US4560685A
Expired / Lapsed
US
⏱️ 0.0 years remaining
2-Piperazino-pteridines useful as antithrombotics and antimetastatics
Assignee: Boehringer Ingelheim Pharma GmbH and Co KG
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Filing: 1984-06-18
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Granted: 1985-12-24
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Expires: 2004-06-18
Abstract
Abstract Compounds of the formula <IMAGE> wherein R1 is phenylalkylamino, alkylamino, dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; R2 is dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; and R3 is halogen, alkoxy, alkylthio, phenylalkoxy or phenylalkylthio; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics and antimetastatics.
Inventors
- 👤 Josef Roch
- 👤 Josef Nickl
- 👤 Erich Muller
- 👤 Berthold Narr
- 👤 Johannes Weisenberger
- 👤 Rainer Zimmermann
- 👤 Walter Haarmann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 09:17
CPC Classifications
C; C07; C07D; C07D475/00; C07D475/06; C07D475/08
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
94 words
A compound of the formula ##STR6## wherein R 1 is [phenyl(alkyl of 1 to 3 carbon atoms)]amino, (alkyl of 1 to 3 carbon atoms)amino, di(alkyl of 1 to 3 carbon atoms)amino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; R 2 is di(alkyl of 1 to 3 carbon atoms)amino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; and R 3 is halogen, alkoxy of 1 to 3 carbon atoms, (alkyl of 1 to 3 carbon atoms)thio, phenyl(alkoxy of 1 to 3 carbon atoms) or phenyl(alkyl of 1 to 3 carbon atoms)thio; or a non-toxic, pharmacologically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
94 words
A compound of the formula ##STR6## wherein R 1 is [phenyl(alkyl of 1 to 3 carbon atoms)]amino, (alkyl of 1 to 3 carbon atoms)amino, di(alkyl of 1 to 3 carbon atoms)amino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; R 2 is di(alkyl of 1 to 3 carbon atoms)amino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; and R 3 is halogen, alkoxy of 1 to 3 carbon atoms, (alkyl of 1 to 3 carbon atoms)thio, phenyl(alkoxy of 1 to 3 carbon atoms) or phenyl(alkyl of 1 to 3 carbon atoms)thio; or a non-toxic, pharmacologically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
57 words
A compound of claim 1, where R 1 is dimethylamino, benzylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; R 2 is dimethylamino, piperidino, morpholino, thiomorpholino or 1-oxidothiomorpholino, and R 3 is chlorine, bromine, alkoxy of 1 to 3 carbon atoms, (alkyl of 1 to 3 carbon atoms)mercapto, benzyloxy or benzylmercapto; or a non-toxic, pharmacologically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
55 words
A compound of claim 1, where R 1 is benzylamino, dimethylamino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; R 2 is dimethylamino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; and R 3 is chlorine, alkoxy of 1 to 3 carbon atoms or (alkyl of 1 to 3 carbon atoms)mercapto; benzyloxy or benzylmercapto; or a non-toxic, pharmacologically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
38 words
A compound of claim 1 where R 1 is benzylamino, dimethylamino, morpholino, or 1-oxido-thiomorpholino; R 2 is dimethylamino, morpholino or 1-oxido-thiomorpholino; and R 3 is chlorine, methylmercapto or benzylmercapto; or a non-toxic, pharmacologically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
17 words
A compound of claim 1, which is 6-benzylthio-4,7-dimorpholino-2-piperazino-pteridine or a non-toxic, pharmacologically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
17 words
A compound of claim 1, which is 6-chloro-4,7-bis(dimethylamino)-2-piperazino-pteridine or a non-toxic, pharmacologically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
17 words
A compound of claim 1, which is 6-benzylthio-4,7-bis(dimethylamino)-2-piperazino-pteridine or a non-toxic, pharmacologically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
26 words
An antithrombotic or antimetastatic pharmaceutical composition consisting essentially of an inert pharmaceutical carrier and an effective antithrombotic or antimetastatic amount of a compound of claim 1.
Claim 10
Dependent Claim
39 words
The method of preventing or relieving thromboses or inhibiting metastases in a warm-blooded animal in need thereof, which comprises perorally, parenterally or rectally administering to said animal an effective antithrombotic or antimetastatic amount of a compound of 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) | 1988-12-23 | 1989-06-24 | 1989-12-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-12-23 | 1993-06-24 | 1993-12-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-12-23 | 1997-06-24 | 1997-12-24 | $7700.00 | Window Closed / Lapsed |