| 摘要 |
Disclosed is a microcrystalline form of (5-fluoro-2-methyl-3-quinolin-2-ylmethyl-indol-1-yl)-acetic acid, wherein at least 90% of the crystals have a diameter not greater than about 3mm. Also disclosed is a process for the preparation of a microcrystalline form of (5-fluoro-2methyl-3-quinolin-2-ylmethyl-indol-1-yl)-acetic acid as described above, the process comprising: i. treating crystalline (5-fluoro-2-methyl-3-quinolin-2-ylmethyl-indol-1-yl)-acetic acid with an aqueous weak base; and ii. treating the mixture with a weak acid; and iii. collecting the precipitated microcrystalline (5-fluoro-2-methyl-3-quinolin-2ylmethyl-indol-1-yl)-acetic acid. The use of the above microcrystalline form of (5-fluoro-2-methyl-3-quinolin-2ylmethyl-indol-1-yl)-acetic acid in the preparation of an agent for the treatment or prevention of allergic asthma, perennial allergic rhinitis, seasonal allergic rhinitis, atopic dermatitis, contact hypersensitivity (including contact dermatitis), conjunctivitis, especially allergic conjunctivitis, eosinophilic bronchitis, food allergies, eosinophilic gastroenteritis, inflammatory bowel disease, ulcerative colitis and Crohn's disease, mastocytosis and also other PGD2-mediated diseases, for example autoimmune diseases such as hyper IgE syndrome and systemic lupus erythematus, psoriasis, acne, multiple sclerosis, allograft rejection, reperfusion injury, chronic obstructive pulmonary disease, as well as rheumatoid arthritis, psoriatic arthritis and osteoarthritis and neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, stroke and amyoptrophic lateral sclerosis is further disclosed.
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