Lazarowych