US4657918A
Expired / Lapsed
US
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3-[6-[3-pyrrolidino-1-(4-tolyl)prop-1e-enyl]-2-pyridyl]propionic acid and derivatives having anti-histaminic activity
Assignee: SmithKline Beecham Corp
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Filing: 1985-09-25
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Granted: 1987-04-14
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Expires: 2005-09-25
Abstract
Abstract This disclosure describes compounds of Formula I. ##STR1## (including their pharmaceutically acceptable salts and esters) which have potent antihistamine activity which are substantially free from sedative effects.
Inventors
- 👤 John W. A. Findlay
- 👤 Geoffrey G. Coker
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 19:59
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/78; C07D213/79; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/47; A61K31/485; A61P; A61P11/00; A61P37/00; A61P37/08; A61P43/00; C07D213/24; C07D213/54; C07D213/55; C07D213/56; C07D213/61; C07D295/00; C07D295/04; C07D295/14; C07D295/155; C07D405/00; C07D405/02; C07D405/04
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
95 words
A compound of formula (I) ##STR11## a straight or branched lower alkyl (1-4 carbon atoms) ester, or a pharmaceutically acceptable salt thereof; wherein R 1 is (CH 2 ) n , n is an integer 1-7, or R 2 and R 3 are the same or different and are hydrogen, C 1-4 alkyl or taken together with the nitrogen to which they are attached form a azacyclobutane, pyrrolidine or piperdine ring; R 4 is hydrogen, halogen, C 1-4 alkoxy or C 1-4 alkoxy or C 1-4 alkyl optionally substituted by one to three halogen atoms.
Claim 2
Dependent Claim
95 words
A compound of formula (I) ##STR11## a straight or branched lower alkyl (1-4 carbon atoms) ester, or a pharmaceutically acceptable salt thereof; wherein R 1 is (CH 2 ) n , n is an integer 1-7, or R 2 and R 3 are the same or different and are hydrogen, C 1-4 alkyl or taken together with the nitrogen to which they are attached form a azacyclobutane, pyrrolidine or piperdine ring; R 4 is hydrogen, halogen, C 1-4 alkoxy or C 1-4 alkoxy or C 1-4 alkyl optionally substituted by one to three halogen atoms.
Claim 3
Dependent Claim
2 words
3-{6-[3-Pyrrolidino-1-(4-tolyl)prop-1E-enyl]-2-pyridyl}propionic acid.
Claim 4
Dependent Claim
2 words
3-{6-[3-Pyrrolidino-1-(4-tolyl)prop-1E-enyl]-2-pyridyl}propionic acid.
Claim 5
Dependent Claim
7 words
A pharmaceutically acceptable salt of 3-{6-[3-Pyrrolidino-1-(4-tolyl)prop-1E-enyl]-2-propionic acid.
Claim 6
Dependent Claim
7 words
A pharmaceutically acceptable salt of 3-{6-[3-Pyrrolidino-1-(4-tolyl)prop-1E-enyl]-2-propionic acid.
Claim 7
Dependent Claim
6 words
The hydrochloride salt of claim 3.
Claim 8
Independent Claim
102 words
A method of providing an antihistiminic effect in a mammal in need thereof comprising administering to said mammal an effective antihistimatic amount of the compound of formula (I), ##STR12## or a pharmaceutically acceptable salt thereof; wherein R 1 is (CH 2 ) n , n is an integer 1-7; R 2 and R 3 are the same or different and are hydrogen, C 1-4 alkyl or taken together with the nitrogen to which they are attached form a azayclobutane, pyrrolidine, or piperdine ring; R 4 is hydrogen, C 1-4 alkoxy or C 1-4 alkyl optionally substituted by one to three halogen atoms.
Claim 9
Independent Claim
102 words
A method of providing an antihistiminic effect in a mammal in need thereof comprising administering to said mammal an effective antihistimatic amount of the compound of formula (I), ##STR12## or a pharmaceutically acceptable salt thereof; wherein R 1 is (CH 2 ) n , n is an integer 1-7; R 2 and R 3 are the same or different and are hydrogen, C 1-4 alkyl or taken together with the nitrogen to which they are attached form a azayclobutane, pyrrolidine, or piperdine ring; R 4 is hydrogen, C 1-4 alkoxy or C 1-4 alkyl optionally substituted by one to three halogen atoms.
Claim 10
Dependent Claim
29 words
A method of obtaining an antihistiminic effect in a mammal in need thereof comprising administering of an effective antihistiminic amount of the compound of claim 2 to said mammal.
Claim 11
Dependent Claim
26 words
A method of obtaining an antihistiminic effect in a mammal in need thereof comprising administering of an effective antihistiminic amount of claim 3 to said mammal.
References Cited (Backward Citations)
GB2114565A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1990-04-13 | 1990-10-13 | 1991-04-14 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-04-13 | 1994-10-13 | 1995-04-14 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-04-13 | 1998-10-13 | 1999-04-14 | $7700.00 | Window Closed / Lapsed |