US4358455A
Expired / Lapsed
US
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Aralkylamindethanol heterocyclic compounds
Assignee: Merck Sharp & Dohme (I.A.) Corp
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Filing: 1980-12-23
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Granted: 1982-11-09
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Expires: 2000-12-23
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.
Inventors
- 👤 Joseph G. Atkinson
- 👤 John J. Baldwin
- 👤 David E. McClure
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 14:53
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: 28
Claim 1
Independent Claim
83 words
Compounds of the formula: ##STR48## tautomers, pharmaceutically acceptable salts and individual enantiomers thereof wherein R 1 is H or OH, ##STR49## 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.
Claim 2
Dependent Claim
83 words
Compounds of the formula: ##STR48## tautomers, pharmaceutically acceptable salts and individual enantiomers thereof wherein R 1 is H or OH, ##STR49## 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.
Claim 3
Dependent Claim
18 words
The compounds of claim 1 formula (a) where R 1 is H, (e) and (g) and its tautomers.
Claim 4
Dependent Claim
15 words
The compounds of claim 2 wherein R 6 is H, OH or OCH 3 .
Claim 5
Dependent Claim
11 words
The compounds of claim 3 wherein Y is CH 2 O.
Claim 6
Dependent Claim
16 words
The compounds of claim 3 wherein Y is CH 2 or (CH 2 ) 2 .
Claim 7
Dependent Claim
13 words
The compounds of claim 5 wherein Y is (CH 2 ) 2 .
Claim 8
Dependent Claim
24 words
The compounds of claim 6 wherein R 3 is ##STR50## wherein R 4 , and R 5 , are either CH 3 or H.
Claim 9
Dependent Claim
10 words
The compounds of claim 7 wherein R 4 is H.
Claim 10
Dependent Claim
10 words
The compounds of claim 7 wherein R 3 is ##STR51##
Claim 11
Dependent Claim
10 words
Compounds of claim 2 having formula (a), (e) or (g).
Claim 12
Dependent Claim
8 words
The compounds of claim 10 having formula (g).
Claim 13
Dependent Claim
12 words
The compounds of claim 10 having the formula ##STR52## and tautomers thereof.
Claim 14
Dependent Claim
12 words
The compound of claim 12 having the formula ##STR53## and its tautomers.
Claim 15
Dependent Claim
18 words
A compound of claim 1 having the formula: ##STR54## their maleate or HCl salts, individual enantiomers and tautomers.
Claim 16
Dependent Claim
8 words
Compounds (c), (d) and (e) of claim 14.
Claim 17
Dependent Claim
5 words
Compound (c) of claim 14.
Claim 18
Dependent Claim
5 words
Compound (d) of claim 14.
Claim 19
Dependent Claim
5 words
Compound (e) of claim 14.
Claim 20
Dependent Claim
28 words
Pharmaceutical compositions for (a) reducing intraocular pressure (b) treating hypertension or (c) effecting bronchodilation containing a therapeutically effective amount of a compound of claim 1 and a carrier.
Claim 21
Dependent Claim
31 words
A method for (a) reducing intraocular eye pressure (b) treating hypertension by or (c) effecting bronchodilation by administering an effective amount of a claim 1 compound in a suitable dosage form.
Claim 22
Dependent Claim
9 words
The S,S isomer of the claim 13 compound claim.
Claim 23
Dependent Claim
8 words
The S,R isomer of the claim 13 compound.
Claim 24
Dependent Claim
8 words
The R,S isomer of the claim 13 compound.
Claim 25
Dependent Claim
8 words
The R,R isomer of the claim 13 compound.
Claim 26
Dependent Claim
11 words
Compounds of claim 1 formula (a) where R 1 is OH.
Claim 27
Dependent Claim
24 words
Compounds of the formula Het-CHOH-CH.sub.2 -NH.sub.2 wherein Het has the formula ##STR55## tautomers and individual isomers thereof, where R 1 is H or OH.
Claim 28
Dependent Claim
24 words
Compounds of the formula Het-CHOH-CH.sub.2 -NH.sub.2 wherein Het has the formula ##STR55## tautomers and individual isomers thereof, where R 1 is H or OH.
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) | 1985-11-08 | 1986-05-10 | 1986-11-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-11-08 | 1990-05-10 | 1990-11-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-11-08 | 1994-05-10 | 1994-11-09 | $7700.00 | Window Closed / Lapsed |