Nicolas C Winssinger

6441186, Aug 27, 2002

Sep 4, 1997

08/923869

Kyriacos C. Nicolaou - La Jolla CA
Yun He - San Diego CA
Sacha Ninkovic - San Diego CA
Joaquin Pastor - San Diego CA
Frank Roschangar - San Diego CA
Francisco Sarabia - Torre de Benagalbón, ES
Hans Vallberg - Huddinge, SE
Dionisios Vourloumis - San Diego CA
Nicolas Winssinger - La Jolla CA
Zhen Yang - San Diego CA
N. Paul King - San Diego CA
M. Ray Finlay - San Diego CA

The Scripps Research Institute - La Jolla CA

C07D41714

548204

Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancer agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the anlogs are demonstrated to have a superior cytotoxic activities as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.

6660758, Dec 9, 2003

Sep 24, 1999

09/319885

Kyriacos C. Nicolaou - La Jolla CA
Yun He - San Diego CA
Sacha Ninkovic - San Diego CA
Joaquin Pastor - Madrid, ES
Frank Roschangar - Durham NC
Francisco Sarabia - Torre De Benagalbón, ES
Hans Vallberg - Huddinge, SE
Dionisios Vourloumis - Apex NC
Nicolas Winssinger - La Jolla CA
Zhen Yang - Brookline MA
Nigel Paul King - Camborne, GB
M. Ray Finlay - Killinchy, GB

The Scripps Research Institute - La Jolla CA

C07D41306

514374, 548235

Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubule assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.

20050153306, Jul 14, 2005

Jul 14, 2004

10/892402

Jennifer Harris - San Diego CA, US
Robert Damoiseaux - Escondido CA, US
Bradley Backes - Chicago IL, US
Nicolas Winssinger - La Jolla CA, US

IRM LLC - Hamilton

C12Q001/68
C07K014/47

435006000, 530350000

The present invention provides, inter alia, fluorogenic enzyme substrates, such as fluorogenic polypeptide substrates, libraries of fluorogenic enzyme substrates and methods for assaying for enzymatically active enzymes, such as hydrolases (e.g., proteases), in biological samples.

59657189, Oct 12, 1999

Sep 1, 1998

9/145376

Kyriacos C. Nicolaou - La Jolla CA
Floris VanDelft - Leiden, NL
Seijiro Hosokawa - Tokyo, JP
Sanghee Kim - Waukegan IL
Tianhu Li - San Diego CA
Takashi Ohshima - San Diego CA
Jeff Pfefferkorn - San Diego CA
Dionisios Vourloumis - San Diego CA
Nicolas Winssinger - La Jolla CA

The Scripps Research Institute - La Jolla CA

C07H 1524
A61K 3170
A61K 3134
C07D30777

536 181

Sarcodictyin A and B, eleutherobin, and bioactive analogs thereof synthesized using solid phase and solution phase chemistries. The synthetic method employs an attachment of common precursors, e. g. , compounds 1880 or 200, on a solid support for generating conjugates 230 and 240, followed by standard chemical manipulations. A combinatorial library of sarcodictyins and eletherobin analogs was constructed with modified C-8 ester, C-15 ester and C-4 ketal functionalities and was screened for activity with respect to tubulin polymerization and cytotoxic activity against tumor cells, including Taxol-resistant lines. Compounds 600, 610, 630, 660-700, 730, 760, 850, and 920 were identified to be of equal or superior biological activities as compared to their corresponding natural product.