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首页> 外国专利> CRYSTALLINE FORM AND tosylate tetracycline compound CRYSTALLINE FORM AND SPECIFIED tosylate polymorph tosylate METHOD FOR PRODUCING tetracycline compound, polymorph obtained by this method, and a pharmaceutical composition based on the above crystalline forms and polymorphs

CRYSTALLINE FORM AND tosylate tetracycline compound CRYSTALLINE FORM AND SPECIFIED tosylate polymorph tosylate METHOD FOR PRODUCING tetracycline compound, polymorph obtained by this method, and a pharmaceutical composition based on the above crystalline forms and polymorphs

机译：结晶形式和甲苯磺酸四环素化合物结晶形式和特定甲苯磺酸酯多晶型物甲苯磺酸酯生产四环素化合物的方法，通过该方法获得的多晶型物以及基于上述结晶形式和多晶型物的药物组合物

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1. The crystalline form of the tetracycline compound encompassed by formula 1:! ! 2. The tosylate of the tetracycline compound encompassed by formula 1:! ! 3. The crystalline form of tosylate according to claim 2. ! 4. The polymorphic modification of the crystalline form according to claim 3, which has a powder X-ray diffraction structure substantially similar to that shown in FIG. ! 5. The modification according to claim 4, which has a powder X-ray diffraction structure including peaks at approximately 8.06, 13.02 and 18.83 ° 2θ using Cu Kα radiation. ! 6. The modification according to claim 4, which has a powder X-ray diffraction structure comprising peaks at approximately 8.06, 11.41, 13.02, 18.83, 20.54 and 24.53 ° 2θ using Cu Kα radiation. ! 7. The modification according to claim 4, which has a structure of x-ray diffraction on the powder, including peaks at approximately 5.60, 8.06, 8.57, 11.41, 13.02, 15.58, 18.83, 20 , 54 and 24.53 ° 2θ when using Cu Kα radiation. ! 8. The modification according to claim 4, which is obtained by crystallization of the tosylate of the tetracycline compound encompassed by formula 1:! ! from isopropanol. ! 9. A method for producing a stable crystalline tosylate of a tetracycline compound encompassed by formula 1:! ! comprising dissolving the free base of a compound encompassed by Formula 1 in a first solvent or combination of solvents to form a first solution, dissolving p-toluenesulfonic acid in a second solvent or combination of solvents to form a second solution, and combining said first and second solutions to form a third solution. ! 10. The method according to claim 9, in which the first solvent or combination rast
机译：1.四环素化合物的结晶形式被式1 ：！ ！ 2.式1 ：!所涵盖的四环素化合物的甲苯磺酸酯。 ！ 3.根据权利要求2的甲苯磺酸盐的结晶形式。 4.根据权利要求3所述的晶型的多晶型物变体，其具有基本上类似于图1所示的粉末X射线衍射结构。 ！ 5.根据权利要求4所述的变型，其具有粉末X射线衍射结构，所述粉末X射线衍射结构包括使用CuKα辐射在大约8.06、13.02和18.83°2θ处的峰。 ！ 6.根据权利要求4所述的变型，其具有粉末X射线衍射结构，所述粉末X射线衍射结构包括使用CuKα辐射在大约8.06、11.41、13.02、18.83、20.54和24.53°2θ处的峰。 ！ 7.根据权利要求4所述的变体，其在粉末上具有X射线衍射的结构，当使用Cu时，所述峰包括在约5.60、8.06、8.57、11.41、13.02、15.58、18.83、20、54和24.53°2θ处的峰。 Kα辐射。 ！ 8.根据权利要求4的修饰物，其通过使式1：所包含的四环素化合物的甲苯磺酸酯结晶而获得。 ！来自异丙醇。 ！ 9.一种制备式1的化合物的稳定的四环素化合物的结晶甲苯磺酸酯的方法。 ！包括将式1所涵盖的化合物的游离碱溶解在第一溶剂或溶剂的组合中以形成第一溶液，将对甲苯磺酸溶解在第二溶剂或溶剂的组合中以形成第二溶液，以及将所述第一和第二解决方案，形成第三解决方案。 ！ 10.根据权利要求9所述的方法，其中所述第一溶剂或混合物

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