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Last Updated: October 18, 2019

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Claims for Patent: 9,220,705

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Summary for Patent: 9,220,705
Title:Method of treating colorectal cancer
Abstract: The present invention relates to the use of certain platinum compounds including [PtCl.sub.2(cis-1,4-diaminocyclohexane)], or combinations of these compounds with a variety of other agents for treating and/or preventing the progression of colorectal cancer in mammals. In particular, the invention provides methods of treating and/or preventing oxaliplatin-refractory colorectal cancer in mammals.
Inventor(s): Hoeschele; James David (Plymouth, MI), Margiotta; Nicola (Barletta, IT), Gandin; Valentina (Tarzo, IT), Petruzzella; Emanuele (Molfetta, IT), Marzano; Cristina (Padua, IT)
Assignee:
Application Number:14/199,858
Patent Claims:1. A method of treating refractory colorectal cancer in a mammal in need of such treatment comprising administering to said mammal a therapeutically effective amount of a compound of formula I ##STR00047## wherein R is --(CH.sub.2).sub.n-- in which n is an integer from one to three; R.sub.1 is hydrogen, carboxyl, an alkyl group of from one to four carbon atoms, an alkyl group of from one to four carbon atoms substituted with an alkoxy group of from one to four carbon atoms, a cycloalkyl group of from three to six carbon atoms, a hydroxyalkyl group of from one to four carbon atoms, an alkoxy group of from one to four carbon atoms or benzyl; and R.sub.2 and R.sub.3 are negatively charged monodentate ligands which may be the same or different and are selected from the group consisting of chloro, bromo, iodo, hydroxo, nitrato, nitrito, acetato and dichloroacetato or R.sub.2 and R.sub.3 taken together form a dinegatively charged bidentate ligand selected from the group consisting of sulfato, oxalato, ##STR00048## in which R.sub.4 is hydrogen, hydroxyl, or an alkyl group of from one to four carbon atoms, ##STR00049## in which o is an integer from one to three and ##STR00050##

2. The method of claim 1 wherein R is --(CH.sub.2).sub.n--, in which n is an integer from two to three; R.sub.1 is hydrogen, carboxyl, an alkyl group of from one to four carbon atoms or an alkoxy group of from one to four carbon atoms; and R.sub.2 and R.sub.3 are negatively charged monodentate ligands which may be the same or different and are selected from the group consisting of chloro and bromo or R.sub.2 and R.sub.3 taken together form a dinegatively charged bidentate ligand selected from the group consisting of ##STR00051##

3. The method of claim 2 wherein R.sub.1 is hydrogen, carboxyl, methyl, or methoxy.

4. The method of claim 1 wherein a compound of formula I is selected from the group consisting of: [SP-4-2-(cis)]-dichloro(1,4-cyclohexanediamine-N,N')platinum; [SP-4-2-(cis)]-dichloro(1,3-cyclopentanediamine-N,N')platinum; [SP-4-2-(cis)]dichloro(1,4-cycloheptanediamine-N,N')platinum; [SP-4-2-(cis)][1,1-cyclobutanedicarboxylato-(2-)O,O.sup.1](1,4-cyclohexan- ediamine-N,N')platinum; [SP-4-2-(cis)]-(1,4-cyclohexanediamine-N,N') [2-hydroxy-5-sulfobenzoato (3)-O.sup.1,O.sup.2]platinate(1-),hydrogen; and [SP-4-2-(cis)]-(1,4,cyclohexanediamine-N,N')[ethanedioato(2)-O,O.sup.- 1]platinum.

5. The method of claim 4 wherein a compound of formula I is ##STR00052##

6. The method of claim 4 wherein a compound of formula I is ##STR00053##

7. The method of claim 5 wherein the refractory colorectal cancer is oxaliplatin-refractory colorectal cancer.

8. The method of claim 7 wherein the mammal is a human.

9. The method of claim 6 wherein the refractory colorectal cancer is oxaliplatin-refractory colorectal cancer.

10. The method of claim 9 wherein the mammal is a human.

11. The method of claim 1 further comprising at least one second therapeutic agent useful in treating refractory colorectal cancer selected from the group consisting of: capecitabine; cetuximab; bevacizumab; a MEK inhibitor; a FOLFOX4 dosing schedule consisting of oxaliplatin, 5-fluorouracil and leucovorin; and a FOLFIRI dosing schedule consisting of irinotecan, 5-fluorouracil and leucovorin.

Details for Patent 9,220,705

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Imclone ERBITUX cetuximab VIAL; INTRAVENOUS 125084 001 2004-06-18   Start Trial 2036-10-26 RX Orphan search
Genentech AVASTIN bevacizumab VIAL; INTRAVENOUS 125085 001 2004-02-26   Start Trial 2036-10-26 RX search
Genentech AVASTIN bevacizumab VIAL; INTRAVENOUS 125085 002 2004-02-26   Start Trial 2036-10-26 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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