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EP0269574A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Novel adenosine derivatives and pharmaceutical compositions containing them as an active ingredient

Assignee: Nippon Zoki Pharmaceutical Co Ltd
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Filing: 1987-11-23
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Granted: —
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Expires: 2007-11-23
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Abstract

Abstract The present invention relates to novel adenosine derivatives having the formula (I): wherein each of R₁, R₂ and R₃, which may be the same or different, is hydrogen or a lower alkyl group; X is hydrogen, a lower alkyl group, an amino group or halogen; and Y is hydrogen or a lower alkyl group; and pharmaceutically acceptable salt thereof. These compounds are useful as antihypertensive agents, for example, for the treatments of hypertension and various diseases caused by hypertension, such as cerebrovascular diseases, cardiopathy or renal insufficiency.

Inventors

  • 👤 Toshio C/O Institute Of Bio-Active Science Yamada
  • 👤 Ken-Ichi Institute Of Bio-Active Science Kageyama

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-30 12:13
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/16; A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/007; A61K9/0073; A61K9/0075; A61K9/06; A61K9/20; A61K9/2004; A61K9/2013; A61K9/2018; A61K9/48; A61K9/4841; A61K9/4858; A61P; A61P9/00; A61P9/08; A61P9/12; A61K9/0031; A61K9/02; A61K9/70; A61K9/7023

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 54 words
An adenosine derivative having the formula (I): wherein each of R₁, R₂ and R₃, which may be the same or different, is hydrogen or a lower alkyl group; X is hydrogen, a lower alkyl group, an amino group or halogen; and Y is hydrogen or a lower alkyl group; or pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 54 words
An adenosine derivative having the formula (I): wherein each of R₁, R₂ and R₃, which may be the same or different, is hydrogen or a lower alkyl group; X is hydrogen, a lower alkyl group, an amino group or halogen; and Y is hydrogen or a lower alkyl group; or pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 19 words
An adenosine derivative or pharmaceutically acceptable salt thereof according to claim 1 wherein R₁ is a lower alkyl group.
Claim 4
Dependent Claim 19 words
An adenosine derivative or pharmaceutically acceptable salt thereof according to claim 2 wherein X is a lower alkyl group.
Claim 5
Dependent Claim 19 words
An adenosine derivative or pharmaceutically acceptable salt thereof according to claim 2 wherein Y is a lower alkyl group.
Claim 6
Dependent Claim 19 words
An adenosine derivative or pharmaceutically acceptable salt thereof according to claim 1 wherein R₃ is a lower alkyl group.
Claim 7
Dependent Claim 19 words
An adenosine derivative or pharmaceutically acceptable salt thereof according to claim 5 wherein X is a lower alkyl group.
Claim 8
Dependent Claim 19 words
An adenosine derivative or pharmaceutically acceptable salt thereof according to claim 5 wherein Y is a lower alkyl group.
Claim 9
Dependent Claim 16 words
An adenosine derivative or pharmaceutically acceptable salt thereof according to claim 1 wherein X is halogen.
Claim 10
Dependent Claim 68 words
An antihypertensive composition comprising as an active ingredient an effective amount of at least one adenosine derivative of the formula (I): wherein each of R₁, R₂ and R₃, which may be the same or different, is hydrogen or a lower alkyl group; X is hydrogen, a lower alkyl group, an amino group or halogen; and Y is hydrogen or a lower alkyl group; or pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim 68 words
An antihypertensive composition comprising as an active ingredient an effective amount of at least one adenosine derivative of the formula (I): wherein each of R₁, R₂ and R₃, which may be the same or different, is hydrogen or a lower alkyl group; X is hydrogen, a lower alkyl group, an amino group or halogen; and Y is hydrogen or a lower alkyl group; or pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim 17 words
An antihypertensive composition according to claim 9, which is formulated into a form suitable for oral administration.
Claim 13
Dependent Claim 131 words
A process for preparing an adenosine derivative of the formula (I): wherein each of R₁, R₂ and R₃, which may be the same or different, is hydrogen or a lower alkyl group; X is hydrogen, a lower alkyl group, an amino group or halogen; and Y is hydrogen or a lower alkyl group; which comprises O-alkylating a compound of the formula (II): wherein each of R₁ʹ, R₂ʹ and R₃ʹ, which may be the same or different, is hydrogen, a lower alkyl group or a protecting group; Xʹ is hydrogen, a lower alkyl group, an amino group or halogen; and Yʹ is an amino group, a lower alkylamino group or halogen; and then, if desired, carrying out an amination or an alkylamination of the 6-position and a removement of a protecting group.
Claim 14
Dependent Claim 131 words
A process for preparing an adenosine derivative of the formula (I): wherein each of R₁, R₂ and R₃, which may be the same or different, is hydrogen or a lower alkyl group; X is hydrogen, a lower alkyl group, an amino group or halogen; and Y is hydrogen or a lower alkyl group; which comprises O-alkylating a compound of the formula (II): wherein each of R₁ʹ, R₂ʹ and R₃ʹ, which may be the same or different, is hydrogen, a lower alkyl group or a protecting group; Xʹ is hydrogen, a lower alkyl group, an amino group or halogen; and Yʹ is an amino group, a lower alkylamino group or halogen; and then, if desired, carrying out an amination or an alkylamination of the 6-position and a removement of a protecting group.

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