Patent US4490527A successfully refreshed from Google Patents.
US4490527A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Benzo-fused heterocyclic anti-ulcer agents
Assignee: Wyeth LLC
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Filing: 1983-02-22
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Granted: 1984-12-25
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Expires: 2003-02-22
Abstract
Abstract Compounds of the formula: ##STR1## wherein B is a moiety having the formula: ##STR2## R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, cycloalkyl of 4-7 carbon atoms, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, lower alkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro. X is SO 2 , SO, S or C═O; and A is amine selected from the group ##STR3## , wherein R 1 is hydrogen or R 2 CH 2 wherein R 2 is mono- or diloweralkylamino, mono- or di-N-lower alkylaminoloweralkyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl; R 3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R 3 is (1-piperidinyl)methyl, R 1 is hydrogen; n is 1 to 4, and the pharmacologically acceptable salts thereof.
Inventors
- 👤 Guy A. Schiehser
- 👤 Donald P. Strike
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 14:24
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/44; C07D209/48; C07D209/46; C07D209/50; C07D275/00; C07D275/04; C07D275/06; C07D277/00; C07D277/02; C07D277/04; C07D295/00; C07D295/04; C07D295/08; C07D295/096; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/52; C07D417/00; C07D417/02; C07D417/12; C07D495/00; C07D495/02; C07D495/04; C07D513/00; C07D513/02; C07D513/04
Claims Analysis
Total Claims: 42
Claim 1
Independent Claim
158 words
A compound having the formula: ##STR21## wherein B is a moiety having the formula: ##STR22## R is hydrogen, mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl of 2-5 carbon atoms, lowercycloalkyl, carboxy, alkoxycarbonyl of 2-7 carbon atoms, mono- or di-loweralkyl substituted amino, alkanoylamino of 2-5 carbon atoms, lower alkyl thio, loweralkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro; X is SO 2 , SO, S or C═O; and A is an amine selected from the group: ##STR23## wherein R 1 is hydrogen or R 2 CH 2 wherein R 2 is mono- or diloweralkylamino, mono- or di-N-loweralkylaminoloweralkyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-tetrahydrothiazolyl, 4-morpholinyl or 4-thiomorpholinyl; R 3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R 3 is (1-piperidinyl)methyl, R 1 is hydrogen; n is 1 to 4, or a pharmacologically acceptable salt thereof.
Claim 2
Dependent Claim
158 words
A compound having the formula: ##STR21## wherein B is a moiety having the formula: ##STR22## R is hydrogen, mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl of 2-5 carbon atoms, lowercycloalkyl, carboxy, alkoxycarbonyl of 2-7 carbon atoms, mono- or di-loweralkyl substituted amino, alkanoylamino of 2-5 carbon atoms, lower alkyl thio, loweralkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro; X is SO 2 , SO, S or C═O; and A is an amine selected from the group: ##STR23## wherein R 1 is hydrogen or R 2 CH 2 wherein R 2 is mono- or diloweralkylamino, mono- or di-N-loweralkylaminoloweralkyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-tetrahydrothiazolyl, 4-morpholinyl or 4-thiomorpholinyl; R 3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R 3 is (1-piperidinyl)methyl, R 1 is hydrogen; n is 1 to 4, or a pharmacologically acceptable salt thereof.
Claim 3
Dependent Claim
11 words
The compound of claim 1, wherein the moiety B is ##STR24##
Claim 4
Dependent Claim
10 words
The compound of claim 1, having the name N-[2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl]-1,2-benzisothiazol-3-amino 1,1-dioxide.
Claim 5
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 6
Dependent Claim
10 words
The compound of claim 1, having the name [4-[[[-2-[(1,2-benzisothiazol-3-yl)amino]ethyl]thio]methyl]-2-thiazol-yl]guanidine S',S'-dioxide.
Claim 7
Dependent Claim
9 words
The compound of claim 1, having the name 3-[[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]amino]]-1H-isoindol-1-one.
Claim 8
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl)]phenoxy]propyl]-6-nitro-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 9
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-6-amino-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 10
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-6-chloro-benzisothiazol-3-amine 1,1-dioxide.
Claim 11
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-6-fluoro-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 12
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-5,6-dichloro-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 13
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-5-methyl-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 14
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-5-chloro-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 15
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-5-methoxy-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 16
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-6-sulfamoyl-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 17
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-6-bromo-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 18
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(1-piperidinyl)methyl]phenoxy]propyl]-5-fluoro-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 19
Dependent Claim
10 words
The compound of claim 1, having the same N-[3-[3-(4-morpholinylmethyl)phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 20
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(dipropylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 21
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(diethylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 22
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-(1-pyrrolidinylmethyl)phenoxy]propyl]-1,2-benzisothiazol-3-amine, 1,1-dioxide.
Claim 23
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(dimethylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 24
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(dibutylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 25
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(4-thiomorpholinyl)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 26
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(hexahydro-1H-azepin-1-yl)methyl]phenoxy]propyl]-1,2-benziosothiazol-3-amine 1,1-dioxide.
Claim 27
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(3-thiazolidinyl)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 28
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(octahydro-1(2H)-azocinyl)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 29
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(cyclohexylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 30
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(cyclopentylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 31
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[[[(2-furanyl)methyl]amino]methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 32
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(benzylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 33
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[[bis(2-methylpropyl)amino]methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 34
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(butylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 35
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(methylpentylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 36
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(butylpropylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 37
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(butylmethylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 38
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[3-[(dipentylamino)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 39
Dependent Claim
10 words
The compound of claim 1, having the name N-[3-[4-[(1-piperidinyl)methyl]phenoxy]propyl]-1,2-benzisothiazol-3-amine 1,1-dioxide.
Claim 40
Dependent Claim
10 words
The compound of claim 1, having the name N-[2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl]thieno[3,4-d]isothiazole-3-amine 1,1-dioxide.
Claim 41
Dependent Claim
11 words
The compound of claim 1, having the name [4-[[[2-[(thieno[3,4-d]isothiazol-3-yl)amino]ethyl]thio]methyl]-2-thiazolyl guanidine S',S'-dioxide.
Claim 42
Dependent Claim
10 words
The compound of claim 1, having the name N-[2-[3-(1-piperidinylmethyl)phenoxy]ethyl]thieno[3,4-d]isothiazol-3-amine 1,1-dioxide.
References Cited (Backward Citations)
US4325963A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-12-25 | 1988-06-25 | 1988-12-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-12-25 | 1992-06-25 | 1992-12-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-12-25 | 1996-06-25 | 1996-12-25 | $7700.00 | Window Closed / Lapsed |