US2023339967A1PendingUtilityA1
Solid forms of an s1p-receptor modulator
Est. expiryOct 31, 2039(~13.3 yrs left)· nominal 20-yr term from priority
Inventors:Stéphane De LombaertAna Rosario Mollo SarnoMichael A. ChristieEdward L. CiolkowskiSusana Del Rio GancedoJoseph Stephen HarrisLucy Kristina MappMateusz PitakScott L. Childs
C07D 498/04C07B 2200/13A61P 25/00A61K 31/437
57
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Claims
Abstract
This application relates to solid forms of an S1P-receptor modulator, which are useful in the treatment of diseases or disorders associated with activity of S1P, including CNS disorders.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A solid form of Compound 1 having the formula:
wherein the solid form is crystalline.
2 - 5 . (canceled)
6 . The solid form of claim 1 , wherein the solid form has Form A, wherein the solid form has at least one characteristic XRPD peak selected from about 4.7, about 9.3, about 13.9, about 15.8, about 18.6, about 19.0, about 21.5, and about 27.4 degrees 2-theta.
7 - 15 . (canceled)
16 . A process for preparing the solid form of claim 6 , comprising recrystallizing Compound 1 in DMSO, wherein the recrystallizing comprises heating a solution of Compound 1 in DMSO to a temperature that is greater than or equal to 90° C.
17 - 19 . (canceled)
20 . A solid form prepared by the process of claim 16 .
21 . The solid form of claim 1 , wherein the solid form has Form B, wherein the solid form has at least one characteristic XRPD peak selected from about 8.5, about 15.1, about 16.5, about 21.5, about 23.5, about 24.6, and about 25.5 degrees 2-theta.
22 - 29 . (canceled)
30 . A process for preparing the solid form of claim 21 , comprising recrystallizing Compound 1 in a mixture of water and acetic acid.
31 . A solid form prepared by the process of claim 30 .
32 . The solid form of claim 1 , wherein the solid form has Form C, wherein the solid form has at least one characteristic XRPD peak selected from about 7.4, about 11.0, about 22.2, about 25.0, about 25.4, about 28.2, and about 29.8 degrees 2-theta.
33 - 39 . (canceled)
40 . A process for preparing the solid form of claim 32 , comprising recrystallizing Compound 1 in a solvent comprising DMSO.
41 . A solid form prepared by the process of claim 40 .
42 . The solid form of claim 1 , wherein the solid form has Form D, having an XRPD pattern with characteristic peaks as substantially shown in Figure 11.
43 . (canceled)
44 . A process for preparing the solid form of claim 42 , comprising recrystallizing Compound 1 in a solvent comprising dimethylacetamide.
45 . A solid form prepared by the process of claim 44 .
46 . The solid form of claim 1 , wherein the solid form has Form E, wherein the solid form has at least one characteristic XRPD peak selected from about 8.7, about 15.3, about 16.2, about 18.3, about 23.2, about 25.5, and about 28.2 degrees 2-theta.
47 - 50 . (canceled)
51 . A process for preparing the solid form of claim 46 , comprising heating Compound 1 Form B to a temperature that is greater than or equal to 150° C.
52 . A solid form prepared by the process of claim 51 .
53 . A pharmaceutical composition comprising a solid form of claim 1 , and at least one pharmaceutically acceptable carrier.
54 . A method of modulating S1P receptor activity, said method comprising contacting a solid form of claim 1 , or a pharmaceutically acceptable salt thereof, with an S1P receptor.
55 . A method of treating a disease or disorder associated with S1P, said method comprising administering to a patient in need thereof a therapeutically effective amount of a solid form of claim 1 , or a pharmaceutically acceptable salt thereof.
56 . A method of treating a CNS disorder in a patient in need thereof, said method comprising administering to the patient a therapeutically effective amount of the solid form of claim 1 , or a pharmaceutically acceptable salt thereof.Cited by (0)
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