Duquesne University of the Holy Spirit

Duquesne University of the Holy Ghost

Wayne State University

Aleem Gangjee

Larry H Matherly

A compound of Formula II, or optionally a salt or a hydrate of the compound of Formula II is provided: wherein Ris selected from the group consisting of a hydrogen, an alkyl group having from one to six carbon atoms, an aryl group, and a heteroaryl group; Ris selected from the group consisting of an alkyl group having from one to six carbon atoms, a hydrogen, a NRRgroup wherein Ris either a hydrogen or an alkyl group having from one to six carbon atoms and Ris either a hydrogen or an alkyl group having from one to six carbon atoms, an aryl group, a heteroaryl group, and a halogen; R is an alkyl group having from one to six carbon atoms; and Ar is selected from the group consisting of an alkyl group having from one to six carbon atoms, a substituted aryl, and a substituted heteroaryl.

Pyrazolo[4,3-d]pyrimidines as antitumor agents

The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic pharmaceutical compositions comprising compounds of Formula IV, and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.

Substituted pyrrolo,-furano, and cyclopentylpyrimidines having antimitotic and/or antitumor activity and methods of use thereof

Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.

Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity and methods of treating a patient

This invention provides substituted bicyclic pyrimidine compounds of the following formula: or a pharmaceutically acceptable salt thereof, wherein R is selected from the group consisting of a straight or a branched chain alkyl group having from 1 to 10 carbon atoms, wherein the alkyl group is partially or completely saturated. Methods of treating a patient diagnosed with cancer are disclosed comprising administering to the patient a therapeutically effective amount of the substituted bicyclic pyrimidine compounds, or a pharmaceutically acceptable salt thereof.

Substituted bicyclic pyrimidine compounds with tubulin and multiple receptor inhibition

A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided: Formula I, wherein, R is one selected from the group consisting of H and CH; n is an integer 4 when X is &#x2014;CH&#x2014; and Ar is 1,4-phenyl, or n is an integer ranging from 1 to 4 when X is &#x2014;CH&#x2014; and Ar is either 2'-fluoro-1,4-phenyl or 2,5-thienyl, or n is an integer ranging from 1 to 4 when X is one selected from the group consisting of O, S, &#x2014;NH&#x2014;, &#x2014;NHCHO&#x2014;, &#x2014;NHCOCH&#x2014;, and &#x2014;NHCOCF&#x2014; and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2&#x2032;-fluoro-1,4-phenyl, and (c) 2,5-thienyl, or n is an integer 3 when X is &#x2014;CH&#x2014;, R is CHand Ar is 1,4-phenyl.

First-in-class of SHMT2 and MTHFD2 inhibitors as antitumor agents

The present invention provides a compound of Formula III, and salts thereof, and a pharmaceutical composition comprising a compound of Formula III: wherein Ris selected from the group consisting of: whereinRis H or an alkyl group having from one to ten carbon atoms; Ris H or an alkyl group having from one to ten carbon atoms; and Ris H or an alkyl group having from one to ten carbon atoms. Methods of treating a patient with cancer with these compounds are also provided.

Cyclopenta[d]pyrimidines and substituted cyclopenta[d]pyrimidines as antitubulin and microtubule targeting agents, monocyclic pyrimidines as tubulin inhibitors, and pyrrolopyrimidines as targeted antifolates and tubulin and multiple receptor tyrosine kinase inhibitor and antitumor agents

The present invention discloses a compound of the formula:  and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.

Pyrimidine compounds and pyrimido indole compounds and methods of use

The present invention provides tricyclic compounds, and pharmaceutically acceptable salts thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.

Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof

The present invention provides a compound of Formula XXVII: wherein X is CHor O, and Ris H or CH; or a salt or a hydrate of the compound, and further provides a pharmaceutical composition comprising the compound of Formula XXVII and one or more acceptable pharmaceutical carriers. A method of treating a patient having cancer comprising administering a therapeutically effective amount of a compound of Formula XXVII, or a pharmaceutical composition comprising a compound of Formula XXVII and one or more acceptable pharmaceutical carriers to the patient is disclosed.

Monocyclic thieno, pyrido, and pyrrolo pyrimidine compounds and methods of use and manufacture of same

Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.

Selective proton coupled folate transporter and folate receptor, and garftase inhibitor compounds and methods of using the same

The present invention discloses a compound of the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CHor O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.

The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, and Formula IV, and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.

Substituted pyrrolo, -furano, and cyclopentylpyrimidines having antimitotic and/or antitumor activity and methods of use thereof

This invention provides substituted bicyclic pyrimidine compounds of the following formula: or a pharmaceutically acceptable salt thereof, wherein R is selected from the group consisting of H and a straight or branched chain alkyl group having from 1 to 10 carbon atoms, wherein the alkyl group is partially or completely saturated, each having tubulin and multiple receptor inhibition properties. Methods of treating a patient diagnosed with cancer are disclosed comprising administering to the patient a therapeutically effective amount of the substituted bicyclic pyrimidine compounds, or a pharmaceutically acceptable salt thereof.

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Allison Park, PA, United States of America

Aleem Gangjee