Patent US3973017A successfully refreshed from Google Patents.
US3973017A
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US
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Imidazothiazines, derivatives and analogues thereof
Assignee: Merck and Co Inc
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Filing: 1975-07-07
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Granted: 1976-08-03
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Expires: 1995-07-07
Abstract
Abstract Disclosed are 2,3,5,6-tetrahydro-8H-imidazo-[2,1-c][1,4]thiazines, analogues and derivatives thereof which are effective in inhibiting indoleamine-N-methyl transferase and thus useful in the treatment of mental aberrations, such as schizophrenia. Also disclosed are processes for the preparation of such imidazothiazines; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions.
Inventors
- 👤 Paul S. Anderson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 06:58
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/04; C07D241/00; C07D241/02; C07D241/06; C07D241/08; C07D265/00; C07D265/28; C07D265/30; C07D265/32; C07D279/00; C07D279/10; C07D279/12; C07D513/00; C07D513/02; C07D513/04
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
65 words
A compound having the structure: ##SPC5## wherein A is selected from the group consisting of S, O, and NR; and wherein R is selected from the group consisting of hydrogen, lower alkyl, or lower alkoxycarbonyl; and R 1 and R 2 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxy carbonyl; and the pharmaceutically acceptable N-acid addition salts thereof.
Claim 2
Dependent Claim
65 words
A compound having the structure: ##SPC5## wherein A is selected from the group consisting of S, O, and NR; and wherein R is selected from the group consisting of hydrogen, lower alkyl, or lower alkoxycarbonyl; and R 1 and R 2 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxy carbonyl; and the pharmaceutically acceptable N-acid addition salts thereof.
Claim 3
Dependent Claim
10 words
A compound according to claim 1 which is 2,3,5,6-tetrahydro-8H-imidazo[2,1-c] [1,4]-thiazine.
Claim 4
Dependent Claim
10 words
A compound according to claim 1 which is 2,3,5,6-tetrahydro-8H-imidazo[2,1-c] [1,4]-oxazine.
Claim 5
Dependent Claim
11 words
A compound according to claim 1 which is ethyl 2,3,5,6,7,8-hexahydroimidazo[1,2-a] -pyrazine-7-carboxylate.
Claim 6
Dependent Claim
76 words
A process for preparing a compound having the structure: ##SPC6## thereof which comprises cyclizing in the presence of base a compound having the structure: ##SPC7## wherein X is halogen; A is selected from the group consisting of S, O, NR; R 1 and R 2 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, or lower alkoxy carbonyl; and R is selected from the group consisting of hydrogen, lower alkyl, and lower alkoxycarbonyl.
Claim 7
Dependent Claim
76 words
A process for preparing a compound having the structure: ##SPC6## thereof which comprises cyclizing in the presence of base a compound having the structure: ##SPC7## wherein X is halogen; A is selected from the group consisting of S, O, NR; R 1 and R 2 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, or lower alkoxy carbonyl; and R is selected from the group consisting of hydrogen, lower alkyl, and lower alkoxycarbonyl.
Claim 8
Dependent Claim
83 words
A pharmaceutical composition comprising a therapeutically effective amount in unitary dosage form of a compound having the structure: ##SPC8## wherein A is selected from the group consisting of S, O, and NR; and wherein R is selected from the group consisting of hydrogen, lower alkyl, or lower alkoxy carbonyl; and R 1 and R 2 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxycarbonyl; and the pharmaceutically acceptable N-acid addition salts thereof; and a pharmaceutical carrier therefor.
Claim 9
Dependent Claim
83 words
A pharmaceutical composition comprising a therapeutically effective amount in unitary dosage form of a compound having the structure: ##SPC8## wherein A is selected from the group consisting of S, O, and NR; and wherein R is selected from the group consisting of hydrogen, lower alkyl, or lower alkoxy carbonyl; and R 1 and R 2 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxycarbonyl; and the pharmaceutically acceptable N-acid addition salts thereof; and a pharmaceutical carrier therefor.
Claim 10
Independent Claim
80 words
A method of treatment comprising administering a therapeutically effective amount in unitary dosage form of a compound having the structure: ##SPC9## wherein A is selected from the group consisting of S, O, and NR; and wherein R is selected from the group consisting of hydrogen, lower alkyl, or lower alkoxy carbonyl; and R 1 and R 2 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxycarbonyl; and the pharmaceutically acceptable N-acid addition salts thereof.
Claim 11
Independent Claim
80 words
A method of treatment comprising administering a therapeutically effective amount in unitary dosage form of a compound having the structure: ##SPC9## wherein A is selected from the group consisting of S, O, and NR; and wherein R is selected from the group consisting of hydrogen, lower alkyl, or lower alkoxy carbonyl; and R 1 and R 2 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxycarbonyl; and the pharmaceutically acceptable N-acid addition salts thereof.
References Cited (Backward Citations)
US3835144A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-08-03 | 1980-02-02 | 1980-08-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-08-03 | 1984-02-02 | 1984-08-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-08-03 | 1988-02-02 | 1988-08-03 | $7700.00 | Window Closed / Lapsed |