Patents by Inventor Elias J. Corey
Elias J. Corey 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: 7511156Abstract: Disclosed herein are analogs of Salinosporamide A, having the Formulae Ia-IVa as follows: Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.Type: GrantFiled: October 9, 2006Date of Patent: March 31, 2009Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 7465720Abstract: Disclosed is a total synthesis of a biologically active ?-Lactam—Compound 3, which is related to Salinosporamide A and Omuralide, both structurally and by its activity as a proteasome inhibitor. Also disclosed are proteasome inhibiting compounds having the formula: wherein: R1 is a cyclolower alkyl group; or R1 is a lower alkyl group; and R2 is either hydrogen or a lower alkyl group; R3 is either hydrogen or a lower alkyl group; R4 a halo-lower alkyl group; and R5 is either hydrogen or a lower alkyl group.Type: GrantFiled: September 12, 2005Date of Patent: December 16, 2008Assignee: President and Fellows of Harvard CollegeInventors: Elias J. Corey, Philip C. Hogan
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Patent number: 7183417Abstract: A simple and effective stereocontrolled synthesis of salinosporamide A(1) has been developed which follows the pathway outlined in the FIGURE. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC50 values of 10 nM or less).Type: GrantFiled: April 9, 2004Date of Patent: February 27, 2007Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 6815544Abstract: An efficient process is described for the synthesis of 5, a key intermediate for the synthesis of the potent antitumor agents ecteinascidin 743 (1) and phthalascidin (2) from the readily available building blocks 3b and 4.Type: GrantFiled: August 7, 2002Date of Patent: November 9, 2004Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 6576781Abstract: The present invention is directed to the synthetic processes outlined in Schemes 1, 2 and 3, to the novel intermediates recited therein, and to the uses of these compounds as synthetic precursors to the pseudopterosins. Other embodiments and aspects of the present invention include the novel synthetic procedures described herein.Type: GrantFiled: June 27, 2001Date of Patent: June 10, 2003Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 6569859Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2Type: GrantFiled: February 14, 2002Date of Patent: May 27, 2003Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Publication number: 20030083495Abstract: An efficient process is described for the synthesis of 5, a key intermediate for the synthesis of the potent antitumor agents ecteinascidin 743 (1) and phthalascidin (2) from the readily available building blocks 3b and 4.Type: ApplicationFiled: August 7, 2002Publication date: May 1, 2003Applicant: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 6423877Abstract: The present invention is directed to a new synthetic route to pseudopterosin aglycone (3): a key intermediate for the synthesis of a group of antiinflammatory natural products including pseudopterosin A (1) and E (2). The pathway of synthesis starts with the abundant and inexpensive (S)-(−)-limonene and its long-known cyclic hydroboration product (4) and leads to the chiral hydroxy ketone (6). Conversion of (6) to (10) followed by a novel aromatic annulation produced (15) which underwent highly diastereoselective cyclization to afford the protected pseudopterosin aglycone (16). The naturally occurring pseudopterosins such as (1) and (2) are readily available from this key intermediate.Type: GrantFiled: November 15, 2000Date of Patent: July 23, 2002Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Publication number: 20020058698Abstract: The present invention is directed to the synthetic processes outlined in Schemes 1, 2 and 3, to the novel intermediates recited therein, and to the uses of these compounds as synthetic precursors to the pseudopterosins. Other embodiments and aspects of the present invention include the novel synthetic procedures described herein.Type: ApplicationFiled: June 27, 2001Publication date: May 16, 2002Inventor: Elias J. Corey
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Patent number: 6348467Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2Type: GrantFiled: February 22, 2000Date of Patent: February 19, 2002Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 6124292Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO.sub.2 R', NO.sub.2, NH.sub.2, NHR', N(R).sub.2, NHC(O)R', CN, halogen, .dbd.O, C(.dbd.O)H, C(.dbd.O)R', CO.sub.2 H, CO.sub.2 R', C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic;wherein each of the R' groups is independently selected from the group consisting of H, OH, NH.sub.2, NO.sub.2, SH, CN, halogen, .dbd.O, C(.dbd.O)H, C(.dbd.O)CH.sub.3, CO.sub.2 H, CO.sub.2 CH.sub.3, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl, aryl, aralkyl, and heteroaromatic;wherein each dotted circle represents one, two or three optional double bonds;wherein R.sub.Type: GrantFiled: September 30, 1998Date of Patent: September 26, 2000Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 5721362Abstract: The present invention is directed to a synthetic process for the formation of ecteinascidin compounds and related structures, such as the saframycins. In one particularly preferred embodiment, the present invention provides a synthetic route for the formation of ecteinascidin 743 (1), ##STR1## an exceedingly potent and rare marine-derived antitumor agent which is slated for clinical trials. The process of this invention is enantio- and stereocontrolled, convergent and short. Also disclosed are novel process intermediates, useful not only in the total synthesis of ecteinascidin 743, but also other known ecteinascidin compounds, including derivatives and analogs thereof.Type: GrantFiled: September 18, 1996Date of Patent: February 24, 1998Assignee: President and Fellows of Harvard CollegeInventors: Elias J. Corey, David Gin
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Patent number: 5096892Abstract: Anigiogenesis is controlled by administering to a mammal an effective amount of an inhibitor of arylsulfatase. Preferably, the arylsulfatase inhibitor is administered in a pharmaceutically acceptable vehicle in combination with an angiostatic steroid and (optionally) heparin (by which term we include all forms and fragments of heparin having the desired angiostatic activity). Hydrocortisone is one specifically preferred steroid. The preferred arylsulfatase inhibitor is a carboxylic acid ester or a sulfuric acid ester of a benzylic alcohol, most preferably the esters defined more particularly below. The arylsulfatase inhibitor is preferably administered locally to the tissue experiencing undesired angiogenesis. Arylsulfatase inhibitor and an angiostatic steroid are included in a pharmaceutically acceptable vehicle, preferably also with heparin, to yield an angiostatic thereapeutic composition.Type: GrantFiled: May 27, 1988Date of Patent: March 17, 1992Assignees: The Children's Medical Center Corporation, President and Fellows of Harvard CollegeInventors: Moses J. Folkman, Neil T. Chen, Elias J. Corey
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Patent number: 4943635Abstract: Chiral 1,3,2-oxazaborolidines and tetrahydro-1,3,2-oxazaborines are effective catalysts for the borane reduction of prochiral ketones to optically active alcohols.Type: GrantFiled: July 29, 1988Date of Patent: July 24, 1990Assignee: President & Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 4214099Abstract: A new synthesis of key prostaglandin precursors and intermediates employed in their preparation. The novel synthetic sequence of this invention is shorter and more efficient than those previously employed to prepare to key intermediate.Type: GrantFiled: June 22, 1978Date of Patent: July 22, 1980Assignee: Pfizer Inc.Inventors: Elias J. Corey, Jasjit S. Bindra, Thomas K. Schaaf
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Patent number: 4122093Abstract: A new synthesis of key prostaglandin precursors and intermediates employed in their preparation. The novel synthetic sequence of this invention is shorter and more efficient than those previously employed to prepare to key intermediate.Type: GrantFiled: April 14, 1977Date of Patent: October 24, 1978Assignee: Pfizer Inc.Inventors: Elias J. Corey, Jasjit S. Bindra, Thomas K. Schaaf
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Patent number: 3992438Abstract: A new synthesis of key prostaglandin precursors and intermediates employed in their preparation. The novel synthetic sequence of this invention is shorter and more efficient than those previously employed to prepare to key intermediate.Type: GrantFiled: November 19, 1975Date of Patent: November 16, 1976Assignee: Pfizer Inc.Inventors: Elias J. Corey, Jasjit S. Bindra, Thomas K. Schaaf
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Patent number: 3992439Abstract: In the synthesis of prostaglandins of the "one" -series an alteration in the conventional reaction sequence avoids side reactions and provides an improved synthesis via a series of novel intermediates. In this improved synthesis the side chain at the 8 position is attached to the five membered ring before the side chain at the 12 position is attached.Type: GrantFiled: February 14, 1975Date of Patent: November 16, 1976Assignee: Pfizer Inc.Inventors: Thomas K. Schaaf, Elias J. Corey
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Patent number: 3974183Abstract: A process for reducing trans-1-(2-carboxymethyl-3-hydroxy-5-acyloxycyclopentyl)-1-octen-3-one-.ga mma.-lactone to the corresponding 3-ol which makes use of trihydrocarbylborohydride reagents, some of which are new, e.g. lithium 2-thexyl-8-methyl-2-borabicyclo-[3,3,1]nonylhydride. A new process for producing this and other lithium thexyl-dihydrocarbylborohydrides which comprises contacting a thexyl-dihydrocarbylborane with an organo-lithium compound having a .beta.-hydrogen atom.Type: GrantFiled: July 12, 1974Date of Patent: August 10, 1976Inventor: Elias J. Corey
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Patent number: RE41614Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHC(?O)R? NHC(?O)R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be are joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2 are each independently defined as above for R1-R8 R1-R6 and R9, and each further includes sType: GrantFiled: December 17, 2003Date of Patent: August 31, 2010Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey