公开(公告)号：WO1997045113A1

公开(公告)日：1997-12-04

申请号：PCT/US1997007568

申请日：1997-05-05

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  JOCHLE, Wolfgang

IPC: A61K31/19

CPC classification number: A61K31/192 ,  A23K20/111 ,  A61K45/06

Abstract: Compositions and methods for regulating the reproductive cycle of domesticated animals using nonsteroidal anti-inflammatory drugs (NSAIDs). Further, the present invention relates to compositions and methods for controlling and managing the breeding of domesticated animals, especially pigs, by synchronizing their reproductive cycles by administering an effective amount of an NSAID compound, preferably ketoprofen. Optionally, one or several additional active ingredients such as a hormone or steroid may be administered in conjunction with the NSAID compound in order to synchronize the reproductive cycle, especially estrus and/or ovulations.

Abstract translation: 使用非甾体抗炎药（NSAIDs）调节驯养动物繁殖周期的组合物和方法。 此外，本发明涉及通过施用有效量的NSAID化合物，优选酮洛芬来同步其生殖周期来控制和管理驯养动物，特别是猪的育种的组合物和方法。 任选地，一种或多种另外的活性成分例如激素或类固醇可以与NSAID化合物一起施用，以使生殖周期，特别是发情和/或排卵同步。

公开(公告)号：WO1996013226A1

公开(公告)日：1996-05-09

申请号：PCT/US1995013989

申请日：1995-10-30

Applicant: SEPRACOR INC. ,  ABERG, A., K., Gunnar

Inventor： SEPRACOR INC.

IPC: A61F02/00

CPC classification number: A61K45/06 ,  A61K31/167 ,  A61K31/60 ,  A61K38/1841 ,  A61K38/1866 ,  A61K38/30 ,  A61K2300/00

Abstract: A method for the treatment of periodontitis and a pharmaceutical composition for use in the method. According to a preferred embodiment, the method comprises administering to a mammal afflicted with periodontitis a therapeutically effective amount of a pharmaceutical composition comprising a polypeptide growth factor and an NSAID to regenerate dental tissue in the mammal afflicted with periodontitis and, thereafter, administering to the mammal a therapeutically effective amount of an NSAID to prevent resorption of the newly regenerated dental tissue.

Abstract translation: 治疗牙周炎的方法和用于该方法的药物组合物。 根据优选的实施方案，所述方法包括向患有牙周炎的哺乳动物施用治疗有效量的包含多肽生长因子和NSAID的药物组合物，以再生患有牙周炎的哺乳动物中的牙齿组织，然后施用于哺乳动物 治疗有效量的NSAID以防止新再生的牙科组织的再吸收。

公开(公告)号：WO1994001112A1

公开(公告)日：1994-01-20

申请号：PCT/US1993006379

申请日：1993-07-06

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  GRAY, Nancy, M. ,  YOUNG, James, W.

IPC: A61K31/445

CPC classification number: A61K31/445 ,  A61K31/4468

Abstract: Methods are disclosed utilizing the optically pure (-) isomer of cisapride. This compound is a potent drug for the treatment of gastro-esophageal reflux disease while avoiding the concomitant liability of adverse effects associated with the racemic mixture of cisapride. This compound is also useful in treating or preventing emesis while avoiding the adverse effects associated with racemic cisapride. The optically pure (-) isomer of cisapride is also useful for the treatment of dyspepsia and such other conditions as may be related to the activity of (-) cisapride as a prokinetic agent such as gastroparesis, constipation, post-operative ileus, and intestinal pseudo-obstruction without the concomitant liability of adverse effects associated with the racemic mixture of cisapride. The (-) isomer of cisapride has been found to exhibit higher bioavailability over the racemic cisapride.

Abstract translation: 公开利用西沙必利的光学纯（ - ）异构体的方法。 该化合物是用于治疗胃食管反流疾病的有效药物，同时避免与西沙必利的外消旋混合物相关的副作用的伴随的责任。 该化合物也可用于治疗或预防呕吐，同时避免与外消旋西沙必利有关的不良反应。 西沙必利的旋光纯（ - ）异构体也可用于治疗消化不良和其他可能与（ - ）西沙必利作为促动力药物如胃轻瘫，便秘，手术后肠梗阻和肠道活动相关的其他病症 假性梗阻与西沙必利的外消旋混合物相关的副作用没有伴随的责任。 已经发现西沙必利的（ - ）异构体比外消旋西沙必利具有更高的生物利用度。

公开(公告)号：WO1994000047A1

公开(公告)日：1994-01-06

申请号：PCT/US1993005967

申请日：1993-06-22

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  YOUNG, James, W.

IPC: A51K31/145

CPC classification number: A61K31/135

Abstract: Methods and compositions are disclosed utilizing the optically pure (+) isomer of sibutramine, which is a potent drug for treatment of depression, Parkinson's disease, cerebral function disorders, obesity, dementia and related disorders, as well as other conditions related to the activity of the compound as an inhibitor of the neuronal reuptake of monoamines. Further, methods and compositions are disclosed utilizing optically pure (+) sibutramine in order to avoid the adverse effects associated with the administration of racemic sibutramine.

Abstract translation: 公开了使用西布曲明的光学纯（+）异构体的方法和组合物，西布曲明是用于治疗抑郁症，帕金森病，脑功能障碍，肥胖，痴呆和相关疾病的有效药物，以及与 该化合物作为单胺神经元再摄取的抑制剂。 此外，利用光学纯（+）西布曲明公开了方法和组合物，以避免与外消旋西布曲明的给药相关的不利影响。

公开(公告)号：WO1993020809A1

公开(公告)日：1993-10-28

申请号：PCT/US1993003041

申请日：1993-03-31

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  BARBERICH, Timothy, J. ,  YOUNG, James, W.

IPC: A61K31/19

CPC classification number: A61K31/405 ,  A61K31/19 ,  A61K31/38 ,  A61K31/40 ,  A61K31/557 ,  A61K2300/00

Abstract: The adverse side effects associated with the administration of arylalkanoic acid derivative drugs such as the arylpropionic acid derivatives ibuprofen, ketoprofen, or flurbiprofen are reduced by administering the S enantiomer of these drugs. In particular, the adverse side effects of gastrointestinal toxicity or irritation and of kidney toxicity are reduced. The S enantiomer drug compositions are also disclosed.

Abstract translation: 通过施用这些药物的S对映异构体，减少与芳基链烷酸衍生物药物如芳基丙酸衍生物布洛芬，酮洛芬或氟比洛芬的给药有关的副作用。 特别是，胃肠道毒性或刺激和肾脏毒性的不良副作用降低。 还公开了S对映异构体药物组合物。

公开(公告)号：WO1996040133A1

公开(公告)日：1996-12-19

申请号：PCT/US1996007159

申请日：1996-05-17

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  MCCULLOUGH, John, R. ,  ABERG, A., K., Gunnar

IPC: A61K31/445

CPC classification number: A61K31/496 ,  A61K31/44 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/495 ,  A61K45/06 ,  A61K2300/00

Abstract: Methods are disclosed utilizing the optically pure (-) isomer of norcisapride. This compound is a potent drug for the treatment of gastro-esophageal reflux disease, emesis, dispepsia and other conditions while substantially reducing the concomitant liability of adverse effects associated with cisapride. The (-) isomer of norcisapride also avoids the adverse drug interactions associated with racemic cisapride and other therapeutic agents.

Abstract translation: 公开利用诺西西滨的旋光纯（ - ）异构体的方法。 该化合物是治疗胃食管反流病，呕吐，消化不良和其他病症的有效药物，同时显着减少与西沙必利相关的副作用的伴随责任。 诺西沙必利的（ - ）异构体也避免与外消旋西沙必利和其他治疗剂相关的不良药物相互作用。

公开(公告)号：WO1995028152A1

公开(公告)日：1995-10-26

申请号：PCT/US1995004508

申请日：1995-04-10

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  YOUNG, James, W. ,  BARBERICH, Timothy, J.

IPC: A61K31/135

CPC classification number: A61K31/135

Abstract: Methods and compositions are disclosed utilizing the pure S(+) isomer of fluoxetine which is a potent antidepressant and appetite suppressant substantially free of unwanted, adverse toxic or psychological effects. In addition, methods and compositions are disclosed utilizing the pure S(+) isomer of fluoxetine which is useful in treating migraine headaches, pain, in particular chronic pain, obsessive-compulsive disorders, sexual dysfunction and memory disorders. Further, methods and compositions for treating a condition alleviated or improved by inhibition of serotonin uptake in serotonergic neurons and platelets in a human using optically pure S(+) fluoxetine are disclosed.

Abstract translation: 公开了使用氟西汀的纯S（+）异构体的方法和组合物，其是有效的抗抑郁药和食欲抑制剂，其基本上不含有害的，不利的毒性或心理作用。 此外，公开了使用氟西汀的纯S（+）异构体的方法和组合物，其可用于治疗偏头痛，疼痛，特别是慢性疼痛，强迫症，性功能障碍和记忆障碍。 此外，公开了通过使用光学纯的S（+）氟西汀在人体中抑制5-羟色胺能神经元和血小板中5-羟色胺摄取而缓解或改善的病症的方法和组合物。

公开(公告)号：WO1994000114A1

公开(公告)日：1994-01-06

申请号：PCT/US1993005966

申请日：1993-06-22

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  YOUNG, James, W.

IPC: A61K31/135

CPC classification number: A61K31/135

Abstract: Methods and compositions are disclosed utilizing the optically pure (-) isomer of sibutramine, which is a potent drug for treatment of depression, Parkinson's disease, cerebral function disorders, obesity, dementia and related disorders, as well as other conditions related to the activity of the compound as an inhibitor of the neuronal reuptake of monoamines. Further, methods and compositions are disclosed utilizing optically pure (-) sibutramine in order to avoid the adverse effects associated with the administration of racemic sibutramine.

Abstract translation: 公开了使用西布曲明的光学纯（ - ）异构体的方法和组合物，其是用于治疗抑郁症，帕金森病，脑功能障碍，肥胖症，痴呆和相关病症的有效药物，以及与 该化合物作为单胺神经元再摄取的抑制剂。 此外，利用旋光纯（ - ）西布曲明来公开方法和组合物，以避免与施用外消旋西布曲明有关的不利影响。

公开(公告)号：WO1996008580A1

公开(公告)日：1996-03-21

申请号：PCT/US1995011860

申请日：1995-09-18

Applicant: SEPRACOR INC. ,  MELNICK, Laurence, M. ,  HEEFNER, Donald, L.

Inventor： SEPRACOR INC.

IPC: C12Q01/37

CPC classification number: C12N9/506 ,  C12N15/1048 ,  C12Q1/37 ,  C12Q1/6811 ,  G01N2333/16 ,  G01N2333/8142 ,  Y10S435/974 ,  Y10S435/975

Abstract: An in vitro method for identifying distinct, first generation, drug-resistant, biologically active, HIV protease mutants that may emerge in vivo in response to a drug targeted thereagainst comprising: (a) preparing, in the presence of the drug, a library of all first-generation mutants of the protease differing therefrom by one to three amino acid substitutions, each of the protease mutants being generated as part of a polyprotein with reverse transcriptase; (b) isolating drug-resistant, biologically-active mutant proteases by assaying for activity of the reverse transcriptase; and (c) identifying the distinct amino acid changes leading to the drug-resistance of the active, mutant proteases so isolated. An in vitro method for evaluating the efficacy of a drug against a biologically active mutant or wild-type form of HIV protease comprising combining the drug and a mutant polyprotein, comprising an inactive HIV protease, HIV reverse transcriptase, and one or more protease cleavage sites, adding biologically-active mutant or wild-type protease, assaying for release of active reverse transcriptase, whereby reverse transcriptase activity indicates that the drug is not efficacious against the mutant or wild-type form of HIV protease tested.

Abstract translation: 一种体外方法，其用于鉴定可能在其靶向靶向药物的体内可能出现的不同的第一代，耐药性，生物活性的HIV蛋白酶突变体，其包括：（a）在所述药物存在下，制备 所有蛋白酶突变体的所有第一代突变体通过一至三个氨基酸取代基与之不同，每个蛋白酶突变体作为具有逆转录酶的多聚蛋白的一部分产生; （b）通过测定逆转录酶的活性来分离耐药性，生物活性的突变型蛋白酶; 和（c）鉴定导致如此分离的活性突变蛋白酶的耐药性的不同氨基酸变化。 一种用于评估药物对生物活性突变体或野生型形式的HIV蛋白酶的功效的体外方法，包括将药物和突变体多蛋白（包括无活性的HIV蛋白酶，HIV逆转录酶和一个或多个蛋白酶切割位点） ，添加生物活性突变体或野生型蛋白酶，测定活性逆转录酶的释放，由此逆转录酶活性表明该药物对于所测试的HIV蛋白的突变体或野生型形式是无效的。

公开(公告)号：WO1994013283A1

公开(公告)日：1994-06-23

申请号：PCT/US1993012299

申请日：1993-12-17

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  BARBERICH, Timothy, J. ,  MATSON, Stephen, L.

IPC: A61K31/40

CPC classification number: A61K31/40

Abstract: A pharmaceutical composition comprising R-ketorolac, substantially free of the S stereoisomer, for use in an analgesic or antipyretic treatment which does not induce significant adverse side effects associated with the administration of racemic ketorolac, comprising administering a therapeutically effective amount of R-ketorolac to a human patient.

Abstract translation: 一种药物组合物，其包含基本上不含S立体异构体的R-酮咯酸，用于镇痛或解热治疗，其不引起与外消旋酮咯酸相关的显着不良副作用，包括给予治疗有效量的R-酮咯酸 一个人的病人。