Crystalline forms of n-[2-[[(2,3-difluorophenyl)methyl]thio]-6--4-pyrimidinyl]-1-azetidinesulfonamide

Abstract

There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.

1 . A crystalline form of N-[2-[[(2,3-di:fluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfon-amide (also referred to as “Compound I”), characterised by a powder X-ray diffraction pattern, measured using a wavelength of X-rays 1.5418 A, comprising at least one crystalline peak with a 2-Theta value (in degrees) of 21.0, 28.8 and/or 29.1. 
     
     
         2 . A compound/form as claimed in  claim 1  characterised by a powder X-ray diffraction pattern, measured using a wavelength of X-rays 1.5418 A, comprising at least 2 crystalline peaks with a 2-Theta value (in degrees) of 21.0, 28.8 and/or 29.1. 
     
     
         3 . A compound/form as claimed in  claim 2  characterised by a powder X-ray diffraction pattern, measured using a wavelength of X-rays 1.5418 A, comprising at least 3 crystalline peaks with a 2-Theta value (in degrees) of 21.0, 28.8 and/or 29.1. 
     
     
         4 . A compound/form as claimed in  claim 1  characterised by a powder X-ray diffraction pattern, measured using a wavelength of X-rays 1.5418 A, comprising a further crystalline peak with a 2-Theta value (in degrees) selected from of 12.9 and 18.0. 
     
     
         5 . A compound/form as claimed in  claim 1  characterised by a powder X-ray diffraction pattern, measured using a wavelength of X-rays 1.5418 A, comprising crystalline peaks with a 2-Theta value (in degrees) of 12.9, 13.1, 18.0, 21.0, 22.5, 25.1, 25.3, 28.8, 29.1 and 30.4. 
     
     
         6 . A crystalline form of Compound I, characterised by a powder X-ray diffraction pattern, measured using a wavelength of X-rays 1.5418 A, comprising at least one crystalline peak with a 2-Theta value (in degrees) of around 12.9, 18.0 and/or 21.0. 
     
     
         7 . A crystalline form of Compound, I which has a melting point (onset) of 152.7° C. 
     
     
         8 . A compound/form as defined in  claim 1 , or a pharmaceutically acceptable salt thereof, for use as a pharmaceutical. 
     
     
         9 . A pharmaceutical formulation including a compound/form as claimed in  claim 1 , or a pharmaceutically acceptable salt thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. 
     
     
         10 . A compound/form as defined in  claim 1 , or a pharmaceutically acceptable salt thereof, for use in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial. 
     
     
         11 . The use of a compound/form as defined in  claim 1 , or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial. 
     
     
         12 . A method of treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial, which method comprises the administration of a compound/form as defined in  claim 1 , or a pharmaceutically acceptable salt thereof, to a patient in need of such treatment. 
     
     
         13 . The method of  claim 12 , wherein the disorder is asthma, allergic rhinitis, COPD, bronchiectasis, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid arthritis, psoriasis or cancer. 
     
     
         14 . A combination product comprising:
 (a) the compound/form as defined in  claim 1 , or a pharmaceutically acceptable salt thereof; and (b) one or more active ingredient that is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial, or a pharmaceutically-acceptable salt thereof.   
     
     
         15 . A combination product comprising:
 (a) pharmaceutical formulation including the compound/form of  claim 1 , or a pharmaceutically acceptable salt thereof, (b) an active ingredient that is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial, or a pharmaceutically-acceptable salt thereof, and (c) a pharmaceutically-acceptable adjuvant, diluent or carrier.   
     
     
         16 . A combination product comprising:
 a kit of parts comprising components: (a) a pharmaceutical formulation including a compound/form as defined in  claim 1 , or a pharmaceutically acceptable salt thereof, in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including an active ingredient that is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial, or a pharmaceutically-acceptable salt thereof, in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier, which components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other.