IP Library › Granted Patent US 10,689,363
Granted Patent B2
US 10,689,363 · App. 16/578,676 · Granted Jun 23, 2020

Crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-piperidin-1-yl)-propenone

Inventors: Axel Becker (Seeheim-Jugenheim, DE); Marco Poma (Rome, IT); Edoardo Burini (Guidonia Montecelio, IT); Christoph Saal (Otzberg, DE); Vedad Theuerkorn (Pfungstadt, DE)
Assignee: Merck Patent GmbH
C07D401/12A61P35/00A61P35/02C07D403/12C07B2200/13
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Quick Facts
Patent No.
US 10,689,363
App. No.
16/578,676
Granted
Jun 23, 2020
Kind
B2
Abstract

A solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, are useful as BTK inhibitors.

Claims (16)

1. A solid form of compound 1,

wherein said solid form is a crystalline form A2,

wherein said form A2 is characterized by a crystal form, having a monoclinic space group P2 1 with the lattice parameters (at 200 K) a=9.4±0.1 Å, b=37.2±0.2 Å, c=12.8±0.1 Å, and β=91.9±0.5° (with α=γ=90°).

2. The solid form of claim 1 , characterized as a mixture of crystalline forms A1 and A2; wherein said crystalline form A1 is characterized by a crystal form, having a monoclinic space group P2 1 with the lattice parameters (at 200 K) a=12.8±0.1 Å, b 9.4±0.1 Å, c=37.3±0.2 Å, and β=98.5±0.5° (with α=γ=90°).

3. A pharmaceutical composition, comprising:

the solid form of compound 1 of claim 1 , and

a pharmaceutically acceptable adjuvant, carrier, or vehicle.

4. A method for treating a BTK-mediated disorder in a patient in thereof, comprising:

administering to said patient a solid form of compound 1 of claim 1 ;

wherein said BTK-mediated disorder is systemic lupus erythematosus (SLE), multiple sclerosis, or rheumatoid arthritis.

5. A pharmaceutical composition, comprising:

a solid form of compound 1 of claim 2 , and

a pharmaceutically acceptable adjuvant, carrier, or vehicle.

6. A method for treating a BTK-mediated disorder in a patient in need thereof, comprising:

administering to said patient a solid form of compound 1 of claim 2 ;

wherein said BTK-mediated disorder is systemic lupus erythematosus (SLE), multiple sclerosis, or rheumatoid arthritis.

Continuity (4)
Continuation 15902482 · Feb 22, 2018
Provisional Application 62463913 · Feb 27, 2017
Provisional Application 62528238 · Jul 3, 2017
Related Publication 20200017464A1 · Jan 16, 2020
Cited By (1)
US 12,251,382