IP Library Granted Patent US 10,076,528
Granted Patent B2
US 10,076,528 · App. 15/854,053 · Granted Sep 18, 2018

System and method for diagnosis and treatment

Inventors: Randice Lisa Altschul (Cliffside Park, NJ); Neil David Theise (New York, NY); Myron Rapkin (Indianapolis, IN); Rebecca O'Brien (Shell Knob, MO)
Assignee: Pop Test Oncology Limited Liability Company
A61K31/58A61K45/06
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Quick Facts
Patent No.
US 10,076,528
App. No.
15/854,053
Granted
Sep 18, 2018
Kind
B2
Abstract

This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.

Claims (13)

1. A pharmaceutical composition for treating neoplasia in a patient in need of such treatment, comprising:

(a) therapeutically effective amounts of at least one PARP inhibitor selected from the group consisting of 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]-methyl]-2H-phthalazin-1-one (Compound B, i.e., Olaparib), 4-iodo-3-nitrobenzamide (Iniparib), 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888), 8-Fluoro-2-{4-[(methylamino)methyl]-phenyl}-1,3,4,5-tetrahydro-6H-azepino-[5,4,3-cd]indol-6-one (AG014699), 4-methoxy-carbazole (CEP 9722), 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide hydrochloride (MK 4827), and 3-aminobenzamide, Iniparib, Olaparib, Rucaparib, Veliparib, CEP-9722, MK4827, BMN-673, pharmaceutically acceptable salts thereof, and combinations thereof;

(b) therapeutically effective amounts of at least one GCR (glucocorticoid receptor) antagonist selected from the group consisting of 11-(substituted phenyl)-estra-4,9-diene derivatives, and 11-(substituted phenyl)-estra-4,9-diene derivatives of formula I

wherein A is a residue of a 5- or 6-membered ring containing 2 heteroatoms which are not connected to each other and independently selected from O and S, the ring being optionally substituted with one or more halogen atoms, or A is a residue of a 5- or 6-membered ring wherein no double C—C bonds are present, containing 1 heteroatom selected from O and S, which heteroatom is connected to the phenyl group at the position indicated with an asterisk, the ring being optionally substituted with one or more halogen atoms; R1 is H or 1-oxo(1-4C)alkyl; R2 is H, (1-8C)alkyl, halogen or CF3; X is selected from (H,OH), O, and NOH; and the interrupted line represents an optional bond, and combinations thereof; and

(c) optionally, at least one pharmaceutically acceptable carrier,

wherein the neoplasia is selected from the group consisting of lung cancer, ovarian cancer, prostate cancer, liver cancer, cancer of the pancreas, cancer of the gastrointestinal tract, and head and neck cancers.

2. A kit for treating comprising:

(a) therapeutically effective amounts of at least one PARP inhibitor selected from the group consisting of 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]-methyl]-2H-phthalazin-1-one (Compound B, i.e., Olaparib), 4-iodo-3-nitrobenzamide (Iniparib), 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888), 8-Fluoro-2-{4-[(methylamino)methyl]-phenyl}-1,3,4,5-tetrahydro-6H-azepino-[5,4,3-cd]indol-6-one (AG014699), 4-methoxy-carbazole (CEP 9722), 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide hydrochloride (MK 4827), and 3-aminobenzamide, Iniparib, Olaparib, Rucaparib, Veliparib, CEP-9722, MK4827, BMN-673, pharmaceutically acceptable salts thereof, and combinations thereof; and

(b) therapeutically effective amounts of at least one GCR (glucocorticoid receptor) antagonist selected from the group consisting of 11-(substituted phenyl)-estra-4,9-diene derivatives, and 11-(substituted phenyl)-estra-4,9-diene derivatives of formula I

wherein A is a residue of a 5- or 6-membered ring containing 2 heteroatoms which are not connected to each other and independently selected from O and S, the ring being optionally substituted with one or more halogen atoms, or A is a residue of a 5- or 6-membered ring wherein no double C—C bonds are present, containing 1 heteroatom selected from O and S, which heteroatom is connected to the phenyl group at the position indicated with an asterisk, the ring being optionally substituted with one or more halogen atoms; R1 is H or 1-oxo(1-4C)alkyl; R2 is H, (1-8C)alkyl, halogen or CF3; X is selected from (H,OH), O, and NOH; and the interrupted line represents an optional bond, and combinations thereof; and

(c) optionally, at least one pharmaceutically acceptable carrier; and

(d) at least one blister package; a lidded blister; a blister card or packet; an intravenous (IV) package, IV packet or IV container; a tray comprising the pharmaceutical composition of (a) and instructions for use of the pharmaceutical composition for treating neoplasia.

3. A product of manufacture for treating neoplasia comprising a blister package; a lidded blister; a blister card or packet; a clamshell; an intravenous (IV) package, IV packette or IV container; a tray or a shrink wrap comprising the pharmaceutical composition of claim 1 , and instructions for use of the pharmaceutical composition for treating neoplasia.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 9, 2018
From: ALTSCHUL, RANDICE LISA; THEISE, NEIL DAVID; RAPKIN, MYRON; O'BRIEN, REBECCA
To: POP TEST ONCOLOGY LIMITED LIABILITY COMPANY
Reel/Frame 046599/0499 →
Continuity (11)
Division 15471123 · Mar 28, 2017
Division 15095293 · Apr 11, 2016
Division 14802060 · Jul 17, 2015
Continuation In Part 14100714 · Dec 9, 2013
Division 13364651 · Feb 2, 2012
Provisional Application 61462492 · Feb 3, 2011
Provisional Application 61463212 · Feb 14, 2011
Provisional Application 61465703 · Mar 23, 2011
Provisional Application 61518248 · May 3, 2011
Provisional Application 61519323 · May 20, 2011
Related Publication 20180117066A1 · May 3, 2018
Cited By (3)
US 12,383,543 US 12,458,620 US 12,734,180