FreshPatents.com Logo
stats FreshPatents Stats
n/a views for this patent on FreshPatents.com
Updated: April 14 2014
newTOP 200 Companies filing patents this week


    Free Services  

  • MONITOR KEYWORDS
  • Enter keywords & we'll notify you when a new patent matches your request (weekly update).

  • ORGANIZER
  • Save & organize patents so you can view them later.

  • RSS rss
  • Create custom RSS feeds. Track keywords without receiving email.

  • ARCHIVE
  • View the last few months of your Keyword emails.

  • COMPANY DIRECTORY
  • Patents sorted by company.

AdPromo(14K)

Follow us on Twitter
twitter icon@FreshPatents

Water-soluble benzoazepine compound and its pharmaceutical composition

last patentdownload pdfdownload imgimage previewnext patent


20120277189 patent thumbnailZoom

Water-soluble benzoazepine compound and its pharmaceutical composition


wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections. or a salt thereof, The present invention provides a benzoazepine compound represented by following general formula (1):

Browse recent Otsuka Pharmaceutical Co., Ltd. patents - ,
Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
USPTO Applicaton #: #20120277189 - Class: 514 80 (USPTO) - 11/01/12 - Class 514 
Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) >Phosphorus Containing Other Than Solely As Part Of An Inorganic Ion In An Addition Salt Doai >Nitrogen Containing Hetero Ring >Polycylo Ring System Having A Ring Nitrogen In The System

view organizer monitor keywords


The Patent Description & Claims data below is from USPTO Patent Application 20120277189, Water-soluble benzoazepine compound and its pharmaceutical composition.

last patentpdficondownload pdfimage previewnext patent

TECHNICAL FIELD

The present invention relates to a novel benzoazepine compound and its pharmaceutical composition.

BACKGROUND OF ART

Tolvaptan represented by the following formula (2) is a known compound, and has been disclosed in, for example, U.S. Pat. No. 5,258,510 specification (Example 1199).

It is known that tolvaptan is useful as a vasopressin antagonist having aquaretic activity (Circulation, 107, pp. 2690-2696 (2003)). However, because of its low water solubility, tolvaptan has problems in that it is poorly absorbed by the intestinal canal, its dosage form and administration route are limited, etc. Although attempts have been made to solve these problems so that, for example, tolvaptan can be administered in the form of an amorphous solid preparation composition (Japanese Unexamined Patent Publication No. 1999-21241), in the application of tolvaptan, its dosage form and administration route still remain limited.

DISCLOSURE OF THE INVENTION

The present invention aims to provide a novel benzoazepine compound for improving the solubility of tolvaptan in water.

The present inventors conducted extensive research to solve the above problem, and as a result found that when tolvaptan is in the form of a phosphate ester compound, the water solubility thereof can be remarkably improved.

The present invention has been accomplished based on this finding.

Specifically, the present invention provides the following benzoazepine compounds, and compositions comprising the same, as described in Item 1 to 13 below.

Item 1. A benzoazepine compound represented by general formula (1)

or a salt thereof,

wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, a mercapto group optionally protected with a protecting group, or an amino group optionally protected with one or two protecting groups; R1 represents a hydrogen atom or a hydroxy-protecting group; and X represents an oxygen atom or a sulfur atom.

Item 2. A benzoazepine compound according to item 1 or a salt thereof, wherein X is an oxygen atom.

Item 3. A benzoazepine compound according to item 1 or 2, or a salt thereof, wherein R is a hydroxy group optionally protected with a protecting group.

Item 4. A benzoazepine compound according to item 1 or 2, or a salt thereof, wherein R is a hydrogen atom, a mercapto group optionally protected with a protecting group, or an amino group optionally protected with one or two protecting groups.

Item 5. A benzoazepine compound according to any one of items 1, 2, 3 and 4, or a salt thereof, wherein R1 is a hydroxy-protecting group.

Item 6. A benzoazepine compound according to any one of items 1, 2, 3 and 4, or a salt thereof, wherein R1 is a hydrogen atom.

Item 7. A benzoazepine compound according to item 1 or a salt thereof, wherein X is a sulfur atom.

Item 8. A benzoazepine compound according to item 1 or a salt thereof, wherein X is an oxygen atom, R is a hydroxy group, and R1 is a hydrogen atom.



Download full PDF for full patent description/claims.

Advertise on FreshPatents.com - Rates & Info


You can also Monitor Keywords and Search for tracking patents relating to this Water-soluble benzoazepine compound and its pharmaceutical composition patent application.
###
monitor keywords



Keyword Monitor How KEYWORD MONITOR works... a FREE service from FreshPatents
1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored.
3. Each week you receive an email with patent applications related to your keywords.  
Start now! - Receive info on patent apps like Water-soluble benzoazepine compound and its pharmaceutical composition or other areas of interest.
###


Previous Patent Application:
Water-soluble benzoazepine compound and its pharmaceutical composition
Next Patent Application:
Aminopyrimidines as syk inhibitors
Industry Class:
Drug, bio-affecting and body treating compositions
Thank you for viewing the Water-soluble benzoazepine compound and its pharmaceutical composition patent info.
- - - Apple patents, Boeing patents, Google patents, IBM patents, Jabil patents, Coca Cola patents, Motorola patents

Results in 1.16559 seconds


Other interesting Freshpatents.com categories:
Computers:  Graphics I/O Processors Dyn. Storage Static Storage Printers -g2--0.3495
     SHARE
  
           

FreshNews promo


stats Patent Info
Application #
US 20120277189 A1
Publish Date
11/01/2012
Document #
13461665
File Date
05/01/2012
USPTO Class
514 80
Other USPTO Classes
540542
International Class
/
Drawings
2



Follow us on Twitter
twitter icon@FreshPatents