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US4826845A Expired / Lapsed US ⏱️ 0.0 years remaining

3(2H)-pyridazinones and pharmaceutical compositions thereof

Assignee: Richter Gedeon Nyrt
•
Filing: 1986-10-29
•
Granted: 1989-05-02
•
Expires: 2006-10-29
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Abstract

Abstract The invention relates to novel 3(2H)-pyridazinone-derivatives of the general formula (I), pharmaceutical compositions containing them and process for their preparation. In the general formula (I) <IMAGE> (I) stands for an ethyl or propyl group substituted by a terminal halogen atom or a hydroxyl or NR1R2 group, wherein R1 represents hydrogen atom or an unsubstituted or optionally substituted benzyl group; R2 represents hydrogen atom or an unsubstituted or optionally substituted benzo[1,4]dioxan-2-yl-methyl or -ethyl group or a (CH2)n-R3 group, wherein n is 2 or 3; and R3 stands for an unsubstituted or optionally substituted phenoxy or phenylthio group; and X stands for a hydrogen or halogen atom or an unsubstituted or optionally substituted, saturated or unsaturated 5- or 6-membered heterocyclic group containing a nitrogen atom and optionally an additional heteroatom, e.g. an oxygen, sulfur or nitrogen atom, with the proviso that R is different from an ethyl or propyl group substituted terminally by a hydroxyl group or halogen atom when X represents a hydrogen or chlorine atom. The compounds of general formula (I) selectively inhibit the adrenergic alpha1 receptors, have a calcium-antagonistic effect and exert blood pressure lowering action.

Inventors

  • 👤 Endre Kasztreiner
  • 👤 Gyorgy Rablocsky
  • 👤 Nandor Makk
  • 👤 Laszlo Jaszlits
  • 👤 Peter Matyus
  • 👤 Gyorgy Cseh
  • 👤 Ildiko Pribusz nee Rapp
  • 👤 Klara Czako
  • 👤 Eszter Diesler
  • 👤 Istvan Elekes
  • 👤 Laszlo Kaufer
  • 👤 Maria Kuhar nee Kurthy
  • 👤 Judit Kincsessy
  • 👤 Judit Kosary
  • 👤 Gyongyi Nagy nee Csokas

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 23:44
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; A; A61; A61P; A61P9/00; A61P9/12; C07D233/00; C07D233/54; C07D233/56; C07D237/00; C07D237/02; C07D237/06; C07D237/08; C07D237/10; C07D237/12; C07D237/20; C07D249/00; C07D249/02; C07D249/08; C07D403/00; C07D403/02; C07D403/04; C07D405/00; C07D405/02; C07D405/12

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 98 words
A 3(2H)-pyridazinone of the formula (I) ##STR7## wherein R stands for an ethyl or propyl group substituted by a terminal NR 1 R 2 group, wherein R 1 represents a hydrogen atom or a benzyl group, R 2 represents a benzo[1,4]dioxan-2-yl-methyl or -ethyl group or a (CH 2 ) n --R 3 group, wherein n is 2 or 3, and R 3 stands for an unsubstituted or a 2-halogen substituted phenoxy group or a phenythio group, and X stands for a hydrogen or a halogen atom, as well as the pharmaceutically acceptable acid addition salts of these compounds.
Claim 2
Dependent Claim 98 words
A 3(2H)-pyridazinone of the formula (I) ##STR7## wherein R stands for an ethyl or propyl group substituted by a terminal NR 1 R 2 group, wherein R 1 represents a hydrogen atom or a benzyl group, R 2 represents a benzo[1,4]dioxan-2-yl-methyl or -ethyl group or a (CH 2 ) n --R 3 group, wherein n is 2 or 3, and R 3 stands for an unsubstituted or a 2-halogen substituted phenoxy group or a phenythio group, and X stands for a hydrogen or a halogen atom, as well as the pharmaceutically acceptable acid addition salts of these compounds.
Claim 3
Dependent Claim 20 words
A compound selected from the group consisting of 2-[3-(benzo[1,4]dioxan-2-yl-methylamino)-1-propyl]-6-chloro-3-(2H)-pyridazinone, 2-[3-(2-phenoxyethylamino)-1-propyl]-6-chloro-3(2H)-pyradazinone, 2-[3-(2-phenoxyethylamino)-1-propyl]-3(2H)-pyridazinone, 2-{3-[2-(2-chlorophenoxy)-ethylamino]-1-propyl}-6-chloro-3(2H)-pyridazinone 2-[3-(benzo[1,4]dioxan-2-yl-methylamino)-1-propyl]-3(2H)-pyridazinone, 2-{3-[2-(2-fluorophenoxy)-ethylamino]-1-propyl}-3(2H)-pyridazinone and the hydrochloride of these compounds.
Claim 4
Dependent Claim 20 words
A compound selected from the group consisting of 2-[3-(benzo[1,4]dioxan-2-yl-methylamino)-1-propyl]-6-chloro-3-(2H)-pyridazinone, 2-[3-(2-phenoxyethylamino)-1-propyl]-6-chloro-3(2H)-pyradazinone, 2-[3-(2-phenoxyethylamino)-1-propyl]-3(2H)-pyridazinone, 2-{3-[2-(2-chlorophenoxy)-ethylamino]-1-propyl}-6-chloro-3(2H)-pyridazinone 2-[3-(benzo[1,4]dioxan-2-yl-methylamino)-1-propyl]-3(2H)-pyridazinone, 2-{3-[2-(2-fluorophenoxy)-ethylamino]-1-propyl}-3(2H)-pyridazinone and the hydrochloride of these compounds.
Claim 5
Dependent Claim 22 words
A method of treating hypertension comprising administering to a patient a therapuetically effective amount of a 3(2H)-pyridazinone as defined in claim 1.
Claim 6
Dependent Claim 39 words
A pharmaceutical composition for treating hypertension in a patient suffering therefrom which comprises: an effective amount of a compound of the formula I as defined in claim 1 as the active agent and a pharmaceutically acceptable carrier and/or additive.
Claim 7
Dependent Claim 22 words
A method of treating hypertension comprising administering to a patient a therapeutically effective amount of a 3(2H)-pyridazinone as defined in claim 2.
Claim 8
Dependent Claim 39 words
A pharmaceutical composition for treating hypertension in a patient suffering therefrom which comprises: an effective amount of a compound of the formula I as defined in claim 2 as the active agent and a pharmaceutically acceptable carrier and/or additive.
Claim 9
Dependent Claim 15 words
The 3(2H)-pyridazinone of the formula I as defined in claim 1 which is 2-[3-(benzo[1,4]dioxan-2-yl-methylamino)-1-propyl]-3(2H)-pyridazinone hydrochloride.
Claim 10
Independent Claim 17 words
A method of treating hypertension comprising administering to a patient a therapeutically effective amount of 2-[3-(benzo[1,4]dioxan-2-yl-methylamino)-1-propyl-3-(2H)-pyridazinone hydrochloride.
Claim 11
Independent Claim 17 words
A method of treating hypertension comprising administering to a patient a therapeutically effective amount of 2-[3-(benzo[1,4]dioxan-2-yl-methylamino)-1-propyl-3-(2H)-pyridazinone hydrochloride.
Claim 12
Dependent Claim 13 words
The 3(2H)-pyridazinone of claim 1 wherein R 3 is an unsubstituted phenoxy group.

References Cited (Backward Citations)

US3658814A Cited
US4298609A Cited
US4304777A Cited
JPS5742676A Cited
JPS58146571A Cited
US4636504A Cited
US4521416A Cited
US4666902A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-05-01 1992-10-31 1993-05-02 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-05-01 1996-10-31 1997-05-02 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-05-01 2000-10-31 2001-05-02 $7700.00 Window Closed / Lapsed

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