US4892947A
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3(2H)Pyridazinone, process for its preparation and anti-allergic agent containing it
Assignee: Nissan Chemical Corp
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Filing: 1986-04-22
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Granted: 1990-01-09
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Expires: 2006-04-22
Abstract
Abstract A 3(2H)pyridazinone of the formula: ##STR1## wherein R 1 is hydrogen, methyl, C 3 -C 6 alkenyl, C 5 or C 6 cycloalkyl, benzyl, phenyl, --(CH 2 ) m CO 2 R 3 (wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4), --(CH 2 ) n A (wherein A is --OH or --N(R 4 ) 2 wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6) or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen, C 1 -C 5 alkyl, C 2 -C 8 alkenyl, halogen, --OR 5 (wherein R 5 is hydrogen, C 1 -C 8 alkyl or ##STR2## wherein q is an integer of from 1 to 4), --CO 2 R 6 (wherein R 6 is hydrogen or C 1 -C 5 alkyl), --N(R 7 ) 2 (wherein R 7 is C 1 -C 4 alkyl) or --SR 8 (wherein R 8 is C 1 -C 4 alkyl); and Y 3 is C 1 -C 5 alkyl, C 2 -C 8 alkenyl, halogen, --OR 5 (wherein R 5 is as defined above), --CO 2 R 6 (wherein R 6 is as defined above), --N(R 7 ) 2 (wherein R 7 is as defined above) or --SR 8 (wherein R 8 is as defined above), or a pharmaceutically acceptable salt thereof.
Inventors
- 👤 Motoo Mutsukado
- 👤 Keizo Tanikawa
- 👤 Ken-ichi Shikada
- 👤 Ryozo Sakoda
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 13:14
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/50; C; C07; C07D; C07D237/00; C07D237/02; C07D237/06; C07D237/10; C07D237/22
Claims Analysis
Total Claims: 36
Claim 1
Independent Claim
211 words
A 3(2H)pyridazinone of the formula: ##STR28## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is halogen; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
211 words
A 3(2H)pyridazinone of the formula: ##STR28## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is halogen; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
220 words
A 3(2H)pyridazinone of the formula: ##STR29## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is --OR 5 , wherein R 5 is as defined above; or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
220 words
A 3(2H)pyridazinone of the formula: ##STR29## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is --OR 5 , wherein R 5 is as defined above; or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
221 words
A 3(2H)pyridazinone of the formula: ##STR30## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(RHD 4) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is --CO 2 R 6 , wherein R 6 is as defined above; or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
221 words
A 3(2H)pyridazinone of the formula: ##STR30## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(RHD 4) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is --CO 2 R 6 , wherein R 6 is as defined above; or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
69 words
The pyridazinone according to claim 2, wherein R 1 is hydrogen; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen, --OR 5 (wherein R 5 is hydrogen or C 1 -C 7 alkyl, benzyl or phenethyl); and Y 3 is --OR 5 (wherein R 5 is hydrogen or C 1 -C 7 alkyl, benzyl or phenethyl).
Claim 8
Dependent Claim
222 words
A 3(2H)pyridazinone of the formula: ##STR31## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is --N(R 7 ) 2 , wherein R 7 is as defined above; or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
222 words
A 3(2H)pyridazinone of the formula: ##STR31## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is --N(R 7 ) 2 , wherein R 7 is as defined above; or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
220 words
A 3(2H)pyridazinone of the formula: ##STR32## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is --SR 8 , wherein R 8 is as defined above; or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
220 words
A 3(2H)pyridazinone of the formula: ##STR32## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is --SR 8 , wherein R 8 is as defined above; or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
215 words
A 3(2H)pyridazinone of the formula: ##STR33## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is C 2 -C 8 alkenyl or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
215 words
A 3(2H)pyridazinone of the formula: ##STR33## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkenyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is C 2 -C 8 alkenyl or a pharmaceutically acceptable salt thereof.
Claim 14
Dependent Claim
164 words
The pyridazinone according to any of claims 7, 1, 2, 3, 5, or 6, wherein R 1 is hydrogen; methyl; allyl; cyclopentyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , wherein R 3 is hydrogen, methyl, ethyl, t-butyl, and m is an integer of 1 or 2; or --(CH 2 ) n A, wherein A is hydroxyl or dimethyl amino, and n is an integer which is 2 or 3; R 2 is chlorine or bromine; each of Y 1 and Y 2 , which may be the same or different, is hydrogen; C 1 -C 4 alkyl; C 3 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl, benzyl, or phenethyl; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 4 alkyl; --N(R 7 ) 2 , wherein R 7 is methyl or ethyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl.
Claim 15
Dependent Claim
15 words
The pyridazinone according to claim 2, which is 4-chloro-5-(3,4-dimethoxybenzylamino)-3(2H)pyridazinone, or a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim
15 words
The pyridazinone according to claim 2, which is 4-bromo-5-(3,4-dimethoxybenzylamino)-3(2H)pyridazinone, or a pharmaceutically acceptable salt thereof.
Claim 17
Dependent Claim
15 words
The pyridazinone according to claim 2, which is 4-chloro-5-(3-ethoxy-4-methoxybenzylamino)-3(2H)pyridazinone, or a pharmaceutically acceptable salt thereof.
Claim 18
Dependent Claim
15 words
The pyridazinone according to claim 2, which is 4-bromo-5-(3-ethoxy-4-methoxybenzylamino)-3(2H)pyridazinone, or a pharmaceutically acceptable salt thereof.
Claim 19
Dependent Claim
15 words
The pyridazinone according to claim 2, which is 4-chloro-5-(3-n-propoxy-4-methoxybenzylamino)-3(2H)pyridazinone, or a pharmaceutically acceptable salt thereof.
Claim 20
Dependent Claim
15 words
The pyridazinone according to claim 2, which is 4-bromo-5-(3-n-propoxy-4-methoxybenzylamino)-3(2H)pyridazinone, or a pharmaceutically acceptable salt thereof.
Claim 21
Dependent Claim
15 words
The pyridazinone according to claim 2, which is 4-chloro-5-(3-n-butoxy-4-methoxybenzylamino-3(2H)pyridazinone, or a pharmaceutically acceptable salt thereof.
Claim 22
Dependent Claim
15 words
The pyridazinone according to claim 2, which is 4-bromo-5-(3-n-butoxy-4-methoxybenzylamino)-3(2H)pyridazinone or a pharmaceutically acceptable salt thereof.
Claim 23
Dependent Claim
9 words
The pyridazinone according to claim 2, which is 4-chloro-5-(3-pentyloxy-4-methoxybenzylamino)-3(2H)pyridazinone.
Claim 24
Dependent Claim
9 words
The pyridazinone according to claim 2, which is 4-bromo-5-(3-n-pentyloxy-4-methoxybenzylamino)-3(2H)pyridazinone.
Claim 25
Dependent Claim
9 words
The pyridazinone according to claim 2, which is 4-chloro-5-(3-n-hexyloxy-4-methoxybenzylamino)-3(2H)pyridazinone.
Claim 26
Dependent Claim
9 words
The pyridazinone according to claim 2, which is 4-bromo-5-(3-n-hexyloxy-4-methoxybenzylamino)-3(2H)pyridazinone.
Claim 27
Dependent Claim
84 words
The pyridazinone according to claim 2, wherein R 1 is hydrogen; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 4 alkyl; --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl; chlorine or --SCH 3 ; and Y 3 is --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl; chlorine or --SCH 3 .
Claim 28
Dependent Claim
75 words
The pyridazinone according to claim 2, wherein R 1 is hydrogen; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen, C 1 -C 4 alkyl or --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl; and Y 3 is --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl.
Claim 29
Dependent Claim
33 words
An anti-allergic agent according to any of claims 7, 1, 2, 3, 5 or 6, comprising an effective amount of said 3(2H)pyridazinone; or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
Claim 30
Independent Claim
304 words
A method of reducing the incidence or severity of allergy induced in a subject by SRS-A, which comprises administering to said subject an amount effective to reduce the incidence or severity of the allergy of a 3(2H)pyridazinone of the formula: ##STR34## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkeyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , whererin R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is C 1-5 alkyl, C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is as defined above; --CO 2 R 6 , wherein R 6 is as defined above; --N(R 7 ) 2 , wherein R 7 is as defined above; or --SR 8 , wherein R 8 is as defined above; or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
Claim 31
Independent Claim
304 words
A method of reducing the incidence or severity of allergy induced in a subject by SRS-A, which comprises administering to said subject an amount effective to reduce the incidence or severity of the allergy of a 3(2H)pyridazinone of the formula: ##STR34## wherein R 1 is hydrogen; methyl; C 3 -C 6 alkeyl; C 5 or C 6 cycloalkyl; benzyl; phenyl; --(CH 2 ) m CO 2 R 3 , whererin R 3 is hydrogen or C 1 -C 5 alkyl, and m is an integer of from 1 to 4; --(CH 2 ) n A, wherein A is --OH or --N(R 4 ) 2 , wherein R 4 is C 1 -C 3 alkyl, and n is an integer of from 2 to 6; or --CH 2 CF 3 ; R 2 is chlorine or bromine; each of Y 1 and Y 2 which may be the same or different, is hydrogen; C 1 -C 5 alkyl; C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is hydrogen, C 1 -C 8 alkyl or --(CH 2 ) q -phenyl, wherein q is an integer of from 1 to 4; --CO 2 R 6 , wherein R 6 is hydrogen or C 1 -C 5 alkyl; --N(R 7 ) 2 , wherein R 7 is C 1 -C 4 alkyl; or --SR 8 , wherein R 8 is C 1 -C 4 alkyl; and Y 3 is C 1-5 alkyl, C 2 -C 8 alkenyl; halogen; --OR 5 , wherein R 5 is as defined above; --CO 2 R 6 , wherein R 6 is as defined above; --N(R 7 ) 2 , wherein R 7 is as defined above; or --SR 8 , wherein R 8 is as defined above; or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
Claim 32
Dependent Claim
71 words
The pyridazinone according to claim 7, 1, 2 or 6, wherein R 1 is hydrogen, allyl or cyclopentyl; R 2 is chlorine or bromine; each of Y 1 and Y 2 , which may be the same or different, is hydrogen; C 1 -C 4 alkyl; C 5 -C 8 alkenyl; --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl; chlorine; or methyl mercapto.
Claim 33
Dependent Claim
76 words
The pyridazinone according to claim 7, wherein R 1 is hydrogen, allyl or cyclopentyl; R 2 is chlorine or bromine; each of Y 1 and Y 2 , which may be the same or different, is hydrogen; C 1 -C 4 alkyl; C 5 -C 8 alkenyl; --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl; chlorine; or methyl mercapto; and Y 3 is C 5 -C 8 alkenyl.
Claim 34
Dependent Claim
72 words
The pyridazinone according to claim 1, wherein R 1 is hydrogen, allyl or cyclopentyl; R 2 is chlorine or bromine; each of Y 1 and Y 2 , which may be the same or different, is hydrogen; C 1 -C 4 alkyl; C 5 -C 8 alkenyl; --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl; chlorine; or methyl mercapto; and Y 3 is chlorine.
Claim 35
Dependent Claim
87 words
The pyridazinone according to claim 2, wherein R 1 is hydrogen, allyl or cyclopentyl; R 2 is chlorine or bromine; each of Y 1 and Y 2 , which may be the same or different, is hydrogen; C 1 -C 4 alkyl; C 5 -C 8 alkenyl; --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl; chlorine; or methyl mercapto; and Y 3 is --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl.
Claim 36
Dependent Claim
73 words
The pyridazinone according to claim 6, wherein R 1 is hydrogen, allyl or cyclopentyl; R 2 is chlorine or bromine; each of Y 1 and Y 2 , which may be the same or different, is hydrogen; C 1 -C 4 alkyl; C 5 -C 8 alkenyl; --OR 5 , wherein R 5 is hydrogen, C 1 -C 7 alkyl, benzyl or phenethyl; chlorine; or methyl mercapto; and Y 3 is methyl mercapto.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-01-08 | 1993-07-10 | 1994-01-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-01-08 | 1997-07-10 | 1998-01-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-01-08 | 2001-07-10 | 2002-01-09 | $7700.00 | Window Closed / Lapsed |