US4694002A
Expired / Lapsed
US
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Benzothiazepine derivatives
Assignee: ER Squibb and Sons LLC
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Filing: 1986-08-21
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Granted: 1987-09-15
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Expires: 2006-08-21
Abstract
Abstract Calcium channel blocking activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein the stereochemistry at the chiral centers in the 3 and 4-positions of the benzothiazepine nucleus is cis, and wherein R 1 is alkyl, aryl, arylalkyl, alkenyl or alkynyl; R 2 and R 5 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; and R 3 and R 4 are each independently alkyl or cycloalkyl or R 3 and R 4 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl.
Inventors
- 👤 David Floyd
- 👤 Karnail Atwal
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 17:29
CPC Classifications
C; C07; C07D; C07D281/00; C07D281/02; C07D281/04; C07D281/08; C07D281/10; A; A61; A61P; A61P3/00; A61P3/12; A61P3/14; A61P9/00; A61P9/12
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
100 words
A compound having the formula ##STR11## or a pharmaceutically acceptable salt thereof, wherein the stereochemistry at the chiral centers in the 2 and 3-positions of the benzothiazepine nucleus is cis, and wherein R 1 is alkyl, aryl, arylalkyl, alkenyl or alkynyl; R 2 and R 5 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; and R 3 and R 4 are each independently alkyl or cycloalkyl or R 3 and R 4 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl.
Claim 2
Dependent Claim
100 words
A compound having the formula ##STR11## or a pharmaceutically acceptable salt thereof, wherein the stereochemistry at the chiral centers in the 2 and 3-positions of the benzothiazepine nucleus is cis, and wherein R 1 is alkyl, aryl, arylalkyl, alkenyl or alkynyl; R 2 and R 5 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; and R 3 and R 4 are each independently alkyl or cycloalkyl or R 3 and R 4 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl.
Claim 3
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is alkyl.
Claim 4
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is aryl.
Claim 5
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is arylalkyl.
Claim 6
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is alkenyl.
Claim 7
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is alkynyl.
Claim 8
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is methyl.
Claim 9
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 2 is hydrogen.
Claim 10
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 5 is hydrogen.
Claim 11
Dependent Claim
15 words
A compound in accordance with claim 1 wherein R 2 and R 5 are hydrogen.
Claim 12
Dependent Claim
16 words
A compound in accordance with claim 1 wherein R 3 and R 4 are each alkyl.
Claim 13
Dependent Claim
16 words
A compound in accordance with claim 1 wherein R 3 and R 4 are each methyl.
Claim 14
Dependent Claim
14 words
The compound in accordance with claim 1, (cis)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-3-methyl-2-phenyl-1,5-benzothiazepin-4(5H)-one, or a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim
14 words
The compound in accordance with claim 1, (cis)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-3-methyl-1,5-benzothiazepin-4(5H)-one, or a pharmaceutically acceptable salt thereof.
Claim 16
Independent Claim
123 words
A method of controlling blood pressure in a mammalian host in need thereof, which comprises administering to said host an effective amount of a compound having the formula ##STR12## or a pharmaceutically accpetable salt thereof, wherein the stereochemistry at the chiral centers in the 2 and 3-position of the benzothiazepine nucleus is cis, and wherein R 1 is alkyl, aryl, arylalkyl, alkenyl or alkynyl; R 2 and R 5 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; and R 3 and R 4 are each independently alkyl or cycloalkyl or R 3 and R 4 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl.
Claim 17
Independent Claim
123 words
A method of controlling blood pressure in a mammalian host in need thereof, which comprises administering to said host an effective amount of a compound having the formula ##STR12## or a pharmaceutically accpetable salt thereof, wherein the stereochemistry at the chiral centers in the 2 and 3-position of the benzothiazepine nucleus is cis, and wherein R 1 is alkyl, aryl, arylalkyl, alkenyl or alkynyl; R 2 and R 5 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; and R 3 and R 4 are each independently alkyl or cycloalkyl or R 3 and R 4 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl.
References Cited (Backward Citations)
US3075967A
Cited
US4590188A
Cited
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) | 1990-09-14 | 1991-03-16 | 1991-09-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-09-14 | 1995-03-16 | 1995-09-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-09-14 | 1999-03-16 | 1999-09-15 | $7700.00 | Window Closed / Lapsed |