Generated: May 25, 2017
|Title:||Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors|
|Abstract:||The invention relates to a pharmaceutical composition of a crystalline monohydrate of the compound of formula (IV) ##STR00001## wherein the crystalline monohydrate is characterized by certain unit cell parameters.|
|Inventor(s):||Lajeunesse; Jean (Candiac, CA), DiMarco; John D. (East Brunswick, NJ), Galella; Michael (Kendall Park, NJ), Chidambaram; Ramakrishnan (Santa Clara, CA)|
|Assignee:||Bristol-Myers Squibb Company (Princeton, NJ)|
1. A pharmaceutical composition comprising, a therapeutically acceptable amount of crystalline monohydrate of the compound of formula (IV) ##STR00062## which is characterized
by unit cell parameters approximately equal to the following: Cell dimensions: a(.ANG.)=13.8632(7); b(.ANG.)=9.3307(3); c(.ANG.)=38.390(2); Volume=4965.9(4).ANG..sup.3 Space group Pbca Molecules/unit cell 8 Density (calculated) (g/cm.sup.3) 1.354;
and pharmaceutically acceptable carriers, including two or more of, a binder, a diluent, a disintegrant, and/or a lubricant.
2. A pharmaceutical composition of claim 1, wherein the compound of formula (IV) is characterized by differential scanning calorimetry thermogram and a thermogravimetric analysis substantially in accordance with that shown in FIG. 2.
3. A pharmaceutical composition of claim 1, wherein the compound of formula (IV) is characterized by an x-ray powder diffraction pattern (CuK.alpha. .lamda.=1.5418 .ANG. at a temperature of about 23.degree. C.) comprising four or more 2.theta. values selected from the group consisting of: 18.0.+-.0.2, 18.4.+-.0.2, 19.2.+-.0.2, 19.6.+-.0.2, 21.2.+-.0.2, 24.5.+-.0.2, 25.9.+-.0.2, and 28.0.+-.0.2.
4. A pharmaceutical composition of claim 1, wherein the compound of formula (IV) is further characterized by a differential scanning calorimetry having a broad peak between approximately 95.degree. C. and 130.degree. C. which corresponds to the loss of one water of hydration on thermogravimetric analysis.
5. A pharmaceutical composition of claim 1, wherein the compound of claim 5, which is further characterized by a weight loss of 3.48% by thermogravimetric analysis between 50.degree. C. and 175.degree. C.
6. A pharmaceutical composition of claim 1, wherein the pharmaceutically acceptable carrier includes hydroxypropyl cellulose, lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate.
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