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US4590291A Expired / Lapsed US ⏱️ 0.0 years remaining

Thrombin inhibitory new dihydroxybenzene ether derivatives

Assignee: Bayer AG
•
Filing: 1982-06-07
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Granted: 1986-05-20
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Expires: 2002-06-07
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Abstract

Abstract An ether derivative of a dihydroxybenzene of the formula ##STR1## in which R 1 is 1 to 3 identical or different substituents selected from hydrogen, halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto and carbalkoxy, with in each case 1 to 4 carbon atoms in the alkyl and alkoxy groups, and R 2 and R 3 are different and each is an alkyl or alkenyl chain in which 1 or 2 CH 2 chain members are optionally replaced by O, S, CO or a phenylene group, and/or in which the chain is optionally substituted by 1 to 3 identical or different substituents selected from hydroxyl, halogen, trifluoromethyl, phenyl, carboxyl, alkyl, alkoxy, alkylmercapto, carbalkoxy, and acyl, the phenyl radical in turn optionally being substituted by halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto or carbaloxy, and the abovementioned alkyl, alkoxy and acyl groups in each case containing 1 to 4 carbon atoms, and in which at least one of the radicals R 2 or R 3 is substituted and/or in at least one of the radicals R 2 or R 3 1 or 2 chain members are replaced by 1 or 2 identical or different radicals selected from O, S, CO and phenylene, is effective in combating cardiac infarcations, angina pectoric, thromboembolic illnesses, in venous and arterial regions and arteriosclerosis.

Inventors

  • 👤 Horst Boshagen
  • 👤 Ulrich Horlein
  • 👤 Gerd Reinhardt
  • 👤 Friedel Seuter
  • 👤 Elisabeth Perzborn

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 19:03
CPC Classifications
C; C07; C07C; C07C65/00; C07C65/21; C07C65/24; A; A61; A61P; A61P7/00; A61P7/02; A61P9/00; A61P9/08; A61P9/10; C07C59/00; C07C59/40; C07C59/58; C07C59/64; C07C59/66; C07C59/68; C07C59/76; C07C59/90; C07C65/32; C07C65/40

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 67 words
An ether derivative of a dihydroxybenzene of the formula ##STR40## wherein the ether groups are either ortho- or meta- to one another; A is selected from the group consisting of --COOH, --COOC 2 H 5 , --CH═CH--COOH and --CH═CH--COOC 2 H 5 ; B is an alkyl radical having from 3 to 6 carbon atoms, and n is 1 to 3, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 67 words
An ether derivative of a dihydroxybenzene of the formula ##STR40## wherein the ether groups are either ortho- or meta- to one another; A is selected from the group consisting of --COOH, --COOC 2 H 5 , --CH═CH--COOH and --CH═CH--COOC 2 H 5 ; B is an alkyl radical having from 3 to 6 carbon atoms, and n is 1 to 3, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 20 words
A compound according to claim 1, wherein such compound is of the formula ##STR41## or a pharmacologically acceptable salt thereof.
Claim 4
Dependent Claim 20 words
A compound according to claim 1, wherein such compound is of the formula ##STR42## or a pharmacologically acceptable salt thereof.
Claim 5
Dependent Claim 20 words
A compound according to claim 1, wherein such compound is of the formula ##STR43## or a pharmacologically acceptable salt thereof.
Claim 6
Dependent Claim 20 words
A compound according to claim 1, wherein such compound is of the formula ##STR44## or a pharmacologically acceptable salt thereof.
Claim 7
Dependent Claim 14 words
A compound according to claim 1, wherein such compound is of the formula ##STR45##
Claim 8
Dependent Claim 20 words
A thrombin-inhibitory composition comprising a thrombin-inhibiting effective amount of a compound according to claim 1 in admixture with a diluent.
Claim 9
Dependent Claim 22 words
A unit dose of a composition according to claim 7 in the form of a tablet, pill, dragee, capsule, ampoule or suppository.
Claim 10
Dependent Claim 40 words
A method of combating cardiac infarctions, angina pectoric, thromboembolic illnesses in the venous and arterial region and arteriosclerosis in human and non-human animals which comprises administering to the animals a thrombin-inhibitory effective amount of a compound according to claim 1.
Claim 11
Dependent Claim 17 words
The method according to claim 9, wherein such compound is ##STR46## or a pharmacologically acceptable salt thereof.

References Cited (Backward Citations)

US3998874A Cited
DE2921778A1 Cited
EP0032063A2 Cited
US4351950A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-05-19 1989-11-18 1990-05-20 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-05-19 1993-11-18 1994-05-20 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1997-05-19 1997-11-18 1998-05-20 $7700.00 Window Closed / Lapsed

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