公开(公告)号：JP2002308772A

公开(公告)日：2002-10-23

申请号：JP2002054838

申请日：2002-02-28

Applicant: SEPRACOR INC

Inventor： WOOSLEY RAYMOND L ,  ABERG A K GUNNAR

IPC: C07D401/12 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/454 ,  A61K45/00 ,  A61K45/06 ,  A61P3/08 ,  A61P3/10 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P31/12 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To provide an antihistaminic agent for treating an allergic disease without inducing significant cardiac arrhythmia in a human patient. SOLUTION: A method for using a composition containing norastemizole or its pharmaceutically permissible salt for manufacturing a pharmaceutical agent to be used in antihistaminic treatment without inducing significant cardiac arrhythmia.

公开(公告)号：JP2002255817A

公开(公告)日：2002-09-11

申请号：JP2002054842

申请日：2002-02-28

Applicant: SEPRACOR INC

Inventor： WOOSLEY RAYMOND L ,  ABERG A K GUNNAR

IPC: C07D401/12 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/454 ,  A61K45/00 ,  A61K45/06 ,  A61P3/08 ,  A61P3/10 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P31/12 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To obtain an antihistaminic agent for treating allergic diseases without inducing any significant cardiac arrhythmia in human patients. SOLUTION: This method is to use a composition comprising norastemizole or its pharmaceutically acceptable salt for producing medicines used in anti- histaminic treatment avoiding the significant cardiac arrhythmia.

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：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

公开(公告)号：HK1045806B

公开(公告)日：2008-03-14

申请号：HK02106014

申请日：2002-08-17

Applicant: SEPRACOR INC

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

IPC: A61K20060101 ,  A61K9/48 ,  C07D211/22 ,  A61K31/137 ,  A61K31/165 ,  A61K31/192 ,  A61K31/445 ,  A61K31/451 ,  A61K31/60 ,  A61K45/00 ,  A61K45/06 ,  A61P20060101 ,  A61P17/00 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00

公开(公告)号：DK1214937T3

公开(公告)日：2007-09-17

申请号：DK02006356

申请日：1993-08-03

Applicant: SEPRACOR INC

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

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

Abstract: Use of a composition comprising a compound of formula I: or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in providing symptomatic relief from dermal irritation, wherein the induction of cardiac arrhythmia is avoided, said treatment comprising administering a therapeutically effective amount of a compound of formula I to a human patient whose hepatic function is not impaired.