| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2015148854 |
| Title |
Substituted Indole Mcl-1 Inhibitors. |
| Abstract |
The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. |
| Applicant(s) |
Vanderbilt University |
| Representative Drug(s) |
D0MZ7I |
Drug Info
|
Ki = 1900 nM |
[1] |
| Patent ID |
WO2012097133 |
| Title |
Compounds and Methods for Inducing Apoptosis In Cancer Cells Using A Bh3 Alpha-Helical Mimetic. |
| Abstract |
A novel BH3 alpha-helical mimetic, BH3-M6, which binds to Bcl-XL and prevents its binding to fluorescently-labeled Bak-BH3 peptide in vitro with an IC50 value of 734 nM is presented herein. BH3-M6 is a pan-Bcl-2 antagonist that inhibits the binding of Bcl-XL, Bcl-2 and Mcl-1 to multi-domain Bax or Bak, or BH3-only Bim or Bad in a cell-free system and in intact human cancer cells, freeing up pro-apoptotic proteins to induce apoptosis. BH3-M6-induced apoptosis is caspase- and Bax- dependent. Furthermore, human cancer cells with high Bcl-2 or Bcl-XL levels are more sensitive to BH3-M6-induced cell death, suggesting that this compound can overcome drug resistance due to Bcl-2 or BCI-XL overexpression. The pan-Bcl-2 inhibitor BH3-M6 may be encapsulated in a micelle to provide a more bioavailable therapeutic agent. Specifically, the BH3-M6 compound may be encapsulated within a micelle comprising a multiblock copolymer according to the methods described herein. |
| Applicant(s) |
H. Lee Moffitt Cancer Center and Research Institute |
| Patent ID |
WO2010120943 |
| Title |
Naphthalene-Based Inhibitors of Anti-Apoptotic Proteins. |
| Abstract |
Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer. |
| Applicant(s) |
Sanford-Burnham Medical Research Institute |
| Patent ID |
WO2009052443 |
| Title |
Naphthalene-Based Inhibitors of Anti-Apoptotic Proteins. |
| Abstract |
Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently selected from the group consisting of H, C(O)X, C(O)NHX, NH(CO)X5 SO2NHX, and NHSO2X5 wherein X is selected from the group consisting of an alkyl, a substituted alkyl, an aryl, a substituted aryl, an alkylaryl, and a heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer. |
| Applicant(s) |
Burnham Institute for Medical Research |
| Patent ID |
WO2009045410 |
| Title |
Process for Preparing R-Gossypol L-Phenylalaninol Dienamine. |
| Abstract |
This invention relates to a process for preparing R-gossypol L-phenylalaninol dienamine using non-chromatographic purification methods. In particular, the invention is directed to resolution of R- and S-gossypol L-phenylalaninol dienamine by crystallization. R-gossypol L-phenylalaninol dienamine is a useful intermediate for the preparation of R-(-)-gossypol and R-(-)-gossypol acetic acid co-crystal. R-(-)-Gossypol acetic acid and its co- crystal is useful for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death. |
| Applicant(s) |
Ascenta Therapeutics, Inc |
| Patent ID |
WO2008150506 |
| Title |
Pulsatile Dosing of Gossypol for Treatment of Disease. |
| Abstract |
This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis. |
| Applicant(s) |
Ascenta Therapeutics, Inc |
| Patent ID |
WO2006050447 |
| Title |
Apogossypolone and The Uses Thereof. |
| Abstract |
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. |
| Applicant(s) |
The Regents of the University of Michigan |
| Patent ID |
WO2006023778 |
| Title |
Small Molecule Inhibitors of Anti-Apoptotic Bcl-2 Family Members and The Uses Thereof. |
| Abstract |
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. |
| Applicant(s) |
The Regents of the University of Michigan |
| Patent ID |
WO2005094804 |
| Title |
Gossypol co-crystals and the use thereof. |
| Abstract |
This invention relates to compositions comprising co-crystals of (-)- gossypol with a C 1-8 carboxylic acid or C 1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co?crystals of (-)-gossypol with a C 1-8 carboxylic acid or C 1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death. |
| Applicant(s) |
The regents of the university of michigan |
| Patent ID |
WO2005069771 |
| Title |
Small Molecule Antagonists of Bcl-2 Family Proteins. |
| Abstract |
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 nati-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/chemotheratpeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs. |
| Applicant(s) |
The Regents of the University of Michigan |
| Patent ID |
WO2002097053 |
| Title |
Small Molecule Antagonists of Bcl2 Family Proteins. |
| Abstract |
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). |
| Applicant(s) |
The Regents of the University of Michigan |
