POLYMORPHIC COMPOUNDS AND USES THEREOF
The present invention relates to compounds and methods useful for selectively modulating mTORC1 activity.
1 . Compound A:
of forms A, B or C.
2 . The compound according to claim 1 , wherein said compound is crystalline.
3 . The compound according to claim 1 , wherein said compound is a crystalline solid substantially free of amorphous compound A.
4 . The compound according to claim 1 , wherein said compound is substantially free of impurities.
5 . The compound according to claim 1 , having one or more peaks in its XRPD selected from those at about 4.4, about 16.2 and about 17.7 degrees 2-theta.
6 . The compound according to claim 5 , having at least two peaks in its XRPD selected from those at about 4.4, about 16.2 and about 17.7 degrees 2-theta.
7 . The compound according to claim 6 , wherein said compound is of Form A.
8 . The compound according to claim 1 , having an XRPD substantially similar to that depicted in FIG. 1 .
9 . The compound according to claim 1 , having one or more peaks in its XRPD selected from those at about 5.0, about 15.2 and about 17.5 degrees 2-theta.
10 . The compound according to claim 9 , having at least two peaks in its XRPD selected from those at about 5.0, about 15.2 and about 17.5 degrees 2-theta.
11 . The compound according to claim 10 , wherein said compound is of Form B.
12 . The compound according to claim 1 , having an XRPD substantially similar to that depicted in FIG. 4 .
13 . The compound according to claim 1 , having one or more peaks in its XRPD selected from those at about 7.0, about 16.1 and about 16.3 degrees 2-theta.
14 . The compound according to claim 9 , having at least two peaks in its XRPD selected from those at about 7.0, about 16.1 and about 16.3 degrees 2-theta.
15 . The compound according to claim 10 , wherein said compound is of Form C.
16 . The compound according to claim 1 , having an XRPD substantially similar to that depicted in FIG. 7 .
17 . A composition comprising the compound according to claim 1 and a pharmaceutically acceptable carrier or excipient.
18 . A method of treating method of treating a disease, disorder, or condition selected from treatment-resistant depression, a lysosomal storage disorder, JNCL, cystinosis, Fabry disease, MLIV, mental retardation or a genetic form of autism,
comprising administering to a patient in need thereof an effective amount of a compound according to claim 1 or composition thereof.
19 . A method of activating mTORC1 in a patient comprising administering to a patient in need thereof an effective amount of a compound according to claim 1 or composition thereof.
20 . Compound 1:
of form A, wherein x is about ¾.
21 . The compound according to claim 20 , wherein said compound is crystalline.
22 . The compound according to claim 20 , wherein said compound is a crystalline solid substantially free of amorphous compound 1.
23 . The compound according to claim 20 , wherein said compound is substantially free of impurities.
24 . The compound according to claim 20 , having one or more peaks in its XRPD selected from those at about 17.1, about 17.3 and about 18.3 degrees 2-theta.
25 . The compound according to claim 24 , having at least two peaks in its XRPD selected from those at about 17.1, about 17.3 and about 18.3 degrees 2-theta.
26 . The compound according to claim 20 , having an XRPD substantially similar to that depicted in FIG. 11 .
27 . A composition comprising the compound according to claim 20 and a pharmaceutically acceptable carrier or excipient.
28 . A method of treating method of treating a disease, disorder, or condition selected from treatment-resistant depression, a lysosomal storage disorder, JNCL, cystinosis, Fabry disease, MLIV, mental retardation or a genetic form of autism,
comprising administering to a patient in need thereof an effective amount of a compound according to claim 20 or composition thereof.
29 . A method of activating mTORC1 in a patient comprising administering to a patient in need thereof an effective amount of a compound according to claim 20 or composition thereof.