Crystalline solids of a MetAP-2 inhibitor and methods of making and using same
US-9371312-B2 · Jun 21, 2016 · US
US9827221B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9827221-B2 |
| Application number | US-201615145403-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 3, 2016 |
| Priority date | Nov 9, 2010 |
| Publication date | Nov 28, 2017 |
| Grant date | Nov 28, 2017 |
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The disclosure is in part directed to crystalline forms of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol and variants thereof.
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What is claimed is: 1. A pharmaceutical composition comprising a crystalline form of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol, free base, wherein the composition is a suspension of the crystalline form in a pharmaceutically acceptable carrier, wherein the crystalline form is characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 2θ at about 13.3, 17.4, and 19.9. 2. The pharmaceutical composition of claim 1 , wherein the crystalline form of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol, free base, is characterized by a powder X-ray diffraction pattern having characteristic peaks in degrees 2θ at about 7.1, 13.3, 16.3, 17.4, 18.6, 19.4, and 19.9. 3. The pharmaceutical composition of claim 2 , wherein the crystalline form of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol, free base, is characterized by a powder X-ray diffraction pattern having characteristic peaks in degrees 2θ at 5.2, 7.1, 10.4, 13.3, 14.2, 16.3, 17.4, 18.6, 19.4, and 19.9. 4. The pharmaceutical composition of claim 1 , wherein the crystalline form of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol, free base, is characterized by the powder X-ray diffraction pattern shown in FIG. 1 . 5. The pharmaceutical composition of claim 1 , wherein the powder X-ray diffraction pattern was obtained using Cu Kα radiation. 6. The pharmaceutical composition of claim 1 , wherein the pharmaceutically acceptable carrier is an aqueous carrier. 7. A method of treating obesity in a patient in need thereof, comprising subcutaneously administering to the patient an effective amount of the pharmaceutical composition of claim 1 .
by esterified hydroxyl radicals · CPC title
having three-membered rings, e.g. oxirane, fumagillin · CPC title
Anorexiants; Antiobesity agents · CPC title
Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title
directly linked by a ring-member-to-ring-member bond · CPC title
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