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US4501735A Expired / Lapsed US ⏱️ 0.0 years remaining

N6-(1- and 2-benzocycloalkyl) adenosines

Assignee: Warner Lambert Co LLC
•
Filing: 1983-12-05
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Granted: 1985-02-26
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Expires: 2003-12-05
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Abstract

Abstract N 6 -(1 and 2-Benzocycloalkyl)adenosines and pharmaceutically acceptable acid addition salts having highly desirable central nervous system and cardiovascular properties, process for their manufacture, pharmaceutical compositions and methods for using said compounds and compositions are described.

Inventors

  • 👤 Bharat Trivedi
  • 👤 Harriet Hamilton
  • 👤 Walter Moos

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 11:36
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/16; A; A61; A61P; A61P25/00; A61P25/04; A61P25/18; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C07D; C07D405/00; C07D405/02; C07D405/04; C07H19/06

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 133 words
A compound of the formula ##STR6## wherein R 1 is of the formula ##STR7## in which n is 1; X is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl, phenyl or phenyl substituted by halogen, hydroxy, lower alkoxy, amino or trifluoromethyl; Y is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy, or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl; Z and Z' are independently hydrogen, halogen, nitro, trifluoromethyl, amino, lower alkyl, hydroxy or lower alkoxy; R 3 is hydrogen or lower alkyl; R' is hydrogen, acetyl or benzoyl; R 2 is hydrogen or halogen; its diastereomers or mixtures thereof, or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim 133 words
A compound of the formula ##STR6## wherein R 1 is of the formula ##STR7## in which n is 1; X is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl, phenyl or phenyl substituted by halogen, hydroxy, lower alkoxy, amino or trifluoromethyl; Y is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy, or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl; Z and Z' are independently hydrogen, halogen, nitro, trifluoromethyl, amino, lower alkyl, hydroxy or lower alkoxy; R 3 is hydrogen or lower alkyl; R' is hydrogen, acetyl or benzoyl; R 2 is hydrogen or halogen; its diastereomers or mixtures thereof, or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim 134 words
A compound of the formula ##STR8## wherein R 1 is of the formula ##STR9## in which n is 1; X is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl, phenyl or phenyl substituted by halogen, hydroxy, lower alkoxy, amino or trifluoromethyl; Y is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy, or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl; Z and Z' are independently hydrogen, halogen, nitro, trifluoromethyl, amino, lower alkyl, hydroxy or lower alkoxy; R 3 is hydrogen or lower alkyl; R' is hydrogen, acetyl or benzoyl, and R 2 is hydrogen or halogen; its diastereomers or mixtures thereof, or a pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim 134 words
A compound of the formula ##STR8## wherein R 1 is of the formula ##STR9## in which n is 1; X is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl, phenyl or phenyl substituted by halogen, hydroxy, lower alkoxy, amino or trifluoromethyl; Y is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy, or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl; Z and Z' are independently hydrogen, halogen, nitro, trifluoromethyl, amino, lower alkyl, hydroxy or lower alkoxy; R 3 is hydrogen or lower alkyl; R' is hydrogen, acetyl or benzoyl, and R 2 is hydrogen or halogen; its diastereomers or mixtures thereof, or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim 15 words
A compound as claimed in claim 2, wherein X, Y, Z, and Z' are hydrogen.
Claim 6
Dependent Claim 21 words
A compound as claimed in claim 3, wherein R 2 is hydrogen or chlorine; R 3 is hydrogen, and n 1.
Claim 7
Dependent Claim 11 words
A compound as claimed in claim 4, wherein R' is hydrogen.
Claim 8
Dependent Claim 12 words
A compound as claimed in claim 5, and being N 6 -(1-indanyl)adenosine.
Claim 9
Dependent Claim 12 words
A compound as claimed in claim 6, and being N 6 -[1-(S)-indanyl]adenosine.
Claim 10
Dependent Claim 12 words
A compound as claimed in claim 6, and being N 6 -[1-(R)-indanyl]adenosine.
Claim 11
Dependent Claim 133 words
A compound of the formula ##STR10## wherein R 1 is of the formula ##STR11## in which n is 1 X is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl, phenyl or phenyl substituted by halogen, hydroxy, lower alkoxy, amino or trifluoromethyl; Y is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy, or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl; Z and Z' are independently hydrogen, halogen, nitro, trifluoromethyl, amino, lower alkyl, hydroxy or lower alkoxy; R 3 is hydrogen or lower alkyl; R' is hydrogen, acetyl or benzoyl; R 2 is hydrogen or halogen; its diastereomers or mixtures thereof, or a pharmaceutically acceptable acid addition salt thereof.
Claim 12
Dependent Claim 133 words
A compound of the formula ##STR10## wherein R 1 is of the formula ##STR11## in which n is 1 X is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl, phenyl or phenyl substituted by halogen, hydroxy, lower alkoxy, amino or trifluoromethyl; Y is hydrogen, lower alkyl or lower alkyl terminally substituted by hydroxy, lower alkoxy, or carboxyl, OR where R is hydrogen, lower alkyl, lower alkanoyl or benzoyl; Z and Z' are independently hydrogen, halogen, nitro, trifluoromethyl, amino, lower alkyl, hydroxy or lower alkoxy; R 3 is hydrogen or lower alkyl; R' is hydrogen, acetyl or benzoyl; R 2 is hydrogen or halogen; its diastereomers or mixtures thereof, or a pharmaceutically acceptable acid addition salt thereof.
Claim 13
Dependent Claim 15 words
A compound as claimed in claim 9, wherein X, Y, Z, and Z' are hydrogen.
Claim 14
Dependent Claim 14 words
A compound as claimed in claim 10, wherein R 3 is hydrogen or methyl.
Claim 15
Dependent Claim 19 words
A compound as claimed in claim 10, wherein R 3 is hydrogen, and R 2 is hydrogen or chlorine.
Claim 16
Dependent Claim 11 words
A compound as claimed in claim 11, wherein R' is hydrogen.
Claim 17
Dependent Claim 12 words
A compound as claimed in claim 12, and being N 6 -(2-indanyl)adenosine.
Claim 18
Dependent Claim 21 words
A pharmaceutical composition comprising an antihypertensive effective amount of a compound according to claim 1 together with a pharmaceutically acceptable carrier.
Claim 19
Dependent Claim 21 words
A method for treating hypertension in mammals suffering therefrom comprising administering to such mammals a pharmaceutical composition according to claim 13.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-02-26 1988-08-27 1989-02-26 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-02-26 1992-08-27 1993-02-26 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-02-26 1996-08-27 1997-02-26 $7700.00 Window Closed / Lapsed

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