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US 2022/0024893 A1Published application
Crystalline forms of 1-((2r,4r)-2-(1h-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate
AssigneePfizer Inc.
InventorsEric Christian Hansen, Christopher Scott Seadeek
Life of this patent
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Abstract
This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
Claims41
1-17. (canceled)
18:
- A method of treating a hematologic malignancy in a mammal, comprising administering to the mammal a pharmaceutical composition comprising a therapeutically effective amount of a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, having the structure:
- and having a powder X-ray diffraction pattern comprising peaks at 2θ values of:
- 11.6, 12.1 and 19.6 °2θ±0.2 °2θ, and a pharmaceutically acceptable excipient.
19:
- A method of treating a hematologic malignancy in a mammal, comprising administering to the mammal a pharmaceutical composition comprising a therapeutically effective amount of a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, having the structure:
- and having:
- (a) a powder X-ray diffraction pattern comprising peaks at 2θ values of:
- 11.6 and 12.1 °2θ±0.2 °2θ;
- and (b) a Raman spectrum comprising wavenumber (cm−1) values of:
- 1612 and 2219 cm−1±2 cm−1, and a pharmaceutically acceptable excipient
3 more elements
20:
- A method of treating a hematologic malignancy in a mammal, comprising administering to the mammal a pharmaceutical composition comprising a therapeutically effective amount of a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, having the structure:
- and having:
- (a) a powder X-ray diffraction pattern comprising peas at 2θ values of:
- 11.6 and 12.1 °2θ±0.2 °2θ;
- (b) a Raman spectrum comprising wavenumber (cm−1) values of:
- 1612 and 2219 cm−1±2 cm−1;
- and (c) a 13C solid state NMR spectrum comprising a resonance (ppm) value of:
- 148.3 ppm±0.2 ppm, and a pharmaceutically acceptable excipient.
5 more elements
21:
- A method of treating a hematologic malignancy in a mammal, comprising administering to the mammal a pharmaceutical composition comprising a therapeutically effective amount of a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, having the structure:
- and having:
- (a) a powder X-ray diffraction pattern comprising peaks at 2θ values of:
- 11.6 and 12.1 °2θ±0.2 °2θ;
- and (b) a 13C solid state NMR spectrum comprising a resonance (ppm) value of:
- 148.3 ppm±0.2 ppm, and a pharmaceutically acceptable excipient.
3 more elements
22:
- The method of claim 18, wherein the pharmaceutical composition is suitable for oral administration.
23:
- The method of claim 19, wherein the pharmaceutical composition is suitable for oral administration.
24:
- The method of claim 20, wherein the pharmaceutical composition is suitable for oral administration.
25:
- The method of claim 21, wherein the pharmaceutical composition is suitable for oral administration.
26:
- The method of claim 22, wherein the pharmaceutical composition is a tablet.
27:
- The method of claim 23, wherein the pharmaceutical composition is a tablet.
28:
- The method of claim 24, wherein the pharmaceutical composition is a tablet.
29:
- The method of claim 25, wherein the pharmaceutical composition is a tablet.
30:
- The method of claim 22, wherein the mammal is a human.
31:
- The method of claim 23, wherein the mammal is a human.
32:
- The method of claim 24, wherein the mammal is a human.
33:
- The method of claim 25, wherein the mammal is a human.
34:
- The method of claim 22, wherein the hematologic malignancy is selected from the group consisting of acute myeloid leukemia, acute lymphoblastic leukemia, chronic myelomonocytic leukemia, myelofibrosis and myelodysplastic syndrome.
35:
- The method of claim 23, wherein the hematologic malignancy is selected from the group consisting of acute myeloid leukemia, acute lymphoblastic leukemia, chronic myelomonocytic leukemia, myelofibrosis and myelodysplastic syndrome.
36:
- The method of claim 24, wherein the hematologic malignancy is selected from the group consisting of acute myeloid leukemia, acute lymphoblastic leukemia, chronic myelomonocytic leukemia, myelofibrosis and myelodysplastic syndrome.
37:
- The method of claim 25, wherein the hematologic malignancy is selected from the group consisting of acute myeloid leukemia, acute lymphoblastic leukemia, chronic myelomonocytic leukemia, myelofibrosis and myelodysplastic syndrome.
38:
- The method of claim 22, wherein the hematologic malignancy is acute myeloid leukemia.
39:
- The method of claim 23, wherein the hematologic malignancy is acute myeloid leukemia.
40:
- The method of claim 24, wherein the hematologic malignancy is acute myeloid leukemia.
41:
- The method of claim 25, wherein the hematologic malignancy is acute myeloid leukemia.
42:
- The method of claim 22, wherein the hematologic malignancy is acute lymphoblastic leukemia.
43:
- The method of claim 23, wherein the hematologic malignancy is acute lymphoblastic leukemia.
44:
- The method of claim 24, wherein the hematologic malignancy is acute lymphoblastic leukemia.
45:
- The method of claim 25, wherein the hematologic malignancy is acute lymphoblastic leukemia.
46:
- The method of claim 22, wherein the hematologic malignancy is chronic myelomonocytic leukemia.
47:
- The method of claim 23, wherein the hematologic malignancy is chronic myelomonocytic leukemia.
48:
- The method of claim 24, wherein the hematologic malignancy is chronic myelomonocytic leukemia.
49:
- The method of claim 25, wherein the hematologic malignancy is chronic myelomonocytic leukemia.
50:
- The method of claim 22, wherein the hematologic malignancy is myelofibrosis.
51:
- The method of claim 23, wherein the hematologic malignancy is myelofibrosis.
52:
- The method of claim 24, wherein the hematologic malignancy is myelofibrosis.
53:
- The method of claim 25, wherein the hematologic malignancy is myelofibrosis.
54:
- The method of claim 22, wherein the hematologic malignancy is myelodysplastic syndrome.
55:
- The method of claim 23, wherein the hematologic malignancy is myelodysplastic syndrome.
56:
- The method of claim 24, wherein the hematologic malignancy is myelodysplastic syndrome.
57:
- The method of claim 25, wherein the hematologic malignancy is myelodysplastic syndrome.