US4590199A
Expired / Lapsed
US
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Antihistaminic 2-(amino ethylamino) pyridines
Assignee: Wellcome Foundation Ltd
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Filing: 1984-07-27
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Granted: 1986-05-20
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Expires: 2004-07-27
Abstract
Abstract The present invention provides a compound of the formula (I): <IMAGE> (I) or a salt, ester or amide thereof; wherein R1 is -COOH, -CH=CH-COOH, -CH2COOH, or (CH2)2COOH. R2 is alkoxy (1-4 carbons), alkyl (1-4 carbons), hydrogen, or halogen. R3 and R4 may be the same or different and can be hydrogen, or lower alkyl(1-4 carbons) or NR3R4 is pyrrolidino. Also disclosed are methods for the preparation of the above compounds and pharmaceutical formulations containing them. The above compounds have antihistaminic activity.
Inventors
- 👤 Geoffrey G. Coker
- 👤 John W. A. Findlay
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 16:53
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/72; C07D213/74; A; A61; A61P; A61P37/00; A61P37/08; A61P43/00; C07D213/78; C07D213/79; C07D213/80; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/553; C07F9/576; C07F9/58
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
67 words
A compound of the formula (I): ##STR8## or a pharmaceutically acceptable salt thereof; wherein R 1 is --COOH, --CH═CH--COOH, --CH 2 COOH, or (CH 2 ) 2 COOH, R 2 is alkoxy (1-4 carbons), alkyl (1-4 carbons), hydrogen, or halogen, R 3 and R 4 may be the same or different and can be hydrogen, or lower alkyl (1-4 carbons) or NR 3 R 4 is pyrrolidino.
Claim 2
Dependent Claim
67 words
A compound of the formula (I): ##STR8## or a pharmaceutically acceptable salt thereof; wherein R 1 is --COOH, --CH═CH--COOH, --CH 2 COOH, or (CH 2 ) 2 COOH, R 2 is alkoxy (1-4 carbons), alkyl (1-4 carbons), hydrogen, or halogen, R 3 and R 4 may be the same or different and can be hydrogen, or lower alkyl (1-4 carbons) or NR 3 R 4 is pyrrolidino.
Claim 3
Dependent Claim
27 words
A compound of claim 1 which is of the formula (Ia): ##STR9## or a pharmaceutically acceptable salt thereof, wherein R 1 -R 4 are as hereinbefore defined.
Claim 4
Dependent Claim
44 words
A compound of claim 1 which is of the formula (Ib): ##STR10## or a pharmaceutically acceptable salt thereof; wherein R 2a is a C 1-4 alkyl or C 1-4 alkoxy group and R 1 , R 3 and R 4 are as hereinbefore defined.
Claim 5
Dependent Claim
44 words
A compound of claim 1 which is of the formula (Ic): ##STR11## or a pharmaceutically acceptable salt thereof, wherein R 1a is a group --CO 2 H or --CH═CHCO 2 H, and R 2a , R 3 and R 4 are as hereinbefore defined.
Claim 6
Dependent Claim
46 words
A compound of claim 1 which is of the formula (Id): ##STR12## or a pharmaceutically acceptable salt thereof, wherein R 3a and R 4a are the same or different and each is a C 1-4 alkyl group; R 1a and R 2a are as hereinbefore defined.
Claim 7
Dependent Claim
13 words
A compound according to claim 5 wherein R 2a is C 1-4 alkoxy.
Claim 8
Dependent Claim
15 words
A compound according to claim 5 wherein R 3 and R 4 are each methyl.
Claim 9
Dependent Claim
11 words
A compound according to claim 5 wherein R 2a is methoxy.
Claim 10
Dependent Claim
11 words
A compound according to claim 7 wherein R 2a is methoxy.
Claim 11
Dependent Claim
8 words
(E)-3-(6-N-dimethylaminoethyl)-4-methoxy-benzylamino)-2-pyridyl)acrylic acid or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
8 words
(E)-3-(6-N-dimethylaminoethyl)-4-methoxy-benzylamino)-2-pyridyl)acrylic acid or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
8 words
(6-(N-(2-dimethylaminoethyl)-4-methoxybenzylamino)nicotinic acid or a pharmaceutically acceptable salt thereof.
Claim 14
Dependent Claim
8 words
(6-(N-(2-dimethylaminoethyl)-4-methoxybenzylamino)nicotinic acid or a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim
10 words
A pharmaceutically acceptable salt of the compound of claim 1.
Claim 16
Dependent Claim
11 words
The salt of claim 10 which is a pharmaceutically acceptable salt.
Claim 17
Dependent Claim
11 words
The salt of claim 11 which is a pharmaceutically acceptable salt.
Claim 18
Dependent Claim
41 words
A method of obtaining an antihistiminic effect in a mammal in need thereof comprising the administration of an effective antihistiminic amount of the compound of claim 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 to said mammal.
References Cited (Backward Citations)
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) | 1989-05-19 | 1989-11-18 | 1990-05-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-05-19 | 1993-11-18 | 1994-05-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-05-19 | 1997-11-18 | 1998-05-20 | $7700.00 | Window Closed / Lapsed |