公开(公告)号：US09255068B2

公开(公告)日：2016-02-09

申请号：US13471275

申请日：2012-05-14

Applicant: Catherine Coulter ,  Sean M. Johnston ,  Farzaneh Seyedi

Inventor： Catherine Coulter ,  Sean M. Johnston ,  Farzaneh Seyedi

IPC: A61K31/65 ,  C07C237/26 ,  C07C309/04 ,  C07C239/20

CPC classification number: C07C237/26 ,  C07B2200/07 ,  C07B2200/13 ,  C07C239/20 ,  C07C309/04 ,  C07C2103/46 ,  C07C2603/46

Abstract: A crystalline mono hydrochloride salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide is disclosed having improved stability. In addition, a crystalline mono mesylate salt and crystalline mono sulfate salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide are also disclosed having improved stability. A pharmaceutical composition containing the crystalline salts and methods of treating inflammatory skin disorders and bacterial infections comprising administering the crystalline salts are also disclosed.

Abstract translation: （4S，4aS，5aR，12aS）-4-二甲基氨基-3,10,12,12a-四羟基-7 - [（甲氧基（甲基）氨基） - 甲基] -1,11-二氧代 - 公开了具有改进的稳定性的1,4,4a，5,5a，6,11,12a-八氢 - 并四烯-2-羧酸酰胺。 另外，（4S，4aS，5aR，12aS）-4-二甲基氨基-3,10,12,12a-四羟基-7 - [（甲氧基（甲基）氨基） - 甲基的结晶单甲磺酸盐和结晶一硫酸盐 ] -1,11-二氧代-1,4,4a，5,5a，6,11,12a-八氢 - 并四苯-2-甲酸酰胺，其具有改进的稳定性。 还公开了含有结晶盐的药物组合物和治疗炎性皮肤病症和细菌感染的方法，包括给予结晶盐。

公开(公告)号：US20130012480A1

公开(公告)日：2013-01-10

申请号：US13471275

申请日：2012-05-14

Applicant: Catherine Coulter ,  Sean M. Johnston ,  Farzaneh Seyedi

Inventor： Catherine Coulter ,  Sean M. Johnston ,  Farzaneh Seyedi

IPC: C07C237/26 ,  A61P31/04 ,  A61P17/10 ,  A61P17/00 ,  A61K31/65 ,  C07C309/04

CPC classification number: C07C237/26 ,  C07B2200/07 ,  C07B2200/13 ,  C07C239/20 ,  C07C309/04 ,  C07C2103/46 ,  C07C2603/46

Abstract: A crystalline mono hydrochloride salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide is disclosed having improved stability. In addition, a crystalline mono mesylate salt and crystalline mono sulfate salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide are also disclosed having improved stability. A pharmaceutical composition containing the crystalline salts and methods of treating inflammatory skin disorders and bacterial infections comprising administering the crystalline salts are also disclosed.

Abstract translation: （4S，4aS，5aR，12aS）-4-二甲基氨基-3,10,12,12a-四羟基-7 - [（甲氧基（甲基）氨基） - 甲基] -1,11-二氧代 - 公开了具有改进的稳定性的1,4,4a，5,5a，6,11,12a-八氢 - 并四烯-2-羧酸酰胺。 另外，（4S，4aS，5aR，12aS）-4-二甲基氨基-3,10,12,12a-四羟基-7 - [（甲氧基（甲基）氨基） - 甲基的结晶单甲磺酸盐和结晶一硫酸盐 ] -1,11-二氧代-1,4,4a，5,5a，6,11,12a-八氢 - 并四苯-2-甲酸酰胺，其具有改进的稳定性。 还公开了含有结晶盐的药物组合物和治疗炎性皮肤病症和细菌感染的方法，包括给予结晶盐。