US4645774A
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Aminoethoxybenzylalcohol derivatives, process for their preparation and pharmaceutical compositions containing them
Assignee: Richter Gedeon Vegyeszeti Gyar Nyrt
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Filing: 1985-12-02
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Granted: 1987-02-24
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Expires: 2005-12-02
Abstract
Abstract The invention relates to new aminoethoxybenzylalcohol derivatives of the formula (I) <IMAGE> (I) wherein R1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms; R2 is halogen, trihalomethyl, or alkoxy having from one to 4 carbon atoms; R3 and R4 stand for methyl or together with the adjacent nitrogen form an up to 8-membered ring optionally containing oxygen, and acid addition or quaternary ammonium salts thereof. The compounds of formula (I) are pharmacologically active, thus show enzyme-inducing effect. The pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
Inventors
- 👤 Edit Toth
- 👤 Jozsef Torley
- 👤 Eva Palosi
- 👤 Szabolcs Szeberenyi
- 👤 Laszlo Szporny
- 👤 Sandor Gorog
- 👤 Istvan Hajdu
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 20:19
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/08; C07D295/084; C07D295/088; A; A61; A61P; A61P43/00
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
53 words
A compound of the Formula (I) ##STR12## wherein R 1 is hydrogen; R 2 is halo, trihalomethyl, or C 1 to C 4 alkoxy; and R 3 and R 4 together with the adjacent nitrogen atom form a piperidinyl, or pyrrolidinyl, group; or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
Claim 2
Dependent Claim
53 words
A compound of the Formula (I) ##STR12## wherein R 1 is hydrogen; R 2 is halo, trihalomethyl, or C 1 to C 4 alkoxy; and R 3 and R 4 together with the adjacent nitrogen atom form a piperidinyl, or pyrrolidinyl, group; or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
Claim 3
Dependent Claim
43 words
The compound of the Formula (I) defined in claim 1 selected from the group consisting of: (a) alpha-ethyl-alpha-(2-methoxy-phenyl)-4-[2-pyrrolidin-l-yl)-ethoxy]-benzyl alcohol; (b) alpha-ethyl-alpha-(4-fluorophenyl)-4-[2-piperidin-l-yl-ethoxy]-benzyl alcohol; (c) alpha-ethyl-alpha-(3-trifluoromethyl-phenyl)-4-[2-(piperidin-l-yl)-ethoxy]-benzyl alcohol; (d) alpha-ethyl-alpha-(3-chloro-phenyl)-4-[2-piperidin-l-yl)-ethoxy]-benzyl alcohol; and (e) alpha-ethyl-alpha-(2-methoxyphenyl)-4-[2-piperidin-l-yl)-ethoxy]-benzyl alcohol; or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
Claim 4
Dependent Claim
18 words
Alpha-ethyl-alpha-(3-trifluoromethyl-phenyl)-4-[2-(piperidin-l-yl)-ethoxy]-benzyl alcohol as defined in claim 1 or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
Claim 5
Dependent Claim
18 words
Alpha-ethyl-alpha-(2-methoxyphenyl)-4-[2-pyrrolidin-l-yl)-ethoxy]-benzyl alcohol as defined in claim 1 or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
Claim 6
Dependent Claim
18 words
Alpha-ethyl-alpha-(4-fluorophenyl)-4-[2-(piperidin-l-yl)-ethoxy]-benzyl alcohol as defined in claim 1 or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
Claim 7
Dependent Claim
48 words
A pharmaceutical composition for inducing the polysubstrate liver monooxygenase enzyme system containing a pharmaceutically effective amount of the compound of the Formula (I) as defined in claim 1 or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, together with a pharmaceutically acceptable carrier or auxiliary substance.
Claim 8
Dependent Claim
45 words
A method of inducing the polysubstrate liver monooxygenase enzyme system in a susceptible subject which comprises administering to said subject an effective amount of the compound of the Formula (I) defined in claim 1 or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
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) | 1990-02-23 | 1990-08-25 | 1991-02-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-02-23 | 1994-08-25 | 1995-02-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-02-23 | 1998-08-25 | 1999-02-24 | $7700.00 | Window Closed / Lapsed |