JPWO2020132381A5 - - Google Patents

Claims (13)

Formula (I)

and a coformer, wherein the coformer is succinic acid or citric acid. 2. The co-crystal of claim 1, wherein the coformer is succinic acid. 3. The co-crystal of claim 2, wherein the co-crystal has one or more of the following characteristics:
a) When the single crystal structure measurements are performed at room temperature, the unit cell parameters are substantially the same as

is a single crystal structure with
b) Substantially Figure 1:

A PXRD pattern indicated by is observed;
c) a PXRD pattern (at room temperature) containing four or more 2-theta values selected from 4.5 ± 0.2, 9.5 ± 0.2, 14.6 ± 0.2, 16.3 ± 0.2, 17.6 ± 0.2, 21.4 ± 0.2, 22.4 ± 0.2, and 25.9 ± 0.2; , CuKα λ=1.5418 Å);
d) Substantially Figure 5:

is an infrared spectrum denoted by; and/or
e) Substantially Figure 6:

is an FT-Raman spectrum indicated by 4. The co-crystal of any of claims 1-3, wherein the ratio of compound of formula (I) to succinic acid is 1:0.5. 2. The co-crystal of claim 1, wherein the coformer is citric acid. 6. The co-crystal of claim 5, which is of the N-1 form and has one or more of the following characteristics:
a) Unit cell parameters substantially the same as

is a single crystal structure with
b) Substantially Figure 6:

is a PXRD pattern denoted by; and/or
c) a PXRD pattern containing 4 or more 2-theta values selected from 6.4 ± 0.2, 12.7 ± 0.2, 14.4 ± 0.2, 17.1 ± 0.2, 23.9 ± 0.2, 25.0 ± 0.2, and 26.6 ± 0.2 (room temperature, CuKα λ = 1.5418 Å). 7. The co-crystal of any of claims 5-6, wherein the ratio of compound of formula (I) to citric acid is 1:1. 8. The co-crystal of any of claims 5-7 consisting essentially of the N-1 form. 6. The co-crystal of claim 5, which is of the N-2 form and has one or more of the following characteristics:
a) When the single crystal structure measurements are performed at room temperature, the unit cell parameters are substantially the same as

is a single crystal structure with
b) Substantially Figure 12:

is a PXRD pattern denoted by; and/or
c) 4 or more 2-theta values selected from 4.6 ± 0.2, 5.5 ± 0.2, 8.4 ± 0.2, 11.3 ± 0.2, 14.6 ± 0.2, 16.4 ± 0.2, 21.1 ± 0.2, 24.2 ± 0.2, and 25.2 ± 0.2 PXRD pattern (room temperature, CuKα λ=1.5418 Å). 10. The co-crystal of claim 9, wherein the ratio of compound of formula (I) to citric acid is 1:1. 10. The co-crystal of claim 9 consisting essentially of the N-2 form. 12. The co-crystal of any one of claims 1-11 in substantially pure form. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a co-crystal as defined in any of claims 1-12, alone or in combination with another therapeutic agent.