Cornelis P Vlaar from San Juan, PR, age 57

Method For Preparing Irbesartan And Intermediates Thereof
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US Patent:

7365208, Apr 29, 2008
Filed:

Mar 20, 2007
Appl. No.:

11/688635
Inventors:

Edgar I. Miranda - Guaynabo PR, US
Cornelis Vlaar - San Juan PR, US
Jingyang Zhu - Monmouth Junction NJ, US
Assignee:

Bristol-Myers Squibb Company - Princeton NJ
International Classification:

C07D 235/02
US Classification:

5483007
Abstract:

A method for preparing irbesartan and intermediates thereof. Irbesartan has the structure of formula I,.

Method For Preparing Irbesartan And Intermediates Thereof
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US Patent:

20060041147, Feb 23, 2006
Filed:

Aug 22, 2005
Appl. No.:

11/209000
Inventors:

Edgar Miranda - Guaynabo PR, US
Cornelis Vlaar - San Juan PR, US
Jingyang Zhu - Monmouth Junction NJ, US
International Classification:

C07D 235/02
US Classification:

548300700
Abstract:

A method for preparing irbesartan and intermediates thereof. Irbesartan has the structure of formula I,

Novel Small-Molecule Inhibitors Of Rac1 In Metastatic Breast Cancer
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US Patent:

20130172552, Jul 4, 2013
Filed:

Sep 18, 2012
Appl. No.:

13/622303
Inventors:

University of Puerto Rico - San Juan PR, US
Cornelis Vlaar - San Juan PR, US
Suranganie Dharmawardhane - San Juan PR, US
Assignee:

UNIVERSITY OF PUERTO RICO - San Juan PR
International Classification:

C07D 413/14
US Classification:

544122
Abstract:

A novel inhibitor of Rac activity based on the structure of the established Rac/Rac-GEF inhibitor NSC23766 is discloses. The compound EHop-016, with an IC50 of 1.1 μM, is a 100-fold more efficient inhibitor of Rac activity than NSC23766. EHop-016 is specific for Rac1 and Rac3 at concentrations ≦5 mM. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells, EHop-016 (≦5 mM) inhibits the association of the Rac-GEF Vav2 with a nucleotide-free Rac1(G15A), which has a high affinity for activated GEFs. EHop-016 does not affect the association of the Rac-GEF Tiam-1 with Rac1(G15A) at similar concentrations. EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac-downstream effects of p21-activated kinase (PAK)1 activity and directed migration of metastatic cancer cells. At low concentrations (

Novel Carbazole Ehop-016 Derivatives As Anti-Cancer And Anti-Migratory Agents
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US Patent:

20200352941, Nov 12, 2020
Filed:

Jul 8, 2020
Appl. No.:

16/923853
Inventors:

- San Juan PR, US
Cornelis P. VLAAR - San Juan PR, US
Suranganie DHARMAWARDHANE FLANAGAN - San Juan PR, US
International Classification:

A61K 31/506
A61K 31/5377
C07D 403/14
C07D 401/14
C07D 403/12
A61P 35/00
Abstract:

A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula (I)Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

Novel Carbazole Ehop-016 Derivatives As Anti-Cancer And Anti-Migratory Agents
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US Patent:

20190125746, May 2, 2019
Filed:

Oct 23, 2018
Appl. No.:

16/168612
Inventors:

- San Juan PR, US
Cornelis P. VLAAR - San Juan PR, US
Suranganie DHARMAWARDHANE FLANAGAN - San Juan PR, US
International Classification:

A61K 31/506
A61K 31/5377
A61P 35/00
Abstract:

A series of novel of EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

Cornelis P Vlaar