US5071844A
Expired / Lapsed
US
⏱️ 0.0 years remaining
5,11-dihydrodibenzo[b,e][1,4]-thiazepines useful as gastro intestinal selective calcium antagonists
Assignee: Pfizer Inc
•
Filing: 1990-05-23
•
Granted: 1991-12-10
•
Expires: 2010-05-23
Abstract
Abstract The invention provides compounds of the formula: ##STR1## wherein k is 1, 2 or 3; m is 1, 2 or 3; n is 1, 2 or 3; p is 0, 1 or 2; X is O, S or a direct link, with the proviso that when X is O or S, n is 2 or 3; R 1 is H or C 1-C 4 alkyl; and R 2 is an optionally substituted phenyl or heteroaryl group; and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of motility disorders, particularly those of the gut such as irritable bowel syndrome.
Inventors
- 👤 David Alker
- 👤 Robert J. Bass
- 👤 Peter E. Cross
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 01:50
CPC Classifications
C; C07; C07D; C07D417/00; C07D417/02; C07D417/06; C07D207/00; C07D207/02; C07D207/04; C07D207/08; C07D207/09; C07D417/14
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
171 words
A compound of the formula: ##STR81## wherein k is 1, 2 or 3; m is 1, 2 or 3; n is 1, 2 or 3; p is 0, 1 or 2; X is 0, S or a direct link, with the proviso that when X is 0 or S, n is 2 or 3; R 1 is H or C 1 -C 4 alkyl; and R 2 is (a) ##STR82## wherein R 3 and R 4 are each independently selected from H, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, --OH, --N(C 1 -C 4 alkyl) 2 , halo and --CF 3 ; (b) ##STR83## wherein q is 1, 2 or 3, and X 1 and X 2 are each independently selected from 0 and --CH 2 --; or (c) a pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl or thienyl group, said group being optionally substituted by up to 2 substituents each independently selected from C 1 -C 4 alkyl and C 1 -C 4 alkoxy, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
171 words
A compound of the formula: ##STR81## wherein k is 1, 2 or 3; m is 1, 2 or 3; n is 1, 2 or 3; p is 0, 1 or 2; X is 0, S or a direct link, with the proviso that when X is 0 or S, n is 2 or 3; R 1 is H or C 1 -C 4 alkyl; and R 2 is (a) ##STR82## wherein R 3 and R 4 are each independently selected from H, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, --OH, --N(C 1 -C 4 alkyl) 2 , halo and --CF 3 ; (b) ##STR83## wherein q is 1, 2 or 3, and X 1 and X 2 are each independently selected from 0 and --CH 2 --; or (c) a pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl or thienyl group, said group being optionally substituted by up to 2 substituents each independently selected from C 1 -C 4 alkyl and C 1 -C 4 alkoxy, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
17 words
A compound of the formula (I) as claimed in claim 1 wherein k is 1 or 2.
Claim 4
Dependent Claim
15 words
A compound of the formula (I) as claimed in claim 2 wherein k is 1.
Claim 5
Dependent Claim
17 words
A compound of the formula (I) as claimed in claim 1 wherein m is 1 or 2.
Claim 6
Dependent Claim
15 words
A compound of the formula (I) as claimed in claim 4 wherein m is 1.
Claim 7
Dependent Claim
15 words
A compound of the formula (I) as claimed in claim 1 wherein n is 2.
Claim 8
Dependent Claim
14 words
A compound of formula (I) as claimed in claim 1 wherein p is 0.
Claim 9
Dependent Claim
17 words
A compound of the formula (I) as claimed in claim 1 wherein X is a direct link.
Claim 10
Dependent Claim
18 words
A compound of the formula (I) as claimed in claim 1 wherein R 1 is H or methyl.
Claim 11
Dependent Claim
16 words
A compound of the formula (I) as claimed in claim 9 wherein R 1 is H.
Claim 12
Dependent Claim
89 words
A compound of the formula (I) as claimed in claim 1 wherein R 2 is (a) ##STR84## wherein R 3 and R 4 are each independently selected from H, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, --OH and halo; (b) ##STR85## wherein X 1 and X 2 are as defined in claim 1; or (c) a pyridinyl, pyrimidinyl or thienyl group, said group being optionally substituted by up to 2 substituents each independently selected from C 1 -C 4 alkyl and C 1 -C 4 alkoxy.
Claim 13
Dependent Claim
28 words
A compound of the formula (I) as claimed in claim 11 wherein R 2 is phenyl, 3-methylphenyl, 4-methylphenyl, 4-hydroxyphenyl, 4-methoxyphenyl, 3,4-dimethoxyphenyl, 4-chlorophenyl, 5-indanyl, 3,4-methylenedioxyphenyl, 2-pyridinyl, 4-pyrimidinyl or 3-thienyl.
Claim 14
Dependent Claim
16 words
A compound of the formula (I) as claimed in claim 12 wherein R 2 is 4-methoxyphenyl.
Claim 15
Dependent Claim
17 words
A (2S)-stereoisomer of a compound of the formula (I) as claimed in claim 1, that is ##STR86##
Claim 16
Dependent Claim
15 words
A maleate salt of a compound of the formula (I) as claimed in claim 1.
Claim 17
Dependent Claim
29 words
A pharmaceutical composition comprising a compound of the formula (I), or a pharmaceutically acceptable salt thereof, as claimed in claim 1, together with a pharmaceutically acceptable diluent or carrier.
Claim 18
Dependent Claim
52 words
A method of treating a mammal afflicted with a motility disorder, particularly of the gut such as irritable bowel syndrome, which comprises treating said animal with an effective amount of a compound of the formula (I), or with, as appropriate, a pharmaceutically acceptable salt or composition thereof, as claimed in claim 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-12-09 | 1995-06-10 | 1995-12-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-12-09 | 1999-06-10 | 1999-12-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-12-09 | 2003-06-10 | 2003-12-10 | $7700.00 | Window Closed / Lapsed |