IP Library › Granted Patent US 9,956,243
Granted Patent B2
US 9,956,243 · App. 14/560,086 · Granted May 1, 2018

Combination treatment for acute myeloid leukemia (AML)

Inventors: Brian Higgins (Fresh Meadows, NY); Gwen Nichols (New York, NY); Kathryn E. Packman (Newton, MA)
Assignee: HOFFMANN-LA ROCHE INC.
A61K31/7068A61K9/0019A61K31/40A61K31/77A61K45/06
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Quick Facts
Patent No.
US 9,956,243
App. No.
14/560,086
Granted
May 1, 2018
Kind
B2
Abstract

The present invention relates to a pharmaceutical product comprising a) as a first component an inhibitor of the MDM2-p53 interaction such as, for example: and b) as a second component cytarabine; as a combined preparation for the sequential or simultaneous use in the treatment of cancer.

Claims (16)

1. A pharmaceutical product, comprising a) as a first component an inhibitor of the MDM2-p53 interaction; and b) as a second component cytarabine, wherein the inhibitor of the MDM2-p53 interaction is a compound of formula (I):

wherein n is from 3 to 70; or a compound of formula (A):

2. The pharmaceutical product according to claim 1 , wherein n is from 30 to 60.

3. A method for treating acute myeloid leukemia, said method comprising: administering to a patient in need thereof the product of claim 2 .

4. The pharmaceutical product according to claim 1 , wherein a is from 40 to 50.

5. A method for treating acute myeloid leukemia, said method comprising: administering to a patient in need thereof the product of claim 4 .

6. The pharmaceutical product according to claim 1 , wherein n is 41, 42, 43, 44, 46, 47, 48 or 49.

7. A method for treating acute myeloid leukemia, said method comprising: administering to a patient in need thereof the product of claim 6 .

8. The pharmaceutical product according to claim 1 , wherein the inhibitor of the MDM2-p53 interaction is 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid 1-mPEG-carbonyloxy-ethyl ester (mPEG, average MW, ˜2000); or wherein the inhibitor of the MDM2-p53 interaction is 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid 1-mPEG-carbonyloxy-ethyl ester (mPEG, average MW, ˜2200); or combinations thereof.

9. A method for treating acute myeloid leukemia, said method comprising: administering to a patient in need thereof the product of claim 8 .

10. The pharmaceutical product according to claim 1 , wherein the inhibitor of the MDM2-p53 interaction is the compound of formula (A)

11. A method for treating acute myeloid leukemia, said method comprising: administering to a patient in need thereof the product of claim 1 .

12. A pharmaceutical product, comprising, a) as a first component a compound of formula (I):

wherein n is from 3 to 70; and b) as a second component the compound cytarabine, wherein the dose of the compound of formula (I) corresponds to a dose of compound (A):

within the range from about 200 to about 1600 mg/day.

13. The pharmaceutical product according to claim 12 , wherein the compound of formula (I) is the compound 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid 1-mPEG-carbonyloxy-ethyl ester (mPEG, average MW, ˜2000); or 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid 1-mPEG-carbonyloxy-ethyl ester (mPEG, average MW, ˜2200); or combinations thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2015
From: HIGGINS, BRIAN; NICHOLS, GWEN; PACKMAN, KATHRYN E.
To: HOFFMANN-LA ROCHE INC.
Reel/Frame 035002/0880 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2015
From: HOFFMANN-LA ROCHE INC.
To: F. HOFFMANN-LA ROCHE AG
Reel/Frame 035002/0911 →
Continuity (2)
Provisional Application 61912152 · Dec 5, 2013
Related Publication 20150157603A1 · Jun 11, 2015