公开(公告)号：US20010053787A1

公开(公告)日：2001-12-20

申请号：US09835149

申请日：2001-04-16

Applicant: Sepracor Inc.

Inventor： Raymond L. Woosley ,  A. K. Gunnar Aberg

IPC: A61K031/445

CPC classification number: A61K31/454 ,  A61K31/445 ,  A61K2300/00

Abstract: Methods and compositions are disclosed utilizing metabolic derivatives of astemizole for the treatment of allergic disorders while avoiding the concomitant liability of adverse effects associated with the astemizole. The metabolic derivatives of astemizole are also useful for the treatment of retinopathy and other small vessel disorders associated with diabetes mellitus and such other conditions as may be related to the antihistamine activity of astemizole. For example, the metabolic derivatives of astemizole are useful for the treatment of asthma, motion sickness, and vertigo, without the concomitant liability of adverse effects associated with astemizole. Furthermore, the metabolic derivatives of astemizole, in combination with non-steroidal anti-inflammatory agents or other non-narcotic analgesics, or in combination with a decongestant, cough suppressant/antitussive or expectorant, are useful for the treatment of cough, cold, cold-like, and/or flu symptoms and the discomfort, headache, pain, fever, and general malaise associated therewith, without the concomitant liability of adverse effects associated with astemizole.

Abstract translation: 公开了利用阿司咪唑的代谢衍生物治疗过敏性疾病的方法和组合物，同时避免与阿司咪唑相关的副作用的伴随的责任。 阿司咪唑的代谢衍生物也可用于治疗与糖尿病相关的视网膜病变和其它小血管障碍以及可能与阿司咪唑的抗组织胺活性相关的其它病症。 例如，阿司咪唑的代谢衍生物可用于治疗哮喘，晕车和眩晕，而不伴随与阿司咪唑有关的不良反应。 此外，阿司咪唑的代谢衍生物与非甾体抗炎剂或其他非麻醉止痛剂组合，或与减充血剂，止咳剂/镇咳药或祛痰剂组合可用于治疗咳嗽，感冒，感冒 类似，和/或流感症状以及与之相关的不适，头痛，疼痛，发烧和全身不适，而不伴随与阿司咪唑有关的不良反应。

公开(公告)号：US20020137768A1

公开(公告)日：2002-09-26

申请号：US10108294

申请日：2002-03-28

Applicant: Sepracor, Inc.

Inventor： Raymond L. Woosley ,  A. K. Gunnar Aberg

IPC: A61K031/454

CPC classification number: A61K31/454 ,  A61K31/445 ,  A61K2300/00

Abstract: Methods and compositions are disclosed utilizing metabolic derivatives of astemizole for the treatment of allergic disorders while avoiding the concomitant liability of adverse effects associated with the astemizole. The metabolic derivatives of astemizole are also useful for the treatment of retinopathy and other small vessel disorders associated with diabetes mellitus and such other conditions as may be related to the antihistamine activity of astemizole. For example, the metabolic derivatives of astemizole are useful for the treatment of asthma, motion sickness, and vertigo, without the concomitant liability of adverse effects associated with astemizole. Furthermore, the metabolic derivatives of astemizole, in combination with non-steroidal anti-inflammatory agents or other non-narcotic analgesics, or in combination with a decongestant, cough suppressant/antitussive or expectorant, are useful for the treatment of cough, cold, cold-like, and/or flu symptoms and the discomfort, headache, pain, fever, and general malaise associated therewith, without the concomitant liability of adverse effects associated with astemizole.

Abstract translation: 公开了利用阿司咪唑的代谢衍生物治疗过敏性疾病的方法和组合物，同时避免与阿司咪唑相关的副作用的伴随的责任。 阿司咪唑的代谢衍生物也可用于治疗与糖尿病相关的视网膜病变和其它小血管障碍以及可能与阿司咪唑的抗组织胺活性相关的其它病症。 例如，阿司咪唑的代谢衍生物可用于治疗哮喘，晕车和眩晕，而不伴随与阿司咪唑有关的不良反应。 此外，阿司咪唑的代谢衍生物与非甾体抗炎剂或其他非麻醉止痛剂组合，或与减充血剂，止咳剂/镇咳药或祛痰剂组合可用于治疗咳嗽，感冒，感冒 类似，和/或流感症状以及与之相关的不适，头痛，疼痛，发烧和全身不适，而不伴随与阿司咪唑有关的不良反应。