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US5401754A Expired / Lapsed US ⏱️ 0.0 years remaining

Agent for treating thrombosis and phosphodiesterase inhibitor

Assignee: Otsuka Pharmaceutical Co Ltd
•
Filing: 1994-03-11
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Granted: 1995-03-28
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Expires: 2014-03-11
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Abstract

Abstract A pharmaceutical preparation comprising at least one compound selected from the group consisting of carbostyril derivatives having the general formula: <IMAGE> wherein R1 is hydrogen or a lower alkyl group optionally having hydroxy group as a substituent; R2 is a phenyl(lower alkyl) group optionally having 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring, pyridyl(lower alkyl) group, or a group of the formula -A-NR3R4 (wherein A is a lower alkylene group, R3 and R4 are the same or different and represent a lower alkyl group or phenyl group), and a salt thereof, which is useful as an agent for treating thrombosis, more particularly, as an agent for inhibiting platelet aggregation and as an agent for platelet aggregate dissociation.

Inventors

  • 👤 Takafumi Fujioka
  • 👤 Shuji Teramoto
  • 👤 Michiaki Tominaga
  • 👤 Yoichi Yabuuchi

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 04:27
CPC Classifications
C; C07; C07D; C07D215/00; C07D215/02; C07D215/16; C07D215/20; C07D215/22; C07D215/227; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61P; A61P11/00; A61P11/06; A61P17/00; A61P17/06; A61P25/00; A61P25/18; A61P3/00; A61P3/08; A61P3/10; A61P35/00; A61P43/00; A61P7/00; A61P7/02; A61P9/00; A61P9/10

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 120 words
A method for treating thrombosis comprising administering to a subject an anti-thrombotic effective amount of a carbostyril derivative of the formula: ##STR3## wherein R 1 represents hydrogen or a lower alkyl group optionally having a hydroxy group as a substituent; R 2 represents a phenyl(lower alkyl) group optionally having 1-3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring; a pyridyl(lower alkyl) group; and a group of the formula --A--NR 3 R 4 , wherein A represents a lower alkylene group, and wherein R 3 and R 4 , which are the same or different, represent a lower alkyl group or phenyl group; or a salt of said carbostyril derivative.
Claim 2
Independent Claim 120 words
A method for treating thrombosis comprising administering to a subject an anti-thrombotic effective amount of a carbostyril derivative of the formula: ##STR3## wherein R 1 represents hydrogen or a lower alkyl group optionally having a hydroxy group as a substituent; R 2 represents a phenyl(lower alkyl) group optionally having 1-3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring; a pyridyl(lower alkyl) group; and a group of the formula --A--NR 3 R 4 , wherein A represents a lower alkylene group, and wherein R 3 and R 4 , which are the same or different, represent a lower alkyl group or phenyl group; or a salt of said carbostyril derivative.
Claim 3
Dependent Claim 15 words
The method for treating thrombosis of claim 1, wherein said method involves inhibiting platelet aggregation.
Claim 4
Dependent Claim 14 words
The method for treating thrombosis of claim 1, wherein the carbostyril derivative is 6-[3-(3-methoxybenzyl)amino-2-hydroxypropoxy]carbostyril.
Claim 5
Dependent Claim 13 words
The method for treating thrombosis of claim 1, wherein the carbostyril derivatives 6-[3-(3,4-dimethoxybenzyl)amino-2-hydroxypropoxy]carbostyril.
Claim 6
Dependent Claim 14 words
The method for treating thrombosis of claim 2, wherein the carbostyril derivative is 6-[3-(3-methoxybenzyl)amino-2-hydroxypropoxy]carbostyril.
Claim 7
Dependent Claim 14 words
The method for treating thrombosis of claim 2, wherein the carbostyril derivative is 6-[3-(3,4-dimethoxybenzyl)amino-2-hydroxypropoxy]carbostyril.
Claim 8
Dependent Claim 38 words
The method for treating thrombosis of claim 1, wherein R 2 is a phenyl(lower alkyl) group optionally having 1-3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring.
Claim 9
Dependent Claim 15 words
The method for treating thrombosis of claim 7, wherein said method involved inhibiting platelet aggregation.
Claim 10
Independent Claim 122 words
A method for dissociating platelet aggregation comprising administering to subject a platelet aggregation dissociation effective amount of a .carbostyril derivative of the formula: ##STR4## wherein R 1 represents hydrogen or a lower alkyl group optionally having a hydroxy group as a substituent; R 2 represents a phenyl(lower alkyl) group optionally having 1-3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring; a pyridyl(lower alkyl) group; and a group of the formula --A--NR 3 R 4 , wherein A represents a lower alkylene group; and wherein R 3 and R 4 , which are the same or different, represent a lower alkyl group or phenyl group; or a salt of said carbostyril derivative.
Claim 11
Independent Claim 122 words
A method for dissociating platelet aggregation comprising administering to subject a platelet aggregation dissociation effective amount of a .carbostyril derivative of the formula: ##STR4## wherein R 1 represents hydrogen or a lower alkyl group optionally having a hydroxy group as a substituent; R 2 represents a phenyl(lower alkyl) group optionally having 1-3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring; a pyridyl(lower alkyl) group; and a group of the formula --A--NR 3 R 4 , wherein A represents a lower alkylene group; and wherein R 3 and R 4 , which are the same or different, represent a lower alkyl group or phenyl group; or a salt of said carbostyril derivative.
Claim 12
Dependent Claim 15 words
The method for dissociating platelet aggregation of claim 9, wherein the carbostyril derivative is 6-[3-(3-methoxybenzyl)amino-2-hydroxypropoxy]carbostyril
Claim 13
Dependent Claim 15 words
The method for dissociating platelet aggregation of claim 9, wherein the carbostyril derivative is 6-[3-(3,4-dimethoxybenzyl)amino-2-hydroxypropoxy]carbostyril.
Claim 14
Dependent Claim 39 words
The method for dissociating platelet aggregation of claim 9, wherein R 2 is a phenyl(lower alkyl) group optionally having 1-3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring.
Claim 15
Independent Claim 37 words
The method according to any one of claims 1, 2, or 9, wherein the effective amount of the carbostyril derivative is in the range of about 0.1 to 10 mg per kg of body weight per day.

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Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1998-03-27 1998-09-26 1999-03-28 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2002-03-27 2002-09-26 2003-03-28 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2006-03-27 2006-09-26 2007-03-28 $7700.00 Window Closed / Lapsed

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