Crystal forms of saxagliptin and processes for preparing same
First Claim
1. A method for treating diabetes, insulin resistance, hyperglycemia, dyslipidemia or elevated blood levels of free fatty acids or glycerol, obesity, Syndrome X, dysmetabolic syndrome, retinopathy, neuropathy, nephropathy, cataracts, hypertriglyceridemia, hyperinsulinemia, atherosclerosis, impaired glucose homeostasis, impaired glucose tolerance, infertility, polycystic ovary syndrome, arthritis, allograft rejection in transplantation, scleroderma, multiple sclerosis, necrotizing enteritis, microvillus inclusion disease, celiac disease, inflammatory bowel syndrome, anorexia nervosa, osteoporosis, lupus erythematosis, psoriasis, Crohn'"'"'s disease, or ulcerative colitis, which comprises administering to a mammalian species in need of treatment or an effective amount of a crystalline compound in a form selected from H2-1 (1HCl), H2-1 (2HCl), H0.75-3, H1.67-1, P-5, N-3, H-1 (1H2O), H-1 (1PhCO2H/1H2O), N-1, and mixtures thereof,wherein the crystalline compound of form H2-1 (1HCl) has structure
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Abstract
Physical crystal structures of a compound of the formula I:
are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
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Citations
31 Claims
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1. A method for treating diabetes, insulin resistance, hyperglycemia, dyslipidemia or elevated blood levels of free fatty acids or glycerol, obesity, Syndrome X, dysmetabolic syndrome, retinopathy, neuropathy, nephropathy, cataracts, hypertriglyceridemia, hyperinsulinemia, atherosclerosis, impaired glucose homeostasis, impaired glucose tolerance, infertility, polycystic ovary syndrome, arthritis, allograft rejection in transplantation, scleroderma, multiple sclerosis, necrotizing enteritis, microvillus inclusion disease, celiac disease, inflammatory bowel syndrome, anorexia nervosa, osteoporosis, lupus erythematosis, psoriasis, Crohn'"'"'s disease, or ulcerative colitis, which comprises administering to a mammalian species in need of treatment or an effective amount of a crystalline compound in a form selected from H2-1 (1HCl), H2-1 (2HCl), H0.75-3, H1.67-1, P-5, N-3, H-1 (1H2O), H-1 (1PhCO2H/1H2O), N-1, and mixtures thereof,
wherein the crystalline compound of form H2-1 (1HCl) has structure
Specification