Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound 1) for use in SIPI receptor-associated disorders
First Claim
1. A method for treating an S1P1 receptor-associated disorder in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a crystalline free-plate habit of L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid;
- wherein said crystalline free-plate habit has a BET specific surface area of about 0.1 m2/g to about 5.0 m2/g, wherein said disorder is selected from the group consisting of;
biliary cirrhosis, psoriatic arthritis, rheumatoid arthritis, type I diabetes, multiple sclerosis, inflammatory skin disease, psoriasis, atopic dermatitis, acne, inflammatory bowel disease, Crohn'"'"'s disease, ulcerative colitis, systemic lupus erythematosus, and transplant rejection.
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Abstract
The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
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25 Claims
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1. A method for treating an S1P1 receptor-associated disorder in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a crystalline free-plate habit of L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid;
- wherein said crystalline free-plate habit has a BET specific surface area of about 0.1 m2/g to about 5.0 m2/g, wherein said disorder is selected from the group consisting of;
biliary cirrhosis, psoriatic arthritis, rheumatoid arthritis, type I diabetes, multiple sclerosis, inflammatory skin disease, psoriasis, atopic dermatitis, acne, inflammatory bowel disease, Crohn'"'"'s disease, ulcerative colitis, systemic lupus erythematosus, and transplant rejection. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25)
- wherein said crystalline free-plate habit has a BET specific surface area of about 0.1 m2/g to about 5.0 m2/g, wherein said disorder is selected from the group consisting of;
Specification