Patents by Inventor Dajun Yang
Dajun Yang 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: 7432304Abstract: The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g.Type: GrantFiled: December 5, 2003Date of Patent: October 7, 2008Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Dajun Yang, Liang Xu
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Patent number: 7427689Abstract: A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is “compound B17”=methyl-(p-nitrophenyl)-2-propynoate.Type: GrantFiled: July 30, 2001Date of Patent: September 23, 2008Assignee: Georgetown UniversityInventors: Shaomeng Wang, Dajun Yang, Istvan Enyedy
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Patent number: 7354928Abstract: The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.Type: GrantFiled: November 1, 2002Date of Patent: April 8, 2008Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Dajun Yang, Istvan J. Enyedy
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Publication number: 20080058322Abstract: The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.Type: ApplicationFiled: June 8, 2007Publication date: March 6, 2008Applicant: The Regents of the University of MichiganInventors: Shaomeng Wang, Dajun Yang, Istvan Enyedy
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Publication number: 20080031812Abstract: A compound of formula: in which (i) aa1 is Adi and aa4 is Glu or (ii) each of aa1 and aa4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is characterized by an IC50 in vivo of less than about 4.0 ?M with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, has a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.Type: ApplicationFiled: August 14, 2007Publication date: February 7, 2008Applicants: GOVERNMENT OF THE USA, REPRESENTED BY THE SECRETARY, DEPA., GEORGETOWN UNIVERSITYInventors: Peter Roller, Ya-Qiu Long, Feng-Di T. Lung, C. Richter King, Dajun Yang, Johannes Voigt
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Publication number: 20080021095Abstract: The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).Type: ApplicationFiled: March 22, 2005Publication date: January 24, 2008Inventors: Jianyong Chen, Zaneta Nikolovska-Coleska, Dajun Yang, Shaomeng Wang, Haiying Sun, Liang Xu, Zengjian Hu
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Publication number: 20070219194Abstract: The present invention provides phenylalanine derivatives that inhibit SH2 domain binding with a phosphoprotein. These derivatives include compounds of the formula: W—Y-(AA)n-Z wherein n is 0 to 15; Y is a phenylalanyl radical having a phenyl ring, an amine end, and a carboxyl end, the phenyl ring having one or more substituents, e.g., hydroxyl, carboxyl, formyl, carboxyalkyl, carboxyalkyloxy, dicarboxyalkyl, dicarboxyalkyloxy, dicarboxyhaloalkyl, dicarboxyhaloalkyloxy, and phosphonoalkyl, or phosphonohaloalkyl; W is a moiety attached to the nitrogen of Y and is, e.g.Type: ApplicationFiled: May 16, 2007Publication date: September 20, 2007Applicants: GEORGETOWN UNIVERSITY, Govt of the U.S.A. Represented by the Secretary, DepInventors: Terrence Burke, Yang Gao, Zhu-jun Yao, Dajun Yang
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Patent number: 7259142Abstract: A compound of formula: in which (i) aa1 is Adi and aa4 is Glu or (ii) each of aa1 and aa4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is characterized by an IC50 in vivo of less than about 4.0 ?M with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, has a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.Type: GrantFiled: September 13, 2005Date of Patent: August 21, 2007Assignee: The United States of America, represented by the Secretary, Department of Health and Human ServicesInventors: Peter P Roller, Ya-Qui Long, Feng-Di T. Lung, C. Richter King, Dajun Yang, Johannes H. Voigt
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Patent number: 7226991Abstract: Disclosed herein are phenylalanine derivative compounds of the following formula W—Y—(AA)n—Z wherein Y is a phenylalanyl radical, AA is an amino acid, n is an integer of 1 to 15, and substituent variables W and Z are as described herein. The compounds can be used to inhibit SH2 binding with phosphoproteins, and to inhibit proliferation of tumor cells.Type: GrantFiled: March 23, 2000Date of Patent: June 5, 2007Assignees: United States of America, represented by the Secretary, Department of Health and Human Services, Georgetown UniversityInventors: Terrence R. Burke, Jr., Yang Gao, Zhu-jun Yao, Dajun Yang
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Publication number: 20060178435Abstract: The invention relates to the compound apogossypolone and salts and prodrugs thereof. Apogossypolone functions as an inhibitor of Bcl-2 family proteins. The invention also relates to the use of apogossypolone for inhibiting hyperproliferative cell growth, for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.Type: ApplicationFiled: November 2, 2005Publication date: August 10, 2006Applicant: The Regents of the University of MichiganInventors: Shaomeng Wang, Jianyong Chen, Zaneta Nikolovska-Coleska, Dajun Yang
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Publication number: 20060084647Abstract: The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.Type: ApplicationFiled: August 22, 2005Publication date: April 20, 2006Applicant: Regents of the University of MichiganInventors: Shaomeng Wang, Guoping Wang, Guozhi Tang, Renxiao Wang, Zaneta Nikolovska-Coleska, Dajun Yang, Liang Xu
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Publication number: 20060014927Abstract: A compound of formula: in which (i) aa1 is Adi and aa4 is Glu or (ii) each of aa1 and aa4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is characterized by an IC50 in vivo of less than about 4.0 ?M with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, has a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.Type: ApplicationFiled: September 13, 2005Publication date: January 19, 2006Applicants: Government of the U.S.A., represented by the Secretary, Dept. of Health and Human Services, Georgetown UniversityInventors: Peter Roller, Ya-Qiu Long, Feng-Di Lung, C. King, Dajun Yang
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Patent number: 6951915Abstract: A compound of formula: in which L is sulfur, sulfoxide, oxygen or methylene, and a compound of formula: in which (i) aa1 is Adi and aa4 is Glu or (ii) each of aa1 and aa4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compounds (and their conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, are non-phosphorylated, are redox-stable in vivo, are characterized by an IC50 in vivo of less than about 4.0 ?M with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, have a turn conformation.Type: GrantFiled: November 30, 2001Date of Patent: October 4, 2005Assignees: The United States of America as represented by the Department of Health and Human Services, Georgetown UniversityInventors: Peter P. Roller, Ya-Qiu Long, Feng-Di T. Lung, C. Richter King, Dajun Yang
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Publication number: 20040214902Abstract: The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g.Type: ApplicationFiled: December 5, 2003Publication date: October 28, 2004Applicants: The Regents of the University of Michigan, Georgetown UniversityInventors: Shaomeng Wang, Dajun Yang
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Patent number: 6703382Abstract: A method for promotion of cell death in tumor cells using tricylo-dibenzo-diazocine-dioxides that bind to a pocket of Bcl-2 and block the Bcl-2 anti-apoptotic function. A method of use of a compound of the general structural Formula (I) for use in treatment of cancer: wherein X and Y, and R and R1, and R2, R3, R4 and R5, and A and A1, have any of the values defined in the specification.Type: GrantFiled: August 16, 2001Date of Patent: March 9, 2004Assignee: Georgetown University Medical CenterInventors: Shaomeng Wang, Dajun Yang, Istvan J. Enyedy
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Publication number: 20040023957Abstract: A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is “compound B17”=methyl-(posa-notrophenyl)-2-propynoate.Type: ApplicationFiled: August 4, 2003Publication date: February 5, 2004Inventors: Shaomeng Wang, Dajun Yang, Istvan Enyedy
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Publication number: 20030078368Abstract: A compound of formula: 1Type: ApplicationFiled: November 30, 2001Publication date: April 24, 2003Applicant: The Govt. of the United States of AmericaInventors: Peter P. Roller, Ya-Qiu Long, Feng-Di T. Lung, C. Richter King, Dajun Yang
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Publication number: 20030008924Abstract: The present invention relates to naturally occurring and chemically synthesized small molecules antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol derivatives and methods of using gossypol derivatives as antagonists of the anti-apoptotic effects of Bcl-2 and Bcl-XL proteins especially in cancer cells that overexpress Bcl-2 family proteins (e.g., Bcl-2 and/or Bcl-XL).Type: ApplicationFiled: May 30, 2002Publication date: January 9, 2003Applicant: The Regents of the University of MichiganInventors: Shaomeng Wang, Dajun Yang
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Publication number: 20020137732Abstract: A method for promotion of cell death in tumor cells using tricylo-dibenzo-diazocine-dioxides that bind to a pocket of Bcl-2 and block the Bcl-2 anti-apoptotic function.Type: ApplicationFiled: August 16, 2001Publication date: September 26, 2002Inventors: Shaomeng Wang, Dajun Yang, Istvan J. Enyedy
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Patent number: 6143740Abstract: The invention provides a method of inhibiting cancer cell growth, and thereby of treating cancer comprising administering to a mammal afflicted with cancer an effective amount of the compound of formula (I), wherein the variables of R.sub.1, and R.sub.2 have the meanings defined in the specification. The present invention also provides novel compounds of formula (I) as well as novel pharmaceutical compositions and intermediates useful for preparing compounds of formula (I). The figure illustrates the structure and binding activity of compounds of the invention and some of the rifamycin analogs.______________________________________ ##STR1##______________________________________ Compounds R.sub.1 = ______________________________________ A1 --OH A2 --OH A3 --OH A4 --OH A5 --OH A6 --OH A7 --OH - A8 ##STR2## ______________________________________ Compounds R.sub.Type: GrantFiled: August 16, 1999Date of Patent: November 7, 2000Assignee: Georgetown UniversityInventors: Dajun Yang, Shaomeng Wang, Alan P. Kozikowski, Marc E. Lippman