Istvan Jozsef Enyedy

6703382, Mar 9, 2004

Aug 16, 2001

09/930237

Shaomeng Wang - Saline MI
Dajun Yang - Rockville MD
Istvan J. Enyedy - Hamden CT

Georgetown University Medical Center - Washington DC

A61K 31655

514183, 540482

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 R , and R , R , R and R , and A and A , have any of the values defined in the specification.

7354928, Apr 8, 2008

Nov 1, 2002

10/286085

Shaomeng Wang - Saline MI, US
Dajun Yang - Rockville MD, US
Istvan J. Enyedy - Milton MA, US

The Regents of the University of Michigan - Ann Arbor MI

A61K 31/44
A61K 31/335
A61K 31/135
A61K 31/505
A61K 31/65

514297, 514648, 514449, 514274, 514152, 514 27, 514 90, 424617

The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-X. 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-Xthat 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-X, 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.

7427689, Sep 23, 2008

Jul 30, 2001

10/343267

Shaomeng Wang - Saline MI, US
Dajun Yang - Rockville MD, US
Istvan Enyedy - Hamden CT, US

Georgetown University - Washington DC

C07C 205/00

562434

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.

7960163, Jun 14, 2011

Feb 29, 2008

12/040467

Robert B. Dickson - Silver Spring MD, US
Michael Johnson - Rockville MD, US
Shaomeng Wang - Saline MI, US
Istvan Enyedy - Hamden CT, US

Georgetown University School of Medicine - Washington DC

C12N 9/00
C12N 9/50
C12N 1/20
C12N 15/00
C07H 21/04

435219, 435183, 4352523, 4353201, 536 232

The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.

20080058322, Mar 6, 2008

Jun 8, 2007

11/811019

Shaomeng Wang - Ann Arbor MI, US
Dajun Yang - Rockville MD, US
Istvan Enyedy - Milton MA, US

The Regents of the University of Michigan - Ann Arbor MI

A61K 31/12
A61K 31/33
A61K 31/40
A61K 31/44
A61K 31/535
A61P 43/00

514229200, 514183000, 514283000, 514297000, 514332000, 514411000, 514680000

The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-X. 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-Xthat 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-X, 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.

20080293696, Nov 27, 2008

Jun 23, 2005

11/630850

Catherine Brennan - Durham NC, US
Julie A. Dixon - Bethany CT, US
William J. Scott - Guilford CT, US
Aniko Redman - Derby CT, US
Benjamin D. Jones - New Haven CT, US
Barton Phillips - New Haven CT, US
Philip Wickens - Wallingford CT, US
Istvan Enyedy - Milton MA, US
Ellalahewage Kumarasinghe - Hamden CT, US
Charles Kreiman - Wallingford CT, US
Jacques Dumas - Bethany CT, US
Uday Khire - Orange CT, US
Chih-Yuan Chuang - San Mateo CA, US
Harold C.E. Kluender - Trumbull CT, US
Zhenqiu Hong - Milford CT, US
Lei Wang - New Haven CT, US
Donald Bierer - Bethany CT, US

Bayer Pharmaceuticals Corporation - West Haven CT

A61K 31/55
C07D 405/12
A61K 31/4433
A61K 31/444
A61P 35/00
C07D 405/14
A61K 31/506

51421704, 5462824, 514338, 514333, 546256, 544333, 514256, 540597

A compound having the formula (1)in which the ring containing E is a phenyl, a pyridine, or a pyrimidine. In formula (1) the symbol A representswherein the group Rrepresents halogen, CF, or H, provided that the maximum number of CFgroups on any A is 2, and the maximum number of hydrogens on A is 2 for the A groups which together with the carbon atoms to which they are attached form 6-membered rings, and the maximum number of hydrogens on A is 1 for the A group which together with the carbon atoms to which it is attached forms a 5-membered ring. Z represents N or CH when E forms a phenyl ring, and represents CH when E forms a pyridine or pyrimidine. The groups R, Rand Rand the subscripts a, b, and d are as defined in the text and claims. Pharmaceutical compositions containing a compound of formula (1) and methods of treating cancer using compounds of formula (1) are also disclosed and claimed.

20110294848, Dec 1, 2011

May 28, 2009

13/058764

Leonard A. Smith - Fort Detrick MD, US
Nizamettin Gul - Fort Detrick MD, US
Rebecca C. Vieira - Fort Detrick MD, US
Susan M. Ensel - Fort Detrick MD, US
David C.H. Yang - Washington DC, US
Istvan J. Enyedy - Washington DC, US
Salimuddin Shah - Washington DC, US

A61K 31/4709
C07D 215/20
A61P 25/00
A61K 31/47
A61K 31/341
C07D 407/12
C07D 401/12

514314, 549473, 546177, 514311, 514471

The invention provides potent quinolinol-based BoNT/A small-molecule inhibitors of botulinum neurotoxins, in particular of serotype A neurotoxins. The invention also provides methods of using these small-molecule inhibitors to inhibit infections by , as well as, methods of preventing infections by through materials that may be ingested.

6677377, Jan 13, 2004

Jun 21, 2001

09/885295

Robert B. Dickson - Kensington MD
Shaomeng Wang - Rockville MD
Istvan Enyedy - Hamden CT
Sheau-Ling Lee - Falls Church VA

Georgetown University School of Medicine - Washington DC

A61K 31155

514636

The present invention relates to a method of inhibiting carcinoma progression wherein matriptase plays a role in a subject in need of such inhibition including administering to a subject an effective amount of a compound comprising two positively charged groups, which are the same or different. The groups are linked by a chemical group having a length of between 5 and 30 A, and preferably between 15 and 24 A. Diagnostic methods based on matriptase action and therapeutic methods involving inhibition of matriptase activity are provided.