公开(公告)号：US20030149304A1

公开(公告)日：2003-08-07

申请号：US10238204

申请日：2002-09-10

Applicant: Sepracor Inc.

Inventor： Gerald J. Tanoury ,  Chris H. Senanayake ,  Donald W. Kessler

IPC: A61K031/137 ,  C07C217/30

CPC classification number: A61K31/205 ,  C07B2200/13 ,  C07C231/24 ,  C07C233/25 ,  C07C233/43

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract translation: 公开了制备R，R-福莫特醇L-酒石酸盐的高纯度盐的方法。 该方法通过重结晶新型多晶型物提供最热力学稳定的多晶型物。

公开(公告)号：US20040176450A1

公开(公告)日：2004-09-09

申请号：US10806993

申请日：2004-03-23

Applicant: SEPRACOR INC.

Inventor： Gerald J. Tanoury ,  Chris H. Senanayake ,  Donald W. Kessler

IPC: A61K031/205 ,  C07C215/46

CPC classification number: A61K31/205 ,  C07B2200/13 ,  C07C231/24 ,  C07C233/25 ,  C07C233/43

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract translation: 公开了制备R，R-福莫特醇L-酒石酸盐的高纯度盐的方法。 该方法通过重结晶新型多晶型物提供最热力学稳定的多晶型物。

公开(公告)号：US20040266864A1

公开(公告)日：2004-12-30

申请号：US10842055

申请日：2004-05-07

Applicant: Sepracor Inc.

Inventor： Larry R. Bush ,  Mark G. Currie ,  Q. Kevin Fang ,  Chris H. Senanayake

IPC: C07D307/78 ,  A61K031/343

CPC classification number: C07D307/87 ,  C07D317/20

Abstract: This invention relates to novel compositions of matter containing enantiomerically enriched (null)-desmethylcitalopram, (null)-didesmethylcitalopram, or (null)-didesmethylcitalopram or mixtures thereof in optimal ratios. Contrary to prior teachings, the enantiomerically enriched citalopram metabolites disclosed herein possess potent serotonin reuptake inhibitory activity, with minimal inhibitory effects on the reuptake of other known monoamines, e.g., norepinephrine (NE) or dopamine (DA). The present invention also discloses methods for treating disorders, dysfunctions and diseases for which inhibition of serotonin reuptake is therapeutically beneficial. In particular, the present invention discloses a method for treating various forms of depression with pharmaceutical compositions described herein.

Abstract translation: 本发明涉及以最佳比例含有对映体富集（ - ） - 去甲基西酞普兰，（+） - 二甲基西酞普兰或（ - ） - 二甲基西酞普兰或其混合物的物质的新型组合物。 与现有技术相反，本文公开的对映异构体富集的西酞普兰代谢物具有有效的5-羟色胺再摄取抑制活性，对其他已知的单胺例如去甲肾上腺素（NE）或多巴胺（DA）的再摄取具有最小的抑制作用。 本发明还公开了治疗疾病，功能障碍和5-羟色胺再摄取抑制治疗有益的疾病的方法。 特别地，本发明公开了一种用本文所述的药物组合物治疗各种形式的抑郁症的方法。

公开(公告)号：US20030176407A1

公开(公告)日：2003-09-18

申请号：US10369828

申请日：2003-02-20

Applicant: SEPRACOR INC.

Inventor： Mark G. Currie ,  Steve Jones ,  Paul Grover ,  Chris H. Senanayake ,  Q. Kevin Fang

IPC: A61K031/573 ,  C07J005/00

CPC classification number: C07J71/0031 ,  A61K31/58 ,  C07J5/0076 ,  C07J5/0092 ,  C07J41/0033 ,  A61K2300/00

Abstract: Carbonates and carbamates of the formula 1 and related steroid carbonates and carbamates are disclosed. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

Abstract translation: 公开了具有式和相关类固醇碳酸酯和氨基甲酸酯的碳酸酯和氨基甲酸酯。 该化合物可用于治疗鼻炎和哮喘，特别是通过吸入治疗和治疗炎症，特别是通过局部或局部给药治疗炎症。

公开(公告)号：US20030130321A1

公开(公告)日：2003-07-10

申请号：US10325686

申请日：2002-12-20

Applicant: Sepracor, Inc.

Inventor： Chris H. Senanayake ,  Gerald J. Tanoury ,  Harold S. Wilkinson ,  Roger P. Bakale ,  Andrei A. Zlota

IPC: C07D213/46 ,  C07D211/82 ,  A01N043/40

CPC classification number: C07D211/90

Abstract: The invention relates to methods of resolving racemic amlodipine into enantiomerically enriched compositions by precipitation with tartaric acid in the presence of a non-aqueous solvent, such as N,Nnull-dimethylacetamide. The molar ratio of tartaric acid:amlodipine is preferably less than 0.25:1.0 or greater than 0.75:1.0.

Abstract translation: 本发明涉及通过在非水溶剂如N，N'-二甲基乙酰胺的存在下用酒石酸沉淀来将外消旋氨氯地平拆分成对映异构体富集的组合物的方法。 酒石酸：氨氯地平的摩尔比优选小于0.25:1.0或大于0.75:1.0。