公开(公告)号：US20020052382A1

公开(公告)日：2002-05-02

申请号：US09988935

申请日：2001-11-19

Applicant: Sepracor Inc.

Inventor： Timothy J. Barberich ,  Paul D. Rubin ,  William E. Yelle

IPC: A61K031/496

CPC classification number: A61K31/496 ,  C07D249/12

Abstract: The R-isomer of the hydroxy metabolite of nefazodone, R-hydroxynefazodone, is an effective treatment for depression which does not give rise to the adverse effects associated with nefazodone. R-hydroxynefazodone is also useful in the treatment of migraine headaches, panic disorders, post traumatic stress disorder and sleep disorders.

Abstract translation: 奈法唑酮的羟基代谢物的R-异构体R-羟基吗啡酮是抑制剂的有效治疗剂，其不会引起与奈法唑酮相关的不良反应。 R-羟基吗唑酮也可用于治疗偏头痛，恐慌症，创伤后应激障碍和睡眠障碍。

公开(公告)号：US20020019398A1

公开(公告)日：2002-02-14

申请号：US09877103

申请日：2001-06-11

Applicant: SEPRACOR, Inc.

Inventor： Thomas P. Jerussi ,  Chrisantha H. Senanayake ,  Paul D. Rubin ,  Yaping Hong ,  Roger A. Bakale ,  Tingjian Xiang ,  Fran A. McConville

IPC: A61K031/4985

CPC classification number: A61K31/4985 ,  A61K31/498 ,  C07B2200/07 ,  C07D487/04

Abstract: The invention is directed to compositions comprising, and methods of using, racemic N-desmethylzopiclone, optically pure (null)-N-desmethylzopiclone, and optically pure (null)-N-desmethylzopiclone in the treatment and prevention of diseases and conditions in mammals. The invention is further directed to novel methods of preparing N-desmethylzopiclone, optically pure (null)-N-desmethylzopiclone, and optically pure (null)-N-desmethylzopiclone.

公开(公告)号：US20010020031A1

公开(公告)日：2001-09-06

申请号：US09809165

申请日：2001-03-16

Applicant: Sepracor Inc.

Inventor： John R. McCullough ,  Thomas P. Jerussi

IPC: A61K031/445

CPC classification number: A61K31/495 ,  A61K31/4468 ,  A61K2300/00

Abstract: Compositons employing and methods utilizing the optically pure (null) isomer of norcisapride are disclosed. This compound has surprisingly been found to be a potent drug for the treatment of disorders of the central nervous system. The compound, (null) norcisapride, has also been found to be a potent antiemetic agent. Finally, the (null) isomer of norcisapride also avoids certain adverse side effects and certain adverse drug interactions.

Abstract translation: 公开了使用诺西西滨的旋光纯（+）异构体的复合物和方法。 令人惊讶地发现，该化合物是用于治疗中枢神经系统疾病的有效药物。 化合物（+）诺西沙必利还被发现是一种有效的止吐剂。 最后，诺西沙必利的（+）异构体也避免了某些不良副作用和某些不良药物相互作用。

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：US20040266792A1

公开(公告)日：2004-12-30

申请号：US10891236

申请日：2004-07-13

Applicant: Sepracor Inc.

Inventor： William E. Yelle

IPC: A61K031/519 ,  A61K031/675

CPC classification number: A61K31/505 ,  A61K31/51 ,  A61K31/675

Abstract: Methods and compositions utilizing compounds represented by Formula III, 1 or a pharmaceutically acceptable salt thereof, for the treatment and prevention of psychoses in humans are disclosed. Compounds of the present invention exhibit fewer side effects than risperidone, a lessened liability toward drug-drug interactions than risperidone and a more predictable dosing regimen than risperidone. Compounds of the invention are also useful for the treatment and prevention of emesis and withdrawal syndromes.

公开(公告)号：US20040235811A1

公开(公告)日：2004-11-25

申请号：US10681614

申请日：2003-10-08

Applicant: Sepracor Inc.

Inventor： Mark G. Currie ,  Steven Jones ,  Charles M. Zepp

IPC: A61K031/56 ,  C07J005/00

CPC classification number: C07J5/00 ,  C07J5/0076 ,  C07J5/0092 ,  C07J71/0031 ,  Y10S514/826 ,  Y10S514/886

Abstract: Compounds are disclosed of the formula 1 in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

Abstract translation: 公开了下式的化合物，其中R 3为C 8至C 24烃或米索前列醇的残基。 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：US20040077688A1

公开(公告)日：2004-04-22

申请号：US10685628

申请日：2003-10-14

Applicant: SEPRACOR INC.

Inventor： William E. Yelle

IPC: A61K031/4439

CPC classification number: A61K31/4439

Abstract: Methods and compositions are disclosed utilizing hydroxylansoprazole for the treatment of ulcers in humans. Hydroxylansoprazole exhibits a lessened liability toward drug-drug interactions than lansoprazole and a more predictable dosing regimen than lansoprazole. Hydroxylansoprazole is also useful for the treatment of gastroesophageal reflux and other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.

Abstract translation: 公开了利用羟基索非唑来治疗人类溃疡的方法和组合物。 羟考兰唑与兰索拉唑相比显着降低药物相互作用的责任，比兰索拉唑更可预测的给药方案。 羟基索非唑还可用于治疗胃食管反流和其他与胃分泌过多相关的病症，例如Zollinger-Ellison综合征。

公开(公告)号：US20040044039A1

公开(公告)日：2004-03-04

申请号：US10653072

申请日：2003-09-03

Applicant: Sepracor Inc.

Inventor： John R. McCullough ,  Thomas P. Jerussi

IPC: A61K031/445

CPC classification number: A61K31/495 ,  A61K31/4468 ,  A61K2300/00

Abstract: Compositons employing and methods utilizing the optically pure (null) isomer of norcisapride are disclosed. This compound has surprisingly been found to be a potent drug for the treatment of disorders of the central nervous system. The compound, (null) norcisapride, has also been found to be a potent antiemetic agent. Finally, the (null) isomer of norcisapride also avoids certain adverse side effects and certain adverse drug interactions.

Abstract translation: 公开了使用诺西西滨的旋光纯（+）异构体的复合物和方法。 令人惊讶地发现，该化合物是用于治疗中枢神经系统疾病的有效药物。 化合物（+）诺西沙必利还被发现是一种有效的止吐剂。 最后，诺西沙必利的（+）异构体也避免了某些不良副作用和某些不良药物相互作用。

公开(公告)号：US20030100581A1

公开(公告)日：2003-05-29

申请号：US09907556

申请日：2001-07-17

Applicant: SEPRACOR INC.

Inventor： Roger P. Bakale ,  Chris Senanayake ,  Yaping Hong ,  Kostas Saranteas ,  Martin P. Redmon ,  Stephen A. Wald

IPC: A61K031/454 ,  C07D43/02

CPC classification number: C07D401/12

Abstract: Polymorphic crystalline forms of the antihistaminic drug norastemizole are disclosed. Processes for the production of the preferred polymorph are also disclosed.

Abstract translation: 公开了抗组胺药物诺尔阿司咪唑的多晶型形式。 还公开了制备优选多晶型物的方法。

公开(公告)号：US20030022942A1

公开(公告)日：2003-01-30

申请号：US10202830

申请日：2002-07-26

Applicant: Sepracor, Inc.

Inventor： James W. Young

IPC: A61K031/137

CPC classification number: A61K31/137 ,  A61K31/135

Abstract: Methods and compositions are disclosed utilizing the optically pure (null)-isomer of bupropion, which is a potent drug for treating depression, Parkinson's disease, obesity, weight gain and other disorders.