Plural Ring Oxygens In The Tricyclo Ring System Patents (Class 549/282)
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Patent number: 10487094Abstract: A compound having the following formula (I): is disclosed. A method of preparing the compound of formula (I) is also disclosed.Type: GrantFiled: September 3, 2018Date of Patent: November 26, 2019Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Chengyuan Liang, Yuzhi Liu, Danni Tian, Jie Li, Songsong Ruan, Han Li, Qianqian Zhao, Xuechuan Wang, Xeufeng Chen
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Patent number: 9671393Abstract: The present invention provides isolated, non-viable bacterial cells comprising a plurality of nucleic acid crosslinks, methods for making said cells, and methods for using said cells to isolate DNA-protein complexes. In particular, the nucleic acids of the cells are crosslinked by contacting the cells with a furocoumarin compound and ultraviolet light.Type: GrantFiled: September 2, 2011Date of Patent: June 6, 2017Assignee: SIGMA-ALDRICH CO., LLCInventors: Vikas B. Palhan, Carol Kreader, Ernie Mueller
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Patent number: 9433219Abstract: The disclosure describes fungal organisms and preparations useful for inhibiting infection by Xylella sp. and in the treatment of Pierce's Disease.Type: GrantFiled: April 20, 2012Date of Patent: September 6, 2016Assignee: The Regents of the University of CaliforniaInventors: Philippe Rolshausen, Mary Caroline Roper
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Patent number: 8951561Abstract: The use of plasmonics enhanced photospectral therapy (PEPST) and exiton-plasmon enhanced phototherapy (EPEP) in the treatment of various cell proliferation disorders, and the PEPST and EPEP agents and probes used therein.Type: GrantFiled: February 20, 2009Date of Patent: February 10, 2015Assignees: Duke University, ImmunolightInventors: Tuan Vo-Dinh, Frederic A. Bourke, Jr.
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Patent number: 8907109Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferatType: GrantFiled: January 11, 2013Date of Patent: December 9, 2014Assignees: Immunolight, LLC, Duke UniversityInventors: Eric Toone, David Gooden, Tuan Vo-Dinh, Frederic A. Bourke, Jr.
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Patent number: 8791275Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferatType: GrantFiled: January 11, 2013Date of Patent: July 29, 2014Assignees: Duke University, Immunolight, LLCInventors: Eric Toone, David Gooden, Tuan Vo-Dinh, Frederic A. Bourke, Jr.
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Publication number: 20140171455Abstract: Methods for deterring microglia-mediated neurotoxicity in a human or non-human animal subjects comprising the step of inhibiting or blocking the intermediate-conductance calcium-activated potassium channel Kv1.3 in microglia, such as in subjects how suffer from neurodegenerative diseases (e.g., Alzheimer's Disease) or ischemic/anoxic/hypoxic conditions. The inhibition or blocking of the KCa1.3 channels may be accomplished by administering a substance that inhibits Kv1.3 in microglia. Examples of Kv1.3 inhibiting substances include certain 5-phenoxyalkoxypsoralens, such as (4-Phenoxybutoxy)psoralen (PAP-1) as well as certain 4-phenoxybutoxy-substituted heterocyclic compounds.Type: ApplicationFiled: June 8, 2012Publication date: June 19, 2014Applicant: The Regents of the University of CaliforniaInventors: Heike Wulff, Lee-Way Jin, Izumi Meezawa
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Publication number: 20130281652Abstract: The present invention relates to compounds of formula I, which are functionalized phenolic compounds, and polymers formed from the same. Ar—[O—(X)p—R?]q??I Polymers formed from the functionalized phenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.Type: ApplicationFiled: October 17, 2012Publication date: October 24, 2013Inventor: Rao S. Bezwada
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Patent number: 8420836Abstract: An NFAT signal inhibitor and the like are provided. An NFAT signal inhibitor and the like, containing, as an active ingredient, at least one compound selected from the group consisting of a coumarin derivative represented by formula [where in the formula (I), R1 and R2, which may be identical with or different from each other, each represent a hydrogen atom or a group represented by formula (II) (where in the formula (II), R3 represents a linear or branched alkyl or alkenyl group having 1 to 20 carbon atoms)] and pharmacologically acceptable salts thereof.Type: GrantFiled: October 21, 2009Date of Patent: April 16, 2013Assignee: Kao CorporationInventors: Mitsuyoshi Sakasai, Yusuke Shibuya, Azumi Nagasawa
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Patent number: 8383836Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferatType: GrantFiled: April 20, 2010Date of Patent: February 26, 2013Assignees: Duke University, Immunolight, LLCInventors: Eric Toone, David Gooden, Tuan Vo-Dinh, Frederic A. Bourke, Jr.
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Publication number: 20120323022Abstract: The present invention relates to a compound of (2?S)-columbianetin having photo-protective effect isolated from Corydalis heterocarpa and a cosmetic composition containing the same, which has great effects on prevention and treatment in UVB-induced skin damage.Type: ApplicationFiled: June 13, 2012Publication date: December 20, 2012Inventors: Se Kwon KIM, Chang Suk Kong, Young Wan Seo, Jung Ae Kim, Byul Nim Ahn
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Publication number: 20120277297Abstract: The present invention relates to pharmaceutical composition comprising the naturally occurring compounds selected from (±) Marrnesin, Columbianetin, Dihydroxanthyletin and substituted coumarin derivatives of 7-allyloxy coumarin, 7-benzyloxy coumarin, 7 -methoxycoumarin, 7-acetyloxy coumarin, 4-methyl-7-hydroxy coumarin and 4-methyl-7-acetyloxy coumarin. The said compositions possess a high degree of acetylcholinesterase inhibitory (AChE) property.Type: ApplicationFiled: April 30, 2012Publication date: November 1, 2012Applicant: Council of Scientific and Industrial ResearchInventors: Janaswamy Madhusudana Rao, Bhimapaka China Raju, Pullela Venkata Srinivas, Katragadda Suresh Babu, Jhillu Singh Yadav, Kondapuram Vijaya Raghvan, Hemant Kumar Singh, Chandiswar Nath
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Patent number: 8071642Abstract: Water-soluble dimethyl amino ethyl ether psoralens useful in the treatment of proliferative skin disorders, microbial infections and diseases, disorders of the blood and bone marrow of mammals and in microbiocidal compositions for sterilization of blood and blood products and surgical implants and inhibition of microbial growth in industrial applications are provided.Type: GrantFiled: June 27, 2008Date of Patent: December 6, 2011Assignees: Rutgers, The State University of New Jersey, University of Medicine and Dentistry of New Jersey, Lehigh UniversityInventors: Jeffrey D. Laskin, Diane E. Heck, Ned D. Heindel
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Patent number: 8067460Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).Type: GrantFiled: July 6, 2009Date of Patent: November 29, 2011Assignee: The Regents of the University of CalifoniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Publication number: 20110263695Abstract: An NFAT signal inhibitor and the like are provided. An NFAT signal inhibitor and the like, containing, as an active ingredient, at least one compound selected from the group consisting of a coumarin derivative represented by formula [where in the formula (I), R1 and R2, which may be identical with or different from each other, each represent a hydrogen atom or a group represented by formula (II) (where in the formula (II), R3 represents a linear or branched alkyl or alkenyl group having 1 to 20 carbon atoms)] and pharmacologically acceptable salts thereof.Type: ApplicationFiled: October 21, 2009Publication date: October 27, 2011Applicant: KAO CORPORATIONInventors: Mitsuyoshi Sakasai, Yusuke Shibuya, Azumi Nagasawa
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Publication number: 20100330009Abstract: The present invention relates to derivatives of the 1H-pyrano[4,3-b]benzofuran-1-one structure and their nitrogen analogues which possess powerful antioxidant properties combined with a highly effective UV absorbing functionality in one molecule. These compounds are especially useful in cosmetical and dermatological formulations.Type: ApplicationFiled: February 29, 2008Publication date: December 30, 2010Applicant: CIBA CORPORATIONInventors: Barbara Wagner, Sebastien Mongiat, Bernd Herzog, Werner Baschong, Andreas Buthe, Reinhold Ohrlein
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TETRACYCLIC DIPYRANO-COUMARIN COMPOUNDS WITH ANTI-HIV AND ANTI-MYCOBACTERIUM TUBERCULOSIS ACTIVITIES
Publication number: 20100324067Abstract: The present invention relates to tetracyclodipyrano-coumarin compounds of general formula (I), wherein the substituents are defined herein. These compounds exihibit dual biological activities of anti human immunodeficiency virus type 1 (HIV-1) infection and anti-Mycobacterium Tuberculosis (TB) infection.Type: ApplicationFiled: November 5, 2007Publication date: December 23, 2010Inventors: Gang Liu, Hai Xue, Tao Ma, Ziwei Chen, Lin Wang -
Publication number: 20100234467Abstract: The present invention provides a method for improving the bioavailability of a renin inhibitor, preferably, of a ?-amino-?-hydroxy-?-aryl-alkanoic acid derivative, which method comprises co-administering to a mammal, especially a human, in need of such treatment, a combination of a renin inhibitor, or a pharmaceutically acceptable salt thereof, and an MDR1 inhibitor selected from a non-pharmacologically active compound.Type: ApplicationFiled: November 23, 2007Publication date: September 16, 2010Inventors: Isabel Ottinger, Gian P. Camenisch, Gerhard Gross, Thomas Faller
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Patent number: 7772408Abstract: Compositions of matter comprising 5-phenylalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or veterinary patients, including autoimmune diseases such as multiple sclerosis. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition.Type: GrantFiled: August 29, 2003Date of Patent: August 10, 2010Assignee: The Regents of the University of CaliforniaInventors: Julia Vennekamp, Heike Wulff, K. George Chandy, Stephan Grissmer, Wolfram Hansel
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Publication number: 20100121059Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).Type: ApplicationFiled: July 6, 2009Publication date: May 13, 2010Applicant: The Regents of the University of CaliforniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Publication number: 20090292012Abstract: A therapeutic agent or prophylactic agent for a disease requiring an anti-foaming action for a cell and/or an inhibitory action for acyl-CoA cholesterol acyltransferase in treatment or prevention, characterized in that the therapeutic agent or prophylactic agent comprises as an effective ingredient a processed product derived from Peucedanum japonicum.Type: ApplicationFiled: January 26, 2006Publication date: November 26, 2009Inventors: Tatsuji Enoki, Yoko Kudo, Katsumi Sugiyama, Hiromu Ohnogi, Hiroaki Sagawa, Ikunoshin Kato
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Patent number: 7557138Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).Type: GrantFiled: October 4, 2004Date of Patent: July 7, 2009Assignee: The Regents of the University of CaliforniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Publication number: 20090155224Abstract: Water-soluble dimethyl amino ethyl ether psoralens useful in the treatment of proliferative skin disorders, microbial infections and diseases, disorders of the blood and bone marrow of mammals and in microbiocidal compositions for sterilization of blood and blood products and surgical implants and inhibition of microbial growth in industrial applications are provided.Type: ApplicationFiled: June 27, 2008Publication date: June 18, 2009Inventors: Jeffrey D. Laskin, Diane E. Heck, Ned D. Heindel
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Patent number: 7498449Abstract: The invention comprises compounds of Formula 1: wherein, R1 is independently H or halogen; R2 is, for example, H or —R10—NR11R12, and wherein R10 is C1-C6 alkyl, and R11 and R12 are independently H, C1-C4 alkyl, and hydrates, solvates, salts and tautomers thereof. The invention further comprises methods for making the compounds of the invention and methods for making compounds useful in the treatment or prevention of cardiac arrhythmia from the compounds of the invention.Type: GrantFiled: July 14, 2006Date of Patent: March 3, 2009Assignee: ARYx TherapeuticsInventors: Pascal Druzgala, Jien-Heh J. Tien, Arthur J. Cooper, Cyrus Becker
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Patent number: 7473789Abstract: The object of the present invention is to provide an antibacterial agent which has an improved antibacterial effect and a wider antibacterial spectrum than conventional antibacterial agents, and which is highly safe to human and the environment. This object is achieved with a novel substance 9-(1?,5?-dimethyl-1?-vinyl-4?-hexenyl)-4-hydroxy-7H-furo[3,2-?][1]benzopyran-7-one and an antibacterial agent comprising thereof.Type: GrantFiled: August 30, 2005Date of Patent: January 6, 2009Assignee: Takasago International CorporationInventors: Ryo Takeuchi, Tadahiro Hiramoto
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Patent number: 7384975Abstract: The invention relates to novel compounds of the formula (I) including all their tautomers, to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof, and to processes and reactive intermediates for the preparation of the compounds of the formula (II) including all their stereoisomers and tautomers to the use of the compounds of the formula (II) as suitable precursors for the preparation of the compounds of the formula (I) as well as to use of the compounds of the formula (I) and of the compounds of the formula (II) as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diesases and conditions in humans.Type: GrantFiled: January 20, 2006Date of Patent: June 10, 2008Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb d.o.o.Inventors: Mladen Mercep, Milan Mesic, Boska Hrvacic, Ivaylo Jivkov Elenkov, Ivica Malnar, Stribor Markovic, Lidija Simicic, Andreja Cempuh Klonkay, Anita Filipovic
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Publication number: 20080081918Abstract: The object of the present invention is to provide an antibacterial agent which has an improved antibacterial effect and a wider antibacterial spectrum than conventional antibacterial agents, and which is highly safe to human and the environment. This object is achieved with a novel substance 9-(1?,5?-dimethyl-1?-vinyl-4?-hexenyl)-4-hydroxy-7H-furo[3,2-?] [1]benzopyran-7-one and an antibacterial agent comprising thereof.Type: ApplicationFiled: August 30, 2005Publication date: April 3, 2008Inventors: Ryo Takeuchi, Tadahiro Hiramoto
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Patent number: 7208518Abstract: The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers thereof, to the pharmaceutically acceptable salts and solvates thereof, to the processes and reactive intermediates for their preparation and to their use in the prophylaxis and treatment of asthma and other inflammatory diseases and/or conditions in humans.Type: GrantFiled: January 23, 2006Date of Patent: April 24, 2007Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.Inventors: Mladen Mercep, Milan Mesic, Boska Hrvacic, Ivaylo Jivkov Elenkov, Ivica Malnar, Stribor Markovic, Lidija Simicic, Andreja Cempuh Klonkay, Anita Filipovic
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Patent number: 7115655Abstract: The present invention relates to compounds of the following formula (I) or pharmaceutically acceptable salts thereof. The present invention also relates to use for a cognitive-enhancing agent of compounds of the following formula (I) or pharmaceutically acceptable salts thereof and to a process for preparing the same. Further, the present invention relates to use for a congnitive-enhancing agent of decursin of the following formula (II) or pharmaceutically acceptable salts thereof. In addition, the present invention relates to extracts of Angelica gigantis Radix comprising decursin of the following formula (II), having cognitive-enhancing effects.Type: GrantFiled: April 9, 2002Date of Patent: October 3, 2006Assignee: Elcom Biotechnology, Co. Ltd.Inventors: Jeong-Seon Yoon, Ji-Young Lee, Young-Choong Kim, Ki-Yong Lee, Sang-Hyun Sung, Hak-Joong Kim, So-Young Kang
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Patent number: 7094378Abstract: Methods and apparatuses for treating fluids to inactivate microorganisms which may be present therein, said fluid containing one or more components selected from the group consisting of protein, blood and blood constituents are provided. The methods comprise adjusting the percentage of plasma in said fluid to a desired value; mixing an inactivation-effective, substantially non-toxic amount of an endogenous photosensitizer or endogenously-based derivative photosensitizer to said fluid; exposing said fluid to photoradiation of sufficient wavelength and energy to activate the photosensitizer, whereby said microorganisms are inactivated.Type: GrantFiled: June 15, 2000Date of Patent: August 22, 2006Assignee: Gambro, Inc.Inventors: Raymond Paul Goodrich, Jr., Dennis Hlavinka
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Patent number: 6924373Abstract: The present invention relates to DNA labeling reagents comprising a furocoumarin derivative and a detectable group with or without bound via a binding enhancer, and acridinium-9-carboxamide derivatives for use as chemiluminescent labels. The present invention also relates to a process of preparing DNA labeling compound.Type: GrantFiled: May 2, 2003Date of Patent: August 2, 2005Assignee: AsiaGen CorporationInventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
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Patent number: 6858742Abstract: The present invention relates to DNA labeling reagents comprising a furocoumarin derivative and a detectable group with or without bound via a binding enhancer, and acridinium-9-carboxamide derivatives for use as chemiluminescent labels. The present invention also relates to a process of preparing DNA labeling compound.Type: GrantFiled: October 22, 2003Date of Patent: February 22, 2005Assignee: AsiaGEN CorporationInventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
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Publication number: 20040162337Abstract: Chemical compounds of the general formula 1Type: ApplicationFiled: January 30, 2003Publication date: August 19, 2004Inventors: Wang Fun Fong, Yiu Cheong Jimmy Wu
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Patent number: 6768007Abstract: 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following formula: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R1, R2, R3, R4, X, and Z are set in the specification. The invention is also directed to pharmaceuticals compositions comprising one or more compounds of Formula I, optionally further comprising one or more anti-viral agents or immunostimulating agents. Further, the invention is directed to the use of compounds of Formula I for the inhibition of a retroviral infection in cells or tissue of an animal, for the treatment of a patient suffering from a retroviral-related pathology, for the prevention of transmission of HIV infection from an HIV infected pregnant woman to a fetus, and for the prevention of transmission of HIV infection during sexual intercourse.Type: GrantFiled: March 13, 2002Date of Patent: July 27, 2004Assignees: Panacos Pharmaceuticals, Inc., The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Lan Xie, Graham P. Allaway, Carl T. Wild
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Patent number: 6734313Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.Type: GrantFiled: May 9, 2003Date of Patent: May 11, 2004Assignee: Bioavailability Systems, LLCInventors: Robert Seemayer, Jack Liang
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Publication number: 20040029897Abstract: Compounds and methods for inactivating pathogens in materials are described, including compositions and methods for inactivating pathogens in biological materials such as red blood cell preparations and plasma. The compounds and methods may be used to treat materials intended for in vitro or in vivo use, such as clinical testing or transfusion. The compounds are designed to specifically bind to and react with nucleic acid, and then to degrade to form breakdown products. The degradation reaction is preferably slower than the reaction with nucleic acid.Type: ApplicationFiled: January 13, 2003Publication date: February 12, 2004Applicant: Cerus CorporationInventors: David Cook, John E. Merritt, Aileen Nerio, Henry Rapoport, Adonis Stassinopoulos, Susan Wollowitz
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Patent number: 6686480Abstract: Psoralen compound compositions are synthesized which have substitutions on the 4, 4′, 5′, and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.Type: GrantFiled: June 3, 2002Date of Patent: February 3, 2004Assignee: Cerus CorporationInventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans Peter Spielmann
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Publication number: 20040018517Abstract: Methods and kits for labeling and detecting thiol containing species and nucleic acids using mercurimethyl-dihydropsoralen compounds and derivatives thereof which intercalate nucleic acids and are highly reactive with thiol containing species are provided. Fluorescent reactions products of the mercurimethyl-dihydropsoralen compounds or derivatives thereof attached to a thiol containing species and nucleic acids fluorescently labeled with these reaction products are also provided.Type: ApplicationFiled: April 4, 2003Publication date: January 29, 2004Inventors: Jeffrey D. Laskin, Christine Martey, Ned Heindel, Marilyn Whittemore, Diane Heck
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Publication number: 20040002611Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.Type: ApplicationFiled: May 9, 2003Publication date: January 1, 2004Applicant: BIOAVAILABILITY SYSTEMS, LLCInventors: Robert Seemayer, Jack Liang
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Patent number: 6670383Abstract: The present invention relates to compounds and compositions useful in treating or preventing conditions and diseases related to Mycobacterium infection, and methods of use directed thereto.Type: GrantFiled: March 15, 2002Date of Patent: December 30, 2003Assignee: Advanced Life Sciences, Inc.Inventors: Ze-Qi Xu, Krzysztof Pupek, Livia Enache, Michael T. Flavin
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Patent number: 6613918Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.Type: GrantFiled: October 22, 2001Date of Patent: September 2, 2003Assignee: Bioavailability Systems, LLCInventors: Robert Seemayer, Jack Liang
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Publication number: 20030105339Abstract: Psoralen compound compositions are synthesized which have substitutions on the 4, 4′, 5′, and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.Type: ApplicationFiled: June 3, 2002Publication date: June 5, 2003Applicant: Cerus CorporationInventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans Peter Spielmann
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Publication number: 20030008891Abstract: 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity.Type: ApplicationFiled: March 13, 2002Publication date: January 9, 2003Applicant: Panacos Pharmaceuticals, Inc.Inventors: Kuo-Hsiung Lee, Lan Xie, Graham P. Allaway, Carl T. Wild
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Patent number: 6503699Abstract: Psoralen compound compositions are synthesized which have substitutions on the 4, 4′, 5′, and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.Type: GrantFiled: August 16, 1999Date of Patent: January 7, 2003Assignee: Cerus CorporationInventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans Peter Spielmann
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Publication number: 20020183346Abstract: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.Type: ApplicationFiled: February 22, 2002Publication date: December 5, 2002Applicant: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Robert I. Higuchi
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Patent number: 6469052Abstract: The present invention includes compositions comprising new psoralens with either a 4 ′, or 5 ′primary amino substituent and a blood product that is suitable for in vivo use. The compositions are useful for the inactivation of pathogens in blood products such as platelets and plasma.Type: GrantFiled: January 22, 2001Date of Patent: October 22, 2002Assignee: Cerus CorporationInventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans Peter Spielmann
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Patent number: 6420570Abstract: Psoralen compound compositions are synthesized which have substitutions on the 4, 4′, 5′, and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.Type: GrantFiled: January 22, 2001Date of Patent: July 16, 2002Assignee: Cerus CorporationInventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans Peter Spielmann
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Patent number: 6420571Abstract: The present invention relates to methods for preparing 2,2-dimethyl-5-acyloxy -10-propyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-8-one (5) and 2,2-dimethyl-5-hydroxy-10 -propyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-8-one (6) and their use as intermediates for the synthesis of antiviral calanolide compounds. For example, Fries rearrangement on compound 5 or Friedel-Crafts reaction on 6, yields intermediate 2,2-dimethyl-5-hydroxy -6-propionyl-10-propyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-8-one (4), which, in turn, can be converted to (+)-calanolide A and (−)-calanolide B. The coupling of compound 6 with the appropriate chiral molecule under Mitsunobu or nucleophilic displacement leads to the asymmetric synthesis of antiviral calanolide compounds.Type: GrantFiled: July 31, 2001Date of Patent: July 16, 2002Assignee: Sarawak MediChem Pharmaceuticals, Inc.Inventors: Ze-Qi Xu, Hongwei Yuan, Jennifer Crabb, Raghu Samy, Ailing Li, Hua Cao
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Patent number: 6384045Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.Type: GrantFiled: June 24, 1999Date of Patent: May 7, 2002Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 6319929Abstract: The present invention is directed to compounds that are analogs of the natural product suksdorfin. Compounds of the present invention include those having Formula IV: wherein R20 through R26, M and Z are defined herein. The invention is also directed to pharmaceutical compositions and methods of using these compositions for treating retroviral infections.Type: GrantFiled: December 8, 1998Date of Patent: November 20, 2001Assignees: The University of North Carolina at Chapel Hill, Panacos Pharmaceuticals, Inc.Inventors: Kuo-Hsiung Lee, Yoshiki Kashiwada, Li Huang, Thomas Tung-Ying Lee, Mark Cosentino, Jim Snider, Mark Manak, Lan Xie