Patent US4568679A successfully refreshed from Google Patents.
US4568679A
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Aralkylaminoethanol heterocyclic compounds
Assignee: Merck and Co Inc
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Filing: 1982-03-25
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Granted: 1986-02-04
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Expires: 2002-03-25
Abstract
Abstract Heterocyclic aminoethanols of the formula Het-CHOH-CH2-NH-aralkyl where het is a 6-10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals for reducing intraocular pressure, for use as alpha - and beta -and adrenergic blocking agents, as antihypertensive agents and for effecting bronchodilation.
Inventors
- 👤 Joseph G. Atkinson
- 👤 John J. Baldwin
- 👤 David E. McClure
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 21:26
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/63; C07D213/64; C07D213/61; C07D213/72; C07D213/73; C07D213/89; C07D263/00; C07D263/52; C07D263/54; C07D263/58; C07D265/00; C07D265/28; C07D265/34; C07D265/36; C07D405/00; C07D405/02; C07D405/04; C07D471/00; C07D471/02; C07D471/04
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
89 words
Compounds of the formula: ##STR53## tautomers, pharmaceutically acceptable salts and individual enantiomers thereof wherein ##STR54## wherein ##STR55## wherein R 4 and R 5 are independently selected from H and C 1 -C 3 alkyl, Y is CH 2 , (CH 2 ) 2 , (CH 2 ) 3 , (CH 2 ) 4 or --CH 2 --O-- R 6 is H, OH, OCH 3 , halogen, methylenedioxy or C 1 -C 3 alkyl and n is 1 or 2; provided that when R 6 is methylenedioxy n is 2.
Claim 2
Dependent Claim
89 words
Compounds of the formula: ##STR53## tautomers, pharmaceutically acceptable salts and individual enantiomers thereof wherein ##STR54## wherein ##STR55## wherein R 4 and R 5 are independently selected from H and C 1 -C 3 alkyl, Y is CH 2 , (CH 2 ) 2 , (CH 2 ) 3 , (CH 2 ) 4 or --CH 2 --O-- R 6 is H, OH, OCH 3 , halogen, methylenedioxy or C 1 -C 3 alkyl and n is 1 or 2; provided that when R 6 is methylenedioxy n is 2.
Claim 3
Dependent Claim
15 words
The compounds of claim 1 wherein R 6 is H, OH or OCH 3 .
Claim 4
Dependent Claim
11 words
The compounds of claim 2 wherein Y is CH 2 O.
Claim 5
Dependent Claim
16 words
The compounds of claim 2 wherein Y is CH 2 or (CH 2 ) 2 .
Claim 6
Dependent Claim
13 words
The compounds of claim 4 wherein Y is (CH 2 ) 2 .
Claim 7
Dependent Claim
24 words
The compounds of claim 5 wherein R 3 is ##STR56## wherein R 4 , and R 5 , are either CH 3 or H.
Claim 8
Dependent Claim
10 words
The compounds of claim 6 wherein R 4 is H.
Claim 9
Dependent Claim
10 words
The compounds of claim 6 wherein R 3 is ##STR57##
Claim 10
Dependent Claim
18 words
A compound of claim 1 having the formula: ##STR58## their maleate or HCl salts, individual enantiomers and tautomers.
Claim 11
Dependent Claim
22 words
A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of claim 1 and an inert non-toxic pharmaceutically acceptable carrier therefor.
Claim 12
Dependent Claim
36 words
A method for reducing intraocular eye pressure by administering a pharmaceutically effective intraocular eye pressure reducing amount of a composition of claim 10 in a suitable dosage form to a subject in need of the same.
Claim 13
Dependent Claim
19 words
Compounds of the formula Het-CHOH-CH 2 -NH 2 wherein Het has the formula ##STR59## tautomers and individual enantiomers thereof.
Claim 14
Dependent Claim
19 words
Compounds of the formula Het-CHOH-CH 2 -NH 2 wherein Het has the formula ##STR59## tautomers and individual enantiomers thereof.
Claim 15
Dependent Claim
31 words
A method for treating hypertension by administering a pharmaceutically effective anti-hypertensive amount of a composition of claim 10 in a suitable dosage form to a subject in need of such treatment.
Claim 16
Dependent Claim
31 words
A method for effecting bronchodilation by administering a pharmaceutically effective bronchodilating amount of a composition of claim 10 in a suitable dosage form to a subject in need of such treatment.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1989-02-03 | 1989-08-05 | 1990-02-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-02-03 | 1993-08-05 | 1994-02-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-02-03 | 1997-08-05 | 1998-02-04 | $7700.00 | Window Closed / Lapsed |