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CRYSTALLINE (R)-5-CARBAMOYLPYRIDIN-3-YL-2-METHYL-4-(3-(TRIFLUOROMETHOXY)BENZYL)PIPERAZINE-1-CARBOXYLATE, COMPOSITIONS AND METHODS OF USE THEREOF

2023
Online Patent

Titel:
CRYSTALLINE (R)-5-CARBAMOYLPYRIDIN-3-YL-2-METHYL-4-(3-(TRIFLUOROMETHOXY)BENZYL)PIPERAZINE-1-CARBOXYLATE, COMPOSITIONS AND METHODS OF USE THEREOF
Link:
Veröffentlichung: 2023
Medientyp: Patent
Sonstiges:
  • Nachgewiesen in: USPTO Patent Applications
  • Sprachen: English
  • Document Number: 20230382861
  • Publication Date: November 30, 2023
  • Appl. No: 18/143765
  • Application Filed: May 05, 2023
  • Claim: 1-61. (canceled)
  • Claim: 62. A single unit dosage form comprising a crystalline form of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, wherein: the crystalline form is Form A of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 18.1, 20.1, and 22.3 degrees 2 θ±0.2 degrees 2 θ; the crystalline form is Form B of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 16.2, 18.2, and 19.2 degrees 2 θ±0.2 degrees 2 θ; the crystalline form is Form C of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 18.0, 20.0, and 21.0 degrees 2 θ±0.2 degrees 2 θ; the crystalline form is Form D of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 13.4, 21.0, and 23.8 degrees 2 θ±0.2 degrees 2 θ; or the crystalline form is Form E of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 17.8, 21.3, and 22.8 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 63. The single unit dosage form of claim 62, wherein the crystalline form is Form A of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoro methoxy)b enzyl)pip e razine -1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 18.1, 20.1, and 22.3 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 64. The single unit dosage form of claim 63, wherein the X-ray powder diffraction pattern further comprises peaks at 9.9, 19.9, and 24.7 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 65. The single unit dosage form of claim 62, wherein the crystalline form is Form B of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 16.2, 18.2, and 19.2 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 66. The single unit dosage form of claim 65, wherein the X-ray powder diffraction pattern further comprises peaks at 15.1, 18.7, and 20.1 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 67. The single unit dosage form of claim 62, wherein the crystalline form is Form C of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 18.0, 20.0, and 21.0 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 68. The single unit dosage form of claim 67, wherein the X-ray powder diffraction pattern further comprises peaks at 12.3, 16.8, and 25.5 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 69. The single unit dosage form of claim 62, wherein the crystalline form is Form D of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoro methoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 13.4, 21.0, and 23.8 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 70. The single unit dosage form of claim 69, wherein the X-ray powder diffraction pattern further comprises peaks at 18.3, 26.7, and 29.5 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 71. The single unit dosage form of claim 62, wherein the crystalline form is Form E of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoro methoxy)benzyl)piperazine-1-carboxylate, having an X-ray powder diffraction pattern comprising peaks at 17.8, 21.3, and 22.8 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 72. The single unit dosage form of claim 71, wherein the X-ray powder diffraction pattern further comprises peaks at 15.8, 18.4, and 21.9 degrees 2 θ±0.2 degrees 2 θ.
  • Claim: 73. The single unit dosage form of claim 62, wherein the single unit dosage form is suitable for oral, mucosal, rectal, nasal, vaginal, parenteral, subcutaneous, intramuscular, bolus injection, intraarterial, intravenous, sublingual, transdermal, buccal, or topical administration.
  • Claim: 74. The single unit dosage form of claim 73, wherein the single unit dosage form is a tablet, caplet, capsule, powder, or sterile solid that can be reconstituted to provide a liquid dosage form.
  • Claim: 75. The single unit dosage form of claim 73, wherein the single unit dosage form is a tablet, caplet, capsule, or liquid suitable for oral administration.
  • Claim: 76. The single unit dosage form of claim 73, wherein the single unit dosage form is a solution ready for injection, dry product ready to be dissolved or suspended in a pharmaceutically acceptable vehicle for injection, suspension ready for injection, or an emulsion ready for injection.
  • Claim: 77. The single unit dosage form of claim 62 comprising about 0.1 mg to about 1,000 mg of the crystalline form.
  • Current International Class: 07; 61

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