Patents by Inventor Alan C. Sartorelli
Alan C. Sartorelli 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: 6960568Abstract: The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and antibacterial applications. Preferred embodiments of the instant invention include novel 2 halogen-substituted, 3 halogen-substituted, and 2?,3?dihalogen-substituted analogues of 3-deazaadenosine, and novel 3 halogen-substituted analogues of 3-deazaguanosine. Compounds of the instant invention, including 4-Amino-6-fluoro-1-(?-D-ribofuranosyl)imidazo[4,5-c]pyridine and 6-Amino-7-bromo-1,5-dihydro-1-?-D-ribofuranosylimidazo[4,5-c]pyridin-4-one, have exhibited potent antiviral and anticancer activity in vitro. The compounds are also useful in the concomitant treatment of bacterial infections associated with viral infections such as AIDS.Type: GrantFiled: December 17, 2002Date of Patent: November 1, 2005Assignee: Yale UniversityInventors: Alan C. Sartorelli, Yung-Chi Cheng, Mao-Chin Liu
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Patent number: 6911460Abstract: The present invention relates to methods of treating viral or fungal infections using 3-aminopyridine-2-carboxyaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) and its prodrug forms and to pharmaceutical compositions comprising these compounds.Type: GrantFiled: April 18, 2002Date of Patent: June 28, 2005Assignees: Vion Pharmaceuticals, Inc., Yale UniversityInventors: Ivan C. King, Terrance W. Doyle, Mario Sznol, Alan C. Sartorelli, Yung-Chi Cheng
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Publication number: 20040116362Abstract: The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and antibacterial applications. Preferred embodiments of the instant invention include novel 2 halogen-substituted, 3 halogen-substituted, and 2′,3′dihalogen-substituted analogues of 3-deazaadenosine, and novel 3 halogen-substituted analogues of 3-deazaguanosine. Compounds of the instant invention, including 4-Amino-6-fluoro-1-(&bgr;-D-ribofuranosyl)imidazo[4,5-c]pyridine and 6-Amino-7-bromo-1,5-dihydro-1-&bgr;-D-ribofuranosylimidazo[4,5-c]pyridin-4-one, have exhibited potent antiviral and anticancer activity in vitro. The compounds are also useful in the concomitant treatment of bacterial infections associated with viral infections such as AIDS.Type: ApplicationFiled: December 17, 2002Publication date: June 17, 2004Inventors: Alan C. Sartorelli, Yung-Chi Cheng, Mao-Chin Liu
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Publication number: 20020188011Abstract: The present invention relates to methods of treating viral or fungal infections using 3-aminopyridine-2-carboxyaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) and its prodrug forms and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: April 18, 2002Publication date: December 12, 2002Inventors: Ivan C. King, Terrance W. Doyle, Mario Sznol, Alan C. Sartorelli, Yung-Chi Cheng
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Patent number: 6040338Abstract: The present invention relates to a compound of the formula wherein R.sup.1 and R.sup.2 are selected from lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms; R.sup.3 is a substituted or unsubstituted lower alkyl group having 1-6 carbons; and R.sup.4 is selected from substituted or unsubstituted lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms. The present invention also relates to a pharmaceutical composition comprising the above compound, as well as a method of treating tumor cells with the compound.Type: GrantFiled: November 3, 1997Date of Patent: March 21, 2000Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh, Shu-Hui Chen
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Patent number: 5721259Abstract: A method of treatment of tumors is provided based upon a compound of the formula ##STR1## wherein one of R.sup.1 is NHR.sup.4 or NR.sup.4 R.sup.5 or R.sup.3 is NHR.sup.4, NR.sub.4 R.sup.5 or OH, and the other is hydrogen;R.sup.2 is hydrogen or C.sub.1-4 lower alkyl;R.sup.4 is hydrogen, hydroxyl or C.sub.1-4 lower alkyl; andR.sup.5 is C.sub.1-4 lower alkyl; ora pharmaceutically acceptable salt or hydrate thereof.In a further aspect there is provided a method for the treatment of a tumor in a mammal which comprises administration of a compound which is 3- or 5-hydroxy-4-methyl-2-formylpyridine thiosemicarbazone to said mammal.Type: GrantFiled: August 22, 1996Date of Patent: February 24, 1998Assignee: Yale UniversityInventors: Alan C. Sartorelli, Tai-Shun Lin
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Patent number: 5637619Abstract: The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhy drazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.Type: GrantFiled: July 5, 1995Date of Patent: June 10, 1997Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 5281715Abstract: A method of treatment of tumors is provided based upon a compound of the formula ##STR1##Some aspects of the invention were supported in part by U.S. Public Health Service Grant CA-02817 from the National Cancer Institute and support from the Northeast NMR Facility at Yale University insofar as the use of high resolution NMR spectra is concerned that was made possible by a grant from the Chemical Division of the National Science Foundation (Grant No. CHE-7916210).Type: GrantFiled: May 13, 1992Date of Patent: January 25, 1994Assignee: Yale UniversityInventors: Alan C. Sartorelli, Tai-Shun Lin
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Patent number: 5256820Abstract: Novel antineoplastic 1-alkyl-2-acyl-1,2-disulfonylhydrazine having the following formula and methods of therapy using those antineoplastic compounds: ##STR1## where R.sub.1 and R.sub.2 are (independently) alkyl, cycloalkyl, aryl, aralkyl or heteroaryl. X is an acyl group, and Z is an alkyl or a haloalkyl group.Type: GrantFiled: November 8, 1991Date of Patent: October 26, 1993Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 5214068Abstract: Sulfonylhydrazines of the formula RSO.sub.2 N(CH.sub.2 CH.sub.2 X)N(SO.sub.2 CH.sub.3).sub.2, wherein R is an alkyl or an aryl and X is a halogen or OSO.sub.2 Y, wherein Y is an alkyl or an aryl. Such sulfonylhydrazines are useful in treating cancer.Methylating agents of the formula(a) R'SO.sub.2 N(CH.sub.3)N(SO.sub.2 CH.sub.3).sub.2, wherein R' is an alkyl or an aryl and(b) R"SO.sub.2 N(CH.sub.3)N(CH.sub.3)SO.sub.2 R", wherein R" is an alkyl or an aryl.Such methylating agents are useful as antitrypanosomal and anticancer agents.Type: GrantFiled: March 12, 1992Date of Patent: May 25, 1993Assignee: Yale UniversityInventors: Alan C. Sartorelli, Alan A. Divo, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 5101072Abstract: Sulfonylhydrazines of the formula RSO.sub.2 N(CH.sub.2 CH.sub.2 X)N(SO.sub.2 CH.sub.3).sub.2, wherein R is an alkyl or an aryl and X is a halogen or OSO.sub.2 Y, wherein Y is an alkyl or an aryl. Such sulfonylhydrazines are useful in treating cancer.Methylating agents of the formula(a) R'SO.sub.2 N(CH.sub.3)N(SO.sub.2 CH.sub.3).sub.2, wherein R' is an alkyl or an aryl and(b) R"SO.sub.2 N(CH.sub.3)N(CH.sub.3)SO.sub.2 R", wherein R" is an alkyl or an aryl. Such methylating agents are useful as antitrypanosomal and anticancer agents.Type: GrantFiled: September 6, 1989Date of Patent: March 31, 1992Assignee: Yale UniversityInventors: Alan C. Sartorelli, Alan A. Divo, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 4962114Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is a lower alkyl of 1-6 carbon atoms, benzyl, phenyl or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substitutents, or --RN(R').sub.2 wherein R and R' are each independently alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent, and each A is an aromatic substitution indpendently selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2,--COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.Type: GrantFiled: June 4, 1987Date of Patent: October 9, 1990Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Robert T. Hrubiec
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Patent number: 4892887Abstract: Compounds of the formula ##STR1## where R is methyl or 2-chloroethyl, and R.sup.1 and R.sup.2 are each an aromatic hydrocarbon, ring substituted aromatic hydrocarbon moiety, or an alkyl moiety. The compounds have been found to be alkylating agents having antineoplastic activity.Type: GrantFiled: August 9, 1988Date of Patent: January 9, 1990Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam
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Patent number: 4849563Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 s an alkyl of 1-6 carbon atoms, benzyl, phenyl, or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substituents, or --RN(R').sub.2 wherein R and R' are each independently an alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent selected from the group consisting of phenyl, benzyl, and naphthyl, and A is an aromatic substitution selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2, --COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.Type: GrantFiled: December 28, 1987Date of Patent: July 18, 1989Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Robert T. Hrubiec
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Patent number: 4806531Abstract: The compounds of the formula: ##STR1## wherein R is selected from the group consisting of: (a) a substituent having the formula: ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen and --NO.sub.2,(b) a substituent having the formula: ##STR3## wherein R.sub.4 is hydrogen or an N(R').sub.2 substituent, wherein R' is an alkyl of 1 to 4 carbon atoms and R.sub.5 is CH or N,(c) alkyl of 1 to 18 carbon atoms,(d) halo-substituted alkyl of 1 to 6 carbon atoms,(e) styrenyl,(f) toluenyl, or(g) camphoryl.The compounds have been found to have anti-neoplastic activity for use in inhibiting the growth of tumors.Type: GrantFiled: February 20, 1986Date of Patent: February 21, 1989Assignee: Yale UniversityInventors: Alan C. Sartorelli, Tai-Shun Lin
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Patent number: 4684747Abstract: Compounds of the formula ##STR1## where R is methyl or 2-chloroethyl, and R.sup.1 and R.sup.2 are each an aromatic hydrocarbon, ring substituted aromatic hydrocarbon moiety, or an alkyl moiety. The compounds have been found to be alkylating agents having antineoplastic activity.Type: GrantFiled: December 18, 1985Date of Patent: August 4, 1987Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam