Patents by Inventor Henry Rapoport
Henry Rapoport has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5654443Abstract: 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: May 31, 1995Date of Patent: August 5, 1997Assignee: Cerus CorporationInventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans Peter Spielmann
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Patent number: 5625079Abstract: Synthesis of 4,8-dialkyl-4'-bromomethyl-5'-methylpsoralen and 4,8-dialkyl-5'-bromomethyl-4'-methylpsoralen compounds useful as intermediates.Type: GrantFiled: June 5, 1995Date of Patent: April 29, 1997Assignee: Cerus CorporationInventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans P. Spielmann, Aileen Nerio
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Patent number: 5602264Abstract: Novel water soluble carbodiimides, and intermediates or derivatives thereof, such as isoureas or isothioureas, are described. A particularly preferred embodiment is bis[4-(2,2-dimethyl-1,3-dioxolyl)methyl] carbodiimide (BDDC), which can be synthesized efficiently from 1,2-isopropylideneglycerol (solketal). The isoureas are effective esterifying agents. The corresponding N-protected amino acid tert-butyl, benzyl, isopropyl, ethyl, and methyl esters can be synthesized in high yield under neutral conditions, with no urea residue after simply washing with aqueous acid. Amino acid couplings utilizing carbodiimide embodiments give peptides in good yield, free of carbodiimide by-products, after washing with dilute acid, while racemization-free peptides are also obtained.Type: GrantFiled: November 28, 1994Date of Patent: February 11, 1997Assignee: The Regents of the University of CaliforniaInventors: Henry Rapoport, Frank S. Gibson
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Patent number: 5593823Abstract: Psoralen compounds are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which permit enhanced binding to nucleic acid of pathogens. Higher psoralen binding levels and lower mutagenicity are described, resulting in safer, more efficient, and reliable inactivation of pathogens in blood products. The invention contemplates inactivation methods using the new psoralens which do not compromise the function of blood products for transfusion.Type: GrantFiled: November 14, 1994Date of Patent: January 14, 1997Assignee: Cerus CorporationInventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans P. Spielmann, Aileen Nerio
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Patent number: 5585503Abstract: 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: May 31, 1995Date of Patent: December 17, 1996Assignee: Steritech, Inc.Inventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans P. Spielmann
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Patent number: 5578736Abstract: 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: May 31, 1995Date of Patent: November 26, 1996Assignee: Steritech, Inc.Inventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans P. Spielmann
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Patent number: 5556993Abstract: Psoralen compounds are synthesized which have substitutions on the 4,4', 5', and 8 positions of the psoralen, which permit enhanced binding to nucleic acid of pathogens. Higher psoralen binding levels and lower mutagenicity are described, resulting in safer, more efficient, and reliable inactivation of pathogens in blood products. The invention contemplates inactivation methods using the new psoralens which do not compromise the function of blood products for transfusion.Type: GrantFiled: June 5, 1995Date of Patent: September 17, 1996Assignee: Steritech, Inc.Inventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans P. Spielmann, Aileen Nerio
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Patent number: 5399719Abstract: 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 28, 1993Date of Patent: March 21, 1995Assignee: Steritech, Inc.Inventors: Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans P. Spielmann
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Patent number: 5322942Abstract: Optically active lactones are described, such as an intermediate lactone having the formula ##STR1## where R and R.sup.2 are each independently alkyl with 1 to 6 carbon atoms, cycloalkyl with 6 to 10 carbon atoms, aryl with 6 to 10 carbon atoms, or arylalkyl with 7 to 19 carbon atoms, R.sup.4 is H or C.sub.1-6 alkyl, and Ar is a homo- or heteroaromatic ring with 5 or 6 ring atoms being optionally substituted by C.sub.1-6 alkyl or alkoxy groups, halogen atoms, cyano or nitro groups. Such optically active, intermediate lactones are prepared from L-aspartic acid, and can be readily converted to (+)-pilocarpine and its analogues by hydrolysis, reduction, and hydrogenation, such as to an optically active lactone having the formula ##STR2## which is (+)-pilocarpine when R is ethyl, R.sup.4 is H, and Ar is 1-methylimidazol-5-yl.Type: GrantFiled: June 3, 1991Date of Patent: June 21, 1994Assignee: Regents of the University of CaliforniaInventors: Henry Rapoport, Jeffrey M. Dener, Lin-hau Zhang
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Patent number: 5252603Abstract: Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## wherein n=1-6R=CH.sub.3, CF.sub.3, --CO.sub.2 R.sup.IV, ##STR2## R.sup.I, R.sup.II =H, F, CH.sub.3, or ##STR3## R.sup.III =H, ##STR4## or tetrazolyl R.sup.IV =H, or alkyland that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.Type: GrantFiled: December 6, 1990Date of Patent: October 12, 1993Assignee: Cetus CorporationInventors: Danute E. Nitecki, Lois Aldwin, Corey H. Levenson, Margaret Moreland, Irwin Braude, David F. Mark, Henry Rapoport
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Patent number: 5216005Abstract: Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.Type: GrantFiled: December 6, 1990Date of Patent: June 1, 1993Assignee: Cetus CorporationInventors: Danute E. Nitecki, Lois Aldwin, Corey H. Levenson, Margaret Moreland, Irwin Braude, David F. Mark, Henry Rapoport
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Patent number: 5173482Abstract: Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.Type: GrantFiled: December 6, 1990Date of Patent: December 22, 1992Assignee: Cetus CorporationInventors: Danute E. Nitecki, Margaret Moreland, Lois Aldwin, Corey H. Levenson, Irwin Braude, David F. Mark, Henry Rapoport
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Patent number: 5025027Abstract: Pilocarpine analogues are provided having the structure ##STR1## where one of R.sub.1 or R.sub.2 is an alkyl, such as methyl, ethyl, propyl, butyl, and so forth, and the corresponding secondary alkyl groups, an aralkyl, such as benzyl, phenylethyl, phenylpropyl, and the corresponding secondary aralkyl residues, or a cycloalkyl having less than about 12 carbon atoms. R.sub.3 has at least two carbon atoms but less than about 9. These pilocarpine analogues have improved duration of biological activity with respect to pilocarpine. A particularly preferred compound is a muscarinic agonist equipotent with pilocarpine, where R.sub.2 is methyl, and R.sub.3 is ethyl.Type: GrantFiled: December 5, 1989Date of Patent: June 18, 1991Assignee: Regents of the University of CaliforniaInventors: Henry Rapoport, Per Sauerberg
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Patent number: 4618710Abstract: An optically active alpha-amino acid derivative having the formula: ##STR1## wherein: X is OH, Cl, Br, I, or OCOR.sub.3 ;Y is a radical selected to stabilize the alpha carbon atom of the alpha-amino acid derivative sufficiently to prevent significant change in symmetry thereof during replacement of X with an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl or alkynaryl radical, or such radical having one or more chemical constituents thereon; andR.sub.1 and R.sub.2 are different from one another and are each hydrogen or an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl, or alkynaryl radical, or such radical having one or more non-protic chemical constituents thereon is conventionally synthesized from the corresponding alpha-amino acid. The ##STR2## portion of the above derivative is converted to a ketone functionality without racemization.Type: GrantFiled: September 13, 1982Date of Patent: October 21, 1986Assignee: The Regents of the University of Calif.Inventors: Henry Rapoport, Thomas F. Buckley, III
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Patent number: 4617261Abstract: Nucleic acids may be labeled by intercalating the alkylating intercalation moiety of a labeling reagent into a partially double-stranded nucleic acid to form a complex and activating the complex to cause covalent bonding between the reagent and the nucleic acid. Preferably, the labeled nucleic acid is a hybridization probe for detecting nucleic acid sequences capable of hybridizing with a hybridizing region of the nucleic acid. Also preferably the label moiety is non-radioactive. The labeling reagent is of the formula:[A--[B--Lwhere A is an alkylating intercalation moiety, B is a divalent organic moiety of the formula: ##STR1## where Y is O, NH or N--CHO, x is a number from 1 to 4, y is a number from 2 to 4, and L is a monovalent label moiety, wherein B is exclusive of any portion of the intercalation and label moieties.Preferably A is a 4-methylene-substituted psoralen moiety, and most preferably A is a 4'-methylene-substituted-4,5',8-trimethylpsoralen moeity and L is biotin.Type: GrantFiled: October 25, 1985Date of Patent: October 14, 1986Assignee: Cetus CorporationInventors: Edward L. Sheldon, III, Corey H. Levenson, Kary B. Mullis, Henry Rapoport, Robert M. Watson
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Patent number: 4582789Abstract: A labeling reagent of the formula:[A][B]Lis prepared where A is an alkylating intercalation moiety, B is a divalent organic spacer arm moiety with a straight chain of at least two carbon atoms, and L is a monovalent label moiety capable of producing a detectable signal, e.g., a signal detectable by spectroscopic, photochemical, chemical, immunochemical or biochemical means. Preferably A is a 4'-methylene-substituted psoralen moiety, and most preferably A is a 4'-methylene-substituted 4,5',8-trimethylpsoralen moiety.This reagent may be used to label nucleic acids, preferably DNA, by intercalating the alkylating intercalation moiety of the reagent into an at least partially double-stranded nucleic acid to form a complex and activating the complex to cause covalent bonding between the reagent and the nucleic acid. Preferably, the labeled nucleic acid is a hybridization probe for detecting nucleic acid sequences capable of hybridizing with a hydridizing region of the nucleic acid.Type: GrantFiled: December 18, 1984Date of Patent: April 15, 1986Assignee: Cetus CorporationInventors: Edward L. Sheldon, III, Corey H. Levenson, Kary B. Mullis, Henry Rapoport
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Patent number: 4435572Abstract: This invention relates to a process for the production of 4a-aryldecahydroisoquinolines where the aryl group is selected as 3-methoxy phenyl. These compounds are morphine analogs and show utility similar to the known morphine, codeine, and thebaine. In this process particular novelty is asserted for the production of a nipecotic ester ethyl 4-(3'-methoxyphenyl)-1-methyl piperidine-3-carboxylate. Furthermore, novelty is asserted for the step of conversion of the nipecotates through cyclization to cis- or trans-tert-butyl 1,6-dioxo-4a-(3'-methoxyphenyl)-2-methyldecahydroisoquinoline-7-carboxylat e, which may also be easily converted to the keto amide, trans-1,6-dioxo-4a-(3'-methoxyphenyl)-2-methyldecahydroisoquinoline.Type: GrantFiled: March 16, 1981Date of Patent: March 6, 1984Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Henry Rapoport, Dwight D. Weller, Richard D. Cless
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Patent number: 4398031Abstract: Two species of a coumarin derivative are disclosed, both of which may be produced from a 7-hydroxycoumarin precursor. The one species is an oxime and the other is a .beta.-haloallyl ester.A method for making a psoralen compound in high yield comprises treating these coumarin derivatives with an acid to fuse a furan ring thereto, and recovering a 5'-methyl psoralen therefrom. The 5'-methyl psoralen may be produced in up to about 70% overall yield with respect to the 7-hydroxycoumarin precursor.Type: GrantFiled: March 9, 1982Date of Patent: August 9, 1983Assignee: The Regents of the University of CaliforniaInventors: Dean R. Bender, John E. Hearst, Henry Rapoport
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Patent number: 4346224Abstract: This invention relates to the production of 4a-aryldecahydroisoquinolines where the aryl group is selected as 3-methoxy phenyl and intermediates. These compounds are morphine analogs and show utility similar to the known morphine, codeine, and thebaine.Type: GrantFiled: January 14, 1981Date of Patent: August 24, 1982Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Henry Rapoport, Dwight D. Weller, Richard D. Gless
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Patent number: 4289882Abstract: This invention relates to the production of 4a-aryldecahydroisoquinolines where the aryl group is selected as 3-methoxy phenyl and intermediates. These compounds are morphine analogs and show utility similar to the known morphine, codeine, and thebaine.Type: GrantFiled: September 5, 1978Date of Patent: September 15, 1981Assignee: The United States of America as represented by the Department of Health & Human ServicesInventors: Henry Rapoport, Dwight D. Weller, Richard D. Gless