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US 2020/0369724 A1Published application
Crystalline salt forms of boc-d-arg-dmt-lys-(boc)-phe-nh2
AssigneeStealth BioTherapeutics Inc.
InventorScott M. Duncan
Life of this patent
Estimating the term…
Abstract
Disclosed are various crystalline salt forms of Boc-D-Arg-DMT-Lys(Boc)-Phe-NH2.
Claims18
A crystalline form of a salt of Compound I,
- (Boc-D-Arg-DMT-Lys(Boc)-Phe-NH2;
- (I)),
- wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta as described in any one of Tables A′-F′;
- wherein Table A′ is:
- Pos. [°2θ]
- 0
- 3.7579
- 4.2659
- 6.5526
- 7.2841
- 8.0800
- 8.5065
- 9.7875
- 10.6288
- 12.0543
- 12.7809
- 13.3068
- 14.1827
- 14.5619
- 15.0219
- 16.1288
- 16.9425
- 18.0211
- 18.7982
- 19.1243
- 19.6849
- 20.1376
- 20.5047
- 20.9553
- 22.0163
- 22.6867
- 23.2292
- 24.0145
- 24.5746
- 25.1662
- 25.9049
- 26.4986
- 27.4092
- 27.9577
- 29.2173
- 30.4972
- 30.9418
- 31.7727
- 32.2938
- 33.4213
- Table B′ is:
- Pos. [°2θ]
- 6
- 3.7036
- 4.4432
- 6.5634
- 7.4018
- 9.7210
- 10.6210
- 11.0920
- 12.7331
- 13.1598
- 14.0930
- 14.7901
- 16.7103
- 17.1509
- 18.0233
- 18.5346
- 18.7979
- 19.1239
- 19.5235
- 19.8085
- 20.1544
- 20.6070
- 20.8573
- 21.3109
- 22.0189
- 22.6758
- 23.0757
- 23.6744
- 23.9728
- 24.4777
- 25.7316
- 26.4407
- 27.7972
- 30.1162
- 32.1646
- Table C′ is:
- Pos. [°2θ]
- 5.1621
- 8.9359
- 10.7664
- 13.3445
- 14.3884
- 15.9863
- 17.2952
- 18.8443
- 19.5521
- 21.0051
- 23.2998
- 24.6506
- Table D′ is:
- Pos. [°2Th.]
- 5.4291
- 8.0335
- 9.0773
- 10.8149
- 13.4288
- 14.7938
- 15.7960
- 17.5693
- 18.9795
- 19.6937
- 21.3056
- 22.2563
- 24.1299
- 25.7352
- 27.6495
- 30.9496
- Table E′ is:
- Pos. [°2θ]
- 4.0824
- 7.2188
- 7.7660
- 8.1685
- 8.7856
- 10.1057
- 11.7275
- 12.0519
- 12.2864
- 12.7774
- 13.2740
- 13.6796
- 14.4861
- 14.9214
- 15.1377
- 15.5347
- 16.1829
- 17.7646
- 18.1548
- 18.5392
- 18.9751
- 19.9095
- 20.3639
- 21.0328
- 21.9414
- 21.9676
- 22.2732
- 22.8116
- 23.3197
- 23.5325
- 24.0190
- 24.8019
- 25.2913
- 25.6339
- 26.6566
- 27.7426
- 28.2705
- 28.9314
- 29.2563
- 30.0846
- 30.7947
- 31.5899
- 31.9371
- 32.8553
- and
- Table F′ is:
- Pos. [°2θ]
- 3.6742
- 4.4204
- 6.7177
- 7.0320
- 8.2133
- 9.8583
- 10.2604
- 12.3942
- 13.2923
- 13.6972
- 14.1013
- 14.6960
- 15.7923
- 16.4926
- 17.0775
- 17.2537
- 18.0813
- 18.4075
- 18.9537
- 19.5451
- 19.7885
- 20.2166
- 20.6718
- 20.8819
- 21.6381
- 22.2851
- 22.6611
- 23.0749
- 24.3020
- 24.7773
- 25.5656
- 26.6658
- 27.2542
- 27.7067
- 28.3209
- 29.3217
- 30.1348
- 30.4172
- 31.1772
- 32.4960
- 33.6018
201 more elements
A crystalline form of a salt of Compound I,
- wherein said crystalline form has characteristic peaks in its XRPD pattern as described in any of the following spectra:
(canceled)
A crystalline form of a hydrochloride salt of Compound I,
- wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of:
- 3.8, 4.3, 9.8, 14.6, 18.0, 18.8, 20.9, and 22.7.
A crystalline form of a hydrochloride salt of Compound I,
- wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of:
- 3.7, 4.4, 6.6, 9.7, 14.8, 18.0, 18.5, 18.8, 19.1, 20.9, and 22.7.
A crystalline form of a tosylate salt of Compound I,
- wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of:
- 5.2, 8.9, 14.4, 17.3, 18.8, 19.5, and 21.0.
A crystalline form of a mesylate salt of Compound I,
- wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of:
- 5.4, 13.4, 14.8, 15.8, 17.6, 19.0, and 21.3.
A crystalline form of an oxalate salt of Compound I,
- wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of:
- 7.8, 10.1, 12.8, 17.8, 18.5, 19.9, and 22.3.
A crystalline form of a benzoate salt of Compound I,
- wherein said crystalline form has characteristic peaks in its XRPD pattern at values of two theta (° 2θ) of:
- 3.7, 4.4, 14.1, 18.1, 18.9, 20.7, 22.3, and 24.3.
A method of making Compound II, the method comprising deprotecting compound (I),
- or a salt thereof, thereby making compound (II)
- or a salt thereof.
Dependencies are inferred from the claim text.