US4483867A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antifibrinolytically active derivatives of tranexamic acid
Assignee: Pfizer Health AB
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Filing: 1982-11-10
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Granted: 1984-11-20
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Expires: 2002-11-10
Abstract
Abstract Novel antifibrinolytically active compounds of the formula ##STR1## and therapeutically acceptable salt thereof, wherein R 1 is selected from the group consisting of (a) alkyl groups containing 1-4 carbon atoms, (b) alkoxy groups containing 1-4 carbon atoms, ##STR2## R 2 is selected from the group consisting of (a) H, (b) alkyl groups containing 1-4 carbon atoms, (c) --COOR 3 , wherein R 3 is an alkyl group containing 1-4 carbon atoms, (d) --CONR 4 R 5 , wherein R 4 and R 5 are the same or different alkyl groups containing 1-3 carbon atoms; or wherein R 1 and R 2 represent together the radical ##STR3##
Inventors
- 👤 Carl M. E. Svahn
- 👤 Ferenc Merenyi
- 👤 Lennart E. Karlsson
- 👤 Gunnar Hanshoff
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 23:03
CPC Classifications
C; C07; C07C; C07C255/00; A; A61; A61P; A61P7/00; A61P7/02; A61P7/04; C07D; C07D307/00; C07D307/77; C07D307/87; C07D307/89
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
104 words
A compound of the formula ##STR74## and therapeutically acceptable salt thereof, wherein R 1 is selected from the group consisting of (a) alkyl groups containing 1-4 carbon atoms, (b) alkoxy groups containing 1-4 carbon atoms, ##STR75## R 2 is selected from the group consisting of (a) H, (b) alkyl groups containing 1-4 carbon atoms, (c) --COOR 3 , wherein R 3 is an alkyl group containing 1-4 carbon atoms, (d) --CONR 4 R 5 , wherein R 4 and R 5 are the same or different alkyl groups containing 1-3 carbon atoms; or wherein R 1 and R 2 represent together the radical ##STR76##
Claim 2
Dependent Claim
104 words
A compound of the formula ##STR74## and therapeutically acceptable salt thereof, wherein R 1 is selected from the group consisting of (a) alkyl groups containing 1-4 carbon atoms, (b) alkoxy groups containing 1-4 carbon atoms, ##STR75## R 2 is selected from the group consisting of (a) H, (b) alkyl groups containing 1-4 carbon atoms, (c) --COOR 3 , wherein R 3 is an alkyl group containing 1-4 carbon atoms, (d) --CONR 4 R 5 , wherein R 4 and R 5 are the same or different alkyl groups containing 1-3 carbon atoms; or wherein R 1 and R 2 represent together the radical ##STR76##
Claim 3
Dependent Claim
20 words
A compound according to claim 1 and therapeutically acceptable salts thereof, wherein R 2 is H or CH 3 .
Claim 4
Dependent Claim
22 words
A compound according to claim 1 and therapeutically acceptable salts thereof wherein R 1 is an alkyl group containing 1-4 carbon atoms.
Claim 5
Dependent Claim
22 words
A compound according to claim 1, and therapeutically acceptable salts thereof, wherein R 1 is an alkoxy group containing 1-4 carbon atoms.
Claim 6
Dependent Claim
16 words
A compound according to claim 1, and therapeutically acceptable salts thereof, wherein R 1 is ##STR77##
Claim 7
Dependent Claim
43 words
A compound according to claim 1, and therapeutically acceptable salt thereof wherein R 1 is an alkyl group containing 1-4 carbon atoms, an alkoxy group containing 1-4 carbon atoms, or the radical ##STR78## and wherein R 2 is H or CH 3 .
Claim 8
Dependent Claim
31 words
A compound according to claim 1, and therapeutically acceptable salts thereof, wherein R 1 is an alkoxy group containing 1-4 carbon atoms and R 2 is H or CH 3 .
Claim 9
Dependent Claim
15 words
A compound of claim 1 having the formula ##STR79## or a therapeutically acceptable salt thereof.
Claim 10
Dependent Claim
15 words
A compound of claim 1 having the formula ##STR80## or a therapeutically acceptable salt thereof.
Claim 11
Dependent Claim
15 words
A compound of claim 1 having the formula ##STR81## or a therapeutically acceptable salt thereof.
Claim 12
Dependent Claim
15 words
A compound of claim 1 having the formula ##STR82## or a therapeutically acceptable salt thereof.
Claim 13
Dependent Claim
13 words
A compound according to claim 1 in the form of its trans isomer.
Claim 14
Dependent Claim
12 words
A compound according to claim 1 in the form of its hydrochloride.
Claim 15
Dependent Claim
36 words
A method for the treatment in mammals and man of ailments due to increased fibrinolysis, characterized by administration to a host in need thereof of a therapeutically effective amount of a compound according to claim 1.
Claim 16
Dependent Claim
31 words
A method for the treatment of peptic ulcers in man, characterized in administration to a host in need thereof of a therapeutically effective amount of a compound according to claim 1.
Claim 17
Dependent Claim
32 words
A method for the treatment of hereditary angioneurotic edema in man, characterized in administration to a host in need thereof of a therapeutically effective amount of a compound according to claim 1.
Claim 18
Dependent Claim
32 words
A pharmaceutical preparation for treatment of ailments due to increase fibrinolysis containing as an active ingredient a compound as defined in claim 1, in an amount effective for treatment of said ailments.
Claim 19
Dependent Claim
22 words
The pharmaceutical preparation of claim 16 which is in dosage unit form for oral application containing 50-500 mg. of said active ingredient.
Claim 20
Dependent Claim
30 words
The pharmaceutical preparation of claim 17 which is in dosage unit form as a liquid preparation for oral application containing about 0.1% to 20% by weight of said active ingredient.
Claim 21
Dependent Claim
12 words
The pharmaceutical preparation of claim 17 which is in dosage unit form.
Claim 22
Dependent Claim
27 words
The pharmaceutical preparation of claim 17 which is in dosage unit form for parenteral application by injection containing from 0.1 to 10 mg. of said active ingredient.
Claim 23
Dependent Claim
32 words
A pharmaceutical preparation for the treatment of peptic ulcers in man containing as active ingredient a compound as defined in claim 1 in an amount effective for the treatment of peptic ulcers.
Claim 24
Dependent Claim
12 words
The pharmaceutical preparation of claim 22 which is in dosage unit form.
Claim 25
Dependent Claim
32 words
The pharmaceutical preparation of claim 22 which is in the form of a liquid unit dosage preparation for oral application containing from about 0.1% to 20% by weight of said active ingredient.
Claim 26
Dependent Claim
25 words
The pharmaceutical preparation of claim 22 which is in the form of a dosage unit for oral preparation containing 50-500 mg. of said active ingredient.
Claim 27
Dependent Claim
35 words
A pharmaceutical preparation for the treatment of hereditary angioneurotic edema in man containing as active ingredient a compound as defined in claim 1 in an amount effective for the treatment of said hereditary antioneurotic edema.
Claim 28
Dependent Claim
11 words
The pharmaceutical preparation of claim 26 being in dosage unit form.
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) | 1987-11-20 | 1988-05-21 | 1988-11-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-11-20 | 1992-05-21 | 1992-11-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-11-20 | 1996-05-21 | 1996-11-20 | $7700.00 | Window Closed / Lapsed |