US4501735A
Expired / Lapsed
US
⏱️ 0.0 years remaining
N6-(1- and 2-benzocycloalkyl) adenosines
Assignee: Warner Lambert Co LLC
•
Filing: 1983-12-05
•
Granted: 1985-02-26
•
Expires: 2003-12-05
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 06:26
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.
References Cited (Backward Citations)
US3590029A
Cited
US3819612A
Cited
NL7116563A
Cited
NL7210023A
Cited
US3901876A
Cited
US4090021A
Cited
DE2402804A1
Cited
US3922261A
Cited
JPS5046689A
Cited
DE2406587A1
Cited
EP0040325A1
Cited
GB2077726A
Cited
EP0062921A1
Cited
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 |