Patent US4650807A successfully refreshed from Google Patents.
US4650807A
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Antihistaminic compositions and methods containing pyridine derivatives
Assignee: SmithKline Beecham Corp
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Filing: 1985-07-08
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Granted: 1987-03-17
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Expires: 2005-07-08
Abstract
Abstract This disclosure describes a compound of Formula I <IMAGE> I (including its pharmaceutically acceptable salts and esters) which has potent antihistamine activity which is substantially free from sedative effects and which has little or no anticholinergic effects.
Inventors
- 👤 John W. A. Findlay
- 👤 Geoffrey G. Coker
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 13:17
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: 35
Claim 1
Independent Claim
44 words
A method of obtaining an antihistaminic effect in a mammal in need thereof comprising the oral, rectal, topical, nasal, ophthalmic or parenteral administration to said mammal of an effective antihistaminic amount of the compound of formula (I), ##STR10## or a pharmaceutically acceptable salt thereof.
Claim 2
Independent Claim
44 words
A method of obtaining an antihistaminic effect in a mammal in need thereof comprising the oral, rectal, topical, nasal, ophthalmic or parenteral administration to said mammal of an effective antihistaminic amount of the compound of formula (I), ##STR10## or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
11 words
The method of claim 1 wherein the mammal is a human.
Claim 4
Dependent Claim
17 words
The method of claim 2 wherein the compound of formula (I) is administered as the hydrochloride salt.
Claim 5
Dependent Claim
17 words
The method of claim 2 wherein the compound of formula (I) is administered as the sulfate salt.
Claim 6
Dependent Claim
17 words
The method of claim 2 wherein the compound of formula (I) is administered as the sodium salt.
Claim 7
Dependent Claim
17 words
The method of claim 2 wherein the compound of formula (I) is administered as the potassium salt.
Claim 8
Dependent Claim
16 words
The method of claim 2 in which the hydrochloride salt of the compound is orally administered.
Claim 9
Dependent Claim
18 words
The method of claim 1 in which the compound is administered orally and the mammal is a human.
Claim 10
Dependent Claim
12 words
The method of claim 8 in which the hydrochloride salt is administered.
Claim 11
Independent Claim
62 words
A method of providing an antihistaminic and decongestant effect in a mammal which comprises the oral, rectal, topical, nasal, ophthalmic or parenteral administration to said mammal of a composition comprising an effective antihistaminic amount of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid or a pharmaceutically acceptable salt thereof and an effective decongestant amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.
Claim 12
Independent Claim
62 words
A method of providing an antihistaminic and decongestant effect in a mammal which comprises the oral, rectal, topical, nasal, ophthalmic or parenteral administration to said mammal of a composition comprising an effective antihistaminic amount of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid or a pharmaceutically acceptable salt thereof and an effective decongestant amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.
Claim 13
Dependent Claim
23 words
The method of claim 10 in which a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1-E-enyl)-2-pyridyl)acrylic acid and a pharmaceutically acceptable salt of pseudoephedrine are administered.
Claim 14
Dependent Claim
12 words
The method of claim 1 in which the salts are administered orally.
Claim 15
Dependent Claim
28 words
A pharmaceutical composition comprising an effective antihistaminic amount of the compound of formula (I), ##STR11## or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier therefor.
Claim 16
Dependent Claim
28 words
A pharmaceutical composition comprising an effective antihistaminic amount of the compound of formula (I), ##STR11## or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier therefor.
Claim 17
Dependent Claim
11 words
The composition as claimed in claim 13 in unit dosage form.
Claim 18
Dependent Claim
19 words
The composition as claimed in claim 14, in the form of a tablet, syrup, suppository or sterile aqueous preparation.
Claim 19
Dependent Claim
32 words
A composition containing 0.25 mg to 20 mg of a compound of formula (I) ##STR12## or a pharmaceutically acceptable salt thereof calculated as the free compound and a pharmaceutically acceptable carrier therefor.
Claim 20
Dependent Claim
32 words
A composition containing 0.25 mg to 20 mg of a compound of formula (I) ##STR12## or a pharmaceutically acceptable salt thereof calculated as the free compound and a pharmaceutically acceptable carrier therefor.
Claim 21
Dependent Claim
9 words
The composition according to claim 16 in a capsule.
Claim 22
Dependent Claim
12 words
The composition according to claim 16 in the form of a tablet.
Claim 23
Dependent Claim
28 words
A composition containing 0.25 mg to 20 mg of a compound of formula (I) ##STR13## or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable liquid carrier therefor.
Claim 24
Dependent Claim
28 words
A composition containing 0.25 mg to 20 mg of a compound of formula (I) ##STR13## or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable liquid carrier therefor.
Claim 25
Dependent Claim
35 words
A composition comprising an effective antihistaminic amount of (E)-3-(6-3-pyrrolidino-1-(4-Tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid or a pharmaceutically acceptable salt thereof and an effective decongestant amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.
Claim 26
Dependent Claim
35 words
A composition comprising an effective antihistaminic amount of (E)-3-(6-3-pyrrolidino-1-(4-Tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid or a pharmaceutically acceptable salt thereof and an effective decongestant amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.
Claim 27
Dependent Claim
36 words
The composition of claim 20 comprising an effective antihistaminic amount of a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid and an effective decongestant amount of a pharmaceutically acceptable salt of psuedophedrine and a pharmaceutically acceptable carrier therefor.
Claim 28
Dependent Claim
27 words
A tablet or capsule suitable for oral administration containing an effective antihistaminic amount of the hydrochloride salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid together with a pharmaceutically acceptable carrier therefor.
Claim 29
Dependent Claim
27 words
A tablet or capsule suitable for oral administration containing an effective antihistaminic amount of the hydrochloride salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid together with a pharmaceutically acceptable carrier therefor.
Claim 30
Dependent Claim
24 words
A pharmaceutical composition containing 0.25 mg to 20 mg of a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid together with a pharmaceutically acceptable carrier therefor.
Claim 31
Dependent Claim
24 words
A pharmaceutical composition containing 0.25 mg to 20 mg of a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl)acrylic acid together with a pharmaceutically acceptable carrier therefor.
Claim 32
Dependent Claim
13 words
The composition of claim 23 in which the salt is the hydrochloride salt.
Claim 33
Dependent Claim
26 words
A pharmaceutical composition for oral administration containing an effective antihistaminic amount of a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridylacrylic acid and a pharmaceutically acceptable liquid carrier therefor.
Claim 34
Dependent Claim
26 words
A pharmaceutical composition for oral administration containing an effective antihistaminic amount of a pharmaceutically acceptable salt of (E)-3-(6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridylacrylic acid and a pharmaceutically acceptable liquid carrier therefor.
Claim 35
Dependent Claim
12 words
The composition of claim 25 in which the salt is the hydrochloride.
References Cited (Backward Citations)
DE1227464B
Cited
GB807757A
Cited
US3370058A
Cited
US4028352A
Cited
US3766174A
Cited
US3862173A
Cited
US3965181A
Cited
US4307245A
Cited
US4355036A
Cited
US4501893A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-03-16 | 1990-09-15 | 1991-03-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-03-16 | 1994-09-15 | 1995-03-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-03-16 | 1998-09-15 | 1999-03-17 | $7700.00 | Window Closed / Lapsed |