US2017015656A1PendingUtilityA1

Novel compounds

64
Assignee: GLAXO GROUP LTDPriority: Apr 30, 2009Filed: Aug 2, 2016Published: Jan 19, 2017
Est. expiryApr 30, 2029(~2.8 yrs left)· nominal 20-yr term from priority
Inventors:Julie Nicole HamblinPaul JonesSuzanne Elaine KeelingJoelle LeCharlotte Jane MitchellNigel James Parr
A61P 7/02A61P 7/00A61P 43/00A61P 9/10A61P 37/00A61P 37/08A61P 9/00A61P 3/10A61P 37/06A61P 33/02A61P 25/04A61P 35/02A61P 31/10A61P 35/00A61P 29/02A61P 31/00A61P 29/00A61P 31/12A61P 25/28A61P 25/00A61P 31/04A61P 1/00A61P 11/06A61P 1/18A61P 1/16A61P 15/08A61P 13/12A61P 17/00A61P 11/00A61P 11/02A61P 19/02A61K 31/535A61K 31/497A61K 31/5377C07D 413/14A61K 31/5375A61K 31/496A61K 45/06C07B 2200/13Y02A50/30
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Claims

Abstract

The invention is directed to certain novel compounds. Specifically, crystalline forms of N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide and crystalline 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole, along with salts thereof.

Claims

exact text as granted — not AI-modified
1 - 12 . (canceled) 
     
     
         13 . N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide or a salt thereof in crystalline form. 
     
     
         14 . The compound according to  claim 13 , wherein N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide is present as free base is present in crystalline form. 
     
     
         15 . The compound according to  claim 14 , wherein N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide has an XRPD (X-ray powder diffraction) pattern having peaks (°2θ) at about 4.5, about 11.7 and/or about 12.9. 
     
     
         16 . The compound according to  claim 14 , wherein N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide has an XRPD pattern comprising peaks substantially as set out in Table 2. 
     
     
         17 . The compound according to  claim 14 , wherein N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide has an XRPD pattern substantially in accordance with  FIG. 2 . 
     
     
         18 . 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole or a salt thereof in crystalline form. 
     
     
         19 . The compound of  claim 18 , wherein 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole is present as the hydrochloride salt in crystalline form. 
     
     
         20 . The compound according to  claim 19 , wherein crystalline 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole hydrochloride has an XRPD (X-ray powder diffraction) pattern with peaks (°2θ) at about 5.2, about 10.3 and/or about 12.8. 
     
     
         21 . The compound according to  claim 19 , wherein crystalline 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole hydrochloride has an XRPD pattern comprising peaks substantially as set out in Table 1. 
     
     
         22 . The compound according to  claim 19 , wherein crystalline 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole hydrochloride has an XRPD pattern substantially in accordance with  FIG. 1 .

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