公开(公告)号：JP2006036791A

公开(公告)日：2006-02-09

申请号：JP2005301318

申请日：2005-10-17

Applicant: Sepracor Inc ,  セプラコア インコーポレイテッド

Inventor： GRAY NANCY M

IPC: A61K31/495 ,  C07D241/04 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P37/08 ,  C07D295/08

CPC classification number: A61K31/495

Abstract: PROBLEM TO BE SOLVED: To provide a composition for treating allergic diseases.
SOLUTION: Optically pure (-) cetirizine is used for the treatment of seasonal and perennial allergic rhinitis in humans, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of cetirizine. The optically pure (-) isomer is also useful for the treatment of allergic asthma and chronic and physical urticaria. The (-) cetirizine is an eosinophilic chemotactic inhibitor, and is thereby useful for treating allergic asthma, seasonal allergic rhinitis, atopic dermatosis, some kinds of parasitic diseases, chronic obstructive pulmonary diseases, and other diseases related to eosinophilia such as specific gastrointestinal tract and urinary organ disorders.
COPYRIGHT: (C)2006,JPO&NCIPI

Abstract translation: 待解决的问题：提供治疗过敏性疾病的组合物。 解决方案：光学纯（ - ）西替利嗪用于治疗人类季节性和常年性过敏性鼻炎，同时避免与西替利嗪的外消旋混合物相关的副作用的伴随责任。 光学纯的（ - ）异构体也可用于治疗过敏性哮喘和慢性和身体性荨麻疹。 （ - ）西替利嗪是一种嗜酸粒细胞趋化性抑制剂，因此可用于治疗过敏性哮喘，季节性过敏性鼻炎，特应性皮肤病，某些寄生虫病，慢性阻塞性肺疾病和其他与嗜酸性粒细胞增多有关的疾病如特异性胃肠道和 泌尿器官功能障碍 版权所有（C）2006，JPO＆NCIPI

公开(公告)号：JP2000086514A

公开(公告)日：2000-03-28

申请号：JP29122399

申请日：1999-10-13

Applicant: SEPRACOR INC ,  UNIV GEORGETOWN

Inventor： YOUNG JAMES W ,  WOOSLEY RAYMOND L ,  GRAY NANCY M ,  CHEN YIWANG

IPC: C07D211/22 ,  A61K9/48 ,  A61K31/137 ,  A61K31/165 ,  A61K31/192 ,  A61K31/445 ,  A61K31/451 ,  A61K31/60 ,  A61K45/00 ,  A61K45/06 ,  A61P17/00 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To obtain the subject composition capable of avoiding cardiovascular system side effects caused by the administration of terfenadine by adding a terfenadine carboxylate and a non-steroidal anti-inflammatory medicine or non-narcotic analgesic medicine. SOLUTION: This medicinal composition contains (A) a terfenadine carboxylate 4-[1-hydroxy-4-(4-hydroxydiphenylmethyl-1-piperidinyl)butyl]-α,α- dimethylbenzene acetate, 1[p-(2-hydroxymethylprop-2-yl-phenyl]-4-[4-(α-hydroxy-α- phenylbenzyl)piperidin-1-yl]butanol, etc.}, of the formula (Z is COOH, COOCH3, etc.), which is a metabolic derivative of the terfenadine, and (B) a non-steroidal anti-inflammatory medicine or a non-narcotic analgesic medicine (for example, acetylsalicylate, ibuprofen). The component A and the component B are preferably contained in amounts of 20-200 mg and 25-600 mg, respectively.

公开(公告)号：JP2000086516A

公开(公告)日：2000-03-28

申请号：JP29123099

申请日：1999-10-13

Applicant: SEPRACOR INC ,  UNIV GEORGETOWN

Inventor： YOUNG JAMES W ,  WOOSLEY RAYMOND L ,  GRAY NANCY M ,  CHEN YIWANG

IPC: C07D211/22 ,  A61K9/48 ,  A61K31/137 ,  A61K31/165 ,  A61K31/192 ,  A61K31/445 ,  A61K31/451 ,  A61K31/60 ,  A61K45/00 ,  A61K45/06 ,  A61P17/00 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To obtain a medicine useful for antihistamine treatments and capable of avoiding to cause cardiac edema by using a composition containing a terfenadine carboxylate. SOLUTION: A medicinal composition containing a terfenadine carboxylate 4-[1-hydroxy-4-(4-hydroxydiphenylmethyl-1-piperidinyl)butyl]-α, α- dimethylbenzene acetic acid methyl ester, 4-[1-hydroxy-4-(4- hydroxydiphenylmethyl-1-piperidinyl)butyl]-α,-α-dimethylbenzene acetic acid, 1-[p-(2-hydroxymethylprop-2-yl)-phenyl]-4-[4-(α-hydroxy-α-phenylbenzyl)piperidin-1- yl]butanol, etc.}, of the formula (Z is COOH, COOCH3, CH2OH) which is a metabolic derivative of the terfenadine is used. The compound of the formula is preferably administered at a daily dose of 0.01-500 mg.

公开(公告)号：JP2000086515A

公开(公告)日：2000-03-28

申请号：JP29122899

申请日：1999-10-13

Applicant: SEPRACOR INC ,  UNIV GEORGETOWN

Inventor： YOUNG JAMES W ,  WOOSLEY RAYMOND L ,  GRAY NANCY M ,  CHEN YIWANG

IPC: C07D211/22 ,  A61K9/48 ,  A61K31/137 ,  A61K31/165 ,  A61K31/192 ,  A61K31/445 ,  A61K31/451 ,  A61K31/60 ,  A61K45/00 ,  A61K45/06 ,  A61P17/00 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To obtain the subject composition capable of avoiding cardiovascular system side effects such as QT extension and ventricular arhythmia caused by the administration of terfenadine by adding a specific optically pure terfenadine carboxylate. SOLUTION: This medicinal composition contains an optically pure R-(+)- terfenadine carboxylate R-(+)-4-[1-hydroxy-4-(4-hydroxydiphenylmethyl-1- piperidinyl)butyl]-α,α-dimethylbenzene acetic acid methyl ester, R-(+)-4-[1- hydroxy-4-(4-hydroxydiphenylmethyl-1-piperidinyl)butyl]-α, α-dimethylbenzene acetic acid, R-(+)-1-[p-(2-hydroxymethylprop-2-yl)-phenyl]-4-[4-(α-hydroxy-α- phenylvenzel)piperidin-1-yl]butanol, etc.}, which does not contain a S(-)- stereoisomer. The compound of the formula (Z is COOH, etc.), is preferably administered at a daily dose of 0.01-500 mg.

公开(公告)号：JP2000086513A

公开(公告)日：2000-03-28

申请号：JP29122099

申请日：1999-10-13

Applicant: SEPRACOR INC ,  UNIV GEORGETOWN

Inventor： YOUNG JAMES W ,  WOOSLEY RAYMOND L ,  GRAY NANCY M ,  CHEN YIWANG

IPC: C07D211/22 ,  A61K9/48 ,  A61K31/137 ,  A61K31/165 ,  A61K31/192 ,  A61K31/445 ,  A61K31/451 ,  A61K31/60 ,  A61K45/00 ,  A61K45/06 ,  A61P17/00 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To obtain the subject composition capable of avoiding cardiovascular system side effects such as QT extension and ventricular arrhythmia caused by the administration of terfenadine by adding a terfenadine carboxylate and a decongestant. SOLUTION: This medicinal composition contains (A) a terfenadine carboxylate 4-[1-hydroxy-4-(4-hydroxydiphenylmethyl-1-piperidinyl)butyl]-α,α- dimethylbenzene acetate, 1-[p-(2-hydroxymethylprop-2-yl)-phenyl]-4-[4-(α- hydroxy-α-phenylbenzyl)piperidin-1-yl]butanol, etc.}, of the formula (Z is COOH, COOCH3, CH2OH) which is a metabolic derivative of the terfenadine, and (B) a decongestant (for example, pseudoephedrine). The component A and the component B are preferably contained in amounts of 20-200 mg and 5-150 mg, respectively, in the composition.

公开(公告)号：JP2000086512A

公开(公告)日：2000-03-28

申请号：JP29121699

申请日：1999-10-13

Applicant: SEPRACOR INC ,  UNIV GEORGETOWN

Inventor： YOUNG JAMES W ,  WOOSLEY RAYMOND L ,  GRAY NANCY M ,  CHEN YIWANG

IPC: C07D211/22 ,  A61K9/48 ,  A61K31/137 ,  A61K31/165 ,  A61K31/192 ,  A61K31/445 ,  A61K31/451 ,  A61K31/60 ,  A61K45/00 ,  A61K45/06 ,  A61P17/00 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To obtain the subject composition capable of avoiding cardiovascular system side effects such as QT extension and ventricular arrhythmia caused by the administration of terfenadine by adding a terfenadine carboxylate. SOLUTION: This medicinal composition contains a terfenadine carboxylate 4-[1-hydroxy-4-(4-hydroxydiphenylmethyl-1-piperidinyl)butyl]-α,α,-dimethylbenzene acetic acid methyl ester, 4-[1-hydroxy-4-(4-hydroxydiphenylmethyl-1-piperidinyl) butyl]-α,α-dimethylbenzene acetic acid, 1-[p-(2-hydroxymethylprop-2-yl)- phenyl]-4-[4-(α-hydroxy-α-phenylbenzyl)piperidin-l-yl]butanol, etc.}, of the formula (Z is COOH, COOCH3, CH2OH) which is a metabolic derivative of the terfenadine. The compound of the formula is preferably administered at a daily dose of 0.01-500 mg.

公开(公告)号：EP0748220A4

公开(公告)日：1997-09-10

申请号：EP95908626

申请日：1995-01-20

Applicant: SEPRACOR INC

Inventor： GRAY NANCY M

IPC: A61K9/20 ,  A61K9/48 ,  A61K31/275 ,  A61K31/277 ,  A61P35/00 ,  C07C317/46

CPC classification number: A61K31/277 ,  A61K31/275 ,  Y10S514/859

公开(公告)号：EP0700292A4

公开(公告)日：1996-09-11

申请号：EP94914911

申请日：1994-04-25

Applicant: SEPRACOR INC

Inventor： GRAY NANCY M

IPC: C07D401/12 ,  A61K31/44 ,  A61K31/4427 ,  A61P1/04

CPC classification number: A61K31/44

公开(公告)号：EP0649307A4

公开(公告)日：1996-06-26

申请号：EP93916996

申请日：1993-07-06

Applicant: SEPRACOR INC

Inventor： GRAY NANCY M ,  YOUNG JAMES W

IPC: C07D211/62 ,  A61K31/445 ,  A61K31/4468 ,  A61P1/00 ,  A61P1/08 ,  A61P1/10 ,  A61P1/14

CPC classification number: A61K31/445 ,  A61K31/4468

公开(公告)号：EP0680324A4

公开(公告)日：1996-04-10

申请号：EP94907326

申请日：1994-01-27

Applicant: SEPRACOR INC ,  UNIV GEORGETOWN

Inventor： GRAY NANCY M ,  WOOSLEY RAYMOND L

IPC: C07D405/14 ,  A61K31/495 ,  A61P31/04 ,  A61K31/50

CPC classification number: A61K31/495