IP Library Granted Patent US 8,487,095
Granted Patent B2
US 8,487,095 · App. 13/415,268 · Granted Jul 16, 2013

Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-iso-propyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms

Inventors: Martin James Drysdale (Berkshire, GB); Brian William Dymock (Singapore, SG); Christoph Krell (Basel, CH); Michael Mutz (Freiburg, DE); Holger Petersen (Eimeldingen, DE); Weijia Zheng (Cambridge, MA)
Assignee: Novartis AG
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Quick Facts
Patent No.
US 8,487,095
App. No.
13/415,268
Granted
Jul 16, 2013
Kind
B2
Abstract

The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations.

Claims (3)

1. A salt which is 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide hydrochloride or a hydrate thereof.

2. A crystalline form of the salt according to claim 1 .

3. A crystalline form according to claim 2 which shows an X-ray diffraction diagram of the type shown in FIG. 10 , in which the relative peak intensities of each peak do not deviate by more than 10% of the relative peak intensities in the diagram shown in FIG. 10 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 26, 2022
From: NOVARTIS AG
To: VERNALIS (R&D) LIMITED
Reel/Frame 058771/0965 →
CHANGE OF NAME Recorded Jan 24, 2022
From: VERNALIS DEVELOPMENT LIMITED
To: LIGAND UK DEVELOPMENT LIMITED
Reel/Frame 058738/0271 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 24, 2022
From: VERNALIS (R&D) LIMITED
To: VERNALIS DEVELOPMENT LIMITED
Reel/Frame 058822/0570 →
Priority Claims (1)
EP 07103346 · Mar 1, 2007 · regional
Continuity (2)
Division 12529090
Related Publication 20120172592A1 · Jul 5, 2012